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11 Cards in this Set

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  • Back
When does the calcium channel open?
Once smooth muscle L-channels are activated -> activate phospholipase C -> activate phosphokinase C -> phosphorylates the calcium channel, which causes it to open and to calcium to flow into the cell
Where are L-voltage dependent calcium channels located?
smooth muscle, caridac, skeletal muscle
What role does Ca++ play in muscle contraction in cardiac tissue?
Na+ influx -> increase Ca++ influx -> increases intracellular Ca++ -> Ca++ released from sarcoplasmic reticulum -> breaks Troponin C-Actin complex forming Troponin C-Ca++ complex --> the released free actin binds to myosin-P-> muscle contraction
What role does Ca++ play in muscle contraction in vascular smooth muscle tissue?
Intracellular Ca++ binds to Calmodulin -> complex converts myosin light chain kinase (inactive) to myosin light chain kinase-P (active) -> phosphorylates myosin which interacts with free actin -> vascular smooth muscle contraction
Drug effectiveness as a function of channel location 1) cardiac L-channels
Verapamil > diltiazem > nifedipine
Drug effectiveness as a function of channel location
2)Vascular Smooth Muscle
Nifedipine > Verapamil > Diltiazem
What is the structure of Verapamil?
What is the structure of Diltiazem?
What is the structure of Nifedipine?
SAR for the Dihydropyridines
1)Dihydropyridine ring system
2)Phenyl group in position #4 w/ an ortho or meta substituent that is EWG (keep aromatic rings perpindicular)
3)Esters in positions #3 and #5 (if cleaved, therapeutic effect is lost)
What drug/food interaction occurs with CCBs?
Grapefruit juice (increases absorption of CCBs except Diltiazem or amlodipine)