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Thursday, 26 July 2012

Propranolol

Dosage Form: capsule, extended release
Propranolol hydrochloride extended-release capsules

DESCRIPTION

Propranolol hydrochloride is a synthetic beta-adrenergic receptor-blocking agent chemically described as 2-Propanol, 1-[(1-methylethyl)amino]-3-(1-naphthalenyloxy)-, hydrochloride,(±)-. Its molecular and structural formulae are:

C16H21NO2 · HCl

Propranolol hydrochloride is a stable, white, crystalline solid which is readily soluble in water and ethanol. Its molecular weight is 295.80.

Propranolol hydrochloride extended-release capsules are formulated to provide a sustained release of Propranolol hydrochloride. Propranolol hydrochloride extended-release capsules are available as 60 mg, 80 mg, 120 mg, and 160 mg capsules for oral administration.

The inactive ingredients contained in Propranolol hydrochloride extended-release capsules are: cellulose, ethylcellulose, gelatin capsules, hypromellose, and titanium dioxide. In addition, Propranolol hydrochloride extended-release 80 mg, and 160 mg capsules contain D&C Red No. 28 and FD&C Blue No. 1. Propranolol hydrochloride extended-release 120 mg capsules contain FD&C Blue No. 1.

These capsules comply with USP Dissolution Test 1.

CLINICAL PHARMACOLOGY

General

Propranolol is a nonselective, beta-adrenergic receptor-blocking agent possessing no other autonomic nervous system activity. It specifically competes with beta-adrenergic receptor-stimulating agents for available receptor sites. When access to beta-receptor sites is blocked by Propranolol, the chronotropic, inotropic, and vasodilator responses to beta-adrenergic stimulation are decreased proportionately. At dosages greater than required for beta blockade, Propranolol also exerts a quinidine-like or anesthetic-like membrane action, which affects the cardiac action potential. The significance of the membrane action in the treatment of arrhythmias is uncertain.

Propranolol hydrochloride extended-release capsules should not be considered a simple mg-for-mg substitute for conventional Propranolol and the blood levels achieved do not match (are lower than) those of two to four times daily dosing with the same dose (see DOSAGE AND ADMINISTRATION). When changing to Propranolol hydrochloride extended-release capsules from conventional Propranolol, a possible need for retitration upwards should be considered, especially to maintain effectiveness at the end of the dosing interval. In most clinical settings, however, such as hypertension or angina where there is little correlation between plasma levels and clinical effect, Propranolol hydrochloride extended-release capsules have been therapeutically equivalent to the same mg dose of conventional Propranolol hydrochloride as assessed by 24-hour effects on blood pressure and on 24-hour exercise responses of heart rate, systolic pressure, and rate pressure product.

Mechanism of Action

The mechanism of the antihypertensive effect of Propranolol has not been established. Among the factors that may be involved in contributing to the antihypertensive action include: (1) decreased cardiac output, (2) inhibition of renin release by the kidneys, and (3) diminution of tonic sympathetic nerve outflow from vasomotor centers in the brain. Although total peripheral resistance may increase initially, it readjusts to or below the pretreatment level with chronic use of Propranolol. Effects of Propranolol on plasma volume appear to be minor and somewhat variable.

In angina pectoris, Propranolol generally reduces the oxygen requirement of the heart at any given level of effort by blocking the catecholamine-induced increases in the heart rate, systolic blood pressure, and the velocity and extent of myocardial contraction. Propranolol may increase oxygen requirements by increasing left ventricular fiber length, end diastolic pressure, and systolic ejection period. The net physiologic effect of beta-adrenergic blockade is usually advantageous and is manifested during exercise by delayed onset of pain and increased work capacity.

Propranolol exerts its antiarrhythmic effects in concentrations associated with beta-adrenergic blockade, and this appears to be its principal antiarrhythmic mechanism of action. In dosages greater than required for beta blockade, Propranolol also exerts a quinidine-like or anesthetic-like membrane action which affects the cardiac action potential. The significance of the membrane action in the treatment of arrhythmias is uncertain.

The mechanism of the anti-migraine effect of Propranolol has not been established. Beta-adrenergic receptors have been demonstrated in the pial vessels of the brain.

PHARMACOKINETICS AND DRUG METABOLISM

Absorption

Propranolol is highly lipophilic and almost completely absorbed after oral administration. However, it undergoes high first pass metabolism by the liver and on average, only about 25% of Propranolol reaches the systemic circulation. Propranolol hydrochloride extended-release capsules (60, 80, 120, and 160 mg) release Propranolol HCl at a controlled and predictable rate. Peak blood levels following dosing with Propranolol hydrochloride extended-release capsules occur at about 6 hours.

The effect of food on Propranolol hydrochloride extended-release capsules bioavailability has not been investigated.

Distribution

Approximately 90% of circulating Propranolol is bound to plasma proteins (albumin and alpha-1-acid glycoprotein). The binding is enantiomer-selective. The S(-)-enantiomer is preferentially bound to alpha-1-glycoprotein and the R(+)-enantiomer is preferentially bound to albumin. The volume of distribution of Propranolol is approximately 4 liters/kg.

Propranolol crosses the blood-brain barrier and the placenta, and is distributed into breast milk.

Metabolism and Elimination

Propranolol is extensively metabolized with most metabolites appearing in the urine. Propranolol is metabolized through three primary routes: aromatic hydroxylation (mainly 4-hydroxylation), N-dealkylation followed by further side-chain oxidation, and direct glucuronidation. It has been estimated that the percentage contributions of these routes to total metabolism are 42%, 41% and 17%, respectively, but with considerable variability between individuals. The four major metabolites are Propranolol glucuronide, naphthyloxylactic acid and glucuronic acid, and sulfate conjugates of 4-hydroxy Propranolol.

In-vitro studies have indicated that the aromatic hydroxylation of Propranolol is catalyzed mainly by polymorphic CYP2D6. Side-chain oxidation is mediated mainly by CYP1A2 and to some extent by CYP2D6. 4-hydroxy Propranolol is a weak inhibitor of CYP2D6.

Propranolol is also a substrate of CYP2C19 and a substrate for the intestinal efflux transporter, p-glycoprotein (p-gp). Studies suggest however that p-gp is not dose-limiting for intestinal absorption of Propranolol in the usual therapeutic dose range.

In healthy subjects, no difference was observed between CYP2D6 extensive metabolizers (EMs) and poor metabolizers (PMs) with respect to oral clearance or elimination half-life. Partial clearance of 4-hydroxy Propranolol was significantly higher and naphthyloxyactic acid was significantly lower in EMs than PMs.

When measured at steady state over a 24-hour period the areas under the Propranolol plasma concentration-time curve (AUCs) for the Propranolol hydrochloride extended-release capsules are approximately 60% to 65% of the AUCs for a comparable divided daily dose of Propranolol hydrochloride extended-release capsules. The lower AUCs for the Propranolol hydrochloride extended-release capsules are due to greater hepatic metabolism of Propranolol, resulting from the slower rate of absorption of Propranolol. Over a twenty-four (24) hour period, blood levels are fairly constant for about twelve (12) hours, then decline exponentially. The apparent plasma half-life is about 10 hours.

Enantiomers

Propranolol is a racemic mixture of two enantiomers, R(+) and S(-). The S(-)-enantiomer is approximately 100 times as potent as the R(+)-enantiomer in blocking beta adrenergic receptors. In normal subjects receiving oral doses of racemic Propranolol, S(-)-enantiomer concentrations exceeded those of the R(+)-enantiomer by 40-90% as a result of stereoselective hepatic metabolism. Clearance of the pharmacologically active S(-)-Propranolol is lower than R(+)-Propranolol after intravenous and oral doses.

Special Population

Geriatric

The pharmacokinetics of Propranolol hydrochloride extended-release capsules have not been investigated in patients over 65 years of age.

In a study of 12 elderly (62-79 years old) and 12 young (25-33 years old) healthy subjects, the clearance of S-enantiomer of Propranolol was decreased in the elderly. Additionally, the half-life of both the R- and S-Propranolol were prolonged in the elderly compared with the young (11 hours vs. 5 hours).

Clearance of Propranolol is reduced with aging due to decline in oxidation capacity (ring oxidation and side chain oxidation). Conjugation capacity remains unchanged. In a study of 32 patients age 30 to 84 years given a single 20-mg dose of Propranolol, an inverse correlation was found between age and the partial metabolic clearances to 4-hydroxyPropranolol (40HP ring oxidation) and to naphthoxylactic acid (NLA-side chain oxidation). No correlation was found between age and the partial metabolic clearance to Propranolol glucuronide (PPLG conjugation).

Gender

In a study of 9 healthy women and 12 healthy men, neither the administration of testosterone nor the regular course of the menstrual cycle affected the plasma binding of the Propranolol enantiomers. In contrast, there was a significant, although non-enantioselective diminution of the binding of Propranolol after treatment with ethinyl estradiol. These findings are inconsistent with another study, in which administration of testosterone cypionate confirmed the stimulatory role of this hormone on Propranolol metabolism and concluded that the clearance of Propranolol in men is dependent on circulating concentrations of testosterone. In women, none of the metabolic clearances for Propranolol showed any significant association with either estradiol or testosterone.

Race

A study conducted in 12 Caucasian and 13 African-American male subjects taking Propranolol, showed that at steady state, the clearance of R(+)- and S(-)-Propranolol were about 76% and 53% higher in African-Americans than in Caucasians, respectively.

Chinese subjects had a greater proportion (18% to 45% higher) of unbound Propranolol in plasma compared to Caucasians, which was associated with a lower plasma concentration of alpha-1-acid glycoprotein.

Renal Insufficiency

The pharmacokinetics of Propranolol hydrochloride extended-release capsules have not been investigated in patients with renal insufficiency.

In a study conducted in 5 patients with chronic renal failure, 6 patients on regular dialysis, and 5 healthy subjects, who received a single oral dose of 40 mg of Propranolol, the peak plasma concentrations (Cmax) of Propranolol in the chronic renal failure group were 2 to 3-fold higher (161±41 ng/mL) than those observed in the dialysis patients (47±9 ng/mL) and in the healthy subjects (26±1 ng/mL). Propranolol plasma clearance was also reduced in the patients with chronic renal failure.

Studies have reported a delayed absorption rate and a reduced half-life of Propranolol in patients with renal failure of varying severity. Despite this shorter plasma half-life, Propranolol peak plasma levels were 3-4 times higher and total plasma levels of metabolites were up to 3 times higher in these patients than in subjects with normal renal function.

Chronic renal failure has been associated with a decrease in drug metabolism via down regulation of hepatic cytochrome P450 activity resulting in a lower "first-pass" clearance.

Propranolol is not significantly dialyzable.

Hepatic Insufficiency

The pharmacokinetics of Propranolol hydrochloride extended-release capsules have not been investigated in patients with hepatic insufficiency.

Propranolol is extensively metabolized by the liver. In a study conducted in 6 patients with cirrhosis and 7 healthy subjects receiving a 160 mg of extended-release preparation of Propranolol once a day for 7 days, the steady-state Propranolol concentration in patients with cirrhosis was increased 2.5-fold in comparison to controls. In the patients with cirrhosis, the half-life obtained after a single intravenous dose of 10 mg Propranolol increased to 7.2 hours compared to 2.9 hours in control (see PRECAUTIONS).

Drug Interactions

All drug interaction studies were conducted with Propranolol. There are no data on drug interactions with Propranolol hydrochloride extended-release capsules.

Interactions with Substrates, Inhibitors or Inducers of Cytochrome P-450 Enzymes

Because Propranolol's metabolism involves multiple pathways in the Cytochrome P-450 system (CYP2D6, 1A2, 2C19), co-administration with drugs that are metabolized by, or affect the activity (induction or inhibition) of one or more of these pathways may lead to clinically relevant drug interactions (see Drug Interactions under PRECAUTIONS).

Substrates or Inhibitors of CYP2D6

Blood levels and/or toxicity of Propranolol may be increased by co-administration with substrates or inhibitors of CYP2D6, such as amiodarone, cimetidine, delavudin, fluoxetine, paroxetine, quinidine, and ritonavir. No interactions were observed with either ranitidine or lansoprazole.

Substrates or Inhibitors of CYP1A2

Blood levels and/or toxicity of Propranolol may be increased by co-administration with substrates or inhibitors of CYP1A2, such as imipramine, cimetidine, ciprofloxacin, fluvoxamine, isoniazid, ritonavir, theophylline, zileuton, zolmitriptan, and rizatriptan.

Substrates or Inhibitors of CYP2C19

Blood levels and/or toxicity of Propranolol may be increased by co-administration with substrates or inhibitors of CYP2C19, such as fluconazole, cimetidine, fluoxetine, fluvoxamine, tenioposide, and tolbutamide. No interaction was observed with omeprazole.

Inducers of Hepatic Drug Metabolism

Blood levels of Propranolol may be decreased by co-administration with inducers such as rifampin, ethanol, phenytoin, and phenobarbital. Cigarette smoking also induces hepatic metabolism and has been shown to increase up to 77% the clearance of Propranolol, resulting in decreased plasma concentrations.

Cardiovascular Drugs

Antiarrhythmics

The AUC of propafenone is increased by more than 200% by co-administration of Propranolol.

The metabolism of Propranolol is reduced by co-administration of quinidine, leading to a two to three fold increased blood concentration and greater degrees of clinical beta-blockade.

The metabolism of lidocaine is inhibited by co-administration of Propranolol, resulting in a 25% increase in lidocaine concentrations.

Calcium Channel Blockers

The mean Cmax and AUC of Propranolol are increased respectively, by 50% and 30% by co-administration of nisoldipine and by 80% and 47%, by co-administration of nicardipine.

The mean Cmax and AUC of nifedipine are increased by 64% and 79%, respectively, by co-administration of Propranolol.

Propranolol does not affect the pharmacokinetics of verapamil and norverapamil. Verapamil does not affect the pharmacokinetics of Propranolol.

Non-Cardiovascular Drugs

Migraine Drugs

Administration of zolmitriptan or rizatriptan with Propranolol resulted in increased concentrations of zolmitriptan (AUC increased by 56% and Cmax by 37%) or rizatriptan (the AUC and Cmax were increased by 67% and 75%, respectively).

Theophylline

Co-administration of theophylline with Propranolol decreases theophylline oral clearance by 30% to 52%.

Benzodiazepines

Propranolol can inhibit the metabolism of diazepam, resulting in increased concentrations of diazepam and its metabolites. Diazepam does not alter the pharmacokinetics of Propranolol.

The pharmacokinetics of oxazepam, triazolam, lorazepam, and alprazolam are not affected by co-administration of Propranolol.

Neuroleptic Drugs

Co-administration of extended-release Propranolol at doses greater than or equal to 160 mg/day resulted in increased thioridazine plasma concentrations ranging from 55% to 369% and increased thioridazine metabolite (mesoridazine) concentrations ranging from 33% to 209%.

Co-administration of chlorpromazine with Propranolol resulted in a 70% increase in Propranolol plasma level.

Anti-Ulcer Drugs

Co-administration of Propranolol with cimetidine, a non-specific CYP450 inhibitor, increased Propranolol AUC and Cmax by 46% and 35%, respectively. Co-administration with aluminum hydroxide gel (1200 mg) may result in a decrease in Propranolol concentrations.

Co-administration of metoclopramide with the extended-release Propranolol did not have a significant effect on Propranolol's pharmacokinetics.

Lipid Lowering Drugs

Co-administration of cholestyramine or colestipol with Propranolol resulted in up to 50% decrease in Propranolol concentrations.

Co-administration of Propranolol with lovastatin or pravastatin, decreased 18% to 23% the AUC of both, but did not alter their pharmacodynamics. Propranolol did not have an effect on the pharmacokinetics of fluvastatin.

Warfarin

Concomitant administration of Propranolol and warfarin has been shown to increase warfarin bioavailability and increase prothrombin time.

PHARMACODYNAMICS AND CLINICAL EFFECTS

Hypertension

In a retrospective, uncontrolled study, 107 patients with diastolic blood pressure 110 to 150 mmHg received Propranolol 120 mg t.i.d. for at least 6 months, in addition to diuretics and potassium, but with no other hypertensive agent. Propranolol contributed to control of diastolic blood pressure, but the magnitude of the effect of Propranolol on blood pressure cannot be ascertained.

Four double-blind, randomized, crossover studies were conducted in a total of 74 patients with mild or moderately severe hypertension treated with Propranolol hydrochloride extended-release capsules 160 mg once daily or Propranolol 160 mg given either once daily or in two 80 mg doses. Three of these studies were conducted over a 4-week treatment period. One study was assessed after a 24-hour period. Propranolol hydrochloride extended-release capsules were as effective as Propranolol in controlling hypertension (pulse rate, systolic and diastolic blood pressure) in each of these trials.

Angina Pectoris

In a double-blind, placebo-controlled study of 32 patients of both sexes, aged 32 to 69 years, with stable angina, Propranolol 100 mg t.i.d. was administered for 4 weeks and shown to be more effective than placebo in reducing the rate of angina episodes and in prolonging total exercise time.

Twelve male patients with moderately severe angina pectoris were studied in a double-blind, crossover study. Patients were randomized to either Propranolol hydrochloride extended-release capsules 160 mg daily or conventional Propranolol 40 mg four times a day for 2 weeks. Nitroglycerine tablets were allowed during the study. Blood pressure, heart rate and ECG's were recorded during serial exercise treadmill testing. Propranolol hydrochloride extended-release capsules were as effective as conventional Propranolol for exercise heart rate, systolic and diastolic blood pressure, duration of anginal pain and ST-segment depression before or after exercise, exercise duration, angina attack rate and nitroglycerine consumption.

In another double-blind, randomized, crossover trial, the effectiveness of Propranolol hydrochloride extended-release capsules 160 mg daily and conventional Propranolol 40 mg four times a day was evaluated in 13 patients with angina. ECG's were recorded while patients exercised until angina developed. Propranolol hydrochloride extended-release capsules were as effective as conventional Propranolol for amount of exercise performed, ST-segment depression, number of anginal attacks, amount of nitroglycerine consumed, systolic and diastolic blood pressures and heart rate at rest and after exercise.

Migraine

In a 34-week, placebo-controlled, 4-period, dose-finding crossover study with a double-blind randomized treatment sequence, 62 patients with migraine received Propranolol 20 to 80 mg 3 or 4 times daily. The headache unit index, a composite of the number of days with headache and the associated severity of the headache, was significantly reduced for patients receiving Propranolol as compared to those on placebo.

Hypertrophic Subaortic Stenosis

In an uncontrolled series of 13 patients with New York Heart Association (NYHA) class 2 or 3 symptoms and hypertrophic subaortic stenosis diagnosed at cardiac catheterization, oral Propranolol 40-80 mg t.i.d. was administered and patients were followed for up to 17 months. Propranolol was associated with improved NYHA class for most patients.

INDICATIONS AND USAGE

Hypertension

Propranolol hydrochloride extended-release capsules are indicated in the management of hypertension. They may be used alone or used in combination with other antihypertensive agents, particularly a thiazide diuretic. Propranolol hydrochloride extended-release capsules are not indicated in the management of hypertensive emergencies.

Angina Pectoris Due to Coronary Atherosclerosis

Propranolol hydrochloride extended-release capsules are indicated to decrease angina frequency and increase exercise tolerance in patients with angina pectoris.

Migraine

Propranolol hydrochloride extended-release capsules are indicated for the prophylaxis of common migraine headache. The efficacy of Propranolol in the treatment of a migraine attack that has started has not been established, and Propranolol is not indicated for such use.

Hypertrophic Subaortic Stenosis

Propranolol hydrochloride extended-release capsules improve NYHA functional class in symptomatic patients with hypertrophic subaortic stenosis.

CONTRAINDICATIONS

Propranolol is contraindicated in 1) cardiogenic shock; 2) sinus bradycardia and greater than first-degree block; 3) bronchial asthma; and 4) in patients with known hypersensitivity to Propranolol hydrochloride.

WARNINGS

Angina Pectoris

There have been reports of exacerbation of angina and, in some cases, myocardial infarction, following abrupt discontinuance of Propranolol therapy. Therefore, when discontinuance of Propranolol is planned, the dosage should be gradually reduced over at least a few weeks, and the patient should be cautioned against interruption or cessation of therapy without the physician's advice. If Propranolol therapy is interrupted and exacerbation of angina occurs, it usually is advisable to reinstitute Propranolol therapy and take other measures appropriate for the management of unstable angina pectoris. Since coronary artery disease may be unrecognized, it may be prudent to follow the above advice in patients considered at risk of having occult atherosclerotic heart disease who are given Propranolol for other indications.

Hypersensitivity and Skin Reactions

Hypersensitivity reactions, including anaphylactic/anaphylactoid reactions, have been associated with the administration of Propranolol (see ADVERSE REACTIONS).

Cutaneous reactions, including Stevens-Johnson Syndrome, toxic epidermal necrolysis, exfoliative dermatitis, erythema multiforme, and urticaria, have been reported with use of Propranolol (see ADVERSE REACTIONS).

Cardiac Failure

Sympathetic stimulation may be a vital component supporting circulatory function in patients with congestive heart failure, and its inhibition by beta- blockade may precipitate more severe failure. Although beta- blockers should be avoided in overt congestive heart failure, some have been shown to be highly beneficial when used with close follow-up in patients with a history of failure who are well compensated and are receiving diuretics as needed. Beta-adrenergic blocking agents do not abolish the inotropic action of digitalis on heart muscle.

In Patients without a History of Heart Failure, continued use of beta-blockers can, in some cases, lead to cardiac failure.

Nonallergic Bronchospasm (e.g., Chronic Bronchitis, Emphysema)

In general, patients with bronchospastic lung disease should not receive beta-blockers. Propranolol should be administered with caution in this setting since it may provoke a bronchial asthmatic attack by blocking bronchodilation produced by endogenous and exogenous catecholamine stimulation of beta-receptors.

Major Surgery

Chronically administered beta-blocking therapy should not be routinely withdrawn prior to major surgery, however the impaired ability of the heart to respond to reflex adrenergic stimuli may augment the risks of general anesthesia and surgical procedures.

Diabetes and Hypoglycemia

Beta-adrenergic blockade may prevent the appearance of certain premonitory signs and symptoms (pulse rate and pressure changes) of acute hypoglycemia, especially in labile insulin-dependent diabetics. In these patients, it may be more difficult to adjust the dosage of insulin.

Propranolol therapy, particularly when given to infants and children, diabetic or not, has been associated with hypoglycemia especially during fasting as in preparation for surgery. Hypoglycemia has been reported in patients taking Propranolol after prolonged physical exertion and in patients with renal insufficiency.

Thyrotoxicosis

Beta-adrenergic blockade may mask certain clinical signs of hyperthyroidism. Therefore, abrupt withdrawal of Propranolol may be followed by an exacerbation of symptoms of hyperthyroidism, including thyroid storm. Propranolol may change thyroid-function tests, increasing T4 and reverse T3, and decreasing T3.

Wolff-Parkinson-White Syndrome

Beta-adrenergic blockade in patients with Wolff-Parkinson-White syndrome and tachycardia has been associated with severe bradycardia requiring treatment with a pacemaker. In one case, this result was reported after an initial dose of 5 mg Propranolol.

PRECAUTIONS

General

Propranolol should be used with caution in patients with impaired hepatic or renal function. Propranolol hydrochloride extended-release capsules are not indicated for the treatment of hypertensive emergencies.

Beta-adrenergic receptor blockade can cause reduction of intraocular pressure. Patients should be told that Propranolol hydrochloride extended-release capsules may interfere with the glaucoma screening test. Withdrawal may lead to a return of increased intraocular pressure.

While taking beta-blockers, patients with a history of severe anaphylactic reaction to a variety of allergens may be more reactive to repeated challenge, either accidental, diagnostic, or therapeutic. Such patients may be unresponsive to the usual doses of epinephrine used to treat allergic reaction.

Clinical Laboratory Tests

In patients with hypertension, use of Propranolol has been associated with elevated levels of serum potassium, serum transaminases, and alkaline phosphatase. In severe heart failure, the use of Propranolol has been associated with increases in Blood Urea Nitrogen.

Drug Interactions

Caution should be exercised when Propranolol hydrochloride extended-release capsules are administered with drugs that have an affect on CYP2D6, 1A2, or 2C19 metabolic pathways. Co-administration of such drugs with Propranolol may lead to clinically relevant drug interactions and changes on its efficacy and/or toxicity (see Drug Interactions in PHARMACOKINETICS AND DRUG METABOLISM).

Alcohol when used concomitantly with Propranolol, may increase plasma levels of Propranolol.

Cardiovascular Drugs

Antiarrhythmics

Propafenone has negative inotropic and beta-blocking properties that can be additive to those of Propranolol.

Quinidine increases the concentration of Propranolol and produces greater degrees of clinical beta-blockade and may cause postural hypotension.

Amiodarone is an antiarrhythmic agent with negative chronotropic properties that may be additive to those seen with β-blockers such as Propranolol.

The clearance of lidocaine is reduced with administration of Propranolol. Lidocaine toxicity has been reported following co-administration with Propranolol.

Caution should be exercised when administering Propranolol hydrochloride extended-release capsules with drugs that slow A-V nodal conduction, e.g., lidocaine and calcium channel blockers.

Digitalis Glycosides

Both digitalis glycosides and beta-blockers slow atrioventricular conduction and decrease heart rate. Concomitant use can increase the risk of bradycardia.

Calcium Channel Blockers

Caution should be exercised when patients receiving a beta-blocker are administered a calcium-channel-blocking drug with negative inotropic and/or chronotropic effects. Both agents may depress myocardial contractility or atrioventricular conduction.

There have been reports of significant bradycardia, heart failure, and cardiovascular collapse with concurrent use of verapamil and beta-blockers.

Co-administration of Propranolol and diltiazem in patients with cardiac disease has been associated with bradycardia, hypotension, high degree heart block, and heart failure.

ACE Inhibitors

When combined with beta-blockers, ACE inhibitors can cause hypotension, particularly in the setting of acute myocardial infarction.

The antihypertensive effects of clonidine may be antagonized by beta-blockers. Propranolol hydrochloride extended-release capsules should be administered cautiously to patients withdrawing from clonidine.

Alpha Blockers

Prazosin has been associated with prolongation of first dose hypotension in the presence of beta-blockers.

Postural hypotension has been reported in patients taking both beta-blockers and terazosin or doxazosin.

Reserpine

Patients receiving catecholamine-depleting drugs, such as reserpine should be closely observed for excessive reduction of resting sympathetic nervous activity, which may result in hypotension, marked bradycardia, vertigo, syncopal attacks, or orthostatic hypotension.

Inotropic Agents

Patients on long-term therapy with Propranolol may experience uncontrolled hypertension if administered epinephrine as a consequence of unopposed alpha-receptor stimulation. Epinephrine is therefore not indicated in the treatment of Propranolol overdose (see OVERDOSAGE).

Isoproterenol and Dobutamine

Propranolol is a competitive inhibitor of beta-receptor agonists, and its effects can be reversed by administration of such agents, e.g., dobutamine or isoproterenol. Also, Propranolol may reduce sensitivity to dobutamine stress echocardiography in patients undergoing evaluation for myocardial ischemia.

Non-Cardiovascular Drugs

Nonsteroidal Anti-Inflammatory Drugs

Nonsteroidal anti-inflammatory drugs (NSAIDs) have been reported to blunt the antihypertensive effect of beta-adrenoreceptor blocking agents.

Administration of indomethacin with Propranolol may reduce the efficacy of Propranolol in reducing blood pressure and heart rate.

Antidepressants

The hypotensive effects of MAO inhibitors or tricyclic antidepressants may be exacerbated when administered with beta-blockers by interfering with the beta- blocking activity of Propranolol.

Anesthetic Agents

Methoxyflurane and trichloroethylene may depress myocardial contractility when administered with Propranolol.

Warfarin

Propranolol when administered with warfarin increases the concentration of warfarin. Prothrombin time, therefore, should be monitored.

Neuroleptic Drugs

Hypotension and cardiac arrest have been reported with the concomitant use of Propranolol and haloperidol.

Thyroxine

Thyroxine may result in a lower than expected T3 concentration when used concomitantly with Propranolol.

Carcinogenesis, Mutagenesis, Impairment of Fertility

In dietary administration studies in which mice and rats were treated with Propranolol hydrochloride for up to 18 months at doses of up to 150 mg/kg/day, there was no evidence of drug-related tumorigenesis. On a body surface area basis, this dose in the mouse and rat is, respectively, about equal to and about twice the maximum recommended human oral daily dose (MRHD) of 640 mg Propranolol hydrochloride. In a study in which both male and female rats were exposed to Propranolol hydrochloride in their diets at concentrations of up to 0.05% (about 50 mg/kg body weight and less than the MRHD), from 60 days prior to mating and throughout pregnancy and lactation for two generations, there were no effects on fertility. Based on differing results from Ames Tests performed by different laboratories, there is equivocal evidence for a genotoxic effect of Propranolol in bacteria (S. typhimurium strain TA 1538).

Pregnancy: Pregnancy Category C

In a series of reproductive and developmental toxicology studies, Propranolol was given to rats by gavage or in the diet throughout pregnancy and lactation. At doses of 150 mg/kg/day, but not at doses of 80 mg/kg/day (equivalent to the MRHD on a body surface area basis), treatment was associated with embryotoxicity (reduced litter size and increased resorption rates) as well as neonatal toxicity (deaths). Propranolol hydrochloride also was administered (in the feed) to rabbits (throughout pregnancy and lactation) at doses as high as 150 mg/kg/day (about 5 times the maximum recommended human oral daily dose). No evidence of embryo or neonatal toxicity was noted.

There are no adequate and well-controlled studies in pregnant women. Intrauterine growth retardation, small placentas, and congenital abnormalities have been reported in neonates whose mothers received Propranolol during pregnancy. Neonates whose mothers are receiving Propranolol at parturition have exhibited bradycardia, hypoglycemia and/or respiratory depression. Adequate facilities for monitoring such infants at birth should be available. Propranolol hydrochloride extended-release capsules should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.

Nursing Mothers

Propranolol is excreted in human milk. Caution should be exercised when Propranolol hydrochloride extended-release capsules are administered to a nursing woman.

Pediatric Use

Safety and effectiveness of Propranolol in pediatric patients have not been established.

Bronchospasm and congestive heart failure have been reported coincident with the administration of Propranolol therapy in pediatric patients.

Geriatric Use

Clinical studies of Propranolol hydrochloride extended-release capsules did not include sufficient numbers of subjects aged 65 and over to determine whether they respond differently from younger subjects. Other reported clinical experience has not identified differences in responses between the elderly and younger patients. In general, dose selection for an elderly patient should be cautious, usually starting at the low end of the dosing range, reflecting the greater frequency of the decreased hepatic, renal or cardiac function, and of concomitant disease or other drug therapy.

ADVERSE REACTIONS

The following adverse events were observed and have been reported in patients using Propranolol.

Cardiovascular: Bradycardia; congestive heart failure; intensification of AV block; hypotension; paresthesia of hands; thrombocytopenic purpura; arterial insufficiency, usually of the Raynaud type.

Central Nervous System: Light-headedness; mental depression manifested by insomnia, lassitude, weakness, fatigue; catatonia; visual disturbances; hallucinations; vivid dreams; an acute reversible syndrome characterized by disorientation for time and place, short-term memory loss, emotional lability, slightly clouded sensorium, and decreased performance on neuropsychometrics. For immediate release formulations, fatigue, lethargy, and vivid dreams appear dose related.

Gastrointestinal: Nausea, vomiting, epigastric distress, abdominal cramping, diarrhea, constipation, mesenteric arterial thrombosis, ischemic colitis.

Allergic: Hypersensitivity reactions, including anaphylactic/anaphylactoid reactions; pharyngitis and agranulocytosis; erythematous rash; fever combined with aching and sore throat; laryngospasm; respiratory distress.

Respiratory: Bronchospasm.

Hematologic: Agranulocytosis, nonthrombocytopenic purpura, and thrombocytopenic purpura.

Autoimmune: Systemic lupus erythematosus (SLE).

Skin and mucous membranes: Stevens-Johnson Syndrome, toxic epidermal necrolysis, dry eyes, exfoliative dermatitis, erythema multiforme, urticaria, alopecia, SLE-like reactions, and psoriasisiform rashes. Oculomucocutaneous syndrome involving the skin, serous membranes, and conjunctivae reported for a beta-blocker (practolol) have not been associated with Propranolol.

Genitourinary: Male impotence; Peyronie's disease.

OVERDOSAGE

Propranolol is not significantly dialyzable. In the event of overdosage or exaggerated response, the following measures should be employed:

General: If ingestion is or may have been recent, evacuate gastric contents, taking care to prevent pulmonary aspiration.

Supportive Therapy: Hypotension and bradycardia have been reported following Propranolol overdose and should be treated appropriately. Glucagon can exert potent inotropic and chronotropic effects and may be particularly useful for the treatment of hypotension or depressed myocardial function after a Propranolol overdose. Glucagon should be administered as 50-150 mcg/kg intravenously followed by continuous drip of 1-5 mg/hour for positive chronotropic effect. Isoproterenol, dopamine or phosphodiesterase inhibitors may also be useful. Epinephrine, however, may provoke uncontrolled hypertension. Bradycardia can be treated with atropine or isoproterenol. Serious bradycardia may require temporary cardiac pacing.

The electrocardiogram, pulse, blood pressure, neurobehavioral status and intake and output balance must be monitored. Isoproterenol and aminophylline may be used for bronchospasm.

DOSAGE AND ADMINISTRATION

General

Propranolol hydrochloride extended-release capsules provide Propranolol hydrochloride in a sustained-release capsule for administration once daily. If patients are switched from Propranolol hydrochloride tablets to Propranolol hydrochloride extended-release capsules, care should be taken to assure that the desired therapeutic effect is maintained. Propranolol hydrochloride extended-release capsules should not be considered a simple mg-for-mg substitute for Propranolol hydrochloride tablets. Propranolol hydrochloride extended-release capsules have different kinetics and produce lower blood levels. Retitration may be necessary, especially to maintain effectiveness at the end of the 24-hour dosing interval.

Hypertension

The usual initial dosage is 80 mg Propranolol hydrochloride extended-release capsules once daily, whether used alone or added to a diuretic. The dosage may be increased to 120 mg once daily or higher until adequate blood pressure control is achieved. The usual maintenance dosage is 120 to 160 mg once daily. In some instances a dosage of 640 mg may be required. The time needed for full hypertensive response to a given dosage is variable and may range from a few days to several weeks.

Angina Pectoris

Starting with 80 mg Propranolol hydrochloride extended-release capsules once daily, dosage should be gradually increased at three- to seven-day intervals until optimal response is obtained. Although individual patients may respond at any dosage level, the average optimal dosage appears to be 160 mg once daily. In angina pectoris, the value and safety of dosage exceeding 320 mg per day have not been established.

If treatment is to be discontinued, reduce dosage gradually over a period of a few weeks (see "WARNINGS").

Migraine

The initial oral dose is 80 mg Propranolol hydrochloride extended-release capsules once daily. The usual effective dose range is 160 to 240 mg once daily. The dosage may be increased gradually to achieve optimal migraine prophylaxis. If a satisfactory response is not obtained within four to six weeks after reaching the maximal dose, Propranolol hydrochloride extended-release capsules therapy should be discontinued. It may be advisable to withdraw the drug gradually over a period of several weeks depending on the patient's age, comorbidity, and dose of Propranolol hydrochloride extended-release capsules.

Hypertrophic Subaortic Stenosis

The usual dosage is 80 to 160 mg Propranolol hydrochloride extended-release capsules once daily.

HOW SUPPLIED

Propranolol hydrochloride extended-release capsules

Each white capsule identified by 3 narrow bands, 1 wide band, and "AK 60," contains 60 mg of Propranolol hydrochloride in bottles of 100 (NDC 43478-900-88).

Each white/light blue capsule identified by 3 narrow bands, 1 wide band, and "AK 80," contains 80 mg of Propranolol hydrochloride in bottles of 100 (NDC 43478-901-88).

Each white/dark blue capsule identified by 3 narrow bands, 1 wide band, and "AK 120," contains 120 mg of Propranolol hydrochloride in bottles of 100 (NDC 43478-902-88).

Each dark blue/light blue capsule identified by 3 narrow bands, 1 wide band, and "AK 160," contains 160 mg of Propranolol hydrochloride in bottles of 100 (NDC 43478-903-88).

Store at 20° to 25°C (68° to 77°F); excursions permitted to 15° to 30°C (59° to 86°F). [See USP Controlled Room Temperature]

Protect from light, moisture, freezing, and excessive heat.

Dispense in a tight, light-resistant container as defined in the USP.

This product's label may have been updated. For current package insert and further product information, please call 1-800-438-1985

Manufactured for Rouses Point Pharmaceuticals, LLC

Cranford, NJ 07016

By Wyeth Pharmaceuticals, Inc., a subsidiary of Pfizer Inc.

Philadelphia, PA 19101

Marketed and Distributed by

Rouses Point Pharmaceuticals, LLC

Cranford, NJ 07016

490F003

11/11

LAB-0554-1.0

Revised November 2011

PRINCIPAL DISPLAY PANEL - 60 mg Capsule

NDC 43478-900-88

Propranolol HYDROCHLORIDE

EXTENDED-RELEASE CAPSULES

60 mg

100 CAPSULES

PRINCIPAL DISPLAY PANEL - 80 mg Capsule

NDC 43478-901-88

Propranolol HYDROCHLORIDE

EXTENDED-RELEASE CAPSULES

80 mg

100 CAPSULES

PRINCIPAL DISPLAY PANEL - 120 mg Capsule

NDC 43478-902-88

Propranolol HYDROCHLORIDE

EXTENDED-RELEASE CAPSULES

120 mg

100 CAPSULES

PRINCIPAL DISPLAY PANEL - 160 mg Capsule

NDC 43478-903-88

Propranolol HYDROCHLORIDE

EXTENDED-RELEASE CAPSULES

160 mg

100 CAPSULES

Propranolol HYDROCHLORIDE ER
Propranolol hydrochloride capsule, extended release

Product Information
Product Type	HUMAN PRESCRIPTION DRUG	NDC Product Code (Source)	43478-900
Route of Administration	ORAL	DEA Schedule

Active Ingredient/Active Moiety
Ingredient Name	Basis of Strength	Strength
Propranolol HYDROCHLORIDE (Propranolol)	Propranolol HYDROCHLORIDE	60 mg

Inactive Ingredients
Ingredient Name	Strength
CELLULOSE, MICROCRYSTALLINE
ETHYLCELLULOSE (100 MPA.S)
GELATIN
HYPROMELLOSE 2910 (6 MPA.S)
TITANIUM DIOXIDE

Product Characteristics
Color	white (white)	Score	no score
Shape	CAPSULE (CAPSULE)	Size	16mm
Flavor		Imprint Code	AK;60
Contains

Packaging

Wednesday, 25 July 2012

Cefaclor

Class: Second Generation Cephalosporins
VA Class: AM116
CAS Number: 53994-73-3

Introduction

Antibacterial; β-lactam antibiotic; second generation cephalosporin.¹⁶⁷ ¹⁶⁸ ¹⁶⁹ ^a

Uses for Cefaclor

Acute Otitis Media (AOM)

Treatment of AOM caused by Streptococcus pneumoniae, Haemophilus influenzae, staphylococci, or S. pyogenes (group A β-hemolytic streptococci).¹⁶⁷ (See Haemophilus influenzae Infections under Cautions.)

Pharyngitis and Tonsillitis

Treatment of pharyngitis and tonsillitis caused by S. pyogenes (group A β-hemolytic streptococci).¹²⁴ ¹³⁵ ¹⁵² ¹⁵³ ¹⁶⁷ ¹⁶⁸ ¹⁶⁹ Generally effective in eradicating S. pyogenes from the nasopharynx, but efficacy in prevention of subsequent rheumatic fever has not been established to date.¹⁶⁷ ¹⁶⁸ ¹⁶⁹

CDC, AAP, IDSA, AHA, and others recommend oral penicillin V or IM penicillin G benzathine as treatments of choice;¹⁰¹ ¹⁰² ¹⁰⁶ ¹⁴⁴ oral cephalosporins and oral macrolides considered alternatives.¹⁰¹ ¹⁰² ¹⁰⁶ ¹⁴⁴ Amoxicillin sometimes used instead of penicillin V, especially for young children.¹⁰¹ ¹⁴⁴

Respiratory Tract Infections

Treatment of lower respiratory tract infections, including pneumonia, caused by susceptible H. influenzae, S. pneumoniae, or S. pyogenes (group A β-hemolytic streptococci).¹⁶⁷ (See Haemophilus influenzae Infections under Cautions.)

Treatment of mild to moderate acute bacterial exacerbations of chronic bronchitis caused by susceptible H. influenzae (β-lactamase negative strains only), Moraxella catarrhalis (including β-lactamase producing strains), or S. pneumoniae.¹⁶⁸ ¹⁶⁹ (See Haemophilus influenzae Infections under Cautions.)

Treatment of secondary bacterial infections of acute bronchitis caused by susceptible H. influenzae (β-lactamase negative strains only) or M. catarrhalis (including β-lactamase producing strains).¹⁶⁸ ¹⁶⁹ (See Haemophilus influenzae Infections under Cautions.)

Skin and Skin Structure Infections

Uncomplicated skin and skin structure infections caused by susceptible Staphylococcus aureus (oxacillin-susceptible strains only)¹³⁶ ¹⁶⁷ ¹⁶⁸ ¹⁶⁹ or S. pyogenes.¹³⁶ ¹⁶⁷

Urinary Tract Infections (UTIs)

Treatment of UTIs (including pyelonephritis and cystitis) caused by susceptible Escherichia coli, Proteus mirabilis, Klebsiella, or coagulase-negative staphylococci.¹⁶⁷

Cefaclor Dosage and Administration

Administration

Oral Administration

Administer orally.¹⁶⁷ ¹⁶⁸ ¹⁶⁹

Conventional capsules or oral suspension: Administer without regard to meals.¹⁶⁷

Extended-release tablets: Administer with meals or within 1 hour of eating.¹⁶⁸ ¹⁶⁹ Should not be cut, crushed, or chewed.¹⁶⁸ ¹⁶⁹

Dosage

Available as cefaclor monohydrate; dosage expressed in terms of anhydrous cefaclor.¹⁶⁷ ¹⁶⁸ ¹⁶⁹

Pediatric Patients

General Pediatric Dosage

Oral

Children ≥1 month of age: AAP recommends 20–40 mg/kg daily in 2 or 3 equally divided doses for treatment of mild or moderate infections.¹⁰¹ AAP states the drug is inappropriate for treatment of severe infections.¹⁰¹

Acute Otitis Media (AOM)

Oral

Children ≥1 month of age: 40 mg/kg daily in divided doses every 8 or 12 hours (as capsules or oral suspension).¹⁶⁷

Pharyngitis and Tonsillitis

Oral

Children ≥1 month of age: 20 mg/kg daily in divided doses every 8 or 12 hours for 10 days (as capsules or oral suspension).¹⁶⁷ For more severe infections or those caused by less-susceptible organisms, 40 mg/kg daily in divided doses every 8 hours (as capsules or oral suspension).¹⁶⁷

Respiratory Tract Infections

Oral

Children ≥1 month of age: 20 mg/kg daily in divided doses every 8 hours (as capsules or oral suspension) for lower respiratory tract infections.¹⁶⁷ For more severe infections or those caused by less-susceptible organisms, 40 mg/kg daily in divided doses every 8 hours (as capsules or oral suspension).¹⁶⁷

Skin and Skin Structure Infections

Oral

Children ≥1 month of age: 20 mg/kg daily in divided doses every 8 hours (as capsules or oral suspension).¹⁶⁷ For more severe infections or those caused by less susceptible organisms, 40 mg/kg daily in divided doses every 8 hours (as capsules or oral suspension).¹⁶⁷

Urinary Tract Infections (UTIs)

Oral

Adults

Acute Otitis Media (AOM)

Oral

250 mg every 8 hours (as capsules or oral suspension).¹⁶⁷ For more severe infections or those caused by less susceptible organisms, 500 mg every 8 hours (as capsules or oral suspension).¹⁶⁷

Pharyngitis and Tonsillitis

Oral

250 mg every 8 hours (as capsules or oral suspension).¹⁶⁷ For more severe infections or those caused by less susceptible organisms, 500 mg every 8 hours (as capsules or oral suspension).¹⁶⁷

375 mg every 12 hours for 10 days (as extended-release tablets).¹⁶⁸ ¹⁶⁹

Respiratory Tract Infections

Lower Respiratory Tract Infections

Oral

250 mg every 8 hours (as capsules or oral suspension).¹⁶⁷ For more severe infections (e.g., pneumonia) or those caused by less susceptible organisms, 500 mg every 8 hours (as capsules or oral suspension).¹⁶⁷

Acute Bacterial Exacerbations of Chronic Bronchitis

Oral

500 mg every 12 hours for 7 days (as extended-release tablets).¹⁶⁸ ¹⁶⁹

Secondary Bacterial Infections of Acute Bronchitis

Oral

500 mg every 12 hours for 7 days (as extended-release tablets).¹⁶⁸ ¹⁶⁹

Skin and Skin Structure Infections

Oral

250 mg every 8 hours (as capsules or oral suspension).¹⁶⁷ For more severe infections or those caused by less susceptible organisms, 500 mg every 8 hours (as capsules or oral suspension).¹⁶⁷

375 mg every 12 hours for 7–10 days (as extended-release tablets).¹⁶⁸ ¹⁶⁹

Urinary Tract Infections (UTIs)

Oral

250 mg every 8 hours (as capsules or suspension).¹⁶⁷ For more severe infections or those caused by less susceptible organisms, 500 mg every 8 hours (as capsules or oral suspension).¹⁶⁷

Prescribing Limits

Pediatric Patients

Maximum 1 g daily.¹⁶⁷

Special Populations

Renal Impairment

No dosage adjustments required.¹⁶⁷

Close clinical observation and appropriate laboratory tests recommended in those with moderate or severe renal impairment.¹⁶⁷ Use with caution in patients with markedly impaired renal function.¹⁶⁷

Geriatric Patients

No age-related dosage adjustments required.¹⁶⁸ ¹⁶⁹

Cautions for Cefaclor

Contraindications

Known hypersensitivity to cefaclor, any other cephalosporin, or any ingredient in the formulation.¹⁶⁷ ¹⁶⁸ ¹⁶⁹

Warnings/Precautions

Warnings

Superinfection/Clostridium difficile-associated Diarrhea and Colitis

Possible emergence and overgrowth of nonsusceptible bacteria or fungi.¹⁶⁷ ¹⁶⁸ ¹⁶⁹ Careful observation of the patient is essential.¹⁶⁷ ¹⁶⁸ ¹⁶⁹ Institute appropriate therapy if superinfection occurs.¹⁶⁷ ¹⁶⁸ ¹⁶⁹

Treatment with anti-infectives may permit overgrowth of Clostridium difficile.¹⁶⁷ ¹⁶⁸ ¹⁶⁹ C. difficile-associated diarrhea and colitis (CDAD; also known as antibiotic-associated diarrhea and colitis or pseudomembranous colitis) has been reported with nearly all anti-infectives, including cefaclor, and may range in severity from mild diarrhea to fatal colitis.¹⁶⁷ ¹⁶⁸ ¹⁶⁹

Consider CDAD if diarrhea develops during or after therapy and manage accordingly.¹⁶⁷ ¹⁶⁸ ¹⁶⁹ Careful medical history is necessary since CDAD has been reported to occur as late as 2 months or longer after anti-infective therapy is discontinued.

If CDAD is suspected or confirmed, the anti-infective may need to be discontinued. Some mild cases may respond to discontinuance alone.¹⁶⁷ ¹⁶⁸ ¹⁶⁹ Manage moderate to severe cases with fluid, electrolyte, and protein supplementation, anti-infective therapy active against C. difficile (e.g., oral metronidazole or vancomycin), and surgical evaluation when clinically indicated.¹⁶⁷ ¹⁶⁸ ¹⁶⁹

Haemophilus influenza Infections

β-lactamase-negative, ampicillin-resistant (BLNAR) strains of H. influenzae should be considered resistant to cefaclor despite apparent in vitro susceptibility of some BLNAR strains.¹⁶⁷ This should be considered when treating infections that may involve these strains (e.g., respiratory tract infections, AOM).¹⁶⁷

Efficacy of extended-release tablets in the treatment of bronchitis known, suspected, or potentially caused by β-lactamase-producing H. influenzae has not been established.¹⁶⁸ ¹⁶⁹

Sensitivity Reactions

Hypersensitivity Reactions

Hypersensitivity reactions such as anaphylaxis, angioedema, serum sickness-like reactions, Stevens-Johnson syndrome, and toxic epidermal necrolysis have been reported.¹⁶⁷ ¹⁶⁸ ¹⁶⁹

If an allergic reaction occurs, discontinue cefaclor and institute appropriate therapy as indicated (e.g., epinephrine, corticosteroids, and maintenance of an adequate airway and oxygen).¹⁶⁷ ¹⁶⁸ ¹⁶⁹

Cross-hypersensitivity

Partial cross-hypersensitivity among cephalosporins and other β-lactam antibiotics, including penicillins and cephamycins.¹⁶⁷ ¹⁶⁸ ¹⁶⁹ ^a

Prior to initiation of therapy, make careful inquiry concerning previous hypersensitivity reactions to cephalosporins, penicillins, or other drugs.¹⁶⁷ ¹⁶⁸ ¹⁶⁹ ^a Cautious use recommended in individuals hypersensitive to penicillins:¹⁶⁷ ¹⁶⁸ ¹⁶⁹ ^a avoid use in those who have had an immediate-type (anaphylactic) hypersensitivity reaction and administer with caution in those who have had a delayed-type (e.g., rash, fever, eosinophilia) reaction.^a

General Precautions

History of GI Disease

Use cephalosporins with caution in patients with a history of GI disease, particularly colitis.¹⁶⁷ (See Superinfection/Clostridium difficile-associated Diarrhea and Colitis under Cautions.)

Specific Populations

Pregnancy

Category B.¹⁶⁷ ¹⁶⁸ ¹⁶⁹

Lactation

Distributed into milk; use with caution.¹⁶⁷ ¹⁶⁸ ¹⁶⁹

Pediatric Use

Safety and efficacy of capsules and oral suspension not established in infants <1 month of age.¹⁶⁷

Safety and efficacy of extended-release tablets not established in children <16 years of age.¹⁶⁸ ¹⁶⁹

Geriatric Use

Safety and efficacy in geriatric adults similar to that in younger adults.¹⁶⁸ ¹⁶⁹

Renal Impairment

Decreased clearance.¹⁶⁷

No dosage adjustment required for patients with renal impairment.¹⁶⁷ Close clinical observation and appropriate laboratory tests recommended in those with moderate or severe renal impairment.¹⁶⁷ Use with caution in patients with markedly impaired renal function.¹⁶⁷

Common Adverse Effects

Diarrhea, genital pruritus or vaginitis, headache, nausea, vomiting, rash.¹²³ ¹²⁵ ¹²⁷ ¹²⁹ ¹³⁰ ¹³² ¹⁵³ ¹⁶⁷ ¹⁶⁸ ¹⁶⁹

Interactions for Cefaclor

Specific Drugs and Laboratory Tests

Drug or Test	Interaction	Comments
Antacids (aluminum- or magnesium-containing)	Decreased absorption of cefaclor extended-release tablets ¹⁶⁸ ¹⁶⁹	Administer cefaclor extended-release tablets at least 1 hour before aluminum- or magnesium-containing antacids¹⁶⁸ ¹⁶⁹
Anticoagulants, oral	Possible enhanced warfarin effects¹⁶⁷ ¹⁶⁸ ¹⁶⁹
Histamine H₂-receptor antagonists	No effect on rate or extent of absorption of cefaclor extended-release tablets¹⁶⁸ ¹⁶⁹
Probenecid	Decreased renal excretion of cefaclor¹⁶⁷ ¹⁶⁸ ¹⁶⁹
Tests for glucose	Possible false-positive reactions in urine glucose tests using Clinitest, Benedict’s solution, or Fehling’s solution¹⁶⁷ ¹⁶⁸ ¹⁶⁹	Use glucose tests based on enzymatic glucose oxidase reactions (e.g., Clinistix, Tes-Tape)^a

Cefaclor Pharmacokinetics

Absorption

Bioavailability

Well absorbed from GI tract following oral administration.¹⁶⁷ ¹⁶⁸ ¹⁶⁹ Peak plasma concentrations attained within 0.5–1 hour with conventional preparations¹⁶⁷ and 1.5–2.7 hours with extended-release tablets.¹⁶⁸ ¹⁶⁹

Food

Peak serum concentrations are lower and attained later when cefaclor capsules are administrated with food, but total amount of drug absorbed is unchanged.¹⁶⁷ ¹⁰⁷ ¹⁰⁸

When extended-release tablets are administered with food, the extent of absorption and peak plasma concentrations of the drug are increased.¹⁶⁸ ¹⁶⁹

Distribution

Extent

Cephalosporins are widely distributed into tissues and fluids.^a

Distributed into milk in low concentrations.¹⁶⁷ ¹⁶⁸ ¹⁶⁹

Plasma Protein Binding

25%.^a

Elimination

Metabolism

Not appreciably metabolized.^a

Elimination Route

Excreted unchanged in urine.¹⁶⁷ About 60–85% is excreted unchanged in urine within 8 hours; majority is excreted during the first 2 hours.¹⁶⁷

Half-life

0.6–1 hour in adults with normal renal function.¹⁶⁷ ¹⁶⁸ ¹⁶⁹

Special Populations

Renal impairment decreases clearance of cefaclor.¹⁶⁷ Serum half-life is 2.3–2.8 hours in anuric patients.¹⁶⁷

Stability

Storage

Oral

Capsules

15–30°C; protect from moisture.¹⁶⁷

For Suspension

15–30°C.¹⁶⁷ After reconstitution, store suspension in tight container in the refrigerator; discard after 14 days.¹⁶⁷

Extended-release Tablets

15–30°C.¹⁶⁸ ¹⁶⁹

Actions and SpectrumActions

Second generation cephalosporin active against some gram-negative bacteria that generally are resistant to first generation cephalosporins, but has a narrower spectrum of activity than third generation cephalosporins.^a Less active against gram-negative bacteria than some other second generation cephalosporins.^a

Usually bactericidal.¹⁶⁷ ¹⁶⁸ ¹⁶⁹

Like other β-lactam antibiotics, antibacterial activity results from inhibition of bacterial cell wall synthesis.¹⁶⁷ ¹⁶⁸ ¹⁶⁹ ^a

In vitro spectrum of activity includes many gram-positive aerobic bacteria, some gram-negative aerobic bacteria, and a few anaerobic bacteria; inactive against fungi and viruses.¹⁶⁷ ¹⁶⁸ ¹⁶⁹ ^a

Gram-positive aerobes: active in vitro and in clinical infections against staphylococci (including coagulase-positive, coagulase-negative, and penicillinase producing strains), Streptococcus pneumoniae, and S. pyogenes (group A β-hemolytic streptococci).¹⁶⁷ ¹⁶⁸ ¹⁶⁹ Enterococci (e.g., Enterococcus faecalis) and oxacillin-resistant (methicillin-resistant) staphylococci are resistant.¹⁶⁷ ¹⁶⁸ ¹⁶⁹ ^a

Gram-negative aerobes: active in vitro and in clinical infections against H. influenzae (except BLNAR strains), Moraxella catarrhalis (including β-lactamase producing strains), Escherichia coli, Klebsiella, and Proteus mirabilis.¹⁶⁷ ¹⁶⁸ ¹⁶⁹ Also active in vitro against H. parainfluenzae, Citrobacter diversus, and Neisseria gonorrhoeae. Inactive against Acinetobacter, Enterobacter, Morganella morganii, Proteus vulgaris, Providencia, Pseudomonas, and Serratia.¹⁶⁷ ¹⁶⁸ ¹⁶⁹

Anaerobes: active in vitro against Bacteroides (excluding B. fragilis), Peptococcus niger, Peptostreptococcus, and Propionibacterium acnes.¹⁶⁷ ¹⁶⁸ ¹⁶⁹

Advice to Patients

Importance of completing full course of therapy.¹⁶⁷

Importance of taking cefaclor extended-release tablets at least 1 hour before antacids containing aluminum or magnesium.¹⁶⁸ ¹⁶⁹

Importance of taking cefaclor extended-release tablets with meals or within 1 hour of eating.¹⁶⁸ ¹⁶⁹

Importance of taking cefaclor extended-release tablets at least 1 hour before antacids containing aluminum or magnesium.¹⁶⁸ ¹⁶⁹

Advise patients that diarrhea is a common problem caused by anti-infectives and usually ends when the drug is discontinued. Importance of contacting a clinician if watery and bloody stools (with or without stomach cramps and fever) occur during or as late as 2 months or longer after the last dose.

Importance of discontinuing cefaclor and informing clinician if an allergic reaction occurs.¹⁶⁷ ¹⁶⁸ ¹⁶⁹

Importance of informing clinicians of existing or contemplated therapy, including prescription and OTC drugs.¹⁶⁷ ¹⁶⁸ ¹⁶⁹

Importance of informing patients of other important precautionary information. (See Cautions.)

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

* available from one or more manufacturer, distributor, and/or repackager by generic (nonproprietary) name

Cefaclor
Routes	Dosage Forms	Strengths	Brand Names	Manufacturer
Oral	Capsules	equivalent to anhydrous cefaclor 250 mg*	Cefaclor Capsules	Ranbaxy
		equivalent to anhydrous cefaclor 500 mg*	Cefaclor Capsules	Ranbaxy
	For suspension	equivalent to anhydrous cefaclor 125 mg/5 mL*	Cefaclor for Suspension	Ranbaxy
		equivalent to anhydrous cefaclor 187 mg/5 mL*	Cefaclor for Suspension	Ranbaxy
		equivalent to anhydrous cefaclor 250 mg/5 mL*	Cefaclor for Suspension	Ranbaxy
		equivalent to anhydrous cefaclor 375 mg/5 mL*	Cefaclor for Suspension	Ranbaxy
	Tablets, extended-release	equivalent to anhydrous cefaclor 500 mg	Cefaclor Extended-Release Tablets (with propylene glycol)	Teva

Comparative Pricing

This pricing information is subject to change at the sole discretion of DS Pharmacy. This pricing information was updated 03/2011. Actual costs to patients will vary depending on the use of specific retail or mail-order locations and health insurance copays.

Cefaclor 125MG/5ML Suspension (RANBAXY PHARMACEUTICALS): 150/$24.99 or 450/$53.98

Cefaclor 125MG/5ML Suspension (RANBAXY PHARMACEUTICALS): 75/$16.99 or 225/$34.97

Cefaclor 250MG Capsules (WEST-WARD): 30/$60.99 or 90/$165.97

Cefaclor 250MG/5ML Suspension (RANBAXY PHARMACEUTICALS): 150/$34.99 or 450/$84.97

Cefaclor 250MG/5ML Suspension (RANBAXY PHARMACEUTICALS): 75/$22.99 or 225/$47.98

Cefaclor 375MG/5ML Suspension (RANBAXY PHARMACEUTICALS): 100/$34.99 or 300/$84.97

Cefaclor 500MG Capsules (RANBAXY PHARMACEUTICALS): 30/$87.99 or 90/$249.98

Disclaimer

This report on medications is for your information only, and is not considered individual patient advice. Because of the changing nature of drug information, please consult your physician or pharmacist about specific clinical use.

The American Society of Health-System Pharmacists, Inc. and Drugs.com represent that the information provided hereunder was formulated with a reasonable standard of care, and in conformity with professional standards in the field. The American Society of Health-System Pharmacists, Inc. and Drugs.com make no representations or warranties, express or implied, including, but not limited to, any implied warranty of merchantability and/or fitness for a particular purpose, with respect to such information and specifically disclaims all such warranties. Users are advised that decisions regarding drug therapy are complex medical decisions requiring the independent, informed decision of an appropriate health care professional, and the information is provided for informational purposes only. The entire monograph for a drug should be reviewed for a thorough understanding of the drug's actions, uses and side effects. The American Society of Health-System Pharmacists, Inc. and Drugs.com do not endorse or recommend the use of any drug. The information is not a substitute for medical care.

AHFS Drug Information. © Copyright, 1959-2011, Selected Revisions March 2008. American Society of Health-System Pharmacists, Inc., 7272 Wisconsin Avenue, Bethesda, Maryland 20814.

References

Only references cited for selected revisions after 1984 are available electronically.

101. American Academy of Pediatrics. 2006 Red Book: Report of the Committee on Infectious Diseases. 27th ed. Elk Grove Village, IL: American Academy of Pediatrics; 2006:754.

102. Dajani A, Taubert K, Ferrieri P et al and the American Heart Association Committee on Rheumatic Fever et al. Treatment of acute streptococcal pharyngitis and prevention of rheumatic fever: a statement for health professionals. Pediatrics. 1995; 96:758-64. [IDIS 355409] [PubMed 7567345]

104. Anon. The choice of antibacterial drugs. Med Lett Drugs Ther. 2001; 43:69-78. [PubMed 11518876]

105. Clinical and Laboratory Standards Institute. Performance standards for antimicrobial susceptibility testing; sixteenth informational supplement. CLSI document M100-S16. Wayne, PA; 2006.

106. Cooper RJ, Hoffman JR, Bartlett JG et al. Principles of appropriate antibiotic use for acute pharyngitis in adults: background. Ann Intern Med. 2001; 134:509-17. [IDIS 460578] [PubMed 11255530]

107. Barbhaiya RH, Shukla UA, Gleason CR et al. Comparison of the effects of food on the pharmacokinetics of cefprozil and cefaclor. Antimicrob Agents Chemother. 1990; 34:1210-3. [IDIS 267827] [PubMed 2393283]

108. Oguma T, Yamade H, Sawaki M et al. Pharmacokinetic analysis of the effects of different foods on absorption of cefaclor. Antimicrob Agents Chemother. 1991; 35:1729-35. [IDIS 287973] [PubMed 1952839]

109. Kearns GL, Wheeler JG, Childress SH et al. Serum sickness-like reactions to cefaclor: role of hepatic metabolism and individual susceptibility. J Pediatr. 1994; 125:805-11. [IDIS 337828] [PubMed 7965438]

110. Reynolds RD. Cefaclor and serum sickness-like reaction. JAMA. 1996; 276:950. [IDIS 372320] [PubMed 8805721]

111. Kelsey DK. Cefaclor and serum sickness-like reaction. JAMA. 1996; 276:950-1. [IDIS 372320] [PubMed 8805721]

112. Stricker BH, Tussen JGP. Serum sickness-like reactions to cefaclor. J Clin Epidemiol. 1992; 45:1177-84. [PubMed 1474414]

113. Platt R, Dreis MW, Kennedy DL et al. Serum sickness-like reactions to amoxicillin, cefaclor, cephalexin, and trimethoprim-sulfamethoxazole. J Infect Dis. 1988; 158:474-7. [IDIS 309474] [PubMed 3261315]

114. Heckbert SR, Stryker WS, Coltin KL et al. Serum sickness in children after antibiotic exposure: estimates of occurrence and morbidity in a health maintenance organization population. Am J Epidemiol. 1990; 132:336-42. [PubMed 2115293]

115. Hebert AA, Sigman ES, Levy ML. Serum sickness-like reactions from cefaclor in children. J Am Acad Dermatol. 1991; 25:805-8. [PubMed 1802903]

116. Kishiyama JL, Adelman DC. The cross-reactivity and immunology of β-lactam antibiotics. Drug Saf. 1994; 10:318-27. [PubMed 8018304]

117. Thompson JW, Jacobs RF. Adverse effects of newer cephalosporins: an update. Drug Saf. 1993; 9:132-42. [PubMed 8397890]

118. Kearns GL, Wheeler JG, Rieder MJ et al. Serum sickness-like reaction to cefaclor: lack of in vitro cross-reactivity with loracarbef. Clin Pharmacol Ther. 1998; 63:686-93. [IDIS 407803] [PubMed 9663184]

119. Vial T, Pont J, Pham E et al. Cefaclor-associated serum sickness-like disease: eight cases and review of the literature. Ann Pharmacother. 1992; 26:910-4. [IDIS 299194] [PubMed 1504397]

120. Stutman HR, Arguedas AG. Comparison of cefprozil and other antibiotic regimens in the treatment of acute otitis media. Clin Infect Dis. 1992; 14(Suppl 2):S204-8. [IDIS 297198] [PubMed 1617039]

121. Kafetzis DA. Multi-investigator evaluation of the efficacy and safety of cefprozil, amoxicillin-clavulanate, cefixime and cefaclor in the treatment of acute otitis media. Eur J Clin Microbiol Infect Dis. 1994; 13:857-65. [PubMed 7889960]

122. Phillips H, Van Hook CJ, Butler T et al. A comparison of cefpodoxime proxetil and cefaclor in the treatment of acute exacerbation of COPD in adults. Chest. 1993; 104:1387-92. [IDIS 322127] [PubMed 8222793]

123. MacLoughlin GJF, Barreto DG, de la Torre C et al. Cefpodoxime proxetil suspension compared with cefaclor suspension for treatment of acute otitis media in paediatric patients. J Antimicrob Chemother. 1996; 37:565-73. [IDIS 365661] [PubMed 9182113]

124. Reed BD, Huck W, Zazove P. Treatment of beta-hemolytic streptococcal pharyngitis with cefaclor or penicillin. J Fam Pract. 1991; 32:138-44. [PubMed 1990041]

125. Perotta R, McCabe R, Rumans L et al. Comparison of the efficacy and safety of ceftibuten and cefaclor in the treatment of acute bacterial bronchitis. Infect Dis Clin Pract. 1994; 3:270-6.

126. Chirurgi VA, Edelstein H, Oster SE et al. Ceftibuten versus cefaclor for the treatment of bronchitis. J Antimicrob Chemother. 1991; 28:577-80. [PubMed 1761452]

127. Blumer JL, McLinn SE, Deabate CA et al and the Ceftibuten Otitis Media International study Group. Pediatr Infect Dis J. 1995; 14:S115-20.

128. Rodriguez WJ, Khan W, Sait T et al. Cefixime vs. cefaclor in the treatment of acute otitis media in children: a randomized, comparative study. Pediatr Infect Dis J. 1993; 12:70-4. [PubMed 8417429]

129. Pichichero M, Aronovitz GH, Gooch WM et al. Comparison of cefuroxime axetil, cefaclor, and amoxicillin-clavulanate potassium suspensions in acute otitis media in infants and children. S Med J. 1990; 83:1174-7.

130. Marchant CD, Shurin PA, Turcyzk VA et al. A randomized controlled trial of cefaclor compared with trimethoprim-sulfamethoxazole for treatment of acute otitis media. J Pediatr. 1984; 105:633-8. [IDIS 190938] [PubMed 6384453]

131. Mandel EM, Kardatzke D, Bluestone CD et al. A comparative evaluation of cefaclor and amoxicillin in the treatment of acute otitis media. Pediatr Infect Dis J. 1993; 12:726-32. [PubMed 8414799]

132. Harrison CJ, Chartrand SA, Pichichero ME. Microbiologic and clinical aspects of a trial of once daily cefixime compared with twice daily cefaclor for treatment of acute otitis media in infants and children. Pediatr Infect Dis J. 1993; 12:62-9. [PubMed 8417428]

133. Mandel EM, Rockette HE, Paradise JL et al. Comparative efficacy of erythromycin-sulfisoxazole, cefaclor, amoxicillin or placebo for otitis media with effusion in children. Pediatr Infect Dis J. 1991; 10:899-906. [PubMed 1766705]

134. Hendrickse WA, Kusmiesz H, Shelton S et al. Five vs. ten days of therapy for acute otitis media. Pediatr Infect Dis J. 1988; 7:14-23. [PubMed 3277153]

135. Christenson JC, Swenson E, Gooch WM et al. Comparative efficacy and safety of cefprozil (BMY-28100) and cefaclor in the treatment of acute group A beta-hemolytic streptococcal pharyngitis. Antimicrob Agents Chemother. 1991; 35:1127-30. [IDIS 283443] [PubMed 1929253]

136. Parish LC, Doyle CA, Durham SJ et al. Cefprozil versus cefaclor in the treatment of mild to moderate skin and skin structure infections. Clin Ther. 1992; 14:458-69. [PubMed 1638587]

137. Kozyrskyj AL, Hildes-Ripstein GE, Longstaffe SEA et al. Treatment of acute otitis media with a shortened course of antibiotics: a meta-analysis. JAMA. 1998; 279:1736-42. [IDIS 409347] [PubMed 9624028]

138. Pichichero ME, Cohen R. Shortened course of antibiotic therapy for acute otitis media, sinusitis and tonsillopharyngitis. Pediatr Infect Dis J. 1997; 16:680-95. [IDIS 390075] [PubMed 9239773]

139. Williams RL, Chalmers TC, Stange KC et al. Use of antibiotics in preventing recurrent acute otitis media and in treating otitis media with effusion: a meta-analytic attempt to resolve the brouhaha. JAMA. 1993; 270:1344-51. [IDIS 319598] [PubMed 8141875]

140. Paradise JL. Treatment guidelines for otitis media: the need for breadth and flexibility. Pediatr Infect Dis J. 1995; 14:429-35. [IDIS 348106] [PubMed 7638033]

141. Berman S. Otitis media in children. N Engl J Med. 1995; 332:1560-5. [IDIS 348227] [PubMed 7739711]

142. The Otitis Media Guideline Panel. Managing otitis media with effusion in young children. Pediatrics. 1994; 94:766-73. [IDIS 337882] [PubMed 7936917]

143. Klein JO. Selection of oral antimicrobial agents for otitis media and pharyngitis. Infect Dis Clin Pract. 1995; 4(Suppl 2):S88-94.

144. Bisno AL, Gerber MA, Gwaltney JM et al et al. Diagnosis and management of group A streptococcal pharyngitis: a practice guideline. Clin Infect Dis. 1997; 25:574-83. [PubMed 9314443]

145. Klein JO. Management of streptococcal pharyngitis. Pediatr Infect Dis J. 1994; 13:572-5. [IDIS 331902] [PubMed 8078757]

146. Pichichero ME, Cohen R. Shortened course of antibiotic therapy for acute otitis media, sinusitis and tonsillopharyngitis. Pediatr Infect Dis J. 1997; 16:680-95. [IDIS 390075] [PubMed 9239773]

147. Tack KJ, Henry DC, Gooch WM et al et al. Five-day cefdinir treatment for streptococcal pharyngitis. Antimicrob Agents Chemother. 1998; 42:1073-5. [IDIS 404900] [PubMed 9593129]

148. Pichichero ME. Cephalosporins are superior to penicillin for treatment of streptococcal tonsillopharyngitis: is the difference worth it? Pediatr Infect Dis. 1993; 12:268-74.

149. Aujard Y, Boucot I, Brahimi N et al. Comparative efficacy and safety of four-day cefuroxime axetil and ten-day penicillin treatment of group A beta-hemolytic streptococcal pharyngitis in children. Pediatr Infect Dis J. 1995; 14:295-300. [IDIS 345876] [PubMed 7603811]

150. Mehra S, Van Moerkerke M, Welck J et al. Short course therapy with cefuroxime axetil for group A streptococcal tonsillopharyngitis in children. Pediatr Infect Dis J. 1998; 17:452-7. [IDIS 408830] [PubMed 9655533]

151. Milatovic D. Evaluation of cefadroxil, penicillin and erythromycin in the treatment of streptococcal tonsillopharyngitis. Pediatr Infect Dis J. 1991; 10:S61-3. [PubMed 1945599]

152. Esposito S, De Ritis G, D’Errico G et al. Clinical comparison of cefaclor twice daily versus amoxicillin-clavulanate or erythromycin three times daily in the treatment of patients with streptococcal pharyngitis. Clin Ther. 1998; 20:72-9. [IDIS 402071] [PubMed 9522105]

153. Derriennic M, Voi M, Thoren LM et al. Cefaclor AF in the treatment of streptococcal pharyngitis/tonsillitis. Postgrad Med J. 1992; 68(Suppl 3):S43-6. [PubMed 1287618]

154. Paradise JL. Short-course antimicrobial treatment for acute otitis media: not best for infants and young children. JAMA. 1997; 278:1640-2. [IDIS 396934] [PubMed 9388072]

155. Adam D, Hostalek U, Troster K. 5-day cefixime therapy for bacterial pharyngitis and/or tonsillitis: comparison with 10-day penicillin V therapy. Infection. 1995; 23(Supp 2):S83-6. [PubMed 8537138]

156. Lowery N, Kearns GL, Young RA et al. Serum sickness-like reactions associated with cefprozil therapy. J Pediatr. 1994; 125:325-8. [IDIS 335503] [PubMed 8040786]

157. Grouhi M, Hummel D, Roifman CM. Anaphylactic reaction to oral cefaclor in a child. Pediatrics. 1999; 103:50-1.

158. Beghetti M, Wilson GJ, Bohn D et al. Hypersensitivity myocarditis caused by an allergic reaction to cefaclor. J Pediatr. 1998; 132:172-3. [IDIS 401043] [PubMed 9470025]

159. Dowell SF, Marcy SM, Phillips WR et al. Otitis media—principles of judicious use of antimicrobial agents. Pediatrics. 1998; 101:165-71.

160. Stool SE, Berg AO, Berman S et al for the Otitis Media Guideline Panel. Otitis media with effusion in young children. Clinical Practice Guideline. Number 12. AHCPR Publication No. 94-0622. Rockville, MD: Agency for Health Care Policy and Research, Public Health Service, US Department of Health and Human Resources. July 1994.

161. Perry BP, Zieno SA, Yonkers AJ. Outcome-oriented managed care comparing efficacies of cefaclor and amoxicillin in acute and recurrent acute otitis media. Ear Nose Throat J. 1995; 74:840-4. [PubMed 8556984]

162. Adderson EE. Preventing otitis media: medical approaches. Pediatr Ann. 1998; 27:101-7. [PubMed 9523298]

163. Klein JO. Protecting the therapeutic advantage of antimicrobial agents used for otitis media. Pediatr Infect Dis J. 1998; 17:571-5. [IDIS 408841] [PubMed 9655563]

164. Dowell SF, Marcy SM, Phillips WR et al. Otitis media—principles of judicious use of antimicrobial agents. Pediatrics. 1998; 101:165-71.

165. American Academy of Pediatrics and American Academy of Family Physicians Subcommittee on Management of Acute Otitis Media. Diagnosis and management of acute otitis media. Pediatrics. 2004: 113:1451-65.

166. American Academy of Pediatrics, American Academy of Family Physicians, American Academy of Otolaryngology-Head and Neck Surgery, and American Academy of Pediatrics Subcommittee on Otitis Media with Effusion. Otitis media with effusion. Pediatrics. 2004: 113:1412-29.

167. Ranbaxy. Cefaclor capsules USP and cefaclor for oral suspension USP prescribing information. Princeton, NJ; 2000 Jan.

168. Teva. Cefaclor extended-release tablets USP prescribing information. Sellersville, PA; 2002 May.

169. Ivax. Cefaclor extended-release tablets USP prescribing information. Miami, FL; 2003 Jan.

a. AHFS Drug Information. McEvoy GK, ed. Cephalosporins General Statement. Bethesda, MD: American Society of Health-System Pharmacists; 2003: 125-39.

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Bladder Infection
Bronchitis
Kidney Infections
Otitis Media
Pneumonia
Sinusitis
Skin and Structure Infection
Skin Infection
Tonsillitis/Pharyngitis
Upper Respiratory Tract Infection
Urinary Tract Infection

Monday, 23 July 2012

FML

fluorometholone

Dosage Form: ophthalmic suspension
FML®

(fluorometholone ophthalmic suspension, USP) 0.1%

Sterile

DESCRIPTION

FML® (fluorometholone ophthalmic suspension, USP) 0.1% is a sterile, topical anti-inflammatory agent for ophthalmic use.

Chemical Name:

Fluorometholone: 9-Fluoro-11β,17-dihydroxy-6α-methylpregna-1,4-diene-3,20-dione.

Structural Formula:

Contains: Active: fluorometholone 0.1%. Preservative: benzalkonium chloride 0.004%. Inactives: edetate disodium; polysorbate 80; polyvinyl alcohol 1.4%; purified water; sodium chloride; sodium phosphate, dibasic; sodium phosphate, monobasic; and sodium hydroxide to adjust the pH. FML® suspension is formulated with a pH from 6.2 to 7.5. It has an osmolality range of 290-350 mOsm/kg.

CLINICAL PHARMACOLOGY

Corticosteroids inhibit the inflammatory response to a variety of inciting agents and probably delay or slow healing. They inhibit the edema, fibrin deposition, capillary dilation, leukocyte migration, capillary proliferation, fibroblast proliferation, deposition of collagen, and scar formation associated with inflammation.

There is no generally accepted explanation for the mechanism of action of ocular corticosteroids. However, corticosteroids are thought to act by the induction of phospholipase A2 inhibitory proteins, collectively called lipocortins. It is postulated that these proteins control the biosynthesis of potent mediators of inflammation such as prostaglandins and leukotrienes by inhibiting the release of their common precursor arachidonic acid. Arachidonic acid is released from membrane phospholipids by phospholipase A2.

Corticosteroids are capable of producing a rise in intraocular pressure. In clinical studies of documented steroid-responders, fluorometholone demonstrated a significantly longer average time to produce a rise in intraocular pressure than dexamethasone phosphate; however, in a small percentage of individuals, a significant rise in intraocular pressure occurred within one week. The ultimate magnitude of the rise was equivalent for both drugs.

INDICATIONS AND USAGE

FML® suspension is indicated for the treatment of corticosteroid-responsive inflammation of the palpebral and bulbar conjunctiva, cornea and anterior segment of the globe.

CONTRAINDICATIONS

FML® suspension is contraindicated in most viral diseases of the cornea and conjunctiva, including epithelial herpes simplex keratitis (dendritic keratitis), vaccinia, and varicella, and also in mycobacterial infection of the eye and fungal diseases of ocular structures. FML® suspension is also contraindicated in individuals with known or suspected hypersensitivity to any of the ingredients of this preparation and to other corticosteroids.

WARNINGS

Prolonged use of corticosteroids may result in glaucoma with damage to the optic nerve, defects in visual acuity and fields of vision, and in posterior subcapsular cataract formation. Prolonged use may also suppress the host immune response and thus increase the hazard of secondary ocular infections.

Various ocular diseases and long-term use of topical corticosteroids have been known to cause corneal and scleral thinning. Use of topical corticosteroids in the presence of thin corneal or scleral tissue may lead to perforation.

Acute purulent infections of the eye may be masked or activity enhanced by the presence of corticosteroid medication.

If this product is used for 10 days or longer, intraocular pressure should be routinely monitored even though it may be difficult in children and uncooperative patients. Steroids should be used with caution in the presence of glaucoma. Intraocular pressure should be checked frequently.

The use of steroids after cataract surgery may delay healing and increase the incidence of bleb formation.

Use of ocular steroids may prolong the course and may exacerbate the severity of many viral infections of the eye (including herpes simplex). Employment of a corticosteroid medication in the treatment of patients with a history of herpes simplex requires great caution; frequent slit lamp microscopy is recommended.

Corticosteroids are not effective in mustard gas keratitis and Sjögren's keratoconjunctivitis.

PRECAUTIONS

General:

The initial prescription and renewal of the medication order beyond 20 milliliters of FML® suspension should be made by a physician only after examination of the patient with the aid of magnification, such as slit lamp biomicroscopy and, where appropriate, fluorescein staining. If signs and symptoms fail to improve after two days, the patient should be re-evaluated.

As fungal infections of the cornea are particularly prone to develop coincidentally with long-term local corticosteroid applications, fungal invasion should be suspected in any persistent corneal ulceration where a corticosteroid has been used or is in use. Fungal cultures should be taken when appropriate.

If this product is used for 10 days or longer, intraocular pressure should be monitored (see WARNINGS).

Information for Patients:

If inflammation or pain persists longer than 48 hours or becomes aggravated, the patient should be advised to discontinue use of the medication and consult a physician.

This product is sterile when packaged. To prevent contamination, care should be taken to avoid touching the bottle tip to eyelids or to any other surface. The use of this bottle by more than one person may spread infection. Keep bottle tightly closed when not in use. Keep out of the reach of children.

The preservative in FML® suspension, benzalkonium chloride, may be absorbed by soft contact lenses. Patients wearing soft contact lenses should be instructed to wait at least 15 minutes after instilling FML® suspension to insert soft contact lenses.

Carcinogenesis, mutagenesis, impairment of fertility:

No studies have been conducted in animals or in humans to evaluate the possibility of these effects with fluorometholone.

Pregnancy:

Teratogenic effects. Pregnancy Category C: Fluorometholone has been shown to be embryocidal and teratogenic in rabbits when administered at low multiples of the human ocular dose. Fluorometholone was applied ocularly to rabbits daily on days 6-18 of gestation, and dose-related fetal loss and fetal abnormalities including cleft palate, deformed rib cage, anomalous limbs and neural abnormalities such as encephalocele, craniorachischisis, and spina bifida were observed. There are no adequate and well-controlled studies of fluorometholone in pregnant women, and it is not known whether fluorometholone can cause fetal harm when administered to a pregnant woman. Fluorometholone should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.

Nursing Mothers:

It is not known whether topical ophthalmic administration of corticosteroids could result in sufficient systemic absorption to produce detectable quantities in human milk. Systemically administered corticosteroids appear in human milk and could suppress growth, interfere with endogenous corticosteroid production, or cause other untoward effects. Because of the potential for serious adverse reactions in nursing infants from fluorometholone, a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother.

Pediatric Use:

Safety and effectiveness in infants below the age of 2 years have not been established.

Geriatric Use:

No overall differences in safety or effectiveness have been observed between elderly and younger patients.

Adverse Reactions

Adverse reactions include, in decreasing order of frequency, elevation of intraocular pressure (IOP) with possible development of glaucoma and infrequent optic nerve damage, posterior subcapsular cataract formation, and delayed wound healing.

Although systemic effects are extremely uncommon, there have been rare occurrences of systemic hypercorticoidism after use of topical steroids.

Corticosteroid-containing preparations have also been reported to cause acute anterior uveitis and perforation of the globe. Keratitis, conjunctivitis, corneal ulcers, mydriasis, conjunctival hyperemia, loss of accommodation and ptosis have occasionally been reported following local use of corticosteroids.

The development of secondary ocular infection (bacterial, fungal and viral) has occurred. Fungal and viral infections of the cornea are particularly prone to develop coincidentally with long-term applications of steroids. The possibility of fungal invasion should be considered in any persistent corneal ulceration where steroid treatment has been used (see WARNINGS).

Transient burning and stinging upon instillation and other minor symptoms of ocular irritation have been reported with the use of FML® suspension. Other adverse events reported with the use of FML® suspension include: allergic reactions, visual disturbance (blurry vision), and taste perversion.

DOSAGE AND ADMINISTRATION

Instill one drop into the conjunctival sac two to four times daily. During the initial 24 to 48 hours, the dosage may be increased to one application every four hours. Care should be taken not to discontinue therapy prematurely.

If signs and symptoms fail to improve after two days, the patient should be re-evaluated (see PRECAUTIONS).

The dosing of FML® suspension may be reduced, but care should be taken not to discontinue therapy prematurely. In chronic conditions, withdrawal of treatment should be carried out by gradually decreasing the frequency of applications.

HOW SUPPLIED

FML® (fluorometholone ophthalmic suspension, USP) 0.1% is supplied sterile in opaque white LDPE plastic bottles with droppers with white high impact polystyrene (HIPS) caps as follows:

     5mL in 10mL bottle NDC 11980-211-05

   10mL in 15mL bottle NDC 11980-211-10

   15mL in 15mL bottle NDC 11980-211-15

Note: Store between 2° and 25°C (36° - 77°F); protect from freezing. Shake well before using.

Rx Only

Revised June 2003

ALLERGAN

NDC 11980-211-15

Rx Only

FML®

(fluorometholone

ophthalmic suspension,

USP) 0.1%

15 mL sterile

ALLERGAN

NDC 11980-211-15 Rx Only

FML®

(fluorometholone

ophthalmic suspension,

USP) 0.1%

15 mL sterile

FML
fluorometholone suspension/ drops

Product Information
Product Type	HUMAN PRESCRIPTION DRUG	NDC Product Code (Source)	11980-211
Route of Administration	OPHTHALMIC	DEA Schedule

Active Ingredient/Active Moiety
Ingredient Name	Basis of Strength	Strength
fluorometholone (fluorometholone)	fluorometholone	1 mg in 1 mL

Inactive Ingredients
Ingredient Name	Strength
benzalkonium chloride
edetate disodium
polysorbate 80
polyvinyl alcohol
water
sodium chloride
sodium phosphate, dibasic
sodium phosphate, monobasic
sodium hydroxide

Product Characteristics
Color		Score
Shape		Size
Flavor		Imprint Code
Contains

Packaging
#	NDC	Package Description	Multilevel Packaging
1	11980-211-05	1 BOTTLE In 1 CARTON	contains a BOTTLE, DROPPER
1		5 mL In 1 BOTTLE, DROPPER	This package is contained within the CARTON (11980-211-05)
2	11980-211-10	1 BOTTLE In 1 CARTON	contains a BOTTLE, DROPPER
2		10 mL In 1 BOTTLE, DROPPER	This package is contained within the CARTON (11980-211-10)
3	11980-211-15	1 BOTTLE In 1 CARTON	contains a BOTTLE, DROPPER
3		15 mL In 1 BOTTLE, DROPPER	This package is contained within the CARTON (11980-211-15)

Marketing Information
Marketing Category	Application Number or Monograph Citation	Marketing Start Date	Marketing End Date
NDA	NDA016851	02/01/1972

Labeler - Allergan, Inc. (144796497)

Establishment
Name	Address	ID/FEI	Operations
Allergan, Inc.		362898611	MANUFACTURE

Revised: 10/2010Allergan, Inc.

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FML Dosage
FML Use in Pregnancy & Breastfeeding
FML Drug Interactions
0 Reviews for FML - Add your own review/rating

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Saturday, 14 July 2012

Varibar Thin oral and rectal

Generic Name: barium sulfate (oral and rectal) (BER ee um SUL fate)

Brand Names: Anatrast, Bar-Test, Baricon, Baro-Cat, Barosperse, Bear-E-Yum GI, CheeTah, CheeTah Butterscotch, CheeTah Chocolaty-Fudge, CheeTah Orange, CheeTah Raspberry, Digibar 190, E-Z AC, E-Z Disk, E-Z Dose Kit with Polibar Plus, E-Z Paste, E-Z-Cat, E-Z-Cat Dry, E-Z-HD, E-Z-Paque, Enecat, Eneset 2, Enhancer, Entero VU, Entero-H, Entrobar, Esopho-Cat, Intropaste, Liqui-Coat HD, Liquid Barosperse, Liquid E-Z Paque, Liquid Polibar, Liquid Polibar Plus, Maxibar, Medebar Plus, Medebar Super 250, Polibar ACB, Readi-Cat, Readi-Cat 2, Scan C, Sitzmarks, Smoothie Readi-Cat 2, Sol-O-Pake, Tagitol V, Tonojug, Tonopaque, Varibar Honey, Varibar Nectar, Varibar Pudding, Varibar Thin, Varibar Thin Honey, Volumen

What is barium sulfate?

Barium sulfate is in a group of drugs called contrast agents. Barium sulfate works by coating the inside of your esophagus, stomach, or intestines which allows them to be seen more clearly on a CT scan or other radiologic (x-ray) examination.

Barium sulfate is used to help diagnose certain disorders of the esophagus, stomach, or intestines.

Barium sulfate may also be used for purposes not listed in this medication guide.

What is the most important information I should know about barium sulfate?

You should not use this medication if you are allergic to barium sulfate. Tell your doctor if you have ever had an allergic reaction to a contrast agent.

Before you use barium sulfate, tell your doctor if you have any allergies, or if you have asthma, cystic fibrosis, heart disease or high blood pressure, rectal cancer, a colostomy, a blockage in your stomach or intestines, a condition called pseudotumor cerebri, or if you have recently had a rectal biopsy or surgery on your esophagus, stomach, or intestines.

Tell your doctor if you are pregnant or breast-feeding before your medical test.

Carefully follow your doctor's instructions about what to eat or drink within the 24-hour period before your test.

Serious side effects of barium sulfate may include severe stomach pain, sweating, ringing in your ears, pale skin, weakness, or severe cramping, diarrhea, or constipation

What should I discuss with my health care provider before using barium sulfate?

You should not use barium sulfate if you are allergic to it. Tell your doctor if you have ever had an allergic reaction to a contrast agent.

To make sure you can safely use barium sulfate, tell your doctor if you have any of these other conditions:

asthma, eczema, or allergies;

a blockage in your stomach or intestines;

cystic fibrosis;

a colostomy;

rectal cancer;

heart disease or high blood pressure;

Hirschsprung's disease (a disorder of the intestines);

a condition called pseudotumor cerebri (high pressure inside the skull that may cause headaches, vision loss, or other symptoms);

a recent history of surgery on your esophagus, stomach, or intestines;

a history of perforation (a hole or tear) in your esophagus, stomach, or intestines;

if you have recently had a rectal biopsy;

if you have ever choked on food by accidentally inhaling it into your lungs;

if you are allergic to simethicone (Gas-X, Phazyme, and others); or

if you are allergic to latex rubber.

It is not known whether barium sulfate will harm an unborn baby, but the radiation used in x-rays and CT scans may be harmful. Before your medical test, tell your doctor if you are pregnant. Barium sulfate may pass into breast milk and could harm a nursing baby. Before your medical test, tell your doctor if you are breast-feeding a baby.

How should I use barium sulfate?

Use this medication exactly as prescribed by your doctor. Do not use it in larger amounts or for longer than recommended.

Barium sulfate comes in tablets, paste, cream, or liquid forms.

In some cases, barium sulfate is taken by mouth. The liquid form may also be used as a rectal enema.

You may need to begin using this medication at home a day before your medical test. Follow your doctor's instructions about how much of the medication to use and how often.

If you are receiving barium sulfate as a rectal enema, a healthcare professional will give you the medication at the clinic or hospital where your testing will take place.

Do not crush, chew, or break a barium sulfate tablet. Swallow the pill whole.

Dissolve the barium sulfate powder in a small amount of water. Stir this mixture and drink all of it right away. To make sure you get the entire dose, add a little more water to the same glass, swirl gently and drink right away.

If you receive the medication as a liquid to take by mouth, shake the liquid well just before you measure a dose. To be sure you get the correct dose, measure the liquid with a marked measuring spoon or medicine cup, not with a regular table spoon. If you do not have a dose-measuring device, ask your pharmacist for one.

Carefully follow your doctor's instructions about what to eat or drink within the 24-hour period before your test.

Store at room temperature away from heat and moisture. Keep the bottle tightly closed when not in use.

What happens if I miss a dose?

If you are using barium sulfate at home, call your doctor for instructions if you miss a dose.

What happens if I overdose?

Seek emergency medical attention or call the Poison Help line at 1-800-222-1222.

Overdose symptoms may include severe stomach pain, ongoing diarrhea, confusion, or weakness.

What should I avoid before or after using barium sulfate?

Follow your doctor's instructions about any restrictions on food, beverages, or activity.

Barium sulfate side effects

Get emergency medical help if you have any of these signs of an allergic reaction: hives; difficulty breathing; swelling of your face, lips, tongue, or throat. Call your doctor at once if you have a serious side effect such as:

severe stomach pain;

severe cramping, diarrhea, or constipation;

sweating;

ringing in your ears;

confusion, fast heart rate; or

pale skin, weakness.

Less serious side effects may include:

mild stomach cramps;

nausea, vomiting;

loose stools or mild constipation.

This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

What other drugs will affect barium sulfate?

There may be other drugs that can interact with barium sulfate. Tell your doctor about all medications you use. This includes prescription, over-the-counter, vitamin, and herbal products. Do not start a new medication without telling your doctor.

More Varibar Thin resources

Varibar Thin Side Effects (in more detail)
Varibar Thin Use in Pregnancy & Breastfeeding
Varibar Thin Support Group
0 Reviews for Varibar Thin - Add your own review/rating

Compare Varibar Thin with other medications

Computed Tomography

Where can I get more information?

Your doctor or pharmacist can provide more information about barium sulfate.

See also: Varibar Thin side effects (in more detail)

Thursday, 12 July 2012

cabazitaxel

Generic Name: cabazitaxel (ka BAZ i TAX el)

Brand Names: Jevtana

What is cabazitaxel?

Cabazitaxel is a cancer medication that interferes with the growth and spread of cancer cells in the body.

Cabazitaxel is used together with prednisone to treat prostate cancer that has spread to other parts of the body (metastatic).

Cabazitaxel is usually given after other cancer medicines have been tried without successful treatment.

Cabazitaxel may also be used for purposes not listed in this medication guide.

What is the most important information I should know about cabazitaxel?

Do not use cabazitaxel if you are pregnant. It could harm the unborn baby. You should not use this medication if you are allergic to cabazitaxel, or if you have liver disease, low white blood cell counts, or an allergy to any medicine that contains polysorbate 80. You should not breast-feed while you are receiving cabazitaxel.

Before you receive cabazitaxel, tell your doctor if you have ever had a severe allergic reaction to any medication.

Cabazitaxel is used together with prednisone, and you may also be given other medications to help prevent certain side effects. Use all medications as directed by your doctor.

To make sure cabazitaxel is helping your condition and not causing harmful effects, your blood will need to be tested often.

What should I discuss with my health care provider before receiving cabazitaxel?

You should not use this medication if you are allergic to cabazitaxel, or if you have:

liver disease;

low white blood cell counts; or

an allergy to any medicine that contains polysorbate 80.

To make sure you can safely receive cabazitaxel, tell your doctor if you have ever had a severe allergic reaction to any medication.

FDA pregnancy category D. Do not use cabazitaxel if you are pregnant. It could harm the unborn baby. Use effective birth control, and tell your doctor if you become pregnant during treatment. It is not known whether cabazitaxel passes into breast milk or if it could harm a nursing baby. You should not breast-feed while you are receiving cabazitaxel. Serious side effects may be more likely in older adults receiving cabazitaxel.

How is cabazitaxel given?

Cabazitaxel is injected into a vein through an IV. You will receive this injection in a clinic or hospital setting. Cabazitaxel must be given slowly, and the IV infusion can take about 1 hour to complete.

Cabazitaxel is usually given once every 3 weeks. You will most likely take prednisone by mouth every day throughout your cabazitaxel treatment. Follow your doctor's dosing instructions very carefully.

Do not stop taking prednisone without your doctor's advice, or you could have unpleasant side effects caused by cabazitaxel. Tell your doctor if you have missed any doses or have stopped taking prednisone for any reason.

About 30 minutes before you receive cabazitaxel, you may be given other medications to help prevent certain side effects.

Use all medications as directed by your doctor. Read the medication guide or patient instructions provided with each medication. Do not change your doses or medication schedule without your doctor's advice.

To make sure this medication is helping your condition and not causing harmful effects, your blood will need to be tested often. Your cancer treatments may be delayed based on the results of these tests. Do not miss any follow-up visits to your doctor.

Your doctor may tell you to check your temperature at home throughout your treatment with cabazitaxel.

Call your doctor if you have ongoing vomiting or diarrhea, or if you are sweating more than usual. You can easily become dehydrated while receiving cabazitaxel, which can lead to a serious electrolyte imbalance.

What happens if I miss a dose?

Call your doctor for instructions if you miss an appointment for your cabazitaxel injection.

What happens if I overdose?

Seek emergency medical attention or call the Poison Help line at 1-800-222-1222.

Overdose symptoms may include some of the serious side effects listed in this medication guide.

What should I avoid while receiving cabazitaxel?

Avoid taking an herbal supplement containing St. John's wort while you are being treated with cabazitaxel.

Cabazitaxel side effects

Get emergency medical help if you have any of these signs of an allergic reaction: hives, red skin rash; difficult breathing; feeling light-headed; swelling of your face, lips, tongue, or throat. Call your doctor at once if you have a serious side effect such as:

fever, cough, chills, muscle aches, flu symptoms, sores in your mouth and throat, rapid and shallow breathing, fainting;

pale skin, feeling light-headed or short of breath, rapid heart rate, trouble concentrating;

severe or ongoing diarrhea;

trouble breathing;

feeling very thirsty or hot, being unable to urinate, heavy sweating, or hot and dry skin;

swelling or rapid weight gain; or

blood in your urine, pain or burning when you urinate.

Less serious side effects may include:

nausea, vomiting, stomach pain;

constipation, mild diarrhea;

weakness, tired feeling;

joint pain, back pain;

numbness, burning pain, or tingly feeling en your hands or feet;

changes in your sense of taste; or

hair loss.

This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

Cabazitaxel Dosing Information

Usual Adult Dose for Prostate Cancer:

Initial dose: 25 mg/m2 IV every 3 weeks in combination with prednisone 10 mg orally once daily.

What other drugs will affect cabazitaxel?

Many drugs can interact with cabazitaxel. Below is just a partial list. Tell your doctor if you are using:

conivaptan (Vaprisol);

imatinib (Gleevec);

isoniazid (for treating tuberculosis);

aprepitant (Emend);

cimetidine (Tagamet);

cyclosporine (Gengraf, Neoral, Sandimmune);

haloperidol (Haldol);

lidocaine (Xylocaine);

an antibiotic such as clarithromycin (Biaxin), dalfopristin/quinupristin (Synercid), doxycycline (Adoxa, Alodox, Avidoxy, Oraxyl, Doryx, Oracea, Vibramycin), erythromycin (E.E.S., EryPed, Ery-Tab, Erythrocin), metronidazole (Flagyl), norfloxacin (Noroxin), telithromycin (Ketek), or tetracycline (Ala-Tet, Brodspec, Panmycin, Sumycin, Tetracap);

antifungal medication such as clotrimazole (Mycelex Troche), fluconazole (Diflucan), itraconazole (Sporanox), ketoconazole (Extina, Ketozole, Nizoral, Xolegal), or voriconazole (Vfend);

an antidepressant such as nefazodone, desipramine (Norpramin), or sertraline (Zoloft);

heart or blood pressure medication such as amiodarone (Cordarone, Pacerone), diltiazem (Cartia, Cardizem), felodipine (Plendil), nifedipine (Nifedical, Procardia), verapamil (Calan, Covera, Isoptin, Verelan), and others; or

HIV/AIDS medicine such as atazanavir (Reyataz), delavirdine (Rescriptor), efavirenz (Sustiva), fosamprenavir (Lexiva), indinavir (Crixivan), nelfinavir (Viracept), saquinavir (Invirase), or ritonavir (Norvir).

This list is not complete and there are many other drugs that can interact with cabazitaxel. Tell your doctor about all medications you use. This includes prescription, over-the-counter, vitamin, and herbal products. Do not start a new medication without telling your doctor. Keep a list of all your medicines and show it to any healthcare provider who treats you.

More cabazitaxel resources

Cabazitaxel Side Effects (in more detail)
Cabazitaxel Dosage
Cabazitaxel Use in Pregnancy & Breastfeeding
Cabazitaxel Drug Interactions
Cabazitaxel Support Group
0 Reviews for Cabazitaxel - Add your own review/rating

cabazitaxel Intravenous Advanced Consumer (Micromedex) - Includes Dosage Information

Cabazitaxel Professional Patient Advice (Wolters Kluwer)

Cabazitaxel MedFacts Consumer Leaflet (Wolters Kluwer)

Cabazitaxel Monograph (AHFS DI)

Jevtana Prescribing Information (FDA)

Jevtana Consumer Overview

Compare cabazitaxel with other medications

Prostate Cancer

Where can I get more information?

Your doctor or pharmacist can provide more information about cabazitaxel.

See also: cabazitaxel side effects (in more detail)

Migraine Medications

Definition of Migraine:

Migraine headaches are a type of headache that some people get repeatedly over time. Migraines are different from other headaches because they occur with symptoms such as nausea, vomiting, or sensitivity to light.

Some people who get migraines have warning symptoms, called an aura, before the actual headache begins. Most people, however, do not have such warning symptoms.

Drugs associated with Migraine

The following drugs and medications are in some way related to, or used in the treatment of Migraine. This service should be used as a supplement to, and NOT a substitute for, the expertise, skill, knowledge and judgment of healthcare practitioners.

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