Pharmacological Intervention A Oral Medications

In the 1990s, Albright reported that oral medications, including benzodiazepines and skeletal muscle relaxants, had been used with limited success to diminish the effects of spasticity. Diazepam, a benzodiazepine, facilitates the inhibitory response of g-aminobutyric acid (GABA) neurotransmitters by increasing the conductance of chloride ions upon binding to GABAa receptors. This results in a presynaptic inhibition at the spinal cord level with resultant relaxation of skeletal muscle. Use of this agent has been associated with adverse effects including sedation and a potential for dependency.

Muscle relaxants used in the treatment of spasticity include dantrolene sodium and baclofen. Dantrolene sodium acts directly on the skeletal muscle by inhibiting the release of calcium from the sarcoplasmic reticulum. The result is an interference with the excitation-contraction coupling and a resultant reduction in contractile force of the muscle. Side effects from dantrolene sodium use include drowsiness and a suggested increase in seizure activity in children with CP.

Baclofen is a skeletal muscle relaxant frequently used in the management of spasticity. It acts throughout the central nervous system and has been shown to be most effective when used to treat spasticity of spinal origin. In spasticity of cerebral origin, spasticity reduction has been reported as mild due to poor lipid solubility of the drug. In actuality, only a small amount of baclofen penetrates the blood-brain barrier, requiring higher doses to achieve an effect. Upon entry, baclofen binds to GABAb receptors to prevent the uptake of calcium necessary for the release of excitatory neurotransmitters, such as aspartate and glutamate. The effect is a decrease in the release of neurotransmitters in the excitatory pathways resulting in a reduction of muscular spasticity. Compared with dantrolene sodium, baclofen use has fewer side effects, with no associated increase in seizure activity. However, drowsiness is frequently experienced.

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