Tizanil
Tizanil: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. For violations of liver function
- 13. Use in the elderly
- 14. Drug interactions
- 15. Analogs
- 16. Terms and conditions of storage
- 17. Terms of dispensing from pharmacies
- 18. Reviews
- 19. Price in pharmacies
Latin name: Tizanil
ATX code: M03BX02
Active ingredient: tizanidine (tizanidine)
Manufacturer: Simpex Pharma Pvt. Ltd (Simpex Pharma Pvt Ltd) (India)
Description and photo updated: 20.11.2018
Prices in pharmacies: from 126 rubles.
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Tizanil is a drug of central muscle relaxant action that reduces muscle tissue tension.
Release form and composition
Dosage form Tizanil - tablets: flat-cylindrical, with a double-sided bevel, from white to almost white:
- dosage of 2 mg: on one side of the risk, on the other - the number 2 (10 pcs. in blisters, in a cardboard box 3 blisters);
- dosage of 4 mg: on one side there is a cruciform risk, on the other - the number 4 (10 pcs. in blisters, in a cardboard box 1 or 3 blisters);
- dosage of 6 mg: on one side there is a cruciform risk, on the other - the number 6 (10 pcs. in blisters, in a cardboard box 3 blisters).
Composition:
- active substance: tizanidine - 2, 4 or 6 mg (in the form of tizanidine hydrochloride - 2.288; 4.576 or 6.864 mg);
- auxiliary components: lactose monohydrate, microcrystalline cellulose, stearic acid, colloidal anhydrous silicon dioxide.
Pharmacological properties
Pharmacodynamics
The active component of Tizanil, tizanidine, is a centrally acting muscle relaxant that reduces the tone of skeletal muscles, reduces the severity of spasm, increases the strength of voluntary contractions and reduces the rigidity of the muscular system during passive movements.
Acting directly on the spinal cord, tizanidine stimulates presynaptic α1-adrenergic receptors, suppressing the release of amino acids that excite receptors for N-methyl-D-aspartate (NMDA receptors), as a result of which polysynaptic transmission of excitation at the level of intermediate neurons of the spinal cord is suppressed. When this mechanism, which is responsible for excess muscle tone, is suppressed, the minimum muscle tension that remains at rest and relaxation is reduced to the maximum.
Pharmacokinetics
- absorption: after oral administration, tizanidine is well absorbed; within 1 hour reaching the maximum plasma concentration (Cmax); bioavailability ~ 34%. The diet (meal time) does not affect the pharmacokinetics of the substance;
- distribution: in equilibrium Vd (volume of distribution) - 160 l; tizanidine binds to plasma proteins by 30%. Pharmacokinetics in the range of recommended daily doses of 4–20 mg is linear;
- metabolism: Tizanyl is rapidly and largely metabolized by the CYP1A2 isoenzyme in the liver (up to 95%) with the formation of inactive metabolites;
- excretion: tizanidine is excreted mainly by the kidneys, up to 70% in the form of metabolites, 2.7% - unchanged. Excretion occurs in 2 stages: half-life (T1 / 2) at the first stage - 2.5 hours; final T1 / 2 - 22 hours. Average T1 / 2 of unchanged substance is from 2 to 4 hours.
In renal failure with creatinine clearance (CC) less than 25 ml / min, the Cmax value doubles, the mean T1 / 2 increases to 14 hours, and the AUC (area under the concentration-time pharmacokinetic curve) increases 6 times.
Indications for use
According to the instruction, Tizanil is recommended for painful muscle spasms of various etiologies, as well as for relieving spasticity in multiple sclerosis, spinal cord injuries and traumatic brain injury.
Contraindications
Absolute:
- severe liver dysfunction;
- use in combination with potent inhibitors of CYP1A2 isoenzymes (including ciprofloxacin, fluvoxamine);
- lactase deficiency, lactose intolerance, glucose-galactose malabsorption;
- children and adolescents under 18 years of age;
- individual hypersensitivity to tizanidine and (or) any of the components of the drug.
Relative contraindications for which Tizanil should be used with caution: arterial hypotension, renal failure, bradycardia, taking simultaneously with oral contraceptives, elderly age from 65 years.
You can not abruptly stop taking Tizanil, the dose of the drug must be reduced gradually.
Instructions for the use of Tizanil: method and dosage
Tizanil tablets are taken orally.
Recommended dosage:
- painful muscle spasm (for relief): 2-4 mg three times a day; in severe course - an additional 2-4 mg before going to bed at night;
- spasticity of skeletal muscles due to neurological diseases (therapy): the initial dose is 2 mg three times a day, the dose is subsequently gradually increased by 2–4 mg with an interval of 3–7 days. The optimal daily dose is 12-24 mg, divided into 3-4 doses, the maximum allowable daily dose is 36 mg.
Side effects
- central nervous system: dizziness, insomnia, drowsiness, sleep disturbance, hallucinations;
- cardiovascular system: bradycardia, decrease in blood pressure (blood pressure), in some episodes pronounced, up to loss of consciousness and collapse;
- digestive system: nausea, dry mouth, dyspepsia, liver failure, increased activity of hepatic transaminases, hepatitis;
- musculoskeletal system: muscle weakness;
- other reactions: hypercreatininemia, increased fatigue.
As a result of the sudden cancellation of Tizanil after prolonged therapy and (or) the use of tizanidine in high doses, as well as after the application simultaneously with antihypertensive drugs, it is possible to: increase blood pressure, tachycardia, acute cerebrovascular accident.
Overdose
Symptoms of a Tizanil overdose are nausea, vomiting, decreased blood pressure, agitation, anxiety, miosis, dizziness, drowsiness, prolongation of the QT interval, respiratory failure, coma.
For the treatment of the condition, it is recommended to perform gastric lavage, give the patient activated charcoal, carry out forced diuresis and, if necessary, carry out symptomatic treatment.
special instructions
There is evidence of liver dysfunctions associated with the intake of tizanidine, but if the requirements for the dosage regimen and the use of daily doses of the drug up to 12 mg were observed, such cases were rarely observed. In order to avoid liver diseases, it is recommended to monitor liver function tests once a month during the first 4 months of treatment when taking tizanidine in a daily dose of 12 mg and above, as well as in patients with clinical signs suggesting liver dysfunction: unexplained nausea, anorexia feeling chronic fatigue. If the serum activity of AST (aspartate aminotransferase) and ALT (alanine aminotransferase) consistently exceeds three times or more the upper limit of the norm, Tizanyl should be canceled.
Preclinical studies of chronic toxicity of the drug in animals (dogs) were carried out, during which an increase in the QT interval was noted in the case of using tizanidine in doses equivalent to the maximum doses for humans. Therefore, with the syndrome of congenital prolongation of the QT interval, Tizanil should be taken with caution.
Patients with coronary artery disease (ischemic heart disease) and (or) heart failure should be monitored regularly with an electrocardiogram (ECG).
With myasthenia gravis, the drug is prescribed with extreme caution, after a careful assessment of the ratio of the benefits expected from therapy, with the possible risk of adverse reactions.
Influence on the ability to drive vehicles and complex mechanisms
As a result of taking Tizanil, dizziness, drowsiness, and a decrease in blood pressure may develop, which requires refraining from potentially hazardous activities, including driving vehicles or working with complex mechanisms.
Application during pregnancy and lactation
Since no controlled studies have been conducted on the use of tizanidine in pregnant women, it should not be used during pregnancy, unless the expected benefit to the mother outweighs the potential risk to the fetus.
Tizanil slightly penetrates into breast milk; during breastfeeding, the drug should be discontinued.
Pediatric use
The use of Tizanil is contraindicated for the treatment of children and adolescents under 18 years of age.
With impaired renal function
Caution is required to use Tizanil in patients with renal failure.
With CC <25 ml / min, treatment begins with a dose of 2 mg once a day. If necessary, it is gradually increased taking into account portability. When a more pronounced therapeutic effect is required, it is recommended first of all to increase the dose prescribed once a day, after which it is possible to increase the frequency of its administration.
For violations of liver function
Tizanil is not prescribed for severe liver dysfunction.
Use in the elderly
Tizanil should be used with caution in elderly patients over 65 years of age.
Drug interactions
- fluvoxamine, ciprofloxacin (inhibitors of the isoenzyme CYP1A2): able to increase the AUC of tizanidine 33 times, which may result in a prolonged and clinically significant decrease in blood pressure, leading to weakness, drowsiness and slowing down of psychomotor reactions, up to loss of consciousness, as well as lengthening the QT interval;
- other inhibitors of the CYP1A2 isoenzyme - antiarrhythmics (amiodarone, propafenone, mexiletine), cimetidine, fluoroquinolones (enoxacin, norfloxacin, pefloxacin), rofecoxib, oral contraceptives, ticlopidine: concomitant use with tizanidine;
- antihypertensive drugs: the risk of a pronounced decrease in blood pressure and bradycardia increases;
- drugs that depress the central nervous system, ethanol: potentiation of the sedative effect of tizanidine is possible, simultaneous use is not recommended.
Analogs
Tizanil's analogs are Sirdalud, Tizanidin, Tizalud, Tizanidin-Teva, etc.
Terms and conditions of storage
Store at temperatures up to 30 ° C in a dry and dark place. Keep out of the reach of children.
The shelf life is 3 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Tizanil
From the few reviews about Tizanil, it is difficult to understand how effective this drug is and whether it is an adequate alternative to more expensive analogues.
Along with the recommendation of the use of the drug for the effective removal of muscle spasms, there are opinions about the absolute ineffectiveness of the drug, aggravated by a strong hypnotic effect, causing apathy to everything around.
The price of Tizanil in pharmacies
Estimated price of Tizanil tablets, 30 pcs. in the package: in a dosage of 2 mg - 165 rubles; at a dosage of 4 mg - 277 rubles.
Tizanil: prices in online pharmacies
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Drug name Price Pharmacy |
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Tizanil tablets 2mg 20 pcs. 126 RUB Buy |
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Tizanil 2 mg tablets 20 pcs. 126 RUB Buy |
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Tizanyl 2mg tablets 30 pcs. 139 RUB Buy |
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Tizanil 2 mg tablets 30 pcs. 139 RUB Buy |
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Tizanil 4 mg tablets 30 pcs. 199 RUB Buy |
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Tizanil 4 mg tablets 20 pcs. 213 r Buy |
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Tizanil tablets 4mg 30 pcs. 227 r Buy |
Maria Kulkes Medical journalist About the author
Education: First Moscow State Medical University named after I. M. Sechenov, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
