Cathinone action

Patel NB. Mechanism of action of cathinone the active ingredient of khat (Catha... 

The plasma half-life of cathinone is 1.5 hours. The primary metabolites are norpseudoephedrine, norephedrine, 3,6-dimethyl-2,5-diphenyl-pyrazine, and l-phenyl-l,2-propanedione (Szendrei 1980 Brenneisen etal. 1986 Guantai and Maitai 1983). However, norpseudoephedrine and norephedrine also originate directly from the leaves, as well as being metabolic products (Widler et al. 1994). Maximal plasma concentrations of norephedrine and norpseudoephedrine are reached at about 3.3 and 3.1 hours, respectively. These two drugs have a much longer duration of action than cathinone, where terminal half-lives could not be calculated after 10 hours. 

Kalix P, Glennon RA. (1986). Further evidence for an amphetamine-like mechanism of action of the alkaloid cathinone. Biochem Pharmacol. 35(18) 3015-19. 

The fresh leaves of the khat shrub (Catha edulis) are chewed by several millions of people in East Africa and the Arabian peninsula for their euphoric and stimulating properties (284). The rather newly discovered alkaloid cathinone [(S)-a-aminopropiophenone] is responsible for the stimulating properties of khat (284). It has been shown that cathinone induces release at physiological catecholamine storage sites in a manner similar to that of amphetamine. Further results suggest that cathinone and amphetamine produce their stimulant effects via the same dopaminergic mechanism (599). The more recently discovered khat constituents merucathinone, merucathine, and pseudomerucathine were found to have only weak dopamine-releasing effects and were therefore considered unlikely to play an important role in the stimulatory actions of khat leaves (414). 

Khat is purchased as bundles of dried and fresh leaves and buds. For transport purposes, it is usually wrapped in plastic bags or banana skins to preserve its moisture content - loss of activity is observed after 48 h if the plant material dries out. However, the drug can also be obtained as dried crushed leaves or in powdered form. These materials are either chewed or used to prepare an infusion which is drunk like tea. The major part of the pharmacological action is due to cathinone, which acts as a central nervous system (CNS) stimulant, promoting excitation, reducing the need to sleep and enhancing communication. 

The most common route of khat administration is chewing the fresh leaves of the plant. The juices are swallowed and contain two stimulants cathine and cathinone. These substances produce effects that are very similar to cocaine and amphetamine mediated by actions on the monoamine neurotransmitter systems. Users report that... 

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