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Pharmacology
Calcium Channel Blockers
20
Pharmacology
Graduate
03/03/2010

Additional Pharmacology Flashcards

 


 

Cards

Term
Alpha 1 subunit
Definition

transmembrane, pore forming

10

Term
Beta
Definition

intracellular

4

Term
Gamma
Definition

2

Transmembrane

Term
Alpha-2-Delta
Definition

3

extracellular

transmembrane

Term
Voltage Gated Calcium Channel L(ente)
Definition
  • Verapamil
  • Diltiazem
  • Nifedipine
Term
Voltage Gated Calcium Channel T(ransient)
Definition

Blocked by:

  • Mibefradil
  • Succinimide (Ethosuximide, Methsuximide)
  • Sulfonimides (Zonisamide)
  • Valproylamides (Valproate)
  • Hydantoins (Phenytoin)
Term
Voltage Gated Ca Channel N(euronal),P,Q,R
Definition
  • Gabapentin
  • Pregabalin
  • alpha-2-delta ligand at PQRS-Ca channel
  • decrease transmitter release
Term

Selectivity of Ca Channel Blockers

Myocardial vs. Vascular

Definition
  • Verapamil 1:1
  • Diltiazem 1:5
  • Nifedipine 1:15
  • Felodipine 1:>100
  • Nimodipine 1:>100
Term
Verapamil effect
Definition
  • 1:1 myocardial:vascular
  • Decreases HR & O2 demand
  • contraindicated in AV conduction abnormal
  • Constipation
  • edema
  • digoxin levels
  • ONLY WORKS FOR ATRIAL ARRYHTHMIA
  • CLass IB works for ventricular arryhthmia
Term
Nifedipine effects
Definition
  • arteriolar (>>vein) vasodilator
  • 1:>100 myocardial:vascular
  • oral (half life 3-4 hrs= frequent dosing)
  • decrease afterload
  • decrease BP
  • increases HR
Term
Diltiazem
Definition
  • 1:5 myocardial:vascular
  • decreased HR & O2 demand (but less of an effect than Verapamil)
  • relieves coronary artery vasospasm (variant angina)
Term
Succinamide
Definition
  • anti-epileptic
  • (T-type are all anti-seizure)
  • Ethosuximide
  • Methsuximide
Term
Sulfonimides
Definition
  • mixed mode of action
  • one MOA is interacts with T-type blocker
  • Zonisamide
Term
Valproylamides
Definition
  • mixed MOA
  • T-type blocker
  • Valproate
  • naturally found in valerian
Term
Phenytoin
Definition
  • Na/Ca channel blocker
  • zero order kinetics (saturable)
  • gum hyperplasia
Term
Folate Antagonism
Definition
  • Phenytoin
  • Triamterene
  • Dapsone
  • Trimethoprim
  • Methotrexate
Term
CYP P450 3A4 inducers
Definition
  • St. John's wort
  • efavirenz, nevirapine
  • glucocorticoids
  • rifampin
  • carbamazepine
  • barbituates
  • phenytoin
Term
Ryanodine Receptor Blocker
Definition
  • in striate muscle, ryanodine receptor controls intracellular Ca release
Term
Dantrolene
Definition
  • Ryanodine Receptor Blocker
  • used in ER (via IV) to take away muscle contraction in cases of muscle hyperactivity causing hyperthermia
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