Tizanidine ratiopharm

Tizanidine Tablets is a muscle relaxant with a central effect on skeletal muscles.

Tizanidine is used as an antispasmodic in the treatment of painful acute muscle spasms, as well as spastic spasms of the cerebral type in a chronic form. The drug reduces resistance to passive movements, inhibits clonic convulsions with spasms, and at the same time can improve voluntary muscle strength. [1]

Indications Tizanidine ratiopharm

It is used for convulsive conditions of the chronic type, provoked by dysfunctions of the central nervous system. In addition, it is prescribed in case of local muscle cramps .

Release form

The drug is released in the form of tablets - 10 pieces inside the cell plate; inside the pack - 3 such plates.

Pharmacodynamics

The drug has a direct effect on the spinal cord, where it slows down the release of excitatory amino acids that stimulate the endings of NMDA. This effect is most likely associated with the stimulation of the activity of the α2-endings. As a result, the polysynaptic transmission of signals through the interneuronal connections inside the spinal cord is suppressed (this transmission leads to excessive muscle tone), which allows to weaken muscle tone. [2]

Pharmacokinetics

Absorption and bioavailability.

The absorption of tizanidine is fast and almost complete, but due to extensive metabolic processes of the 1st passage, the average level of bioavailability of the substance is only about 34%. Indicators of plasma Cmax are noted after 1 hour from the moment of taking drugs. [3]

Distribution processes.

The average value of the stable distribution volume (Vss) with intravenous administration of the substance is 2.6 l / kg. Protein synthesis rate - 30%.

In the case of drug administration in 4-12 mg portions, linear pharmacokinetic parameters are observed. The low variability of AUC and Cmax values in different people simplifies the process of reliable assessment of the plasma level of LA after oral administration.

Exchange processes.

Tizanidine undergoes extensive intrahepatic metabolic processes at a high rate. Metabolism is realized in vitro mainly with the participation of the hemoprotein P4501A2. The metabolic components of tizanidine have no therapeutic activity.

Excretion.

The final half-period of drug elimination from the circulatory system is on average 2-4 hours. Tizanidine is excreted mainly through the kidneys (approximately 70% of the dosage) in the form of metabolic elements. About 2.7% of the excreted component is the unchanged active substance.

In persons with insufficient kidney function (CC level below 25 ml / minute), the Cmax indicator is 2 times higher than in a healthy person. The final term of the half-life is also prolonged to almost 14 hours, due to which the AUC level also increases (almost sixfold).

Dosing and administration

Adults should use 2-6 mg of the medication 3-4 times a day. The starting serving size should not exceed 6 mg 3 times a day. The dosage of the medication is increased gradually, by 2-4 mg, 1-2 times per week.

The medicinal effect usually develops in the case of taking a daily dosage of 12-24 mg, divided into 3-4 uses in equal portions. A maximum of 36 mg of the substance is allowed per day.

The duration of therapy is selected individually.

In the case of renal / hepatic dysfunctions, the dosage of drugs is reduced. It is required to start with a serving of 2 mg, once a day. The dosage should be increased gradually. If there is no effect from the initial portion, first, the daily dose used for 1 use is increased, and then the number of doses is increased.

• Application for children

The medicine is not used in pediatrics because there is not enough information regarding its use in children.

Use Tizanidine ratiopharm during pregnancy

Animal tests have not determined the presence of teratogenic effects. Controlled testing of the drug during pregnancy has not been performed, which is why Tizanidine-ratiopharm is not used during the specified period (except for cases where the possible benefits of therapy are more likely than any risks).

Experimental tests have shown that small amounts of tizanidine are excreted with milk in animals; the medication is not allowed to be used for HB.

Contraindications

The main contraindications:

• severe intolerance to tizanidine or other elements of the drug;
• severe hepatic dysfunction;
• bulbar syndrome of asthenic type;
• combined use with fluvoxamine or ciprofloxacin.

Side effects Tizanidine ratiopharm

Among the side signs:

• mental disorders: occasionally insomnia, sleep problems and hallucinations develop;
• problems with the work of the NA: dizziness or drowsiness is often observed;
• disorders of the CVS function: often there is a decrease in blood pressure and bradycardia;
• symptoms associated with digestive activity: xerostomia often occurs. Dyspeptic disorders and nausea are occasionally observed;
• lesions of the hepatobiliary system: hepatitis appears singly;
• disorders in the area of connective tissues, muscles with bones and joints: occasionally muscle weakness occurs;
• systemic manifestations: increased fatigue is often noted;
• change in test readings: often a decrease in blood pressure occurs. Occasionally, serum transaminase values increase.

Overdose

Signs of poisoning: vomiting, dizziness, nausea, decreased blood pressure, miosis and coma.

Symptomatic actions are performed.

Interactions with other drugs

It is forbidden to combine the drug with ciprofloxacin or fluvoxamine (each of these drugs slows down the effect of human CYP4501A2), because this increases the AUC value of tizanidine (10 and 33 times, respectively). As a result, a prolonged, clinically significant decrease in blood pressure develops, the symptoms of which are dizziness, drowsiness, and weakening of psychomotor activity.

Do not combine tizanidine ratiopharm with other drugs that slow down the activity of CYP1A2. Among them are certain antiarrhythmic drugs (mexeletin with amiodarone and propafenone), rofecoxib, cimetidine with ticlopidine, certain fluoroquinolones (pefloxacin and norfloxacin with enoxacin, and also ciprofloxacin) and oral contraception.

Administration together with antihypertensive medications (among them diuretics) can lead to bradycardia and a decrease in blood pressure.

Sedatives and alcohol can potentiate the sedative effect of tizanidine.

Storage conditions

Tizanidine Tablets should be kept out of the reach of small children. Temperature indicators - no more than 25 ° С.

Shelf life

Tizanidine ratiopharm can be used for a 3-year term from the date of manufacture of the therapeutic product.

Analogs

Analogues of drugs are Tizalud preparations with Sirdalud.