Vaxcel Heparin Sodium

Vaxcel Heparin Sodium

heparin

Manufacturer:

Kotra

Distributor:

Fair Deal
Full Prescribing Info
Contents
Heparin sodium.
Description
Each 1-mL solution contains heparin sodium (bovine mucosa) 5000 IU.
It also contains benzyl alcohol 10 mg as preservative.
Action
Pharmacology: Pharmacodynamics: Heparin inhibits reactions that lead to the clotting of blood and the formation of fibrin clots in vitro and in vivo. Heparin acts at multiple sites in the normal coagulation system. Small amounts of heparin in combination with antithrombin III (heparin cofactor) can inhibit thrombosis by inactivating activated Factor X and inhibiting the conversion of prothrombin to thrombin. Clotting time is prolonged by full therapeutic doses of heparin, in most cases, it is not measurably affected by low doses of heparin. Peak plasma levels of heparin are achieved 2-4 hrs following SC administration, although there are considerable individual variations. Heparin does not have fibrinolytic activity, therefore it will not lyse existing clots.
Pharmacokinetics: Heparin is not absorbed from the GIT. It is extensively bound to plasma proteins following IV or SC injection. It does not cross the placenta and not excreted in breast milk. The half-life of heparin depends on the dose and route of administration as well as the method of calculation and is subject to wide inter- and intraindividual variation, a range of 1-6 hrs with an average of 1.5 hrs. It may be slightly prolonged in renal impairment, decreased in patients with pulmonary embolism and either increased or decreased in patients with liver disorder. Heparin is taken up by the reticuloendothelial system. It is excreted in the urine, mainly as metabolites, although, following administration of large doses, up to 50% may be excreted unchanged.
Indications/Uses
Prophylaxis and treatment of venous thrombosis and pulmonary embolism; treatment of myocardial infarction and arterial embolism; prevention of clotting in arterial and heart surgery and prevention of cerebral thrombosis; and as an anticoagulant in blood transfusions, extracorporal circulation, dialysis and for laboratory purposes.
Dosage/Direction for Use
IV Administration: 5,000-10,000 IU every 4 hrs either by bolus injection or continuous infusion in sodium chloride injection or dextrose injection. However, the dose should be monitored with coagulation tests performed just before each administration and varied according to individual response.
The clotting time should be 2-3 times the control value.
SC Administration (Therapeutic Dosage): 10,000 IU may be given every 6 hrs after an initial IV bolus injection of 5,000 IU.
Low-Dose Heparin Prophylaxis: 5,000 IU in 0.2 mL SC, should be given 2-6 hrs preoperatively and every 8-12 hrs postoperatively for 10-14 days or until the patient is mobile, whichever is longer.
Haemodialysis: The dosage must be determined individually, depending on the patients coagulations status and the type of apparatus used.
Myocardial Infarction: 5,000 IU SC every 12 hrs beginning during the 12 hrs following the first sign of myocardial infarction.
Open-Heart Surgery: Operations <2 hrs, 120 IU/kg/hr. For operations of longer duration, 1½ times this dose should be given. For each 450 mL of blood used, 2,000 IU are needed.
Treatment periods vary from 10-14 days in perioperative prophylaxis to as much as 6 weeks in the treatment of established thrombosis.
It is anticipated that heparin will have disappeared from the blood stream 4 hrs after IV injection of 5,000IU and 6-8 hrs after 10,000 IU and 15,000 IU of IV heparin, respectively.
The IM route cannot be recommended because of high incidence of haematoma. The increase in clotting time provided by heparin becomes apparent immediately after administration and last for 4-6 hrs after IV injection and for about 8 hrs after SC injection. Heparin without preservatives should be used in premature infants.
Elderly: Elderly women have a greater tendency to bleed and it may be necessary to reduce the dose according to coagulant tests, but dosage alterations are unlikely for prophylaxis.
Administration: Administered by SC or IV injection or by IV infusion after dilution with a suitable vehicle solution.
Overdosage
Bleeding may be a complication of therapy.
Slight epistaxis, occasional red cells in the urine and bruising are signs of overdosage.
Slight haemorrhage due to overdosage can usually be treated by withdrawing heparin sodium. Severe bleeding may be reduced by the administration of protamine sulphate.
The effect of heparin can be reversed immediately by IV administration of 1% protamine sulphate solution. The injection should be given very slowly (over 1-3 min). The quantity of protamine required for neutralization falls rapidly with the lapse of time after administration of heparin. If given within 15 min of the heparin injection, 10 mg of protamine will neutralize 1,000 IU of heparin, while 30 min after the heparin injection of 1,000 IU, only 5 mg of protamine sulphate is needed. If more time has elapsed after the administration of heparin, the dose of protamine sulphate required for neutralization should be determined accurately by titrating with the patient's plasma.
It is important to avoid overdosage of protamine sulphate because protamine itself has anticoagulant properties.
The dosage should not exceed the equivalent of 50 mg protamine sulphate in any 10-min period. IV injection of protamine may cause a sudden fall in blood pressure, bradycardia, dyspnoea and transitory flushing, but these may be avoided or diminished by slow administration.
Contraindications
Patients known to have hypersensitivity to heparin. It is also contraindicated when suitable blood coagulation tests - eg, the whole blood clotting time, partial thromboplastin time - cannot be performed at the required intervals. There is usually no need to monitor the effect of low dose heparin in patients with normal coagulation parameters. Heparin sodium is contraindicated during any uncontrolled active bleeding state (see Precautions).
Heparin without preservative should be used in premature infants.
Special Precautions
When heparin sodium is administered in therapeutic amounts, its dosage should be regulated by frequent blood coagulation tests. If the coagulation test is unduly prolonged or if haemorrhage occurs, heparin sodium should be discontinued promptly (see Overdosage).
Some of the condition in which increased danger of haemorrhage exists are as follows: Cardiovascular: Subacute bacterial endocarditis, arterial sclerosis, increased capillary permeability; during and immediately following: Spinal tap or spinal anaesthesia or major surgery, especially involving the brain, spinal cord or eye.
Haematologic: Conditions associated with increased bleeding tendencies, eg, haemophilia, some purpuras and thrombocytopenia.
Gastrointestinal (GI) inaccessible ulcerative lesions and continuous tube drainage of the stomach or small intestine. Heparin may prolong the one-stage prothrombin time. Therefore, when heparin sodium is given with dicumarol or warfarin sodium, a period of at least 5 hrs after the last IV dose or 24 hrs after the last SC dose should elapse before blood is drawn if a valid prothrombin time is obtained.
Heparin therapy should be given with caution to patients about to undergo surgery and those with impaired renal or hepatic function.
If oral anticoagulants are started, heparin should be continued in slightly decreasing doses for another 4-5 days until the oral drug has attained full prothrombin depressing activity.
Heparin should be used with caution in any patient with a history of allergy. Before a therapeutic dose is given to such a patient, a trial dose of 1,000 u may be advisable.
Use in pregnancy & lactation: The antithrombotic drug of choice during pregnancy should be heparin, even taking into consideration the fact that long-term (≥6 months) application of heparin can cause severe osteoporosis in the mother. To minimize the risk of osteoporosis, heparin is given in the 1st trimester, followed by coumarin therapy until about the 36th week, and then heparin is given for the last few weeks. Heparin therapy should be completely stopped 6 hrs before delivery.
Heparin does not cross the placental barrier and is not secreted into breast milk.
Use in children: Vaxcel heparin sodium contains benzyl alcohol, its use should be avoided in children <2 years.
Not to be used in neonates.
Use In Pregnancy & Lactation
The antithrombotic drug of choice during pregnancy should be heparin, even taking into consideration the fact that long-term (≥6 months) application of heparin can cause severe osteoporosis in the mother. To minimize the risk of osteoporosis, heparin is given in the 1st trimester, followed by coumarin therapy until about the 36th week, and then heparin is given for the last few weeks. Heparin therapy should be completely stopped 6 hrs before delivery. Heparin does not cross the placental barrier and is not secreted into breast milk.
Side Effects
Transient alopecia and diarrhoea may occur. Thrombocytopenia and osteoporosis with spontaneous fractures have been reported. Febrile or allergic reactions have occasionally been reported.
Drug Interactions
Drugs (eg, acetylsalicylic acid, dextran, phenylbutazone, ibuprofen, indomethacin, dipyridamole and hydroxychloroquine) that interfere with platelet-aggregation reactions may induce bleeding and should be used with caution in patients receiving heparin. It may be necessary to increase doses of heparin in the febrile state.
Digitalis, tetracycline, nicotine or antihistamines may partially counteract the anticoagulant action of heparin sodium. An increased resistance to heparin sodium is frequently encountered in thrombosis, thrombophlebitis, infection with thrombosing tendencies, myocardial infarction, cancer and postsurgical patients.
Storage
Store below 25°C.
If withdrawal of injection solution from the container is performed under aseptic conditions, a vial can be stored over up to 14 days after the first use. The date of first withdrawal must be noted on the label.
Not to be used if solution is not clear.
Shelf-Life: 2 years.
ATC Classification
B01AB01 - heparin ; Belongs to the class of heparin group. Used in the treatment of thrombosis.
Presentation/Packing
Inj (vial) (sterile, clear solution) 25,000 IU/5 mL x 10's.
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