pharmacopeia
GET
/api/v1/drug/bisoprolol
2D structure
1-(propan-2-ylamino)-3-[4-(2-propan-2-yloxyethoxymethyl)phenoxy]propan-2-ol
SMILES CC(C)NCC(COC1=CC=C(C=C1)COCCOC(C)C)O
InChIKey VHYCDWMUTMEGQY-UHFFFAOYSA-N

Mechanism of action

Sourced from openFDA

Mechanism-of-action classes: Adrenergic beta-Antagonists; Adrenergic beta1-Antagonists.

Indications

Sourced from openFDA
  • Bisoprolol fumarate tablets are indicated in the management of hypertension. It may be used alone or in combination with other antihypertensive agents.ICD-10: I10

Contraindications

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

Dosage & administration

Sourced from openFDA

The dose of bisoprolol fumarate tablets 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 tablets.

Warnings & precautions

Sourced from openFDA

Click here to enter 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 tablets 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 tablets over approximately one week with the patient under careful observation. If withdrawal symptoms occur, bisoprolol fumarate tablets therapy should be reinstituted, at least temporarily.

Adverse reactions

Sourced from openFDA

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 5-20 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 (2.5-40 mg), as well as for a subgroup that was treated with doses within the recommended dosage range (5-20 mg). Of the adverse events listed in the table, bradycardia, diarrhea, asthenia, fatigue, and sinusitis appear to be dose related.

Use in specific populations

Sourced from openFDA

Pregnancy 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 tablets should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.

Overdosage

Sourced from openFDA

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 tablets 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.

Approval history

Sourced from openFDA
  • Mar 26, 1993NDANDA020186Teva Branded Pharm
  • Sep 25, 2000ANDAANDA075768Mylan
  • Nov 16, 2000ANDAANDA075643Rubicon Research
  • Oct 25, 2002ANDAANDA075474Tp Anda Holdings
  • Dec 14, 2005ANDAANDA075831Natco Pharma Usa
  • Dec 27, 2006ANDAANDA077910Aurobindo Pharma
  • Aug 18, 2009ANDAANDA078635Unichem
  • Jul 28, 2010ANDAANDA079106Unichem

FAERS reports

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Reference statistics only. FAERS reports are voluntarily submitted and are not incidence rates, safety signals, or causal evidence. Counts reflect reporting volume — how often a reaction was reported, not how often it occurs. For decision-grade use, consult openFDA and the FAERS Public Dashboard directly.
0 total reports matchedShare = reports listing the reaction ÷ total matched reports. Rows can sum to >100% because a single report often lists multiple reactions.
  1. 1Dyspnoea9,034—
  2. 2Acute Kidney Injury7,006—
  3. 3Fatigue7,003—
  4. 4Diarrhoea6,470—
  5. 5Nausea6,298—
  6. 6Dizziness6,104—
  7. 7Drug Interaction5,707—
  8. 8Off Label Use5,553—
  9. 9Hypotension5,351—
  10. 10Fall5,289—
  11. 11Vomiting4,916—
  12. 12Malaise4,797—
  13. 13Asthenia4,774—
  14. 14Drug Ineffective4,695—
  15. 15Headache4,374—

Literature

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Recent PubMed references pinned to Bisoprolol as a MeSH major topic. Citations link to pubmed.ncbi.nlm.nih.gov.

Clinical trials

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The 10 most recently updated of 141 ClinicalTrials.gov registrations naming Bisoprolol as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

Pharmacogenomics

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CPIC-curated drug–gene pairs for Bisoprolol. Levels describe the strength of curated evidence and guideline status — never a recommendation to test or to adjust therapy.

Structural analogs

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Ranked by 2D fingerprint (Tanimoto) similarity over PubChem structures. Structural proximity only — not a claim of therapeutic equivalence.

Frequently asked questions

How does Bisoprolol work?
Mechanism-of-action classes: Adrenergic beta-Antagonists; Adrenergic beta1-Antagonists.
What is Bisoprolol used for?
According to FDA labeling, Bisoprolol carries indications including: Bisoprolol fumarate tablets are indicated in the management of hypertension. It may be used alone or in combination with other antihypertensive agents.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.
What class of drug is Bisoprolol?
Bisoprolol is classified as Beta blocking agents, selective, beta-Adrenergic Blocker, Adrenergic beta-Antagonists, Adrenergic beta1-Antagonists, Decreased Blood Pressure, Negative Chronotropy, Negative Inotropy.
What are the brand names for Bisoprolol?
Bisoprolol is marketed under brand names including Ziac.
What are the contraindications for Bisoprolol?
Bisoprolol labeling lists contraindications including: Bisoprolol fumarate tablets are contraindicated in patients with cardiogenic shock, overt cardiac failure, second or third degree AV block, and marked sinus bradycardia.. Always consult the full prescribing information and a clinician.
Note. Data for bisoprolol is illustrative MVP content compiled from public sources. pharmacopeia is for educational and informational use only and is not a substitute for professional medical advice.

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