The habit of Catha edulis Forsk (khat) chewing has prevailed for centuries among populations in the horn of Africa and the Arabian peninsula. Fresh leaves of Catha edulis are customarily chewed to attain a state of stimulation. The fact that cathinone has a closer structural similarity with amphetamine, and both share common pharmacodynamic features, led to the conclusion that cathinone is the most important active ingredient of Catha edulis, which causes the major pharmacological effects. Problems associated with repeated consumption of Catha edulis leaves are becoming evident. Literature surveys and clinical diagnostic studies revealed an association with prevalence of psychiatric morbidity. Repeated intermittent oral administration of Catha edulis to laboratory animals lead to development and expression of locomotor sensitisation. Catha edulis also leads to several peripheral effects that include increases in blood pressure and has been associated with the increased incidence of acute coronary vasospasm and myocardial infarction. Catha edulis also accounts for a number of gastrointestinal tract problems, oesophagitis, gastritis and delay intestinal absorption, as well as the development of oral keratotic white lesions at the site of chewing. Administration of Catha edulis extracts showed a deranged systemic capacity to handle oxidative radicals and induces cytotoxic effects in cells of liver and kidney, as well as induction of cell death in various human leukaemia cell lines and in peripheral human blood leukocytes.