Heparin

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

Heparin inhibits reactions that lead to the clotting of blood and the formation of fibrin clots both 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. Once active thrombosis has developed, larger amounts of heparin can inhibit further coagulation by inactivating thrombin and preventing the conversion of fibrinogen to fibrin. Heparin also prevents the formation of a stable fibrin clot in inhibiting the activation of the fibrin stabilizing factor.

Bleeding time is usually unaffected by heparin. Clotting time is prolonged by full therapeutic doses of heparin; in most cases, it is not measurably affected by low doses of heparin.

Unfractionated heparin is a highly acidic mucopolysaccharide formed of equal parts of sulfated D-glucosamine and D-glucuronic acid with sulfaminic bridges. The molecular weight ranges from 3000 to 30,000 daltons. Heparin is obtained from liver, lung, mast cells, and other cells of vertebrates. Heparin is a well-known and commonly used anticoagulant which has antithrombotic properties. Heparin inhibits reactions that lead to the clotting of blood and the formation of fibrin clots both in vitro and in vivo. Small amounts of heparin in combination with antithrombin III, a heparin cofactor,) can inhibit thrombosis by inactivating Factor Xa and thrombin. Once active thrombosis has developed, larger amounts of heparin can inhibit further coagulation by inactivating thrombin and preventing the conversion of fibrinogen to fibrin. Heparin also prevents the formation of a stable fibrin clot by inhibiting the activation of the fibrin stabilizing factor. Heparin prolongs several coagulation tests. Of all the coagulation tests, activated partial prothrombin time (aPTT) is the most clinically important value.

Trade Name Heparin
Availability Prescription only
Generic Heparin
Heparin Other Names Eparina, Heparina, Heparine, Heparinic acid, Heparinum, Unfractionated heparin
Related Drugs amlodipine, aspirin, lisinopril, metoprolol, carvedilol, propranolol, Xarelto, Eliquis, warfarin, atenolol
Weight 2500iu/ml, , 5000iuperml
Type Injection (gland Pharma), Injection, Solution, Concentrate, Intravenous Kit, Intravenous Solution, Flush
Protein binding

Very high, mostly to low-density lipoproteins. It is also extensively bound by globulins and fibrinogens.

Groups Approved, Investigational
Therapeutic Class Parenteral anti-coagulants
Manufacturer Gland Pharma Limited, Panpharma Uk Ltd, Drug Pharm (pvt) Ltd, , Pratapa Nirmala
Available Country India, United Kingdom, Australia, Pakistan, United States, Indonesia
Last Updated: September 19, 2023 at 7:00 am
Heparin
Heparin

Uses

Heparin sodium is used for:

Atrial fibrillation with embolization:

  • Treatment of acute and chronic consumption coagulopathies (disseminated intravascular coagulation);
  • Prevention of clotting in arterial and heart surgery;
  • Anticoagulant therapy in prophylaxis and treatment of venous thrombosis and its extension;
  • (In a low-dose regimen) for prevention of postoperative deep venous thrombosis and pulmonary embolism in patients undergoing major abdomino-thoracic surgery or who for other reasons are at risk of developing thromboembolic disease
  • Prophylaxis and treatment of pulmonary embolism;
  • Prophylaxis and treatment of peripheral arterial embolism.

Heparin is also used to associated treatment for these conditions: Blunt Injuries, Clotting, Coagulopathy, Consumption, Contusions, Disseminated Intravascular Coagulation (DIC), External Hemorrhoid, Inflammation, Inflammatory, non-infectious pruritic dermatosis, Interstitial Cystitis, Pulmonary Embolism, ST Elevation Myocardial Infarction (STEMI), Sprains, Thromboembolism, Thrombosis, Venous, Unstable Angina Pectoris, Venous Thromboembolism, Embolization, Hematomas, Peripheral arterial embolism, Varicosities of the great saphenous vein, Maintenance of patency of IV injection devices

How Heparin works

Under normal circumstances, antithrombin III (ATIII) inactivates thrombin (factor IIa) and factor Xa. This process occurs at a slow rate. Administered heparin binds reversibly to ATIII and leads to almost instantaneous inactivation of factors IIa and Xa The heparin-ATIII complex can also inactivate factors IX, XI, XII and plasmin. The mechanism of action of heparin is ATIII-dependent. It acts mainly by accelerating the rate of the neutralization of certain activated coagulation factors by antithrombin, but other mechanisms may also be involved. The antithrombotic effect of heparin is well correlated to the inhibition of factor Xa. Heparin is not a thrombolytic or fibrinolytic. It prevents progression of existing clots by inhibiting further clotting. The lysis of existing clots relies on endogenous thrombolytics.

Dosage

Heparin dosage

Intravenous-Prophylaxis of re-occlusion of the coronary arteries following thrombolytic therapy in myocardial infarction

  • Adult: 60 U/kg (max: 4,000 U) or a bolus of 5,000 U if streptokinase was used, followed by 12 U/kg/hr (max: 1,000 U/hr) w/ a treatment duration of 48 hr.

Intravenous-

Peripheral arterial embolism, Unstable angina, Venous thromboembolism

  • Adult: 75-80 U/kg or 5,000 U (10,000 U in severe pulmonary embolism) IV loading dose followed by 18 U/kg or 1,000-2,000 U/hr continuous infusion. Alternatively, intermittent inj of 5,000-10,000 U 4-6 hrly.
  • Child: 50 U/kg loading dose, followed by an infusion of 15-25 U/kg/hr.
  • Elderly: Lower dosages may be required.

Subcutaneous-

Prophylaxis of postoperative venous thromboembolism

  • Adult: 5,000 U given 2 hr before surgery then 8-12 hrly for 7 days or until the patient is ambulant.

Subcutaneous-

Venous thromboembolism

  • Adult: 15,000-20,000 U 12 hrly or 8,000-10,000 U 8 hrly.
  • Child: 250 U/kg bid.
  • Elderly: Lower dosages may be required.

Side Effects

Hypersensitivity reactions (e.g. chills, fever, urticaria, asthma, rhinitis); painful, ischaemic and cyanosed limbs; osteoporosis (in long-term admin), suppression of aldosterone synthesis leading to hyperkalaemia, cutaneous necrosis, delayed transient alopecia, priapism, rebound hyperlipaemia; increased serum concentrations of AST and ALT, prolonged prothrombin time; local irritation, erythema, mild pain, haematoma or ulceration on inj site.

Toxicity

In mouse, the median lethal dose is greater than 5000 mg/kg. Another side effect is heparin-induced thrombocytopenia (HIT syndrome). Platelet counts usually do not fall until between days 5 and 12 of heparin therapy. HIT is caused by an immunological reaction that makes platelets form clots within the blood vessels, thereby using up coagulation factors. It can progress to thrombotic complications such as arterial thrombosis, gangrene, stroke, myocardial infarction and disseminated intravascular coagulation. Symptoms of overdose may show excessive prolongation of aPTT or by bleeding, which may be internal or external, major or minor. Therapeutic doses of heparin give for at least 4 months have been associated with osteoporosis and spontaneous vertebral fractures. Osteoporosis may be reversible once heparin is discontinued. Although a causal relationship has not been established, administration of injections preserved with benzyl alcohol has been associated with toxicity in neonates. Toxicity appears to have resulted from administration of large amounts (i.e., about 100–400 mg/kg daily) of benzyl alcohol in these neonates. Its use is principally associated with the use of bacteriostatic 0.9% sodium chloride intravascular flush or endotracheal tube lavage solutions.

Precaution

Patient with increased risk of bleeding complications, HTN, DM, pre-existing metabolic acidosis. Do not use in catheter lock flushing. Hepatic and renal impairment. Elderly. Pregnancy and lactation.

Interaction

Enhanced anticoagulant effect with other drugs affecting platelet function or the coagulation system (e.g. platelet aggregation inhibitors, thrombolytic agents, salicylates, NSAIDs, vit K antagonists, dextrans, activated protein C). Decreased anticoagulant effect with gyceryl trinitrate infusion. Increased risk of hyperkalaemia with ACE inhibitors or angiotensin II antagonists.

Food Interaction

  • Administer calcium supplement. This drug decreases calcium levels.
  • Avoid herbs and supplements with anticoagulant/antiplatelet activity. Examples include garlic, ginger, bilberry, danshen, piracetam, and ginkgo biloba.

Heparin 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.

Volume of Distribution

40-70 mL/min (approximately the same as blood volume) Although heparin does not distribute into adipose tissues, clinicians should use actual body weight in obese patients to account for extra vasculature.

Elimination Route

Heparin must be given parenterally as it is not absorbed through the gastrointestinal mucosa. It is usually given by iv infusion or deep sc injection. The onset of action is immediate after iv injection but can be delayed 20 to 60 minutes following sc injection.

Plasma heparin concentrations may be increased and activated partial thromboplastin times (aPTTs) may be more prolonged in geriatric adults (older than 60 years of age) compared with younger adults.

Half Life

1.5 hours.

The plasma half-life of heparin increases from about 60 minutes with a 100 unit/kg dose to about 150 minutes with a 400 unit/kg dose.

Clearance

Adult Clearance = 0.43 ml/kg/min 25-28 weeks gestation = 1.49 ml/kg/min

Elimination Route

The drug appears to be removed mainly by the reticuloendothelial system. A small fraction of unchanged heparin also appears to be excreted in urine. Heparin cannot be eliminated by hemodialysis.

Pregnancy & Breastfeeding use

Pregnancy Category C. Either studies in animals have revealed adverse effects on the foetus (teratogenic or embryocidal or other) and there are no controlled studies in women or studies in women and animals are not available. Drugs should be given only if the potential benefit justifies the potential risk to the foetus.

Nursing Mothers: Due to its large molecular weight, heparin is not likely to be excreted in human milk, and any heparin in milk would not be orally absorbed by a nursing infant. Benzyl alcohol present in maternal serum is likely to cross into human milk and may be orally absorbed by a nursing infant. Exercise caution when administering Heparin Sodium Injection to a nursing mother.

Contraindication

Current or history of heparin-induced thrombocytopenia; generalised or local haemorrhagic tendency, including uncontrolled severe HTN, severe liver insufficiency, active peptic ulcer, acute or subacute septic endocarditis, intracranial haemorrhage or injuries and operations on the CNS, eyes and ears, and in women with abortus imminens; epidural anaesth during birth; locoregional anaesth in elective surgical procedures (in patients receiving heparin for treatment rather than prophylaxis).

Special Warning

Pediatric Use: There are no adequate and well controlled studies on heparin use in pediatric patients. Pediatric dosing recommendations are based on clinical experience. Carefully examine all Heparin Sodium Injection vials to confirm choice of the correct strength prior to administration of the drug. Pediatric patients, including neonates, have died as a result of medication errors in which vials have been confused with “catheter lock flush” vials

Acute Overdose

Symptoms: Bleeding (nose bleeds, blood in urine or tarry stools may be noted as the 1st sign of bleeding).

Management: May give protamine sulfate by slow IV infusion over 10 min to treat severe bleeding (1 mg of protamine sulfate neutralises approx 100 U of heparin). Max: 50 mg as a single dose.

Storage Condition

Store between 20-25° C. Protect from freezing.

Innovators Monograph

You find simplified version here Heparin

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

FAQ

What is Heparin used for?

Heparin is used to decrease the clotting ability of the blood and help prevent harmful clots from forming in blood vessels. This medicine is sometimes called a blood thinner, although it does not actually thin the blood. Specifically it is also used in the treatment of heart attacks and unstable angina.

How safe is Heparin?

Heparin comes with serious risks if you don't take it as prescribed. Unfractionated Heparin has been classified as a high-alert drug by the Institute for Safe Medication Practices.

How does Heparin work?

Heparin acts as an anticoagulant, preventing the formation of clots and extension of existing clots within the blood.

What are the common side effects of Heparin?

Common side effects of Heparin are include:

  • Abdominal or stomach pain or swelling
  • back pain or backaches
  • bleeding from the gums when brushing teeth
  • blood in the urine
  • constipation
  • coughing up blood
  • dizziness
  • headaches, severe or continuing
  • heavy bleeding or oozing from cuts or wounds
  • joint pain, stiffness, or swelling
  • menstrual bleeding, unexpected or unusually heavy
  • unexplained bruising or purplish areas on the skin
  • unexplained nosebleeds
  • vomiting of blood or material that looks like coffee grounds

Is Heparin safe during pregnancy?

Unfractionated Heparin and low molecular weight Heparin do not cross the placenta and are safe for the fetus, but long-term treatment with UFH is problematic because of its inconvenient administration, the need to monitor anticoagulant activity and because of its potential side effects, such as Heparin-induced.

Is Heparin safe during breastfeeding?

Heparin low molecular weight Heparin, and fondaparinux are considered compatible with breastfeeding as they are unlikely to transfer into milk in clinically significant amounts, and are not absorbed from the infant's GI tract due to large molecular weight.

Can I drink alcohol with Heparin?

Combination of alcohol and Heparin can result in harmful side effects to the liver and severe bleeding in the stomach.

Can I drive after taking Heparin?

This Heparin should not have any effect on your ability to drive or use machines.

Does Heparin make me tired?

Heparin injectable solution doesn't cause drowsiness, but it can cause other side effects.

When should be taken of Heparin?

Heparin is usually used when the catheter is first put in place, and every time that blood is drawn out of the catheter or medication is given through the catheter.

What is the best time to take Heparin?

Take the dose at the same time each day. We recommend 5:00 p.m. Heparin can be taken before or after eating.

How many time can I take Heparin daily?

Heparin is sometimes injected one to six times a day and sometimes given as a slow, continuous injection into the vein.

How long does Heparin take to work?

Heparin works within 20 to 60 minutes following deep SC injection.

How long does Heparin stay in my system?

Although the metabolism of Heparin is complex, it may, for the purpose of choosing a protamine dose, be assumed to have a half-life of about 1/2 hour after intravenous injection.

What happen If I suddenly stop taking Heparin?

If you stop taking the Heparin suddenly or don't take it at all: You may develop a blood clot, or an existing blood clot could get worse. These blood clots can be fatal (cause death).

Who should not take Heparin?

You should not use Heparin if you have uncontrolled bleeding or a severe lack of platelets in your blood, or if you have ever had low platelets caused by using heparin or pentosan polysulfate. Do not use Heparin injection to flush (clean out) an intravenous (IV) catheter, or fatal bleeding could result.

What happens if I miss a dose?

Call your doctor for instructions if you miss a dose.

What happens if I overdose?

Seek emergency medical attention. Overdose symptoms may include easy bruising, nosebleeds, blood in your urine or stools, black or tarry stools, or any bleeding that will not stop.

Can Heparin affects my heart ?

Heparin-induced thrombocytopenia. This is low platelet levels caused by heparin use. It can cause new or worsening clots in your blood vessels. These may lead to a stroke or heart attack.

Can Heparin affect my kidneys?

 If you have severe kidney disease or a history of kidney disease, taking Heparin can increase your risk of bleeding.

Can Heparin affects my liver?

Heparin have not been associated with clinically significant liver injury.

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