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Beta-1 antagonist

Beta-1 antagonist (1/2)

• Reduced heart rate, cardiac contractility, and systolic blood pressure
• Antiarrhythmic effects
• PR interval prolongation
• Possibility of fatigue
• Masks adrenergic warning symptoms of hypoglycemia (tachycardia)
• 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

Beta-1 antagonist (2/2)

• 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 — Beta blocker with partial agonism; sometimes used to accelerate antidepressant response.
• 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.

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