Analgin-chinin (Tablets) Instructions for Use

Marketing Authorization Holder

Sopharma, JSC (Bulgaria)

ATC Code

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

Active Substances

Metamizole sodium (Rec.INN registered by WHO)

Quinine (BAN adopted for use in the United Kingdom)

Dosage Form

Analgin-chinin

Film-coated tablets, 200 mg+50 mg: 20 pcs.

Dosage Form, Packaging, and Composition

Film-coated tablets green in color, round, biconvex.

Excipients: microcrystalline cellulose (Avicel PH101) – 75 mg, sodium carboxymethyl starch (primogel) – 26 mg, kollidon-25 (povidone) – 3 mg, talc – 5 mg, magnesium stearate – 1 mg.

Shell composition: talc – 4.1 mg, titanium dioxide – 1.3005 mg, eudragit L 12.5 P (methacrylic acid and methyl methacrylate copolymer) – 1.6832 mg, macrogol 400 – 1.1 mg, glycerol – 0.28 mg, castor oil – 0.036 mg, pigment green dye (quinoline yellow dye E104, patent blue V E131) – 0.0001 mg.

10 pcs. – blisters (2) – cardboard packs.

Clinical-Pharmacological Group

Combination analgesic-antipyretic

Pharmacotherapeutic Group

Non-narcotic analgesic agent

Pharmacological Action

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

Quinine depresses the thermoregulatory center, and in high doses – the auditory and visual areas of the cerebral hemispheres. Quinine also inhibits the development of erythrocytic forms of schizonts and gamonts of malaria by suppressing DNA replication, and has a local irritant and local anesthetic effect.

The pharmacological effect develops 20-40 minutes after taking the drug and reaches a maximum after 2 hours.

Pharmacokinetics

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.

Indications

Pain syndrome of various etiologies (including headache, neuralgia, arthralgia, myalgia, myositis, algodysmenorrhea, postoperative pain); renal and biliary colic (in combination with antispasmodics); febrile conditions in infectious and inflammatory diseases.

ICD codes

Dosage Regimen

Take orally. Based on Metamizole sodium, a single dose is 500 mg, the maximum single dose is 12 g, the maximum daily dose is 4 g. The maximum frequency of administration is 4 times/day.

The duration of administration (without consulting a doctor) as an antipyretic is no more than 3 days, as an analgesic – no more than 5 days.

The minimum dose sufficient to control pain and fever should be used.

When used as an analgesic, the duration of therapy is 1-5 days; when used as an antipyretic, it is 1-3 days.

The drug should not be used for a long time or the dose increased without a doctor’s prescription.

If the pain syndrome persists or intensifies, it is necessary to consult a doctor to determine the cause of the symptoms. With long-term use, it is necessary to monitor the number of blood cells (including counting individual types of leukocytes).

Adverse Reactions

From the digestive system: nausea, vomiting, pain and discomfort in the epigastric region and abdominal area, diarrhea; rarely – ulceration of the gastrointestinal mucosa, gastrointestinal bleeding.

From the nervous system: headache, dizziness, rapid fatigue, insomnia, tremor of the extremities.

From the sensory organs: tinnitus and hearing loss, visual impairment (blurred vision, scotoma, photophobia, diplopia, decreased visual fields, impaired color vision).

From the cardiovascular system: angina pectoris, palpitations, fainting.

From the hematopoietic system: leukopenia, agranulocytosis, hypoprothrombinemia.

From the urinary system: impaired renal function (including oliguria, anuria, proteinuria), retention of water and electrolytes.

Allergic reactions: sometimes – itching, eczema, enanthema, urticaria, angioedema; rarely – anaphylactic shock; in some cases – malignant exudative erythema (Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell’s syndrome), bronchospastic syndrome.

Other: increased body temperature.

Contraindications

Hypersensitivity to metamizole sodium and other pyrazolone derivatives; severe liver dysfunction; severe renal dysfunction; bronchial asthma; asthma induced by salicylates or other NSAIDs; diseases accompanied by bronchospasm; hereditary hemolytic anemia caused by glucose-6-phosphate dehydrogenase deficiency; bone marrow depression (agranulocytosis, neutropenia, leukopenia); severe myasthenia gravis; diseases of the middle and inner ear, hearing loss; optic neuritis; pregnancy, breastfeeding period; children under 15 years of age.

With caution

Hypersensitivity to other NSAIDs, arterial hypotension, bronchial asthma, especially in combination with concomitant polypous rhinosinusitis, in case of food, drug or other forms of allergy (including hay fever, bronchial asthma), granulocytopenia (control of hematological parameters is necessary), alcoholism.

Use in Pregnancy and Lactation

Contraindicated for use during pregnancy and breastfeeding.

Use in Hepatic Impairment

Should be used with caution in patients with impaired liver function. Contraindicated in severe liver dysfunction.

Use in Renal Impairment

Should be used with caution in patients with impaired renal function. Contraindicated in severe renal dysfunction.

Pediatric Use

Contraindication: children under 15 years of age.

Geriatric Use

Elderly patients should reduce the dose, since the excretion of metamizole sodium metabolites may be slowed.

Special Precautions

During treatment, X-ray contrast agents, colloidal blood substitutes and penicillin should not be used.

With long-term (more than 7 days) use, peripheral blood counts should be monitored.

The drug should not be used for acute abdominal pain (until the cause is determined).

If side effects develop (including those not listed above), the patient should stop taking this drug and consult a doctor.

In patients suffering from bronchial asthma and hay fever, hypersensitivity reactions may develop.

Effect on the ability to drive vehicles and machinery

During use, you should not drive vehicles or work with machinery, because there is a risk of decreased ability to concentrate and speed of psychomotor reactions.

Drug Interactions

Simultaneous use of metamizole sodium with other analgesic-antipyretics may lead to mutual enhancement of toxic effects.

Tricyclic antidepressants, oral contraceptives, allopurinol disrupt the metabolism of metamizole sodium in the liver and increase its toxicity.

Barbiturates and phenylbutazone weaken the effect of metamizole sodium.

Sedatives and tranquilizers enhance the analgesic effect of metamizole sodium.

Metamizole sodium enhances the effect of ethanol-containing drinks.

Metamizole sodium, by displacing oral hypoglycemic drugs, indirect anticoagulants, corticosteroids and indomethacin from protein binding, enhances their effect.

Quinine may potentiate the effect of agents that block neuromuscular transmission.

Quinine increases the plasma concentration of digoxin and enhances its effect.

Cimetidine reduces the clearance and increases the T_1/2 of quinine.

Simultaneous use with cyclosporine reduces the level of the latter in the blood.

Inducers of microsomal oxidation accelerate metabolism and reduce the effectiveness of the drug; inhibitors of microsomal oxidation increase effectiveness and the risk of side effects.

When used simultaneously with thiamazole and sarcolysin, the risk of leukopenia increases.

Codeine, propranolol enhance the effect of this combination.

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.