The primary pharmacologically active agents (metabolites) in khat are cathinone and cathine (dextro-norpseudoephedrine). These are both central nervous system (CNS) stimulants, but have a considerably lower potency than amphetamine, one of the best known CNS stimulants. The effects of khat are broadly similar to amphetamines, in that it also produces an increase in levels of epinephrine and norepinephrine (adrenaline and noradrenaline, respectively) and serotonin.

Due to the nature of the molecular structure of the active metabolites in khat and the route of administration, the release of these transmitters is slow.

It is predominantly these cathinones in khat that provide the user with the sought after euphoric and stimulating effects.