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Management of hypertension
Treatment of stable angina pectoris
Moderate to severe chronic heart failure (as part of a comprehensive regimen)
Not recommended for emergency hypertensive crises.
(Use under registered physician’s guidance)
Highly selective β₁-adrenergic antagonist: Blocks cardiac β₁-receptors, reducing heart rate, cardiac output, and renin release.
Cardioprotective: Maintains HDL cholesterol levels without adverse lipid metabolism effects.
| Parameter | Profile |
|---|---|
| Absorption | >90% oral bioavailability; food does not affect absorption. |
| Distribution | Volume: 3.5 L/kg. Extensive tissue distribution. |
| Metabolism | Primarily hepatic (CYP3A4; minor CYP2D6). Metabolites inactive. |
| Elimination | Half-life: 10–12 hrs. Renal (50% unchanged) and hepatic (50%) elimination. |
| Dialysis | Not dialyzable. |
Hypertension/Angina: Start at 5 mg once daily. Titrate to 10 mg or 20 mg daily at 2-week intervals.
Heart Failure: Start at 1.25 mg daily; double dose every 2–4 weeks (max 10 mg/day).
*Max dose: 20 mg/day (limited additional benefit beyond this).*
| Group | Dosing Guidance |
|---|---|
| Renal/Hepatic Impairment | Initial dose: 5 mg/day. Titrate cautiously (CrCl <40 mL/min or cirrhosis). |
| Geriatrics | No adjustment unless renal/hepatic impairment present. |
| Children | Safety not established. |
| (Follow registered physician’s advice) |
| Drug Class | Risk |
|---|---|
| Other β-blockers | ↑ Risk of bradycardia, AV block (avoid combination). |
| Calcium Channel Blockers (Verapamil/Diltiazem) | ↑ Myocardial depression, hypotension, or heart failure. |
| Clonidine | Rebound hypertension if withdrawn concurrently. |
| Antiarrhythmics (Disopyramide) | ↑ Negative inotropy, conduction delays. |
| Reserpine/Guanethidine | ↑ Sympathetic inhibition → severe hypotension. |
Cardiogenic shock
Sinus bradycardia or ≥2nd-degree AV block
Overt heart failure (unless managed for chronic HF)
Right ventricular failure due to pulmonary hypertension
Common (>1%):
Fatigue, dizziness, headache
GI disturbances (nausea, diarrhea, constipation)
Cold extremities, muscle cramps
Serious (Monitor Closely):
Bronchospasm (in asthma/COPD patients)
Bradycardia, heart failure exacerbation
Hypotension
Pregnancy: Use only if benefit justifies fetal risk (embryolethal in animal studies).
Lactation: Avoid nursing (excretion in rat milk; human data unknown).
Abrupt Withdrawal: Taper gradually (↑ angina/HTN risk).
Anaphylaxis: May impair epinephrine response in allergies.
Renal/Hepatic Impairment: Dose adjustments essential.
Diabetes: Masks hypoglycemia symptoms (tachycardia excluded).
Peripheral Artery Disease: May worsen symptoms.
Cardioselective β₁-Adrenoceptor Blocker
Conditions: Below 30°C; protect from light and moisture.
Keep out of reach of children.
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