Stereoselective pharmacokinetics of 3,4‐methylenedioxymethamphetamine in the rat
Robert L. Fitzgerald, Robert V. Blanke, Alphonse Poklis
Chirality 1990 DOI: 10.1002/chir.530020409 (opens in new tab)
Study at a glance
AI-extracted from the abstract| Characteristics | Pharmacokinetic study Peer reviewed |
|---|---|
| Population | Rats |
| Intervention | racemic MDMA |
| Dose | 20 and 40 mg/kg for subcutaneous; 10 and 20 mg/kg for intravenous |
| Topics | MDMA |
| Keywords | Pharmacokinetics Pharmacology Metabolite Dosing Toxicokinetics |
| Citations | 50 |
| Key points | The (+)-(S)-MDMA enantiomer is cleared more rapidly than (−)-(R)-MDMA, with average half-lives of 2.2 and 2.5 hours, respectively. |
Abstract
Abstract Studies to characterize the pharmacokinetics of the enantiomers of MDMA were conducted in rats using the iliac arterial cannulation. Two routes of administration, intravenous and subcutaneous, were evaluated at two dose levels for each route [20 and 40 mg/kg (±)‐MDMA for subcutaneous, 10 and 20 mg/kg (±)‐MDMA for intravenous administrations]. The average half‐life (±SD) for all dosing groups was 2.5 ± 0.8 h for (−)‐(R)‐MDMA and 2.2 ±0.8 h for (+)‐(S)‐MDMA. The more rapid clearnace of (+)‐(S)‐MDMA compared with (−)‐(R)‐MDMA is consistent with the area under the curve (AUC) data of the parent drug and its primary metabolite MDA. The mean (±SD) AUC S/R ratios of MDMA and MDA were 0.70 ± 0.05 and 3.1 ± 0.8, respectively. Following a 20 mg/kg dose of racemic MDMA iv the mean (±SD) of the percent dose excreted as (−)‐(R)‐MDMA, (+)‐(S)‐MDMA, (−)‐(R)‐MDA, and (+)‐(S)‐MDA were 20 ± 10, 12 ± 6, 3 ± 1, and 6 ± 2, respectively.
Comparable studies
Other preclinical and animal studies on MDMA, most cited first.
Citations in the library
Cited by 12
- Stereospecific Analysis and Enantiomeric Disposition of 3,4-Methylenedioxymethamphetamine (Ecstasy) in Humans Clinical Chemistry July 1, 1999
- Reinforcing Effects of MDMA (‘Ecstasy’) in Drug-Naive and Cocaine-Trained Rats Pharmacology 2001
- A developmental comparison of the neurobehavioral effects of ecstasy (MDMA) Neurotoxicology and Teratology October 21, 2006
- Synthetic Aminoindanes: A Summary of Existing Knowledge Frontiers in Psychiatry November 17, 2017
- Acute effects of 3,4-methylenedioxymethamphetamine (MDMA) and R(-) MDMA on actigraphy-based daytime activity and sleep parameters in rhesus monkeys. Experimental and Clinical Psychopharmacology June 25, 2018
and 7 more in the library
Cites 8
- Neurotoxicity of the psychedelic amphetamine, methylenedioxymethamphetamine. Journal of Pharmacology and Experimental Therapeutics 1987
- 3,4-Methylenedioxymethamphetamine and 3,4-methylenedioxyamphetamine destroy serotonin terminals in rat brain: quantification of neurodegeneration by measurement of [3H]paroxetine-labeled serotonin uptake sites. Journal of Pharmacology and Experimental Therapeutics September 1, 1987
- Hallucinogenic Amphetamine Selectively Destroys Brain Serotonin Nerve Terminals Science September 6, 1985
- (±3,4-Methylenedioxymethamphetamine Selectively Damages Central Serotonergic Neurons in Nonhuman Primates JAMA July 1, 1988
- ECSTACY: A Review of MDMA and MDA The International Journal of Psychiatry in Medicine December 1, 1987
and 3 more in the library