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At least 19 recordsLinked to original sources
PubMed1978

Mass fragmentographic determination of methadyl acetate in urine using stable isotope labeled analog as internal standard.

A quantitative GLC-mass spectrometric assay was developed for the determination of methadyl acetate in urine. The assay utilized selective ion focusing to monitor, in a GLC effluent, the M--15 ion generated by electron-impact ionization of methadyl acetate. Methadyl acetate-d4 was used as an internal standard. The assay can measure 10 ng of drug/ml with about 6% precision. The curve relating the amounts of drug added to control urine versus the amounts experimentally found over a large concentration range is a straight line with a slope of 0.98 +/- 0.02 and a nearly zero intercept. Assay specificity was confirmed by complete identity of the mass spectrum of methadyl acetate in the biological extract with that of the authentic material. The method was used for the urinary analysis of methadyl acetate in a rabbit given a single intravenous dose. The animal excreted less than 1% of the intact drug with a half-life of approximately 15 hr. Consequently, the long-acting characteristic of methadyl acetate must be attributed to its metabolism into active metabolites.

Animals↗
PubMed1977

Methadyl acetate and methadone. An open comparison.

Heroin addicts were recruited for a 14-week open clinical comparison of methadone hydrochloride and methadyl acetate. Patients were randomly assigned to a methadyl acetate clinic in which methadyl acetate was dispensed to patients three times per week or to a methadone clinic in which methadone was dispensed six days per week. No statistically significant differences were observed between groups in retention rates, illicit drug use, employment rates, or arrest rates. The group treated with methadyl acetate had more dropouts in the first seven weeks than the second seven weeks: this pattern was reversed for the methadone-treated group. The differences were significant (P = .01). Spontaneously reported symptoms suggest that induction with methadyl acetate may be a more clinically variable phenomenon than induction with methadone. The reduction of number of clinic visits in the group treated with methadyl acetate was not a source of variance in treatment effectiveness.

Adult↗
PubMed1976

Methadyl acetate and methadone as maintenance treatments for heroin addicts. A veterans administration cooperative study.

This was a double-blind comparison of methadyl acetate and two dose levels of methadone hydrochloride in the maintenance of 430 street heroin addicts from 12 Veterans Administration hospitals. The starting sample consisted of 146 patients receiving low-dose methadone, 142 patients receiving methadyl acetate. Patients were first given 30 mg of both drugs, and doses were incremented by 10 mg/week until they stabilized at methadyl acetate, 80 mg three times a week, and methadone hydrochloride, 50 mg daily or 100 mg daily. Dosage was fixed for the balance of the 40-week treatment period. Safety was evaluated by clinical and laboratory observations conducted at frequent intervals throughout the study. Relative efficacy was evaluated by illicit drug use, program retention and attendance, and global staff judgments. It is concluded that methadyl acetate is as safe a drug as methadone and that it compares favorably with highdose methoadone in terms of efficacy. Both methyadyl acetate and high-dose methadone appear to be better maintenance regimens than low-dose methadone under the conditions of this study.

Adolescent↗
PubMed1978

A cooperative clinical study of methadyl acetate. I. Three-times-a-week regimen.

This was an open clinical trial of methadyl acetate (LAAM) compared with methadone in the maintenance of 636 heroin addicts who had previously been stabilized on a maintenance regimen of methadone. The starting sample assembled by the 13 cooperating clinics were randomly assigned to continued maintenance on methadone (= 308) or crossed over to methadyl acetate (= 328) for a period of 40 weeks. The starting dose was identical to the previously established dose of methadone, but beginning with the second visit, dosage was flexible. Safety was evaluated by clinical and laboratory observations conducted at four-week intervals throughout the study. Relative efficacy was evaluated by illicit drug use, program retention and attendance, and global staff judgments. It is concluded that methadyl acetate is as safe as methadone and, when given three times a week, is an acceptable and effective maintenance drug for many heroin addicts.

Adult↗
PubMed1977

Methadyl acetate versus methadone: the experience of one hospital.

Sixty subjects participated in a double-blind study comparing methadyl acetate (80 mg) with two dosages of methadone (50 mg and 100 mg) in the maintenance of opiate addicts. The safety of all three regimens was supported and methadyl acetate was as effective as methadone in the retention of subjects.

Adult↗
PubMed1978

Chromosomes in patients receiving methadone and methadyl acetate.

Chromosomes of peripheral leukocytes were examined in 28 addicts participating in a Veterans Administration-Special Action Office for Drug Abuse Prevention (SAODAP) cooperative study of methadyl acetate vs methadone. Blood samples for 72-hour leukocyte cultures were drawn after nearly 40 weeks of maintenance therapy while subjects were receiving active medication. For comparison, ten nondrug users were also studied. The frequency of chromosome damage was not greater in subjects maintained on methadyl acetate or methadone than in nondrug users.

Adult↗
PubMed1978

Acceptability of methadyl acetate (LAAM) as compared with methadone in a treatment program for heroin addicts.

Heroin addicts who had been maintained for at least three months on LAAM (levo-alpha-acetylmethadol, methadyl acetate) and at least three months on methadone were asked to compare the two drugs on a number of criteria. The responses were highly selective, indicating that a desire to please the investigators was not an important factor. Overwhelmingly, the majority of patients reported that LAAM provided better heroin "blockade", that it was more effective in reducing craving, and that actual use of heroin was less on LAAM than on methadone. In other respects, such as sexual performance, sleep, and appetite, most patients perceived no difference between the drugs. In no respect was methadone preferred by a majority, although methadone was viewed more favorably on some criteria by some patients. These findings indicate that for most heroin addicts LAAM will be an acceptable maintenance drug.

Heroin Dependence↗
PubMed1976

Extraction method and thin-layer chromatographic system for the determination of alpha-l-acetylmethadol and metabolites in biological fluids.

An extraction method and thin-layer chromatographic (TLC) system for the determination of alpha-l-acetylmethadol and its known metabolites (methadol, noracetylmethadol, dinoracetylmethadol, normethadol, 6-acetamide-4,4-diphenyl-3-heptanol, and N-methyl-6-acetamido-4,4-diphenyl-3-heptanol) are described. The parent drug and metabolites are extracted from biological fluids with ethyl acetate and separated by TLC using silica gel plates and a developing system of ethyl acetate-methanol-water-ammonia (85:10:1:1). This system may be used to quantitatively determine levels of radiolabeled drug and metabolites by scraping the TLC plates into 3-mm zonal fractions and measuring the amount of radioactivity by scintillation counting. A representative radiochromatogram obtained from an extract of monkey urine is shown.

Animals↗
PubMed1977

Failure of methadone and levomethadyl acetate (levo-alpha-acetylmethadol, LAAM) maintenance to affect memory.

Memory tests were administered to 30 patients taking methadone hydrochloride and 31 taking levomethadyl acetate (levo-alpha-acetylmethadol, LAAM) both prior to treatment and after one and three months of continuous treatment. A group of nonopiate using matched control subjects was administered the tests at similar intervals. No statistically significant difference in test performance was found among these groups at any of the three sessions. The methadone and control groups also did not differ significantly in the frequency of subjective reports of decreased memory function. Previous reports of memory deflicits during long-term methadone administration may be a result of comparing methadone and control groups at a single point in time and assuming that prior to methadone maintenance the groups were equivalent.

Adult↗
PubMed1975

Disposition of acetylmethadol in relation to pharmacologic action.

The levels of acetylmethadol and its active biotransformation products were quantitated in the plasma and urine of subjects on acetylmethadol maintenance by the use of solvent extraction and gas-liquid chromatography. The time-course of plasma acetylmethadol, noracetylmethadol, and dinoracetylmethadol over 48 hr was determined concurrently with the time-action of pupillary constriction in 8 subjects receiving an average oral maintenance dose of 50 mg. The plasma level of acetylmethadol reached a peak at 4 hr and had nearly disappeared by 24 hr. The mean apparent half-life was 7 hr. The plasma level of noracetylmethadol peaked at 4 to 8 hr and slowly declined over the next 40 hr. The mean apparent half-life of noracetylmethadol was 48 hr. Dinoracetylmethadol plasma levels remained relatively constant throughout the dosing interval. The miotic effect reached a peak at 8 hr and decayed at a rate slower than that of plasma elimination of acetylmethadol but more rapidly than that of noracetylmethadol and dinoracetylmethadol. Substantial variation in the plasma levels of the compounds was observed in subjects after the same doses. The study indicated that the relatively long duration of opiate effects of acetylmethadol results from biotransformation to active and persistent metabolites.

Adult↗
PubMed1977

Plasma l-alpha-Acetylmethadol (LAAM) after acute and chronic administration.

l-alpha-Acetylmethadol (LAAM) was administered orally to two groups of subjects; one group received methadone, 50 mg/day, for three months previously and the other group were heroin addicts who had no prior exposure to methadone or LAAM. Plasma elimination curves for methadone, LAAM, and its metabolites, noracetylmethadol (N-LAAM) and dinoracetylmethadol (DN-LAAM), were determined after acute and chronic administration. The plasma decay curve for LAAM was biexpoenential (t1/2alpha = 6 hr; t1/2beta greater than 50 hr) following acute or chronic administration. Following chronic administration, N-LAAM and DN-LAAM plasma levels increased 5- to 10-fold. At this time, N-LAAM had a t1/2 of 31 hr and DN-LAAM had a t1/2 of greater than 100 hr. There appear to be at least two factors which determine the long duration of action of LAAM: metabolic conversion to active metabolites and tissue or plasma binding. Both methadone and LAAM may compete for plasma protein or tissue binding sites. The clinical implications of this potential drug-drug interaction are discussed.

Adult↗
PubMed1977

Head-shake distributions during self-maintained dependence on morphine, methadone, and l-alpha-acetylmethadol (LAAM) in the rat.

Adult female Sprague-Dawley rats were prepared with chronic cortical and muscle electrodes and i.v. cannulas, made tolerant to and physically dependent on morphine, and trained to level press for i.v. morphine self-injections to maintain dependence. Methadone or l-alpha-acetylmethadol (LAAM) was then substituted for morphine in some of these rats. During self-maintained dependence on either morphine or methadone, head shakes appeared and increased in frequency before lever pressing for self-injections. In contrast, there were fewer head shakes during LAAM dependence, which were evenly distributed over the entire duration of the interinjection interval. These findings suggest a relationship between head-shake distributions, drug-seeking behavior and the pharmacodynamics of these three narcotics.

Animals↗