title: Gender differences in the pharmacokinetics of rivastigmine in rats.
abstract: The effect of gender on the pharmacokinetics of rivastigmine (CAS 123441-03-2) was studied in male and female Wistar rats following intravenous bolus administration. The area under the plasma concentration-time curve (AUC), apparent volume of distribution (Vd), systemic clearance (CL), and terminal plasma halflife (t1/2) of rivastigmine were compared between male and female rats. Compared to male rats, female rats exhibited higher plasma rivastigmine levels showing significantly (p < 0.05) larger AUC (226.77 vs. 149.68 ng h/ml), Vd (6.70 vs. 4.13 L), t1/2 (0.84 vs. 0.34 h) and a lower CL (5.51 vs. 8.35 L/h). The male rats had a 2.5 fold greater elimination rate constant than female rats (2.02 vs. 0.82 h(-1)). Gender had a significant effect on the pharmacokinetics of rivastigmine. Gender differences were reported due to gonadal hormones, and the observed difference in pharmacokinetics of rivastigmine might be attributed to testosterone in male rats.
authors.affiliation: Manipal College of Pharmaceutical Sciences, Manipal University, Manipal, Karnataka, India.
authors.forename: Karthik
authors.initials: K
authors.lastname: Arumugam
authors.forename: Mallikarjuna Rao
authors.initials: MR
authors.lastname: Chamallamudi
authors.forename: Surulivel Rajan
authors.initials: SR
authors.lastname: Mallayasamy
authors.forename: Subramanian
authors.initials: S
authors.lastname: Ganesan
authors.forename: Gopal V
authors.initials: GV
authors.lastname: Shavi
authors.forename: Ranjithkumar
authors.initials: R
authors.lastname: Averineni
authors.forename: Ravindranath
authors.initials: R
authors.lastname: Reddy
authors.forename: Krishnamurthy
authors.initials: K
authors.lastname: Bhat
authors.forename: Nayanabhirama
authors.initials: N
authors.lastname: Udupa
mesh_terms: D000818:Animals; D002851:Chromatography, High Pressure Liquid; D005260:Female; D006207:Half-Life; D007275:Injections, Intravenous; D008297:Male; D018696:Neuroprotective Agents / Q000097:blood / Q000493:pharmacokinetics*; D009919:Orchiectomy; D048448:Phenylcarbamates / Q000097:blood / Q000493:pharmacokinetics*; D051381:Rats; D017208:Rats, Wistar; D012015:Reference Standards; D015203:Reproducibility of Results; D000068836:Rivastigmine; D012727:Sex Characteristics; D012996:Solutions
chemical_list: D018696:Neuroprotective Agents; D048448:Phenylcarbamates; D012996:Solutions; D000068836:Rivastigmine