Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0085580 (essential hypertension)
 14,686 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

We investigated the effects of the calcium channel blocker amlodipine besilate on serum levels of adrenal androgens and insulin in 20 men with essential hypertension and obesity (age: 51.9+/-4.7 years, body mass index: 27.7+/-1.5 kg/m2). All were treated with amlodipine besilate (Norvasc) for 3 months. Blood pressure, fasting plasma glucose (FPG), HbA1c and serum levels of insulin, dehydroepiandrosterone (DHEA), DHEA sulfate (DHEA-S), and lipids were measured before and after a 3-month period. In 10 patients, 75 g oral glucose tolerance test (75 g-OGTT) was also performed. Amlodipine besilate treatment 1) lowered the fasting serum insulin level and total serum insulin level during 75 g-OGTT and 2) increased serum DHEA and DHEA-S levels. No changes in fasting plasma glucose, HbA1c and serum lipids were observed during treatment. We conclude that amlodipine besilate improves insulin resistance and consequently increases serum DHEA and DHEA-S levels.
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PMID:Effects of amlodipine on serum levels of adrenal androgens and insulin in hypertensive men with obesity. 1135 51

Amlodipine, marketed primarily as a besylate salt, is a calcium channel blocker used for treating essential hypertension. Amlodipine maleate is another salt that is considered, in terms of pharmacokinetics and pharmacodynamics, similar to amlodipine besylate. This open, randomized, two-period crossover trial has investigated in 24 healthy volunteers over a 144 h period the bioequivalence of amlodipine maleate tablets 10 mg versus amlodipine besylate tablets (Norvasc 10 mg). Plasma amlodipine concentrations were assessed by ultra performance liquid chromatography interfaced with a double quadrupole mass spectrometer. The area under the curve total (AUC(t)) and the area under the curve to infinity (AUC(inf)) values, peak plasma concentration (C(max)), and time to attain peak (t(max)) were not statistically different between the two drugs. AUC(t) and AUC(inf) values were higher (p < 0.05) in females than in males. The tolerability profile was comparable for the two salts of amlodipine. These findings indicate that amlodipine maleate and besylate are bioequivalent and were well tolerated, which suggests that the plasma kinetics of amlodipine depend on the properties of the molecule itself. Hence, the two salts investigated could be used interchangeably in clinical practice.
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PMID:Single-dose, randomized, crossover bioequivalence study of amlodipine maleate versus amlodipine besylate in healthy volunteers. 1805 79