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Clinical Pharmacokinetics
Published in: Clinical Pharmacokinetics 3/2004

01-03-2004 | Review Article

Clinical Pharmacokinetics of Amfetamine and Related Substances

Monitoring in Conventional and Non-Conventional Matrices

Authors: Rafael de la Torre, Magí Farré, Mónica Navarro, Roberta Pacifici, Piergiorgio Zuccaro, Dr Simona Pichini

Published in: Clinical Pharmacokinetics | Issue 3/2004

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Abstract

Consumption of amfetamine-type stimulants, including classical amfetamines and ‘designer drugs’, has been recognised as one of the most significant trends in drug abuse at the end of the past century and at the beginning of the current one. The first cause is the increasing consumption amongst youth of methylenedioxy- and methoxy-substituted amfetamines, of which the pharmacology in humans is currently under investigation. Secondly, the abuse of more classical amfetamines, such as amfetamine itself and metamfetamine, continues to be highly prevalent in some geographical regions.
Amfetamines are powerful psychostimulants, producing increased alertness, wakefulness, insomnia, energy and self-confidence in association with decreased fatigue and appetite as well as enhanced mood, well-being and euphoria. From a clinical pharmacokinetic perspective, amfetamine-type stimulants are rather homogeneous. Their oral bioavailability is good, with a high distribution volume (4 L/kg) and low binding to plasma proteins (less than 20%). The elimination half-life is 6–12 hours. Both hepatic and renal clearance contribute to their elimination from the body. Hepatic metabolism is extensive in most cases, but a significant percentage of the drug always remains unaltered.
Amfetamine and related compounds are weak bases, with a pKa around 9.9, and a relatively low molecular weight. These characteristics allow amfetamine-type stimulants to diffuse easily across cell membranes and lipid layers and to those tissues or biological substrates with a more acidic pH than blood, facilitating their detection in alternative matrices at relatively high concentrations. In most cases, the concentrations found are higher than expected from the Henderson-Hasselbach equation. Drug monitoring in non-conventional biological matrices (e.g. saliva, hair, nails, sweat) has recently gained much attention because of its possible applications in clinical and forensic toxicology. An individual’s past history of medication, compliance or drug abuse can be obtained from testing of hair and nails, whereas data on current status of drug use can be provided by analysis of sweat and saliva.
Because of the physicochemical properties of amfetamine-type stimulants, this group of drugs is one of the most suitable for drug testing in non-conventional matrices.
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Metadata
Title
Clinical Pharmacokinetics of Amfetamine and Related Substances
Monitoring in Conventional and Non-Conventional Matrices
Authors
Rafael de la Torre
Magí Farré
Mónica Navarro
Roberta Pacifici
Piergiorgio Zuccaro
Dr Simona Pichini
Publication date
01-03-2004
Publisher
Springer International Publishing
Published in
Clinical Pharmacokinetics / Issue 3/2004
Print ISSN: 0312-5963
Electronic ISSN: 1179-1926
DOI
https://doi.org/10.2165/00003088-200443030-00002