Megaparin

Megaparin Uses, Dosage, Side Effects, Food Interaction and all others data.

Megaparin is a low molecular weight heparin with anticoagulant properties. It acts by enhancing the inhibition rate of activated clotting factors including thrombin and factor Xa through its action on antithrombin III.

This drug has an immediate onset of action. Megaparin 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 subcutaneously 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. Megaparin at 1 mg/kg subcutaneously every 12 hours led to aPTT values of 45 seconds or less in most patients. Average aPTT prolongation time on Day 1 was approximately 16% higher than on Day 4 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.

Trade Name Megaparin
Availability Prescription only
Generic Enoxaparin
Related Drugs amlodipine, aspirin, lisinopril, metoprolol, carvedilol, propranolol, Xarelto, clopidogrel, Eliquis, warfarin
Type Pf Syringe
Protein binding

Enoxaparin binds to antithrombin III. The percentage of plasma protein binding for enoxaparin is not readily available in the literature.

Groups Approved
Therapeutic Class Parenteral anti-coagulants
Manufacturer Venus Remedies Ltd
Available Country India
Last Updated: September 19, 2023 at 7:00 am
Megaparin
Megaparin

Uses

Megaparin is used for:

Treatment of deep vein thrombosis, with or without pulmonary embolism.

Treatment of unstable angina and non-Q-wave myocardial infarction, administered concurrently with aspirin.

Prevention of thrombus formation in the extra-corporal circulation during haemodialysis.

Prophylaxis of venous thromboembolic disease (prevention of blood clot formation in the veins), in particular those which may be associated with orthopedic or general surgery.

Prophylaxis of venous thromboembolic disease in medical patients bedridden due to acute illness, including cardiac insufficiency, respiratory failure, severe infections, rheumatic diseases.

Megaparin is also used to associated treatment for these conditions: Acute Coronary Syndrome (ACS), Acute ST-segment Elevation Myocardial Infarction, Deep Vein Thrombosis, Ischemic complications caused by non-q wave myocardial infarction, Ischemic complications caused by unstable angina, Percutaneous Coronary Intervention (PCI)

How Megaparin works

Megaparin binds to antithrombin III, a serine protease inhibitor, forming a complex that irreversibly inactivates factor Xa, which is frequently used to monitor anticoagulation in the clinical setting. Following factor Xa inactivation, enoxaparin is released and binds to other anti-thrombin molecules. Factor IIa (thrombin) is directly inhibited by enoxaparin, however with less potency than unfractionated heparin (UFH). Due to the cascade of effects resulting from enoxaparin binding, thrombin is unable to convert fibrinogen to fibrin and form a clot, preventing thromboembolic events.

Dosage

Megaparin dosage

Adults:

Prophylaxis of venous thromboembolism: In patients with a low to moderate risk of venous thromboembolism the recommended dosage is 20 mg (2,000 IU) once daily by subcutaneous injection for 7 to 10 days, or until the risk of thromboembolism has diminished. In patients undergoing surgery, the initial dose should be given approximately 2 hours pre-operatively. In patients with a higher risk, such as in orthopaedic surgery, the dosage should be 40 mg (4,000 IU) daily by subcutaneous injection with the initial dose administered approximately 12 hours before surgery.

Prophylaxis of venous thromboembolism in medical patients: The recommended dose of enoxaparin sodium is 40 mg (4,000 IU) once daily by subcutaneous injection. Treatment with enoxaparin sodium is prescribed for a minimum of 6 days and continued until the return to full ambulation, for a maximum of 14 days.

Treatment of venous thromboembolism: Megaparin should be administered subcutaneously as a single daily injection of 1.5 mg/kg (150 IU/kg). Megaparin treatment is usually prescribed for at least 5 days and until adequate oral anticoagulation is established.

Treatment of unstable angina and non-Q-wavemyocardial infarction: The recommended dose is 1 mg/kg Megaparin every 12 hours by subcutaneous injection, administered concurrently with oral aspirin (100 to 325 mg once daily). Treatment with Megaparin in these patients should be prescribed for a minimum of 2 days and continued until clinical stabilisation. The usual duration of treatment is 2 to 8 days.

Treatment of acute ST-segment Elevation Myocardial Infarction: The recommended dose of enoxaparin sodium is a single IV bolus of 30 mg plus a 1mg/kg SC dose followed by 1 mg/kg administered SC every 12 hours (max 100mg for the first two doses only, followed by 1 mg/kg dosing for the remaining doses).

Prevention of extracorporeal thrombus formation during haemodialysis: A dose equivalent to 1 mg/kg (100 IU/kg) introduced into the arterial line at the beginning of a dialysis session is usually sufficient for a 4 hour session. If fibrin rings are found, such as after a longer than normal session, a further dose of 0.5 to 1 mg/kg (50 to 100 IU/kg) may be given. For patients at a high risk of haemorrhage the dose should be reduced to 0.5 mg/kg (50 IU/kg) for double vascular access or 0.75 mg/kg (75 IU/kg) for single vascular access.

Elderly:

For treatment of acute ST-segment Elevation Myocardial Infarction in elderly patients 75 years of age, do not use an initial IV bolus. Initiate dosing with 0.75 mg/kg SC every 12 hours (maximum 75 mg for the first two doses only, followed by 0.75 mg/kg dosing for the remaining doses). For other indications, no dosage adjustments are necessary in the elderly, unless kidney function is impaired.

Children:

Not recommended, as dosage not established.

Side Effects

Haemorrhage (bleeding), Thrombocytopenia, elevations of serum aminotransferase. Pain, bluish marks at injection sites to skin rash at injection sites. Cases of neuraxial hematomas with the concurrent use of Megaparin and spinal/epidural anesthesia or spinal puncture have resulted in varying degrees of neurologic injuries.

Toxicity

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. Megaparin 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.

Precaution

Megaparin injection should not be administered by intramuscular route. Megaparin should be used with caution in conditions with increased potential for bleeding, such as impaired hemostasis, history of peptic ulcer, recent ischemic stroke, uncontrolled severe arterial hypertension, diabetic retinopathy, recent neuro or opthalmologic surgery and low weight patients. It is recommended that the platelet count be measured befored the initiation of the treatment and regularly thereafter during treatment.

Interaction

It is recommended that agents which affect haemostasis should be discontinued prior to enoxaparin therapy unless their use is essential, such as: systemic salicylates, acetylsalicylic acid, NSAIDs including ketorolac, dextran, and clopidogrel, systemic glucocorticoids, thrombolytics and anticoagulants. If the combination cannot be avoided, enoxaparin should be used with careful clinical and laboratory monitoring.

Food Interaction

  • Avoid herbs and supplements with anticoagulant/antiplatelet activity. Examples include garlic, ginger, bilberry, danshen, piracetam, and ginkgo biloba.

Megaparin Hypertension interaction

[Major] Heparin should be used with extreme caution in patients with uncontrolled or severe hypertension as these conditions may predispose the patient to hemorrhage during heparin administration.

Blood coagulation tests (e.g., whole blood clotting time, activated partial thromboplastin time) should be performed at appropriate intervals during full-dose heparin administration.

In addition, periodic platelet counts, hematocrits, and tests for occult blood in stool are recommended during the entire course of heparin therapy.

Clinical monitoring of blood pressure is recommended.

Hypertension interaction

[Moderate] Anticoagulants should be used with extreme caution in patients at increased risk for hemorrhage, including those patients with severe hypertension.

Volume of Distribution

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

Elimination Route

Mean absolute bioavailability of enoxaparin, after 1-2 mg/kg given subcutaneously 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 to 5 hours after a subcutaneous injection. A 30 mg IV bolus preceding an immediate 1 mg/kg SC 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. The AUC under the thrombin generation curve was 305 +/- 48.

Half Life

The half-life of enoxaparin is about 4 hours after a single dose administered subcutaneously and about 7 hours after several doses. One source mentions a half-life ranging from 1 hour to 4.5 hours.

Clearance

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

Elimination Route

Megaparin 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.

Pregnancy & Breastfeeding use

Pregnancy category B. In humans, there is no evidence that Megaparin crosses the placental barrier Megaparin should be used during pregnancy only if the physician has established a clear need. Megaparin is not recommended for use in pregnant women with prosthetic heart valves.

Lactation: It is not known whether this drug is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when Megaparin injection is administered to nursing women.

Contraindication

Hyper-sensitivity to either Megaparin, heparin or other low molecular weight heparins; major clotting disorders like history of thrombocytopenia, active gastro-intestinal ulcer or organic lesion likely to bleed, recent haemorrhagic vascular cerebral stroke. Although rare, cutaneous or systemic allergic reactions may occur.

Special Warning

Dose in Renal Impairment: Although no dosage adjustment is recommended in patients with moderate (creatinine clearance: 30-50 ml/min) and mild (creatinine clearance: 50-80 ml/min) renal impairment, all such patients should be observed carefully for signs and symptoms of bleeding. For patients with severe (creatinine clearance <30 ml/min) renal impairment, following dosage adjustments are recommended: Prophylactic dose ranges: 2000 anti Xa IU once daily; Therapeutic dose ranges: 100 anti-Xa lU/kg once daily.

Dose in Hepatic Impairment: Caution should be used in hepatically impaired patients.

Acute Overdose

Accidental overdosage following administration of Megaparin may lead to hemorrhagic complications. Injected Megaparin may be largely neutralized by the slow i.v. injection of protamine sulfate (1% solution) The dose of protamine sulfate should be equal to the dose of Megaparin injected: 1 mg protamine sulfate should be administered to neutralize 1 mg Megaparin.

Storage Condition

Store below 25° C. Do not freeze. Keep out of the reach of children.

Innovators Monograph

You find simplified version here Megaparin

Megaparin contains Enoxaparin see full prescribing information from innovator Megaparin Monograph, Megaparin MSDS, Megaparin FDA label

FAQ

What is Megaparin used for?

Megaparin is used to prevent deep venous thrombosis, a condition in which harmful blood clots form in the blood vessels of the legs. These blood clots can travel to the lungs and can become lodged in the blood vessels of the lungs, causing a condition called pulmonary embolism.  It is also used in those with acute coronary syndrome and heart attacks.

How safe is Megaparin?

This could lead to serious problems, such as a stroke or death. Extra care is needed because Megaparin is a high-alert medicine. High-alert medicines have been proven to be safe and effective. But these medicines can cause serious injury if a mistake happens while taking them. Megaparin injectable solution is used for short-term treatment. It comes with risks if you don't take it as prescribed. If you stop taking the drug suddenly or don't take it at all: You'll have a higher risk for a blood clot.

How does Megaparin work?

Megaparin works by blocking the body's natural clotting factors. This makes your blood less likely to form dangerous clots. It keeps clots you do have from getting bigger.

What are the common side effects of Megaparin?

Common side effects of Megaparin are include:

  • Bruising
  • chest discomfort
  • collection of blood under the skin
  • confusion
  • continuing bleeding or oozing from the nose and/or mouth, or surgical wound
  • convulsions (seizures)
  • fever
  • irritability
  • lightheadedness
  • lower back pain
  • pain or burning while urinating
  • swelling of the hands or feet
  • tightness in the chest
  • uncontrolled bleeding at the site of injection
  • vomiting of blood or material that looks like coffee grounds
  • wheezing

Is Megaparin safe during pregnancy?

Megaparin does not cross the placenta and is safe for the fetus. This Megaparin should be used during pregnancy only if clearly needed.

Is Megaparin safe during breastfeeding?

Safe During Breastfeeding: You will pass enoxaparin into breast milk, but the impact on the fetus is not thought to be harmful.

Can I drink alcohol with Megaparin?

Alcohol isn't safe to use as a blood thinner. Limit alcohol while taking this drug because it may increase the risk of stomach bleeding.

Can I drive after taking Megaparin?

Yes, you can drive.

Does Megaparin work immediately?

Megaparin works fairly quickly when used to prevent blood clots from forming.

When should not take Megaparin?

You should not use Megaparin if you are allergic to Megaparin, heparin, benzyl alcohol, or pork products, or if you have: active or uncontrolled bleeding; or. if you had decreased platelets in your blood after testing positive for a certain antibody while using Megaparin within the past 100 days.

What happens if I miss a dose?

If you miss a dose of Megaparin, inject it as soon as you remember. If it is too near the next dose, skip the missed dose and go back to your usual dosing times. Do not double dose.

What happen if I overdose on Megaparin?

You could have dangerous levels of the drug in your body. This could lead to bleeding. Symptoms of an overdose of this drug can include: abdominal pain. Seek emergency medical attention. Overdose may cause excessive bleeding.

What happen If I suddenly stop taking Megaparin?

If you stop taking the Megaparin suddenly or don't take it at all: You'll have a higher risk for a blood clot. This could lead to serious problems, such as a stroke or death. Take this Megaparin on the schedule set by your doctor. Don't stop taking it without speaking with your doctor first.

How long does Megaparin take to work?

Megaparin starts to work within 2 hours and the effects last up to 12 hours.

How long does Megaparin stay in my system?

Megaparin has a half-life of around 4.5 to 7 hours after administration, and its anticoagulant effects last up to 12 hours. Because of its long half-life and predictable effects, Megaparin does not need extensive monitoring or supervision to use it.

Can Megaparin affect my kidney?

A disadvantage of Megaparin is reliance on kidney function for excretion and potential accumulation of its anticoagulant effect in patients with declining renal function.

Can Megaparin affects my liver?

Megaparin induced hepatotoxicity is an under-recognized adverse effect and one that, if monitored, might prevent possible hepatic injury and reduce the amount of invasive workups usually prompted by deranged liver function tests.

Can Megaparin affects my heart ?

Blood clots are dangerous because they can lead to serious blockages in your blood vessels. This can cause a stroke or a heart attack.

Can Megaparin be given with food?

Medicines can interact with certain foods. In some cases, this may be harmful and your doctor may advise you to avoid certain foods. In the case of Megaparin, there are no specific foods that you must exclude from your diet when receiving Megaparin.

Does Megaparin affect blood pressure?

Taking this drug puts you at high risk for hemorrhage (severe, life-threatening bleeding). For people with high blood pressure: This Megaparin can cause bleeding. If you have high blood pressure that isn't controlled, you're at high risk for hemorrhage (severe, life-threatening bleeding).

Does Megaparin make me tired?

Mild irritation, pain, bruising, redness, and swelling at the injection site may occur. Fatigue or fever may also occur.

*** Taking medicines without doctor's advice can cause long-term problems.
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