Bemiparin sodium - instructions for use, dose, side effects, contraindications

Clinical and pharmacological group: & nbsp

Anticoagulants

Included in the formulation

Cibor® 2500

solution PC

BERLIN-PHARMA, CJSC Russia

Cibor® 3500

solution PC

BERLIN-PHARMA, CJSC Russia

АТХ:

B.01.A.B.12 Bemiparin sodium

B.01.A.B Heparin and its derivatives

Pharmacodynamics:

Bemiparin is a low molecular weight heparin, obtained as a result of depolymerization of sodium heparin isolated from the intestinal mucosa of a pig. The average molecular weight of bemiparin is about 3600 Da.

Clinical use of bemiparin sodium confirms its anticoagulant activity and, when the recommended dosage is observed, does not cause a significant increase in clotting time.

In experimental studies on animals, the anticoagulant effect of sodium bemiparin and the moderate hemorrhagic effect are shown.

Pharmacokinetics:

After a subcutaneous injection beemiparin sodium quickly absorbed.

Bioavailability is 96%.

The half-life of sodium bemiparin when administered at doses between 2500 and 12 500 IU is approximately 5-6 hours.

At present, there is no data on the binding of bemiparin to plasma proteins, its metabolism and excretion in humans.

The maximum anti-Ha-factor activity in blood plasma when administered in preventive doses (2500 and 3500 IU) is achieved after 2-3h after subcutaneous administration of sodium bemiparin with a maximum activity of about 0.34 ± 0.08 and 0.45 ± 0.07 IU of anti-Xa factor / ml, respectively. Anti-IIa-factor activity at the indicated doses is not manifested.

Maximum anti-Ha-factor activity in blood plasma when administered at doses of 5000; 7500; 10 000 and 12 500 IU is achieved 3-4 hours after a subcutaneous injection of sodium bemiparin with a maximum activity of the order of 0.54 ± 0.06; 1.22 ± 0.27; 1.42 ± 0.19 and 2.03 ± 0.25 IU of anti-Xa factor / ml, respectively.

Indications:

Prevention of thromboembolism in patients with orthopedic surgery.

Prevention of blood clotting in the system of extracorporeal circulation during hemodialysis.

Preventing the development of thromboembolism in patients with general surgical interventions.

ICD-10

IX.I26-I28.I26 Pulmonary embolism

IX.I80-I89.I82 Embolism and thrombosis of other veins

IX.I70-I79.I74 Embolism and thrombosis of the arteries

Contraindications:

Bleeding or an increased risk of bleeding due to a clotting disorder.

Severe violations of the liver and pancreas.

Injuries or surgical interventions in the field of the central nervous system, the organ of vision or the organ of hearing.

The syndrome of disseminated intravascular coagulation in the context of heparin-induced thrombocytopenia.

Immunologically due to heparin thrombocytopenia or suspicion of it, or having it in history.

Acute bacterial endocarditis and chronic endocarditis. Pathological conditions with a high risk of bleeding, for example, an active peptic ulcer, hemorrhagic stroke, an aneurysm of cerebral vessels or neoplasms of the brain. Hypersensitivity to bemiparin and heparin sodium.

Carefully:

Caution should be used in patients with hepatic or renal insufficiency, vascular disorders of the iris and retina, as well as with any other organic disorders associated with an increased risk of bleeding, uncontrolled arterial hypertension, peptic ulcer of the stomach and duodenum in history, thrombocytopenia, urolithiasis, as well as in patients with spinal or epidural anesthesia and / or lumbar puncture.

Pregnancy and lactation:

Clinical data regarding the use of bemiparin in pregnant women are not available, so pregnant drug is prescribed with caution.

At present, there is no data on the ability of bemiparin to penetrate the placental barrier.

AT experimental research there were no signs of teratogenicity in animals.

Dosing and Administration:

In general-surgical interventions with a moderate risk of venous thromboembolism, a single dose is 2500 IU subcutaneously 2 hours before or 6 hours after the end of the operation, on subsequent days - every 24 hours. Preventively applied during the period of risk of thromboembolism or until the motor activity is completely restored patient. Usually such preventive treatment is carried out at least 7-10 days after the operation.

In order to prevent blood clotting in the extracorporeal circulation system in hemodialysis in patients undergoing multiple hemodialysis of no more than 4 hours, provided there is no risk of bleeding, the prevention of blood coagulation in the extracorporeal circulation system during the dialysis procedure is achieved by a single dose of beemiparin sodium by bolus injections into the arterial bed at the beginning of the hemodialysis session.For patients with a body weight ≤ 60 kg, the dose is 2500 IU, and with a body weight> 60 kg - 3500 IU.

In orthopedic operations with a high risk of venous thromboembolism, a single dose of 3500 IU subcutaneously 2 hours before or 6 hours after the end of the operation, on subsequent days - every 24 hours. Preventively applied during the period of risk of thromboembolism or until the recovery of motor activity patient. Usually, such preventive treatment is carried out at least 7-10 days after surgery.

Enter subcutaneously in the anterolateral area of the abdomen or in the posterolateral lumbar region, alternately from the right and left sides.

Side effects:

From the coagulation system of the blood: often - bleeding from the skin, mucous membrane, wounds, gastrointestinal tract, genito-urinary tract; sometimes - mild, transient thrombocytopenia; rarely severe thrombocytopenia. Epidural and spinal hematoma after epidural spinal anesthesia or lumbar puncture. These hematomas lead to neurologic disorders of varying severity, including prolonged or persistent paralysis.

From the digestive system: often - a mild, transient increase in the activity of transaminases and gamma-GT; rarely - nausea, vomiting.

Allergic reactions: sometimes - hives, itching; rarely - anaphylactic reactions (choking, bronchospasm, laryngeal edema), arterial hypotension.

Local reactions: very often - the ecchymosis at the injection site; often - hematoma and pain at the injection site; rarely - skin necrosis at the injection site.

Other: long-term use of drugs of the heparin group can lead to the development of osteoporosis.

Overdose:

No data. Treatment is symptomatic.

Interaction:

The use of bemiparin sodium, as well as other drugs of heparin, simultaneously with nitroglycerin for intravenous administration leads to a decrease in the effectiveness of the anticoagulant.

Vitamin K antagonists and other anticoagulants, non-steroidal anti-inflammatory drugs, including acetylsalicylic acid and other salicylates, ticlopidine, clopidogrel and other platelet aggregation inhibitors, systemic glucocorticosteroids and dextran increase the pharmacological effect of bemiparin sodium on coagulation and / or platelet function,which increases the risk of bleeding. If the simultaneous use of drugs can not be avoided, beemiparin sodium must be used under close clinical and laboratory control.

Special instructions:

The drug is not intended for intramuscular injection. In connection with the risk of developing hematomas, intramuscular injections of other drugs should be avoided during the treatment with bemiparin.

Preventive use of bemiparin sodium in combination with epidural or spinal anesthesia or lumbar puncture in rare cases can lead to the development of epidural or spinal hematoma, which can lead to prolonged or persistent paralysis. The risk of developing a hematoma increases with the use of an epidural or spinal catheter for anesthesia, with the concomitant use of drugs that affect blood clotting, for example, non-steroidal anti-inflammatory drugs, platelet aggregation inhibitors or anticoagulants, or with traumatic or multiple punctures. When deciding on the interval between the last administration of bemiparin sodium in a prophylactic dose andby introducing or removing an epidural or spinal catheter, the characteristic of the dosage form and the clinical status of the patient must be taken into account. After removal of the catheter, the next dose of sodium bemiparin can be administered no earlier than 4 hours. The administration of the next dose of bemiparin should also be delayed until the completion of the surgical procedure.

When deciding on the appointment of anticoagulant therapy in the context of epidural or spinal anesthesia, it is necessary to be extremely cautious and to conduct frequent monitoring of the patient's condition in order to detect signs and symptoms of neurological disorders, in particular back pain, sensitivity disorders and motor skills (numbness and weakness of the lower limbs ), as well as dysfunction of the intestine and bladder. If there is a suspicion of the presence of an epidural or spinal hematoma, an immediate diagnosis should be clarified with appropriate therapeutic measures up to spinal decompression.

The combined use of drugs that increase the concentration of potassium in the blood should be carried out under particularly careful control.

Older patients do not need a dose adjustment. A limited amount of data does not make it possible to give recommendations for correcting the dosage of bemiparin sodium for these patients.

Bemiparin is able to inhibit the secretion of aldosterone by the adrenal glands, which may lead to the development of hyperkalemia, especially in patients with diabetes mellitus, chronic renal insufficiency, metabolic acidosis, potassium at elevated levels in blood plasma or in patients receiving diuretics, potassium sparing drugs. The risk of developing hyperkalemia increases in proportion to the duration of therapy, but this hyperkalemia, as a rule, is transient. In patients at risk, it is necessary to determine the level of electrolytes in blood plasma before the appointment of beemiparin sodium and monitor it regularly during treatment, especially if the duration of therapy is 7 days.

Use in Pediatrics

Safety and effectiveness of the use of bemiparin in children are not established, therefore, use in pediatrics is not recommended.

Instructions

Bemiparin sodium (Bemiparinum natrium)