Methaqualone pharmacokinetics after single- and multiple-dose administration in man

Drug Kinetics and Artificial Kidneys1

“…3 Furesz et al (1967) 6-6.5 5 Iwainsky et al (1974 0 3.0 5 65-80 Mannisto (1977) 2 to 2.8±0.8 Acocella et al (1972) '" 88.9± 1.0 Boman and Ringberger(1974) :j' , (1956)(1957) :::l 11.0 ± 2.3 EG Geraci et al ( 1956Geraci et al ( -1957 Thomson et al (1973) .j:> w :::l 11 Reidenberg et al (1975) a. Stanski et al (1976) Olsen et al (1975 Clements and Prescott ( Cummins et al (1971) Curry et al (1971) Maher (1970 Forsman and Ohman (1976) Forsman et al (1974) Hughes et al (1976) Greenblatt et al (1977) Nayak et al (1974 Christensen and Holfort (1975) Alvan et al (1974) Tognoni et al (1975) Shull et al (1976) Ehrnebo (1974) Smith et al (1973) Bloomer (1966 Goldbaum and Smith (1954) Reidenberg et al (1976) Butler et al (1954) Campion and North (1965) Bloomer (1966 Jorgensen andWeith (1963) Fazekas et al (19561 Clifford et al (1974) Smith (1954) Bloomer( 1966) …”

The kinetics of the urinary excretion of the N-oxide and glucuronides of methaqualone in man

“…Their study involved the use of isotopic dilution and field ionisation mass spectrometry which had a limit of sensitivity for urine samples of 200 pg cm -3. This was much lower than that achievable by the chromatographic procedure in the current work or the spectrofluorometric technique used by Nayak et al (15).…”

“…The post-absorption phase was biexponential. Values of all the kinetic parameters calculated from the serum data together with the corresponding values previously reported by Alvan et of (14) and Nayak et of (15) are presented in Table I. For a given subject, the semi logarithmic plots of the rate of metabolite excretion against time for the six metabolites were not parallel to the plot for methaqualone excretion.…”

The effect of some formulation variables on the bioequivalence of methaqualone preparations

“…We feel in the particular case of hypnotics which have very long half-lives, e.g. methaqualone (Alvan et a/., 1973,1974), barbiturates (Clifford et al, 1974), nitrazepam (Reider, 1973), that the total amount of drug reaching the systemic circulation as indicated by AUCm bears no useful relationship to the effect of a drug designed for acute administration: it is the initial time/plasma concentration relationship which is important and requires definition as has been discussed with particular reference to methaqualone by Alvan et al (1973,1974) and Nayak et al (1974). The 'useful time', which is the time during which the hypnotic effect is required, for methaqualone is the initial 6-h period following its administration, and it is during this period of time that our studies have been conducted.…”