Management of trigeminal neuralgia, a severe facial pain, remains difficult. All patients are initially treated with drugs. Since the seventeenth century more than 40 different preparations have been used; some of these, although effective, had toxic side effects. The most useful drugs at present are carbamazepine, phenytoin, baclofen, and clonazepam. A new drug, oxcarbazepine, is showing therapeutic promise. The most common reason for therapeutic failure with antineuralgic drugs is inadequate dosage. We review here the pharmacokinetics, side effects, possible drug interactions, plasma and serum therapeutic concentrations, and the available formulations of each drug. On the basis of these considerations and clinical reports describing the use of these drugs, we make dosage recommendations to enable the practitioner to individualize therapeutic regimens.