Mydocalm tablets 150mg, No. 30

• Symptomatic treatment of stroke-related spasticity in adults;

• myofascial pain syndrome of moderate and severe degree (including muscle spasm with dorsopathies).

The drug is taken orally, after meals, without chewing, with a glass 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.

The recommended daily dose, depending on the individual need and the patient's tolerance of the drug, is 150-450 mg, divided into 3 doses.

Patients with renal impairment

Experience with the use of tolperisone in patients with renal insufficiency is limited, in this category of patients, adverse reactions often occurred. Therefore, in patients with moderate renal impairment, it is necessary to select a dose of tolperisone with careful monitoring of the patient's health and control of renal function. In severe kidney damage, the appointment of tolperisone is not recommended.

Patients with hepatic impairment

The experience of using tolperisone in patients with hepatic impairment is limited, in this category of patients adverse reactions often occurred. Therefore, in patients with moderate hepatic dysfunction, it is necessary to select a dose of tolperisone with careful monitoring of the patient's health and control of liver function. In severe liver damage, the appointment of tolperisone is not recommended.

Film-coated tablets

1 tab.

tolperisone hydrochloride

Excipients: citric acid monohydrate, colloidal silicon dioxide, stearic acid, talc, microcrystalline cellulose type 102, corn starch, lactose monohydrate.

• Hypersensitivity to any component of the drug or chemically similar epireson;

• myasthenia gravis;

• pregnancy;

• breastfeeding period;

• children under 18 years of age;

• intolerance to galactose, lactase deficiency, glucose-galactose malabsorption.

With caution: the drug should be used with caution in women, patients with hypersensitivity to lidocaine and / or other drugs, or with a history of allergies (see section 'Special instructions'), in patients with renal and hepatic insufficiency (see section' Dosage regimen ').

If the patient has any of the above conditions / diseases, it is imperative to consult a doctor before taking the drug.

pharmachologic effect

Tolperisone is a centrally acting muscle relaxant. The exact 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 the spinal reflex arcs. Probably, this effect, together with the elimination of the facilitation of the conduction of excitation 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 voltage-gated sodium channels. Accordingly, the amplitude and frequency of the action potential decreases.

An inhibitory effect on voltage-gated calcium channels has been proven.

It is assumed that in addition to its membrane-stabilizing action, tolperisone may also inhibit the release of the mediator. Tolperisone has some weak alpha-adrenergic antagonist properties and antimuscarinic action.

Pharmacokinetics

Suction

After oral administration, tolperisone is well absorbed in the small intestine. Plasma Cmax is observed 0.5-1.0 hours after administration. Due to the pronounced presystemic metabolism, bioavailability is about 20%. Food rich in fat increases the bioavailability of ingested tolperisone by about 100% and increases the plasma Cmax by about 45% compared to taking the drug on an empty stomach, delaying the time to reach Cmax by about 30 minutes.

Metabolism

Tolperisone is extensively metabolized in the liver and kidneys. The pharmacological activity of the metabolites is unknown.

Withdrawal

Almost completely (more than 99%) is excreted by the kidneys in the form of metabolites. T1 / 2 after oral administration - about 2.5 hours.

Side effect

From the side of the blood and lymphatic system: very rarely - anemia, lymphadenopathy.

From the immune system: rarely - hypersensitivity reaction, anaphylactic reaction; very rarely - anaphylactic shock; frequency unknown - angioedema, including edema of the face, lips.

From the side of metabolism: infrequently - anorexia; very rarely - polydipsia.

Mental disorders: infrequently - insomnia, sleep disturbances; rarely - decreased activity, depression; very rarely - confusion.

From the nervous system: infrequently - headache, dizziness, drowsiness; rarely - disturbance of attention, tremor, epilepsy, hypesthesia, paresthesia, lethargy.

From the side of the organ of vision: rarely - blurred vision.

On the part of the organ of hearing and labyrinthine disorders: rarely - tinnitus, vertigo.

From the side of the heart: rarely - angina pectoris, tachycardia, palpitations; very rarely - bradycardia.

From the side of the vessels: infrequently - arterial hypotension; rarely - hot flashes.

From the respiratory system: rarely - shortness of breath, epistaxis, rapid breathing.

From the digestive system: infrequently - abdominal discomfort, diarrhea, dry mouth, dyspepsia, nausea; rarely - epigastric pain, constipation, flatulence, vomiting.

From the liver and biliary tract: rarely - mild hepatic failure.

Skin and subcutaneous tissue disorders: rarely - allergic dermatitis, excessive sweating, itching, urticaria, rash.

From the side of the kidneys and urinary tract: rarely - enuresis, proteinuria.

From the musculoskeletal system: infrequently - muscle weakness, myalgia, pain in the limbs; rarely - discomfort in the limbs; very rarely - osteopenia.

General reactions: infrequently - asthenia, discomfort, fatigue; rarely - a feeling of intoxication, a feeling of heat, irritability, thirst; very rarely - chest discomfort.

Laboratory and instrumental data: rarely - lowering blood pressure, hyperbilirubinemia, changes in the activity of liver enzymes, thrombocytopenia, leukocytosis; very rarely - an increase in the concentration of creatinine in the blood plasma.

Application during pregnancy and lactation

In experimental studies on animals, no teratogenic effects of tolperisone have been revealed. Due to the lack of significant clinical data, tolperisone should not be used during pregnancy, unless the expected benefit definitely justifies the potential risk to the fetus.

Since there are no data on the release of tolperisone in breast milk, the use of the drug during breastfeeding is contraindicated.

Application for violations of liver function

The drug should be used with caution in liver failure.

Application for impaired renal function

The drug should be used with caution in case of renal failure.

Application in children

Use is contraindicated in children under 18 years of age.

special instructions

The most common adverse reactions when using tolperisone in the post-registration period were hypersensitivity reactions. Their severity ranges from mild skin reactions to severe systemic reactions, including anaphylactic shock. Symptoms of hypersensitivity reactions may include erythema, rash, urticaria, pruritus, angioedema, tachycardia, arterial hypotension, or shortness of breath.

Women and patients with hypersensitivity to other drugs or with a history of allergies may be at a higher risk of hypersensitivity to tolperisone.

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

Patients should be advised to be alert to possible allergy symptoms. Patients should be aware that if symptoms of allergy occur, they should stop taking tolperisone and seek immediate medical attention.

After an episode of hypersensitivity to tolperisone, the drug cannot be re-prescribed.

MidocalmЃ contains lactose monohydrate. Patients with rare hereditary galactose intolerance, lactase deficiency and glucose-galactose malabsorption should not take MydocalmЃ.

Influence on the ability to drive vehicles and mechanisms

Tolperisone does not affect the ability to drive vehicles and mechanisms. Patients who have dizziness, drowsiness, impaired attention, epilepsy, blurred vision, or muscle weakness while taking tolperisone should consult a doctor.

Overdose

Overdose symptoms most often include: drowsiness, gastrointestinal disturbances (nausea, vomiting, epigastric pain), tachycardia, increased blood pressure, bradykinesia and vertigo. In severe cases, convulsions and coma.

Treatment: there is no specific antidote, symptomatic therapy is recommended.

Drug interactions

In pharmacokinetic studies of drug interactions, it was found that the joint administration of tolperisone with the substrate of the CYP2D6 isoenzyme dextrametorphan increases the concentration in the blood of drugs that are metabolized predominantly by the CYP2D6 isoenzyme, for example, thioridazine, tolterodine, venlafaxine, atomoxetine, desipramine, dextrolopromethorphan, nebromethorphene, desipramine, dextrolopromethorphan, dextrolophene.

In vitro studies on human liver microsomes and human hepatocytes, pronounced inhibition or induction of other isoenzymes (CYP2B6, CYP2C8, CYP2C9, CYP2C19, CYP1A2, CYP3A4) have not been confirmed.

An increase in the exposure of tolperisone is not expected after the simultaneous administration of substrates of the isoenzyme CYP2D6 and / or other drugs due to the variety of metabolic pathways of tolperisone.

The bioavailability of tolperisone decreases when taken on an empty stomach, therefore, the use of the drug is recommended after a meal.

Although tolperisone affects the central nervous system, its potential for sedation is low. In the case of joint administration with other centrally acting muscle relaxants, the need to reduce the dose of tolperisone should be assessed.

Tolperisone enhances the effect of niflumic acid, therefore, the dose of niflumic acid or other NSAIDs should be reduced in case of simultaneous use with tolperisone.