Tempalgin

General characteristics. Structure:

Active agents: Metamizol sodium of 500 mg; Tempidon of 20 mg.

Other ingredients: starch wheat, cellulose microcrystallic (type 101), K 25 povidone, magnesium stearate, talc, titanium dioxide (Е 171), macrogoal 400, dye Evroblend green (Е 102, E 133), castor oil, glycerin, dibutyl phthalate, methacrylate copolymer (type A).

Pharmacological properties:

Metamizole sodium as analgeziruyushchy means has soothing and antiinflammatory effect. It slows down synthesis of prostaglandins, inhibiting TsOG, has the known membrane stabilizing effect, slows down formation of endogenous pyrogens.
Tempidon has the expressed anxiolytic activity and eliminates a condition of concern, fear and tension. Reduces motive excitement, has the central N-cholinolytic effect, strengthens and extends analgeziruyushchy effect of metamizol. Tempidon favorably influences also an emotional component of pain. The combination of metamizole sodium and a tempidon strengthens analgesic effect of metamizol and increases duration of its action.
After oral administration metamizol is hydrolyzed in a GIT. Active metabolites are 4-methyl-aminoantipyrine (MAA) and 4 aminoantipyrine (AA). MAA is characterized by a bystry and full resorption. Cmax in a blood plasma is reached within 1–2 h. Bioavailability of MAA makes about 90%. Food does not influence metamizol pharmacokinetics.
Tempidon rezorbirutsya in upper parts of a GIT. Therapeutic concentration in a blood plasma are established in 30 min. after reception.
Cmax in a blood plasma of 0,8 mkg/ml is reached within 60 min.
Metamizole sodium partially contacts blood plasma proteins.
The data obtained in pilot studies on animals show that distribution of a tempidon in fabrics considerable.
Metamizole sodium is exposed to intensive metabolism in a liver. Its main metabolites — 4-MMA, 4-AA — pharmacological are active.
It is removed with urine in the form of metabolites, and only 3% of the marked-out amount of metamizol reveal in not changed look. Metabolites of metamizol are allocated in breast milk.
Tempidon is brought with urine in not changed look, in quantity ⅔ the applied dose.
Patients with abnormal liver functions: Т½ an active metabolite of MAA at patients with abnormal liver functions it is extended approximately by 3 times. Treatment by metamizol in lower doses is recommended to this patients.
Patients with renal failures: at patients with a renal failure extent of removal of some metabolites is lowered. Treatment by metamizol in lower doses is recommended to this patients.

Indications to use:

Short symptomatic treatment at a pain syndrome, from weak to moderately expressed, at the following states: headache, dentagra and dental manipulations, mialgiya, neuralgia, arthralgia.

Route of administration and doses:

Pill is taken orally, washing down with water, it is more preferable after meal.
The course of treatment makes 3 days. Drug use longer span or in higher doses is possible only after consultation with the doctor.
Dosage
The dose depends on expressiveness of pain and individual sensitivity to drug.
Adults
Usual dose — on 1 tablet 1–2 times a day, depending on weight of clinical symptoms. The maximum single dose should not exceed 1 tablet. The maximum daily dose makes 2 tablets.
At dental manipulations — on 1 tablet in 30 min. before intervention.
Children are aged more senior than 15 years
On 1 tablet a day. The maximum daily dose — 1 tablet, depends on weight of clinical symptoms.
Patients are aged more senior than 65 years
Usually the dose decline is not required. Patients with age renal failures and a liver, have to have a short treatment. The maximum daily dose should not exceed 2 tablets.
Patients with an abnormal liver function
At such patients increase Т½ in metabolites of metamizol is possible. At patients with moderate defeats use of ½ recommended doses for adults is recommended (the maximum daily dose — 1 tablet).
Patients with a renal failure
Metamizol and its metabolites are emitted with kidneys. At patients with a renal failure treatment by drug Tempalgin should be carried out, applying ½ recommended doses to adults (the maximum daily dose — 1 tablet).

Features of use:

Treatment by drug Tempalgin (because of the content of metamizol) is carried out only a short span.
Prior to treatment of patients it is necessary to warn that at emergence of bleeding of gums, blanching of integuments, an adynamy, emergence of an enanthesis and mucous membranes it is necessary to stop administration of drug and to see immediately a doctor.
At more long treatment by drug Tempalgin is required to control a blood pattern, including a leukocytic formula because of the increased risk of development of an agranulocytosis.
It is not necessary to exceed the recommended drug doses. As metamizol has the antiinflammatory and anesthetizing properties, it can mask symptoms of an infection, symptoms of noninfectious diseases and complications with a pain syndrome that can complicate their diagnosis.
Use for children should be carried out under constant observation of the doctor. It is necessary to control qualitative and quantitative composition of peripheral blood.
It is necessary to apply carefully at patients with allergic diseases, hypersensitivity to analgetics and antirheumatic medicines (intolerance of analgetics) and to others medicinal means or to foodstuff, because of increase in risk of development of allergic reactions and asthmatic attacks.
With care it is necessary to apply at patients of such categories: advanced age — can lead to increase in frequency of side reactions, especially from a digestive tract; with renal failures, with diseases of function of kidneys in the anamnesis (pyelonephritis, a glomerulonephritis); with inflammatory diseases of intestines, including nonspecific ulcer colitis and a disease Krone; with cardiovascular insufficiency; with an alcoholism.
Metamizol can provoke hypotensive reactions. Treatment by drug Tempalgin should be carried out with extra care at patients with arterial hypotension, volume deficit or dehydration, unstable blood circulation.
At simultaneous use with alcohol the risk of development of side effects increases.
It is necessary to apply with care at patients with abnormal liver functions of moderate severity.
At administration of drug coloring of urine in red color due to removal of a metabolite of metamizole sodium is possible.
It is not necessary to use drug longer than an established period without consultation with the doctor! If symptoms of a disease do not begin to disappear or, on the contrary, the state of health will worsen, or there will be undesirable phenomena, it is necessary to stop administration of drug and to see behind consultation a doctor of rather further use.
The wheat starch which is a part of drug may contain only traces of gluten and it is considered safe for persons with a Gee's disease.
Tartrazine (E102) which can cause allergic reactions is a part of drug.
Use during pregnancy and feeding by a breast
Pregnancy period. Controlled clinical trials at pregnant women were not conducted and there are no data of observations on use of drug for this group. In spite of the fact that metamizol is weak inhibitor of synthesis of prostaglandins, there is a probability of premature closing of a botallov of a channel and perinatal complications as a result of decrease in aggregation of thrombocytes at a fruit and mother. Treatment by drug contraindicated pregnant women.
Feeding period breast. Metabolites of metamizol get into breast milk. In need of treatment by drug chest feeding should be stopped.
Children. Do not apply at children aged up to 15 years.
Ability to influence speed of response at control of vehicles or work with other mechanisms. Tempalgin reduces ability to concentration of attention and slows down conditioned reflexes therefore drivers of vehicles and persons whose work demands the high speed of mental and physical reactions should not appoint it.

Side effects:

At drug use Tempalgin possible side effects are more often caused by metamizole sodium.
Side reactions are classified by bodies and systems.
From system of blood and lymphatic system: agranulocytosis, leukopenia, aplastic anemia, thrombocytopenia, hemolitic anemia. The risk of emergence of an agranulocytosis cannot be provided. The agranulocytosis can appear also at patients who applied metamizol in the past without emergence of side effects. The risk of emergence of an agranulocytosis increases at prolonged use (> 1 week) metamizol.
From immune system: the fixed medicinal dieback, makulopapulezny rash, anaphylactic or anaphylactoid reactions. Easier actions are shown by typical reactions from skin and mucous membranes — an itch, burning, reddening, an urtikariya, hypostases (generalized or local), диспноэ and is rare — disturbances from a GIT. Such easy reactions can pass into more severe forms with a generalized urtikariya, a heavy Quincke's disease (including laryngeal), a heavy bronchospasm, disturbances of a cordial rhythm, decrease in the ABP (sometimes with the previous increase in the ABP), an asthmatic attack (at patients with aspirinovy asthma); Stephens's syndrome — Johnson and Layell; circulator shock.
From a metabolism and food: loss of appetite.
From a nervous system: headache, dizziness.
From heart: palpitation, tachycardia, cyanosis.
From vessels: arterial hypotension.
From a GIT: nausea, vomiting, pain and discomfort in a stomach; in isolated cases — ultseration and bleeding.
Gepatobiliarny disturbances: increase in level of liver enzymes (ASAT, ALAT), cholestasia, hyperbilirubinemia.
From kidneys and urinary tract: polyuria, oliguria, anury, proteinuria, intersticial nephrite. At use of drug in high doses — renal failures.

Interaction with other medicines:

Effect of tricyclic antidepressants (Imipraminum, amitriptyline), peroral contraceptive means, analgetics, Allopyrinolum and alcohol is exponentiated at simultaneous use with drug Tempalgin.
Simultaneous use with other analgetics and NPVP increases risk of development of manifestations of hypersensitivity and emergence of other side effects.
Barbiturates, глютетимид and phenylbutazone reduce expressiveness and time of pharmakodinamichesky effects of metamizol owing to induction of enzymes of a liver.
Metamizol reduces activity of coumarinic anticoagulants at simultaneous use as a result of induction of hepatic enzymes.
Analgeziruyushchy effect of drug is strengthened by sedatives and tranquilizers (diazepam, trimetozine, the combined drugs containing phenobarbital, этилбромизовалерианат, codeine, etc.).
Metamizol reduces concentration of cyclosporine in a blood plasma.
At simultaneous use with Chlorpromazinum there can come the hypothermia.
Cytostatics (Sacrolysinum, methotrexate), the gold drugs, mercazolil (Thiamazolum), chloramphenicol and other drugs braking a hemogenesis strengthen myelotoxic effect of metamizol.
Care at simultaneous use with diuretics is necessary (furosemide).
X-ray contrast medicines, colloid blood substitutes and penicillin should not be applied during treatment by metamizole sodium.
Tempidon exponentiates sedative action of hypnagogues, the general anesthetics, narcotic and non-narcotic analgesics.

Contraindications:

Hypersensitivity to active or to excipients of drug; hypersensitivity to other pyrazolon drugs; acute hepatic porphyria; inborn insufficiency glyukozo-6-fosfatdegidrogenazy; serious illness of kidneys or liver; dysfunction of marrow (for example after treatment by cytostatics) or diseases of system of blood (aplastic anemia, a leukopenia and an agranulocytosis); anemia of any etiology, cytostatic or infectious neutropenia; arterial hypotension with ABP values <100 mm of mercury.; period of pregnancy and feeding by a breast; children aged up to 15 years.

Overdose:

Symptoms: a gastrointestinal syndrome (nausea, vomiting, a stomach ache, at high doses — a hematemesis and a melena); a cerebral syndrome (the menyeropodobny phenomena, a sonitus, weakness, an ataxy, drowsiness, an apnoea, consciousness disturbance, nonsense, a coma with arterial hypotension and toniko-clonic spasms); hematologic syndrome (agranulocytosis, aplastic anemia, hemorrhagic diathesis); metabolic syndrome (metabolic alkalosis); a renal (renal) syndrome (from an oliguria to an anury); acute liver failure and OPN; a toksiko-allergic syndrome (violent уртикарная and petekhialny, sometimes to bark - or typhus-like rash; at some patients toksiko-allergic shock can develop); a hypothermia, a heart consciousness, the expressed decrease in the ABP, tachycardia, a dysphagy, short wind, gastralgia/gastritis, paralysis of respiratory muscles.
At the first symptoms of overdose it is necessary to ask for medical care immediately!
Treatment: symptomatic therapy — a gastric lavage, monitoring of activity of respiratory and cardiovascular systems, administration of liquids, an artificial diuresis, if necessary — a hemodialysis.

Storage conditions:

In original packaging (in the dry, protected from light place) at a temperature not above 25 °C.

Issue conditions:

According to the recipe

Packaging:

Tab. п / oh, No. 10, No. 20.