Fraxiparine solution for injections 5700me syringe 0,6ml N10
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Active ingredients
Calcium Nadroparin
Release form
Solution
Composition
Active ingredient: Nadroparin calcium Concentration of active ingredient (unit): 5700 ME
Pharmacological effect
Nadroparin calcium is a low molecular weight heparin (LMWH), obtained by depolymerization from standard heparin, is a glycosaminoglycan with an average molecular weight of 4300 daltons. Shows a high ability to bind to the blood plasma protein antithrombin III (AT III). This binding leads to accelerated inhibition of factor Xa, and this is due to the high antithrombotic potential of nadroparin. Other mechanisms that provide the antithrombotic effect of nadroparin include activation of a tissue factor conversion inhibitor (TFPI), activation of fibrinolysis by direct release of a tissue plasminogen activator from endothelial cells and modification of rheological properties blood (decrease in blood viscosity and increase in the permeability of platelet and granulocyte membranes). Nadroparin calcium It is characterized by higher anti-Xa factor activity compared to anti-IIa factor or antithrombotic activity and has both immediate and prolonged antithrombotic activity. Compared with unfractionated heparin, nadroparin has a lower effect on platelet function and aggregation and a slight effect on primary hemostasis . At prophylactic doses, nadroparin does not cause a pronounced decrease in aPTT. During a course of treatment during the period of maximum activity, an increase in the APTT to the value of I, 1.4 times the standard. Such prolongation reflects the residual antithrombotic effect of nadroparin calcium.
Pharmacokinetics
Pharmacokinetic properties are determined on the basis of changes in plasma anti-Xa-factor activity. Absorption After subcutaneous injection of Cmax in the blood plasma is reached in 3-5 hours, suproparin is absorbed almost completely (about 88%). With intravenous administration, the maximum anti-Xa activity is achieved in less than 10 minutes, T1 / 2 is about 2 hours. Metabolism Metabolized mainly in the liver by desulfation and depolymerization. Output After subcutaneous injection of T1 / 2 is about 3.5 hours.However, anti-Xa activity persists for at least 18 hours after an injection of nadroparin at a dose of 1900 anti-Xa ME. Pharmacokinetics in special clinical situations in elderly patients due to physiological deterioration of renal function, elimination of nadroparin slows down. Possible renal failure in this group of patients requires an assessment and appropriate dose adjustment. In clinical studies of the pharmacokinetics of nadroparin when i / v administration to patients with renal insufficiency of varying severity, a correlation was established between clearance of nadroparin and creatinine clearance. When comparing the values obtained with those in healthy volunteers, it was found that AUC and T1 / 2 in patients with mild renal insufficiency (CC 36-43 ml / min) were increased to 52% and 39%, respectively, and plasma clearance of nadroparin was reduced to 63% of normal values. In patients with severe renal failure (CK 10–20 ml / min), AUC and T1 / 2 were increased to 95% and 112%, respectively, and the plasma clearance of nadroparin was reduced to 50% of normal values. In patients with severe renal failure (CK 3–6 ml / min) and on hemodialysis, AUC and T1 / 2 were increased to 62% and 65%, respectively, and plasma clearance of nadroparin was reduced to 67% of normal values. Results of the study showed that a small accumulation of nadroparin can be observed in patients with mild to moderate renal insufficiency (CC ≥ 30 ml / min and <60 ml / min). Therefore, Fraxiparine should be reduced by 25% in patients receiving Fraxiparine to treat thromboembolism, unstable angina / myocardial infarction without a Q wave. Patients with severe renal insufficiency are contraindicated in patients with moderate or moderate renal insufficiency. degree when using Fraxiparine to prevent thromboembolism, the accumulation of nadroparin does not exceed that in patients with normal renal function, taking Fraxiparine in l therapeutic doses. When using Fraxiparine for the prevention of dose reduction in this category of patients is not required. In patients with severe renal insufficiency who receive Fraxiparine in prophylactic doses, a dose reduction of 25% is necessary. Low molecular weight heparin is injected into the arterial dialysis loop in high enough doses to prevent blood from clotting in the dialysis loop.Pharmacokinetic parameters are not fundamentally changed, except in the case of overdose, when the passage of the drug into the systemic circulation can lead to an increase in anti-Xa factor activity, due to the final phase of renal failure.
Indications
- prevention of thromboembolic complications (with surgical and orthopedic interventions; in patients with a high risk of thrombus formation in acute respiratory and / or heart failure under conditions of ICU); - treatment of thromboembolism; - prevention of blood coagulation during hemodialysis; Q wave.
Contraindications
history of thrombocytopenia with nadroparin, signs of bleeding or an increased risk of bleeding associated with impaired hemostasis (except for DIC, not caused by heparin); organic diseases with a tendency to bleeding (for example, acute gastric or duodenal ulcer); trauma or surgery on the brain and spinal cord or on the eyes; intracranial hemorrhage; acute septic endocarditis; severe renal failure (CC <30 ml / min) in patients receiving Fraxiparine for the treatment of thromboembolism, unstable angina and myocardial infarction without a Q wave; childhood and adolescence (up to 18 years); hypersensitivity to nadroparin or any other components of the drug. With caution, Fraxiparine should be prescribed in situations associated with an increased risk of bleeding: in liver failure, in renal failure, in severe hypertension, anamnesis of peptic ulcers or other diseases with an increased risk of bleeding, in violation of blood circulation in the choroid and retina, in the postoperative period after operations on tin and spinal cord or in the eyes, in patients with a body weight less than 40 kg, with a duration of therapy exceeding the recommended (10 days), in case of non-compliance with the recommended treatment conditions (especially increasing the duration and dose for a course of use), when combined with drugs, increase the risk of bleeding ..
Precautionary measures
If there is a history of heparin-induced thrombocytopenia (with normal or low molecular weight heparins), Fraxiparine may be administered if necessary. However, in this situation, strict clinical monitoring and, at a minimum, daily measurement of platelet count are shown. If thrombocytopenia occurs, use of Fraxiparine should be immediately discontinued. If tharbocytopenia occurs on the background of heparins (normal or low molecular weight), then the possibility of prescribing anticoagulants of other groups should be considered. If other drugs are not available, it is possible to use another low molecular weight heparin. It should daily monitor the number of platelets in the blood. If signs of initial thrombocytopenia continue to be observed after replacement of the drug, then treatment should be stopped as soon as possible.
Use during pregnancy and lactation
Currently, there are only limited data on the penetration of nadroparin through the placental barrier in humans. Therefore, the use of Fraxiparine during pregnancy is not recommended, except in cases where the potential benefit to the mother exceeds the risk to the fetus. Currently, there are only limited data on the release of nadroparin with breast milk. In this regard, the use of nadroparin during lactation (breastfeeding) is not recommended. In experimental animal studies, no teratogenic effect of nadroparin calcium was detected.
Dosage and administration
When s / c administration, it is preferable to administer the drug in the patient's position, in the s / c tissue of the anterolateral or posterolateral surface of the abdomen, alternately on the right and left side. An introduction to the thigh is allowed. In order to avoid loss of the drug when using syringes, you should not remove air bubbles before injection. Needle should be inserted perpendicular, rather than at an angle, into a pinched skin fold formed between the thumb and index finger. The fold should be maintained throughout the entire period of drug administration. Do not rub the injection site after the injection.
Side effects
On the part of the blood coagulation system: very often - bleeding from various sites,more often in patients with other risk factors. From the hematopoietic system: rarely - thrombocytopenia; very rarely - eosinophilia, reversible after discontinuation of the drug. From the digestive system: often - increased activity of hepatic transaminases (usually transient). Allergic reactions: very rarely - angioedema, skin reactions. Local reactions: very often - formation of a small subcutaneous hematoma in injection site; in some cases, there is the appearance of dense nodules (not meaning encapsulation of heparin), which disappear after a few days; very rarely, skin necrosis, usually at the injection site. Necrosis is usually preceded by purpura or an infiltrative or painful erythematous spot, which may or may not be accompanied by general symptoms (in such cases, treatment with Fraxiparine should be stopped immediately). in patients at risk).
Overdose
Symptoms: The main symptom of an overdose is bleeding; it is necessary to monitor the number of platelets and other parameters of the blood coagulation system. Treatment: minor bleeding does not require special therapy (it is usually enough to reduce the dose or postpone the subsequent administration). Protamine sulfate has a pronounced neutralizing effect on the anticoagulant effects of heparin, but in some cases, anti-Xa activity may partially recover. The use of protamine sulfate is necessary only in severe cases. Note that 0.6 ml of protamine sulfate neutralizes about 950 anti-Xa ME nadroparin. The dose of protamine sulfate is calculated taking into account the time elapsed after the administration of heparin, with a possible reduction in the dose of the antidote.
Interaction with other drugs
The risk of developing hyperkalemia increases with the use of Fraxiparine in patients receiving potassium salts, potassium-sparing diuretics, ACE inhibitors, angiotensin II receptor antagonists, NSAIDs, heparins (low molecular weight or unfractionated), cyclosporine and tacrolimus, trimethoprim.parapiparas, and heparin. such as acetylsalicylic acid and other NSAIDs, vitamin K antagonists, fibrinolytics and dextran. Platelet aggregation inhibitors (other than acetylsalicylic acid as nalgeziruyuschego and antipyretic drug, i.e.at a dose of more than 500 mg; NSAIDs): abciximab, acetylsalicylic acid as an antiplatelet agent (i.e. at a dose of 50-300 mg) for cardiological and neurological indications, beraprost, clopidogrel, eptifibatid, iloprost, ticlopidine, tirofiban increase the risk of bleeding.
special instructions
Particular attention should be paid to specific instructions for use for each drug belonging to the class of low molecular weight heparins, since they can be used in various dosage units (U or mg). Because of this, the alternation of Fraxiparine with other LMWH with long-term treatment is unacceptable. You also need to pay attention to what kind of drug is used - Fraxiparine or Fraxiparine Forte, because This affects the dosing regimen. Graduated syringes are designed to adjust the dose depending on the patient's body weight. Fraxiparine is not intended for intramuscular administration. Since there is a possibility of thrombocytopenia (heparin-induced thrombocytopenia) when using heparins, Fraxiparine is necessary during the entire course of treatment. monitor platelet count. It was reported rare cases of thrombocytopenia, sometimes severe, which could be associated with arterial or venous thrombosis, which is important to consider in the following cases: for thrombocytopenia; with a significant decrease in platelet levels (by 30-50% compared with normal rates); with the negative dynamics of the thrombosis, about which the patient receives treatment; with DIC syndrome. In these cases, treatment with Fraxiparine should be discontinued. Thrombocytopenia is immuno-allergic in nature and usually occurs between the 5th and 21st days of therapy, but may occur earlier if the patient has a history of heparin-induced thrombocytopenia. It is necessary to remember that control of platelet aggregation based on in vitro tests, is of limited value in the diagnosis of heparin-induced thrombocytopenia. In elderly patients, before starting therapy with Fraxiparine, it is necessary to evaluate kidney function. Heparins suppress aldosterone secretion, which can lead to hyperkalemia, especially in patients with elevated levels of potassium in the blood or in patients at risk for developing hyperkalemia (in diabetes mellitus, chronic renal failure, metabolic acidosis, or with the simultaneous use of drugs that can cause hyperkalemia, during long-term therapy).In patients with an increased risk of hyperkalemia, the level of potassium in the blood should be monitored. The risk of spinal / epidural hematomas increases in patients with established epidural catheters or with the concomitant use of other drugs that affect hemostasis (NSAIDs, antiplatelet agents, other anticoagulants). The risk is also likely to increase with traumatic or repeated epidural or spinal punctures. The question of the combined use of neuroaxial blockade and anticoagulants should be decided individually, after evaluating the effectiveness / risk ratio. In patients who already receive anticoagulants, the need for spinal or epidural anesthesia should be justified. In patients who are planning elective surgical intervention using spinal or epidural anesthesia, the need to introduce anticoagulants should be justified. If a patient is undergoing lumbar puncture or spinal or epidural anesthesia, a sufficient time interval between the administration of Fraxiparine and the introduction or removal of a spinal / epidural catheter or needle should be observed. Careful monitoring of the patient is necessary to identify signs and symptoms of neurological disorders. When violations are found in the patient’s neurological status, urgent appropriate therapy is required. When preventing or treating venous thromboembolism, as well as preventing blood coagulation in the extracorporeal circulation during hemodialysis, it is not recommended to co-administer Fraxiparine with drugs such as acetylsalicylic acid, other salicylates, NSAIDs, and anti-antagents with anti-inflammatory drugs, such as acetylsalicylic acid, other salicylates, NSAIDs, and anti-antagens, and anti-antagents with anti-antagens and anti-antagens. because this may increase the risk of bleeding. Fraxiparine should be used with caution in patients receiving oral anticoagulants, GCS for systemic use and dextrans. When oral anticoagulants are prescribed to patients receiving Fraxiparine, its use should be continued until the prothrombin time is stabilized to the desired value. Effect on the ability to drive vehicles and control mechanisms There is no data on the effect of Fraxiparine on the ability to drive a car or other mechanisms.