Tolmio 2.5mg/ml +100 mg/ml 1 ml, 5 pcs.

Pharmacotherapeutic group:
central myorelaxant
ATX code:
MO3BX04
Pharmacological properties
Pharmacodynamics
Tolperisone hydrochloride is a central myorelaxant. The exact mechanism of action is unknown. As a result of its membrane-stabilizing action, it prevents excitation in primary afferent fibers by blocking mono- and polysynaptic reflexes of the spinal cord. Probably the secondary mechanism of action is to block the release of the transmitter by blocking the entry of calcium ions into synapses.
Reduces reflex readiness in the reticulospinal pathways of the brainstem.
Increases peripheral blood circulation. This effect is not related to the effect of the drug on the central nervous system and may be due to the weak antispasmodic and antiadrenergic action of tolperizone.
Lidocaine hydrochloride has local anesthetic effect and has no systemic action if the drug is dosed according to the instructions.
Pharmacokinetics
Tolperizone hydrochloride undergoes intensive metabolism in liver and kidneys. It is excreted by the kidneys, almost exclusively (>99%) as metabolites, pharmacological activity of which is unknown. With intravenous administration the elimination half-life is ~ 1.5 hours.
Lidocaine hydrochloride is completely absorbed (absorption rate depends on the site of administration and dose). Time of reaching maximum concentration during intramuscular injection is 30-45 min. Binding with plasma proteins is 50-80%. It is rapidly distributed in the tissues and organs. It penetrates the blood-brain barrier and placental barrier, is secreted with the mother’s 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 breaking the amide bond to form active metabolites. It is excreted with bile (part of the dose is reabsorbed in the gastrointestinal tract) and by the kidneys (up to 10% unchanged).

Indications

Active ingredient

Composition

How to take, the dosage

Interaction

Special Instructions

Contraindications

Side effects

World Health Organization (WHO) recommended frequency of side effects:

Blood and lymphatic system disorders: very rare – anemia, lymphadenopathy.
Immune system disorders: rare – hypersensitivity reactions, anaphylactic reactions, very rare – anaphylactic shock.
Metabolic and nutritional disorders: infrequent – anorexia; very rare – polydipsia.
Mental disorders: infrequent – insomnia, sleep disorders, rarely – loss of activity, depression.
Nervous system disorders: infrequent – headache, dizziness, somnolence, rarely – attention deficit syndrome, tremors, seizures, loss of sensitivity, sensory disorders, lethargy.
Visual disorders: rare – visual perception disorders.
Hearing organ disorders and labyrinth disorders: rarely – tinnitus, vertigo.
Heart disorders: rare – angina pectoris, tachycardia, palpitations, very rare – bradycardia.
Vascular disorders: infrequent – hypotension; rarely – hot flashes.
Respiratory system, chest and mediastinum disorders: rarely – shortness of breath, nasal bleeding, rapid breathing.
Gastrointestinal disorders: infrequent – gastrointestinal discomfort, diarrhea, dry mouth, dyspepsia, nausea, rarely – pain in epigastrium, constipation, flatulence, vomiting.
Liver and biliary tract disorders: rarely – liver function disorders.
Skin and subcutaneous tissue disorders: rare – allergic dermatitis, sweating, itching, urticaria, skin rash.
Musculoskeletal and connective tissue disorders: infrequent – muscle weakness, myalgia, pain in the extremities, rare – discomfort in the extremities, very rare – osteopenia.
Renal and urinary tract disorders: rarely – enuresis, proteinuria.
General disorders and disorders at the injection site: frequently – reddening of the injection site; infrequently – asthenia (weakness), malaise, fatigue; rarely – feeling of intoxication, fever, irritability, thirst; very rarely – feeling of discomfort in the chest.
Laboratory and instrumental data: rare – decreased blood pressure, increased bilirubin concentration, abnormal liver function tests, decreased platelet count, increased white blood cell count, very rare – increased creatinine level.

Overdose

Pregnancy use

Similarities