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BMS60044
Drugs acting on calcium channels
Question | Answer |
---|---|
L type drugs | verapamil, diltiazem, nifedipine; -pamil, -dipine |
T type drugs | mibefradil, ethosuximide, methsuximide, zonisamide, valproate, phenytoin |
PQRN drugs | Gabapentin, pregabaline |
Selectivity of verapamil (myocardial vs vascular) | 1:1 |
Selectivity of diltiazem(myocardial vs vascular) | 1:5 |
Selectivity of nifedipine(myocardial vs vascular) | 1:15 |
Selectivity of felodipine and nimodipine(myocardial vs vascular) | 1:>10 |
What Vaughan-Williams class are Ca channel blockers? | Class IV |
verapamil | decreases HR and O2 demand; contraindicated in AV conduction;get constipation,oedema, increases digoxin levels |
nifedipine | MAIN ACTION: LOWERS BP; arteriolar>> (vein); vasodilator, decreases afterload, orally, short t1/2 --> frequent dosing, increases HR |
felodipine and nimodipine | same as nifedipine but have long t1/2 |
diltiazem | lowers HR and O2 demand (less than verapamil; used for coronary artery vasospasm relief (variant angina) |
mibefradil | Ca channel blocker; taken off the market due to drug-drug interactions |
ethosuximide | used for absence (petit mal) seizures |
methsuximide | similar to ethosuximide |
zonisamide | mixed MOA; used in chronic pain tx |
valproate | mixed MOA; oldest t-type channel blocker |
phenytoin | Na and Ca channel blocker; anti-seizure; SE: gum hyperplasia, megaloblastic anemia, folate deficiency; zero order kinetics; 3A4 inducer |
gabapentin and pregabalin | alpha-2/delta 1&2 ligands; reduce transmitter release |
dantrolene | given i.v.; RyR receptor blocker; used for malignant hyperthermia; inhibits the release of intracellular Ca from skeletal muscle SR |