Amlodipine pretreatment and the ischemic heart.
Amlodipine is a long-acting dihydropyridine-based Ca2+ channel blocker, developed for use on a once-daily basis. Experiments using hearts from amlodipine-pretreated rats were undertaken to further test the hypothesis that Ca2+ channel blockers can be used as prophylactic therapy to reduce the severity of the mechanical and biochemical consequences of ischemia and reperfusion. Amlodipine was given intravenously, 0.25 mg/kg, 5 hours before excising the hearts. Ischemia (global) was induced at 37 degrees C for 10, 30 or 60 minutes, and was followed by reperfusion. Protection was quantitated in terms of functional recovery, adenosine triphosphate and creatine phosphate retention, tissue acidosis and Ca2+ gain. The results show that amlodipine pretreatment supplied protection, provided that the ischemic episode did not exceed 30 minutes. The protection resulted in improved recovery of peak developed tension on reperfusion, reduced Ca2+ gain, retention of tissue adenosine triphosphate and creatine phosphate, and reduced acidosis.
Nayler
W G
WG
Department of Medicine, University of Melbourne, Victoria, Australia.
D000138:Acidosis / Q000209:etiology; D000255:Adenosine Triphosphate / Q000378:metabolism; D017311:Amlodipine; D000818:Animals; D002118:Calcium / Q000378:metabolism; D002121:Calcium Channel Blockers; D003327:Coronary Disease / Q000150:complications / Q000378:metabolism / Q000503:physiopathology; D006339:Heart Rate / Q000187:drug effects; D066298:In Vitro Techniques; D008297:Male; D009200:Myocardial Contraction / Q000187:drug effects; D015428:Myocardial Reperfusion Injury / Q000517:prevention & control*; D009206:Myocardium / Q000378:metabolism; D009543:Nifedipine / Q000494:pharmacology; D010725:Phosphocreatine / Q000378:metabolism; D051381:Rats; D011919:Rats, Inbred Strains; D015424:Reperfusion; D013997:Time Factors
D002121:Calcium Channel Blockers; D010725:Phosphocreatine; D017311:Amlodipine; D000255:Adenosine Triphosphate; D009543:Nifedipine; D002118:Calcium