Calmyrex solution for injection, 1ml # 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).

For adults, the drug is prescribed daily, intramuscularly, 100 mg 2 times / day, or intravenously, 100 mg 1 time / day.

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

1 amp.

tolperisone hydrochloride 100 mg

lidocaine hydrochloride 2.5 mg

Excipients: methyl parahydroxybenzoate - 0.6 mg, diethylene glycol monoethyl ether - 0.3 ml, concentrated hydrochloric acid - up to pH 3.0-4.5, water d / i - up to 1 ml.

• Severe myasthenia gravis;

• pregnancy;

• lactation period;

• children and adolescents up to 18 years old;

• hypersensitivity to drug components, incl. to lidocaine.

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

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. 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 and, when dosed according to the instructions, 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 and nutrition: 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

The use of the drug during pregnancy and lactation is contraindicated.

Application for violations of liver function

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

Application for impaired renal function

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

Application in children

The use of the drug in children and adolescents under 18 years of age is contraindicated.

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.

Overdose

Symptoms: ataxia, tonic and clonic seizures, dyspnea, respiratory arrest.

Treatment: symptomatic and supportive therapy is recommended. There is no specific antidote.

Drug interactions

There is no data on drug interactions limiting the use of CalmirexЃ.

Although tolperisone has an effect on the central nervous system, the drug 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.