Stagemin - Instructions For Use, Price, Analogues, Reviews

2024 Author: Rachel Wainwright | [email protected]. Last modified: 2023-12-15 07:39

Stagemin

Stagemin: instructions for use and reviews

1. 1. Release form and composition
2. 2. Pharmacological properties
3. 3. Indications for use
4. 4. Contraindications
5. 5. Method of application and dosage
6. 6. Side effects
7. 7. Overdose
8. 8. Special instructions
9. 9. Application during pregnancy and lactation
10. 10. Use in childhood
11. 11. In case of impaired renal function
12. 12. Drug interactions
13. 13. Analogs
14. 14. Terms and conditions of storage
15. 15. Terms of dispensing from pharmacies
16. 16. Reviews
17. 17. Price in pharmacies

Latin name: Stagemin

ATX code: B02AA02

Active ingredient: tranexamic acid (Tranexamic acid)

Producer: JSC "Novosibkhimfarm" (Russia)

Description and photo update: 2019-08-07

Prices in pharmacies: from 328 rubles.

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Stagemin is a drug used to treat and prevent bleeding.

Release form and composition

Dosage form - solution for intravenous administration: clear liquid, colorless or with a light brown tint (in 5 ml ampoules: 10 ampoules in a cardboard box; in blisters of 5 ampoules, in a cardboard box 1, 2 or 10 packages; in blister packs of 10 ampoules, in a cardboard box 1, 2 or 5 packs; each pack also contains instructions for the use of Stagemin).

Composition: 1 ml solution:

• active substance: tranexamic acid - 50 mg;
• additional component: water for injection - up to 1 ml.

Pharmacological properties

Pharmacodynamics

Tranexamic acid - the active component of Stagemin, is an antifibrinolytic substance, a competitive inhibitor (when used in high concentrations - non-competitive) of plasminogen activation and its transformation into plasmin.

It has a local and systemic hemostatic effect in bleeding associated with an increase in fibrinolysis (for example, in patients with menorrhagia or platelet abnormalities). Against the background of the use of Stagemin, the formation of kinins and other active peptides is suppressed, which take part in the reactions of inflammatory and allergic etiology.

It has anti-inflammatory, anti-allergic, anti-tumor and anti-infective properties. During experimental studies, the presence of its own analgesic activity of tranexamic acid, as well as the potentiating effect of the substance in relation to the analgesic activity of opioid analgesics, was confirmed.

Tranexamic acid, used at a concentration of 1 mg / ml, does not aggregate platelets; if used at a concentration of up to 10 mg / ml of blood, the substance does not affect the number of platelets, blood clotting time or various clotting factors in whole or citrated blood in a healthy person. In this case, the drug at a concentration of 1 and 10 mg / ml of blood causes an increase in thrombin time.

Pharmacokinetics

Tranexamic acid is characterized by a relatively uniform distribution in tissues, with the exception of cerebrospinal fluid, where the concentration is 0.1 of the plasma concentration.

The substance penetrates the blood-brain and placental barrier (after administration of 10 mg / kg tranexamic acid to a woman, the concentration in the umbilical cord blood can be quite high, approximately 0.03 mg / ml of fetal serum). It is excreted in breast milk (reaches approximately 1% of the plasma concentration in the mother). It is found in semen, where it leads to a decrease in fibrinolytic activity, while therapy does not affect sperm migration.

Tranexamic acid rapidly diffuses through the synovial membranes and into the joint fluid. In the joint fluid, the substance is detected in the same concentration as in the blood serum. The biological T _1/2 (half-life) from the articular fluid is approximately 180 minutes. The initial V _d (volume of distribution) ranges from 9 to 12 liters. Tranexamic acid binds to plasma proteins (profibrinolysin) at a level of less than 3%.

In the blood, about 3% of the substance is bound to a protein (plasminogen). The values of the total renal and plasma clearance are equal and amount to 7 l / h.

The time of maintaining the concentration of tranexamic acid, which has antifibrinolytic activity: in plasma - up to 7-8 hours, in various tissues - 17 hours.

The substance is metabolized slightly. AUC (area under the concentration-time curve) has a three-phase form, in the terminal phase T _1/2 - 2 hours. Excretion is carried out by the kidneys (the main route of excretion is glomerular filtration), more than 95% of the dose is excreted unchanged in the first 12 hours after administration. After the application of 10 mg / kg tranexamic acid for 24 hours, approximately 90% of the dose is excreted by glomerular filtration.

As a result of biotransformation of tranexamic acid, two metabolites are formed: deaminated and N-acetylated derivatives.

In patients with impaired renal function, there is a risk of accumulation of the substance.

Indications for use

Stagemin is prescribed for the treatment and prevention of bleeding, which are caused by local or generalized fibrinolysis in adults and children from 1 year old.

The use of Stagemin is indicated in the following cases:

• metrorrhagia, menorrhagia and other bleeding caused by generalized / local fibrinolysis; bleeding after surgery on the bladder and prostate gland; gastrointestinal bleeding (therapy);
• bleeding during surgical interventions in the oral cavity, pharynx and nose (tonsillectomy, adenoidectomy, tooth extraction); abdominal, thoracic and other major surgical interventions (including cardiac surgery); gynecological surgical interventions (therapy and prevention);
• bleeding associated with the use of fibrinolytic drugs (therapy);
• obstetric and gynecological bleeding (therapy).

Contraindications

Absolute:

• the risk of development and an indication in the history of thrombosis in case of impossibility of the simultaneous use of anticoagulants;
• active thromboembolic diseases, including deep vein thrombosis, cerebral thrombosis, pulmonary embolism;
• acquired color vision impairment;
• subarachnoid hemorrhage (associated with the risk of heart attack and cerebral edema);
• hematuria associated with diseases of the renal parenchyma, bleeding from the upper urinary tract (associated with the risk of secondary mechanical obstruction of the urinary tract by a blood clot with the occurrence of anuria);
• combined use with drugs of blood coagulation factors II, VII, IX and X in combination (prothrombin complex) or with an anti-inhibitory coagulant complex;
• severe chronic renal failure in patients with a glomerular filtration rate less than 30 mg / ml / 1.73 m ² (associated with the risk of cumulation);
• fibrinolysis associated with consumption coagulopathy [hypocoagulant stage of DIC syndrome (disseminated intravascular coagulation syndrome)];
• a history of convulsions;
• age up to 1 year; for the treatment of menorrhagia - up to 16 years;
• the presence of hypersensitivity to the components of the drug.

Relative (Stagemin is prescribed under medical supervision):

• high risk of thrombosis: a history of thromboembolic events or a family history of thromboembolism;
• combined use with combined oral contraceptives (due to an increased risk of venous thromboembolic complications and arterial thrombosis);
• combined therapy with anticoagulants (experience of use is limited).

Stagemin, instructions for use: method and dosage

Stagemin is administered intravenously (jet, drip). For infusion administration, the drug must be diluted in 0.9% sodium chloride solution.

Recommended dosage regimen:

• generalized fibrinolysis: every 6-8 hours, 15 mg / kg at a rate of 1 ml / min;
• use in cardiac surgery, during operations in extracorporeal circulation: 15 mg / kg Stagemin is administered during the induction of anesthesia prior to sternotomy, then intraoperatively at the rate of 4.5 mg / kg, of which 0.6 mg / kg is injected into the primary filling volume of the AIC (heart-lung machine);
• local fibrinolysis: 2–3 times a day, 250–500 mg;
• prostatectomy or bladder surgery: during surgery, a dose of 1000 mg, then the same dose is administered every 8 hours for 3 days; in the future, until the disappearance of macrohematuria, taking the drug in tablet form is indicated
• obstetric and gynecological bleeding: every 6-8 hours, 15 mg / kg; Stagemin is used from the moment bleeding appears until it stops;
• bleeding caused by the use of fibrinolytic drugs: every 6-8 hours, 10 mg / kg; the drug is used from the moment bleeding appears until it stops;
• states before tooth extraction in patients with coagulopathies: 10 mg / kg, after tooth extraction, the patient is transferred to the intake of tranexamic acid in tablet form.

Dose adjustment is required in patients with impaired renal function. At a glomerular filtration rate of 60–89 ml / min / 1.73 m ^{2, a} single dose is 10 mg / kg, the drug is administered 2 times a day. In patients with 30–59 ml / min / 1.73 m ² Stagemin is used in the same single dose once a day.

Side effects

When using Stagemin, the following side reactions can be observed (> 10% - very often;> 1% and 0.1% and 0.01% and <0.1% - rarely; <0.01% - very rarely):

• blood coagulation system: very rarely - thromboembolism, thrombosis;
• nervous system: rarely - convulsions; very rarely - weakness, dizziness, drowsiness;
• digestive system: often - heartburn, nausea, anorexia, vomiting, diarrhea;
• cardiovascular system: rarely - thromboembolic complications, a significant decrease in blood pressure (usually due to excessively rapid intravenous administration of Stagemin); very rarely - arterial / venous thrombosis of different localization; with an unknown frequency - deep vein thrombosis of the legs, acute myocardial infarction, thrombosis of cerebral arteries, stroke, thrombosis of the carotid arteries, pulmonary thromboembolism, occlusion of aorto-coronary bypass graft, renal artery thrombosis, accompanied by the occurrence of acute renal failure and cortical necrosis
• immune system: very rarely - hypersensitivity reactions, including anaphylactic shock;
• organ of vision: rarely - retinal vascular thrombosis, visual impairment, including impaired color perception;
• skin and subcutaneous tissues: rarely - allergic skin reactions, including allergic dermatitis;
• allergic reactions: rarely - itchy skin, rash, urticaria.

Overdose

• main symptoms: visual impairment, rash, myoclonus, nausea, diarrhea, vomiting, orthostatic hypotension, arterial / venous thromboembolism, changes in mental status;
• therapy: the patient must be hospitalized. The antidote is unknown. To enhance renal excretion, oral or parenteral administration of large amounts of fluid is recommended, forced diuresis is performed, and the amount of urine excreted is monitored. Some patients are prescribed anticoagulants.

special instructions

Before and during therapy, the patient should be examined by an optometrist (color vision, visual acuity, fundus).

In rare cases, with hematuria from the upper urinary tract, there may be a risk of mechanical anuria, which is associated with the formation of a clot in the urethra.

The concentration of tranexamic acid in the blood in patients with renal insufficiency increases, in such cases it is recommended to reduce the dose of the drug.

The condition of patients with disseminated intravascular coagulation (DIC) undergoing treatment with Stagemin should be closely monitored.

In the presence of a high risk of thrombosis, the drug can be used under strict medical supervision only in cases where there is an urgent need. Before using Stagemin, an examination should be carried out, the purpose of which is to identify risk factors for thromboembolic complications.

In patients with blood in cavities, for example, in the joint cavities, pleural cavity and urinary tract (including in the bladder and renal pelvis), therapy can lead to the formation of insoluble clots in them (associated with extravascular blood coagulation), which can be resistant to physiological fibrinolysis.

In case of irregular menstrual bleeding, Stagemin should not be prescribed until the cause of dysmenorrhea is established. Episodes in which the volume of menstrual bleeding is inadequately reduced during therapy warrant consideration of alternative treatment.

The combined use of Stagemin and anticoagulants should be carried out under the close supervision of a physician who has experience in treating blood clotting disorders (due to the lack of adequate clinical studies).

Influence on the ability to drive vehicles and complex mechanisms

During the period of treatment with Stagemin, performing types of work requiring increased concentration of attention and high speed of psychomotor reactions, including driving vehicles, should be abandoned.

Application during pregnancy and lactation

During pregnancy, Stagemin can be prescribed only if absolutely necessary.

Breastfeeding should be interrupted for breastfeeding women during therapy.

Tranexamic acid penetrates the placental barrier; in the umbilical cord blood, the substance is found in a concentration close to that of the mother. In animal studies, it was found that the drug does not affect the embryonic / neonatal development of offspring. Strictly controlled and adequate surveys have not been carried out in pregnant women.

The study of reproductive function in animals does not in all cases allow predicting reactions in humans, therefore Stagemin in pregnant women can be used only for vital indications.

Tranexamic acid passes into breast milk and reaches approximately 1% of the concentration in the mother's blood plasma. If it is necessary to use Stagemin, breastfeeding should be interrupted.

Pediatric use

Due to the limited experience of use, Stagemin therapy is contraindicated before the age of 1 year. In the treatment of menorrhagias, the drug is not prescribed for patients under 16 years of age.

With impaired renal function

Severe chronic renal failure (in patients with a glomerular filtration rate less than 30 mg / ml / 1.73 m ²) is a contraindication to the use of Stagemin.

Drug interactions

Pharmaceutical incompatibility of tranexamic acid is noted with the following drugs: urokinase, dipyridamole, hypertensive drugs (norepinephrine), diazepam.

Clinical studies on the interaction of Stagemin with other drugs / substances have not been conducted.

Possible interactions:

• fibrinolytic drugs: Stagemin is able to prevent the development of their thrombolytic effect;
• hemostatic drugs: activation of thrombus formation may be observed;
• preparations of coagulation factors II, VII, IX and X in combination (prothrombin complex) or anti-inhibitory coagulant complex: there is an increase in the likelihood of thrombosis;
• combined oral contraceptives: the risk of arterial thrombosis and venous thromboembolic complications (including ischemic stroke and myocardial infarction) increases; there is no information about this complex application.

Tranexamic acid solution is compatible with unfractionated heparin, most infusion solutions including dextrans, 0.9% sodium chloride solution, Ringer's solution, amino acid solutions, 5% dextrose solution.

It is impossible to mix tranexamic acid with blood products and solutions of antibacterial drugs (penicillins, tetracyclines).

Analogs

Analogues of Stagemin are Sanksamik, Gemtranix, Trameston, Traksara, Tranexamic acid, Tranexam, Transamcha, Tranexolon, Troxaminat, Exatsil, Cyclocapron, Cyclohemal, etc.

Terms and conditions of storage

Store at 2-25 ° C. Keep out of the reach of children.

Shelf life is 2 years.

Terms of dispensing from pharmacies

Dispensed by prescription.

Reviews about Stagemin

Reviews about Stagemin are extremely rare. The drug is often used in ENT practice, according to doctors - it is effective for bleeding from niches of the tonsils and nosebleeds. But it should be used with caution in heart disease, thrombophlebitis and vascular disease.

According to the expert, Stagemin's price is very high.

Price for Stagemin in pharmacies

The approximate price of Stagemin, a solution for intravenous administration of 50 mg / ml, for 10 ampoules of 5 ml each is 1625 rubles.

Stagemin: prices in online pharmacies

Drug name Price Pharmacy

Stagemin 50 mg / ml solution for intravenous administration 5 ml 10 pcs. 328 RUB Buy

Stagemin solution for intravenous injection 50mg / ml 5ml 10 pcs. 604 RUB Buy

Anna Kozlova Medical journalist About the author

Education: Rostov State Medical University, specialty "General Medicine".

Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!