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BMS60045
Drugs acting at the potassium channel
| Question | Answer |
|---|---|
| uses of K channel blockers | anti-arrhythmic; used to treat ventricular and supraventricular arrhythmias; hypoglicemic agents |
| what class are K channel blockers? | class III |
| how do K channel blockers work? | they block phase 3 of cardiac action potential, thereby prolonging QT wave and repolarization will take longer (prolong phase 3 refractory period) |
| what are the class III drugs? | sotalol, bretylium, amiodarone, dronedarone, dofetilide, ibutilide |
| amiodarone | class X; anti-arrythmic; excretion is mainly hepatic; t1/2 = 58 days (36 for DEA -active metabolite)so it favors toxicity; structurally similar to thyroixine (affects thyroid fx) |
| Amiodarone SE | dose related; thyroid, lung (-itis, fibrosis), liver, eyes (corneal microdeposits) |
| dronedarone | less toxic amiodarone; doesn't effect thyroid, smaller Vd, and shorter t1/2 |
| sotalol | non-selective beta-blocker; torsade de pointes |
| what do SUs (Gl- drugs) do? | block K channels; activate cell depolarization; open Ca channels and allow Ca enter cell and insulin to be released |
| Gl- | sulfonyl urea |
| SE of SE | weight gain and hypoglycemia |
| metformin | used for diabetes control; uses guanadine (found in urine); inhibits lactate uptake by liver; inhibits gluconeogenesis via activation of AMPK |
| -glinide | non-SU; increase insulin release; ROSA; weight gain and hypoglycemia reduced in comparison to SU |
| clinical uses of K channel openers | vascular (arterial) relaxation (decrease after load, decrease bp, increase perfusion); promote hair growth |
| nicorandil | K channel opener; used for arterial relaxation, Tx and prevention of angina, CHF, hypertension; stim guanylate cyclase (increasing cGMP) --> relaxation of venous smooth muscle (decreases pre-load); SE: oral ulceration |
| minoxidil | K channel opener; promotes hair growth |