Trinalgin 5ml 10 pcs. solution for intravenous and intramuscular administration

pharmachologic effect

Combined analgesic and antispasmodic agent.
The combination of the components of the drug leads to a mutual enhancement of their pharmacological action. Metamizole sodium, a pyrazolone derivative, has an analgesic, antipyretic and weak anti-inflammatory effect, the mechanism of which is associated with inhibition of prostaglandin synthesis.

Pitophenone hydrochloride has a direct myotropic effect on the smooth muscles of internal organs and causes its relaxation (papaverine-like effect).

Phenpiverinium bromide has an m-anticholinergic effect and has an additional myotropic effect on smooth muscles.

Composition and release form Trinalgin 5ml 10 pcs. solution for intravenous and intramuscular administration

Solution - 1 ml:

Active ingredients: metamizole sodium 500 mg, pitofenone hydrochloride 2 mg, fenpiverinium bromide 0.02 mg.
Excipients: sodium disulfite - 1 mg, sodium hydroxide solution 2M - sufficient to bring the pH to 6.0-7.5, water for injection - up to 1 ml.

5 ml - light-protective glass ampoules (10) - cardboard boxes.

5 ml - light-protective glass ampoules (5) - contour cell packaging made of polyvinyl chloride film (2) - cardboard packs.

Description of the dosage form

Solution for intravenous and intramuscular administration; white, round, flat, with cut edges and a dividing groove.

Directions for use and doses

Inside

Adults and adolescents over 15 years old: 1-2 tablets. 2-3 times a day, without chewing, with a small amount of liquid.

Children aged 12-14 years: single dose - 1 tablet, maximum daily dose - 6 tablets. (1.5 tablets 4 times/day), children aged 8-11 years - 0.5 tablets, maximum daily dose - 4 tablets. (1 tablet 4 times/day), children aged 5-7 years - 0.5 tablet, maximum daily dose - 2 tablets. (0.5 tablet 4 times/day).

Parenteral (i.v., i.m.)

For adults and adolescents over 15 years of age with acute severe colic, 2 ml are administered intravenously slowly (1 ml over 1 minute); if necessary, re-inject after 6-8 hours. IM - 2-5 ml of solution 2-3 times a day. The maximum daily dose should not exceed 10 ml (corresponding to 5 g of metamizole sodium).

The duration of treatment is determined depending on the clinical symptoms and etiopathogenesis of the disease, but should not exceed 5 days.

Dose calculation for children with IV and IM administration: 3-11 months (5-8 kg) - IM only - 0.1-0.2 ml; 1-2 years (9-15 kg) - IV - 0.1-0.2 ml, IM - 0.2-0.3 ml; 3-4 years (16-23 kg) - IV - 0.2-0.3, IM - 0.3-0.4 ml; 5-7 years (24-30 kg) - IV - 0.3-0.4 ml, IM - 0.4-0.5 ml; 8-12 years (31-45 kg) - IV - 0.5-0.6 ml, IM - 0.6-0.7 ml; 12-15 years - IV and IM - 0.8-1 ml.

Before administering the injection solution, it should be warmed in your hand.

Pharmacokinetics

Metamizole sodium

After oral administration, metamizole sodium is rapidly absorbed from the gastrointestinal tract. In the intestinal wall it is hydrolyzed to form an active metabolite. Unchanged metamizole sodium is not detectable in the blood (only after intravenous administration it is found in the blood plasma in a small concentration and quickly becomes inaccessible for determination). After intramuscular administration, the active substances of the drug are quickly and largely absorbed from the injection site.

Binding to blood plasma proteins is 50-60%. When taken in therapeutic doses, it is excreted in breast milk.

Metamizole sodium undergoes intensive biotransformation in the liver. The main metabolites are 4-methylaminoantipyrine, 4-formylaminoantipyrine, 4-aminoantipyrine and 4-acetylaminoantipyrine. About 20 additional metabolites have been identified, including glucuronic acid derivatives. The main four metabolites are found in the cerebrospinal fluid. It is excreted mainly by the kidneys.

Pitophenone

Rapidly absorbed from the gastrointestinal tract when taken orally. Cmax in blood plasma is reached after 30-60 minutes. It is quickly distributed in organs and tissues and does not penetrate the BBB.

Metabolized in the liver by oxidative reactions. Excreted in urine. T1/2 is 1.8 hours.

Phenpiverinium bromide

When taken orally, it is quickly absorbed from the gastrointestinal tract. Cmax in blood plasma is achieved within 1 hour. Does not penetrate the BBB. Excreted unchanged in urine 32.4-40.4%, in bile - 2.3-5.3%.

Indications for use Trinalgin 5ml 10 pcs. solution for intravenous and intramuscular administration

Pain syndrome (mild or moderate) with spasms of smooth muscles of internal organs: renal colic, spasm of the ureter and bladder; biliary colic; biliary dyskinesia; postcholecystectomy syndrome; intestinal colic; chronic colitis; algodismenorrhea; diseases of the pelvic organs.

For short-term treatment of arthralgia; myalgia; neuralgia, sciatica.

As an auxiliary drug for pain after surgical interventions and diagnostic procedures.

Contraindications

Severe liver and/or renal failure; inhibition of bone marrow hematopoiesis; deficiency of glucose-6-phosphate dehydrogenase; tachyarrhythmia; severe angina; decompensated chronic heart failure; collapse; angle-closure glaucoma; prostatic hyperplasia (with clinical manifestations); intestinal obstruction; megacolon; pregnancy (especially the first trimester and the last 6 weeks); lactation period; children under 3 months of age or body weight less than 5 kg (for intravenous administration); children under 5 years of age (for tablets); hypersensitivity (including to pyrazolone derivatives).

With ;caution: ;renal/liver failure; bronchial asthma; tendency to arterial hypotension; hypersensitivity to NSAIDs; urticaria or acute rhinitis caused by taking acetylsalicylic acid or other NSAIDs.

Application Trinalgin 5ml 10 pcs. solution for intravenous and intramuscular administration during pregnancy and lactation

The use of the drug is contraindicated during pregnancy (especially in the first trimester and in the last 6 weeks).

If it is necessary to use the drug during lactation, breastfeeding should be discontinued.

Use in children

IV administration of the drug is contraindicated in children under 3 months of age or with a body weight of less than 5 kg.

The use of the drug in tablet form is contraindicated in children under 5 years of age.

special instructions

With long-term (more than a week) treatment, monitoring of the peripheral blood picture and the functional state of the liver is necessary.

If agranulocytosis is suspected or thrombocytopenia is present, the drug should be discontinued.

The use of the drug to relieve acute abdominal pain is unacceptable until the cause of the disease is determined.

Intolerance is very rare, but the risk of developing anaphylactic shock after intravenous administration of the drug is relatively higher than after taking the drug orally.

In patients with atopic bronchial asthma and hay fever, the risk of developing allergic reactions increases.

Parenteral administration of the drug should be used only in cases where oral administration is impossible or absorption from the gastrointestinal tract is impaired.

The IV injection should be carried out slowly, with the patient lying down and under the control of blood pressure, heart rate and respiratory rate.

Particular care must be taken when administering more than 2 ml of solution (there is a risk of a sharp decrease in blood pressure).

For intramuscular administration it is necessary to use a long needle.

When treating children under 5 years of age and patients receiving cytostatics, the use of metamizole sodium should only be carried out under medical supervision.

It is possible that the urine may turn red due to the release of a metabolite (it has no clinical significance).

During treatment with the drug, it is not recommended to take ethanol.

Impact on the ability to drive vehicles and operate machinery

During treatment, drivers of vehicles and persons engaged in potentially hazardous activities that require rapid psychomotor reactions should be careful.

Overdose

Symptoms: nausea, vomiting, gastralgia, hypothermia, decreased blood pressure, tachycardia, shortness of breath, tinnitus, drowsiness, delirium, disturbances of consciousness, acute agranulocytosis, hemorrhagic syndrome, oliguria, acute renal and/or liver failure, convulsions, respiratory muscle paralysis .

Treatment: gastric lavage, use of activated carbon, water-salt solutions, forced diuresis, hemodialysis; with the development of convulsive syndrome - intravenous administration of diazepam and fast-acting barbiturates.

Side effects Trinalgin 5ml 10 pcs. solution for intravenous and intramuscular administration

Allergic reactions: urticaria (including on the conjunctiva and mucous membranes of the nasopharynx), angioedema, in rare cases - malignant exudative erythema (Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell's syndrome), bronchospasm, anaphylactic shock.

From the hematopoietic system: thrombocytopenia, leukopenia, agranulocytosis (may be manifested by the following symptoms: unmotivated rise in temperature, chills, sore throat, difficulty swallowing, stomatitis, as well as the development of vaginitis or proctitis).

From the cardiovascular system: ;decrease in blood pressure.

From the urinary system: impaired renal function, oliguria, anuria, proteinuria, interstitial nephritis, red staining of urine.

Anticholinergic effects: dry mouth, decreased sweating, accommodation paresis, tachycardia, difficulty urinating.

Local reactions: with intramuscular injection, infiltrates are possible at the injection site.

Drug interactions

Histamine H1 receptor blockers, butyrophenones, phenothiazines, tricyclic antidepressants, amantadine and quinidine; - may enhance the m-anticholinergic effect.

Chlorpromazine or other phenothiazine derivatives; - severe hyperthermia may develop.

Non-narcotic analgesics, tricyclic antidepressants, oral hormonal contraceptives and allopurinol increase the toxicity of the drug.

Phenylbutazone, barbiturates and other inducers of microsomal enzymes - reduce the effectiveness of metamizole sodium.

Sedatives and anxiolytics (tranquilizers); - enhancing the analgesic effect of metamizole sodium.

Radiocontrast drugs, colloidal blood substitutes and penicillin; - combinations with drugs containing metamizole sodium should not be used.

Cyclosporine; - the concentration of cyclosporine in the blood may decrease.

Oral hypoglycemic agents, indirect anticoagulants, corticosteroids and indomethacin; - metamizole sodium displaces these agents from binding with proteins, as a result of which the severity of their action may increase.

Thiamazole and cytostatics; - increased risk of developing leukopenia.

Medicines with myelotoxic effects: increased hematotoxic effect of the drug.

Codeine, histamine H2 receptor blockers, propranolol; - increased effect of the drug due to slower inactivation of metamizole sodium.

Ethanol; - enhanced effects of ethanol.

The solution for injection is pharmaceutically incompatible with other drugs.

Trinalgin solution for intravenous and intramuscular injection 5 ml amp/pack cards x5

ATX code: N02BB52 (Metamizole sodium in combination with other drugs (excluding psycholeptics)) Active substances metamizole sodium Rec.INN WHO registered pitofenone Rec.INN WHO registered fenpiverinium bromide Rec.INN WHO registered Dosage form TRINALGIN solution for intravenous and intramuscular administration 500 mg + 2 mg + 0.02 mg: 2 ml or 5 ml amp. 5 or 10 pcs. reg. No.: LP-001826 dated 09/10/12 - Valid Release form, composition and packaging Solution for intravenous and intramuscular administration, white, round, flat, with cut edges and a dividing groove.

1 ml metamizole sodium 500 mg pitofenone hydrochloride 2 mg fenpiverinium bromide 0.02 mg

Excipients: sodium disulfite 1 mg, sodium hydroxide solution 2 M sufficient to bring the pH to 6.0-7.5, water for up to 1 ml.

2 ml - light-protective glass ampoules (10) - cardboard boxes. 2 ml - light-protective glass ampoules (5) - contour cell packaging made of polyvinyl chloride film (1) - cardboard packs. 2 ml - light-protective glass ampoules (5) - contour cell packaging made of polyvinyl chloride film (2) - cardboard packs. 5 ml - light-protective glass ampoules (5) - contour cell packaging made of polyvinyl chloride film (1) - cardboard packs. 5 ml - light-protective glass ampoules (5) - contour cell packaging made of polyvinyl chloride film (2) - cardboard packs.

Clinical-pharmacological group: Spasmoanalgesic Pharmaco-therapeutic group: Analgesic non-narcotic drug (non-narcotic analgesic + antispasmodic) Pharmacological action Combined analgesic and antispasmodic drug, the combination of drug components leads to a mutual enhancement of their pharmacological action.

Metamizole sodium is a pyrazolone derivative that has an analgesic and antipyretic effect.

Pitophenone hydrochloride has a direct myotropic effect on smooth muscles (papaverine-like effect).

Phenpiverinium bromide has an m-anticholinergic effect and has an additional myotropic effect on smooth muscles. Indications Pain syndrome (mild or moderately severe) with spasms of smooth muscles of internal organs: renal colic, spasm of the ureter and bladder, biliary colic, intestinal colic, biliary dyskinesia, postcholecystectomy syndrome, chronic colitis, algodismenorrhea, diseases of the pelvic organs.

For short-term treatment: arthralgia, myalgia, neuralgia, sciatica.

As an auxiliary drug: pain syndrome after surgical interventions and diagnostic procedures. ICD-10 codes ICD-10 code Indication K80 Gallstone disease [cholelithiasis] (including hepatic colic) K82.8 Other specified diseases of the gallbladder and cystic duct (including dyskinesia) K91.5 Postcholecystectomy syndrome M25. 5 Joint pain M54.3 Sciatica M54.4 Lumbago with sciatica M79.1 Myalgia M79.2 Neuralgia and neuritis, unspecified N23 Renal colic, unspecified N94.4 Primary dysmenorrhea N94.5 Secondary dysmenorrhea R10.4 Other and unspecified pain in the abdominal area ( colic) R51 Headache R52.0 Acute pain R52.2 Other persistent pain (chronic)

Dosage regimen: Orally: adults and adolescents over 15 years of age: 1-2 tablets. 2-3 times a day, without chewing, with a small amount of liquid.

Children 12-14 years old: single dose - 1 tablet, maximum daily dose - 6 tablets. (1.5 tablets 4 times/day), 8-11 years old - 0.5 tablets, maximum daily dose - 4 tablets. (1 tablet 4 times/day), 5-7 years - 0.5 tablets, maximum daily dose - 2 tablets. (0.5 tablet 4 times/day).

Parenterally (i.v., i.m.).

For adults and adolescents over 15 years of age with acute severe colic, 2 ml are administered intravenously slowly (1 ml over 1 minute), if necessary, re-injected after 6-8 hours. IM - 2-5 ml of solution 2-3 times/day The daily dose should not exceed 10 ml. The duration of treatment is no more than 5 days.

Dose calculation for children with IV and IM administration: 3-11 months (5-8 kg) - only IM - 0.1-0.2 ml, 1-2 years (9-15 kg) - IV - 0.1-0.2 ml, IM - 0.2-0.3 ml, 3-4 years (16-23 kg) - IV - 0.2-0.3, IM - 0.3-0.4 ml, 5-7 years (24-30 kg) - IV - 0.3-0.4 ml, IM - 0.4-0.5 ml, 8-12 years (31-45 kg) - IV - 0.5-0.6 ml, IM - 0.6-0.7 ml, 12-15 years - IV and IM - 0.8-1 ml.

Before administering the injection solution, it should be warmed in your hand. Side effects Allergic reactions: urticaria (including on the conjunctiva and mucous membranes of the nasopharynx), angioedema, in rare cases - malignant exudative erythema (Stevens-Johnson syndrome), toxic epidermal necrolysis (Lyell's syndrome), bronchospastic syndrome, anaphylactic shock .

From the urinary system: impaired renal function, oliguria, anuria, proteinuria, interstitial nephritis, red staining of urine.

From the cardiovascular system: decreased blood pressure.

Anticholinergic effects: dry mouth, decreased sweating, accommodation paresis, tachycardia, difficulty urinating.

Local reactions: with intramuscular injection, infiltrates are possible at the injection site. Contraindications for use Hypersensitivity (including to pyrazolone derivatives), inhibition of bone marrow hematopoiesis, severe hepatic and/or renal failure, glucose-6-phosphate dehydrogenase deficiency, tachyarrhythmias, severe angina pectoris, decompensated chronic heart failure, angle-closure glaucoma, prostatic hyperplasia (with clinical manifestations), intestinal obstruction, megacolon, collapse, pregnancy (especially in the first trimester and the last 6 weeks), lactation.

For intravenous administration - infancy (up to 3 months) or body weight less than 5 kg. For tablets - children's age (up to 5 years).

With caution: renal/liver failure, bronchial asthma, tendency to arterial hypotension, hypersensitivity to NSAIDs, urticaria or acute rhinitis caused by taking acetylsalicylic acid or other NSAIDs.

Use during pregnancy and breastfeeding Contraindicated during pregnancy (especially in the first trimester and the last 6 weeks).

Use in nursing mothers requires cessation of breastfeeding.

Use for liver dysfunction Contraindicated in severe liver failure. With caution: moderate or mild liver failure. Use for impaired renal function. Contraindicated in cases of severe renal failure. With caution: moderate or mild renal failure Use in children Contraindications for intravenous administration - infancy (up to 3 months) or body weight less than 5 kg, for tablets - children's age (up to 5 years).

Treatment of children under 5 years of age should only be carried out under medical supervision.

Special instructions During treatment with the drug, it is not recommended to take ethanol.

With long-term (more than a week) treatment, monitoring of the peripheral blood picture and the functional state of the liver is necessary.

If agranulocytosis is suspected or thrombocytopenia is present, the drug should be discontinued.

It is not permissible to use it to relieve acute abdominal pain (until the cause is determined).

Intolerance is very rare, but the risk of developing anaphylactic shock after intravenous administration of the drug is relatively higher than after taking the drug orally. Patients with atopic bronchial asthma and hay fever have an increased risk of developing allergic reactions.

Parenteral administration should be used only in cases where oral administration is not possible (or absorption from the gastrointestinal tract is impaired). Special caution is required when administering more than 2 ml of solution (risk of a sharp decrease in blood pressure). The IV injection should be carried out slowly, in the “lying” position and under the control of blood pressure, heart rate and respiratory rate.

When treating children under 5 years of age and patients receiving cytostatics, metamizole sodium should only be taken under medical supervision.

For intramuscular administration it is necessary to use a long needle.

It is possible that the urine may turn red due to the release of a metabolite (it has no clinical significance).

Impact on the ability to drive vehicles and operate machinery

During treatment, drivers of vehicles and persons engaged in potentially hazardous activities that require quick physical and mental reactions should be careful.

Overdose Symptoms: vomiting, decreased blood pressure, drowsiness, confusion, nausea, pain in the epigastric region, impaired liver and kidney function, convulsions.

Treatment: gastric lavage, administration of activated carbon, symptomatic therapy. Drug interactions The solution for injection is pharmaceutically incompatible with other drugs.

When combined with histamines and H1-blockers, butyrophenones, phenothiazines, tricyclic antidepressants, amantadine and quinidine, the m-anticholinergic effect may be enhanced.

Enhances the effects of ethanol; simultaneous use with chlorpromazine or other phenothiazine derivatives can lead to the development of severe hyperthermia.

Tricyclic antidepressants, oral contraceptives and allopurinol increase the toxicity of the drug.

Phenylbutazone, barbiturates and other liver enzyme inducers, when administered simultaneously, reduce the effectiveness of metamizole sodium.

Sedative and anxiolytic drugs (tranquilizers) enhance the analgesic effect of metamizole sodium.

Radiocontrast drugs, colloidal blood substitutes and penicillin should not be used during treatment with drugs containing metamizole sodium.

With simultaneous administration of cyclosporine, the concentration of the latter in the blood decreases.

Metamizole sodium, displacing oral hypoglycemic drugs, indirect anticoagulants, corticosteroids and indomethacin from protein binding, can increase the severity of their action.

Thiamazole and cytostatics increase the risk of developing leukopenia.

The effect is enhanced by codeine, H2-histamine receptor blockers and propranolol (slows down the inactivation of metamizole sodium).