Journal article
Pharmacokinetics of high doses of intramuscular and oral heroin in narcotic addicts.
- Girardin F Division of Clinical Pharmacology and Toxicology, Department of Medicine, University Hospital, Zürich, Switzerland.
- Rentsch KM
- Schwab MA
- Maggiorini M
- Pauli-Magnus C
- Kullak-Ublick GA
- Meier PJ
- Fattinger K
- 2003-10-10
Published in:
- Clinical pharmacology and therapeutics. - 2003
Administration, Oral
Adult
Area Under Curve
Biological Availability
Female
Half-Life
Heroin
Heroin Dependence
Humans
Injections, Intramuscular
Injections, Intravenous
Male
Metabolic Clearance Rate
Narcotics
English
BACKGROUND
In several countries medical prescription of diacetylmorphine is currently being evaluated as a treatment option for heavily dependent narcotic addicts. Because of damaged veins, many patients administer diacetylmorphine intramuscularly or orally. Therefore we characterized the pharmacokinetics of intramuscular and oral diacetylmorphine in the high dose range usually required in narcotic addicts.
METHODS
Three intramuscular doses, 3 oral doses, and 1 intravenous dose of diacetylmorphine and oral and intravenous test doses of deuterium-labeled morphine (morphine-N-methyl-d3 [morphine-d3]) were administered to 8 heroin-addicted patients. Arterial plasma concentrations of diacetylmorphine, monoacetylmorphine, morphine, morphine-3-glucuronide, morphine-6-glucuronide, and morphine-d3 were measured by liquid chromatography-mass spectrometry.
RESULTS
Intramuscularly administered diacetylmorphine (
CONCLUSIONS
On the basis of the linear pharmacokinetics, the high bioavailability of intramuscular diacetylmorphine, and the rapid and extended morphine absorption from oral diacetylmorphine, the intramuscular and oral routes can be recommended as safe and feasible alternatives to the intravenous route for medical prescription of diacetylmorphine.
In several countries medical prescription of diacetylmorphine is currently being evaluated as a treatment option for heavily dependent narcotic addicts. Because of damaged veins, many patients administer diacetylmorphine intramuscularly or orally. Therefore we characterized the pharmacokinetics of intramuscular and oral diacetylmorphine in the high dose range usually required in narcotic addicts.
METHODS
Three intramuscular doses, 3 oral doses, and 1 intravenous dose of diacetylmorphine and oral and intravenous test doses of deuterium-labeled morphine (morphine-N-methyl-d3 [morphine-d3]) were administered to 8 heroin-addicted patients. Arterial plasma concentrations of diacetylmorphine, monoacetylmorphine, morphine, morphine-3-glucuronide, morphine-6-glucuronide, and morphine-d3 were measured by liquid chromatography-mass spectrometry.
RESULTS
Intramuscularly administered diacetylmorphine (
CONCLUSIONS
On the basis of the linear pharmacokinetics, the high bioavailability of intramuscular diacetylmorphine, and the rapid and extended morphine absorption from oral diacetylmorphine, the intramuscular and oral routes can be recommended as safe and feasible alternatives to the intravenous route for medical prescription of diacetylmorphine.
- Language
-
- English
- Open access status
- closed
- Identifiers
-
- DOI 10.1016/S0009-9236(03)00199-1
- PMID 14534521
- Persistent URL
- https://folia.unifr.ch/global/documents/210701
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