Food-drug interactions: effect of capsaicin on the pharmacokinetics of simvastatin and its active metabolite in rats. 2013

Xue-jia Zhai, and Jian-guo Chen, and Jin-mei Liu, and Fang Shi, and Yong-ning Lu
Department of Pharmacy, Union Hospital, Huazhong University of Science and Technology, Wuhan 430022, People's Republic of China.

Capsaicin (trans-8-methy-N-vanilly-6-nonenamide, CAP), the main ingredient responsible for the hot pungent taste of chilli peppers. However, little is known about the metabolic interactions between CAP and clinically used drugs. This study attempted to investigate the effect of CAP on the pharmacokinetics of simvastatin (SV), a cytochrome P450 (CYP) 3A substrate and an important cholesterol-lowering agent. CAP (3, 8 or 25 mg/kg), ketoconazole, dexamethasone or 5% CMC-Na was given to rats for seven consecutive days and on the seventh day SV (80 mg/kg) was administered orally. The results showed that when a single dose of SV was administered to rats fed with CAP over one week, AUC(0→∞), C(max) of SV and its acid metabolite was significantly decreased in comparison to the control treatment. Pretreatment of rats with CAP resulted in an decrease in the AUC(0-∞) of SV of about 67.06% (CAP 3 mg/kg, P<0.05), 73.21% (CAP 8 mg/kg, P<0.01) and 77.49% (CAP 25 mg/kg, P<0.01) compared with the control group. The results demonstrate that chronic ingestion of high doses of CAP will decrease the bioavailability of SV to a significant extent in rats.

UI MeSH Term Description Entries
D007654 Ketoconazole Broad spectrum antifungal agent used for long periods at high doses, especially in immunosuppressed patients. Nizoral,R-41400,R41,400,R41400,R 41400
D002211 Capsaicin An alkylamide found in CAPSICUM that acts at TRPV CATION CHANNELS. 8-Methyl-N-Vanillyl-6-Nonenamide,Antiphlogistine Rub A-535 Capsaicin,Axsain,Capsaicine,Capsicum Farmaya,Capsidol,Capsin,Capzasin,Gelcen,Katrum,NGX-4010,Zacin,Zostrix,8 Methyl N Vanillyl 6 Nonenamide,NGX 4010,NGX4010
D002212 Capsicum A plant genus of the family SOLANACEAE. The hot peppers yield CAPSAICIN, which activates VANILLOID RECEPTORS. Several varieties have sweet or pungent edible fruits that are used as vegetables when fresh and spices when the pods are dried. Bell Pepper,Cayenne Pepper,Chili Pepper,Chilli Pepper,Green Pepper,Jalapeno Pepper,Paprika,Pimiento,Red Pepper,Capsicum annuum,Cayenne,Chile Pepper,Hot Pepper,Sweet Pepper,Bell Peppers,Cayenne Peppers,Chile Peppers,Chili Peppers,Chilli Peppers,Green Peppers,Hot Peppers,Jalapeno Peppers,Pepper, Bell,Pepper, Cayenne,Pepper, Chile,Pepper, Chili,Pepper, Chilli,Pepper, Green,Pepper, Hot,Pepper, Jalapeno,Pepper, Red,Pepper, Sweet,Peppers, Bell,Peppers, Cayenne,Peppers, Chile,Peppers, Chili,Peppers, Chilli,Peppers, Green,Peppers, Hot,Peppers, Jalapeno,Peppers, Red,Peppers, Sweet,Red Peppers,Sweet Peppers
D002853 Chromatography, Liquid Chromatographic techniques in which the mobile phase is a liquid. Liquid Chromatography
D003907 Dexamethasone An anti-inflammatory 9-fluoro-glucocorticoid. Hexadecadrol,Decaject,Decaject-L.A.,Decameth,Decaspray,Dexasone,Dexpak,Hexadrol,Maxidex,Methylfluorprednisolone,Millicorten,Oradexon,Decaject L.A.
D005260 Female Females
D000284 Administration, Oral The giving of drugs, chemicals, or other substances by mouth. Drug Administration, Oral,Administration, Oral Drug,Oral Administration,Oral Drug Administration,Administrations, Oral,Administrations, Oral Drug,Drug Administrations, Oral,Oral Administrations,Oral Drug Administrations
D000818 Animals Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA. Animal,Metazoa,Animalia
D000924 Anticholesteremic Agents Substances used to lower plasma CHOLESTEROL levels. Cholesterol Inhibitors,Hypocholesteremic Agents,Anticholesteremic Drugs,Anticholesteremics,Inhibitors, Cholesterol,Agents, Anticholesteremic,Agents, Hypocholesteremic,Drugs, Anticholesteremic
D001682 Biological Availability The extent to which the active ingredient of a drug dosage form becomes available at the site of drug action or in a biological medium believed to reflect accessibility to a site of action. Availability Equivalency,Bioavailability,Physiologic Availability,Availability, Biologic,Availability, Biological,Availability, Physiologic,Biologic Availability,Availabilities, Biologic,Availabilities, Biological,Availabilities, Physiologic,Availability Equivalencies,Bioavailabilities,Biologic Availabilities,Biological Availabilities,Equivalencies, Availability,Equivalency, Availability,Physiologic Availabilities

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