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Antimicrobial Agents and Chemotherapy, August 2003, p. 2458-2463, Vol. 47, No. 8
0066-4804/03/$08.00+0     DOI: 10.1128/AAC.47.8.2458-2463.2003
Copyright © 2003, American Society for Microbiology. All Rights Reserved.

Pharmacokinetics and Metabolism of [14C]Viramidine in Rats and Cynomolgus Monkeys

Chin-Chung Lin,* Kenneth Luu, David Lourenco, and Li-Tain Yeh

Research and Development, Ribapharm, Inc., Costa Mesa, California 92626

Received 10 February 2003/ Returned for modification 21 March 2003/ Accepted 5 May 2003

The pharmacokinetics of [14C]viramidine, a prodrug of ribavirin, were studied in rats (30 mg/kg of body weight) and monkeys (10 mg/kg) following intravenous (i.v.) and oral administration. The levels of oral absorption and bioavailabilities were 61.7 and 9.91%, respectively, in rats and 43.9 and 13.6%, respectively, in monkeys. Following i.v. administration, the elimination half-lives were 2.7 h in rats and 28.9 h in monkeys. Total body clearances were 14.0 liters/h/kg in rats and 1.23 liters/h/kg in monkeys; the apparent volumes of distribution were 15.6 liters/kg in rats and 18.6 liters/kg in monkeys. Following oral administration, viramidine was extensively converted to ribavirin, followed by further metabolism of ribavirin in both species, with a faster rate of metabolism in rats than in monkeys. In rats, excretion of total radioactivity in urine accounted for 77.0% of the i.v. dose and 60.8% of the oral dose, while in monkeys it accounted for 44.4% of the i.v. dose and 39.0% of the oral dose. The amount of unchanged viramidine and ribavirin in urine was small in both species after i.v. and oral administration of viramidine.

* Corresponding author. Mailing address: Ribapharm, Inc., 3300 Hyland Ave., Costa, Mesa, CA 92626. Phone: (714) 427-6236, ext. 2062. Fax: (714) 641-7201. E-mail: cclin{at}ribapharm.com.

Antimicrobial Agents and Chemotherapy, August 2003, p. 2458-2463, Vol. 47, No. 8
0066-4804/03/$08.00+0     DOI: 10.1128/AAC.47.8.2458-2463.2003
Copyright © 2003, American Society for Microbiology. All Rights Reserved.



This article has been cited by other articles:

  • Lin, C.-c., Xu, C., Zhu, N., Yeh, L.-T. (2006). Absorption, Metabolism, and Excretion of [14C]Viramidine in Humans.. Antimicrob. Agents Chemother. 50: 2368-2373 [Abstract] [Full Text]  
  • Wu, J. Z., Larson, G., Hong, Z. (2004). Dual-Action Mechanism of Viramidine Functioning as a Prodrug and as a Catabolic Inhibitor for Ribavirin. Antimicrob. Agents Chemother. 48: 4006-4008 [Abstract] [Full Text]  
  • Lin, C.-C., Lourenco, D., Xu, G., Yeh, L.-T. (2004). Disposition and Metabolic Profiles of [14C]Viramidine and [14C]Ribavirin in Rat and Monkey Red Blood Cells and Liver. Antimicrob. Agents Chemother. 48: 1872-1875 [Abstract] [Full Text]  


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