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Centrally acting muscle relaxants (A) lower muscle tone by augmenting the activity of intraspinal inhibitory interneurons. They are used in the treatment of painful muscle spasms, e. g. , in spinal disorders. Benzodiazepines enhance the effectiveness of the inhibitory transmitter GABA (p. 226) at GABAA receptors. Baclofen stimulates GABAB receptors.
Drugs having ability to diffuse and partition into the epithelium of the upper GIT (log P > 1, or preferable > 2); and those able to permeate oral mucosal tissue are considered ideal for ODT formulations. Patients who concurrently take anticholinergic medications may not be the best candidates for these drugs.


The concentration of nicotine in the synaptic cleft can neither build up as rapidly as that of ACh released from nerve terminals nor can nicotine be eliminated from the synaptic cleft as quickly as ACh. The ganglionic effects of ACh can be blocked by tetraethylammonium, hexamethonium, and other substances (ganglionic blockers).
Lipophilic substances (red dots) may enter the membrane from the extracellular space (area shown in ochre), accumulate in the membrane, and exit into the cytosol (blue area). Direction and speed of permeation depend on the relative concentrations in the fluid phases and the membrane. The steeper the gradient (concentration difference), the more drug will be diffusing per unit of time.


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