Aparin

Aparin 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.

Aparin
Uses
Dosage
Side Effect
Precautions
Interactions
Uses during Pregnancy
Uses during Breastfeeding
Accute Overdose
Food Interaction
Half Life
Volume of Distribution
Clearance
Interaction With other Medicine
Contradiction
Storage

Trade Name	Aparin
Generic	Heparin + Benzyl Nicotinate
Type	Ointment
Therapeutic Class
Manufacturer	Leeford Healthcare Ltd
Available Country	India
Last Updated:	September 19, 2023 at 7:00 am

Uses

Benzyl nicotinate is a rubefacient and vasodilator used in combination with analgesics in topical preparations.

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.

Aparin is also used to associated treatment for these conditions: Back Pain Lower Back, Bursitis, Osteoarthritis (OA), Periarthritis, Rheumatism, Sciatica, Spondylosis, Acute nonspecific tenosynovitisBlunt 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 Aparin 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

Aparin 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.

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.