Midocalm Richter solution for injection, 1ml No. 5

• Symptomatic treatment of stroke-related spasticity in adults;

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

Adults daily 1 ml (100 mg tolperisone) 2 times / day, i / m or 1 ml (100 mg tolperisone) 1 time / day i / v, slowly.

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.

Application in children

The drug Midocalm-Richter is not intended for use in children and adolescents under the age of 18 years.

The solution for intravenous and intramuscular administration is transparent, colorless or slightly greenish, with a characteristic odor.

1 ml

tolperisone hydrochloride 100 mg

lidocaine hydrochloride 2.5 mg

Excipients: methyl parahydroxybenzoate, diethylene glycol monoethyl ether, water d / i.

• Hypersensitivity to tolperisone or chemically similar eperisone or to any of the components of the drug (including lidocaine);

• myasthenia gravis;

• pregnancy;

• breastfeeding period;

• children and adolescents under 18 years of age.

Carefully

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

pharmachologic effect

Tolperisone hydrochloride is a centrally acting muscle relaxant. It has a membrane stabilizing, local anesthetic effect, inhibits the conduction of nerve impulses in the primary afferent fibers and motor neurons, which leads to blocking of spinal mono- and polysynaptic reflexes. Presumably, tolperisone mediates blocking the release of mediators by inhibiting the flow of calcium ions into synapses. It inhibits the conduction of excitation along the reticulospinal pathway in the brain stem.

Regardless of the effect on the central nervous system, it enhances peripheral circulation. This action is not associated with the effect of the drug on the central nervous system and may be due to the weak antispasmodic and antiadrenergic action of tolperisone.

Lidocaine hydrochloride has a local anesthetic effect and, when dosed according to the instructions, does not have a systemic effect.

Pharmacokinetics

Tolperisone is extensively metabolized in the liver and kidneys. It is excreted by the kidneys, almost completely (more than 99%) in the form of metabolites, the pharmacological activity of which is unknown. With intravenous administration, T1 / 2 is approximately 1.5 hours.

Lidocaine: absorption - complete (the rate of absorption depends on the site of administration and dose). TCmax with intramuscular injection - 30-45 min. Plasma protein binding - 50-80%.

It is quickly distributed in tissues and organs. Penetrates the BBB and the placental barrier, secreted with breast milk (40% of the concentration in the mother's plasma). It is metabolized in the liver (90-95%) with the participation of microsomal enzymes by dealkylation of the amino group and rupture of the amide bond with the formation of active metabolites. It is excreted in the bile (part of the dose is reabsorbed in the gastrointestinal tract) and by the kidneys (up to 10% unchanged).

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 gastrointestinal tract: 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 and connective tissue: infrequently - muscle weakness, myalgia, pain in the extremities; rarely - discomfort in the limbs; very rarely - osteopenia.

General disorders and disorders at the injection site: 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

Pregnancy

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.

Breastfeeding period

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

Application for violations of liver function

The drug should be used with caution in liver failure. No dose adjustment is required.

Application for impaired renal function

The drug should be used with caution in case of renal failure. No dose adjustment is required.

Application in children

The use is contraindicated under the age of 18 years.

special instructions

The most frequent 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 a history of allergies may be at a higher risk of hypersensitivity to tolperisone.

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

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

Excipients

The drug contains methyl parahydroxybenzoate, which can cause allergic reactions (possibly delayed) and, in exceptional cases, bronchospasm.

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 using 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, ataxia, tonic-clonic seizures, shortness of breath and respiratory paralysis.

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

Drug interactions

Studies of pharmacokinetic drug interactions with a marker substrate of the CYP2D6 isoenzyme dextrametorphan have shown that the simultaneous use of tolperisone can increase the blood levels of drugs that are metabolized mainly by the CYP2D6 isoenzyme (thioridazine, tolterodine, venlafaxine, atomoxetine, desipramine, neboloprometorphan).

In laboratory experiments on human liver microsomes and human hepatocytes, significant inhibition or induction of other CYP isoenzymes (CYP2B6, CYP2C8, CYP2C9, CYP2C19, CYP1A2, CYP3A4) was not found.

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

Despite the fact that tolperisone is a centrally acting drug, its sedative effect is very low. With simultaneous use with other centrally acting muscle relaxants, the dose of tolperisone should be reduced.

Tolperisone enhances the effect of niflumic acid, therefore, with simultaneous use, a decrease in the dose of niflumic acid or other NSAIDs should be considered.