Absorption of clonazepam after intranasal and buccal administration

Serum concentrations of clonazepam after intranasal, buccal and intravenous administration were compared in a cross‐over study in seven healthy male volunteers. Each subject received a 1.0 mg dose of clonazepam intranasally and buccally and 0.5 mg intravenously. A Cmax of 6.3 +/‐ 1.0 ng ml‐1 (mean;...

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Published inBritish journal of clinical pharmacology Vol. 39; no. 4; pp. 449 - 451
Main Authors Schols‐Hendriks, MW, Lohman, JJ, Janknegt, R, Korten, JJ, Merkus, FW, Hooymans, PM
Format Journal Article
LanguageEnglish
Published Oxford, UK Blackwell Publishing Ltd 01.04.1995
Blackwell Science
Subjects
Absorption
Administration, Buccal
Administration, Intranasal
Adult
Anticonvulsants. Antiepileptics. Antiparkinson agents
Biological and medical sciences
Chromatography, High Pressure Liquid
Clonazepam - administration & dosage
Clonazepam - blood
Clonazepam - pharmacokinetics
Cross-Over Studies
Humans
Injections, Intravenous
Male
Medical sciences
Middle Aged
Neuropharmacology
Pharmacology. Drug treatments
Human
Absorption
Sublingual administration
Benzodiazepine derivatives
Anticonvulsant
Normal
Pharmacokinetics
Intranasally administration
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Summary:Serum concentrations of clonazepam after intranasal, buccal and intravenous administration were compared in a cross‐over study in seven healthy male volunteers. Each subject received a 1.0 mg dose of clonazepam intranasally and buccally and 0.5 mg intravenously. A Cmax of 6.3 +/‐ 1.0 ng ml‐1 (mean; +/‐ s.d.) was measured 17.5 min (median) (range 15‐20 min) after intranasal administration. A second peak (4.6 +/‐ 1.3 ng ml‐1) caused by oral absorption was seen after 1.7 h (range 0.7‐3.0 h). After buccal administration a Cmax of 6.0 +/‐ 3.0 ng ml‐1 was measured after 50 min (range 30‐90 min) with a second peak of 6.5 +/‐ 2.5 ng ml‐1 after 3.0 h (range 2.0‐4.0 h). Two minutes after i.v. injection of 0.5 mg clonazepam the serum concentration was 27 +/‐ 18 ng ml‐1. It is concluded that intranasal clonazepam is an alternative to buccal administration. However, the Cmax of clonazepam after intranasal administration is not high enough to recommend the intranasal route as an alternative to intravenous injection.
Bibliography:ObjectType-Article-2
SourceType-Scholarly Journals-1
ObjectType-Feature-1
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ISSN:0306-5251
1365-2125
DOI:10.1111/j.1365-2125.1995.tb04476.x