Gender differences in the pharmacokinetics of rivastigmine in rats.
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.
Arumugam
Karthik
K
Manipal College of Pharmaceutical Sciences, Manipal University, Manipal, Karnataka, India.
Chamallamudi
Mallikarjuna Rao
MR
Mallayasamy
Surulivel Rajan
SR
Ganesan
Subramanian
S
Shavi
Gopal V
GV
Averineni
Ranjithkumar
R
Reddy
Ravindranath
R
Bhat
Krishnamurthy
K
Udupa
Nayanabhirama
N
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
D018696:Neuroprotective Agents; D048448:Phenylcarbamates; D012996:Solutions; D000068836:Rivastigmine