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 half-life (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.

Original languageEnglish
Pages (from-to)493-497
Number of pages5
JournalArzneimittel-Forschung/Drug Research
Volume59
Issue number10
Publication statusPublished - 2009

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Rivastigmine
Pharmacokinetics
Area Under Curve
Gonadal Hormones
Intravenous Administration
Half-Life
Testosterone
Wistar Rats

All Science Journal Classification (ASJC) codes

  • Drug Discovery

Cite this

Arumugam, Karthik ; Chamallamudi, Mallikarjuna Rao ; Mallayasamy, Surulivel Rajan ; Ganesan, Subramanian ; Shavi, Gopal V. ; Averineni, Ranjithkumar ; Reddy, Ravindranath ; Bhat, Krishnamurthy ; Udupa, Nayanabhirama. / Gender differences in the pharmacokinetics of rivastigmine in rats. In: Arzneimittel-Forschung/Drug Research. 2009 ; Vol. 59, No. 10. pp. 493-497.
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Gender differences in the pharmacokinetics of rivastigmine in rats. / Arumugam, Karthik; Chamallamudi, Mallikarjuna Rao; Mallayasamy, Surulivel Rajan; Ganesan, Subramanian; Shavi, Gopal V.; Averineni, Ranjithkumar; Reddy, Ravindranath; Bhat, Krishnamurthy; Udupa, Nayanabhirama.

In: Arzneimittel-Forschung/Drug Research, Vol. 59, No. 10, 2009, p. 493-497.

Research output: Contribution to journalArticle

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AU - Arumugam, Karthik

AU - Chamallamudi, Mallikarjuna Rao

AU - Mallayasamy, Surulivel Rajan

AU - Ganesan, Subramanian

AU - Shavi, Gopal V.

AU - Averineni, Ranjithkumar

AU - Reddy, Ravindranath

AU - Bhat, Krishnamurthy

AU - Udupa, Nayanabhirama

PY - 2009

Y1 - 2009

N2 - 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 half-life (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.

AB - 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 half-life (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.

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