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Amitriptyline metabolism: Relationship to polymorphic debrisoquine hydroxylation
Author(s) -
Mellström B,
Bertilsson L,
Lou YC,
Säwe J,
Sjöqvist F
Publication year - 1983
Publication title -
clinical pharmacology and therapeutics
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.941
H-Index - 188
eISSN - 1532-6535
pISSN - 0009-9236
DOI - 10.1038/clpt.1983.207
Subject(s) - debrisoquine , demethylation , nortriptyline , hydroxylation , clinical pharmacology , urine , pharmacology , chemistry , plasma levels , amitriptyline , pharmacokinetics , metabolite , metabolism , medicine , cyp2d6 , biochemistry , enzyme , cytochrome p450 , gene expression , dna methylation , gene
Amitriptyline AT demethylation to nortriptyline NT was determined in nine healthy subjects who had been phenotyped with respect to debrisoquine D hydroxylation capacity. AT demethylation was calcuculated from the ratio between the plasma AUCs of NT after single oral doses of AT and NT. Plasma clearance of AT by demethylation did not correlate with the ratio between D and 4‐hydroxy‐D in urine (r s = −0.55). Clinical Pharmacology and Therapeutics (1983) 34, 516–520; doi: 10.1038/clpt.1983.207