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Background.—The overuse of short-acting barbiturate medications for the acute treatment of headache is a common problem in the United States. Most experts agree that withdrawal from these medications is necessary for subsequent headache treatment to be successful, yet there are few published articles outlining effective methods of drug withdrawal. Objective.—To evaluate the safety and effectiveness of phenobarbital loading for withdrawal from overuse of short-acting barbiturate compounds in inpatients with headache. Design and Methods.—We performed a retrospective chart review of 18 consecutive patients in an inpatient pain rehabilitation program who were withdrawn from overuse of butalbital-combination medications using a phenobarbital-loading protocol. Results.—Eighteen patients with headache hospitalized in an inpatient pain unit for withdrawal from overuse of combination butalbital preparations underwent a phenobarbital-loading protocol. Short-acting barbiturate medications were discontinued, and patients received 120 mg of oral phenobarbital until their score on a predetermined scale reached target levels, and the drug was then discontinued. All patients were effectively treated with no serious adverse events. The median number of doses required varied significantly, and could not be predicted by the patient's prior intake. Conclusions.—Management of butalbital withdrawal can be simplified by using a phenobarbital-loading protocol, taking advantage of the natural tapering afforded by the drug's long half-life. This method possesses most of the characteristics of an ideal drug withdrawal program for patients with headache who are overusing medications. [ABSTRACT FROM AUTHOR]