ISSN:
1432-1041
Keywords:
Drug metabolism
;
methaqualone
;
methaqualone metabolites
;
interindividual variation
Source:
Springer Online Journal Archives 1860-2000
Topics:
Chemistry and Pharmacology
,
Medicine
Notes:
Summary The urinary excretion of fiveC-monohydroxy metabolites and theN-oxide metabolite of methaqualone in the 24h period immediately after oral dosing with 250 mg methaqualone (Melsed) has been measured in nineteen healthy adults (13 male, 6 female) to assess interindividual variations and in five adults (3 male, 2 female) on five separate occasions to assess intraindividual variations. The overall importance of the six metabolites was 4′-hydroxy $$ 〉 〉 $$ N-oxide $$ 〉 〉 $$ 2′-hydroxymethyl 〉 3′-hydroxy 〉 6-hydroxy = 2-hydroxymethyl. Variations in this order both within the 24h period and within each of the three eight-hour periods constituting the 24 hours were minor and variations in the absolute amount of each metabolite excreted ranged from two to three-fold. Intraindividual variations were generally smaller than interindividual variations and for each individual the pattern of metabolism was similar on the five occasions. There is evidence that theC-oxidation of methaqualone may be more sensitive to cyclical variations in hormone levels than isN-oxidation.
Type of Medium:
Electronic Resource
URL:
http://dx.doi.org/10.1007/BF00716365
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