Analginum

General characteristics. Structure:

Active agent: Metamizole sodium (analginum) – 0,1 g and 0,25 g (in terms of dry matter);
Bases for suppositories:
Fat firm (витепсол (brands H 15, W 35), суппосир (brands NA 15, NAS 50)) - enough before receiving suppository weighing 1,25 g.
Description: Suppositories white, white with yellowish or color, white with a creamy shade, a torpedo-shaped form.

Pharmacological properties:

Pharmacodynamics. Derivative pyrazyl ketone, on the action mechanism significantly does not differ from non-steroidal anti-inflammatory drugs (not selectively blocks cyclooxygenase and reduces formation of prostaglandins from arachidonic acid).

Interferes with carrying out painful extra-and proprioceptive impulses on Gaulle and Burdakh's bunches, raises an excitation threshold of the thalamic centers of painful sensitivity, increases a thermolysis.

Drug renders analgeziruyushchy, febrifugal and some spasmolytic action (concerning smooth muscles of urinary and bilious tract).

Action develops in 20-40 minutes after use and reaches a maximum in 2 hours.

Distinctive feature of metamizole sodium is insignificant expressiveness of antiinflammatory effect, and also lack of influence on a water salt metabolism and a mucous membrane of a stomach.

Pharmacokinetics. Bioavailability makes 54%. It is metabolized in a liver, removed by kidneys. Not changed metamizole sodium in blood is not defined. Communication of metabolites with proteins - 50-60%.

Indications to use:

Feverish syndrome at acute respiratory diseases, children's infectious and other infectious and inflammatory diseases. Pain syndrome (weak and moderate expressiveness), including: headache, dentagra, neuralgia, mialgiya, arthralgia, bilious colic, renal colic, injuries, burns, postoperative pain syndrome, альгодисменорея

Route of administration and doses:

Rektalno. After a cleansing enema or spontaneous bowel emptying suppositories exempt from planimetric packaging (previously having cut it by means of scissors) and enter into a rectum.

The average daily dose makes 10 mg/kg of body weight in 2-3 receptions.

Suppositories on 100 mg are recommended for use for children: from 3 to 7 years – on 1-2 suppository 2 times a day.

Suppositories on 250 mg are recommended for use for children: from 7 to 14 years - on 1-2 suppository 2 times a day.

After administration of suppository the child has to be in a prone position of 20-30 minutes. Duration of treatment is no more than 3 days. Further treatment by drug according to the recommendation of the doctor.

Features of use:

It is not necessary to use along with the drugs containing metamizole sodium (Analginum) and non-steroidal anti-inflammatory drugs. At treatment of children of 3-5 years and children receiving cytostatic medicines, reception of metamizole sodium has to be carried out only under observation of the doctor.

The intolerance meets very seldom. The children sick with atopic bronchial asthma and pollinoses, have an increased risk of development of allergic reactions.

Against the background of reception of metamizole sodium development of an agranulocytosis in this connection, at identification of unmotivated rise in temperature, a fever, pharyngalgias, the complicated swallowing, stomatitis, erosive cankers of an oral cavity, a vaginitis or a proctitis, immediate drug withdrawal is necessary is possible. At prolonged use it is necessary to control a pattern of peripheral blood.

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

Coloring of urine in red color is possible.

Side effects:

Allergic reactions: small tortoiseshell, Quincke's disease, bronkhospastichesky syndrome, acute anaphylaxis. In rare instances - a malignant exudative erythema (Stephens-Johnson's syndrome), a toxic epidermal necrolysis (Lyell's disease).

From an urinary system: a renal failure, an oliguria, an anury, a proteinuria, intersticial nephrite, coloring of urine in red color.

From bodies of a hemopoiesis: agranulocytosis, leukopenia, thrombocytopenia.

Others: lowering of arterial pressure.

Interaction with other medicines:

Simultaneous use with Chlorpromazinum or other derivatives of a fenotiazin can lead to development of the expressed hyperthermia.

X-ray contrast medicines, colloid blood substitutes and penicillin should not be applied during treatment by metamizol.

At simultaneous use of cyclosporine concentration of the last in blood decreases.

Pharmaceutical activity of drugs which metamizole sodium forces out from communication with protein (peroral hypoglycemic medicines, indirect anticoagulants, glucocorticoids and indometacin) increases.

Phenylbutazone, barbiturates and other inductors of a microsomal oxidation in a liver at simultaneous use reduce efficiency of metamizole sodium.

Simultaneous use with other non-narcotic analgesics, tricyclic antidepressants, contraceptive hormonal medicines and Allopyrinolum can lead to strengthening of toxicity of metamizole sodium.

Sedative and anxiolytic medicines strengthen analgeziruyushchy effect of metamizole sodium.

Thiamazolum and cytostatics increase risk of development of a leukopenia.

The effect is strengthened by codeine, H2 blockers - histamine receptors and propranolol (slows down an inactivation).

Metamizole sodium strengthens effects of ethanol.

The medicines possessing a miyelotoksichnost at simultaneous use strengthen a drug gematotoksichnost

Contraindications:

Hypersensitivity. The bronchial asthma induced by reception of acetylsalicylic acid, salicylates or other non-steroidal anti-inflammatory drugs. Hemopoiesis oppression (agranulocytosis, cytostatic or infectious neutropenia). Anemia, a leukopenia, a liver and/or renal failure, the hereditary hemolitic anemia connected with deficit glyukozo-6-fosfatdegidrogenazy. Age up to 3 years.
With care: Diseases of kidneys (pyelonephritis, a glomerulonephritis - including in the anamnesis).

Overdose:

Symptoms: nausea, vomiting, pains in a stomach, an oliguria, a hypothermia, a lowering of arterial pressure, tachycardia, short wind, a sonitus, drowsiness, nonsense, consciousness disturbance, an acute agranulocytosis, a hemorrhagic syndrome, an acute renal and/or liver failure, spasms, paralysis of respiratory muscles.

Treatment: salt laxatives, carrying out an artificial diuresis, a hemodialysis, at development of a convulsive syndrome – intravenous administration of diazepam and high-speed barbiturates. There is no specific antidote.

Storage conditions:

To store in the place protected from light at a temperature not over 25 to °s.khranit in the place, unavailable to children.

Issue conditions:

Without recipe

Packaging:

Suppositories 100 mg and 250 mg, rectal for children. On 5 suppositories in a blister strip packaging. Two blister strip packagings together with the instruction on a medical use of drug place in a pack from a cardboard.