Carvedilol

byAbdelwahab Ward, BS Pharm, PharmD - last updated
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Editor: Abdelwahab Ward, PharmD.
This topic was published in Sep 16, 2020.

Pharmacology

  • Drug Classes
    1. Alpha- and beta-adrenergic blocker
    2. Antihypertensive
  • Therapeutic Actions
    • Competitively blocks alpha-, beta-, and beta2-adrenergic receptors and has some sympathomimetic activity at beta2-receptors. Both alpha- and beta-blocking actions contribute to the BP-lowering effect; beta blockade prevents the reflex tachycardia seen with most alpha-blocking drugs and decreases plasma renin activity. Significantly reduces plasma renin activity.
  • Tade name: Dilatrend, Carvid, Dilatrol 
  • Available Forms
    • Tablets — 3.125, 6.25, 12.5, 25 mg 
  • Pregnancy category: C

Indications

  • Hypertension, alone or with other oral drugs, especially diuretics
  • Treatment of mild to severe heart failure of ischemic or cardiomyopathic origin with digitalis, diuretics, ACE inhibitors
  • Left ventricular dysfunction (LVD) after MI
  • Unlabeled uses: Angina (25–50 mg bid), hiccups, idiopathic cardiomyopathy

Contraindications

  1. Contraindicated with decompensated heart failure, bronchial asthma, heart block, cardiogenic shock, hypersensitivity to carvedilol, pregnancy, lactation.
  2. Use cautiously with hepatic impairment, peripheral vascular disease, thyrotoxicosis, diabetes, anesthesia, major surgery.

Doses

  • Adults
    • Hypertension: 6.25 mg PO bid; maintain for 7–14 days, then increase to 12.5 mg PO bid if needed to control BP. Do not exceed 50 mg/day.
    • Heart failure: Monitor patient very closely, individualize dose based on patient response. Initial dose, 3.125 mg PO bid for 2 wk, may then be increased to 6.25 mg PO bid. Do not increase doses at intervals shorter than 2 wk. Maximum dose, 25 mg PO bid in patients weighing less than 85 kg or 50 mg PO bid in patients weighing more than 85 kg.
    • LVD following MI: 6.25 mg PO bid; increase after 3–10 days to target dose of 25 mg bid.
  • Pediatric patients
    • Safety and efficacy not established.
  • Patients with hepatic impairment
    • Do not administer to any patient with severe hepatic impairment.

Pharmacokinetics

  • Route: Oral
  • Peak: 30 min
  • Duration: 8–10 hr
  • Metabolism: Hepatic; T1/2: 7–10 hr
  • Distribution: Crosses placenta; may enter breast milk
  • Excretion: Bile, feces

Adverse Effects

  1. CNS: Dizziness, vertigo, tinnitus, fatigue, emotional depression, paresthesias, sleep disturbances
  2. CV: Bradycardia, orthostatic hypertension, heart failure, cardiac arrhythmias, pulmonary edema, hypotension
  3. GI: Gastric pain, flatulence, constipation, diarrhea, hepatic failure
  4. Respiratory: Rhinitis, pharyngitis, dyspnea
  5. Other: Fatigue, back pain, infections

Interactions

  • Drug-drug 
    • Increased effectiveness of antidiabetics; monitor blood glucose and adjust dosages appropriately
    • Increased effectiveness of clonidine; monitor patient for potential severe bradycardia and hypotension
    • Increased serum levels of digoxin; monitor serum levels and adjust dosage accordingly
    • Increased plasma levels of carvedilol with rifampin
    • Potential for dangerous conduction system disturbances with verapamil or diltiazem; if this combination is used, closely monitor ECG and BP
  • Drug-food
    • Slowed rate of absorption but not decreased effectiveness with food

References

  1. Singh, S. and Preuss, C.V. (2020). Carvedilol. [online] PubMed. Available at: https://www.ncbi.nlm.nih.gov/books/NBK534868/
  2. Lexicomp, www.lexicomp.com 
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