Calcium Channel Blockers Flashcards
What are calcium channel blockers?
- drugs that block Ca2+ entering a muscle cell
What are the 2 main groups of calcium channel blockers?
1 - dihydopyridines (mainly blood vessel dilation)
2 - non-dihydopyridines (mainly effects on heart)
What is the most commonly prescribed calcium channel blocker in the UK, that is a dihydopyridine?
- Amlodipine
What are 2 other drugs that are classed as non-dihydopyridines that can be prescribed as calcium channel blockers?
- Diltiazem - Verapamil
Generally out of the 2 groups of calcium channel blockers, which drugs work almost entirely on the smooth muscle and is used to treat hypertension?
- drug class = dihydopyridines
- drug name = amlodipine
Generally out of the 2 groups of calcium channel blockers, which drugs were almost entirely on the heart?
- drug class = non-dihydopyridines
- drug name = Diltiazem and Verapamil
Out of the 3 calcium channel blocker drugs that we need to know (Diltiazem, Verapamil and Amlodipine) which one is able to act on the heart and the smooth muscles?
- drug class = non-dihydopyridines
- drug name = Diltiazem
What are L-type calcium channels?
- L means long lasting
- responsible for the excitation-contraction coupling
- located in all muscle cells
- located in endocrine cells of adrenal cortex (involved in aldosterone release)
How do L-type Ca2+ channels in cardiac and smooth muscle become activated?
- cells receive action potential
- Na+ channel opens
- T-type Ca2+ channel opens
- Na+ and Ca2+ from T-type Ca2+ channels ⬆️ voltage
- L-type Ca2+ channel opens causing action potential
What is the mechanism of action of Amlodipine?
- non competitive antagonist
- binds to L-type Ca2+ channels
- ⬇️ Ca2+ in cells and inhibit vasoconstriction
What effects can Ca2+ channel blockers have on the cardiovascular system?
- ⬇️ SA node activity = ⬇️ HR
- ⬇️ cardiomyocyte Ca2+ = ⬇️ inotrope force
- ⬇️ smooth muscle Ca2+ = ⬇️ vasoconstriction
Out of the 3 calcium channel blocker drugs that we need to know (Diltiazem, Verapamil and Amlodipine) which one would be used to treat angina?
- drug class = non-dihydopyridines
- drug name = Diltiazem
Out of the 3 calcium channel blocker drugs that we need to know (Diltiazem, Verapamil and Amlodipine) which one would be used to treat arrhythmia’s?
- drug class = non-dihydopyridines
- drug name = Verapamil
In addition to treating hypertension, what other syndrome can Amlodipine be used to treat?
- Raynauds syndrome
- causes severe vasoconstriction
What is the most common side effect to Ca2+ channel blockers?
- ankle swelling