Tolizor capsules 150mg, 30pcs

Composition

Active ingredient:  Tolperisone hydrochloride-150,00 mg; excipients: microcrystalline cellulose-70.00 mg; lactose monohydrate (milk sugar) – 43.50 mg; croscarmellose sodium -12.00 mg; hypromellose-3.00 mg; citric acid monohydrate-4.50 mg; magnesium stearate -2.00 mg. capsule body composition: iron oxide black dye-0.0500%; titanium dioxide-2.0000%; water -14.50%; gelatin – up to 100%. capsule cap composition: quinoline yellow dye-0.7500%; sunset yellow dye-0.0059%; titanium dioxide-2.0000%; water -14.50%; gelatin – up to 100%.

Pharmacological action

Tolperisone is a centrally acting muscle relaxant. The mechanism of action is not fully understood. Tolperisone has a high affinity for nervous tissue, reaching the highest concentrations in the brain stem, spinal cord and peripheral nervous system. The main effect of Tolperisone is mediated by inhibition of spinal reflex arcs. Probably, this effect, together with the elimination of facilitation of arousal along the descending pathways, provides the therapeutic effect of Tolperisone. The chemical structure of tolperisone is similar to that of lidocaine. Like lidocaine, it has a membrane-stabilizing effect and reduces the electrical excitability of motor neurons and primary afferent fibers. Tolperisone dose-dependently inhibits the activity of potential-dependent sodium channels. Accordingly, the amplitude and frequency of the action potential decreases. A depressing effect on potential-dependent calcium channels has been proven. It is assumed that in addition to its membrane-stabilizing effect, Tolperisone may also inhibit the release of the mediator. Tolperisone has some weak properties of a-adrenergic antagonists and antimuscarinic action.

Indications

Symptomatic treatment of spasticity in adults due to stroke.

Contraindications

Hypersensitivity to any of the components of the drug. Myasthenia gravis. Children under 18 years of age. Breast-feeding. Lactose intolerance, lactase deficiency, glucose-galactose malabsorption.

Side effects

The safety profile of Tolperisone drugs is confirmed by data on its use in more than 12,000 patients. According to these data, disorders of the skin and subcutaneous tissues, general, neurological and gastrointestinal disorders are most often described. In the post-marketing period, the number of reports received about the development of hypersensitivity reactions associated with the use of Tolperisone was about 50-60% of all reports received. In most cases, these were not serious adverse reactions. Life-threatening allergic reactions have been reported very rarely. The frequency of adverse reactions is classified according to the recommendations of the World Health Organization, characterized as: very common (>1/10), often (>>1/100, >><1/10), infrequently (>1/1000, <1/10), infrequently (><1/100), rarely (>1/10000, <1/100), rarely (><1/1000), very rarely ( From the blood and lymphatic system: very rarely – anemia, lymphadenopathy. From the immune system: rarely-hypersensitivity reactions*, anaphylactic reactions; very rarely-anaphylactic shock. From the side of metabolism and nutrition: infrequently-anorexia; very rarely-polydipsia. From the side of the psyche: infrequently-sleep disturbance, insomnia; rarely-weakness, depression; very rarely-confusion. From the nervous system: infrequently-headache, dizziness, drowsiness; rarely-attention deficit disorder, tremor, convulsions, paresthesia, malaise, lethargy. From the side of the organ of vision: rarely-decreased visual acuity. From the side of the organ of hearing: rarely-tinnitus, vertigo. From the cardiovascular system: infrequently-hypotension; rarely-angina pectoris, tachycardia, palpitation, “flushes” of blood to the face; very rarely-bradycardia. From the respiratory system: rarely-shortness of breath, nosebleeds, tachypnea. From the gastrointestinal tract: infrequently-abdominal discomfort, dyspepsia, diarrhea, dry mouth, nausea; rarely-epigastric pain, constipation, flatulence, vomiting. From the liver and biliary tract: rarely-moderate hepatic insufficiency. From the skin and subcutaneous tissues: rarely-allergic dermatitis, hyperhidrosis, pruritus, skin rash, urticaria. Musculoskeletal and connective tissue disorders: infrequently-muscle pain, muscle weakness, pain in the extremities; rarely – discomfort in the extremities; very rarely-osteopenia. From the side of the kidneys and urinary tract: rarely-enuresis, proteinuria. General disorders and reactions at the injection site: infrequently-asthenia, fatigue, malaise; rarely-a feeling of intoxication, a feeling of warmth, irritability, thirst; very rarely-chest discomfort. Laboratory parameters: rarely-hyperbilirubinemia, impaired liver function, thrombocytopenia, leukocytosis; very rarely-hypercreatininemia. * Angioedema, including facial and lip edema, has been reported in post-marketing monitoring (frequency unknown).

Interaction

Studies of the pharmacokinetic drug interaction with the marker substrate of the CYP2D6 isoenzyme dextromethorphan have shown that simultaneous use of Tolperisone can increase the blood content of drugs that are mainly metabolized by the CYP2D6 isoenzyme (thioridazone, tolterodine, venlafaxine, atomoxetine, desipramine, dextromethorphan, metoprolol, nebivolol, perphenazine). No significant inhibition or induction of other CYP isoenzymes (CYP2B6, CYP2C8, CYP2C9, CYP2C19, CYP1A2, and CYP3A4) was found in laboratory experiments on human liver microsomes and human hepatocytes. Due to the diversity of Tolperisone’s metabolic pathways, no increase in Tolperisone exposure is expected with concomitant use of CYP2D6 isoenzyme substrates and / or other drugs. The bioavailability of tolperisone decreases when taken on an empty stomach. Despite the fact that Tolperisone is a centrally acting drug, its sedative effect is very low. When used concomitantly with other centrally acting muscle relaxants, the dose of tolperisone should be reduced. Tolperisone enhances the effect of niflumic acid, so when used simultaneously, a reduction in the dose of niflumic acid or other nonsteroidal anti-inflammatory drugs (NSAIDs) should be considered.

How to take, course of use and dosage

Inside, after eating, without chewing, without opening the capsule, with a small amount of water. The bioavailability of tolperisone decreases when taken on an empty stomach. The dose of the drug is selected based on the individual needs of the patient and the tolerability of the drug. 50 mg 3 times a day, gradually increasing the dose to 150 mg 3 times a day. The recommended daily dose is 150-450 mg, divided into 3 parts. Patients with renal insufficiency The experience of using Tolperisone in patients with renal insufficiency is limited, and this category of patients more often experienced adverse reactions. Therefore, in patients with moderate renal impairment, it is necessary to select the dose of Tolperisone, with careful monitoring of the patient’s health and monitoring of renal function. The use of the drug is not recommended in patients with severe renal insufficiency. Patients with hepatic insufficiency The experience of using Tolperisone in patients with hepatic insufficiency is limited, and this category of patients more often experienced adverse reactions. Therefore, in patients with moderate hepatic impairment, it is necessary to select the dose of Tolperisone, with careful monitoring of the patient’s health and monitoring of liver function. The use of the drug is not recommended in patients with severe hepatic insufficiency.

Overdose

Data on Tolperisone overdose are scarce. In preclinical acute toxicity studies, high doses of Tolperisone have caused ataxia, tonic-clonic seizures, shortness of breath, and respiratory paralysis. Tolperisone does not have a specific antidote. In case of overdose, symptomatic and supportive treatment is recommended.

Special instructions

The most common adverse reactions are hypersensitivity reactions. Allergic reactions range from mild skin reactions to severe systemic reactions, including anaphylactic shock.

Symptoms of an allergic reaction include redness, rash, urticaria, pruritus, angioedema (angioedema), tachycardia, hypotension, and shortness of breath.

Female patients with a history of hypersensitivity reactions to other medications or allergic reactions are at a higher risk.

In the case of known hypersensitivity to lidocaine, increased caution should be exercised when using Tolperisone due to possible cross-reactions.

Patients should be alert for any symptoms of hypersensitivity. If symptoms occur, you should immediately stop taking Tolperisone and immediately consult a doctor. Do not re-prescribe Tolperisone after an episode of hypersensitivity to a drug containing it.

Effect of the drug on the ability to drive vehicles and mechanisms

Tolizor does not affect the ability to drive vehicles and mechanisms. Patients who experience dizziness, drowsiness, impaired attention, seizures, visual impairment, or muscle weakness while taking the drug should consult a doctor!

Storage conditions

In a dark place at a temperature not exceeding 25°C. Keep out of reach of children.

Shelf

life is 3 years. Do not use after the expiration date indicated on the package.

Active ingredient

Tolperisone

Conditions of release from pharmacies

By prescription

Dosage form

Capsules