calcium channel blockers

pcol exam 2

what is the generic name of Norvasc

amlodipine

what is the generic name of Calan

verapamil

what is the generic name of Verelan

verapamil

what is the generic name of Covera HS

verapamil

what is the generic name of Isoptin SR

verapamil

what is the generic name of Cardizem

diltiazem

what is the generic name of Cartia XT

diltiazem

what is the generic name of Tiazac

diltiazem

what is the generic name of Procardia XL

nifedipine ER

what is the generic name of Adalat CC

nifedipine ER

what is the generic name of Cardene

nicardipine

what are the two different types of calcium channel blockers

dihydropyridine (DHP) and non-dihydropyridine (non-DHP)

what calcium channel blockers have oral osmotic gel matrix formulations that leave a ghost tablet in the stool

procardia XL, adalat CC, covera HS

what types of drugs are used in hypertension

diuretics

sympathoplegic blockers

vasodilators

angiotensin antagonists

renin inhibitor (aliskiren)

where are L type calcium channels located

cardiac system, blood vessels, skeletal muscles, neurons, endocrine cells, and bones

what type of calcium channel provides a long duration of calcium influx and is slowly inactivated

L type channel

what type of calcium channel requires high voltage to be activated

L type channel

what subunits are in L type calcium channels

alpha 1, alpha 2, beta, gamma, and delta

what can block L type calcium channels

non-DHP calcium channel blocker

DHP calcium channel blocker

Cd²⁺

what happens when L type calcium channels are stimulated

vascular smooth muscle constriction — primarily arterial

increased contractility

increased conduction of SA and AV nodes

cerebral vasospasm associated with stroke

where are T type calcium channels located

heart (vascular smooth muscle, SA, and AV node) and neurons

what type of calcium channel requires low voltage to be activated

T type channels

what type of calcium channel is rapidly inactivated

T type channels

where are N type calcium channels located

neurons and sperm

where are P/Q type calcium channels located

neurons

where are R type calcium channels located

neurons and sperm

is calcium normally high or low intracellularly

low

where is calcium stored intracellularly

sarcoplasmic reticulum (SR)

what does elevated calcium levels lead to

cell activation

contraction of blood vessel smooth muscle

contraction and increased conductivity of cardiac myocytes

what can cause calcium channels to open

directly — depolarization

indirectly — ligands

how does extracellular calcium enter the cell

via opening of selective calcium channels

how do calcium channel blockers work

competitively bind to L type channels → block open channels during voltage change → reduce influx of calcium → diminish response of cell

what happens to the blood vessels when a calcium channel blocker is given

vasodilation — primarily arterial

decrease in total peripheral resistance

what happens in the heart when a non-DHP calcium channel blocker is given

decreased cardiac output

negative inotropic effect

negative chronotropic effect

negative dromotropic effect

what does a negative ionotropic effect mean

slow force of heart contraction

what does a negative chronotropic effect mean

slow rate of heart contraction

what does a negative dromotropic effect mean

slow AV node conduction

what is the overall effect of calcium channel blockers

reduced blood pressure

what are the sites of action of calcium channel blockers

SA node and AV node

cardiac myocytes

coronary arteries

peripheral arteries

what does dilation of coronary arteries lead to

increase in myocardial oxygen supply

what does dilation of peripheral arteries lead to

decreased after load → decreased myocardial oxygen demand

what effect do calcium channel blockers cause in the AV and SA nodes

SA node — decreased automaticity

AV node — decreased conduction

what is preload

pressure generated at the end of diastole

what is afterload

resistance to ejection during systole

what calcium channel blockers are dihydropyridines (DHPs)

nifedipine, amlodipine, felodipine, nicardipine

what is the primary action of DHP calcium channel blockers

vasodilation

what are DHP calcium channel blockers used for

hypertension and angina

what are the adverse reactions of DHP calcium channel blockers

reflex tachycardia

headache

gingival hyperplasia

flushing

peripheral edema

palpitations

hypotension

what drug can DHP calcium channel blockers be used with

beta blockers

what drugs are non-DHP calcium channel blockers

verapamil and diltiazem

what are non-DHP used for

arrhythmias and A-fib

how do non-DHP calcium channel blockers work

slow heart rate and non-selectively vasodilate

negative chronotropy and inotropy

what are the adverse reactions for non-DHP calcium channel blockers

constipation

gingival hyperplasia

edema

headache

dizziness

arrhythmia

heart failure

what can happen when using a non-DHP calcium channel blocker and beta blocker

cardiac depression or heart block

which formulation of calcium channel blocker is better tolerated for hypertension treatment

long acting or slow release

what enzyme mediates the metabolism of calcium channel blockers

CYP3A4

what are some CYP3A4 inhibitors

grapefruit juice, ketoconazole

what are some CYP3A4 inducers

st johns wort, rifampin, carbamazepine

what is the only calcium channel blocker that is more fecally excreted than renally excreted

diltiazem

when should diltiazem and verapamil not be used

heart failure, AV block

when should beta blockers/labetalol not be used

AV block, diabetes, dyslipidemia, asthma

when should hydralazine not be used

coronary artery disease, post-MI

when should thiazides not be used

diabetes, gout, hypokalemia

when should furosemide not be used

diabetes, gout, hypokalemia

when should K+ sparing diuretics not be used

renal insufficiency, hyperkalemia

when should diuretics not be used

dyslipidemia

when should ACEIs not be used

hyperkalemia

when should ARBs not be used

hyperkalemia

what anti-hypertensives are preferred in patients >65 years

diuretics, ACEIs and CCBs

what anti-hypertensives are preferred in people with african heritage

diuretics (plus or minus ACEIs or ARBs) or CCBs

what anti-hypertensives are preferred in pregnant patietns

methyldopa or labetalol

what anti-hypertensives are preferred for angina

beta blockers or CCBs

what anti-hypertensives are preferred for MI

beta blocker, ACEIs, aldosterone antagonist

what anti-hypertensives are preferred in heart failure

ACEIs, ARBs, beta blockers, diuretics, aldosterone antagonists

what anti-hypertensives are preferred in stroke prevention

diuretics + ACEI or ARB

what anti-hypertensives are preferred in kidney disease

ACEI or ARB (plus or minus verapamil or diltiazem)

what anti-hypertensives are preferred in diabetes

ACEI or ARB (plus or minus beta blocker, diuretic, or CCB)

what anti-hypertensives are preferred in asthma

CCB, ACEI, or ARB

what anti-hypertensives are preferred in benign prostatic hyperplasia

alpha blockers

what anti-hypertensives are preferred in migraines

beta blockers or CCBs

what anti-hypertensives are preferred in osteoporosis

diuretics, thiazides

what drugs can cause or worsen hypertension

corticosteroids

alcohol

amphetamine

appetite suppressants

caffeine

calcineurin antagonist

decongestants

erythropoisis stimulating agents

estrogen

NSAIDs

oncology drugs

thyroid hormones

SNRIs