12. β-receptor antagonists Flashcards
β-receptor antagonists
non selective & selective β1
non selective β-receptor antagonists
Propranolol Pindolol Timolol Carvedilol Labetalol Sotalol Celiprolol
β1 selective blockers
cardioselective
Nebivolol Metoprolol Betaxolol Esmolol Acebutolol Atenolol
Propranolol
highest lipid solubility
local anesthetics effect (NA+ channel blocked)
Pindolol
partial agonist (ISA) local anesthetics effect (NA+ channel blocked)
Carvedilol & Labetalol
also blocks α1 => vasodilation
dual effect in hypertension
Sotalol
lowest lipid solubility
K+ channel blocker => antiarrhythmic
Nebivolol
highest lipid solubility
very long half life (10hr)
leads to vasodilation by NO
Metoprolol
local anesthetics effect (NA+ channel blocked)
Betaxolol
very long half life (20hr)
Esmolol
very short half life (10min)
Acebutolol
partial agonist (ISA) lowest lipid solubility local anesthetics effect (NA+ channel blocked) also cues NA+ channel blocking
Atenolol
lowest lipid solubility
ISA
intrinsic sympathomimetic activity
a group of beta blockers that are able to stimulate beta-adrenergic receptors (agonist effect) and to oppose the stimulating effects of catecholamines (antagonist effect) in a competitive way