Cyclohemal
Cyclohemal: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. Application during pregnancy and lactation
- 10. Use in childhood
- 11. In case of impaired renal function
- 12. For violations of liver function
- 13. Use in the elderly
- 14. Drug interactions
- 15. Analogs
- 16. Terms and conditions of storage
- 17. Terms of dispensing from pharmacies
- 18. Reviews
- 19. Price in pharmacies
Latin name: Cyclogemal
ATX code: B02AA02
Active ingredient: tranexamic acid (Tranexamic acid)
Manufacturer: JSC "Pharmstandard-Tomskkhimfarm" (Russia) for JSC "Otisipharm" (Russia)
Description and photo update: 2020-01-04
Prices in pharmacies: from 73 rubles.
Buy
Cyclohemal is a hemostatic drug.
Release form and composition
Cyclohemal is produced in the form of film-coated tablets: white or almost white, biconvex, in a dosage of 250 mg - round, in a dosage of 500 mg - oblong; the core of tablets of white or almost white color (10 pcs. in blisters, in a cardboard box of 1, 2, 3 or 6 packs and instructions for the use of Cyclohemal).
1 tablet contains:
- active substance: tranexamic acid - 250 mg or 500 mg;
- auxiliary components: microcrystalline cellulose, pregelatinized starch, sodium stearyl fumarate, sodium carboxymethyl starch, colloidal silicon dioxide, talc;
- composition of the film shell: VIVACOAT PA-1P-000 [polyethylene glycol, hypromellose 6 cps (hydroxypropyl methylcellulose 6 cps), polydextrose (E1200), titanium dioxide, talc].
Pharmacological properties
Pharmacodynamics
Cyclohemal is a hemostatic drug that has an antifibrinolytic effect. Its active ingredient, tranexamic acid, is a specific inhibitor of the activation of profibrinolysin (plasminogen) and its conversion to fibrinolysin (plasmin). Has a local and systemic hemostatic effect in bleeding caused by increased fibrinolysis. By inhibiting the formation of active peptides (including kinins) involved in inflammatory and allergic reactions, it has anti-inflammatory, anti-allergic and analgesic effects.
Compared to epsilon aminocaproic acid, the antifibrinolytic activity of tranexamic acid is about 10 times higher.
Pharmacokinetics
After oral administration of tranexamic acid in a dose of 500 mg to 2000 mg, absorption in the gastrointestinal tract is 30-50%. The maximum concentration (C max) in the blood is reached after 3 hours, while taking a single dose of 500 mg it is 0.005 mg / ml, 1000 mg - 0.008 mg / ml, 2000 mg - 0.015 mg / ml. Simultaneous food intake does not affect the absorption of the active substance.
Communication with plasma proteins (profibrinolysin) - less than 3% of the dose taken, tranexamic acid does not bind to albumin.
Therapeutic concentration in blood plasma is 5–10 mg / l.
The initial volume of distribution is 9–12 liters.
The concentration in the cerebrospinal fluid is 1/10 of the plasma level; in other tissues, tranexamic acid is distributed relatively evenly. It overcomes the blood-brain barrier, penetrates into the intra-articular fluid, synovial membranes, through the placental barrier and into breast milk. Up to 1% of the content in the mother's plasma is found in breast milk. The antifibrinolytic concentration of tranexamic acid in plasma is maintained for 7-8 hours, in various tissues - 17 hours.
It is biotransformed to an insignificant extent, 2 metabolites have been identified - N-acetylated and deaminated derivatives.
The pharmacokinetic curve has a three-phase shape. The half-life in the final phase is 3 hours.
The total renal and plasma clearance is 7 l / h.
Tranexamic acid is excreted through the kidneys during the first 12 hours more than 95% unchanged. The main route of elimination is glomerular filtration.
After oral administration in a dose of 10-15 mg / kg of the patient's body weight, 1% of the dose taken is excreted during the first hour, 7% in three hours, and 39% and 79% in 24 hours and 48 hours, respectively.
The risk of cumulation of tranexamic acid occurs with impaired renal function.
Indications for use
The use of Cyclohemal is indicated for the short-term treatment of bleeding caused by an increase in fibrinolysis, in the following pathological conditions / injuries:
- nose bleed;
- surgical interventions on the bladder;
- prostatectomy;
- conization of the cervix;
- menorrhagia;
- traumatic hyphema (hemorrhage in the anterior chamber of the eye).
In addition, in patients with hemophilia, Cyclohemal is prescribed for the prevention and treatment of bleeding during minor surgical interventions (including tooth extraction).
With hereditary angioedema, the drug is used to prevent exacerbations of the disease.
Contraindications
Absolute:
- fibrinolysis due to consumption coagulopathy or hypocoagulation stage of DIC syndrome (disseminated intravascular coagulation syndrome);
- chronic form of severe renal failure [glomerular filtration rate (GFR) less than 30 mg / ml / 1.73 m 2];
- deep vein thrombosis of the legs, thromboembolism of the pulmonary artery, thrombosis of intracranial vessels and other types of venous or arterial thrombosis (including history) - if the simultaneous use of anticoagulants is impossible;
- acquired color vision impairment;
- a history of convulsions;
- subarachnoid hemorrhage;
- treatment of menorrhagias under the age of 16;
- age up to 3 years;
- hypersensitivity to tranexamic acid and / or auxiliary components of the drug.
Cyclohemal tablets should be taken with caution in the presence of one of the following conditions or diseases: hematuria (caused by diseases of the renal parenchyma); bleeding from the upper urinary tract; a verified diagnosis of thrombophilia, a history of thromboembolic events, or a family history of thromboembolic diseases; DIC syndrome; the presence of blood in the pleural cavity, joint cavities and urinary tract or other cavities; concomitant anticoagulant therapy; simultaneous use of combined oral contraceptives, drugs of the prothrombin complex (coagulation factors II, VII, IX and X in combination) or anti-inhibitory coagulant complex; the period of pregnancy and lactation.
Cyclohemal, instructions for use: method and dosage
Cyclohemal tablets are taken orally, regardless of food intake.
Recommended dosage:
- bleeding due to increased fibrinolysis: the standard dose is 15–25 mg / kg of body weight (approximately 1000–1500 mg) 2-3 times a day for a short course of treatment;
- recurrent nosebleeds: 1000 mg 3 times a day. The duration of the course of treatment is 7 days;
- prostatectomy, surgical interventions on the bladder: 6 hours before the operation - 1000 mg, then 1000 mg 3-4 times a day. Reception of Cyclohemal is continued until the disappearance of gross hematuria, but no more than 14 days after surgery;
- menorrhagia: 1000 mg 3 times a day until the relief of menorrhagia, but not more than 4 days. In the treatment of profuse bleeding, the daily dose can be increased to 4000 mg. You should not start taking the pills before your menstrual bleeding occurs. It is important to take into account that the safety and efficacy of Cyclohemal was established on the results of clinical studies of the use of tranexamic acid only for three menstrual cycles in a row;
- conization of the cervix: 1500 mg 3 times a day for 12 days after surgery;
- traumatic hyphema: 25 mg / kg of body weight or 1000-1500 mg 3 times a day. The course of treatment is 7 days;
- prevention and treatment of bleeding during minor surgery in patients with hemophilia: 2 hours before tooth extraction - at a dose of 25 mg / kg body weight. Then, within 6-8 days, Cyclohemal should be taken 1000-1500 mg 3 times a day simultaneously with drugs of coagulation factors VIII or IX;
- hereditary angioedema: 1000-1500 mg 2-3 times a day. The patient must take the tablets constantly. If the patient is able to anticipate an exacerbation of the condition, Cyclohemal can be taken only when prodromal symptoms appear.
For mild to moderate renal impairment, it is required to adhere to a dosage regimen adjusted depending on the GFR index:
- GFR 60–89 ml / min / 1.73 m 2: 15 mg / kg of body weight 2 times a day;
- GFR 30–59 ml / min / 1.73 m 2: 15 mg / kg body weight once a day.
If liver function is impaired and in elderly patients, dose adjustment is not required.
For children over the age of three, Cyclohemal is prescribed in a dose of 25 mg / kg of body weight 2-3 times a day.
If you accidentally miss taking the next dose at the set time, you do not need to reimburse it by doubling the next dose.
Side effects
- from the gastrointestinal tract: often - nausea, vomiting, diarrhea;
- on the part of the skin and subcutaneous tissues: rarely - allergic dermatitis and other skin allergic reactions;
- on the part of the organ of vision: rarely - visual impairment, including retinal vascular thrombosis, impaired color perception;
- on the vascular side: rarely - a pronounced decrease in blood pressure (BP), thromboembolic complications; very rarely - venous and arterial thrombosis of various localization; frequency not established - cerebral artery thrombosis, deep vein thrombosis of the legs, carotid artery thrombosis, acute myocardial infarction, pulmonary embolism, stroke, coronary artery bypass graft occlusion, renal artery thrombosis with the development of cortical necrosis and acute renal artery disease and retinal vein thrombosis
- from the immune system: very rarely - hypersensitivity reactions, including anaphylactic shock;
- from the nervous system: rarely - dizziness; convulsions.
Overdose
Symptoms: nausea, vomiting, diarrhea, headache, dizziness, orthostatic symptoms (including dizziness when moving from horizontal to vertical position), orthostatic arterial hypotension, increased risk of thrombosis in predisposed patients.
Treatment: no specific antidote. Therefore, if an overdose of Cyclohemal is suspected, it is necessary to immediately induce vomiting followed by gastric lavage. To reduce the absorption of tranexamic acid during the first two hours after an overdose, the intake of activated carbon is indicated. If the patient is unconscious or if swallowing is impaired, a nasogastric tube can be used to administer activated charcoal. In order to enhance renal excretion, the patient must enter a large amount of fluid orally or parenterally. After hospitalization, forced diuresis is used, controlling the volume of urine excreted. If necessary, the appointment of anticoagulants is allowed.
special instructions
Before taking the drug, patients with hereditary angioedema need to undergo an ophthalmological examination to determine visual acuity, color vision and the state of the fundus. In this category of patients, treatment with Cyclohemal must be accompanied by regular monitoring of liver function indicators, visual acuity, color perception, intraocular pressure, visual fields and fundus. If any visual impairment is detected while taking tranexamic acid, therapy should be discontinued.
To eliminate side effects from the gastrointestinal tract, it is required to reduce the dose of Cyclohemal.
Patients with hematuria caused by diseases of the renal parenchyma should be aware that tranexamic acid preparations can aggravate the condition of the affected kidneys.
Antifibrinolytic therapy for massive bleeding of any etiology from the upper urinary tract increases the risk of blood clots in the renal pelvis and / or ureter, secondary mechanical obstruction of the urinary tract and the development of anuria.
When prescribing Cyclohemal, research is required to identify risk factors for thromboembolic complications. Due to the high probability of thrombosis, the use of tranexamic acid in patients with a verified diagnosis of thrombophilia, a history of thromboembolic complications or the presence of thromboembolic diseases in their relatives is allowed only in cases of extreme necessity and under the supervision of a physician.
The use of Cyclohemal in the presence of blood in various cavities (including the pleural cavity, joint cavities and urinary tract) due to extravascular coagulation of blood can cause the formation of an insoluble clot in them, which is resistant to physiological fibrinolysis.
With irregular menstrual bleeding, Cyclohemal should be prescribed only after establishing the cause of dysmenorrhea. If during treatment with tranexamic acid there is an inadequate decrease in the volume of menstrual bleeding, it is necessary to consider transferring the patient to alternative therapy.
In case of visual impairment caused by taking the drug, treatment with tranexamic acid is stopped.
Influence on the ability to drive vehicles and complex mechanisms
In connection with the possible development of dizziness or visual impairment during the period of application of Cyclohemal, patients are advised to be careful when performing potentially hazardous activities that require increased concentration of attention and high speed of psychomotor reactions, including driving and complex mechanisms.
Application during pregnancy and lactation
Cyclohemal should be used with caution during pregnancy and breastfeeding, only in cases of extreme necessity.
Pediatric use
The use of Cyclohemal is contraindicated for all indications in children under 3 years of age, for the treatment of menorrhagia - in children and adolescents under the age of 16 years.
Information on the efficacy and safety of tranexamic acid in pediatric patients is limited.
Recommended dosage for children: at the rate of 25 mg / kg of body weight 2-3 times a day.
With impaired renal function
The use of Cyclohemal is contraindicated in severe chronic renal failure (GFR less than 30 mg / ml / 1.73 m 2).
With mild to moderate renal impairment, correction of the dosage regimen is required taking into account the GFR indicator.
For violations of liver function
In case of impaired liver function, dose adjustment of Cyclohemal is not required.
Use in the elderly
For elderly patients, dose adjustment is not required.
Drug interactions
Cyclohemal prevents the development of the pharmacological action of fibrinolytics (thrombolytic drugs).
Women taking combined oral contraceptives should be especially careful while using tranexamic acid. Since this combination of drugs contributes to an additional increase in the risk of arterial thrombosis and venous thromboembolic complications (including myocardial infarction, ischemic stroke).
The risk of thrombosis increases with concomitant therapy with drugs of coagulation factors II, VII, IX and X in combination (prothrombin complex) or anti-inhibitory coagulant complex.
The likelihood of thrombotic complications (including myocardial infarction) may increase with the simultaneous administration of tranexamic acid with drugs such as ranitidine, hydrochlorothiazide, ampicillin sulbactam, nitroglycerin, desmopressin.
Thrombus activation is possible when combined with hemostatic drugs.
Due to the limited experience in the use of tranexamic acid with anticoagulants, combination therapy with drugs of this pharmacological group should be accompanied by close supervision of a physician with experience in the treatment of blood coagulation disorders.
Analogs
Analogs of Cyclohemal are Tranexamic acid, Tranexamic acid-Akrikhin, Tranexamic acid-SOLOpharm, Tranexamic acid-TRIVIUM, Bitranex, GEMTRANIX, Sansamik, Stagemin, Traxara, Trameston, Tranexam, Troxaminate, etc.
Terms and conditions of storage
Keep out of the reach of children.
Store at temperatures up to 25 ° C.
Shelf life is 2 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Cyclohemal
There are currently no reviews of Cyclohemal.
The price of Cyclohemal in pharmacies
The price of Cyclohemal, film-coated tablets (dosage 250 mg) per pack containing 10 pcs., Can range from 147 rubles, per pack 30 pcs. - from 430 rubles.
Cyclohemal: prices in online pharmacies
|
Drug name Price Pharmacy |
|
Cyclohemal 250 mg film-coated tablets 10 pcs. 73 rbl. Buy |
|
Cyclohemal tab p.p. 250mg 10 pcs. 170 RUB Buy |
|
Cyclohemal 250 mg film-coated tablets 30 pcs. 223 r 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!
