Spazmaton (Tablets, Solution) Instructions for Use

ATC Code

N02BB52 (Metamizole sodium in combination with other drugs, excluding psycholeptics)

Active Substances

Metamizole sodium (Rec.INN registered by WHO)

Pitofenone (Rec.INN registered by WHO)

Fenpiverinium bromide (Rec.INN registered by WHO)

Clinical-Pharmacological Group

Spasm analgesic

Pharmacotherapeutic Group

Combined analgesic agent (non-narcotic analgesic agent + spasmolytic agent)

Pharmacological Action

Combined analgesic and spasmolytic agent. The combination of the components of the agent leads to a mutual enhancement of their pharmacological action.

Metamizole sodium is a pyrazolone derivative that has analgesic, antipyretic, and weak anti-inflammatory effects, the mechanism of which is associated with the inhibition of prostaglandin synthesis.

Pitofenone hydrochloride has a direct myotropic effect on the smooth muscles of internal organs and causes its relaxation (papaverine-like action).

Fenpiverinium bromide has an m-cholinolytic action and exerts an additional myotropic effect on smooth muscles.

Pharmacokinetics

Metamizole sodium

After parenteral administration, unchanged Metamizole sodium is not detected in the blood (only after IV administration it is detected in blood plasma in a low concentration and quickly becomes undetectable). After IM administration, the active substances of the agent are rapidly and substantially absorbed from the injection site.

Plasma protein binding is 50-60%. When used in therapeutic doses, it is excreted in breast milk.

Metamizole sodium undergoes intensive biotransformation in the liver. The main metabolites are 4-methylaminoantipyrine, 4-formylaminoantipyrine, 4-aminoantipyrine, and 4-acetylaminoantipyrine. About 20 additional metabolites have been identified, including glucuronic acid derivatives. The main four metabolites are found in the cerebrospinal fluid. It is excreted mainly by the kidneys.

Pitofenone

Rapidly distributed in organs and tissues, does not penetrate the BBB.

Metabolized in the liver by oxidative reactions. Excreted in the urine. T_1/2 is 1.8 h.

Fenpiverinium bromide

Does not penetrate the BBB. Excreted unchanged in the urine 32.4-40.4%, in the bile – 2.3-5.3%.

Indications

Pain syndrome (mild or moderate) with spasms of the smooth muscles of internal organs: renal colic, spasm of the ureter and bladder; biliary colic; biliary dyskinesia; postcholecystectomy syndrome; intestinal colic; chronic colitis; algodysmenorrhea; diseases of the pelvic organs.

For short-term treatment of arthralgia; myalgia; neuralgia, sciatica.

As an auxiliary medicinal product for pain syndrome after surgical interventions and diagnostic procedures.

ICD codes

Dosage Regimen

Solution

Used IM and IV. For adults and adolescents over 15 years of age with acute severe colic, administer IV slowly (1 ml over 1 min) 2 ml; if necessary, repeat after 6-8 hours. IM – 2-5 ml of solution 2-3 times/day. The maximum daily dose should not exceed 10 ml (which corresponds to 5 g of metamizole sodium).

The duration of the treatment course is determined depending on the clinical symptoms and etiopathogenesis of the disease, but should not exceed 5 days.

Dosage calculation for children with IV and IM administration: 3-11 months (5-8 kg) – IM only – 0.1-0.2 ml; 1-2 years (9-15 kg) – IV – 0.1-0.2 ml, IM – 0.2-0.3 ml; 3-4 years (16-23 kg) – IV – 0.2-0.3, IM – 0.3-0.4 ml; 5-7 years (24-30 kg) – IV – 0.3-0.4 ml, IM – 0.4-0.5 ml; 8-12 years (31-45 kg) – IV – 0.5-0.6 ml, IM – 0.6-0.7 ml; 12-15 years – IV and IM – 0.8-1 ml.

Before administering the injection solution, it should be warmed in the hand.

Tablets

Orally: after meals, without chewing, with water.

Recommended daily doses

For adults and children over 15 years 1-2 tablets 2-3 times a day. Maximum daily dose 6 tablets.

In children, the drug is used only as prescribed by a doctor.

For children

From 13 to 15 years – 1 tablet 2-3 times a day. Maximum daily dose – 6 tablets (1.5 tablets 4 times a day).

From 9 to 12 years – ¹/₂ tablet 2-3 times a day. Maximum daily dose – 4 tablets (1 tablet 4 times a day).

From 6 to 8 years – ¹/₂ tablet 2 times a day. Maximum daily dose – 2 tablets (¹/₂ tablet 4 times a day).

The duration of administration should not exceed more than 5 days.

Adverse Reactions

Allergic reactions urticaria (including on the conjunctiva and mucous membranes of the nasopharynx), angioedema, rarely – malignant exudative erythema (Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell’s syndrome), bronchospasm, anaphylactic shock.

From the hematopoietic system thrombocytopenia, leukopenia, agranulocytosis (may manifest with the following symptoms: unmotivated fever, chills, sore throat, difficulty swallowing, stomatitis, as well as the development of vaginitis or proctitis).

From the cardiovascular system decrease in BP.

From the urinary system impaired renal function, oliguria, anuria, proteinuria, interstitial nephritis, red coloration of urine.

Anticholinergic effects dry mouth, decreased sweating, accommodation paresis, tachycardia, difficult urination.

Local reactions with IM administration, infiltrates at the injection site are possible.

Contraindications

Hypersensitivity (including to pyrazolone derivatives); severe hepatic and/or renal impairment; bone marrow depression; glucose-6-phosphate dehydrogenase deficiency; tachyarrhythmia; severe angina; decompensated chronic heart failure; collapse; closed-angle glaucoma; prostatic hyperplasia (with clinical manifestations); intestinal obstruction; megacolon; pregnancy (especially the first trimester and the last 6 weeks); lactation period (breastfeeding); children under 3 months of age or body weight less than 5 kg (for IV administration).

With caution renal/hepatic impairment; bronchial asthma; tendency to arterial hypotension; hypersensitivity to NSAIDs; urticaria or acute rhinitis provoked by the intake of acetylsalicylic acid or other NSAIDs.

Use in Pregnancy and Lactation

The use of the agent is contraindicated during pregnancy (especially in the first trimester and the last 6 weeks).

If it is necessary to use the agent during lactation, breastfeeding should be discontinued.

Use in Hepatic Impairment

The use of the agent is contraindicated in severe hepatic impairment.

The agent should be prescribed with caution in hepatic impairment.

Use in Renal Impairment

The use of the agent is contraindicated in severe renal impairment.

The agent should be prescribed with caution in renal impairment.

Pediatric Use

IV administration of the agent is contraindicated in children under 3 months of age or with body weight less than 5 kg. The agent should be used for the treatment of children under 5 years of age only under medical supervision.

Special Precautions

With long-term (more than a week) treatment, monitoring of the peripheral blood picture and functional state of the liver is necessary.

If agranulocytosis is suspected or if thrombocytopenia is present, it is necessary to discontinue the use of the agent.

The use of the agent to relieve acute abdominal pain is unacceptable until the cause of the disease is clarified.

Intolerance is very rare, however, the threat of anaphylactic shock after IV administration of the agent is relatively higher than after oral administration of the agent.

In patients with atopic bronchial asthma and hay fever, the risk of developing allergic reactions increases.

Parenteral administration of the agent should be used only in cases where oral intake is impossible or absorption from the gastrointestinal tract is impaired.

IV injection should be performed slowly, with the patient in a lying position and under the control of BP, heart rate, and respiratory rate.

Particular caution is necessary when injecting more than 2 ml of solution (there is a risk of a sharp decrease in BP).

For IM administration, a long needle must be used.

When treating children under 5 years of age and patients receiving cytostatics, the use of metamizole sodium should be carried out only under medical supervision.

Red coloration of urine is possible due to the excretion of a metabolite (of no clinical significance).

During treatment with the agent, it is not recommended to take ethanol.

Effect on the ability to drive vehicles and mechanisms

During the use of the agent, patients should exercise caution when driving vehicles and mechanisms, as well as when engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Drug Interactions

Histamine H₁-receptor blockers, butyrophenones, phenothiazines, tricyclic antidepressants, amantadine and quinidine – possible enhancement of m-cholinolytic action.

Chlorpromazine or other phenothiazine derivatives – possible development of severe hyperthermia.

Non-narcotic analgesics, tricyclic antidepressants, oral hormonal contraceptives and allopurinol – increase the toxicity of the agent.

Phenylbutazone, barbiturates and other inducers of microsomal enzymes – reduction of the effectiveness of metamizole sodium.

Sedatives and anxiolytics (tranquilizers) – enhancement of the analgesic effect of metamizole sodium.

Radiocontrast agents, colloidal blood substitutes and penicillin – combinations with drugs containing Metamizole sodium should not be used.

Cyclosporine – possible decrease in the concentration of cyclosporine in the blood.

Oral hypoglycemic agents, indirect anticoagulants, corticosteroids and indomethacin – Metamizole sodium displaces these agents from protein binding, which may lead to an increase in the severity of their action.

Thiamazole and cytostatics – increased risk of leukopenia.

Medicinal products with myelotoxic action enhancement of the hematotoxic effect of the agent.

Codeine, histamine H₂-receptor blockers, propranolol – enhancement of the action of the agent due to slowing down the inactivation of metamizole sodium.

Ethanol – enhancement of the effects of ethanol.

The injection solution is pharmaceutically incompatible with other medicinal products.

Storage Conditions

Store at 2°C (36°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.