Heparin


Thông tin thuốc gốc
Chỉ định và Liều dùng
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.
Tương kỵ
Alteplase, reteplase, amikacin sulfate, amiodarone HCl, ampicillin Na, aprotinin, benzylpenicillin K or Na, cefalotin Na, ciprofloxacin lactate, cytarabine, dacarbazine, daunorubicin HCl, diazepam, dobutamine HCl, doxorubicin HCl, droperidol, erythromycin lactobionate, gentamicin sulfate, haloperidol lactate, hyaluronidase, hydrocortisone Na succinate, kanamycin sulfate, meticillin Na, netilmicin sulfate, some opioid analgesics, oxytetracycline HCl, some phenothiazines, polymyxin B sulfate, streptomycin sulfate, tetracycline HCl, tobramycin sulfate, vancomycin HCl, vinblastine sulfate, cisatracurium besilate, labetalol HCl, levofloxacin, nicardipine HCl, vinorelbine tartrate, and cefmetazole Na.
Chống chỉ định
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 w/ abortus imminens; epidural anaesth during birth; locoregional anaesth in elective surgical procedures (in patients receiving heparin for treatment rather than prophylaxis).
Thận trọng
Patient w/ 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.
Phản ứng phụ
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.
Potentially Fatal: Heparin-induced thrombocytopenia w/ or w/out thrombosis, severe haemorrhage.
IV/Parenteral/SC: C
Thông tin tư vấn bệnh nhân
Preservative-free formulation is recommended in neonates, infants, pregnant women and nursing mothers.
MonitoringParameters
Monitor Hb, haematocrit, signs of bleeding; faecal occult blood test; aPTT (or antifactor Xa activity levels) or activated clotting time (ACT) depending upon indication.
Quá liều
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.
Tương tác
Enhanced anticoagulant effect w/ 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 w/ gyceryl trinitrate infusion. Increased risk of hyperkalaemia w/ ACE inhibitors or angiotensin II antagonists.
Lab Interference
May interfere w/ sulfobromophthalein test. May cause falsely elevated results in the competitive binding methods for serum thyroxine determinations.
Tác dụng
Description: Heparin potentiates the action of antithrombin III, thereby inactivates thrombin as well as activated coagulation factors IX, X, XI, XII and plasmin, and inhibits the conversion of fibrinogen to fibrin. It also stimulates release of lipoprotein lipase which hydrolyses triglycerides to glycerol and free fatty acids.
Onset: Anticoagulation: Immediate (IV); approx 20-30 min (SC).
Pharmacokinetics:
Absorption: Absorbed from systemic circulation.
Distribution: Plasma protein binding: Extensive.
Metabolism: Partially metabolised in the liver to uroheparin (partially desulfated heparin); appears to be removed from the circulation mainly by the reticuloendothelial system and may localise on arterial venous endothelium.
Excretion: Via urine (as metabolites, or up to 50% as unchanged drug after admin of large doses). Half-life: 1-6 hr.
Bảo quản
Store between 20-25°C. Protect from freezing.
References
Anon. Heparin. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 13/08/2014.

Buckingham R (ed). Heparin. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 13/08/2014.

Heparin Sodium Injection, Solution (Hospira, Inc). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 13/08/2014.

Heparin Sodium Injection. U.S. FDA. https://www.fda.gov/. Accessed 13/08/2014.

McEvoy GK, Snow EK, Miller J et al (eds). Heparin Sodium. AHFS Drug Information (AHFS DI) [online]. American Society of Health-System Pharmacists (ASHP). https://www.medicinescomplete.com. Accessed 13/08/2014.

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