Central Muscle Relaxants

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These are used to control spastic muscle tone. These drugs include diazepam (which binds to GABA receptors), dantrolene (which acts directly on muscles by interfering with the release of calcium from the sarcoplasmic reticulum) and baclofen (which probably acts at GABA receptors in the CNS.

Actions: The benzodiazepines relax the spasticity of skeletal muscle, probably by increasing presynaptic inhibition in the spinal cord.

Therapeutic Uses: Diazepam is useful in the treatment of skeletal muscle spasms such as occur in muscle strain, and in treating spasticity from degenerative disorders, such as multiple sclerosis and cerebral palsy.

Pharmacokinetics: The benzodiazepines are lipophilic and are rapidly and completely absorbed after oral administration and are distributed throughout the body. Most are metabolised by the hepatic microsomal metabolising system to compounds that are also active.

Adverse Effects: Drowsiness and confusion are the two most common side effects of the benzodiazepines.

Category: Pharmacology Notes



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