Cited by 28Pharmacogenetics and Drug MetabolismPharmaceutical studies and practicesAnimal testing and alternatives

Correlation of Unbound Plasma Clearances of Fifteen Extensively Metabolized Drugs Between Humans and Rats

Chiou, Win L., Hsu, Fung-Hwa·1988·Pharmaceutical Research

Abstract

Unbound plasma clearances (CLu) in humans and rats of 15 extensively metabolized drugs (phenytoin, hexobarbital, pentobarbital, phenylbutazone, warfarin, tolbutamide, valproate, phenobarbital, amobarbital, quinidine, chlorpromazine, propranolol, pentazocin, antipyrine, and diazepam), studied earlier by Sawada et al. (J. Pharmacokin, Biopharm. 13:477-491, 1985), were calculated. It was found that the ratio of CLu per square meter of body surface area between human and rat ranged from 0.38 for pentobarbital to 2.34 for tolbutamide, with a mean ratio of 1.07. When body weight (BW) was used for correlation, the mean CLu was proportional to BW 0.657 +/- 0.0935. A rationale for the above empirical findings is postulated. The present study seems to indicate the existence of a general similarity or predictability in the CLu of drugs between rats and humans. Low correlations were generally obtained when total (bound and unbound) plasma clearances were used for comparison.

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Crossref · 10.1023/a:1015935206569

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Authors
Chiou, W. L., & Hsu, F.-H.
Affiliations
University of Illinois Chicago (US)
Venue
Pharmaceutical Research
Published
1988-10
Volume
5
Issue
10
Pages
668-672
ISSN
  • 0724-8741 (ISSN-L)
  • 1573-904X
OpenAlex
W39205234
Cited by
28
References
35
Citations by year
2024: 1 · 2023: 1 · 2022: 1 · 2019: 1 · 2018: 1 · 2017: 1
FWCI
0.81
Type
journal article
Language
en
Open access
closed
Locations
  • Pharmaceutical Research (publishedVersion)
  • PubMed (publishedVersion)
Topics
  • Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmacology › Pharmacogenetics and Drug Metabolism
  • Health Sciences › Medicine › Pediatrics, Perinatology and Child Health › Pharmaceutical studies and practices
  • Health Sciences › Veterinary › Small Animals › Animal testing and alternatives
Keywords
human-rat comparison, body surface area, body weight, drug metabolism, phenytoin, barbiturates, antiepileptic drugs, antipsychotic drugs, antihypertensive drugs, antipyrine, diazepam, warfarin, quinidine, chlorpromazine, propranolol, tolbutamide, valproic acid
MeSH terms
Animals, Body Surface Area, Pharmaceutical Preparations, Humans, Liver, Male, Species Specificity, Rats

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