Spasmaton - instructions for use, dose, side effects, contraindications

active substances: metamizole sodium in terms of 100% substance - 2500 mg, pituophenone hydrochloride in terms of 100% substance - 10 mg, fenpiverinia bromide in terms of 100% substance - 0.10 mg;

Excipients: 0.1 M hydrochloric acid solution to pH 6.0, water for injection to 5.0 ml.

Description:Pgreenish-yellow translucent liquid.

Pharmacotherapeutic group:Analgesic combined (analgesic non-narcotic agent + antispasmodic)

ATX: & nbsp

N.02.B.B.52 Metamizole sodium in combination with other drugs, excluding psycholeptics

Pharmacodynamics:

Combined analgesic and antispasmodic agent, the combination of components of which leads to mutual potentiation of their pharmacological action.

Metamizol sodium - derivative of pyrazolone, has analgesic, antipyretic and anti-inflammatory effect.

Pitophenone has direct myotropic antispasmodic action on smooth muscles (papaverin-like action).

Fentipierinium bromide has m-anticholinergic action and has an additional myotropic antispasmodic effect on smooth muscles.

Pharmacokinetics:

Absorption

After intramuscular injection metamizol sodium quickly absorbed. Systemic bioavailability of metamizole sodium is about 85%.

Distribution

The connection with plasma proteins metamizole sodium is 50-60%. Penetrates through blood-brain and placental barriers. The volume of distribution is about 0.7 l / kg. Pitophenone and fenpiverinia bromide do not penetrate the blood-brain barrier.

Metabolism

Metamizole sodium is subjected to intensive biotransformation in the liver. Its main metabolite, 4-methylaminoantipyrine (MAA), is metabolized in the liver to form other metabolites, including pharmacologically active 4-aminoantipyrine (AA). The maximum plasma concentrations (of all metabolites) are reached after approximately 30-90 minutes.The four main metabolites of metamizole sodium are: 4-methylaminoantipyrine (MAA), active; 4-aminoantipyrine (AA), active; 4-formylaminoantipyrine (FAA), inactive; 4-acetylaminoantipyrine (AAA), inactive.

Pitophenone and fenpiverinia bromide are metabolized in the liver, mainly by oxidation.

Excretion

Metamizole sodium is excreted by the kidneys in the form of metabolites, about 3% - in unchanged form. The half-life is about 10 hours. In therapeutic concentrations it penetrates into breast milk.

The half-life of the pituopenone and fenpiverinium bromide is about 10 hours.

Almost 90% of the pituopenone and fenpiverinia bromide are excreted by the kidneys in the form of metabolites and 10% through the intestine in unchanged form.

Patients with hepatic impairment

The half-life of the MAA (active metabolite) in patients with impaired liver function increases approximately 3-fold. Such patients are recommended to lower the dose.

Patients with impaired renal function

In patients with impaired renal function, a decrease in the elimination of certain metabolites is observed. Such patients are recommended to lower the dose.

Indications:

For short-term symptomatic treatment of acute pain syndrome of strong and moderate severity with spasms of smooth muscles of internal organs:

- gastric and intestinal colic;

- renal colic in case of nephrolithiasis;

- spastic dyskinesia of bile ducts;

- algodismenorea.

Contraindications:

Hypersensitivity to the components of the drug, as well as to pyrazolone derivatives, inhibition of bone marrow hematopoiesis, disorders of bone marrow hematopoiesis (eg, due to treatment with cytostatics) or diseases of the hematopoietic system (agranulocytosis, leukopenia, aplastic anemia), marked hepatic and / or renal insufficiency, glucose-6 deficiency -phosphate dehydrogenase, tachyarrhythmias, severe angina pectoris, decompensated chronic heart failure, angle-closure glaucoma, prostatic hyperplasia glands (with clinical manifestations), intestinal obstruction, megacolon, collapse, pregnancy, lactation, atony of the gallbladder and urinary bladder.

For intravenous administration - infant age (up to 1 year) or body weight less than 9 kg.

For intramuscular injection - infant age (up to 3 months.) Or body weight less than 5 kg.

Carefully:

Renal and / or hepatic insufficiency, bronchial asthma, propensity to arterial hypotension,hypersensitivity to other non-steroidal anti-inflammatory drugs (NSAIDs) or non-narcotic analgesics, urticaria and / or acute rhinitis, triggered by the use of acetylsalicylic acid or other NSAIDs.

Pregnancy and lactation:

The use of the drug is contraindicated in pregnancy and during breastfeeding, tk. possibly premature closure of the arterial (Botallov) duct and perinatal complications due to the effect of metamizole sodium on the ability of platelets of the mother and fetus to aggregate.

Dosing and Administration:

Parenteral (intravenously (intravenously) and intramuscularly (IM)).

Adults and children over 15 years of age: single dose is 2-5 ml (IV or IM), daily dose - up to 10 ml.

In / in the administration of a single dose exceeding 2 ml (1 g in terms of metamizol sodium), is possible only after careful statement of testimony.

In any way of administration, the maximum single dose should not exceed 5 ml (equivalent to 2.5 g of metamizole sodium), the maximum daily dose should not exceed 10 ml of the solution (equivalent to 5 g of metamizole sodium). The maximum duration of treatment is no more than 5 days.

Children from 3 months to 15 years: a single dose is set taking into account the body weight (see table):

Body weight / age	Solution for injection, intravenous	Solution for injection, intramuscular injection
infants 5-8 kg; 3-11 months	intravenous administration is contraindicated	0.1-0.2 ml
children 9-15 kg; 1 -2 years	0.1-0.2 ml	0.2-0.3 ml
children 16-23 kg; 3-4 years	0.2-0.3 ml	0.3-0.4 ml
children 24-30 kg; 5-7 years	03, -0.4 ml	0.4-0.5 ml
children 31-45 kg; 8-12 years old	0.5-0.6 ml	0.6-0.7 ml
children 46-53 kg; 12-15 years old	0.8-1.0 ml	0.8-1.0 ml

If necessary, repeated administration of the drug in the same doses may be prescribed.

Patients over 65 years of age: as a rule, dose adjustment in this category of patients is not required. If such patients have renal or hepatic insufficiency, a dose reduction is recommended because of a possible increase in the half-life of metamizole sodium.

Patients with impaired hepatic and renal function: Maximum dosage should be avoided. It is possible to conduct short-term therapy (1-2 injections) without reducing the dose, but long-term use of Spasmaton for 2 or more days is possible only if the dose is reduced by 50% from that recommended for patients with normal liver and kidney function.In severe renal failure (creatinine clearance less than 30 ml / min), the dose should be reduced 3 times.

Before the injection of the injection solution, the ampoule with the drug should be warmed to the body temperature.

The solution is pharmaceutically incompatible with other drugs!

Side effects:

Adverse reactions (HP) are grouped according to systems and bodies in accordance with the vocabulary MedDRA and classification of the frequency of development HP WHO:

Very often (≥ 1/10)

Frequently (≥ 1/100 to <1/10)

Infrequently (≥ 1/1000 to <1/100)

Rarely (≥ 1/10000 to <1/1000)

Very rarely (<1/10000)

The frequency is unknown (the frequency can not be determined from the available data).

The undesirable reactions listed below are mainly caused by metamizol sodium, which is part of the drug.

On the part of the blood and lymphatic system

Rarely: leukopenia.

Very rarely: agranulocytosis, thrombocytopenia, anemia (hemolytic anemia, aplastic anemia). The risk of the appearance of agranulocytosis can not be predicted. Agranulocytosis may occur in patients who have been taking metamizol sodium in the past without the appearance of similar HP.

From the immune system

Rarely: anaphylactic shock, anaphylactic or anaphylactoid reactions, especially after parenteral use. Such reactions may occur during the administration of the drug or immediately after discontinuation of administration, but may occur within a few hours. They usually develop within the first hour after the injection. Easier reactions manifest themselves in the form of typical reactions from the skin and mucous membranes (for example, itching, burning, redness, urticaria, swelling - local or general), dyspnea and rarely complaints from the gastrointestinal tract. Light reactions can go into more severe forms with generalized urticaria, severe angioedema, including laryngospasm, severe bronchospasm, cardiac rhythm disturbance, lowering blood pressure (sometimes with a previous increase in blood pressure).

For this reason, if any skin reaction of hypersensitivity occurs, symptoms of renal dysfunction or hematotoxic reactions, the drug should be discontinued immediately.

Very rarely: an attack of bronchial asthma (in patients with "aspirin" asthma), circulatory shock.Shock can be accompanied by cold sweat, dizziness, drowsiness, oppression of consciousness, paleness of the skin, sensation of squeezing in the heart, superficial breathing or tachypnea, tachycardia, cold extremities, severe drop in blood pressure. At the first signs of shock, the drug should be discontinued and appropriate emergency measures taken.

From the skin and subcutaneous tissue

Infrequent: fixed drug exanthema.

Rarely: maculopapular and other types of rashes, Lyell syndrome or Stevens-Johnson syndrome, angioedema, sweating.

In the event of any skin reactions, the use of the drug should be immediately discontinued.

From the nervous system

Dizziness, headache.

From the sense organs (vision)

Visual disturbances, violation of accommodation.

From the heart

Infrequent: palpitation, tachycardia, cardiac rhythm disturbances, cyanosis.

From the side of the vessels

Infrequent: arterial hypotension, hyperemia.

Hypotensive reactions can rarely occur during or after application.They may or may not be accompanied by other symptoms of anaphylactoid or anaphylactic reactions.

Rarely such reactions can be the result of a sharp drop in blood pressure. Rapid administration increases the risk of hypotensive reactions.

A critical reduction in blood pressure without other signs of hypersensitivity is dose-dependent and may manifest as hyperpyrexia.

From the gastrointestinal tract

The frequency is unknown: dry mouth, nausea, vomiting, abdominal pain and discomfort, constipation, exacerbation of gastritis and gastric ulcer, rare vomiting with blood and intestinal bleeding, ulceration, burning sensation in the epigastric region.

From the liver and biliary tract

Hepatitis.

From the urinary system

Rarely: proteinuria, oliguria, anuria, polyuria, interstitial nephritis, urine staining in red, difficulty urinating, impaired renal function.

Frequency unknown: retention of urine.

From the respiratory system

Bronchospasm.

General disorders and disorders at the site of administration

When parenteral application - asthenia, pain at the injection site and local reactions.

Overdose:

Symptoms: nausea, vomiting, pain in the epigastric region, lowering blood pressure, tachycardia, acute agranulocytosis, hemorrhagic syndrome, hypothermia, oliguria, dyspnea, tinnitus, drowsiness, delirium, confusion, liver and kidney dysfunction, convulsions, respiratory muscle paralysis.

Treatment: symptomatic therapy.

Interaction:

The solution for intravenous and intramuscular administration is pharmaceutically incompatible with other drugs.

With blockers H₁-gistaminovyh receptors, derivatives of butyrophenone and phenothiazine, amantadine and quinidine

When used simultaneously with blockers H₁-gistaminovyh receptors, derivatives of butyrophenone and phenothiazine, amantadine and quinidine, the m-cholinoblocking effect of the drug may be enhanced.

With alcohol

Enhances the effects of ethanol.

With other non-narcotic analgesics Simultaneous use with other non-narcotic analgesics can lead to mutual enhancement of toxic effects.

FROM tricyclic antidepressants, oral contraceptives, allopurinol

Tricyclic antidepressants, oral contraceptives, allopurinol disrupt the metabolism of metamizole sodium in the liver and increase its toxicity.

With simultaneous use of the drug with tricyclic antidepressants, it is possible to enhance its m-cholinergic blocking action.

With barbiturates, phenylbutazone and other inducers of microsomal enzymes

Barbiturates, phenylbutazone and other inducers of microsomal liver enzymes weaken the action of metamizole sodium.

With sedatives and tranquilizers

Sedatives and anxiolytics (tranquilizers) increase the analgesic effect of the drug.

Simultaneous use with chlorpromazine or other phenothiazine derivatives can lead to the development of severe hyperthermia.

With radiopaque substances, colloid blood substitutes, penicillin

Radiocontrast agents, colloidal blood substitutes and penicillin should not be used during treatment with drugs containing metamizol sodium (increased risk of anaphylactic / anaphylactoid reactions).

FROM cyclosporin

Metamizole sodium can reduce the concentration of cyclosporine in the serum, so when using Spazmaton with cyclosporine, the concentrations of cyclosporin should be monitored.

With drugs that are highly associated with plasma proteins (oral hypoglycemic agents, indirect anticoagulants, glucocorticosteroids and indomethacin)

Metamizole sodium, displacing from the connection with plasma proteins, oral hypoglycemic drugs, indirect anticoagulants, glucocorticosteroids and indomethacin, increases their activity.

FROM myelotoxic drugs

Myelotoxic drugs increase the manifestation of hematotoxicity of the drug.

With methotrexate

Adding the drug to the treatment with methotrexate may increase the hematotoxic effect of the latter, especially in elderly patients. Therefore, this combination of drugs should be avoided.

With thiamazole and sarcolysin

Simultaneous use with thiamazole and sarcolysin increases the risk of developing leukopenia.

With codeine, H blockers₂-gistaminovyh receptors and propranolol

Codeine, blockers H₂-gistaminovyh receptors and propranolol enhance the effects of metamizole sodium.

Special instructions:

When treating children under 5 and patients receiving cytotoxic drugs, treatment with the drug should be carried out only under the supervision of a doctor.

When choosing the method of drug administration, it should be taken into account that parenteral use is associated with a higher risk of anaphylactic / anaphylactoid reactions. Parenteral application is recommended to use in cases when oral intake is impossible or impaired absorption from the gastrointestinal tract.

Increased risk of development of hypersensitivity reactions to the drug metamizol sodium stipulate the following states:

- bronchial asthma, especially in combination with polypous rhinosinusitis;

- chronic urticaria;

- alcohol intolerance (hypersensitivity to alcohol), against which even with the intake of a small amount of some alcoholic drinks, patients experience sneezing, lacrimation, and severe reddening of the face. Alcohol intolerance may indicate a previously unidentified syndrome of aspirin asthma;

- intolerance or hypersensitivity to dyes (for example, tartrazine) or preservatives (for example, benzoate).

Before using Spazmaton, a thorough questioning of the patient is necessary. If the risk of developing an anaphylactoid reaction is identified, Spazmaton's use is only possible after assessing the risk / benefit ratio.

In the case of Spazmaton, these patients need strict medical control over their condition and necessarily have the means to provide them with emergency care in case of anaphylactic / anaphylactoid reactions.

In predisposed patients, anaphylactic shock can occur, so patients with asthma or atopy Spasmaton should be administered with caution.

On the background of the use of metamizole sodium, life-threatening skin reactions such as Stevens-Johnson syndrome and toxic epidermal necrolysis have been described. When symptoms of these diseases appear (such as a progressive skin rash, often with blisters or mucosal lesions), Spasmaton should be discontinued immediately and should not be re-started.

During therapy with metamizol-containing drugs, the development of agranulocytosis is possible. It lasts at least a week, does not depend on the dose, can be heavy, endanger life and even lead to the death of the patient. In this regard, if symptoms appear to be associated with neutropenia (fever, chills, sore throat, difficulty swallowing, stomatitis, erosive ulceration of the oral cavity, vaginitis or proctitis, a decrease in the number of neutrophils in the peripheral blood is less than 1500 mm³), it is necessary to stop Spazmaton's treatment and consult a doctor.

If the patient receives antibiotic therapy, typical manifestations of agranulocytosis can be minimally expressed. The rate of erythrocyte sedimentation increases significantly, while the enlargement of the lymph nodes is weak or absent. Typical symptoms of thrombocytopenia are increased tendency to bleeding and the occurrence of petechia on the skin and mucous membranes.

In the case of pancytopenia, treatment should be stopped immediately, it is necessary to monitor the indicators of the developed blood test until normalization.

All patients should be aware that when symptoms of abnormal blood changes appear (for example, general malaise, infections, persistent fever, hematoma formation, bleeding, pallor of the skin), Spasmaton should be consulted immediately.

The administration of a metamizol-containing drug can induce individual hypotensive reactions. These reactions may depend on the dose of the drug and are more likely to occur after parenteral administration.

To avoid the development of severe hypotensive reactions, the following recommendations should be adhered to:

- iv Spasmodon should be administered slowly, in the "lying" position;

- should monitor blood pressure, heart rate and breathing;

- patients with existing hypotension, decreased circulating blood volume, dehydration, unstable hemodynamics, or with an initial stage of circulatory insufficiency, normalization of hemodynamics is required;

Care should be taken when treating patients with high body temperature.

Patients who should avoid reducing blood pressure (for example,with severe ischemic heart disease or stenosis of blood vessels that supply blood to the brain), Spasmaton should be administered only with close monitoring of hemodynamics.

During the treatment with the drug should refrain from drinking alcohol. It is inadmissible to use the drug to stop acute pain in the abdomen (until finding out their cause).

In patients with impaired liver or kidney function, it is recommended to avoid the use of Spasmactone in high doses due to a decrease in the rate of excretion of the drug.

In / in the introduction of Spasmaton should be carried out very slowly (not more than 1 ml / min), so that at the first signs of anaphylactic / anaphylactoid reactions, the injection could be stopped and the risk of individual hypotensive reactions minimized.

With the / m introduction, you need to use a needle for intramuscular injection.

Against the background of the use of the drug, it is possible to stain the urine red because of the presence of the metabolite - rubanzonic acid (it has no clinical significance).

Effect on the ability to drive transp. cf. and fur:

The active substance fenpiverinia bromide has holinoliticheskoe action and can cause dizziness and violation of accommodation.Patients who drive vehicles or work with machines should be warned about possible side effects of the drug. Activities that require increased attention should be discontinued until the side effects disappear.

Form release / dosage:

Solution for intravenous and intramuscular injection.

Packaging:

5 ml per ampoule of glass.

For 10 ampoules, together with a knife or scarifier for opening ampoules and instructions for medical use, are placed in a box made of cardboard with a corrugated corrugated paper liner.

5 ampoules are placed in a blister pack. 1 or 2 blister packs with ampoules together with a knife or scarifier for opening ampoules and instructions for medical use are placed in a pack of cardboard.

For 5 or 10 ampoules, together with a knife or scarifier for opening ampoules and instructions for medical use, put in a pack with a cardboard insert to fix the ampoules.

In case of using ampoules with a break ring or a notch and a break point, the insertion of the knife for opening ampoules is not provided.

Storage conditions:

In the dark place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

2 years.

Do not use after expiry date.

Terms of leave from pharmacies:On prescription

Registration number:LP-003740

Date of registration:19.07.2016

Expiration Date:19.07.2021

The owner of the registration certificate:BORISOVSKIY FACTORY OF MEDPREPARATES, OJSC BORISOVSKIY FACTORY OF MEDPREPARATES, OJSC Republic of Belarus

Manufacturer: & nbsp

BORISOVSKIY FACTORY OF MEDPREPARATES, OJSC Republic of Belarus

Representation: & nbspBORISOVSKIY FACTORY OF MEDPREPARATES, OJSCBORISOVSKIY FACTORY OF MEDPREPARATES, OJSC

Information update date: & nbsp01.09.2016

Illustrated instructions

Instructions

Spasmaton (Spasmaton)