I took pills, # 20

Weak or moderate pain syndrome with spasms of smooth muscles of internal organs: renal, hepatic, biliary and intestinal colic, biliary dyskinesia, algomenorrhea.

For short-term symptomatic treatment: arthralgia, neuralgia, myalgia, sciatica.

As an auxiliary drug: pain syndrome after surgical interventions and diagnostic procedures.

If necessary, the drug can be used to reduce elevated body temperature in case of colds and infectious and inflammatory diseases (tablets).

Inside

Adults and adolescents over 15 years old: 1-2 tab. 2-3 times / day, without chewing, with a small amount of liquid.

Children aged 12-14 years: single dose - 1 tab., Maximum daily dose - 6 tab. (1.5 tab. 4 times / day), children aged 8-11 years - 0.5 tab., The maximum daily dose - 4 tab. (1 tab. 4 times / day), children aged 5-7 years - 0.5 tab., the maximum daily dose - 2 tab. (0.5 tab. 4 times / day).

The tablets are pale yellow, round, flat, with beveled edges, scored on one side and 'MICRO' engraved on the other.

1 tab.

metamizole sodium 500 mg

pitofenone hydrochloride 5 mg

fenpiverinium bromide 0.1 mg

Excipients: lactose, corn starch (anhydrous), povidone, methylhydroxybenzoate, purified talc, magnesium stearate.

• Hypersensitivity to pyrazolone derivatives (butadione, tribuzone), other components of the drug,

• oppression of bone marrow hematopoiesis,

• stable and unstable angina pectoris,

• chronic heart failure in the stage of decompensation,

• severe liver or kidney dysfunction,

• deficiency of glucose-6-phosphate dehydrogenase,

• tachyarrhythmia,

• acute 'intermittent' porphyria,

• angle-closure glaucoma,

• hyperplasia of the prostate gland (with clinical manifestations),

• intestinal obstruction,

• megacolon,

• collapse,

• granulocytopenia,

• pregnancy (especially the first trimester and the last 6 weeks),

• breastfeeding period,

• children's age (up to 5 years - tablets, up to 3 months or with a body weight <5 kg - injection solution).

With caution and under the supervision of a physician - for patients with impaired liver or kidney function, with a tendency to arterial hypotension (SBP <100 mm Hg), bronchospasm, bronchial asthma, increased individual sensitivity to NSAIDs or non-narcotic analgesics (incl. History of aspirin triad).

For children and adolescents under 18 years of age, the drug should be used only as directed by a doctor.

pharmachologic effect

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

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

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

Fenpiverinium bromide has an m-anticholinergic effect and has an additional myotropic effect on smooth muscles.

Pharmacokinetics

Metamizole sodium

After oral administration, metamizole sodium is rapidly absorbed from the gastrointestinal tract. In the intestinal wall, it is hydrolyzed to form an active metabolite. Unchanged metamizole sodium in the blood is not detected (only after intravenous administration is it found in blood plasma in an insignificant concentration and quickly becomes unavailable for determination). After i / m administration, the active substances of the drug are rapidly and largely absorbed from the injection site.

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 derivatives of glucuronic acid. 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. Cmax in blood plasma is reached after 30-60 minutes. It is quickly distributed in organs and tissues, does not penetrate the BBB.

It is metabolized in the liver by oxidative reactions. It is excreted in the urine. “1 / 2 is 1.8 hours.

Fenpiverinium bromide

When taken orally, it is rapidly absorbed from the gastrointestinal tract. Cmax in blood plasma is reached within 1 hour. Does not penetrate the BBB. It is excreted unchanged in the urine 32.4-40.4%, in the bile - 2.3-5.3%.

Side effect

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

On the part of 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 side of the cardiovascular system: lowering blood pressure.

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

Anticholinergic effects: dry mouth, decreased sweating, accommodation paresis, tachycardia, difficulty urinating.

Local reactions: with intramuscular injection, infiltrates at the injection site are possible.

Application during pregnancy and lactation

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

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

Application for violations of liver function

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

The drug should be prescribed with caution in liver failure.

Application for impaired renal function

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

The drug should be prescribed with caution in case of renal failure.

special instructions

With prolonged (more than a week) treatment, it is necessary to control the picture of peripheral blood and the functional state of the liver.

If agranulocytosis is suspected or if thrombocytopenia is present, 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.

Intolerance is very rare, but the threat of anaphylactic shock after intravenous administration of the drug is relatively higher than after taking the drug inside.

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.

IV injection should be carried out slowly, with the patient lying down and under the control of blood pressure, heart rate and respiratory rate.

Special care must be taken when administering more than 2 ml of solution (there is a risk of a sharp decrease in blood pressure).

For intramuscular injection, a long needle must be used.

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

It is possible that urine is stained red due to the release of a metabolite (it has no clinical significance).

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

Influence on the ability to drive vehicles and mechanisms

During treatment, caution should be exercised by vehicle drivers and persons engaged in potentially hazardous activities that require the speed of psychomotor reactions.

Drug interactions

Blockers of histamine H1 receptors, butyrophenones, phenothiazines, tricyclic antidepressants, amantadine and quinidine - the m-anticholinergic action may be enhanced.

Chlorpromazine or other phenothiazine derivatives - severe hyperthermia may develop.

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

Phenylbutazone, barbiturates and other inducers of microsomal enzymes - a decrease in the effectiveness of metamizole sodium.

Sedatives and anxiolytics (tranquilizers) - enhance the analgesic effect of sodium metamizole.

Radiopaque drugs, colloidal blood substitutes and penicillin - combinations with drugs containing metamizole sodium should not be used.

Cyclosporine - a decrease in the concentration of cyclosporine in the blood is possible.

Oral hypoglycemic agents, indirect anticoagulants, GCS and indomethacin - sodium metamizole displaces these agents from the connection with proteins, as a result of which an increase in the severity of their action is possible.

Thiamazole and cytostatics - increase the risk of developing leukopenia.

Medicines with myelotoxic effect: increased hematotoxic effect of the drug.

Codeine, blockers of histamine H2-receptors, propranolol - an increase in the effect of the drug due to a slowdown in the inactivation of metamizole sodium.

Ethanol - enhance the effects of ethanol.

Solution for injection is pharmaceutically incompatible with other drugs.