Generic Name

Carvedilol

Mechanism

• Carvedilol is a non‑selective β‑adrenergic antagonist (β1/β2) with α1‑adrenergic blockade.
• It reduces cardiac output by dampening sympathetic stimulation of β receptors while lowering peripheral resistance through α1 blockade, leading to vasodilation.
• The dual action translates into decreased heart rate, reduced myocardial oxygen demand, and improved coronary perfusion.
• Additionally, carvedilol exhibits antioxidant activity by scavenging free radicals, which contributes to its cardioprotective effects post‑myocardial infarction.

Pharmacokinetics

Indications

• Heart failure (HF) – chronic, symptomatic HF (NYHA II–IV) to improve mortality and functional capacity.
• Hypertension – adjunct therapy or monotherapy in patients with uncontrolled BP.
• Post‑myocardial infarction (MI) – first‑line to reduce adverse remodeling and decrease sudden cardiac death risk.
• Stable angina – improves exercise tolerance (used less frequently due to β2 blockade).

Contraindications

• Absolute Contraindications
• Severe bradycardia (HR < 45 bpm).
• Second or third‑degree AV block without pacemaker.
• Systolic HF with EF < 20 % (unless under strict monitoring).
• New‑onset uncontrolled hypotension.
• Relative
• Asthma or severe COPD (β2 blockade may precipitate bronchospasm).
• Severe peripheral vascular disease (α1 blockade can aggravate symptoms).
• Uncontrolled diabetes (blunted hypoglycaemic recognition).
• Warnings
• Renal or hepatic impairment → dose adjustment and close monitoring.
• Concurrent use with other antihypertensives may cause additive hypotension.

Dosing

• Administer with food → ↑ bioavailability.
• For rapid titration, split the daily dose (morning/afternoon).
• Special populations: In patients with hepatic dysfunction, start at 1.56 mg BID and titrate cautiously.

Adverse Effects

• Common (≥ 10 % incidence)
• Fatigue, dizziness, post‑ural hypotension.
• Sleep disturbances (insomnia, vivid dreams).
• Headache, mild hypotension.
• Mild skin rashes.
• Serious (≤ 1 % incidence)
• Severe bradycardia, AV block.
• Hypotension leading to syncope.
• Fluid retention, worsening pulmonary edema (rare).
• Allergic reactions (rash, angioedema).
• Monitoring‑Related AEs
• Hypoglycaemia unawareness in diabetics.
• Masking of tachycardia post‑MI.

Monitoring

• Baseline: BP, HR, ECG (QRS, QTc), CBC, electrolytes, renal/ hepatic panel.
• During titration:
• BP and HR weekly for first 4 weeks, then monthly.
• ECG at 4 weeks and if symptomatic.
• Chronic:
• Monthly BP/HR until stable (6 months).
• Annual renal panel, liver function tests.
• HbA1c and fasting glucose if diabetic.
• Adverse event surveillance:
• Report any syncope, dizziness, or new dyspnea.

Clinical Pearls

1. Early‑onset β1 blockade may unmask latent conduction disease; baseline ECG is essential.

2. Carvedilol’s α1‑activity gives it a distinct advantage over cardio‑selective β1 blockers in reducing afterload, making it the preferred agent for HFrEF.

3. Non‑oral dosing: 30 min to 1 h after breakfast improves absorption; avoid with high‑fat meals.

4. CYP2D6 poor metabolizers may experience higher plasma concentrations; consider dose reduction or therapeutic drug monitoring.

5. Bronchodilatory support: In patients with reactive airway disease, co‑prescribe short‑acting β2 agonists; monitor for paradoxical bronchoconstriction.

6. Post‑MI windows: Initiate carvedilol 1–3 days after reperfusion; evidence shows benefit only if started early.

7. Fluid overload caution: Despite β‑blocker benefits, carvedilol can mask worsening pulmonary congestion; integrate diuretics and diuretic‑response monitoring.

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• Key Terms: Carvedilol, β‑blocker, α1‑blocker, heart failure, post‑MI, pharmacokinetics, CYP2D6.

Reference-friendly: Use PubMed and UpToDate for latest evidence on dosing and safety.