. Mechanism & Class
Class: Cardioselective β₁-blocker
Action:
Blocks cardiac β₁-receptors → ↓ heart rate, ↓ contractility, ↓ renin release
Reduces cardiac output → lowers BP
Key Limitation:
Lacks vasodilatory effects (unlike carvedilol/nebivolol)
Minimal CNS penetration (vs. propranolol)
2. FDA-Approved Uses
| Indication | Dosage Range | Notes |
|---|---|---|
| Hypertension | 25-100 mg daily | Not first-line per guidelines |
| Angina Pectoris | 50-200 mg daily | Reduces attack frequency |
| Arrhythmias | 50-100 mg daily | SVT/Ventricular control |
3. Dosing Protocol
Starting: 25-50 mg once daily
Titration: ↑ by 25 mg weekly (max 100 mg/day)
Take: On empty stomach (food ↓ absorption 20%)
Renal Adjustment:
CrCl (mL/min) Dose Adjustment 15-35 Max 50 mg/day <15 Max 25 mg/day or avoid
4. Black Box Warnings & Contraindications
| Risk | Critical Considerations |
|---|---|
| Abrupt Withdrawal | ↑ Angina/MI risk – taper over 1-2 weeks |
| Heart Failure Decompensation | Avoid in acute HF or HFrEF (NYHA IV) |
| Absolute Contraindications | • Asthma/COPD (relative) • Heart block >1st degree • Cardiogenic shock |
5. Adverse Effects
| Common (>10%) | Serious (<1%) |
|---|---|
| Fatigue | Bradycardia (<45 bpm) |
| Cold extremities | Heart block |
| Sexual dysfunction | Masked hypoglycemia (diabetics) |
| Metabolic: ↑ TG, ↓ HDL-C, insulin resistance |
6. Modern Role in Hypertension
❌ Not recommended as first-line monotherapy per ACC/AHA 2023 guidelines:
Inferior stroke prevention vs. ARBs/CCBs (LIFE trial)
↑ Diabetes risk by 28% (ASCOT trial)
✅ Consider when:
Coexisting angina or tachyarrhythmias
Post-MI patients (if no HF)
Pregnancy (Category C)
7. Drug Interactions
| Interacting Drug | Risk | Action |
|---|---|---|
| Verapamil/Diltiazem | ↑ Bradycardia/AV block | Avoid combo |
| Insulin/Sulfonylureas | Masked hypoglycemia | Educate diabetic patients |
| NSAIDs | ↓ Antihypertensive effect | Monitor BP |
8. Clinical Pearls
Elderly: ↑ Risk of bradycardia – start at 12.5 mg/day
Diabetics: Avoid – worsens glycemic control; use carvedilol/nebivolol
Pregnancy: Safer than ACEi/ARBs but less effective than labetalol
Cocaine-Induced HTN: Contraindicated (unopposed α-vasoconstriction)
🆚 Atenolol vs. Newer Beta-Blockers
| Parameter | Atenolol | Carvedilol | Nebivolol |
|---|---|---|---|
| Vasodilation | None | α-blockade | NO-mediated |
| Metabolic Effects | Worsens insulin resistance | Neutral | Improves insulin sensitivity |
| HFrEF Mortality | No benefit | Proven ↓ mortality | Proven ↓ mortality |
| Guideline Status | Deprecated | Preferred | Preferred |
9. Patient Counseling
"Never stop suddenly – taper over 2 weeks."
"Check pulse daily – hold dose if <55 bpm."
"Diabetics: Monitor glucose closely – hides low sugar symptoms."
"Report: Shortness of breath, ankle swelling, dizziness."
"Avoid decongestants (e.g., pseudoephedrine)."
⚠️ Red Flags:
Heart rate <50 bpm → reduce/stop dose
New dyspnea/edema → evaluate for heart failure
Sources: ACC/AHA Hypertension Guideline (2023), LIFE Trial (Lancet), NICE Guidelines (2023).
Prescribing Insight: Reserve for specific scenarios like angina with HTN – not routine hypertension management.
Comments
Post a Comment