THERANOX

Enoxaparin is a common low-molecular-weight heparin (LMWH) used in the prevention and management of various thromboembolic disorders.

Initially approved by the

FDA in 1993, it is administered by a subcutaneous or intravenous injection and marketed by several pharmaceutical companies.

Enoxaparin markedly reduces the incidence of venous thromboembolism in hospitalized patients when compared to unfractionated heparin, without increasing the risk of serious bleeding. 5, 7.

Enoxaparin is indicated for the prevention of ischemic complications in unstable angina and in non Q-wave myocardial infarction; it is indicated in conjunction with percutaneous intervention and/or other treatment for the management of acute ST elevation myocardial infarction.

Enoxaparin is also indicated in the prophylaxis of DVT in abdominal surgery, hip replacement, knee replacement, or medical patients with severely restricted mobility during acute illness.

Additionally, enoxaparin is indicated for the inpatient treatment of DVT with or without pulmonary embolism and the treatment of outpatient DVT without pulmonary embolism.

This drug has an immediate onset of action.

Enoxaparin increases Thrombin

Time (TT) and activated partial thromboplastin time (aPTT), preventing and reducing thromboembolic complications such as DVT, pulmonary embolism, and ischemic cardiac complications.

Administered at 1.5 mg/kg Subcutaneous in a pharmacodynamic study, enoxaparin led to a higher ratio of anti-Factor Xa to anti-Factor IIa activity (mean ±SD, 14.0±3.1) (based on areas under anti-Factor activity versus time curves) when compared to that of heparin (mean ±SD, 1.22±0.13).

Increases in the

TT and aPTT were 1.8 times those of the control group.

Enoxaparin at 1 mg/kg Subcutaneous every 12 hours led to aPTT values of 45 seconds or less in most patients.

Average aPTT prolongation time on

Day was approximately 16% higher than on Day of enoxaparin therapy.

Caution is advised during treatment with enoxaparin.

• the risk of hemorrhage and thrombocytopenia is increased.

In pregnant women with prosthetic mechanic heart valves, the risk of thromboembolism is increased.

Mean absolute bioavailability of enoxaparin, after 1-2 mg/kg given Subcutaneous is approximately 100% in healthy volunteers.

The absorption of enoxaparin is proportional to the dose, demonstrating linear absorption.

The average maximum plasma anti-Xa activity is reached 3-5 hours after a subcutaneous injection. 9, 13 A 30 mg Intravenous bolus preceding an immediate 1 mg/kg Subcutaneous every twice a day led to maximum anti-Factor Xa levels of 1.16 IU/mL.

Steady-state is reached within 3-4 days of treatment with a Cmax of 1.2 IU/mL.

AUC under the thrombin generation curve was 305 +/.

The volume of distribution of enoxaparin is approximately 4-5 L, similar to normal blood volume. 11, 13.

Enoxaparin is mainly metabolized by the liver via desulfation and/or depolymerization to lower and less potent molecular weight metabolites. 11, 13.

Enoxaparin is mainly excreted by the kidneys.

Renal clearance of active fragments represents about 10% of the administered dose and total renal excretion of active and non-active fragments 40% of the dose.

The half-life of enoxaparin is about 4 hours after a single dose administered Subcutaneous and about 7 hours after several doses.

One source mentions a half-life ranging from 1 hour to 4.5 hours.

The mean clearance of enoxaparin is 0.74 L/h after a 1.5 mg/kg intravenous infusion over 6 hours 13; clearance of enoxaparin is significantly decreased in patients with severe renal impairment.

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The oral

LD50 for enoxaparin in mice is >5000 mg/kg; the subcutaneous LD50 of enoxaparin in mice is >2500 mg/kg.

Accidental overdose after the administration of enoxaparin may cause hemorrhage.

Enoxaparin administered by injection is mainly neutralized by gradual intravenous injection of a 1% protamine sulfate solution.

The dose of protamine sulfate should be equal to the dose of enoxaparin administered: 1 mg protamine sulfate for 1 mg enoxaparin, of enoxaparin was administered in the previous 8 hours.

If a minimum of 12 hours has passed since the last enoxaparin dose, protamine may not be necessary; it is important to avoid an overdose with protamine, as fatal reactions may occur.