ASPECTS OF THE AMLODIPINE PLEIOTROPY IN BIOCHEMISTRY, PHARMACOLOGY AND CLINICSAbstract
Amlodipine is the third generation calcium antagonist, 1,4-dihydropyridine derivative with the prolonged duration of the antihypertensive action, especially blocking L-type Ca2+ ion channels. It promotes beneficial therapeutic effect by coronary and other blood vessel diseases and thus delays development of the atherosclerosis. It has several known trade names, the most mentioned is Norvasc. Amlodipine is well tolerated in the clinics, it could be used in combinations with other drugs – diuretics, angiotensin-converting enzyme inhibitors, angiotensin II receptor antagonists, statins. Amlodipine at nanomolar concentrations binds to the voltage-dependent L-type calcium channels. It possesses optimal lipophylicity. Amlodipine also influences the NO-dependent metabolic processes, stimulates NO synthesis and prolongs NO action duration. Results of the studies of the amlodipine pharmacological and clinical properties are summarized in several reviews. The present review contains opinion from the scientific works of the last decades about the multisided or pleiotropic amlodipine mechanisms of action, it contains information about sometimes controversial clinicalstudies of the amlodipine vaso- and cardioprotective activity.
Rasma Vitolina, Aivars Krauze, Gunars Duburs and Astrida Velena*
Latvian Institute of Organic Synthesis, Laboratory of membrane active compunds and β-diketones, Aizkraukles str. 21, Riga, Latvia, LV-1006
12 December, 2011
11 April, 2012
27 April, 2012
01 May, 2012