The study examined the effect of Khat chewing on ampicillin and amoxycillin bioavailability following the administration of a 500 mg single dose of each antibiotic at different times relative to Khat chewing. Using a urinary excretion method the bioavailabilities of ampicillin and amoxycillin were determined in eight healthy adult male Yemeni volunteers. The extent and rate of ampicillin bioavailability were reduced significantly by Khat chewing except when administered 2 h after the Khat chewing session. However, the bioavailability of amoxycillin was only significantly reduced when the antibiotic was taken midway through the Khat chewing session. It was concluded that the two antibiotics, particularly ampicillin, should be taken 2 h after Khat chewing.