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Medication Description: Tizanidine (Tizanidine)

TIZANIDIN (Tizanidine). 5-Chloro-4- (2-imidazolin-2-yl-amino) -2, 1, 3-benzothiadiazole.

Available in the form of hydrochloride.

Synonyms: Sirdalud, Sirdalud ("SANDOZ").

White or slightly yellow crystalline powder.

A muscle relaxant centrally acting. Suppresses polysynaptic spinal reflexes and has an antispastic effect with increased muscle tone, relieves spasms and clonic convulsions.

By its pharmacological properties, tizanidine is similar to mydocalm and baclofen, but differs from them in the mechanism of action. Thus, baclofen increases the activity of the inhibitory GABAergic mediator system, and the effect of tizanidine is associated with a decrease in the release of excitatory mediator amino acids from the internes (see Glutamic Acid).

Tizanidine is rapidly and almost completely absorbed when taken orally. The maximum concentration in the blood plasma is observed after 1 to 2 hours. In unchanged form, the drug and metabolites are excreted mainly in the urine.

Tizanidine is used for painful muscle spasms associated with static and functional lesions of the spine (cervical and lumbar syndromes), and after surgery (for herniation of the intervertebral disc or hip osteoarthritis), as well as for spasticity caused by multiple sclerosis, chronic myelopathy, degenerative diseases. spinal cord, stroke and convulsions of central origin.

Take tizanidine inside in pill form. To relieve muscle spasm pain prescribed for adults 2-4 mg (0.002-0.004 g) 3 times a day (regardless of meal times). If the effect is insufficient, take an additional 2 - 4 mg at night. With spasticity due to neurological disorders, prescribed in individually selected doses, starting with a daily dose of 6 mg (in 3 doses); gradually increase the daily dose (with breaks of 4-7 days) by 2-4 mg. The optimal daily dose is usually 12 to 14 mg (in 3-4 doses). The daily dose should not exceed 36 mg.

Tizanidine is usually well tolerated, but drowsiness, tiredness, dizziness, dry mouth, nausea, and a slight decrease in blood pressure may be observed. At higher doses, muscle weakness, insomnia, hypotension, bradycardia are possible; in some cases, a temporary increase in transaminase activity in the serum.

The drug should not be taken during pregnancy and lactation. There is not enough experience of using it in children.

When violations of the liver and kidneys reduce the dose.

In connection with possible drowsiness and muscular weakness, care should be taken when prescribing the drug to persons whose work requires a quick mental and physical reaction (operators, drivers of motor vehicles, etc.).