Pharmacological properties

a Pharmacodynamics.spazmalgon — the combined medicine with the expressed spasmolytic and analgeziruyushchy activity.

Metamizol has the expressed analgeziruyushchy and febrifugal effect in combination with weaker anti-inflammatory and spasmolytic activity. Its action is result of oppression of synthesis of prostaglandins and endogenous algogen, increases in an excitation threshold in a thalamus, influences on a hypothalamus and formation of endogenous pyrogens.

Fenpiverin has moderate ganglioblokiruyushchy and cholinolytic effect. Suppresses a tone and motility of unstriated muscles of a stomach, intestines, zhelche- and urinary tract.

Pitofenon's

hydrochloride shows papaverinopodobny action with the expressed spasmolytic activity in relation to unstriated muscles.

Pharmacokinetics. Absorption: at application in oil it rezorbirutsya quickly. System bioavailability of metamizol — 85%.

Distribution: metamizol contacts plasma proteins for 50–60%. Gets through GEB and a placental barrier. Distribution volume — about 0.7 l/kg of body weight.

Metabolism: metamizol is exposed to intensive biotransformation in a liver, and its main metabolites are pharmacological active. The C _max in blood plasma (concerning all metabolites) establish approximately in 30–90 min.

Removal: only 3% of the marked-out amount of metamizol — in not changed look.T _½ — about 10 h

are allocated with kidneys in the form of metabolites, and to

Patients with abnormal liver functions: The t _½ an active metabolite of 4-methyl-amino-antipyrine at patients with abnormal liver functions is extended approximately by 3 times. Treatment by metamizol in low doses is recommended to these patients.

Patients with renal failures: at patients with renal failures the extent of removal of some metabolites decreases. Treatment by metamizol in low doses is recommended to these patients.

Indication

Short-term symptomatic treatment at patients with a pain syndrome at spasms of unstriated muscles of internals: gastric or intestinal colic; renal colic at a nephrolithiasis; spastic dyskinesia of biliary tract; dysmenorrhea.

Use

Spazmalgon, solution for injections, are entered only by in oil! to apply only to short-term treatment!

Solution to injections should be applied under accurate control of the doctor in connection with risk of emergence of an acute anaphylaxis in patients with hypersensitivity to metamizol or derivatives of pyrazyl ketone.

Adults and children aged from 15 years. To adults and children 15 years are aged more senior (with the body weight of 53 kg) in oil to enter 2–5 ml of solution for injections. If necessary the dose is repeated in 6–8 h. The maximum daily dose should not exceed 6 ml of solution for injections (3 g of metamizole sodium are equivalent). Treatment duration — 2–3 days. After achievement of therapeutic effect it is possible to pass to treatment with oral anesthetics and antispasmodics. In case of lack of therapeutic effect to stop treatment.

Patients aged from 65 years. Usually there is no need for a dose decline. At patients with the abnormal liver functions and kidneys connected with age it is necessary to lower a dose as increase in T _½ metamizol metabolites is possible.

Patients with renal failures. Metamizol is removed with urine in the form of metabolites. At patients with a slight and moderate renal failure it is recommended to apply ½ doses to adults.

Patients with abnormal liver functions. At these patients of T _½ active metabolites of metamizol slows down. At persons with abnormal liver functions it is necessary to avoid use of medicine in high doses. At short-term application there is no need to reduce doses.

patients have

no sufficient experience of prolonged use with renal failures or a liver.

Contraindication

Hypersensitivity to the active agents derivative of pyrazyl ketone (including at patients with an agranulocytosis in the anamnesis at the previous use of similar medicines) or others npvp. heavy abnormal liver functions and kidneys. sharp hepatic porphyria. deficiency glyukozo-6-fosfatdegidrogenazy. impassability of a GIT and megacolon. violation of functions of marrow (for example after treatment by cytostatics). diseases of a hemopoietic system (Agranulocytosis, leukopenia, anemia of any etiology, including aplastic anemia, infectious neutropenia). adenoma of a prostate of ii and iii of degree. atony bilious and bladder. suspicion of surgical pathology. hypotonic states and hemodynamic instability. kollaptoidny states. tachyarrhythmia. closed-angle glaucoma. oh.

Side effects

Listed side reactions are caused generally by the metamizol which is a part of medicine.

from blood and lymphatic system: leukopenia, Agranulocytosis, thrombocytopenia, anemia (hemolytic anemia, aplastic anemia). The risk of appearance of an agranulocytosis cannot be predicted. The agranulocytosis can arise also at the patients applying metamizol in the past without emergence of similar side reactions.

from the immune system: an acute anaphylaxis, anaphylactic or anaphylactoid reactions, especially after parenteral application. Such reactions can arise at introduction of medicine or directly after the introduction termination, but can appear also in several hours. Usually they come within the first hour after an injection. Easier reactions are shown in the form of typical reactions from skin and a mucous membrane (such as itch, burning, reddening, urticaria, hypostases local or the general), short wind and is rare — complaints from a GIT. Easy reactions can pass into more severe forms with generalized urticaria, heavy angioedemy (including laryngeal), into a heavy bronchospasm, violation of a warm rhythm, decrease in the ABP (sometimes with the previous increase in the ABP). Therefore in case of any skin reaction of hypersensitivity, symptoms of a renal failure or gematotoksichesky reactions medicine should be cancelled immediately.

Asthmatic attack (at patients with analgetic asthma), circulator shock. Shock can be followed cold then, dizziness, drowsiness, consciousness changes, pallor of skin, squeezing in area of heart, shallow breathing or the Tachypnea, tachycardia, cold extremities, considerable decrease in the ABP. At the first signs of shock treatment it is necessary to cancel and take the appropriate measures of emergency aid.

from skin and hypodermic cellulose: the fixed medicinal dieback, makulopapulezny and other types of rashes, a Lyell's disease or Stephens's syndrome — Johnson, a Quincke's disease, sweating reduction.

in case of any skin reaction use of metamizol should be stopped immediately.

from nervous system: dizziness, headache.

from sense bodys (sight): visual violations, accommodation violation.

from a cardiovascular system: palpitation, tachycardia, violations of a warm rhythm, cyanosis, arterial hypotension, hyperaemia. Hypotensive reactions can seldom be shown in time or after application. They can be followed or not be followed by other symptoms of anaphylactoid or anaphylactic reactions. Seldom such reactions can be result of sharp decrease in the ABP. Fast in/in introduction increases risk of development of hypotensive reactions.

Critical decrease in the ABP without other signs of hypersensitivity is dose-dependent and can be shown by a hyper pyrexia.

from digestive system: dryness in a mouth, nausea, vomiting, an abdominal pain and discomfort, a lock, exacerbation of gastritis and stomach ulcer, in rare instances vomiting with impurity of blood and intestinal bleedings, ultseration, burning sensation in epigastric area.

from a liver and biliary tract: hepatitis.

from an urinary system: a proteinuria, an oliguria, an anury, a polyuria, interstitial nephrite, coloring of urine in red color, an ischuria, the complicated urination, violation of functions of kidneys.

from a respiratory system: bronchospasm.

General frustration and violations in the injection site: at parenteral application — an adynamy, pain in the injection site and local reactions.

Special instructions

At medicament treatment spazmalgon risk of development of anaphylactic reactions exists. at the first signs of hypersensitivity introduction of medicine it is necessary to stop and take immediately urgent measures for knocking over of a state (epinephrine, gks, antihistaminic medicines).

Risk of emergence of reactions of hypersensitivity (anaphylactoid reactions) at use of metamizol considerably increases at patients with:

• food and medicinal hypersensitivity or atopic disease (senny rhinitis);
• a syndrome of analgetic asthma or an analgetic idiosyncrasy in the form of a small tortoiseshell, an angioedema, especially at the accompanying rinosinusit and polyps of a nose;
• chronic small tortoiseshell;
• an idiosyncrasy to dyes (for example to tartrazine), to preservatives (for example to benzoates);
• intolerance of alcohol. Such patients react to use of the minimum quantity of alcoholic beverages such symptoms as sneezing, dacryagogue and the expressed disorder of vision. The similar intolerance of alcohol can be sign of not diagnosed syndrome of analgetic asthma.

Spazmalgon contains medicinal substance metamizol, at treatment which there is a small, but life-threatening risk of emergence of shock and an agranulocytosis. Development of an agranulocytosis does not depend on a dose and it cannot be predicted. It can appear after the first dose or after repeated application. Typical symptoms of an agranulocytosis is fever, a sore throat, morbidity when swallowing, inflammation of a mucous membrane of a mouth, nose, throat, anorectal and genital area. At sudden deterioration in the general state and emergence of symptoms of an agranulocytosis the treatment by metamizol should be stopped immediately, without waiting for laboratory confirmation.

needs to use Drug with care at patients with an alcoholism; to elderly people, as it can lead to increase in frequency of emergence of side reactions, especially from digestive system. It is necessary to use with care medicament to patients at simultaneous application with cytostatic medicines (only under control of the doctor).

not to apply

to knocking over of an acute pain in a stomach.

At the Spazmalgon medicament treatment of patients with hematologic diseases or having them in the anamnesis needs to carry out the ratio assessment risk/advantage and to control the hematologic status during treatment.

should use Drug with care at patients with renal failures and diseases of kidneys in the anamnesis (pyelonephritis, a glomerulonephritis).

In diseases of kidneys and a liver the mode of dosing should be selected individually because of possible side effects of metamizol on kidneys and increases in T _½ metamizol metabolites at dysfunctions of hepatocytes.

should use Drug with care at patients with obstructive gastrointestinal diseases (achalasia, a piloroduodenalny stenosis). Repeated use of the medicine Spazmalgon in these cases can cause a delay of evacuation of gastrointestinal contents and intoxication.

Use of the medicine Spazmalgon for patients with a gastroesophageal reflux disease, an intestines atony, inflammatory bowel diseases, including nonspecific ulcer colitis and Crohn's disease, glaucoma, a myasthenia gravis, heart diseases (arrhythmia, an ischemic heart disease, stagnant heart failure) demands extra care and control of the doctor.

should use Drug with care at patients with a myocardial infarction, with the expressed arterial hypotension and also at treatment of patients with systolic arterial blood pressure of 100 mm Hg.

metamizol which is a part of the medicine Spazmalgon can cause hypotensive reactions. These reactions depend on a dose and are more often observed at parenteral application. The risk of emergence of such reactions increases in the following cases:

• at patients with the previous arterial hypotension, reduction of volume of liquid and electrolytes or dehydration, an unstable hemodynamics or circulator insufficiency (for example at persons with a myocardial infarction or a polyinjury);
• at patients with fervescence.

At such patients should carry out the careful assessment of need of use of medicine and stringent control. There can be a need to take precautionary measures (for example blood circulation stabilization) for reduction of risk of development of arterial hypotension.

Spazmalgon should be applied only when carrying out careful control of a hemodynamics at patients at whom it is necessary to avoid decrease in the ABP without fail, for example, a heavy ischemic heart disease or a considerable stenosis of vessels of a brain.

Spazmalgon should apply only after strict assessment of a ratio advantage/risk and the taken appropriate measures of precaution at patients with renal failures or a liver.

should not exceed the recommended medicine doses.

Use during pregnancy and feeding by a breast. Pregnancy. Use of medicine during pregnancy contraindicated due to the lack of clinical data.

Feeding by a breast. As metabolites of metamizol are excreted with mother's milk, it is not necessary to appoint medicine during feeding a breast. If it is impossible to avoid use of medicine, it is necessary to stop feeding by a breast for 48 h from the moment of administration of medicine.

Children. Not to use medicament for treatment at children aged up to 15 years.

Ability to influence speed of response at control of vehicles or work with other mechanisms. Active agent the fenpiveriniya bromide has cholinolytic effect and can cause dizziness and violation of accommodation. Metamizol is capable to make an adverse effect on attention and to break speed of response. Patients who run vehicles or work with mechanisms, it is necessary to warn about possible side effect of medicine. The activity requiring special attention should be stopped before disappearance of side effects.

Interaction

medicine Combination spazmalgon with other medicines demands extra care because of the content of metamizol which is the inductor of liver enzymes.

At use of medicine should avoid alcohol intake as there is a possibility of mutual potentiation of action.

Coumarinic anticoagulants: at their combined application, metamizol can reduce activity of coumarinic anticoagulants as a result of induction of liver enzymes.

Chlorpromazinum and other derivatives of a fenotiazin: at simultaneous application with metamizol there is a risk of emergence of a heavy hypothermia.

Cyclosporine: metamizol lowers cyclosporine level in blood plasma at the combined application.

Chloramphenicol and other myelotoxic medicines: at simultaneous application with metamizol there is an increased risk of emergence of oppression of marrow.

Inductors of enzymes (barbiturates, glutetimid, phenylbutazone) can weaken effect of metamizol.

Metamizol considerably increases _{values C of max} Chloroquinum in blood plasma.

central nervous system Depressants at a combination with metamizol strengthen its analgeziruyushchy action.

Tricyclic antidepressants (Imipraminum, amitriptyline), oral contraceptive medicines, analgetics, Allopyrinolum and alcohol slow down metamizol metabolism, strengthen its action at simultaneous application and increase its toxicity.

Combined application with other analgetics and NPVP increases risk of development of manifestations of hypersensitivity and emergence of other side effects.

Sedatives and tranquilizers strengthen the anesthetizing effect of medicine.

At a concomitant use of the medicine Spazmalgon with medicines of quinine strengthening of anticholinergic effect is possible

.

Spazmalgon can be applied combined with giostsinbutilbromidy, furosemide, glibenclamide.

knows that they can interact with captopril, lithium, a methotrexate and Triamterenum and also to change

About a class of derivatives of pyrazyl ketone efficiency of antihypertensive medicines and diuretics. To what degree metamizol causes these interactions, it is unknown.

Incompatibility. Administration of medicine is combined with other medicines in one syringe inadmissibly.

Overdose

Symptoms: symptoms of metamizolovy intoxication combined with cholinolytic manifestations prevail. most often note a toksiko-allergic syndrome, a gematotoksichnost, gastrointestinal violations, cerebral manifestations, including a hypothermia, the expressed decrease hell, heart consciousness, an asthma, sonitus, nausea, a rovta, a gastralgia, weakness, an oliguria, an anury, drowsiness, nonsense, consciousness violation, tachycardia, a convulsive syndrome; development of a sharp aganulotsitoz, hemorrhagic syndrome, a sharp renal and liver failure, paralysis of respiratory muscles is possible.

Treatment: use of medicine stops and measures are taken for its fast removal from an organism (an artificial diuresis, introduction of water-salt solutions, if necessary — a hemodialysis). Apply symptomatic means. There is no specific antidote.

Storage conditions

In original packing at a temperature not above 25 °C. not to freeze!