Beta-1 antagonist
Beta-1 adrenergic receptor antagonist
- ↓ heart rate, contractility and AV conduction
- PR interval prolongation
- ↓ renin release
- Antiarrhythmic and blood-pressure lowering
- Masks tachycardia as an adrenergic warning sign of hypoglycemia
- Possibility of fatigue
- For β blockers that cross the blood-brain barrier (BBB):
- anxiolytic effect
- possible mitigation of fear conditioning of traumatic memories (PTSD prevention, investigational)
- slightly increased risk of depression (evidence mixed)
- migraine prevention
- Akathisia treatment
- may reduce ↓ tremulous adrenergic arousal and sympathetic “inner motor” amplification
- ↓ aqueous humor production → glaucoma treatment
Drugs with this mechanism (19)
- Acebutolol — Cardioselective beta-blocker with intrinsic sympathomimetic activity.
- Atenolol — Hydrophilic cardioselective beta-blocker with fewer CNS effects.
- Betaxolol — Cardioselective beta-blocker; also a topical glaucoma agent.
- Bisoprolol — Cardioselective beta-blocker proven in heart failure.
- Carteolol — Ophthalmic beta blocker with intrinsic sympathomimetic activity; gentler on lipids than timolol.
- Carvedilol — Nonselective beta-blocker with alpha-1 block; a heart-failure standard.
- Celiprolol — Beta-1 blocker with beta-2 partial agonism; studied for reducing arterial complications in vascular Ehlers-Danlos syndrome.
- Esmolol — Ultra-short IV beta-1 blocker for acute rate and blood-pressure control.
- Labetalol — Combined alpha/beta blocker; a mainstay for hypertension in pregnancy.
- Metoprolol — The most-prescribed cardioselective beta-blocker; succinate proven in heart failure.
- Nadolol — Long-acting, renally cleared beta blocker for hypertension, angina, and portal hypertension.
- Nebivolol — Beta-1 blocker with beta-3 agonism and nitric-oxide-mediated vasodilation.
- Pindolol — Nonselective beta blocker whose intrinsic sympathomimetic activity preserves resting heart rate; hypertension.
- Propranolol — Non-selective beta-blocker used for performance anxiety, tremor, and migraine.
- Propranolol ER — Extended-release nonselective beta blocker for hypertension, migraine prevention, and tremor.
- Sotalol — Beta-blocker with Class III antiarrhythmic action; QT monitoring at initiation.
- Talinolol — Beta-1-selective blocker used in some countries; also a transporter-probe drug in pharmacokinetic research.
- Timolol — Ophthalmic beta blocker; systemic absorption can cause bradycardia and bronchospasm.
- Metoprolol succinate ER — Extended-release beta-1 blocker with proven heart-failure benefit.
Self-check
- What ECG interval is prolonged by beta-1 blockade?
PR. - Which warning sign of hypoglycemia can beta-1 blockade mask?
Tachycardia.
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