Spasmopharm (Solution) Instructions for Use

Marketing Authorization Holder

Danson-BG (Bulgaria)

Manufactured By

Vetprom, AD (Bulgaria)

ATC Code

A03DA02 (Pitophenone and analgesics)

Active Substances

Metamizole sodium (Rec.INN registered by WHO)

Pitofenone (Rec.INN registered by WHO)

Fenpiverinium bromide (Rec.INN registered by WHO)

Dosage Form

Spasmopharm

Solution for intramuscular injection 500 mg+2 mg+0.02 mg: amp. 2 ml or 5 ml 10 pcs.

Dosage Form, Packaging, and Composition

Solution for intramuscular injection from light yellow to greenish-yellow in color, transparent.

Excipients: water for injection – up to 1 ml.

2 ml – dark glass type I ampoules (10) – blisters (1) – cardboard boxes.
5 ml – dark glass type I ampoules (10) – blisters (1) – cardboard boxes.

Clinical-Pharmacological Group

Spasm analgesic

Pharmacotherapeutic Group

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

Pharmacological Action

Combined analgesic and spasmolytic agent.

Metamizole sodium has analgesic, antipyretic, and weak anti-inflammatory action, the mechanism of which is associated with the inhibition of prostaglandin synthesis.

Fenpiverinium bromide has a moderate m-cholinoblocking action, reduces the tone and motility of the smooth muscles of the stomach, intestines, biliary and urinary tracts.

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

Pharmacokinetics

Metamizole sodium

After intramuscular injection, unchanged Metamizole sodium is rapidly absorbed. The systemic bioavailability of sodium metamizole is about 85%.

Plasma protein binding is 50-60%. It penetrates the blood-brain barrier and placental barrier. V_d – about 0.7 l/kg.

When used in therapeutic doses, it is excreted in breast milk.

It undergoes intensive biotransformation in the liver. The main metabolites are 4-methylaminoantipyrine, 4-formylaminoantipyrine, 4-aminoantipyrine, and 4-acetylaminoantipyrine. Maximum plasma concentrations (of all metabolites) are reached approximately after 30-90 minutes.

It is excreted by the kidneys in the form of metabolites, about 3% – unchanged. T_1/2 – about 10 hours.

Pitofenone

Rapidly distributed in organs and tissues, does not penetrate the blood-brain barrier.

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

Fenpiverinium bromide

Does not penetrate the blood-brain barrier. Metabolized in the liver, mainly by oxidation. Almost 90% is excreted by the kidneys as metabolites and 10% through the intestines unchanged.

Indications

For short-term symptomatic treatment of acute pain syndrome of severe and moderate intensity during spasms of the smooth muscles of internal organs: gastric and intestinal colic; renal colic in renal stone disease; spastic dyskinesia of the biliary tract; algodysmenorrhea.

ICD codes

Dosage Regimen

Administer strictly intramuscularly. Use only for short-term symptomatic control of acute pain.

For adults and children over 15 years, inject 2 ml to 5 ml intramuscularly. Do not exceed this initial dose.

If required, a subsequent dose may be administered after 6-8 hours. Monitor patient response before re-administration.

The maximum daily dose must not exceed 6 ml, equivalent to 3 grams of metamizole sodium.

Limit the total duration of treatment to 2-3 days. Do not extend therapy beyond this period without re-evaluation.

Use a long needle for deep intramuscular injection to minimize local reactions. Avoid intravenous administration.

Discontinue use immediately if symptoms of agranulocytosis (e.g., fever, sore throat) or allergic reactions occur.

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 blood pressure.

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 intramuscular injection, infiltrates at the injection site are possible.

Contraindications

Hypersensitivity (including to pyrazolone derivatives); severe hepatic and/or renal impairment; acute hepatic porphyria; glucose-6-phosphate dehydrogenase deficiency; disorders of bone marrow hematopoiesis (for example, due to cytostatic treatment) and diseases of the hematopoietic system (agranulocytosis, leukopenia, aplastic anemia); prostate hyperplasia (with clinical manifestations); intestinal obstruction; megacolon; atony of the gallbladder and urinary bladder; arterial hypotension and hemodynamic instability; pregnancy (especially the first trimester and the last 6 weeks); lactation period (breastfeeding); children under 15 years of age.

Use in Pregnancy and Lactation

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

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

Use in Hepatic Impairment

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

The drug should be prescribed with caution in hepatic impairment.

Use in Renal Impairment

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

The drug should be prescribed with caution in renal impairment.

Pediatric Use

Contraindicated for use in children under 15 years of age.

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, the use of the drug should be discontinued.

The use of the drug for the relief of acute abdominal pain is unacceptable until the cause of the disease is clarified.

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

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

For intramuscular injection, a long needle must be used.

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

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

Effect on the ability to drive vehicles and mechanisms

During the use of the drug, 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-cholinoblocking 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 drug.

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

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

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.

Drugs with myelotoxic action enhancement of the hematotoxic effect of the drug.

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

Ethanol – enhancement of the effects of ethanol.

The injection solution is pharmaceutically incompatible with other drugs.

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.