Spasmastop^® (Tablets) Instructions for Use

Marketing Authorization Holder

YUGPHARM, LLC (Russia)

ATC Code

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

Active Substances

Metamizole sodium (Rec.INN registered by WHO)

Fenpiverinium bromide (Rec.INN registered by WHO)

Pitofenone (Rec.INN registered by WHO)

Dosage Form

Spasmastop®

Tablets 500 mg+5 mg+0.1 mg: 10, 20, 30, 40, 50, or 60 pcs.

Dosage Form, Packaging, and Composition

Tablets white or almost white, round, with a bevel and a score on one side.

Excipients: lactose monohydrate, povidone K25, magnesium stearate, colloidal silicon dioxide.

10 pcs. – blister packs (1) – cardboard packs.
10 pcs. – blister packs (2) – cardboard packs.
10 pcs. – blister packs (3) – cardboard packs.
10 pcs. – blister packs (4) – cardboard packs.
10 pcs. – blister packs (5) – cardboard packs.
30 pcs. – jars – cardboard packs.
40 pcs. – jars – cardboard packs.
50 pcs. – jars – cardboard packs.
60 pcs. – jars – cardboard packs.
100 pcs. – jars – cardboard packs.

Clinical-Pharmacological Group

Spasm analgesic

Pharmacotherapeutic Group

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

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 – a pyrazolone derivative, has analgesic, antipyretic and weak anti-inflammatory action, 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 oral administration, Metamizole sodium is rapidly absorbed from the gastrointestinal tract. It is hydrolyzed in the intestinal wall to form an active metabolite. Unchanged Metamizole sodium is not detected in the blood.

Plasma protein binding is 50-60%. When taken 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

It is rapidly absorbed from the gastrointestinal tract when taken orally. C_max in blood plasma is reached within 30-60 minutes. It is rapidly distributed in organs and tissues, does not penetrate the blood-brain barrier.

It is metabolized in the liver by oxidative reactions. It is excreted in the urine. T_1/2 is 1.8 hours.

Fenpiverinium bromide

When taken orally, it is rapidly absorbed from the gastrointestinal tract. C_max in blood plasma is reached within 1 hour. It does not penetrate the blood-brain barrier. It is excreted unchanged in the urine 32.4-40.4%, with bile – 2.3-5.3%.

Indications

Pain syndrome (mild or moderate) with spasms of 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

Administer tablets orally with a sufficient amount of water.

For adults and adolescents over 15 years of age, the typical single dose is one to two tablets.

Do not exceed a maximum single dose of two tablets.

The maximum daily dose is six tablets.

For children aged 5 to 7 years, administer half a tablet per dose.

For children aged 8 to 12 years, administer three-quarters of a tablet per dose.

For children aged 13 to 15 years, administer one tablet per dose.

Repeat dosing, if necessary, two to three times per day.

Maintain an interval of at least 4-6 hours between doses.

Adjust the dosage and frequency based on the intensity of pain and spasm, and the patient’s individual response.

Use the lowest effective dose for the shortest duration necessary to control symptoms.

The duration of treatment without medical supervision should not exceed three to five days as an analgesic.

Discontinue use immediately and consult a physician if pain persists or worsens.

Do not use to relieve acute abdominal pain until the cause is diagnosed by a physician.

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.

Contraindications

Hypersensitivity (including to pyrazolone derivatives); severe hepatic and/or renal impairment; bone marrow depression; glucose-6-phosphate dehydrogenase deficiency; tachyarrhythmia; severe angina pectoris; 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; children under 5 years of age.

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

The use of the agent orally is contraindicated in children under 5 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 agent should be discontinued.

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 intravenous 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.

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

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

Influence 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 action 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.

Drugs 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.

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

Over-the-Counter

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.