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Online Journal of Veterinary Research ©
Volume 25 (3): 168-172, 2021
Pharmacokinetics of nifedipine in hyperlipidemic male Wistar rats.
Venkata Rajesham V1, Rama Narsimha Reddy A2, Rajyalakshmi G2, †Anbu J1, †Narsimha Reddy Y2
1Department of Pharmacology, Velís college of Pharmacy, Chennai, 2Department of Pharmacology, University College of Pharmaceutical Sciences, Kakatiya University, Warangal, India.
Rajesham V, Reddy RN, Rajyalakshmi G,† Anbu J,† Reddy NY, Pharmacokinetics of nifedipine in hyperlipidemic male Wistar rats, Onl J Vet Res., 25 (3): 168-172, 2021. We report effects of hyperlipidemia on pharmacokinetics of nifedipine in male adult Wistar rats. Cholesterol was fed daily for 30 days to induce hyperlipidemia confirmed by lipid profiles. Then, 20mg/kg nifedipine from Nicholus Piramils supplement was fed daily for 7 days to 6 normal controls and 6 hyperlipidemic rats. On the 1st and 8th day, blood was taken for plasma nifedipine determined by HPLC. Compared with normal rats, in those fed high fat diet, plasma cholesterol increased ~52, trigliceride 48~ and low density lipoprotein 57% (P < 0.0005) by 30 days confirming hyperlipidemia. Compared with controls, at day 1 of nifepidime treatment we found increased peak concentrations (Cmax) 30%, area under curve (AUC) 34-48%, half-life (t1/2) 21%, clearance (CL/f) 25 and volume distribution V/F 28%(P < 0.05) in rats fed high fat diet. By day 8, Cmax increased 24%, half-life 21% and AUC0-α 13% due to 12% reduced clearance of nifedipine. These findings suggest that hyperlipidemia may reduce clearance of nifedipine due to altered protein binding or inhibition of cytochrome P-450 by excessive cell membrane cholesterol.
KEY-WORDS: Nifedipine, hyperlipidemia, Pharmacokinetics, standard cholesterol diet.