Beta Blockers Flashcards
Pharmacologic properties of β-Blockers:
Relative affinity for β1 and β2 receptors Intrinsic sympathetic action Differences in solubility Membrane stabilizing activity Capacity to induce vasodilation α1 and β receptor blockade Difference in pharmacokinetic parameters
This genotype is a major determinant of interindividual metoprolol clearance:
CYP2D6
Initially, PVR is ____ and CO is ___ during β-blocker therapy:
increased; decreased
β-blocker with no effect on plasma renin activity:
Pindolol
MOA of β-blockers anti-HTN action:
Sustained low total PVR
Decreased renin release
Decreased NE release
Peripheral vasodilation (some)
NE release is decreased due to blockade of ____:
presynaptic β receptors
Non-selective β-blockers augment pressor response to ___ due to blockade of ___:
epinephrine; β2
β-blockers that stimulate NO production:
Celiprolol
Nebivolol
β-blockers with α1 antagonistic activity:
Carvedilol
Labetalol
β-blockers with Ca entry blockade activity:
Carvedilol
Betaxolol
β-blockers that open K channels:
Tilisolol
β-blocker that acts as β2 receptor agonist:
Celiprolol
β-blockers with membrane stabilizing activity:
PALOCA
Propranolol Alprenolol Labetalol Oxprenolol Carvedilol Acebutolol
Cardioselective β1 blockers:
CABNAME
Celiprolol Atenolol Betaxolol Nebivolol Acebutolol Metoprolol Esmolol
β1 blockers are preferred in patients with:
Bronchospasm
Diabetes
Peripheral vascular disease
β-blockers with intrinsic sympathetic activity:
APOCAP
Alprenolol Pindolol Oxprenolol Carteolol Acebutolol Penbutolol
Major adverse effect of β-blockers:
Bronchoconstriction (use CABNAME or APOCAP)
ISA β-blockers are useful in patients with:
Diminished cardiac reserve Propensity for bradycardia Bronchospasm Diabetes Peripheral vascular disease
Non-cardio selective β-blockers are used in wide/open-angle glaucoma:
Timolol
Levobunolol
Carteolol
Metipranolol
β1 blockers used in wide/open-angle glaucoma:
Betaxolol
Levobetaxolol
Important adverse effects of propanolol:
Prolonged hypoglycemia
Uterine contractions
Increased risk of atherosclerosis
Withdrawal syndrome
PK properties of propanolol:
Highly lipophilic 25-30% oral bioavailability (increases with fatty food) Saturable hepatic extraction Large volume of distribution Weakly β-antagonistic active metabolite
Therapeutic uses of propanolol:
HTN Angina pectoris Arrhythmias MI CHF Thyroid storm Prophylaxis for migraine
β-blockers used for migraine:
Propanolol Metoprolol Atenolol Nadolol Timolol
