Peringatan Keamanan

The oral LD50 for enoxaparin in mice is >5000 mg/kg; the subcutaneous LD50 of enoxaparin in mice is >2500 mg/kg.L31558
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.L31393

Enoxaparin

DB01225

small molecule approved

Deskripsi

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.L31393 Enoxaparin markedly reduces the incidence of venous thromboembolism in hospitalized patients when compared to unfractionated heparin, without increasing the risk of serious bleeding.A228178,A228313

Struktur Molekul 2D

Struktur tidak tersedia

Peta Jejaring Molekuler
Legenda: ObatTargetGenEnzim(Panah → menunjukkan arah efek / relasi)TransporterCarrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) The half-life of enoxaparin is about 4 hours after a single dose administered subcutaneously and about 7 hours after several doses.[L31538] One source mentions a half-life ranging from 1 hour to 4.5 hours.[A228363]
Volume Distribusi The volume of distribution of enoxaparin is approximately 4-5L, similar to normal blood volume.[L31393,L31538]
Klirens (Clearance) The mean clearance of enoxaparin is 0.74 L/h after a 1.5 mg/kg intravenous infusion over 6 hours[L31538]; clearance of enoxaparin is significantly decreased in patients with severe renal impairment.[A228133]

Absorpsi

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.A228363,L31538 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 daysA228363 of treatment with a Cmax of 1.2 IU/mL.L31538 The AUC under the thrombin generation curve was 305 +/- 48.A228318

Metabolisme

Enoxaparin is mainly metabolized by the liver via desulfation and/or depolymerization to lower and less potent molecular weight metabolites.L31393,L31538

Rute Eliminasi

Enoxaparin is mainly excreted by the kidneys.A228143 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.L31538

Interaksi Makanan

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

Interaksi Obat

860 Data
Apixaban Apixaban may increase the anticoagulant activities of Enoxaparin.
Dabigatran etexilate Dabigatran etexilate may increase the anticoagulant activities of Enoxaparin.
Dasatinib The risk or severity of bleeding and hemorrhage can be increased when Dasatinib is combined with Enoxaparin.
Deferasirox The risk or severity of gastrointestinal bleeding can be increased when Enoxaparin is combined with Deferasirox.
Ursodeoxycholic acid The risk or severity of bleeding and bruising can be increased when Enoxaparin is combined with Ursodeoxycholic acid.
Glycochenodeoxycholic Acid The risk or severity of bleeding and bruising can be increased when Enoxaparin is combined with Glycochenodeoxycholic Acid.
Cholic Acid The risk or severity of bleeding and bruising can be increased when Enoxaparin is combined with Cholic Acid.
Glycocholic acid The risk or severity of bleeding and bruising can be increased when Enoxaparin is combined with Glycocholic acid.
Deoxycholic acid The risk or severity of bleeding and bruising can be increased when Enoxaparin is combined with Deoxycholic acid.
Taurocholic acid The risk or severity of bleeding and bruising can be increased when Enoxaparin is combined with Taurocholic acid.
Obeticholic acid The risk or severity of bleeding and bruising can be increased when Enoxaparin is combined with Obeticholic acid.
Chenodeoxycholic acid The risk or severity of bleeding and bruising can be increased when Enoxaparin is combined with Chenodeoxycholic acid.
Taurochenodeoxycholic acid The risk or severity of bleeding and bruising can be increased when Enoxaparin is combined with Taurochenodeoxycholic acid.
Tauroursodeoxycholic acid The risk or severity of bleeding and bruising can be increased when Enoxaparin is combined with Tauroursodeoxycholic acid.
Bamet-UD2 The risk or severity of bleeding and bruising can be increased when Enoxaparin is combined with Bamet-UD2.
Dehydrocholic acid The risk or severity of bleeding and bruising can be increased when Enoxaparin is combined with Dehydrocholic acid.
Hyodeoxycholic Acid The risk or severity of bleeding and bruising can be increased when Enoxaparin is combined with Hyodeoxycholic Acid.
Edoxaban The risk or severity of bleeding can be increased when Edoxaban is combined with Enoxaparin.
Ibrutinib The risk or severity of bleeding and hemorrhage can be increased when Ibrutinib is combined with Enoxaparin.
Obinutuzumab The risk or severity of bleeding and hemorrhage can be increased when Enoxaparin is combined with Obinutuzumab.
Rivaroxaban Enoxaparin may increase the anticoagulant activities of Rivaroxaban.
Sugammadex The risk or severity of bleeding and hemorrhage can be increased when Enoxaparin is combined with Sugammadex.
Tibolone Tibolone may increase the anticoagulant activities of Enoxaparin.
Tipranavir The risk or severity of bleeding and hemorrhage can be increased when Tipranavir is combined with Enoxaparin.
Urokinase Urokinase may increase the anticoagulant activities of Enoxaparin.
Vitamin E Vitamin E may increase the anticoagulant activities of Enoxaparin.
Vorapaxar The risk or severity of bleeding and hemorrhage can be increased when Vorapaxar is combined with Enoxaparin.
Trandolaprilat The risk or severity of hyperkalemia can be increased when Trandolaprilat is combined with Enoxaparin.
Moexiprilat The risk or severity of hyperkalemia can be increased when Moexiprilat is combined with Enoxaparin.
Cilazaprilat The risk or severity of hyperkalemia can be increased when Cilazaprilat is combined with Enoxaparin.
Ginkgo biloba Ginkgo biloba may increase the anticoagulant activities of Enoxaparin.
Ifosfamide The risk or severity of bleeding can be increased when Ifosfamide is combined with Enoxaparin.
Quinine The therapeutic efficacy of Enoxaparin can be increased when used in combination with Quinine.
Quinidine The therapeutic efficacy of Enoxaparin can be increased when used in combination with Quinidine.
Tamoxifen The risk or severity of bleeding can be increased when Tamoxifen is combined with Enoxaparin.
Toremifene The risk or severity of bleeding can be increased when Toremifene is combined with Enoxaparin.
Corticorelin ovine triflutate The risk or severity of hypotension and sinus node depression can be increased when Enoxaparin is combined with Corticorelin ovine triflutate.
Oritavancin The therapeutic efficacy of Enoxaparin can be decreased when used in combination with Oritavancin.
Streptokinase Streptokinase may increase the anticoagulant activities of Enoxaparin.
Telavancin The therapeutic efficacy of Enoxaparin can be decreased when used in combination with Telavancin.
Palifermin The serum concentration of Palifermin can be increased when it is combined with Enoxaparin.
Pentoxifylline The therapeutic efficacy of Enoxaparin can be increased when used in combination with Pentoxifylline.
Pentosan polysulfate Pentosan polysulfate may increase the anticoagulant activities of Enoxaparin.
Levocarnitine The therapeutic efficacy of Enoxaparin can be increased when used in combination with Levocarnitine.
Diethylstilbestrol Diethylstilbestrol may decrease the anticoagulant activities of Enoxaparin.
Chlorotrianisene Chlorotrianisene may decrease the anticoagulant activities of Enoxaparin.
Conjugated estrogens Conjugated estrogens may decrease the anticoagulant activities of Enoxaparin.
Mestranol The risk or severity of adverse effects can be increased when Mestranol is combined with Enoxaparin.
Estrone sulfate Estrone sulfate may decrease the anticoagulant activities of Enoxaparin.
Quinestrol Quinestrol may decrease the anticoagulant activities of Enoxaparin.
Hexestrol Hexestrol may decrease the anticoagulant activities of Enoxaparin.
Synthetic Conjugated Estrogens, A Synthetic Conjugated Estrogens, A may decrease the anticoagulant activities of Enoxaparin.
Synthetic Conjugated Estrogens, B Synthetic Conjugated Estrogens, B may decrease the anticoagulant activities of Enoxaparin.
Polyestradiol phosphate Polyestradiol phosphate may decrease the anticoagulant activities of Enoxaparin.
Esterified estrogens Esterified estrogens may decrease the anticoagulant activities of Enoxaparin.
Zeranol Zeranol may decrease the anticoagulant activities of Enoxaparin.
Equol Equol may decrease the anticoagulant activities of Enoxaparin.
Methallenestril Methallenestril may decrease the anticoagulant activities of Enoxaparin.
Epimestrol Epimestrol may decrease the anticoagulant activities of Enoxaparin.
Moxestrol Moxestrol may decrease the anticoagulant activities of Enoxaparin.
Estradiol acetate Estradiol acetate may decrease the anticoagulant activities of Enoxaparin.
Estradiol benzoate Estradiol benzoate may decrease the anticoagulant activities of Enoxaparin.
Estradiol cypionate Estradiol cypionate may decrease the anticoagulant activities of Enoxaparin.
Estradiol valerate Estradiol valerate may decrease the anticoagulant activities of Enoxaparin.
Biochanin A Biochanin A may decrease the anticoagulant activities of Enoxaparin.
Formononetin Formononetin may decrease the anticoagulant activities of Enoxaparin.
Estriol Estriol may decrease the anticoagulant activities of Enoxaparin.
Limaprost The risk or severity of adverse effects can be increased when Limaprost is combined with Enoxaparin.
Icosapent The risk or severity of bleeding and hemorrhage can be increased when Icosapent is combined with Enoxaparin.
Mesalazine The risk or severity of bleeding can be increased when Mesalazine is combined with Enoxaparin.
Indomethacin The risk or severity of bleeding and hemorrhage can be increased when Indomethacin is combined with Enoxaparin.
Nabumetone The risk or severity of bleeding and hemorrhage can be increased when Nabumetone is combined with Enoxaparin.
Ketorolac The risk or severity of bleeding and hemorrhage can be increased when Ketorolac is combined with Enoxaparin.
Tenoxicam The risk or severity of bleeding and hemorrhage can be increased when Tenoxicam is combined with Enoxaparin.
Celecoxib The risk or severity of bleeding and hemorrhage can be increased when Celecoxib is combined with Enoxaparin.
Tolmetin The risk or severity of bleeding and hemorrhage can be increased when Tolmetin is combined with Enoxaparin.
Rofecoxib The risk or severity of bleeding and hemorrhage can be increased when Rofecoxib is combined with Enoxaparin.
Piroxicam The risk or severity of bleeding and hemorrhage can be increased when Piroxicam is combined with Enoxaparin.
Fenoprofen The risk or severity of bleeding and hemorrhage can be increased when Fenoprofen is combined with Enoxaparin.
Valdecoxib The risk or severity of bleeding and hemorrhage can be increased when Valdecoxib is combined with Enoxaparin.
Diclofenac The risk or severity of bleeding and hemorrhage can be increased when Diclofenac is combined with Enoxaparin.
Sulindac The risk or severity of bleeding and hemorrhage can be increased when Sulindac is combined with Enoxaparin.
Flurbiprofen The risk or severity of bleeding and hemorrhage can be increased when Flurbiprofen is combined with Enoxaparin.
Etodolac The risk or severity of bleeding and hemorrhage can be increased when Etodolac is combined with Enoxaparin.
Mefenamic acid The risk or severity of bleeding and hemorrhage can be increased when Mefenamic acid is combined with Enoxaparin.
Naproxen The risk or severity of bleeding and hemorrhage can be increased when Naproxen is combined with Enoxaparin.
Sulfasalazine The risk or severity of bleeding and hemorrhage can be increased when Sulfasalazine is combined with Enoxaparin.
Phenylbutazone The risk or severity of bleeding and hemorrhage can be increased when Phenylbutazone is combined with Enoxaparin.
Meloxicam The risk or severity of bleeding and hemorrhage can be increased when Meloxicam is combined with Enoxaparin.
Carprofen The risk or severity of bleeding and hemorrhage can be increased when Carprofen is combined with Enoxaparin.
Diflunisal The risk or severity of bleeding and hemorrhage can be increased when Diflunisal is combined with Enoxaparin.
Salicylic acid The risk or severity of bleeding and hemorrhage can be increased when Salicylic acid is combined with Enoxaparin.
Meclofenamic acid The risk or severity of bleeding and hemorrhage can be increased when Meclofenamic acid is combined with Enoxaparin.
Oxaprozin The risk or severity of bleeding and hemorrhage can be increased when Oxaprozin is combined with Enoxaparin.
Ketoprofen The risk or severity of bleeding and hemorrhage can be increased when Ketoprofen is combined with Enoxaparin.
Balsalazide The risk or severity of bleeding and hemorrhage can be increased when Balsalazide is combined with Enoxaparin.
Olsalazine The risk or severity of bleeding can be increased when Enoxaparin is combined with Olsalazine.
Lumiracoxib The risk or severity of bleeding and hemorrhage can be increased when Lumiracoxib is combined with Enoxaparin.
Magnesium salicylate The risk or severity of bleeding and hemorrhage can be increased when Magnesium salicylate is combined with Enoxaparin.
Salsalate The risk or severity of bleeding and hemorrhage can be increased when Salsalate is combined with Enoxaparin.

Target Protein

Antithrombin-III SERPINC1
Coagulation factor X F10
Prothrombin F2

Referensi & Sumber

Synthesis reference: Jorgen I. Nielsen, "Process of using light absorption to control enzymatic depolymerization of heparin to produce low molecular weight heparin." U.S. Patent US5106734, issued May, 1981.
Artikel (PubMed)
  • PMID: 21470072
    Iqbal Z, Cohen M: Enoxaparin: a pharmacologic and clinical review. Expert Opin Pharmacother. 2011 May;12(7):1157-70. doi: 10.1517/14656566.2011.570261. Epub 2011 Apr 7.
  • PMID: 11927128
    Sanderink GJ, Guimart CG, Ozoux ML, Jariwala NU, Shukla UA, Boutouyrie BX: Pharmacokinetics and pharmacodynamics of the prophylactic dose of enoxaparin once daily over 4 days in patients with renal impairment. Thromb Res. 2002 Feb 1;105(3):225-31. doi: 10.1016/s0049-3848(02)00031-2.
  • PMID: 8703665
    Azizi M, Veyssier-Belot C, Alhenc-Gelas M, Chatellier G, Billaud-Mesguish E, Fiessinger JN, Aiach M: Comparison of biological activities of two low molecular weight heparins in 10 healthy volunteers. Br J Clin Pharmacol. 1995 Dec;40(6):577-84.
  • PMID: 12968985
    Bruno R, Baille P, Retout S, Vivier N, Veyrat-Follet C, Sanderink GJ, Becker R, Antman EM: Population pharmacokinetics and pharmacodynamics of enoxaparin in unstable angina and non-ST-segment elevation myocardial infarction. Br J Clin Pharmacol. 2003 Oct;56(4):407-14. doi: 10.1046/j.1365-2125.2003.01904.x.
  • PMID: 21232002
    Laporte S, Liotier J, Bertoletti L, Kleber FX, Pineo GF, Chapelle C, Moulin N, Mismetti P: Individual patient data meta-analysis of enoxaparin vs. unfractionated heparin for venous thromboembolism prevention in medical patients. J Thromb Haemost. 2011 Mar;9(3):464-72. doi: 10.1111/j.1538-7836.2011.04182.x.
  • PMID: 26780737
    Nutescu EA, Burnett A, Fanikos J, Spinler S, Wittkowsky A: Pharmacology of anticoagulants used in the treatment of venous thromboembolism. J Thromb Thrombolysis. 2016 Jan;41(1):15-31. doi: 10.1007/s11239-015-1314-3.
  • PMID: 15151480
    Hofmann T: Clinical application of enoxaparin. Expert Rev Cardiovasc Ther. 2004 May;2(3):321-37. doi: 10.1586/14779072.2.3.321.
  • PMID: 26733269
    Wei MY, Ward SM: The Anti-Factor Xa Range For Low Molecular Weight Heparin Thromboprophylaxis. Hematol Rep. 2015 Nov 23;7(4):5844. doi: 10.4081/hr.2015.5844. eCollection 2015 Nov 23.
Menampilkan 8 dari 10 artikel.

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