Calmirex solution 2.5mg/ml+100mg/ml ampoules, 5pcs

Composition

Auxiliary substances:

methyl parahydroxybenzoate-0.6 mg,

diethylene glycol monoethyl ether-0.3 ml,

concentrated hydrochloric acid-up to pH 3.0-4.5,

d/i water – up to 1 ml

Pharmacological action

Clinical and pharmacological group: Central action muscle relaxantpharmacotherapy group: Central action muscle relaxantpharmacological action of Tolperisone hydrochloride is a central action muscle relaxant. It has a membrane-stabilizing, local anesthetic effect, inhibits the conduction of nerve impulses in primary afferent fibers and motor neurons, which leads to blocking of spinal mono – and polysynaptic reflexes. It probably mediates the blocking of the release of mediators by inhibiting the entry of calcium ions into synapses. Inhibits the conduction of excitation along the reticulospinal pathway in the brain stem. Regardless of its effect on the central nervous system, it increases peripheral blood flow. A 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 does not have a systemic effect when dosed according to the instructions. Pharmacokinetics of ATolperisone Hydrochloride ATolperisone is extensively metabolized in the liver and kidneys. It is excreted in the urine almost exclusively (>99%) as metabolites. The pharmacological activity of the metabolites is unknown. T 1/2 after intravenous use – about 1.5 h. Lidocaine hydrochloride absorption is complete (the rate of absorption depends on the site of use and dose). The time to reach Cmax in blood plasma with intravenous use is 30-45 minutes. Binding to plasma proteins is 50-80%. It is rapidly distributed in tissues and organs. Penetrates through the BBB and placental barrier, penetrates into breast milk (40% of the concentration in the mother’s plasma). It is metabolized in the liver (by 90-95%) with the participation of microsomal enzymes by dealkylation of the amino group and breaking 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 kidneys (up to 10% unchanged).

Indications

-hypertonus and spasm of striated muscles resulting from organic diseases of the central nervous system (including damage to the pyramidal pathways, 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, obliterating thrombangiitis, Raynaud’s disease, diffuse scleroderma);— in diseases that arise on the basis of vascular innervation disorders (acrocyanosis, intermittent angioedema).

Contraindications

-severe myasthenia gravis; – pregnancy; – lactation period— – children and adolescents under 18 years of age;- hypersensitivity to the components of the drug, including lidocaine. The drug should be used with caution in patients with renal and hepatic insufficiency (no dose adjustment is required).

Side effects

Frequency of side effects: very common (≥1/10), common (≥1/100 to <1/10), infrequent (≥1/1000 to <1/100), rare (≥1/10,000 to <1/1000), very rare (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, tremor, convulsions, loss of sensitivity, sensitivity disorders, lethargy. From the side of the visual organ: rarely-visual perception disorders. From the side of the organ of hearing and labyrinth disorders: rarely-tinnitus, vertigo. From the cardiovascular system: infrequently-hypotension; rarely-angina pectoris, tachycardia, rapid heartbeat; very rarely-bradycardia, hot flashes. From the respiratory system: rarely-shortness of breath, nosebleeds, rapid breathing. From the digestive system: infrequently-gastrointestinal discomfort, diarrhea, dry mouth, dyspepsia, nausea; rarely-epigastric pain, constipation, flatulence, vomiting, liver function disorders. From the skin and subcutaneous tissues: rarely-allergic dermatitis, sweating, pruritus, urticaria, skin rash. From the musculoskeletal system: infrequently-muscle weakness, myalgia, pain in the extremities; rarely – discomfort in the extremities; 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 bilirubin concentration, a violation of liver function tests, a decrease in the number of platelets, an increase in the number of white blood cells; very rarely – an increase in creatinine levels.

Interaction

There are no data on drug interactions limiting the use of Calmirex®. Although Tolperisone has an effect on the central nervous system, the drug does not cause sedation, so it can be used in combination with sedatives, sleeping pills and drugs containing ethanol. It does not enhance the effect of ethanol on the central nervous system. Increases the effect of NSAIDs, so when used simultaneously, it may be necessary to reduce the dose of the latter.

How to take, course of use and dosage

For adults, the drug is prescribed daily in / m at 100 mg 2 times/day or in / v at 100 mg 1 time/day.

Overdose

Symptoms: ataxia, tonic and clonic seizures, dyspnoea, respiratory arrest. Treatment: Symptomatic and supportive care is recommended. There is no specific antidote.

Special instructions

Influence on the ability to drive vehicles and mechanisms: You should be careful when driving vehicles and engaging in other potentially dangerous activities that require increased concentration of attention and speed of psychomotor reactions.

Form of production

Solution for intravenous and intramuscular use.

Storage conditions

The drug should be stored out of the reach of children, protected from light at a temperature of 8°C to 15°C.

Shelf

life is 2 years.

Active ingredient

Lidocaine, Tolperisone

Conditions of release from pharmacies

Prescription