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Pharmacology

Calcium channel blockers

QuestionAnswer
ca+ enters cell via 3 types of voltage-dependent ca+ channels L-type, N-type, T-type; L-type are long lasting channels predominant in cardiac and smooth muscle, ones blocked by most CCBs
result of CCBs is marked decrease in transmembrane ca+ content and prolonged vascular smooth muscle relaxation
blocking action of CCBs occurs via 3 different receptors diphenylalkylamine-based and benzothiazepine-based (type 1); dihydropyridine-based (type 2)
only CCB to cross the blood brain barrier? nimodipine (Nimitop) used for subarachnoid hemorrhage from ruptured intracranial berry aneurysm
CCB of choice during lactation? nifedipine (Procardia)
dosage reduction for renal impairment is recommended only for? nicardipine (Cardene)
Verapamil should be avoided in CHF because? it has the strongest negative inotropic effect
type 1's are contraindicated for pts with EF<40% and for all other pts early post MI because? negative inotropic and bradycardic effects
Type 1's should not be used pts with? ventricular dysfunction, sa or av nodal conduction disturbances, sbp<90 d/t high risk for HF and hypotension
Type 2's (dihydropyridines) should be avoided in post MI, unstable angina, significant peripheral edema d/t their strong peripheral vasodilating effects and may lead to reflex tachycardia
Type 1's: Diltiazem, verapamil
Type 2's: dihydropyridines amlodipine (Norvasc), felodipine (Plendil), isradipine (Dynacirc), nicardipine (Cardene), nifedipine (Procardia), nisoldipine (Sular)
Adverse drug rxns occur less often with long-acting formulations
decreased myocardial contractility may lead to HF
verapamil, Cardizem, and Procardia may increase risk of digoxin? toxicity
drugs that inhibit the CYP3A4 system (including grapefruit juice) may increase? free drug levels of CCB
effective in tx of stable and exertional angina on supply and demand side demand by: peripheral vasodilation and negative inotropism; supply by: dilation of coronary arteries
Norvasc is not a sustained release but has a long half life of 30-50 hours which means? it can be crushed unlike a sustained release but still provide the benefits of less venous pooling, less reflex tachycardia, and once daily dosing
constipation occurs in almost 100% of pts taking? verapamil
CCBs used to treat Prinzmetal's angina Cardizem, Procardia xl, norvasc
CCBs not first line for unstable angina but if used ? is the drug of choice verapamil
only used in htn after ? have been considered ACEIs, ARBs, diuretics, BBs
Tx of SVT and Afib Type 1's (verapamil and Cardizem) verapamil for PSVT prophylaxis
if verapamil is used with dig it increases the risk of dig toxicity
should not be used in WPW CCBs, digoxin
Migrain h/a prophylaxis verapamil at least 3 months of therapy needed to determine effectiveness
Raynaud's syndrome Type 2 (dihydropiridines) d/t their peripheral vasodilating effects, and platelet inhibition first choice: Procardia xl
esophageal spasm Cardizem has been used but should not be used with GERD
with severe hepatic impairment dosage reductions are recommended
most common adverse reaction is hypotension
Created by: heatherbrown2020