Apparatus and methods for the dose-to-effect transmucosal administration of medicaments are disclosed. The present invention relates to such apparatus and methods which are useful in administering medicaments in a dose-to-effect manner such that sufficient drug is administered to produce precisely a desired effect. The invention also relates to an apparatus capable of placement directly on the patient's buccal mucosa having the capability of adjusting the drug surface area in direct contact with the mucosal tissue thereby enabling the proper amount of therapeutic agent or drug to be administered while accounting for individual needs and susceptibilities of the drug.Through the use of selected permeation enhancers, the present invention enables lipophilic and nonlipophilic medicaments, which are not suitable for oral administration, to be rapidly administered noninvasively. Employing the present invention the drug may be introduced into the patient's bloodstream almost as fast as through injection, and much faster than using the oral administration route, while avoiding the negative aspects of both of these methods.