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

Composition:For 1 tablet:
Active substance: tranexamic acid 250 mg / 500 mg.
Excipients (core): microcrystalline cellulose 28 mg / 56 mg, povidone K-30 9.5 mg / 19 mg, croscarmellose sodium 7.5 mg / 15 mg, silicon colloidal oxide 3.75 mg / 7.5 mg, talc purified 3 , 5 mg / 7 mg, magnesium stearate 3.75 mg / 7.5 mg.Excipients (shell) hypromellose 5.085 mg / 10.17 mg Titanium dioxide 1.95 mg / 3.9 mg, 0.965 mg of propylene glycol / 1.93 mg, 1 mg diethylphthalate / 2 mg.

Description:For a dosage of 250 mg. Round, biconvex tablets, covered with a film coat from white to almost white. On the cross-section - the core is from white to almost white.
For a dosage of 500 mg. Round, biconvex tablets, covered with a film coat from white to almost white. On the cross-section - the core is from white to almost white.

Pharmacotherapeutic group:Hemostatic agent.

ATX: & nbsp

B.02.A.A Amino acids

B.02.A.A.02 Tranexamic acid

Pharmacodynamics:Antifibrinolytic agent. Tranexamic acid specifically inhibits the activation of profibrinolysin (plasminogen) and its conversion to fibrinolysin (plasmin). Has a local and systemic hemostatic effect in bleeding associated with increased fibrinolysis (platelet pathology, menorrhagia). Also tranexamic acid, By suppressing the formation of kinins and other active peptides involved in allergic and inflammatory reactions, have anti-allergic and anti-inflammatory action.

Pharmacokinetics:Absorption at oral intake of doses in the range of 0.5-2 g is 30-50%. The time to reach the maximum concentration (T_max) with oral administration of 0.5, 1 and 2 g - 3 hours, the maximum concentration level (C_max) - 5, 8 and 15 μg / ml, respectively. The connection with plasma proteins (profibrinolysin) is less than 3%.
It is distributed in tissues relatively evenly (except for cerebrospinal fluid, where the concentration is 1/10 of the plasma one); penetrates the placental barrier, into breast milk (about 1% of the concentration in the mother's plasma). It is found in seminal fluid, where it reduces fibrinolytic activity, but does not affect the migration of spermatozoa. The initial volume of distribution is 9-12 liters. Antifibrinolytic concentration in various tissues persists for 17 hours, in plasma up to 7-8 hours.
Metabolizes a small part. The curve AUC has a three-phase form with a half-life (T_1/2) in the final phase - 3 hours. The total renal clearance is equal to the plasma clearance (7 l / h). It is excreted by the kidneys (the main way is glomerular filtration) -more than 95% unchanged during the first 12 hours.
Two metabolites of tranexamic acid have been identified: N-acetylated and deaminated derivatives.With impaired renal function, there is a risk of cumulation of tranexamic acid.

Indications:Prevention and treatment of bleeding on the background of increased generalized or local fibrinolysis in adults over 18 years of age. Local fibrinolysis can occur in the following cases:
- prostatectomy or other surgical interventions on the organs of the urinary system;
- hematuria;
- Menorrhagia;
- nosebleeds;
- uterine bleeding, including against the background of Willebrand disease and other coagulopathies;
- operation of conization of the cervix;
- traumatic hyphema;
- extraction of teeth in patients with coagulopathy;
- gastrointestinal bleeding (ulcerative colitis).
Generalized fibrinolysis can occur in the following cases:
- malignant neoplasms of the pancreas and prostate gland;
- obstetric complications (bleeding, placental abruption, postpartum haemorrhage);
- manual separation of the afterburn;
- operations on the thorax and other extensive surgical interventions;
- Leukemia and liver disease with the appointment of thrombolytic therapy with streptokinase.
Hereditary angioedema.
To reduce peri-and postoperative blood loss and during blood transfusion in adult patients who underwent heart surgery or total knee or hip arthroplasty.

Contraindications:- Hypersensitivity to the active substance or any of the excipients.
- Venous or arterial thrombosis at present or in anamnesis (deep vein thrombosis of the legs, pulmonary thromboembolism, thrombosis of the intracranial vessels, etc.).
- Fibrinolysis due to consumption coagulopathy, except for the preferential activation of the fibrinolytic system in severe acute bleeding.
- Severe chronic renal failure (glomerular filtration rate [GFR] less than 30 mg / ml / 1.73 m²) due to the risk of cumulation.
- A convulsive syndrome in the anamnesis.
- Acquired violations of color vision. If a visual impairment occurs during the course of treatment, the drug must be canceled.
- Subarachnoid hemorrhage.
- Childhood.

Carefully:- renal impairment due to the risk of cumulation;
- severe bleeding from the upper urinary tract due to the risk of thrombus formation and obstruction of the urinary tract;
- Hematuria caused by diseases of the renal parenchyma, because of the risk of mechanical anuria due to the formation of a thrombus in the ureter; with massive renal bleeding because of the risk of fixing a thrombus in the calyx-pelvis kidney system;
- thromboembolic complications in anamnesis and complicated family history of thromboembolism; tranexamic acid such patients should be prescribed for strict medical indications and under the strict supervision of a doctor because of the risk of thrombosis of the central artery and retinal vein;
- women taking oral contraceptives, because of the risk of thrombosis;
- taking Factor IX complex or anti-inhibitory anticoagulant complex because of the risk of thrombosis;
- if there is a congestion of blood in the pleural cavity, articular cavity, bladder and bowel-kidney system due to the development of an insoluble clot in these cavities due to its resistance to physiological fibrinolysis;
- women with irregular menstrual bleeding;
- verified diagnosis of thrombophilia;
- Patients receiving anticoagulant and heparin therapy;
- violation of color vision in the anamnesis;
- intravascular disseminated coagulation (DVS-syndrome).

Pregnancy and lactation:In preclinical studies tranexamic acid had no teratogenic effect. Adequate and strictly controlled studies of the efficacy and safety of the use of tranexamic acid preparations in pregnant women have not been conducted. Tranexamic acid penetrates the placenta and can be contained in cord blood in a concentration close to the mother's. Because studies of reproductive function in animals do not always allow predicting reactions in humans, tranexamic acid should be used during pregnancy only in case of emergency. Tranexamic acid penetrates into breast milk (the concentration of the drug in milk is about 1% of the concentration in the blood plasma of the mother). The development of antifibrinolytic effect in an infant is unlikely. Nevertheless, caution should be exercised when using tranexamic acid in nursing mothers.

Dosing and Administration:Inside. Swallow the whole tablet with water.
With local fibriosis the recommended standard dose for adults is 1000-1500 mg 2-3 times a day (in adults the recommended dose is 20-25 mg / kg body weight per day).
With prostatectomy therapy is prescribed from intravenous administration during the operation and during the first 3 days after the operation with the subsequent transition to oral administration of 1000-1500 mg 3-4 times a day until macroscopic confirmation of the absence of hematuria.
With haematuria prescribe 1000-1500 mg 2-3 times a day until macroscopic confirmation of the absence of hematuria.
With menorrhagia prescribe 1000-1500 mg 3-4 times a day for 3-4 days. Therapy with tranexamic acid begins when bleeding becomes profuse.
When bleeding against the background of von Willebrand disease and other coagulopathy appoint 1000-1500 mg 3-4 times a day. Duration of treatment - 3-10 days
With nasal bleeding appoint 1000 mg 3 times a day for 4-10 days. After the operation, conization of the cervix is prescribed 1500 mg 3 times a day for 12-14 days.
When bleeding during pregnancy prescribe 250-500 mg 3-4 times a day until the complete stop of bleeding. The average duration of the course of treatment is 7 days.
In case of traumatic hyphema prescribe 1000-1500 mg 3 times a day.
Patients with coagulopathy after extraction of a tooth prescribe 25 mg / kg body weight 3-4 times a day for 6-8 days.
With hereditary angioedema prescribe 1000-1500 mg 2-3 times a day as a permanent or intermittent therapy, depending on whether the patient has any prodromal signs of angioedema.
With generalized fibrinolysis therapy begins with parenteral (intravenous) administration followed by a transition to oral intake of 1000-1500 mg 2-3 times a day.
Renal impairment
T_1/2 increases, so it is recommended to reduce the dose of tranexamic acid.
In adults, WSCF (calculated glomerular filtration rate) ≥ 90 ml / min / 1.73 m² usually indicates a normal kidney function, but does not exclude patients with initial signs of renal dysfunction. If there is a suspicion of renal failure, other criteria for assessing kidney function may be used to select a dose, including a nephrologist. Patients with impaired renal function are recommended the following doses:

Level of creatinine in serum, μmol / l	Oral dose	Frequency
120-249	15 mg / kg	2 times a day
250-500	15 mg / kg	1 time per day
>500	7.5 mg / kg	1 time per day

Side effects:Determination of the frequency of adverse reactions: very often (more than 10%); often (from 1 to 10%); rarely (from 0.1 to 1%); very rarely (less than 0.1%).
Disorders from the digestive system: often - nausea, vomiting, diarrhea.
Disturbances from the skin and skin appendages: rarely - cutaneous allergic reactions.
Disorders from the cardiovascular system: rarely - thromboembolism; very rarely - lowering blood pressure with or without loss of consciousness, arterial and venous thrombosis.
Impaired nervous system: very rarely - dizziness, convulsions.
Disorders from the side of the organ of vision: rarely - violations of color perception and other visual disturbances, occlusion of the retina artery.
Immune system disorders: very rarely - hypersensitivity reactions, incl. anaphylactic shock.
Other: very rarely - a feeling of malaise.

Overdose:Possible symptoms: dizziness, headache, nausea, vomiting, diarrhea, orthostatic hypotension.
There is no specific antidote. In case of an overdose, treatment should be symptomatic. You can induce vomiting if the patient is conscious, rinsing the stomach, prescribing Activated carbon and carry out forced diuresis. Thrombotic patients are at risk for thrombosis. It is recommended to monitor the patient and control the function of vital organs and systems. In some cases, the use of anticoagulants may be justified.

Interaction:Simultaneous use of tranexamic acid with preparations of coagulation factors II, VII, IX and X in combination [prothrombin complex] or anti-inhibitory coagulant complex increases the risk of thrombosis.
Possible increased risk of thrombotic complications (in particular, myocardial infarction) with the simultaneous use of tranexamic acid with hydrochlorothiazide, desmopressin, ampicillin-sulbactam, ranitidine and nitroglycerin.
When combined with hemostatic drugs, activation of thrombosis is possible.
Tranexamic acid prevents the thrombolytic effect of fibrinolytic drugs.
When tranexamic acid is combined with anticoagulants, the patient should be under constant medical supervision.
With the combined use of tranexamic acid with estrogens, there is a theoretical risk of increased thrombogenesis (thrombogenic potential).

Special instructions:Extraction of the tooth in patients with coagulopathy: it may be necessary to use the Coagulation Factor concentrate. This decision should be made after consultation with the hemostasist.
Fertility: There are no clinical data on the effects of tranexamic acid on fertility.

Effect on the ability to drive transp. cf. and fur:Some of the side effects of tranexamic acid, such as dizziness, impaired color perception, other visual impairment, retinal artery occlusion, seizures, can adversely affect the ability to drive a vehicle and carry out potentially dangerous activities requiring increased concentration and speed of psychomotor reactions.

Form release / dosage:Tablets, film-coated, 250 mg, 500 mg.

Packaging:For 10 tablets in a blister of aluminum foil and colorless transparent polyvinyl chloride film. For 3 blisters together with instructions for use in a cardboard box.
For 100, 500 or 1000 tablets per package of polyethylene.A package in a plastic jar, sealed with aluminum foil with a polyethylene coating, with a screw cap; on the bank paste a label from paper label or writing or from polymer materials, self-adhesive. At 1,5, 10, 20 or 40 cans, together with an equal number of instructions for medical use in a group package - a box of corrugated cardboard (for hospitals).

Storage conditions:At a temperature of no higher than 25 ° C. Keep out of the reach of children.

Shelf life:3 years. Do not use after the expiration date printed on the package.

Terms of leave from pharmacies:Without recipe

Registration number:LP-003853

Date of registration:21.09.2016

Expiration Date:21.09.2021

The owner of the registration certificate:SP.INKOMED, LLC SP.INKOMED, LLC Russia

Manufacturer: & nbsp

SANJIVANI PARANTERAL, Limited India

Representation: & nbspSP.INKOMED LLCSP.INKOMED LLC

Information update date: & nbsp2016-10-09

Illustrated instructions

Instructions

Sanssamik (sanxamik)