Medicine guide

Bisoprolol Fumarate

5 mg · Tablet, Film Coated

  • Prescription only
  • beta-Adrenergic Blocker
Active substance
Bisoprolol Fumarate
Made by
AvPAK

Quoted from the official source. Not yet reviewed by Mediclarum — the leaflet in your pack is authoritative.

At a glance

Quoted from the official label · 2024-01-09

What it is

beta-Adrenergic Blocker

Used for
  • Bisoprolol fumarate tablets are indicated in the management of hypertension. They may be used alone or in combination with other antihypertensive agents.
The label’s usual adult dose

The usual starting dose is 5 mg once daily.

Full directions ↓
Do not take it if

Bisoprolol fumarate tablets are contraindicated in patients with cardiogenic shock, overt cardiac failure, second or third degree AV block, and marked sinus bradycardia.

All warnings ↓
Good to know
  • Prescription only
  • FDA enforcement reports list no ongoing recall, and none from the last two years, for this product code · checked 2026-10-02
46other products contain Bisoprolol Fumarate — compare makers, forms and strengths

Every line above is selected, not written, from the official label. Nothing is reworded. DailyMed

What it is for

  • Bisoprolol fumarate tablets are indicated in the management of hypertension. They may be used alone or in combination with other antihypertensive agents.

From the official label · 2024-01-09 · DailyMed

How it works

From this product’s own US prescribing label.

Bisoprolol fumarate is a beta 1 -selective (cardioselective) adrenoceptor blocking agent without significant membrane stabilizing activity or intrinsic sympathomimetic activity in its therapeutic dosage range.

Cardioselectivity is not absolute, however, and at higher doses (≥20 mg) bisoprolol fumarate also inhibits beta 2 -adrenoceptors, chiefly located in the bronchial and vascular musculature; to retain selectivity it is therefore important to use the lowest effective dose.

Peak level after2–4 h
Half-life9–12 h
Mostly cleared after≈ 2 daysfive half-lives — our arithmetic
PeakHalf gone2 days0
The shape is a standard model drawn from the two times above, not a measurement. How fast a medicine acts and wears off also depends on the dose, the form and the person.
How the body breaks it down

Bisoprolol fumarate is not metabolized by cytochrome P450 II D6 (debrisoquin hydroxylase).

How it leaves the body

Bisoprolol fumarate is eliminated equally by renal and non-renal pathways with about 50% of the dose appearing unchanged in the urine and the remainder appearing in the form of inactive metabolites.

With food

Absorption is not affected by the presence of food.

Quoted from the prescribing label, sections “Mechanism of Action” and “Pharmacokinetics”. DailyMed · 2024-01-09

Do not take it if

Bisoprolol fumarate tablets are contraindicated in patients with cardiogenic shock, overt cardiac failure, second or third degree AV block, and marked sinus bradycardia.

Quoted from the official label, section “Contraindications”.

How to take it

These directions are for this exact strength and form. Another one is different.

  • The dose of bisoprolol fumarate must be individualized to the needs of the patient.
  • The usual starting dose is 5 mg once daily.
  • In some patients, 2.5 mg may be an appropriate starting dose (see Bronchospastic Disease in WARNINGS ).
  • If the antihypertensive effect of 5 mg is inadequate, the dose may be increased to 10 mg and then, if necessary, to 20 mg once daily.
  • Patients with Renal or Hepatic Impairment In patients with hepatic impairment (hepatitis or cirrhosis) or renal dysfunction (creatinine clearance less than 40 mL/min), the initial daily dose should be 2.5 mg and caution should be used in dose-titration.
  • Since limited data suggest that bisoprolol fumarate is not dialyzable, drug replacement is not necessary in patients undergoing dialysis.
  • Geriatric Patients It is not necessary to adjust the dose in the elderly, unless there is also significant renal or hepatic dysfunction (see above and Geriatric Use in PRECAUTIONS ).
  • Pediatric Patients There is no pediatric experience with bisoprolol fumarate.

Quoted from the official label, section “Dosage & Administration”.

Other warnings

  • Cardiac Failure Sympathetic stimulation is a vital component supporting circulatory function in the setting of congestive heart failure, and beta-blockade may result in further depression of myocardial contractility and precipitate more severe failure.
  • In general, beta-blocking agents should be avoided in patients with overt congestive failure.
  • However, in some patients with compensated cardiac failure it may be necessary to utilize them.
  • In such a situation, they must be used cautiously.
  • In Patients Without a History of Cardiac Failure Continued depression of the myocardium with beta-blockers can, in some patients, precipitate cardiac failure.
  • At the first signs or symptoms of heart failure, discontinuation of bisoprolol fumarate should be considered.
  • In some cases, beta-blocker therapy can be continued while heart failure is treated with other drugs.
  • Abrupt Cessation of Therapy Exacerbation of angina pectoris, and, in some instances, myocardial infarction or ventricular arrhythmia, have been observed in patients with coronary artery disease following abrupt cessation of therapy with beta-blockers.
  • Such patients should, therefore, be cautioned against interruption or discontinuation of therapy without the physician‘s advice.
  • Even in patients without overt coronary artery disease, it may be advisable to taper therapy with bisoprolol fumarate over approximately one week with the patient under careful observation.
  • If withdrawal symptoms occur, bisoprolol fumarate therapy should be reinstituted, at least temporarily.
  • Peripheral Vascular Disease Beta-blockers can precipitate or aggravate symptoms of arterial insufficiency in patients with peripheral vascular disease.
  • Caution should be exercised in such individuals.
  • Bronchospastic Disease PATIENTS WITH BRONCHOSPASTIC DISEASE SHOULD, IN GENERAL, NOT RECEIVE BETA-BLOCKERS.
  • Because of its relative beta 1 -selectivity, however, bisoprolol fumarate may be used with caution in patients with bronchospastic disease who do not respond to, or who cannot tolerate other antihypertensive treatment.
  • Since beta 1 -selectivity is not absolute, the lowest possible dose of bisoprolol fumarate should be used, with therapy starting at 2.5 mg.
  • A beta 2 agonist (bronchodilator) should be made available.
  • 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-blockers may mask some of the manifestations of hypoglycemia, particularly tachycardia.
  • Nonselective beta-blockers may potentiate insulin-induced hypoglycemia and delay recovery of serum glucose levels.
  • Because of its beta 1 -selectivity, this is less likely with bisoprolol fumarate.
  • However, patients subject to spontaneous hypoglycemia, or diabetic patients receiving insulin or oral hypoglycemic agents, should be cautioned about these possibilities and bisoprolol fumarate should be used with caution.
  • Thyrotoxicosis Beta-adrenergic blockade may mask clinical signs of hyperthyroidism, such as tachycardia.
  • Abrupt withdrawal of beta-blockade may be followed by an exacerbation of the symptoms of hyperthyroidism or may precipitate thyroid storm.
  • Impaired Renal or Hepatic Function Use caution in adjusting the dose of bisoprolol fumarate in patients with renal or hepatic impairment (see CLINICAL PHARMACOLOGY and DOSAGE AND ADMINISTRATION ).
  • Drug Interactions Bisoprolol fumarate should not be combined with other beta-blocking agents.
  • Patients receiving catecholamine-depleting drugs, such as reserpine or guanethidine, should be closely monitored, because the added beta-adrenergic blocking action of bisoprolol fumarate may produce excessive reduction of sympathetic activity.
  • In patients receiving concurrent therapy with clonidine, if therapy is to be discontinued, it is suggested that bisoprolol fumarate be discontinued for several days before the withdrawal of clonidine.
  • Bisoprolol fumarate should be used with care when myocardial depressants or inhibitors of AV conduction, such as certain calcium antagonists (particularly of the phenylalkylamine [verapamil] and benzothiazepine [diltiazem] classes), or antiarrhythmic agents, such as disopyramide, are used concurrently.
  • Both digitalis glycosides and beta-blockers slow atrioventricular conduction and decrease heart rate.
  • Concomitant use can increase the risk of bradycardia.
  • Concurrent use of rifampin increases the metabolic clearance of bisoprolol fumarate, resulting in a shortened elimination half-life of bisoprolol fumarate.
  • However, initial dose modification is generally not necessary.
  • Pharmacokinetic studies document no clinically relevant interactions with other agents given concomitantly, including thiazide diuretics and cimetidine.
  • There was no effect of bisoprolol fumarate on prothrombin time in patients on stable doses of warfarin.
  • Risk of Anaphylactic Reaction:
  • 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 reactions.
  • Information for Patients Patients, especially those with coronary artery disease, should be warned about discontinuing use of bisoprolol fumarate without a physician‘s supervision.
  • Carcinogenesis, Mutagenesis, Impairment of Fertility Long-term studies were conducted with oral bisoprolol fumarate administered in the feed of mice (20 and 24 months) and rats (26 months).
  • No evidence of carcinogenic potential was seen in mice dosed up to 250 mg/kg/day or rats dosed up to 125 mg/kg/day.
  • On a body weight basis, these doses are 625 and 312 times, respectively, the maximum recommended human dose (MRHD) of 20 mg, (or 0.4 mg/kg/day based on a 50 kg individual); on a body surface area basis, these doses are 59 times (mice) and 64 times (rats) the MRHD.
  • The mutagenic potential of bisoprolol fumarate was evaluated in the microbial mutagenicity (Ames) test, the point mutation and chromosome aberration assays in Chinese hamster V79 cells, the unscheduled DNA synthesis test, the micronucleus test in mice, and the cytogenetics assay in rats.
  • There was no evidence of mutagenic potential in these in vitro and in vivo assays.
  • Reproduction studies in rats did not show any impairment of fertility at doses up to 150 mg/kg/day of bisoprolol fumarate, or 375 and 77 times the MRHD on the basis of body weight and body surface area, respectively.
  • Pregnancy Category C In rats, bisoprolol fumarate was not teratogenic at doses up to 150 mg/kg/day which is 375 and 77 times the MRHD on the basis of body weight and body surface area, respectively.
  • Nursing Mothers Small amounts of bisoprolol fumarate (<2% of the dose) have been detected in the milk of lactating rats.
  • Pediatric Use Safety and effectiveness in pediatric patients have not been established.
  • Geriatric Use Bisoprolol fumarate has been used in elderly patients with hypertension.

Quoted from the official label, section “Warnings”.

Pregnancy and breastfeeding

  • Category C In rats, bisoprolol fumarate was not teratogenic at doses up to 150 mg/kg/day which is 375 and 77 times the MRHD on the basis of body weight and body surface area, respectively.
  • Bisoprolol fumarate was fetotoxic (increased late resorptions) at 50 mg/kg/day and maternotoxic (decreased food intake and body weight gain) at 150 mg/kg/day.
  • The fetotoxicity in rats occurred at 125 times the MRHD on a body weight basis and 26 times the MRHD on the basis of body surface area.
  • The maternotoxicity occurred at 375 times the MRHD on a body weight basis and 77 times the MRHD on the basis of body surface area.
  • In rabbits, bisoprolol fumarate was not teratogenic at doses up to 12.5 mg/kg/day, which is 31 and 12 times the MRHD based on body weight and body surface area, respectively, but was embryolethal (increased early resorptions) at 12.5 mg/kg/day.
  • There are no adequate and well-controlled studies in pregnant women.
  • Bisoprolol fumarate should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.
  • Small amounts of bisoprolol fumarate (<2% of the dose) have been detected in the milk of lactating rats.
  • It is not known whether this drug is excreted in human milk.
  • Because many drugs are excreted in human milk caution should be exercised when bisoprolol fumarate is administered to nursing women.

Quoted from the official label, section “OTC — Pregnancy or Breast Feeding”.

If you take too much

In an emergency, call your local emergency number or a poison control centre.

  • The most common signs expected with overdosage of a beta-blocker are bradycardia, hypotension, congestive heart failure, bronchospasm, and hypoglycemia.
  • To date, a few cases of overdose (maximum:
  • 2000 mg) with bisoprolol fumarate have been reported.
  • Bradycardia and/or hypotension were noted.
  • Sympathomimetic agents were given in some cases, and all patients recovered.
  • In general, if overdose occurs, bisoprolol fumarate therapy should be stopped and supportive and symptomatic treatment should be provided.
  • Limited data suggest that bisoprolol fumarate is not dialyzable.
  • Based on the expected pharmacologic actions and recommendations for other beta-blockers, the following general measures should be considered when clinically warranted:
  • Bradycardia Administer IV atropine.
  • If the response is inadequate, isoproterenol or another agent with positive chronotropic properties may be given cautiously.
  • Under some circumstances, transvenous pacemaker insertion may be necessary.
  • Hypotension IV fluids and vasopressors should be administered.
  • Intravenous glucagon may be useful.
  • Heart Block (second or third degree) Patients should be carefully monitored and treated with isoproterenol infusion or transvenous cardiac pacemaker insertion, as appropriate.
  • Congestive Heart Failure Initiate conventional therapy (i.e., digitalis, diuretics, inotropic agents, vasodilating agents).
  • Bronchospasm Administer bronchodilator therapy such as isoproterenol and/or aminophylline.
  • Hypoglycemia Administer IV glucose.

Quoted from the official label, section “Overdosage”.

Use in children

Safety and effectiveness in pediatric patients have not been established.

Quoted from the official label, section “Pediatric Use”.

Use in older people

  • Bisoprolol fumarate has been used in elderly patients with hypertension.
  • Response rates and mean decreases in systolic and diastolic blood pressure were similar to the decreases in younger patients in the U.S. clinical studies.
  • Although no dose response study was conducted in elderly patients, there was a tendency for older patients to be maintained on higher doses of bisoprolol fumarate.
  • Observed reductions in heart rate were slightly greater in the elderly than in the young and tended to increase with increasing dose.
  • In general, no disparity in adverse experience reports or dropouts for safety reasons was observed between older and younger patients.
  • Dose adjustment based on age is not necessary.

Quoted from the official label, section “Geriatric Use”.

Side effects

  • Safety data are available in more than 30,000 patients or volunteers.
  • Frequency estimates and rates of withdrawal of therapy for adverse events were derived from two U.S. placebo-controlled studies.
  • In Study A, doses of 5, 10, and 20 mg bisoprolol fumarate were administered for 4 weeks.
  • In Study B, doses of 2.5, 10, and 40 mg of bisoprolol fumarate were administered for 12 weeks.
  • A total of 273 patients were treated with 5 to 20 mg of bisoprolol fumarate; 132 received placebo.
  • Withdrawal of therapy for adverse events was 3.3% for patients receiving bisoprolol fumarate and 6.8% for patients on placebo.
  • Withdrawals were less than 1% for either bradycardia or fatigue/lack of energy.
  • The following table presents adverse experiences, whether or not considered drug related, reported in at least 1% of patients in these studies, for all patients studied in placebo-controlled clinical trials (2.5 to 40 mg), as well as for a subgroup that was treated with doses within the recommended dosage range (5 to 20 mg).
  • Of the adverse events listed in the table, bradycardia, diarrhea, asthenia, fatigue, and sinusitis appear to be dose related.
  • Body System/Adverse Experience All Adverse Experiences (% a ) Bisoprolol Fumarate Placebo (n=132) % 5 to 20 mg (n=273) % 2.5 to 40 mg (n=404) % a percentage of patients with event Skin increased sweating 1.5 0.7 1 Musculoskeletal arthralgia 2.3 2.2
  • 2.7 Central Nervous System dizziness 3.8 2.9 3.5 headache 11.4 8.8 10.9 hypoaesthesia 0.8 1.1
  • 1.5 Autonomic Nervous System dry mouth 1.5 0.7
  • 1.3 Heart Rate/Rhythm bradycardia 0 0.4
  • 0.5 Psychiatric vivid dreams 0 0 0 insomnia 2.3 1.5 2.5 depression 0.8 0
  • 0.2 Gastrointestinal diarrhea 1.5 2.6 3.5 nausea 1.5 1.5 2.2 vomiting 0 1.1
  • 1.5 Respiratory bronchospasm 0 0 0 cough 4.5 2.6 2.5 dyspnea 0.8 1.1 1.5 pharyngitis 2.3 2.2 2.2 rhinitis 3 2.9 4 sinusitis 1.5 2.2
  • 2.2 URI 3.8 4.8 5 Body as a Whole asthenia 0 0.4 1.5 chest pain 0.8 1.1 1.5 fatigue 1.5 6.6 8.2 edema (peripheral) 3.8 3.7 3 The following is a comprehensive list of adverse experiences reported with bisoprolol fumarate in worldwide studies, or in postmarketing experience (in italics):
  • Central Nervous System Dizziness, unsteadiness , vertigo, syncope , headache, paresthesia, hypoaesthesia, hyperesthesia, somnolence, sleep disturbances , anxiety/restlessness, decreased concentration/memory.
  • Autonomic Nervous System Dry mouth.
  • Cardiovascular Bradycardia, palpitations and other rhythm disturbances, cold extremities, claudication, hypotension, orthostatic hypotension, chest pain, congestive heart failure, dyspnea on exertion.
  • Psychiatric Vivid dreams, insomnia, depression.
  • Gastrointestinal Gastric/epigastric/abdominal pain, gastritis, dyspepsia, nausea, vomiting, diarrhea, constipation, peptic ulcer.
  • Musculoskeletal Muscle/joint pain, arthralgia , back/neck pain, muscle cramps, twitching/tremor.
  • Skin Rash, acne, eczema, psoriasis , skin irritation, pruritus, flushing, sweating, alopecia, dermatitis , angioedema, exfoliative dermatitis, cutaneous vasculitis.
  • Special Senses Visual disturbances, ocular pain/pressure, abnormal lacrimation, tinnitus, decreased hearing , earache, taste abnormalities.
  • Metabolic Gout.
  • Respiratory Asthma/bronchospasm, bronchitis, coughing, dyspnea, pharyngitis, rhinitis, sinusitis, URI.
  • Genitourinary Decreased libido/impotence, Peyronie‘s disease, cystitis, renal colic, polyuria.
  • Hematologic Purpura.
  • General Fatigue, asthenia, chest pain, malaise, edema, weight gain, angioedema.
  • In addition, a variety of adverse effects have been reported with other beta-adrenergic blocking agents and should be considered potential adverse effects of bisoprolol fumarate:
  • Central Nervous System Reversible mental depression progressing to catatonia, hallucinations, an acute reversible syndrome characterized by disorientation to time and place, emotional lability, slightly clouded sensorium.
  • Allergic Fever, combined with aching and sore throat, laryngospasm, respiratory distress.
  • Hematologic Agranulocytosis, thrombocytopenia, thrombocytopenic purpura.
  • Gastrointestinal Mesenteric arterial thrombosis, ischemic colitis.
  • Miscellaneous The oculomucocutaneous syndrome associated with the beta-blocker practolol has not been reported with bisoprolol fumarate during investigational use or extensive foreign marketing experience.
  • LABORATORY ABNORMALITIES In clinical trials, the most frequently reported laboratory change was an increase in serum triglycerides, but this was not a consistent finding.
  • Sporadic liver test abnormalities have been reported.
  • In the U.S. controlled trials experience with bisoprolol fumarate treatment for 4 to 12 weeks, the incidence of concomitant elevations in SGOT and SGPT from 1 to 2 times normal was 3.9%, compared to 2.5% for placebo.
  • No patient had concomitant elevations greater than twice normal.
  • In the long-term, uncontrolled experience with bisoprolol fumarate treatment for 6 to 18 months, the incidence of one or more concomitant elevations in SGOT and SGPT from 1 to 2 times normal was 6.2%.
  • The incidence of multiple occurrences was 1.9%.
  • For concomitant elevations in SGOT and SGPT of greater than twice normal, the incidence was 1.5%.
  • The incidence of multiple occurrences was 0.3%.
  • In many cases these elevations were attributed to underlying disorders, or resolved during continued treatment with bisoprolol fumarate.
  • Other laboratory changes included small increases in uric acid, creatinine, BUN, serum potassium, glucose, and phosphorus and decreases in WBC and platelets.
  • These were generally not of clinical importance and rarely resulted in discontinuation of bisoprolol fumarate.
  • As with other beta-blockers, ANA conversions have also been reported on bisoprolol fumarate.
  • About 15% of patients in long-term studies converted to a positive titer, although about one-third of these patients subsequently reconverted to a negative titer while on continued therapy.
  • To report SUSPECTED ADVERSE REACTIONS contact AvKARE at 1-855-361-3993; email drugsafety@avkare.com; or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch.

Quoted from the official label, section “Adverse Reactions”.

What to discuss with your doctor

  • Patients, especially those with coronary artery disease, should be warned about discontinuing use of bisoprolol fumarate without a physician‘s supervision.
  • Patients should also be advised to consult a physician if any difficulty in breathing occurs, or if they develop signs or symptoms of congestive heart failure or excessive bradycardia.
  • Patients subject to spontaneous hypoglycemia, or diabetic patients receiving insulin or oral hypoglycemic agents, should be cautioned that beta-blockers may mask some of the manifestations of hypoglycemia, particularly tachycardia, and bisoprolol fumarate should be used with caution.
  • Patients should know how they react to this medicine before they operate automobiles and machinery or engage in other tasks requiring alertness.

Quoted from the official label, section “Patient Counseling Information”.

What it looks like and how it is packed

  • Bisoprolol fumarate is supplied as 5 mg and 10 mg tablets.
  • Bisoprolol Fumarate Tablets, USP 5 mg are pink colored, circular, biconvex, film coated tablets, debossed with ‘C and break line’ on one side and ‘86’ on the other side.
  • NDC 50268-127-15 (10 tablets per card, 5 cards per carton) Bisoprolol Fumarate Tablets, USP 10 mg are white, circular, biconvex, film coated tablets, debossed with ‘C’ on one side and ‘87’ on the other side.
  • 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 and moisture.
  • Dispensed in Unit Dose Packaging.
  • For Institutional Use Only.
  • Manufactured for: AvKARE Pulaski, TN 38478 Mfg.
  • Rev. 10/21 AV 11/21 (P) AvPAK

Quoted from the official label, section “How Supplied”.

What is in it

  • Bisoprolol fumarate is a synthetic, beta 1 -selective (cardioselective) adrenoceptor blocking agent. The chemical name for bisoprolol fumarate is (±)-1-[4-[[2-(1-Methylethoxy)ethoxy]methyl]phenoxy]-3-[(1-methylethyl)amino]-2-propanol( E )-2-butenedioate (2:1) (salt). It possesses an asymmetric carbon atom in its structure and is provided as a racemic mixture. The S(-) enantiomer is responsible for most of the beta-blocking activity. Its molecular formula is (C 18 H 31 NO 4 ) 2
  • C 4 H 4 O 4 and its structure is:
  • Bisoprolol fumarate has a molecular weight of 766.97. It is a white crystalline powder which is approximately equally hydrophilic and lipophilic, and is readily soluble in water, methanol, ethanol, and chloroform. Bisoprolol fumarate is available as 5 and 10 mg tablets for oral administration. Inactive ingredients include microcrystalline cellulose, anhydrous dibasic calcium phosphate, crospovidone, colloidal silicon dioxide, magnesium stearate, hypromellose, polyethylene glycol, polysorbate 80, and titanium dioxide. The 5 mg tablets also contain red and yellow iron oxide. chemical structure

Quoted from the official label, section “Description”.

Ingredients people check for

Lactose, gluten, dyes, sugars and other ingredients that matter with an allergy, intolerance or diet — as this product’s FDA label lists them.

  • Titanium dioxidetitanium dioxideA whitening agent no longer allowed in food in the EU (E171).

Quoted from the FDA label. A label that does not name an ingredient is not a guarantee that the product is free of it, and formulations change. With an allergy, check the pack and ask a pharmacist.

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Details

Made byAvPAK
Active substanceBisoprolol Fumarate
Used inHeart, blood pressure and circulation
Strength5 mg
FormTablet, Film Coated
RouteOral
Packs50 BLISTER PACK in 1 BOX / 1 TABLET, FILM COATED in 1 BLISTER PACK
NDC50268-127

Source: NDC Directory · 2026-09-13 · not reviewed by a clinician

Source: US Food and Drug Administration, NDC Directory. Reuse terms: US government work (FDA).

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