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Pharmacology of Tizanidine (Sirdalud) ; Mechanism of action, Pharmacokinetics, Uses, Effects
Tizanidine is a centrally acting skeletal muscle relaxant used for the short-term treatment of muscle spasticity. Here’s a breakdown of its pharmacology:
Mechanism of Action
Tizanidine is an alpha-2 adrenergic agonist. It works by stimulating presynaptic alpha-2 receptors, which inhibits the release of excitatory neurotransmitters that cause muscle spasms. This leads to a reduction in muscle tone and alleviation of spasms2.
Pharmacokinetics
Absorption: Tizanidine is rapidly absorbed, reaching peak plasma concentration in approximately 1 hour after dosing.
Distribution: It is only about 30% bound to plasma proteins and readily crosses the blood-brain barrier.
Metabolism: Tizanidine undergoes rapid and extensive metabolism in the liver, primarily by cytochrome P450 1A2.
Excretion: The metabolites are primarily excreted via the renal route. The elimination half-life of tizanidine from plasma is 2-4 hours.
Therapeutic Uses
Tizanidine is indicated for the relief of muscle spasticity, which can interfere with daily activities. It is often used for conditions such as multiple sclerosis, stroke, brain injury, or spinal cord injury2.
Side Effects
Common side effects include:
Drowsiness
Dizziness
Dry mouth
Hypotension (low blood pressure)
Weakness
Warnings and Precautions
Hypotension: Monitor for signs and symptoms of hypotension, especially in patients receiving concurrent antihypertensives.
Liver Injury: Monitor liver function tests; discontinue tizanidine if liver injury occurs.
Sedation: Tizanidine may interfere with everyday activities; avoid alcohol and other central nervous system depressants
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