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ximelagatran (Exanta)

zye-mel-a-gat-ran. Not yet available in US. May have been removed from market. [11] Tradename: Exanta [5] Indications: 1) prophylaxis for venous thromboembolism/deep vein thrombosis 2) anticoagulation for non-valvular atrial fibrillation [2,6] 3) prophylaxis for recurrent acute coronary syndromes? [4] ? ref 4 finds benefit Dosage: 1) 20-40 mg PO BID (beginning morning after surgery) 2) 20-60 mg PO BID (atrial fibrillation) 3) 36 mg PO BID [10] NO need to monitor INR Adverse effects: 1) minor bleeding (6-12%) warfarin> 2) transient elevation in serum ALT (4-12%) 3) severe hepatic impairment (0.5%) [7] 4) death (0.05%) [7] 5) increased risk* of myocardial infarction [8,9] * less than that for patients taking warfarin [10] Mechanism of action: -> direct thrombin inhibitor

Interactions

drug interactions drug adverse effects of antithrombotic agent(s)

Related

thrombin; coagulation factor IIa

General

thrombin inhibitor

Properties

INHIBITS: thrombin

Database Correlations

PUBCHEM correlations

References

  1. Journal Watch 22(24):180, 2002 Francis CW et al Ann Inter Med 137:648, 2002
  2. Journal Watch 23(16):125, 2003 Peterson P et al, J Am Coll Cardio 41:1445, 2003 PMID: 12742279
  3. Journal Watch 23(23):182, 2003 Francis CW et al, N Engl J Med 349:1703, 2003 PMID: 14585938 Schulman S et al, N Engl J Med 349:1713, 2003 PMID: 14585939
  4. Journal Watch 23(23):182-83, 2003 Wallentin L et al, Lancet 362:789, 2003 PMID: 13678873 Giugliano RP & Brunwald E Lancet 362:757, 2003
  5. Prescriber's Letter 10(12):72 2003 Detail-Document#: 191216 (subscription needed) http://www.prescribersletter.com
  6. Journal Watch 22(1):1, 2004 Sportif II Investigators, Lancet 362:1691, 2003 PMID: 14643116
  7. Setter SM. In: Intensive Course in Geriatric Medicine & Board Review, Marina Del Ray, CA, Sept 29-Oct 2, 2004
  8. Prescriber's Letter 11(11): 2004 Ximelagatran (Exanta) and Liver Toxicity Detail-Document#: 201106 (subscription needed) http://www.prescribersletter.com
  9. Weitz JI. New anticoagulants for treatment of venous thromboembolism. Circulation. 2004 Aug 31;110(9 Suppl 1):I19-26. Review. PMID: 15339877
  10. Journal Watch 25(6):52, 2005 - Fiessinger JN, Huisman MV, Davidson BL, Bounameaux H, Francis CW, Eriksson H, Lundstrom T, Berkowitz SD, Nystrom P, Thorsen M, Ginsberg JS; THRIVE Treatment Study Investigators. Ximelagatran vs low-molecular-weight heparin and warfarin for the treatment of deep vein thrombosis: a randomized trial. JAMA. 2005 Feb 9;293(6):681-9. PMID: 15701909 - Albers GW, Diener HC, Frison L, Grind M, Nevinson M, Partridge S, Halperin JL, Horrow J, Olsson SB, Petersen P, Vahanian A; SPORTIF Executive Steering Committee for the SPORTIF V Investigators. Ximelagatran vs warfarin for stroke prevention in patients with nonvalvular atrial fibrillation: a randomized trial. JAMA. 2005 Feb 9;293(6):690-8. PMID: 15701910 - Gurewich V. Ximelagatran--promises and concerns. JAMA. 2005 Feb 9;293(6):736-9. No abstract available. PMID: 15701916
  11. Physician's First Watch, November 15, 2012 David G. Fairchild, MD, MPH, Editor-in-Chief Massachusetts Medical Society