Lidamitol solution for injection 100mg / + 2.5mg / ml, 1ml No. 5

• Hypertonicity and spasm of striated muscles arising from organic diseases of the central nervous system (including lesions of the pyramidal tract, multiple sclerosis, stroke, myelopathy, encephalomyelitis), musculoskeletal system (including spondylosis, spondyloarthrosis, cervical and lumbar syndromes, arthrosis of large joints);

• rehabilitation treatment after orthopedic and traumatological operations.

  As part of complex therapy:

• with obliterating vascular diseases (obliterating atherosclerosis, diabetic angiopathy, thromboangiitis obliterans, Raynaud's disease, diffuse scleroderma);

• in diseases arising on the basis of a disorder of the innervation of the vessels (acrocyanosis, intermittent angioedema dysbasia).

Adults daily 1 ml 2 times a day intramuscularly or 1 ml 1 time a day intravenously.

The procedure for working with a polymer ampoule:

1. Take the ampoule and shake it while holding the neck.

2. Rotate and separate the valve from the ampoule.

3. Immediately connect the luer of the syringe to the ampoule through the hole formed.

4. Draw the contents of the ampoule into the syringe.

5. Put the needle on the syringe.

Solution for intravenous and intramuscular administration in the form of a transparent, colorless or colored liquid with a specific odor.

1 amp.

tolperisone hydrochloride 100 mg

lidocaine hydrochloride (in the form of lidocaine hydrochloride monohydrate) 2.5 mg

Excipients: methyl parahydroxybenzoate - 0.6 mg, propylene glycol - 0.3 ml, 0.1 M hydrochloric acid solution - up to pH 3.0-4.5, water d / i - up to 1 ml.

• Hypersensitivity to the components of the drug, severe myasthenia gravis;

• pregnancy, breastfeeding period;

• children and adolescents up to 18 years old;

• The agent should be used with caution in renal and hepatic insufficiency (dose adjustment is not required).

pharmachologic effect

Combined product, the action of which is due to the properties of the components that make up its composition.

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. Probably, it 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 blood flow. The weak antispasmodic and antiadrenergic effect of tolperisone may play a role in the development of this effect.

Lidocaine hydrochloride has a local anesthetic effect; when used in recommended doses, it does not have a systemic effect.

Pharmacokinetics

Tolperisone hydrochloride

Tolperisone is extensively metabolized in the liver and kidneys. Excreted in the urine almost exclusively (> 99%) as metabolites. The pharmacological activity of the metabolites is unknown. T1 / 2 after intravenous administration - about 1.5 hours.

Lidocaine hydrochloride

Absorption - complete (absorption rate depends on the site of administration and dose). Time to reach Cmax in blood plasma with intramuscular injection is 30-45 minutes. Plasma protein binding - 50-80%.

It is quickly distributed in tissues and organs. Penetrates the BBB and the placental barrier, enters breast milk (40% 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 hematopoietic system: very rarely - anemia, lymphadenopathy.

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

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

Mental disorders: infrequently - insomnia, sleep disorders; rarely - loss of activity, depression.

From the nervous system: infrequently - headache, dizziness, drowsiness; rarely - attention deficit disorder, tremors, seizures, loss of sensitivity, sensory disorders, lethargy.

From the side of the organ of vision: rarely - visual impairment.

On the part of the organ of hearing and labyrinth disorders: rarely - ringing in the ears, vertigo.

From the side of the cardiovascular system: infrequently - arterial hypotension; rarely - angina pectoris, tachycardia, heart palpitations; very rarely - bradycardia, flushing.

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

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

Skin and subcutaneous tissue disorders: rarely - allergic dermatitis, sweating, pruritus, urticaria, skin rash.

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

From the urinary system: rarely - enuresis, proteinuria.

General disorders and disorders at the injection site: often - redness of the injection site; infrequently - asthenia (weakness), malaise, fatigue; rarely - a feeling of intoxication, a feeling of heat, irritability, thirst; very rarely - a feeling of discomfort in the chest.

Laboratory and instrumental data: rarely - a decrease in blood pressure, an increase in the concentration of bilirubin, a violation of liver function tests, a decrease in the number of platelets, an increase in the number of leukocytes; very rarely - an increase in creatinine levels.

Application during pregnancy and lactation

Use during pregnancy is indicated only in cases where the intended benefit to the mother outweighs the potential risk to the fetus.

During the period of treatment, it is necessary to resolve the issue of stopping breastfeeding.

Use during pregnancy and breastfeeding is contraindicated.

Application for violations of liver function

It should be used with caution in liver failure (dose adjustment is not required).

Application for impaired renal function

It should be used with caution in renal failure (dose adjustment is not required).

Application in children

It is contraindicated for use in children and adolescents under 18 years of age.

special instructions

Influence on the ability to drive vehicles and mechanisms

Care must be taken when driving vehicles and engaging in other potentially hazardous activities that require increased concentration of attention and speed of psychomotor reactions.

Drug interactions

There is no data on the interaction of this drug with other drugs, limiting the use of the drug.

Although tolperisone has an effect on the central nervous system, the agent does not cause a sedative effect, therefore it can be used in combination with sedatives, hypnotics and drugs containing ethanol.

Does not enhance the effect of ethanol on the central nervous system.

Strengthens the effect of NSAIDs, therefore, with simultaneous use, it may be necessary to reduce the dose of the latter.