Tolizor, 50 mg capsules 30 pcs

Pharmacotherapeutic group: myorelaxant of central action.

ATX code: M03BX04

Pharmacological properties.

Indications

Active ingredient

Composition

Active ingredients: Tolperisone hydrochloride 50 mg

Auxiliary substances: microcrystalline cellulose – 55.22 mg, lactose monohydrate (milk sugar) – 34.33 mg, croscarmellose sodium – 6.32 mg, hypromellose – 1.58 mg, citric acid monohydrate – 1.5 mg, magnesium stearate – 1.05 mg.

How to take, the dosage

The drug is taken orally after a meal, without chewing, without opening the capsule, with a small amount of water. Bioavailability of Tolperisone is reduced when taken on an empty stomach.

The dose of the drug is adjusted according to individual patient need and tolerance of the drug.

Prescribe 50 mg 3 times daily, gradually increasing the dose to 150 mg 3 times daily. The recommended daily dose is 150-450 mg divided into three doses.

The experience of using tolperizone in patients with renal impairment is limited; adverse reactions were more frequent in this category of patients. Therefore, in patients with moderate renal dysfunction it is necessary to adjust the dose of tolperizone, with close monitoring of the patient’s health status and control of renal function. The use of the drug is not recommended in patients with severe renal insufficiency.

The experience of using tolperizone in patients with hepatic impairment is limited, adverse reactions were more frequent in this category of patients. Therefore, in patients with moderate liver dysfunction it is necessary to adjust the dose of tolperizone, with close monitoring of the patient’s health status and control of liver function. The use of the drug is not recommended in patients with severe hepatic impairment.

Interaction

Studies of pharmacokinetic drug-drug interactions with the CYP2D6 isoenzyme marker substrate dextromethorphan have shown that concomitant use of tolperizone may increase blood levels of drugs that are metabolized primarily by the CYP2D6 isoenzyme (thioridazone, tolterodine, venlafaxine, atomoxetine, desipramine, dextromethorphan, metoprolol, nebivolol, perphenazine).

In laboratory experiments on human liver microsomes and human hepatocytes no significant inhibition or induction of other CYP isoenzymes (CYP2B6, CYP2C8, CYP2C9, CYP2C19, CYP1A2, CYP3A4) was found.

Due to the variety of metabolic pathways of tolperisone, increased exposure of tolperisone is not expected with concomitant use of CYP2D6 isoenzyme substrates and/or other drugs.

The bioavailability of tolperizone is reduced when taken on an empty stomach.

While tolperizone is a centrally acting drug, its sedative effect is very low. When concomitant use with other central muscle relaxants, the dose of tolperizone should be reduced.

Tolperisone increases the effect of niflumic acid, so a reduction in the dose of niflumic acid or other NSAIDs should be considered when used concomitantly.

Special Instructions

The most common adverse reactions are hypersensitivity reactions.

Allergic reactions range from mild skin to severe systemic, including anaphylactic shock. Symptoms of allergic reactions include redness, rash, urticaria, itching, angioedema (Quincke’s edema), tachycardia, arterial hypotension and shortness of breath.

Patients who are female and have a history of hypersensitivity to other drugs or allergic reactions are at higher risk.

In patients with known hypersensitivity to lidocaine, extra caution should be exercised when using tolperizone because of possible cross-reactions.

Patients should be alert for any symptoms of hypersensitivity. If symptoms occur, tolperizone should be discontinued immediately and a physician should be consulted immediately. Tolperizone should not be re-prescribed after an episode of hypersensitivity to a drug containing it.

Influence on the ability to drive vehicles and mechanisms

Tolizor does not affect the ability to drive vehicles and mechanisms. Patients who have experienced dizziness, drowsiness, impaired attention, seizures, visual impairment, or muscle weakness while taking the drug should see their physician.

Contraindications

Side effects

The safety profile of tolperizone has been confirmed by data on use in more than 12,000 patients. According to these data, the most frequent were skin and subcutaneous tissue abnormalities, general disorders, nervous system and gastrointestinal disorders.

In the post-registration period, hypersensitivity reactions accounted for about 50-60% of all adverse reactions. Most adverse reactions were not serious and went away on their own. Life-threatening hypersensitivity reactions were very rarely reported.

The adverse reactions are listed below according to MedDRA classification and frequency: infrequent (≥1/1000, < 1/100), rare (≥1/10000, < 1/1000), very rare (< 1/10000), frequency unknown (cannot be estimated from available data).

Blood and lymphatic system disorders:very rarely, anemia, lymphadenopathy.

From the immune system: rarely – hypersensitivity reactions, anaphylactic reactions; very rare – anaphylactic shock.

Metabolism and nutrition: infrequent – anorexia; very rare – polydipsia.

Mental disorders: infrequent – sleep disturbance, insomnia; rare – weakness, depression; very rare – confusion.

Nervous system disorders: infrequent – headache, dizziness, somnolence; rare – attention deficit disorder, tremor, convulsions, malaise, paresthesia, lethargy.

Visual organ: rarely – decrease in visual acuity.

Hearing organ and labyrinth disorders: rarely – tinnitus, vertigo.

Cardiovascular system disorders: infrequent – arterial hypotension; rare – angina, tachycardia, palpitations, “rushes” of blood to the face; very rare – bradycardia.

In the respiratory system: rarely – shortness of breath, nasal bleeding, rapid breathing.

The digestive system: infrequent – abdominal discomfort, dyspepsia, diarrhea, dry mouth, nausea; rarely – epigastric pain, constipation, flatulence, vomiting.

Hepatic and biliary tract disorders: rarely – moderate hepatic insufficiency.

Skin and subcutaneous tissue disorders: rarely – allergic dermatitis, increased sweating, skin itching, skin rash, urticaria.

Muscular system disorders: infrequent – muscle weakness, muscle pain, pain in the extremities; rare – discomfort in the extremities; very rare – osteopenia.

With the urinary system: rarely – enuresis, proteinuria.

General disorders and reactions at the site of administration: infrequent – asthenia, discomfort, feeling tired; rare – feeling intoxicated, feeling hot, irritability, thirst; very rare – discomfort in the chest.

From laboratory parameters: rarely – hyperbilirubinemia, changes in the activity of liver enzymes, thrombocytopenia, leukocytosis; very rarely – hypercreatininemia.

* Angioneurotic edema, including facial and lip edema, has been reported in post-registration monitoring (frequency unknown).

If any of the reactions listed in the instructions worsen or any other adverse reactions not listed in the instructions are noted, the patient should inform the physician.

Overdose

Pregnancy use

Pregnancy

The experimental studies on animals did not reveal teratogenic effect of tolperizone. Because of the lack of significant clinical data, tolperizone should not be used in pregnancy (especially in the first trimester), except when the expected benefits definitely justify the potential risk to the fetus.

Breastfeeding period

There is no data on excretion of tolperizone with breast milk, so the use of the drug during breastfeeding is contraindicated.

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