Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0599766 (functional recovery)
 13,441 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Amlodipine is a long-acting dihydropyridine calcium antagonist with vascular selectivity. Although structurally related to nifedipine, amlodipine differs in several important respects, including its slow rate of onset and slow recovery. These effects probably reflect the relatively slow rate of association and dissociation of amlodipine with its binding site. The interaction of amlodipine with the calcium antagonist binding site associated with the slow Ca2+ channels differs from that of other dihydropyridines in that it involves the binding domains for the phenylalkylamine- and benzothiazepine-based antagonists, as well as for the dihydropyridines. The prolonged duration of action of amlodipine makes it suitable for use in conditions where calcium channel blockade is required on a 24-h basis. To determine whether amlodipine has a vascular protective effect, amlodipine was given orally to either cholesterol-fed rabbits or stroke-prone hypertensive rats. In the cholesterol-fed rabbits amlodipine (1 or 5 mg/kg/day) produced a significant, dose-dependent reduction in the incidence of atheromatous lesions in the thoracic aorta over an 8-week period. In stroke-prone rats the administration of amlodipine at a dose of 5 mg/kg/day reduced the incidence of mortality over a 30-week treatment period. In spontaneously hypertensive rats amlodipine (5 mg/kg/day) caused a fall in systolic blood pressure, accompanied by a significant (P less than 0.01) reduction in cardiac hypertrophy. When administered intravenously (0.25 mg/kg) 5 h before hearts were excised and made globally ischaemic for short periods (the 'stunned' heart) amlodipine pretreatment improved functional recovery associated with reperfusion.
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PMID:Vascular and myocardial effects of amlodipine: an overview. 183 39

Amlodipine is a long-acting dihydropyridine-based calcium antagonist developed for use on a once-a-day basis. Experiments were undertaken to establish whether the chronic administration of amlodipine prevents the rise in blood pressure in spontaneously hypertensive rats (SHR), and whether it attenuates cardiac hypertrophy caused by hypertension. The experiments were performed in spontaneously hypertensive rats, and normotensive Wistar-Kyoto (WKY) and Sprague-Dawley (SD) rats. Amlodipine was given orally to provide a daily intake of 10 mg kg-1 day-1. The rats were 8 weeks old at the start of the therapy. In the SHR, but not in the WKY or SD rats, the blood pressure was reduced (p less than 0.01) after 30 weeks in the rats receiving amlodipine but not in the placebo-treated rats. At the same time the heart-to-body-weight ratio was reduced in the amlodipine-treated SHR but not in the SD or WKY rats. This same amlodipine regimen (10 mg kg-1 day-1 orally) or amlodipine i.v. (0.25 mg/kg, 5 h before excising the hearts) improved functional recovery (p less than 0.01) of hearts "stunned" by 10 min ischemia and attenuated (p less than 0.05) calcium ion gain on reperfusion after 30 to 60 min ischemia. These results indicate that prophylactic therapy with amlodipine lowers blood pressure in hypertensive rats, prevents hypertension-induced hypertrophy, and exerts a cardiac-protective effect during short periods of ischemia.
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PMID:The effect of amlodipine on hypertension-induced cardiac hypertrophy and reperfusion-induced calcium overload. 246 27

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.
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PMID:Amlodipine pretreatment and the ischemic heart. 253 Aug 87