Pharmacological properties

Pharmacodynamics. spazmalgon — the combined medicine with analgeziruyushchy, spasmolytic (papaverinopodobny), cholinolytic (atropinopodobny) and some anti-inflammatory action.

Metamizole sodium possesses the expressed analgeziruyushchy and febrifugal action in a combination with less expressed anti-inflammatory and spasmolytic activity. Its effects are a consequence of oppression of synthesis of prostaglandins and endogenous allogenes, increases in an excitation threshold in a thalamus and carrying out painful ekstero- and interoceptive impulses in central nervous system; it also influences a hypothalamus and formation of endogenous pyrogens.

Fenpiveriny has moderate ganglioblokiruyushchy and parasympathetic effect, reduces a tone and motility of unstriated muscles of a stomach, intestines, bilious and urinary tract.

Pitofenon has papaverinopodobny effect on unstriated muscles of vessels and internals with the expressed spasmolytic effect.

Pharmacokinetics. The fast and full resorption is characteristic of metamizol. In 30 min. after intake in blood plasma the amount of medicine which is 50% of the C _{max is defined} . Partially contacts blood proteins. In a human body is exposed to intensive biotransformation. At the same time its main metabolites pharmacological are active. It Eliminirutsya with urine in the form of metabolites. Only 3% of quantity which is distinguished are represented by not changed metamizol. Degree of biotransformation is influenced also by genetically caused acetylation type. Data in available medical literature on processes of a resorption and distribution of a pitofenon and a fenpiveriniya very little. It is known that the resorption occurs in upper parts of a GIT and is incomplete. Chemical compounds are exposed to considerable ionization and have a weak liporastvorimost that determines the weak level of penetration through GEB. The profile of their concentration in blood plasma has two-phase character.

Pitofenon and fenpiveriniya is metabolized by

in a liver, mainly — by oxidation, at the same time about 90% of substance in the form of metabolites are removed with urine and about 10% — with a stake in the form of not changed connection. There are data that their T _½ makes 10 h of blood plasma. Separate components are removed with breast milk.

Indication

Symptomatic treatment at poorly and moderate pain syndrome at spasms of unstriated muscles of internals:

• renal colic and inflammatory diseases of urinary tract proceeding with pain and dysuric disorders;
• spasms of a stomach and intestines, hepatic colic, dyskinesia of bilious ways;
• spastic dysmenorrhea.

Use

Pill of a spazmalgon is taken inside after a meal, washing down with water. the recommended daily dose for adults and children aged from 15 years — on 1–2 tablets, the maximum daily dose — 2 tablets.

Duration of application of Spazmalgon — no more than 3 days.

Children. Spazmalgon do not appoint to children aged up to 15 years.

Contraindication

Hypersensitivity to metamizol, derivatives of pyrazyl ketone and/or any component of a medicinal soyedstvo; gastrointestinal impassability and megacolon; atony bilious or bladder; heavy renal failures and liver; change of composition of peripheral blood (Agranulocytosis, leukopenia); blood diseases (anemia of any etiology, cytostatic or infectious neutropenia); deficiency glyukozo-6-fosfatdegidrogenazy; liver porphyria; closed-angle glaucoma; suspicion of sharp surgical pathology; oh; kollaptoidny states; tachyarrhythmia; a prostatauxe with a tendency to an ischuria; period of pregnancy or feeding by a breast.

Side effects

Side reactions at use of medicine spazmalgon most often have temporality and disappear after the treatment termination.

from the immune system: urticaria, skin rashes, itch, conjunctivitis; seldom — a bronchospasm, a Quincke's disease, an acute anaphylaxis, a toxic epidermal necrolysis and Stephens's syndrome — Johnson.

from digestive system: discomfort, dryness in a mouth, a lock, exacerbation of gastritis, stomach ulcer and duodenum.

from a cardiovascular system: palpitation, decrease in the ABP, tachycardia, violations of a warm rhythm.

from nervous system: dizziness, disorder of vision.

from the system of blood formation: granulocytopenia, anemia, Agranulocytosis, thrombocytopenia, leukopenia.

from an urinary system: an oliguria, an anury, a proteinuria, coloring of urine in red color, development OPN and interstitial nephrite.

At prolonged use in high doses the depression of function of kidneys (especially at the persons having diseases of kidneys in the anamnesis), in certain cases — papillary necrosis is possible

.

Others: hepatitis, decrease in sweating.

Special instructions

use Drug with care at:

• renal failure and/or liver;
• stomach diseases (achalasia, gastroesophageal reflux, stenosis of peloric department of a stomach);
to
• tendency to arterial hypotension and orthostatic reactions;
• chronic bronchitis and a bronchospasm (medicine increases viscosity of a bronchial secret);
• presence of a hyperthyroidism;
• violations of a rhythm of warm activity, an ischemic heart disease (especially at a sharp myocardial infarction), chronic stagnant heart failure;
• availability of data on hypersensitivity to NPVP and/or non-narcotic analgesics or other manifestations of an allergy (allergic rhinitis).

At prolonged use of Spazmalgon needs to check a condition of peripheral blood and function of a liver.

emergence or increase in severity of the available headache after long-term analgetic treatment (3 months) at use of analgetics every other day and more often Is possible

.

Headache caused by excessive use of analgetics should not be stopped to

, raising their dose. In such cases the analgetic treatment needs to be stopped after consultation with the doctor.

Drug can affect a psychophysical condition of patients at simultaneous application with the alcohol and medicines suppressing central nervous system.

is not recommended to apply other medicines which part metamizol, along with Spazmalgon is.

Considering the content of starch wheat as a part of medicine, patients with a gluten enteropathy should not apply it.

Considering lactose content, it is not necessary to use this medicament to patients with rare congenital forms of intolerance of a galactose, insufficiency of lactase or a syndrome of glyukozo-galaktozny malabsorption.

Metabolites of metamizole sodium can change

color of urine to red that has no clinical value.

Use during pregnancy and feeding by a breast. Do not apply.

Ability to influence speed of response at control of vehicles or work with other mechanisms. During use of the medicine Spazmalgon it is necessary to be careful at control of vehicles or work with other mechanisms as because of existence of cholinolytic effect the prolonged use of Spazmalgon can lead to dizziness and disturbance of accommodation.

Interaction

Metamizol increases concentration in chloroquine blood plasma, reduces concentration in blood plasma and reduces expressiveness of effects of coumarinic anticoagulants and cyclosporine. increases gematotoksichesky effect of myelotoxic medicines, chloramphenicol. neuroleptics, sedative medicines and tranquilizers strengthen the anesthetizing effect of metamizol. tempidon and tricyclic antidepressants, oral contraceptives, Allopyrinolum break metabolism of metamizol and increase its toxicity. barbiturates, phenylbutazone and other inductors of microsomal enzymes of a liver can reduce expressiveness of effect of metamizol. the combined use of medicine with other analgetics and npvp increases risk of development of toxic effects. metamizol reduces concentration of cyclosporine and in blood plasma, its simultaneous application can be risky in case of the available transplantation of fabrics. combination of a spazmalgon and other medicines demands extra care in view of the content of metamizol which is the inductor of enzymes.

Overdose

Symptoms: at overdose, metamizol intoxication symptoms in a combination with cholinolytic effects prevail; abnormal liver function, kidneys, paralysis of airways. the toksiko-allergic syndrome, symptoms of defeat of functions of blood formation, gastrointestinal frustration, in hard cases — symptoms of damage of a brain is most often observed.

Treatment. At suspicion on overdose it is necessary to stop immediately use of medicine and to take measures to its fast removal from an organism (to cause vomiting, to make gastric lavage, to increase urine discharge). Apply symptomatic means. There is no specific antidote.

Storage conditions

B the dry, protected from light place at a temperature not above 25 °C.

Information on medicine for experts of health care.