Analgin - instructions for use, dose, side effects, contraindications

Excipients: - sucrose (sugar) - 6.7 mg, potato starch - 21.22 mg, calcium stearate-5.5 mg, talc -2.75 mg, povidone (polyvinylpyrrolidone low molecular weight medical 12600 ± 2700) - 8.33 mg, silicon colloidal dioxide (aerosil) - 5.5 mg.

Description:Tablets are white or white with a slightly yellowish hue of color, flat-cylindrical with a facet and a risk.

Pharmacotherapeutic group:Analgesic non-narcotic remedy

ATX: & nbsp

Metamizol sodium

Pharmacodynamics:

Analgin unselectively blocks cyclooxygenase and reduces the formation of prostaglandins from arachidonic acid, prevents painful extra- and proprioceptive impulses.Analgin has a weakly expressed anti-inflammatory effect, which causes a small effect on water-salt metabolism (sodium and water retention) and gastrointestinal mucosa. Has a spasmolytic effect on the smooth muscles of the urinary and biliary tract.

Metamizole sodium is a derivative of pyrazolone, which has analgesic, antipyretic and antispasmodic effect. The mechanism of action is not fully understood. According to the results of the studies metamizole and its active metabolite (4N-methylaminoantipyrine) possess a central and peripheral mechanism actions.

Pharmacokinetics:

Well and quickly absorbed from the digestive tract, which provides rapid development of clinical effect. The action develops 20-40 minutes after ingestion. When taken in therapeutic doses penetrates into the mother's milk. The maximum concentration in the plasma is achieved after 1-1,5 h after ingestion. In the intestinal wall, it hydrolyses with the formation of an active metabolite, 4-methyl-aminoglypirin, which in turn is metabolized to 4-formylamino-antipyrine and other metabolites. The level of binding of the active metabolite with proteins is 50-60%.Excretion of metabolites passes through the kidneys. In addition, metabolites are excreted in breast milk. After oral administration metamizol sodium is hydrolyzed to pharmacologically active 4N-methylaminoantipyrine (MAA). Bioavailability of MAA after oral administration is 90%, which is somewhat higher than with parenteral administration. Simultaneous food intake does not have a significant effect on the pharmacokinetics of metamizole sodium.

Clinical efficacy is determined primarily by MAA, and also to a lesser extent by metabolites 4N -aminoangipyrine (AA). The area under the "kontsen" curveTrace-time " (AUC) AA is 25% of this value for the IAA. Metabolites 4N -Acetylaminoantipyrine (AAA) and 4N-formylaminoantipyrine (FAA) do not possess pharmacological activity. All metabolites are characterized by non-linear pharmacokinetics. The clinical significance of this phenomenon is not known. In the short term, cumulation of metabolites does not play a big role. Metamizole sodium penetrates the placenta. Metabolites metamizole penetrate into breast milk. The connection with plasma proteins MAA is 58%, AA - 48%, FAA - 18% and AAA - 14%.After a single oral administration 85 % dose is found in the urine in the form of metabolites, of which 3 ± 1 % - MAA, 6 ± 3% - AA, 26 ± 8 % - AAA and 23 ± 4 % - FAA. Renal clearance after a single dose of 1 g of metamizole sodium inside for MAA is 5 ± 2 ml / min, AA - 38 ± 13 ml / min, AAA - 61 ± 8 ml / min and FAA - 49 ± 5 ml / min. The corresponding half-lives from plasma for MAA are 2.7 ± 0.5 h, AA - 3.7 ± 1.3 h, AAA - 9.5 ± 1.5 h and FAA - 11.2 ± 1.5 h.

Elderly

In elderly patients AUC increases 2-3 times. In patients with cirrhosis of the liver, the half-lives of MAA and FAA with a single dose of the drug increase approximately 3-fold, while the half-lives of AA and AAA do not follow the same pattern. Such patients should avoid the use of high doses.

Impaired renal function

According to available data, with renal failure, the rate of excretion of some metabolites (AAA and FAA) decreases. Such patients should avoid the use of high doses.

Indications:

Severe acute or chronic pain syndrome with trauma and postoperative pain syndrome, with colic, with oncological diseases and other conditions, where other therapeutic measures are contraindicated.

Fever resistant to other methods of treatment.

Contraindications:

Hypersensitivity to metamizole sodium and other pyrazolone derivatives, as well as to pyrazolidines, for example, phenylbutazone (including patients who have undergone agranulocytosis due to the use of these drugs), or other components of the drug;
Analgesic bronchial asthma or intolerance to analgesics (type of urticaria-angioneurotic edema), i.e. patients with bronchospasm or other forms of anaphylactoid reactions (eg urticaria, rhinitis, angioedema) in response to the use of salicylates, paracetamol or non-steroidal anti-inflammatory drugs such as diclofenac, ibuprofen, indomethacin or naproxen;
Disturbance of bone marrow hematopoiesis (eg, after cytostatic therapy) or diseases of the hematopoietic organs;
Congenital insufficiency of glucose-6-phosphate dehydrogenase (risk of hemolysis);
Acute intermittent hepatic porphyria (risk of developing porphyria attacks);
Children up to 15 years.

Carefully:

With kidney diseases (pyelonephritis, glomerulonephritis - including in the anamnesis), with mild renal impairment, bronchial asthma,chronic urticaria, predisposition to the development of arterial hypotension, acute cardiovascular pathology, myocardial infarction, long-term alcohol abuse, and also intolerance to dyes (tartrazine) and consideboards (benzoates). Relative contraindications: decompensation of cardiac activity. With caution apply the drug at a potential risk of severe anaphylactoid reactions and skin reactions.

Pregnancy and lactation:

During pregnancy and during lactation, the drug is contraindicated.

Pregnancy

Data on the use of sodium metamizole during pregnancy are limited. Metamizol sodium penetrates the placenta. According to the results of preclinical studies, the teratogenic effect of metamizole sodium was not detected. Although metamizol sodium weakly inhibits the synthesis of prostaglandins, premature (intrauterine) closure of the arterial duct, as well as perinatal complications caused by a violation of platelet aggregation in the mother or newborn can not be ruled out.

Breast-feeding

Metabolites metamizol sodium penetrate into breast milk, so when using the drug, as well as within 48 hours after the administration / administration of the last dose should be abandoned breastfeeding.

Dosing and Administration:

The dose depends on the severity of the pain or fever, as well as the individual susceptibility to the action of analgesics.

Tablets should be swallowed whole, squeezed with a sufficient amount of liquid (for example, a glass of water).

Initially, the lowest effective dose should be used.

The maximum effect of the drug develops, usually after 30-60 minutes after ingestion.

A single dose for adults and adolescents older than 15 years (with a body weight> 53 kg) is 250-500 mg (0.5-1 tablet). The maximum single dose is 1000 mg, the daily dose is 3000 mg (6 tablets).

Duration of reception no more than 5 days as an anesthetic and no more than 3 days as an antipyretic.

Elderly: elderly patients need to reduce the dose, because they can be reduced excretion of metamizole sodium metabolites.

Severe general condition and impaired creatinine clearance: patients with severe general condition and impaired creatinine clearance should reduce the dose,because they can be reduced excretion of metamizole sodium metabolites.

Renal or hepatic insufficiency: since in patients with impaired renal or hepatic function the rate of drug withdrawal is reduced, multiple high doses should be avoided. In the short term, dose reduction is not required. Experience with prolonged use is absent.

Side effects:

The frequency of potential adverse reactions is classified as follows: very often (> 1/10), often (> 1/100 to <1/10), infrequently (> 1/1000 to <1/100), rarely (> 1/10 000 up to <1/1000), very rarely (up to <1/10 000) and the frequency is unknown (it is impossible to estimate based on available data).

From the side of the blood and lymphatic system:

Rarely: leukopenia

Very rarely: agranulocytosis, aplastic anemia, including fatal cases, thrombocytopenia

There are a number of signs of increased risk of agranulocytosis. It is manifested by high fever, chills, sore throat, pain when swallowing, inflammation of the mucous membranes of the mouth, nose, throat, genital and anal area. A small increase in lymph nodes and spleen.

Tactics of treatment: involves the immediate cancellation of the drug.

When pancytopenia, the drug should be immediately abolished and monitor the total blood test before returning its indicators to normal.

From the immune system:

Rarely: anaphylactoid or anaphylactic reactions.

Very rarely: analgesic bronchial asthma. In patients with analgesic bronchial asthma, intolerance is usually manifested by attacks of bronchial asthma. Anaphylactic shock.

From the side of the vessels:

Infrequently: an isolated reduction in blood pressure (lowering blood pressure can be pronounced)

From the side of the kidneys and urinary tract:

Very rarely: acute renal dysfunction, which in very rare cases can lead to proteinuria, oligo- or anuria and acute renal failure, acute interstitial nephritis, urine staining to red.

From the skin and subcutaneous tissues:

Infrequent: persistent drug rash Rarely: rash (eg, maculopapular)

Very rarely: Stevens-Johnson syndrome, toxic epidermal necrolysis.

Overdose:

Symptoms: Acute overdose is manifested by nausea, vomiting, abdominal pain, impaired renal function / acute renal insufficiency (eg, as a manifestation of interstitial nephritis).Rarely: it is marked by symptoms from the side of the central nervous system (dizziness, drowsiness, coma, convulsions) and a decrease in arterial pressure leading to tachycardia and shock.

With a high overdose, the excretion of rubric acid can stain the urine red.

Treatment: a specific antidote is not known. In case of a recent overdose, in order to limit the intake of the drug, primary detoxification (for example, gastric lavage) or sorption therapy (for example, Activated carbon). The main metabolite (4N-methylaminoantipyrine) is removed during hemodialysis, haemofiltration, hemoperfusion and plasmafiltration.

Treatment of an overdose, as well as the prevention of serious complications, may require general and special intensive medical supervision and treatment.

With the development of convulsive syndrome - intravenous diazepam and high-speed barbiturates.

Interaction:

With cyclosporine: metamizol sodium can cause a decrease in the plasma concentration of cyclosporine, so when they are used simultaneously, the concentration of cyclosporin should be monitored.

With chlorpromazine: with the simultaneous use of metamizole sodium and chlorpromazine may develop severe hypothermia.

With methotrexate: simultaneous use of metamizole sodium and methotrexate or other myelotoxic agents may increase the hematotoxicity of the latter, especially in elderly patients. Therefore, this combination should be avoided.

With other non-narcotic analgesics: the simultaneous use of metamizole sodium with other non-narcotic analgesics can lead to a mutual enhancement of toxic effects.

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

With barbiturates, phenylbutazone and other inducers of microsomal liver enzymes: barbiturates, phenylbutazone and other inducers of microsomal liver enzymes weaken the action of metamizole sodium.

With sedatives and tranquilizers: sedatives and tranquilizers increase the analgesic effect of metamizole sodium.

With drugs that are highly associated with plasma proteins (oral hypoglycemic agents, indirect anticoagulants, glucocorticosteroids and indomethacin): metamizol sodium, displacing from the connection with plasma proteins, oral hypoglycemic agents, indirect anticoagulants, glucocorticosteroids and indomethacin, ortheir activity.

With timazole: Thymazole increases the risk of developing leukopenia.

With codeine, H blockers₂-gistaminovyh receptors and propranolol: codeine, blocktori H₂-gistaminovyh receptors and propranolol enhance the effects of metamizole sodium.

With acetylsalicylic acid (ASA): with simultaneous application metamizol sodium can reduce the effect of ASA on platelet aggregation. Therefore, this combination should be used with caution in the treatment of patients taking ASA as an antiplatelet agent.

With bupropion: metamizol sodium can reduce the concentration of bupropion in the blood, which should be taken into account when they are used simultaneously.

With other medicinal products: it is well known,that pyrazolone derivatives can interact with indirect anticoagulants, captopril, lithium and triamterene, and also affect the effectiveness of antihypertensive agents and diuretics. The drug interaction of metamizole sodium with these drugs has not yet been studied.

In view of the increased risk of anaphylactic / anaphylactoid reactions during treatment with metamizole sodium, radiocontrast agents, colloidal blood substitutes and penicillin should not be used.

Special instructions:

Patients who have anaphylactic or other immuno-mediated reactions (eg, agranulocytosis) in response to metamizole sodium use are also at risk of developing them in response to the use of other pyrazolones and pyrazolidines.

Pancytopenia, agranulocytosis

With the development of pancytopenia and agranulocytosis, the drug should be immediately discontinued and the general blood test should be monitored until the parameters return to normal. All patients should be advised to seek medical help immediately if there are signs and symptoms reminiscent of blood disorders during treatment (for example, general weakness,infection, persistent fever, the appearance of bruising, bleeding, pallor).

Anaphylactic / anaphylactoid reactions

Before using metamizole sodium it is necessary to conduct a thorough questioning of the patient. An increased risk of hypersensitivity reactions metamizol sodium stipulate the following states:

- analgesic bronchial asthma or intolerance to analgesics (type of urticaria-angioneurotic edema);

- bronchial asthma, especially accompanied by rhinosinusitis and polyposis of the nose;

- chronic urticaria;

- intolerance to dyes (eg tartrazine), preservatives (eg benzoates);

- alcohol intolerance.

Severe skin reactions

Stevens-Johnson syndrome (SDS) and toxic epidermal necrolysis (TEN). When there are signs of SS or TENS (such as a progressive skin rash, often accompanied by blisters or ulceration of the mucous membrane), treatment with metamizole should be stopped immediately and never restarted.

Skin reactions should be carefully monitored, especially during the first weeks of treatment.

Isolated hypotensive reactions

These reactions can be dose-dependent.The risk of such reactions is increased with: previous arterial hypotension, decreased circulating blood volume or dehydration, unstable hemodynamics, or acute circulatory disturbance (eg, in patients with myocardial infarction or trauma), in patients with high fever.

In such patients, detailed diagnostics should be carried out and careful monitoring should be performed.

In patients who have a reduction in blood pressure should be avoided at all costs, metamizol sodium It can only be used with careful monitoring of hemodynamic parameters.

Abdominal pain

It is inadmissible to use the drug to relieve acute pain in the abdomen (until finding out their cause).

Impaired renal or hepatic function

In patients with impaired renal or hepatic function metamizol sodium It is allowed only with a rigorous assessment of the benefits and risks, observing all necessary precautions.

Effect on the ability to drive transp. cf. and fur:

In the recommended range of doses, the influence on the concentration of attention and the speed of psychomotor reactions is not established. When taking high doses, it is recommended to use caution when driving vehicles,work with mechanisms and engage in other potentially dangerous activities that require increased concentration and speed of psychomotor reactions.

Form release / dosage:

Tablets 500 mg.

Packaging:

For 10 tablets in a contour non-jellied package or in a contour mesh package.

For 1 or 2 contour mesh packages along with the instruction for use are placed in a pack of cardboard.

For 700 contiguous cellless or contiguous cell packs, together with an equal number of instructions for use, are placed in a group package (for hospitals).

Storage conditions:

In a dry, dark place at a temperature of 2 to 25 ° C.

Keep out of the reach of children.

Shelf life:

5 years. Do not use after expiry date.

Terms of leave from pharmacies:Without recipe

Registration number:P N001051 / 01

Date of registration:18.04.2007 / 14.03.2016

Expiration Date:Unlimited

The owner of the registration certificate:DALHIMFARM, OJSC DALHIMFARM, OJSC Russia

Manufacturer: & nbsp

DALHIMFARM, OJSC Russia

Information update date: & nbsp25.08.2017

Illustrated instructions

Instructions

Analgin (Analgin)