Romanian Society of Pharmaceutical Sciences
 

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INFLUENCE OF FLUVOXAMINE ON CARVEDILOL'S PHARMACOKINETICS IN RATS

MARIA BIANCA ABRUDAN 1, DANA MARIA MUNTEAN 1*, LAURIAN VLASE 1, ANA-MARIA GHELDIU 1, CRISTIAN BERCE 2, LAURENȚIU STOICESCU 3, MARIA ADRIANA NEAG 4

1.Department of Pharmaceutical Technology and Biopharmaceutics, Faculty of Pharmacy, “Iuliu Hațieganu” University of Medicine and Pharmacy, 41 Victor Babeș, Cluj-Napoca 400012, Romania
2 .Centre for Experimental Medicine, “Iuliu Hațieganu” University of Medicine and Pharmacy, 6 Louis Pasteur, Cluj-Napoca 400349, Romania
3 .Department of Cardiology, Vth Medical Clinic, Clinical Municipal Hospital, “Iuliu Hațieganu” University of Medicine and Pharmacy, Faculty of Medicine, 11 Tăbăcarilor, Cluj-Napoca 400139, Romania
4 .Department of Pharmacology, Toxicology and Clinical Pharmacology, Faculty of Medicine, “Iuliu Hațieganu” University of Medicine and Pharmacy, 41 Victor Babeș, Cluj-Napoca 400012, Romania

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Carvedilol is one of the most used cardiovascular drugs, highly metabolized by CYP450 2D6, 1A2, 2C9. Fluvoxamine, an antidepressant agent, is a moderate/potent inhibitor of these enzymes. There is the risk of drug-drug interaction when these two drugs are concomitantly administered. The aim of this study was to investigate the drug-drug interactions between carvedilol and fluvoxamine in rats. There were two periods: reference and test. In the first period each rat received an oral dose of 3.57 mg/kg body weight carvedilol. In the test period, carvedilol was administered after a pre-treatment with multiple oral doses of fluvoxamine (14.28 mg/kg b.w.). HPLC-MS was used to determine the plasma concentration of carvedilol. The PK parameters were calculated by non-compartmental analysis. Fluvoxamine co-administered with carvedilol can change the PK parameters (increase AUC, t1/2, decrease the Cl). The present study demonstrated the pharmacokinetic drug-drug interaction between carvedilol and fluvoxamine in vivo.