Pharmacodynamics and pharmacokinetics of khat: A controlled study

Widler, Peter; Mathys, K.; Brenneisen, Rudolf; Kalix, Peter; Fisch, Hans-Ulrich

doi:10.1038/clpt.1994.69

Cited by 206 publications

(137 citation statements)

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“…Peripherally, cathinone and cathine are equipotent in the release of noradrenaline at the presynaptic storage sites; thus, both have sympathicomimetic effects. The short-term physiological effects of khat reflect the sympathicomimetic and central dopaminergic activity, e. g. increased heart rate and elevated diastolic and systolic blood pressure (Brenneisen, Fisch, Koelbing, Geisshusler & Kalix, 1990;Hassan et al, 2000;Toennes et al, 2003;Widler et al, 1994). The immediate emotional effects in experimental human settings are euphoria (Brenneisen et al, 1990;Widler et al, 1994) and a subsequent depressive reaction (Hassan, Gunaid, El-Khally & Murray-Lyon, 2002).…”

Section: Chemical Agents Pharmacology and Neurophysiological Effectsmentioning

confidence: 99%

“…For cathinone, maximal plasma concentrations are reached 2 to 2.5 hours after the start of a session; for cathine, after 2.6 hours. Cathinone has a mean terminal elimination half-life of 1.5 -4.5 hours; for cathine it is approximately 5 hours (Toennes et al, 2003;Widler, Mathys, Brenneisen, Kalix & Fisch, 1994). In different experimental khat sessions, after the ingestion of 0.6 and 0.8 g of khat leaves per kg of body weight, the maximum concentrations of cathinone in plasma have been 58.9 ± 18.8 ng/ml and 127 ± 53 ng/ml; for cathine, they have been 71.2 ± 13.9 ng/ml and 89 ± 49 ng/ml (Toennes et al, 2003;Widler et al, 1994).…”

Section: Chemical Agents Pharmacology and Neurophysiological Effectsmentioning

confidence: 99%

“…Cathinone has a mean terminal elimination half-life of 1.5 -4.5 hours; for cathine it is approximately 5 hours (Toennes et al, 2003;Widler, Mathys, Brenneisen, Kalix & Fisch, 1994). In different experimental khat sessions, after the ingestion of 0.6 and 0.8 g of khat leaves per kg of body weight, the maximum concentrations of cathinone in plasma have been 58.9 ± 18.8 ng/ml and 127 ± 53 ng/ml; for cathine, they have been 71.2 ± 13.9 ng/ml and 89 ± 49 ng/ml (Toennes et al, 2003;Widler et al, 1994). After ingestion, S-(-)-cathinone is reduced to its main metabolites R,S-(-)-norephedrine and S,S-(+)-norpseudoephedrine (Brenneisen, Geisshusler & Schorno, 1986;Toennes et al, 2003).…”

Section: Chemical Agents Pharmacology and Neurophysiological Effectsmentioning

confidence: 99%

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Chronic khat use and psychotic disorders: A review of the literature and future prospects

Odenwald¹

2007

SUCHT

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Aims: In recent decades, the traditional habit of chewing the khat leaves, which contain the amphetamine-like cathinone, has undergone profound changes in African and Arab countries, from a socially regulated use pattern to uncontrolled consumption. This is of special public mental-health concern. In this article, a review of the scientific literature on the relationship between khat use and psychosis is provided. Results: Several case studies, but only a few group and community-based studies, have addressed this topic. The studies show inconsistent results, have methodological problems, and fail to report quantitative results. Many important questions remain unaddressed. Conclusions: The frequently stated association between khat use and psychosis contrasts with the small number of sound studies. Currently, only a few conclusions can be drawn, that excessive khat use can cause brief psychotic disorders and that people with a preexisting vulnerability should be discouraged to use it. The direction of causality between general psychopathology and khat use remains unclear. This review confirms the need for quantitative, controlled, and longitudinal studies,

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Section: Chemical Agents Pharmacology and Neurophysiological Effectsmentioning

confidence: 99%

Section: Chemical Agents Pharmacology and Neurophysiological Effectsmentioning

confidence: 99%

Section: Chemical Agents Pharmacology and Neurophysiological Effectsmentioning

confidence: 99%

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Chronic khat use and psychotic disorders: A review of the literature and future prospects

Odenwald¹

2007

SUCHT

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“…Les concentrations en alcaloïdes sont variables (pour 100 grammes de feuilles fraîches) : 36 à 114 mg de cathinone, 83 à 120 mg de cathine, et 8 à 47 mg de noréphé-drine [10,18,19]. Al Motarreb et coll.…”

Section: Compositionunclassified

“…La consommation régulière de khat est aussi associée à une élévation de la pression artérielle diastolique [46,47]. Chez le volontaire sain, l'augmentation de pression artérielle coïncide avec des concentrations plasmatiques de cathinone élevées [19]. Plusieurs observations expérimentales permettent de considérer la cathinone comme un agent sympathomimétique indirect [9].…”

Section: Effets Cardio-vasculairesunclassified

La toxicité du khat impose-t-elle une modification de la réglementation de son usage en Europe?

et al. 2012

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Résumé -Objectif : La consommation de khat (Catha edulis Forsk) est une pratique largement répandue dans les populations de l'est de l'Afrique. En Europe, elle concerne les migrants de première génération et leurs descendants. Le khat ne fait pas l'objet de contrôle au titre des conventions de l'ONU, lesquelles s'appuient sur une recommandation de l'OMS. Cependant, les États demeurent libres de réglementer le khat dans le cadre de leur législation nationale ; c'est le cas de la France et de certains pays européens. Cette discordance entre les réglementations interroge sur la dangerosité réelle ou supposée de cette plante. Méthodes : Nous avons utilisé le moteur de recherche bibliographique PubMed pour identifier les publications pertinentes relatives à sa toxicité. Résultats : L'usage chronique de khat est associé à des altérations de la régulation de la pression artérielle, et à une augmentation du risque d'infarctus du myocarde. Comme le cannabis, le khat peut être impliqué dans la survenue de troubles psychotiques. Le risque addictif n'est pas exclu. Chez l'animal, plusieurs études suggèrent que l'usage de khat favorise l'agressivité. Le caractère cancérogène n'est pas établi même si la génotoxicité est suspectée in vivo. Conclusion : Le risque de complications cardio-vasculaires et psychiatriques de l'usage régulier de khat, son caractère potentiellement cancérogène et la parenté chimique de la cathinone avec l'amphétamine sont autant d'arguments pour justifier l'inscription du khat sur la liste des stupéfiants réglementés. Mots clés : Khat, stupéfiant, réglementationAbstract -Objectives: Khat (Catha edulis Forsk) consumption is a widespread practice in populations of Eastern Africa. In Europe, it concerns the first-generation migrants and their descendants. Khat is not subject to control under UN conventions, which are based on a WHO recommendation. However, states remain free to regulate khat within the framework of their national legislation, such as in France and some European countries. This discordance among regulations questions the real or supposed dangerousness of this plant. Methods: We used the search engine of the bibliographic database PubMed, in order to identify the relevant publications on khat's toxicity. Results: Chronic use of khat is associated with deteriorations in the regulation of blood pressure, and an increased risk of myocardial infarction. Like cannabis, khat can be involved in the onset of psychotic disorders. The risk of addiction is not excluded. In animals, several studies suggest that khat use encourages aggressiveness. The carcinogenic nature has not been established, although genotoxicity is suspected in vivo. Conclusions: The risk of cardiovascular and psychiatric complications due to frequent use of khat, its potentially carcinogenic nature, and the chemical relationship of cathinone with amphetamine justify the inscription of khat in the list of controlled narcotics.

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Direct Enantiomeric Separation of Cathinone and One Major Metabolite on Cellobiohydrolase (CBH-I) Chiral Stationary Phase

Aboul‐Enein

Serignese

1997

Biomed. Chromatogr.

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A direct, isocratic high‐performance liquid chromatographic (HPLC) method is described for the enantiomeric separation of racemic cathinone and one of its metabolites, (+/−)‐norephedrine, on a protein‐based chiral stationary phase (CSP), cellobiohydrolase, known as CBH‐I, under reversed‐phase conditions. It was determined that the S‐(−)‐enantiomer eluted first for cathinone while the 1S,2R‐(+)‐enantiomer eluted first for norephedrine. The procedure is simple with no sample derivatization required and a short assay time. © 1997 by John Wiley & Sons, Ltd.

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Pharmacodynamics and pharmacokinetics of khat: A controlled study

Abstract: Our results provide objective evidence for the amphetamine-like stimulatory effects of khat leaves. These effects were closely similar to those observed after cathinone, 0.5 mg/kg body weight, although peak plasma concentrations of cathinone after khat were delayed.

Cited by 206 publications

References 3 publications

Chronic khat use and psychotic disorders: A review of the literature and future prospects

Chronic khat use and psychotic disorders: A review of the literature and future prospects

La toxicité du khat impose-t-elle une modification de la réglementation de son usage en Europe?

Direct Enantiomeric Separation of Cathinone and One Major Metabolite on Cellobiohydrolase (CBH-I) Chiral Stationary Phase

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