Cyclogemal pills 250mg, 10pcs

Composition

Active ingredient:  

tranexamic acid – 250 mg or 500 mg.

Excipients: microcrystalline cellulose-45.05 mg or 90.10 mg, pregelatinized starch-4.85 mg or 9.70 mg, sodium carboxymethyl starch-6.20 mg or 12.40 mg, talc – 7.99 mg or 15.98 mg, colloidal silicon dioxide-6.01 mg or 12.02 mg, sodium stearyl fumarate-9.90 mg or 19.80 mg.

Shell: VIVACOAT®PA-1P-000 [6 GPa hypromellose (hydroxypropyl methylcellulose 6 SDR) is 3,51 mg or 7,02 mg, titanium dioxide – 2,70 5,40 mg or mg, Polydextrose (E 1200) – 1,35 2,70 mg or mg, talc – 0,90 1,80 mg or mg, polyethylene glycol-3350 – 0,54 mg or 1.08 mg] – 9,00 18,00 mg or mg.

Pharmacological action

Antifibrinolytic agent. Tranexamic acid specifically inhibits the activation of profibrinolysin (plasminogen) and its conversion to fibrinolysin (plasmin). The antifibrinolytic activity of tranexamic acid is approximately 10 times higher than that of epsilon-aminocaproic acid.

Tranexamic acid has a local and systemic hemostatic effect in bleeding associated with increased fibrinolysis. In addition, tranexamic acid has analgesic, anti-allergic and anti-inflammatory effects by suppressing the formation of kinins and other active peptides involved in allergic and inflammatory reactions.

Pharmacokinetics

Absorption at oral doses in the range of 0.5-2 g is 30-50%. The time to reach the maximum concentration with oral use of 0.5,1 and 2 g of tranexamic acid is 3 hours, the maximum concentration is 5.8 and 15 mcg / ml, respectively. Food intake does not affect the absorption of tranexamic acid in the gastrointestinal tract.

Plasma protein binding (profibrinolysin) is less than 3%. Tranexamic acid does not bind to albumin. The therapeutic concentration of tranexamic acid in blood plasma is 5-10 mg/l.

It is distributed relatively evenly in the tissues (except for the cerebrospinal fluid, where the concentration is 1/10 of the plasma); it penetrates through the placental barrier, into breast milk (about 1% of the concentration in the mother’s plasma), through the blood-brain barrier, into the intra-articular fluid and synovial membranes. The initial volume of distribution is 9-12 liters. Antifibrinolytic concentration in various tissues is maintained for 17 hours, in plasma – up to 7-8 hours.

It is only slightly metabolized. The pharmacokinetic curve has a three-phase form with a half-life in the final phase of 3 hours. Total renal clearance is equal to plasma (7 l / h). Excreted by the kidneys (the main route is glomerular filtration) – more than 95% unchanged during the first 12 hours.

Two metabolites of tranexamic acid were identified: N-acetylated and deaminated derivatives.

After oral use of tranexamic acid at a dose of 10-15 mg / kg during the first hour,3 hours,24 hours and 48 hours,1%,7%,39% and 79% of the dose is excreted, respectively.

If renal function is impaired, there is a risk of accumulation of tranexamic acid.

Indications

Short-term treatment of bleeding associated with increased fibrinolysis in the following pathological conditions:

•  Prostatectomy; surgical interventions on the bladder

• * Menorrhagia

• * Nosebleeds;•

Conization of the cervix;

•  Traumatic hyphema (hemorrhage in the anterior chamber of the eye).

Prevention and treatment of bleeding in patients with hemophilia who undergo minor surgical intervention (including tooth extraction).

Hereditary angioedema (prevention of exacerbations of the disease).

Bleeding during pregnancy.

Use during pregnancy and lactation

In preclinical studies, tranexamic acid did not have a teratogenic effect. Adequate and strictly controlled studies of the efficacy and safety of tranexamic acid preparations in pregnant women have not been conducted. Tranexamic acid passes through the placenta and can be found in umbilical cord blood in concentrations close to maternal.

Since studies of reproductive function in animals do not always predict reactions in humans, tranexamic acid should only be used during pregnancy if absolutely necessary.

Tranexamic acid penetrates into breast milk (the concentration of the drug in milk is about 1% of the concentration in the mother’s blood plasma). The development of an antifibrinolytic effect in an children is unlikely. However, caution should be exercised when using tranexamic acid in nursing mothers.

Contraindications

• Hypersensitivity to tranexamic acid or other components of the drug;

• Severe chronic renal failure (glomerular filtration rate [GFR] less than 30 mg / ml/1.73 m2) due to the risk of accumulation;

• Venous or arterial thrombosis currently or in the anamnesis (deep leg vein thrombosis, pulmonary embolism, intracranial vascular thrombosis, etc. ) when simultaneous anticoagulant therapy is not possible;

• Fibrinolysis due to consumption coagulopathy (hypocoagulation stage of disseminated intravascular coagulation syndrome [DIC-syndrome]);

• A history of seizures.

• Acquired color vision disorder;

• Subarachnoid hemorrhage (due to the risk of brain edema, ischemia, and infarction);

• Children under 3 years of age (solid dosage form).

With caution

• Tranexamic acid should be used with caution in the following situations: :

• Hematuria caused by diseases of the renal parenchyma and bleeding from the upper urinary tract (risk of secondary mechanical obstruction of the urinary tract by a blood clot with the development of anuria) (See the section “Special instructions”);

• Patients at high risk of developing thrombosis (a history of thromboembolic events or a family history of thromboembolic diseases, a verified diagnosis of thrombophilia);

• Disseminated intravascular coagulation syndrome (DIC);

• The presence of blood in cavities, for example, in the pleural cavity, joint cavities and urinary tract;

• Patients receiving anticoagulant therapy (limited experience);

• Concomitant use of blood clotting factors II, VII, IX and X in combination with [prothrombin complex] or an anti-inhibitory anticoagulant complex (See the section “Interaction with other drugs”);

• Treatment of menorrhagia in patients under 15 years of age (limited experience);

• Patients taking combined oral contraceptives (due to an increased risk of venous thromboembolic complications and arterial thrombosis) (See the section “Interaction with other medications”).

Side effects

the incidence of adverse drug reactions identified in accordance with the who classification: very often (> 1/10), often (> 1/100, ≤ 1/10), infrequently (> 1/1000, ≤ 1/100), rare (> 1/10000, ≤ 1/1000), very rare (less than 1/10000), frequency unknown (cannot be installed according to the available data).

Disorders of the gastrointestinal tract: often – nausea, vomiting, diarrhea (symptoms disappear when the dose is reduced).

Skin and subcutaneous tissue disorders: rarely – allergic skin reactions, including allergic dermatitis.

Visual disturbances: rarely-visual disturbances, including color perception disorders, retinal vascular thrombosis.

Vascular disorders: rarely – thromboembolic complications, marked decrease in blood pressure (usually due to excessively rapid intravenous use, in exceptional cases – after oral use);very rarely –arterial and venous thrombosis of various localization; frequency unknown – acute myocardial infarction, cerebral artery thrombosis, carotid artery thrombosis, stroke, deep vein thrombosis of the legs, pulmonary embolism, renal artery thrombosis with the development of cortical necrosis and acute renal failure, occlusion of the aorto-coronary shunt, thrombosis of the central artery and retinal vein.

Immune system disorders: very rarely – hypersensitivity reactions, including anaphylactic shock.

Nervous system disorders: rarely-dizziness; convulsions (usually with intravenous use).

Interaction

No specific clinical studies have been conducted to investigate the interactions of tranexamic acid with other drugs.

Tranexamic acid prevents the development of the pharmacological effect of fibrinolytic (thrombolytic) drugs.

Combined oral contraceptives increase the risk of venous thromboembolic complications and arterial thrombosis (in particular, ischemic stroke and myocardial infarction).

There is no experience of using tranexamic acid in women taking combined oral contraceptives.Since tranexamic acid has an antifibrinolytic effect, concomitant use with combined oral contraceptives may lead to an additional increase in the risk of thrombotic complications.

Concomitant use of tranexamic acid with coagulation factor II, VII, IX and X preparations in combination with [prothrombin complex] or an anti-inhibitory coagulant complex increases the risk of thrombosis.

There may be an 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.

Concomitant use of tranexamic acid with anticoagulants should be carried out under strict medical supervision (limited experience).

How to take, course of use and dosage

Inside, regardless of food intake.

Short-term treatment of bleeding caused by increased fibrinolysis: the recommended standard dose of tranexamic acid is 15-25 mg/kg of body weight, on average 1000-1500 mg 2-3 times a day.

For prostatectomy and surgical interventions on the bladder: 1000 mg 6 hours before surgery, then 1000 mg 3-4 times a day until the macrohematuria disappears. It is not recommended to use the drug for more than 2 weeks after surgery.

For menorrhagia:the recommended daily dose is 1000 mg 3 times a day until the end of menorrhagia, but not more than 4 days. With profuse bleeding, the dose of the drug can be increased, while the total daily dose should not exceed 4000 mg. Treatment with tranexamic acid should not be started before menstrual bleeding occurs. In clinical trials, tranexamic acid was not used for more than three consecutive menstrual cycles.

For recurrent nosebleeds: 1000 mg 3 times a day for 7 days.

After the operation of conization of the cervix: 1500 mg 3 times a day for 12 days after the operation.

For traumatic hyphema: 1000-1500 mg 3 times a day (target dose 25 mg / kg body weight) for 7 days.

Patients with hemophilia: the drug is prescribed orally at a dose of 25 mg/kg of body weight 2 hours before tooth extraction, and then 1000-1500 mg 3 times a day for 6-8 days. Blood clotting factors VIIII or IX should be administered simultaneously.

For hereditary angioedema: 1000-1500 mg 2-3 times a day. If the patient can anticipate an exacerbation of the disease, the drug can be taken intermittently, depending on the presence of prodromal symptoms. In all other cases, the drug should be taken constantly.

Bleeding during pregnancy: 250-500 mg 3-4 times a day until the bleeding stops completely. The average duration of treatment is 7 days.

Overdose

There are limited data on overdose cases. One case of overdose has been reported (taking 37 g of tranexamic acid).

Symptoms: dizziness, headache, nausea, vomiting, diarrhea, orthostatic symptoms (including dizziness when moving from horizontal to vertical position), orthostatic hypotension. Predisposed patients have an increased risk of thrombosis.

Treatment: The antidote is unknown. If an overdose of tranexamic acid is suspected, hospitalization is required. When providing assistance, you should induce vomiting, then conduct gastric lavage. Activated charcoal reduces the absorption of tranexamic acid when taken orally within the first 1-2 hours after an overdose. If the patient is unconscious or has difficulty swallowing, activated charcoal can be administered through a nasogastric tube. Oral or parenteral use of a large amount of fluid is recommended to increase renal excretion, forced diuresis, and control of the amount of urine released. In some cases, the use of anticoagulants may be justified.

Special instructions

In patients with hereditary angioedema, consultation with an ophthalmologist is necessary before starting treatment (determination of visual acuity, color vision, fundus condition). During treatment, regular ophthalmological examination is necessary (including assessment of visual acuity and color perception, examination of the fundus with a slit lamp, measurement of intraocular pressure, assessment of visual fields). If visual disturbances occur during treatment with tranexamic acid, the drug should be discontinued.

In patients with hereditary angioedema who have been receiving tranexamic acid preparations for a long time, regular laboratory monitoring of liver function is necessary.

Tranexamic acid preparations should be used with caution in hematuria caused by diseases of the renal parenchyma, since in these conditions intravascular deposition of fibrin is often observed, which can aggravate kidney damage. In addition, in cases of massive bleeding of any etiology from the upper urinary tract, antifibrinolytic therapy increases the risk of blood clots in the renal pelvis and/or ureter and, accordingly, secondary mechanical obstruction of the urinary tract and the development of anuria.

Although clinical studies have not shown a significant increase in the incidence of thrombosis, the risk of thrombotic complications cannot be completely excluded. Cases of venous and arterial thrombosis and thromboembolism have been described in patients treated with tranexamic acid. In addition, cases of occlusion of the central retinal artery and central retinal vein have been reported. Several patients developed intracranial thrombosis during treatment with tranexamic acid. Accordingly, in patients with a high risk of developing thrombosis (a history of thromboembolic complications, cases of thromboembolism in relatives, a verified diagnosis of thrombophilia), tranexamic acid should be used only if absolutely necessary and under strict medical supervision. Before using tranexamic acid, an examination should be performed to identify risk factors for thromboembolic complications.

The presence of blood in cavities, for example, in the pleural cavity, joint cavities and urinary tract (including in the renal pelvis and bladder) can lead to the formation of an “insoluble clot” in them due to extravascular blood clotting, which can be resistant to physiological fibrinolysis.

Patients with irregular menstrual bleeding should not be prescribed tranexamic acid until the cause of dysmenorrhea is established. If the volume of menstrual bleeding is not adequately reduced during treatment with tranexamic acid, alternative treatment should be considered.

The efficacy and safety of tranexamic acid preparations in the treatment of menorrhagia in patients under 16 years of age have not been established.

Tranexamic acid should be used with caution in women who are taking combined oral contraceptives at the same time, due to the increased risk of thrombosis (See the section “Interaction with other medications”).

In patients with DIC who require treatment with tranexamic acid, therapy should be carried out under the close supervision of a doctor who has experience in the treatment of this disease.

Due to the lack of adequate clinical studies, the concomitant use of tranexamic acid with anticoagulants should be carried out under the careful supervision of a specialist with experience in the treatment of blood clotting disorders.

If there is a visual impairment while taking tranexamic acid, you should stop taking the drug and consult a doctor.

Influence on the ability to drive vehicles and mechanisms

The ability of tranexamic acid to affect the rate of psychomotor reactions and the ability to drive vehicles or other mechanical devices has not been studied. Tranexamic acid can cause dizziness and visual disturbances, and, accordingly, can affect the ability to engage in potentially dangerous activities that require increased concentration and speed of psychomotor reactions.

Storage conditions

At a temperature not exceeding 25 °C.

Keep out of reach of children.

Shelf

life is 2 years.

Active ingredient

Tranexamic Acid

Conditions of release from pharmacies

By prescription

Dosage form

Tablets

Purpose

For adults as directed by your doctor

Indications

Bleeding, Nosebleed