Analginum

General characteristics. Structure:

Active ingredient: 500 mg of metamizole sodium in 1 tablet.

Excipients: potato starch, talc, icing sugar, calcium stearate.

Pharmacological properties:

Pharmacodynamics. Analginum possesses analgetic, febrifugal and antiinflammatory actions. Activity of cyclooxygenase oppresses, reduces formation of prostaglandins, endoperoxides, active oxygen radicals.

Reduces carrying out painful impulses on gangliobulbarny and spinotalamichesky paths, raises an excitation threshold of the thalamic centers of painful sensitivity. Increases a thermolysis.

Pharmacokinetics. At intake it is quickly and fully absorbed. The beginning of action fluctuates from 30 to 60 min. after intake and in 30 min. after parenteral administration and reaches a maximum in 2 h. In a wall of intestines it is hydrolyzed with formation of an active metabolite – invariable metamizol in blood is absent (only after intravenous administration its insignificant concentration are found in plasma).

Level of linkng of an active metabolite with proteins makes 50-60%. Collapses in a liver. Excretion passes through kidneys.

Indications to use:

-  an acute pain after an injury or operation;

-  the acute pains caused by spasms of muscles of internals;

-  the pain caused by tumoral process;

-  other acute or chronic megalgias when other medical actions are impossible;

-  the increased temperature, in the absence of effect of other febrifugal medicines.

Route of administration and doses:

The dosage depends on intensity of pain, fever and individual reaction in response to Analginum reception. The smallest effective doses controlling pain and fever have to be chosen. Tablets should be swallowed entirely, with enough liquid (for example, a glass of water).

For children 10 years and teenagers aged up to 14 years a single dose of metamizol of 8-16 mg/kg are more senior (as febrifugal – 10 mg/kg). To adults and teenagers 15 years (> are more senior than 53 kg) it is possible to accept to 1000 mg on one reception. In case of insufficient effect of a single dose, it is possible to accept the maximum single dose to 4 times in days. The table given below contains the recommended dosage and the maximum doses.

Age (Body weight)	Single dose	Maximum daily dose
10-14 years (32-53 kg)	on 1 tablet (500 mg of metamizole sodium)	to 4 tablets (2000 mg of metamizole sodium)
To adults and teenagers 15 years (> are more senior than 53 kg)	1-2 tablets (500-1000 mg of metamizole sodium	to 8 tablets (4000 mg of metamizole sodium)

Elderly patients. At elderly patients the dose has to be reduced as removal of metabolites can be slowed down at Analginum reception.

At depression of function of kidneys and disturbance of clearance of creatinine the dose has to be reduced as removal of metabolites can be slowed down.

Disturbance of renal or hepatic function. It is necessary to avoid high doses at reduced renal or hepatic function. Perhaps short-term use without dose decline. Prolonged use is inadmissible.

Duration of treatment depends on a look and disease severity. At long-term treatment regular control of blood, including calculation of leukocytes is required.

Features of use:

At use of drug development of an agranulocytosis in this connection at identification of unmotivated temperature increase, a fever, pharyngalgias, the complicated swallowing, stomatitis, and also an inflammation of external genitals and an anus immediate drug withdrawal is necessary is possible.

The risk of potentially heavy anaphylactoid reactions to Analginum considerably increases at patients with:

- a syndrome of asthma or a Quincke's disease on non-narcotic analgesics;

- bronchial asthma with accompanying rinosinusity and polyps in a nose, a chronic small tortoiseshell,

- intolerance of dyes (tartrazine) and preservatives (benzoates);

- intolerance of alcohol.

At appointment as the patient with acute cardiovascular pathology careful control of a hemodynamics in connection with hypotensive action is necessary. With care apply at patients with the level of the arterial pressure (AP) below 100 mm of mercury., at a myocardial infarction, a multiple injury, with anamnestic instructions on diseases of a liver and kidneys (pyelonephritis, a glomerulonephritis), at treatment by cytostatics, blood diseases. The risk of such reactions is also increased at patients with dehydration or dehydration, unstable arterial pressure or with the beginning circulatory unefficiency (for example, at patients with multiple injuries or heart attack), at patients with high temperature.

Careful survey and careful control is required from similar patients. Preventive measures (such as blood circulation stabilization) can be necessary for decrease in risk of hypotensive reactions.

In exceptional cases Analgin can be used at patients at whom the lowering of arterial pressure is inadmissible, for example, at heavy coronary heart disease or the corresponding stenosis of brain arteries. In such cases use of Analginum is possible only after careful control of indicators of a hemodynamics.

At patients with a renal or liver failure Analginum should be accepted only after careful assessment of advantage, risks and necessary precautionary measures.

At patients with the increased risk of anaphylactic reactions Analginum can be used only after the careful analysis of possible risks concerning the expected benefits. At reception of Analginum in such cases, the patient has to be controlled carefully for ensuring medical care and readiness for emergency situations.

Use of medicine for removal of acute abdominal pains is inadmissible (before clarification of the reason).

Coloring of urine in red color due to allocation of a metabolite is possible (does not matter).

Pregnancy and lactation. There are no sufficient data about safety of use of Analginum during pregnancy at people. In researches on animals of teratogenic effect at Analginum it is not revealed. As there are no sufficient data for people, Analginum should not be accepted in the first trimester of pregnancy, in the second trimester it is applied only after strict assessment of medical advantage and risk.

As Analginum is weak inhibitor of synthesis of prostaglandins, at the same time the possibility of premature closing of an arterial channel and perinatal complications is not excluded. Analginum is contraindicated during the last trimester of pregnancy.

Metabolites of Analginum are allocated in breast milk therefore its use at a lactation is not recommended. In exceptional cases feeding is possible later 48 h after analginum reception.

Influence on ability to drive the car or to work with the equipment. The recommended range of doses does not influence concentration and speed of response. As precautionary measures it is necessary to avoid driving of cars, vehicles or other dangerous types of activity at reception of high doses.

Side effects:

Frequency of the possible side effects which are listed below is defined as: very often (≥ 1/10); often (≥1/100 to <1/10); infrequently (≥ 1/1000 to <1/100); seldom (≥ 1/10 000 to <1/1000), it is very rare (<1/10 000) and it is unknown (it cannot be estimated on the basis of the available data).

Allergic reactions. Infrequently: rash; seldom: makulopapulezny dieback, anaphylactic or anaphylactoid reactions. Meet preferential within the first hour after reception. Are usually shown in the form of skin reactions, such as: an itch, burning, reddening, rash, hypostasis, it is rare − an asthma. Can proceed with more severe forms, such as: a small tortoiseshell, a Quincke's edema of heavy degree (including throats), a heavy bronchospasm, disturbances of a cordial rhythm, arterial hypotension (increase in arterial pressure sometimes precedes); very seldom: an analgetic - the induced bronchial asthma (including patients with an aspirinovy form have asthmas), Stephens-Johnson's syndrome or a Lyell's disease, shock.

Reception of Analginum at emergence of skin reactions has to be immediately stopped.

Blood and lymphatic system. Seldom: leukopenia. Very seldom: agranulocytosis or thrombocytopenia. These reactions probably are immunological. They can arise even if earlier Analginum was applied without complications. The risk of development of an agranulocytosis can be increased if Analgin is accepted more than 1 week.

The agranulocytosis is shown by high temperature, the fever, pharyngalgias complicated by swallowing, an inflammation in a mouth, a nose, a throat and generative organs or a proctal itch. The Blood Sedimentation Rate (BSR) considerably accelerates, the quantity of granulocytes considerably decreases or completely is absent. As a rule, but not always, values of hemoglobin, erythrocytes and thrombocytes remains within norms.

Reception of Analginum has to be immediately stopped, even in case of lack of results of laboratory diagnostic tests, on condition of sudden deterioration in the general condition of the patient.

Cardiovascular system. Infrequently: hypotensive reactions in time or after medicine use. Even at a hyperthermia there can be a lowering of arterial pressure without any signs of reaction of hypersensitivity.

Diseases of kidneys and urinary tract. Very seldom: acute deteriorations in renal function after which can develop a proteinuria, oligo-or an anury and an acute renal failure, acute intersticial nephrite. Coloring of urine in red color.

Interaction with other medicines:

Ethanol − amplifies effect of ethanol.

Chlorpromazinum or other derivatives фенотиазина− can lead simultaneous use to development of the expressed hypothermia.

Radiopaque substances, colloid blood substitutes and penicillin should be applied at treatment by Analginum.

Cyclosporine − at simultaneous use decreases concentration of cyclosporine in blood.

Peroral hypoglycemic drugs, indirect anticoagulants, glucocorticosteroids (GKS) and indometacin – Analgin increases activity of these drugs by replacement them from communication with protein.

Phenylbutazone, barbiturates and other gepatoinduktorypr simultaneous use reduce efficiency of Analginum.

Non-narcotic analgesics, tricyclic antidepressants, hormonal contraceptives and Allopyrinolum - simultaneous use of Analginum with these drugs can lead to strengthening of its toxicity.

Sedatives and tranquilizers (Sibazonum, Trioxazinum, valocordin) strengthen the anesthetizing effect of Analginum.

Codeine, antihistamines also propranololusilivat effect of Analginum.

Care at simultaneous use with sulfanamide glucose-lowering drugs (hypoglycemic action amplifies) and diuretics is necessary (furosemide).

Myelotoxic medicines, Thiamazolum and sarcolysine lead to strengthening of a gematotoksichnost.

Contraindications:

- hypersensitivity to Analgin and other derivatives of pyrazyl ketone or Pyrazolidinums (including patients at whom the agranulocytosis was revealed) or to any other components of tablets;

- children aged up to 10 years;

- first and last trimesters of pregnancy;

- aspirinovy asthma in the anamnesis or a syndrome of intolerance of non-steroidal anti-inflammatory drugs and analgetics (a small tortoiseshell, a Quincke's disease);

- dysfunction of marrow (for example, after treatment by cytostatics) or diseases of the hemopoietic system;

- the hereditary hemolitic anemia connected with deficit glyukozo-6-fosfatdegidrogenazy;

- the patient with systolic arterial pressure below 100 mm of mercury. at the acute alternating porphyria (risk of emergence of an attack of a porphyria).

With care appoint at diseases of kidneys (pyelonephritis, a glomerulonephritis − including in the anamnesis), a long alcohol abuse.

Overdose:

Symptoms: a hypothermia, the expressed lowering of arterial pressure, heartbeat, an asthma, a sonitus, nausea, vomiting, a gastralgia, weakness, an oliguria, an anury, drowsiness, nonsense, consciousness disturbance, tachycardia, a convulsive syndrome; development of an acute agranulocytosis, hemorrhagic syndrome, an acute renal and liver failure, paralysis of respiratory muscles is possible.

Treatment: induction of vomiting, probe gastric lavage, purpose of salt laxatives, absorbent carbon. Carrying out an artificial diuresis, hemodialysis, blood alkalization, the symptomatic therapy directed to maintenance of the vital functions. At development of a convulsive syndrome carry out intravenous administration of diazepam and high-speed barbiturates.

Storage conditions:

In the place protected from light and moisture, at a temperature not over 25 ºС. To store in the place, unavailable to children. A period of validity - 5 years. Medicine cannot be used after the term specified on packaging.

Issue conditions:

Without recipe

Packaging:

In a blister strip packaging No. 10, in packaging No. 10×2. In planimetric bezjyacheykovy packaging No. 10, in packaging No. 10×1.

For hospitals: in a blister strip packaging No. 10, in packaging No. 10×300. In planimetric bezjyacheykovy packaging No. 10, in packaging No. 10×390.