Spasmopharm - instructions for use, doses, side effects, contraindications

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Dosage form: & nbspRAsterol for intramuscular injection.

Composition:Hand 1 ml of the preparation:

active substances: metamizole sodium - 500 mg, pituopenona hydrochloride - 2.0 mg, fenpiverinia bromide - 0.02 mg;

Excipients: water for injection - up to 1 ml.

Description:

Transparent, from a light yellow to a greenish-yellow solution.

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

ATX: & nbsp

Pitophenone in combination with analgesics

Pharmacodynamics:

SPASMOFARM is a combined medicinal product with a pronounced antispasmodic and analgesic effect.

Metamizol sodium has a pronounced analgesic and antipyretic effect in combination with less pronounced anti-inflammatory and spasmolytic activity. Its effect is due to the inhibition of the synthesis of prostaglandins and endogenous algogens, an increase in the threshold of excitability in the thalamus, influence on the hypothalamus, and the formation of endogenous pyrogens.

Fentipierinium bromide has a mild anticholinergic action, reduces the tone and motility of the smooth muscles of the stomach, intestines, bile and urinary tract.

Pitophenone has a papaverin-like effect on the smooth muscles of blood vessels and internal organs with a pronounced antispasmodic effect.

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 blood-brain barrier.

Metabolism. Metamizol sodium is subjected to intensive biotransformation in the liver. Its main metabolite, 4-methyl-amino-antipyrine (MAA), is metabolized in the liver to form other metabolites, including pharmacologically active 4-amino-antipyrine (AA). The maximum plasma concentrations (of all metabolites) are reached after approximately 30-90 minutes.

The four main metabolites of metamizole sodium:

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 degree 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 any component of the drug;

- hypersensitivity to pyrazolone derivatives (including patients who undergone agranulocytosis due to the use of these drugs) or other NSAIDs;

- severe renal and hepatic insufficiency;

- acute hepatic porphyria;

- deficiency of glucose-6-phosphate dehydrogenase;

- intestinal obstruction and megacolon;

- disorders of bone marrow hematopoiesis (for example, due to treatment with cytostatics) and diseases of the hematopoietic system (agranulocytosis, leukopenia, aplastic anemia);

- hyperplasia of the prostate of II - III degree;

- atony of the gallbladder and bladder;

- Arterial hypotension and hemodynamic instability;

- pregnancy and breastfeeding;

- children's age till 15 years.

Pregnancy and lactation:

Pregnancy

The results of the study on animals indicate that the drug does not have embryotoxic and teratogenic potential. Strictly controlled studies in pregnant women have not been carried out to date. Although metamizol sodium is a weak inhibitor of the synthesis of prostaglandins, it is impossible to exclude the possibility of premature closure of the arterial (Botallova) duct, as well as perinatal complications due to a decrease in aggregation of platelets of the fetus and matherthe use of the drug in pregnancy is contraindicated.

Breast-feeding

Since metabolites of metamizole sodium are excreted in breast milk, if necessary, use of the drug should stop breastfeeding.

Dosing and Administration:

Enter strictly intramuscularly!

The drug is intended for short-term use!

Management should be carried out under the strict supervision of a physician, with the capacity to provide emergency care in connection with the risk of anaphylactic shock in patients with hypersensitivity to metamizole sodium or a derivative of pyrazolone.

Adults and children over 15 years of age (> 53 kg)

Adults and children over 15 years of age, the drug is administered intramuscularly in a volume of 2-5 ml. If necessary, repeat the dose after 6-8 hours. The maximum daily dose should not exceed 6 ml of the drug (equivalent to 3 g of metamizole sodium).

Duration of treatment is 2-3 days.

After achieving a therapeutic effect, it is allowed to switch to oral analgesia and antispasmodics.

In the absence of a therapeutic effect, treatment is discontinued.

Patients over the age of 65 years

Dose reduction is usually not required.In patients with age-related disorders of the liver and kidneys, it is necessary to reduce the dose, since it is possible to increase the half-life of metabolites of metamizole sodium (see section "Pharmacokinetics").

Patients with impaired renal function

Metamizole sodium is excreted in the urine in the form of metabolites. In patients with mild to moderate renal failure, half the dose for adults is recommended.

Patients with hepatic impairment

In such patients, the half-life of active metabolites of metamizole sodium increases. In patients with impaired liver function, high doses should be avoided. In case of short-term use, it is not necessary to reduce the dose.

There is insufficient experience of prolonged use in patients with impaired renal or hepatic function.

Children

The drug is contraindicated in children under the age of 15 (see section "Contraindications").

Side effects:

Undesirable reactions are grouped according to systems and organs, as well as the frequency of their occurrence:

Frequency grading: very often (≥ 1/10), often (≥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.

Hematologic and lymphatic disorders

Rarely: leukopenia.

Very rarely: agranulocytosis, thrombocytopenia, anemia (hemolytic anemia, aplastic anemia).

The risk of agranulocytosis can not be foreseen. Agranulocytosis can occur in patients who have previously taken metamizol sodium without the occurrence of such undesirable reactions.

Immune disorders:

Infrequent: limited exanthema.

Rarely: maculopapular rash, anaphylactic or anaphylactoid reactions, especially after parenteral administration.

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. Lighter 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 less frequent 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).

In this regard, if any skin reaction occurs, the drug should be discontinued immediately.

Very rarely: an attack of bronchial asthma (in patients with "aspirin" asthma), Stevens-Johnson syndrome, Lyell syndrome, circulatory shock.

Neurological disorders: dizziness, headache.

Disorders from the side of the organ of vision: visual disturbances, violation of accommodation.

Heart Disease:

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

Vascular disorders:

Infrequent: arterial hypotension.

Gastrointestinal disorders:

The frequency is unknown: dry mouth, nausea, vomiting, abdominal pain and discomfort, constipation, exacerbation of gastritis and gastric ulcer, in rare cases, ulceration and vomiting with an admixture of blood.

Disorders from the kidneys and urinary tract:

Rarely: proteinuria, oliguria, anuria, polyuria, interstitial nephritis, urine staining in red.

Frequency unknown: retention of urine.

General disorders and disorders at the site of administration: with parenteral application - pain at the injection site and local reactions.

Overdose:

Symptoms: symptoms of "metamizol" intoxication in combination with m-cholinoblocking manifestations predominate. Most often there is a toxic-allergic syndrome, hematotoxicity, gastrointestinal disturbances, cerebral manifestations.

Treatment: stop the use of the drug and take measures for its rapid removal from the body (forced diuresis, infusion of water-salt solutions, if necessary, hemodialysis). Apply symptomatic. There is no specific antidote.

Interaction:

Combination of the drug SPASMOFARM with other drugs requires special care because of the content of metamizole sodium, which is an inducer of microsomal liver enzymes.

Indirect anticoagulants

With simultaneous application metamizol sodium can reduce the activity of coumarin anticoagulants as a result of induction of microsomal liver enzymes.

Chlorpromazine and other phenothiazine derivatives

With simultaneous use with metamizole sodium there is a risk of severe hypothermia.

Cyclosporin A

Metamizole sodium reduces the plasma concentration of cyclosporin A when used simultaneously.

Chloramphenicol and other myelotoxic agents

With simultaneous use with metamizole sodium there is an increased risk of myelosuppression.

Inductors of enzymes

Barbiturates, glutethimide, phenylbutazone can weaken the action of metamizole sodium.

The drugs that oppress the central nervous system

The drugs that depress the central nervous system can enhance the analgesic effect of sodium metamizole.

Tricyclic antidepressants (imipramine, amitriptyline), oral contraceptives, analgesics, allopurinol

Strengthening the effect with simultaneous use with metamizol sodium.

Simultaneous application from other analgesics and NSAIDs increases the risk of hypersensitivity and other undesirable reactions.

The derivatives of pyrazolone are able to interact with Captopril, lithium, methotrexate and triamterene, and also change the efficiency antihypertensive drugs, diuretics. The magnitude of such interactions is unknown.

Special instructions:

When treating with the drug SPASMOFARM there is a risk of developing anaphylactic reactions. At the first sign of hypersensitivity, the drug should be discontinued and urgent therapeutic measures taken (epinephrine, glucocorticosteroids, antihistamines).

The risk of anaphylactoid reactions when using metamizole sodium is significantly increased in patients with:

- syndrome of analgesic asthma or idiosyncrasy to analgesics in the form of urticaria of the angioedurotic type;

- bronchial asthma, especially accompanied by rhinosinusitis and polyposis of the nasal mucosa;

- chronic urticaria;

- idiosyncrasy to colorants (for example, tartrazine) and, accordingly, preservatives (for example, benzoate);

- intolerance to alcohol. Such patients respond to the use of a minimum amount of alcoholic beverages with symptoms such as sneezing, lacrimation, and severe visual impairment. Such alcohol intolerance can be a sign of an undiagnosed syndrome of "aspirin" asthma.

SPASMOFARM contains metamizol sodium, in the treatment of which there is a small but life-threatening risk of developing shock and agranulocytosis. The development of agranulocytosis is not dose dependent and can not be predicted. It may appear after the first dose or after repeated use. Typical signs of agranulocytosis are fever, sore throat, soreness in swallowing, inflammation of the mucous membrane of the mouth, nose, pharynx, anorectal genital area. With a sudden deterioration in the general condition and the appearance of signs of agranulocytosis, the drug should be stopped immediately, without waiting for laboratory confirmation.

When treating patients with hematologic diseases with a drug SPASMOFARM, or having them in the anamnesis, it is necessary to control the hematologic status during treatment.

The drug should be used with caution in patients with obstructive diseases of the gastrointestinal tract (achalasia cardia, pyloroduodenal stenosis). Multiple application of the drug SPASMOFARM in these cases can cause a delay in the evacuation of gastrointestinal contents and intoxication.Application of the drug SPASMOFARM in patients with gastroesophageal reflux disease, intestinal atony, paralytic intestinal obstruction, glaucoma, myasthenia gravis gravis, heart diseases (arrhythmias, ischemic heart disease, chronic heart failure) requires special care and control of the doctor.

Metamizole sodium, which is part of the drug SPASMOFARM, can cause hypotensive reactions (see section "Side effect"). These reactions depend on the dose and are more often observed with parenteral application.

The risk of such reactions increases in the following cases:

- in patients with a history of arterial hypotension, a decrease in fluid volume and electrolyte content, or dehydration, unstable hemodynamics, or circulatory insufficiency (eg, in patients with myocardial infarction or polytrauma);

- in patients with increased body temperature.

Such patients should carefully assess the need for the drug and establish strict control after them, therapeutic measures (for example, stabilizing the blood circulation) may be required to reduce the risk of hypotension.SPASMOPHARM should be used only when carefully monitoring hemodynamics in patients who do not show mandatory forced reduction in blood pressure, for example, in severe coronary heart disease or stenosis of cerebral vessels.

SPASMOPHARM should only be used after a thorough assessment of the relationship of benefit and risk, taking appropriate precautions in patients with impaired renal or hepatic function (see section "Method of administration and dose").

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

Fentivirinium bromide has m-holinoblokiruyuschee effect and can cause dizziness and violation of accommodation. Metamizol sodium can negatively affect the ability to concentrate and reduces the speed of reaction.

Patients driving vehicles or working with mechanisms should be warned about possible unwanted reactions to the drug. Activities that require increased attention should be discontinued until the disappearance of unwanted reactions.

Form release / dosage:Solution for intramuscular injection, 500 mg / ml + 2 mg / ml + 0.02 mg / ml.

Packaging:

For 2 or 5 ml of the drug in a vial of dark glass type I; 10 ampoules per blister; 1 blister together with instructions for use are placed in a cardboard box.

Storage conditions:

Store at a temperature not exceeding 25 ° C.

Keep out of the reach of children.

Shelf life:

5 years.

Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LP-003618

Date of registration:12.05.2016

Expiration Date:12.05.2021

The owner of the registration certificate:VetProm ADVetProm AD Bulgaria

Manufacturer: & nbsp

VETPROM, AD Bulgaria

Representation: & nbspVETPROM ADVETPROM ADBulgaria

Information update date: & nbsp10.07.2016

Illustrated instructions

Instructions

Spasmopharm (Spasmopharm)