TY - JOUR
T1 - Noninteraction of temazepam and cimetidine
AU - Greenblatt, David J.
AU - Abernethy, Darrell R.
AU - Divoll, Marcia
AU - Locniskar, Ann
AU - Harmatz, Jerold S.
AU - Shader, Richard I.
N1 - Funding Information:
ACKNOWLEDGMENTS Supported in part by United States Public Health Service Grant MH-34223, by a Clinical Pharmacology Developmental Grant from The Pharmaceutical Manufacturers’ Association Foundation, and by a Grant-in-Aid from Sandoz, Inc.
PY - 1984/3
Y1 - 1984/3
N2 - The possible kinetic interaction of the hypnotic temazepam and the H2‐receptor antagonist cimetidine was evaluated. Nine healthy male and female volunteers received a 30‐mg oral dose of temazepam on two occasions in random sequence, separated by at least 1 week. On one occasion, temazepam was given in the otherwise drug‐free state; on the other, temazepam was given with concurrent administration of cimetidine, 300 mg every 6 h. Mean pharmacokinetic parameters for temazepam in control versus cimetidine trials were: peak plasma concentration, 560 versus 498 ng/mL; time of peak concentration, 2.0 versus 2.1 h after the dose; volume of distribution, 1.30 versus 1.39 L/kg; elimination half‐life, 9.9 versus 11.4 h; total clearance, 1.59 versus 1.60 mL/min/kg; free fraction of temazepam in plasma, 4.1 versus 3.8% unbound. Cimetidine has been shown to reduce the metabolic clearance of the benzodiazepines that are biotransformed by oxidative mechanisms. Temazepam, transformed by conjugation, appears unaffected by the coadministration of cimetidine.
AB - The possible kinetic interaction of the hypnotic temazepam and the H2‐receptor antagonist cimetidine was evaluated. Nine healthy male and female volunteers received a 30‐mg oral dose of temazepam on two occasions in random sequence, separated by at least 1 week. On one occasion, temazepam was given in the otherwise drug‐free state; on the other, temazepam was given with concurrent administration of cimetidine, 300 mg every 6 h. Mean pharmacokinetic parameters for temazepam in control versus cimetidine trials were: peak plasma concentration, 560 versus 498 ng/mL; time of peak concentration, 2.0 versus 2.1 h after the dose; volume of distribution, 1.30 versus 1.39 L/kg; elimination half‐life, 9.9 versus 11.4 h; total clearance, 1.59 versus 1.60 mL/min/kg; free fraction of temazepam in plasma, 4.1 versus 3.8% unbound. Cimetidine has been shown to reduce the metabolic clearance of the benzodiazepines that are biotransformed by oxidative mechanisms. Temazepam, transformed by conjugation, appears unaffected by the coadministration of cimetidine.
KW - Cimetidine—noninteraction with temazepam, pharmacokinetics
KW - Pharmacokinetics—noninteraction of temazepam and cimetine
KW - Temazepam—noninteraction with cimetidine, pharmacokinetics
UR - http://www.scopus.com/inward/record.url?scp=0021364624&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=0021364624&partnerID=8YFLogxK
U2 - 10.1002/jps.2600730329
DO - 10.1002/jps.2600730329
M3 - Article
C2 - 6143815
AN - SCOPUS:0021364624
VL - 73
SP - 399
EP - 401
JO - Journal of Pharmaceutical Sciences
JF - Journal of Pharmaceutical Sciences
SN - 0022-3549
IS - 3
ER -