Entecavir Monohydrate interactions

Food & lifestyle

• high-fat foods

  Moderate

  Absorption

  Food delays the oral absorption and reduces the oral bioavailability of entecavir. According to the product labeling, administration of entecavir 0.5 mg with a standard high-fat meal or a light meal resulted in a delay in absorption by 0.25 to 0.75 hours, a decrease in the peak plasma concentration (Cmax) by 44% to 46%, and a decrease in the area under the plasma concentration-time curve (AUC) by 18% to 20% compared to administration in the fasting state.

  What to do: To ensure maximal oral absorption, entecavir should be administered on an empty stomach at least 2 hours after a meal and 2 hours before the next meal.

  1 source

  1. "Product Information. Baraclude (entecavir)." Bristol-Myers Squibb (2005):

Conditions

Conditions in which Entecavir Monohydrate needs care, as documented in this source.

• Liver Diseases

  Major

  Hepatotoxicity including lactic acidosis, severe hepatomegaly with steatosis, fulminant hepatitis, and hepatic failure has been associated with the use of some nucleoside reverse transcriptase inhibitors (NRTIs) alone or in combination with other antiretroviral agents. Therapy with NRTIs should be administered cautiously in patients with preexisting liver disease, a history of alcohol abuse, or hepatitis. Therapy should be suspended if clinical or laboratory findings suggestive of lactic acidosis or pronounced hepatotoxicity occur. The use of abacavir is contraindicated in patients with moderate to severe hepatic impairment as its safety and efficacy has not been established on these patients.

  24 sources

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  2. Dolin R, Lambert JS, Morse GD, et al. "2',3'-dideoxyinosine in patients with AIDS or AIDS-related complex." Rev Infect Dis 12 (1990): s540-51
  3. Lai KK, Gang DL, Zawacki JK, Cooley TP "Fulminant hepatic failure associated with 2',3'-dideoxyinosine (ddI)." Ann Intern Med 115 (1991): 283-4
  4. Dubin G, Braffman MN "Zidovudine-induced hepatotoxicity." Ann Intern Med 110 (1989): 85-6
  5. Shriner K, Goetz MB "Severe hepatoxicity in a patient receiving both acetaminophen and zidovudine." Am J Med 93 (1992): 94-6
  6. Gradon JD, Chapnick EK, Sepkowitz DV "Zidovudine-induced hepatitis." J Intern Med 231 (1992): 317-8
  7. Chen SC, Barker SM, Mitchell DH, et al. "Concurrent zidovudine-induced myopathy and hepatoxicity in patients treated for human immunodeficiency virus (HIV) infection." Pathology 24 (1992): 109-11
  8. "Product Information. Videx (didanosine)." Bristol-Myers Squibb (2002):

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  9. "Product Information. HIVID (zalcitabine)." Roche Laboratories (2001):
  10. "Product Information. Retrovir (zidovudine)." Glaxo Wellcome (2001):
  11. Pike IM, Nicaise C "The didanosine Expanded Access Program: safety analysis." Clin Infect Dis 16 (1993): S63-8
  12. Shintaku M, Nasu K, Shimizu T "Fulminant hepatic failure in an AIDS patient: possible zidovudine- induced hepatotoxicity." Am J Gastroenterol 88 (1993): 464-6
  13. Montaner JSG, Rachlis A, Beaulieu R, Gill J, Schlech W, Phillips P, Auclair C, Boulerice F, Schindzielorz A, Smaldone L, Wainber "Safety profile of didanosine among patients with advanced HIV disease who are intolerant to or deteriorate despite zidovudine therapy: results of the canadian open ddi treatment program." J Acquir Immune Defic Syndr 7 (1994): 924-30
  14. "Product Information. Epivir (lamivudine)." Glaxo Wellcome (2001):
  15. "Product Information. Ziagen (abacavir)." Glaxo Wellcome (2001):
  16. Miller KD, Cameron M, Wood LV, Dalakas MC, Kovacs JA "Lactic acidosis and hepatic steatosis associated with use of stavudine: report of four cases." Ann Intern Med 133 (2000): 192-6
  17. Lhouri S, Cushing H "Lactic acidosis secondary to nucleoside analog antiretroviral therapy." Infect Med 17 (2000): 547-54
  18. Pai VB, Koranyi K, Nahata MC "Acute hepatitis and bleeding possibly induced by zidovudine and ritonavir in an infant with HIV infection." Pharmacotherapy 20 (2000): 1135-40
  19. Lonergan JT, Behling C, Pfander H, Hassanein TI, Mathews WC "Hyperlactatemia and hepatic abnormalities in 10 human immunodeficiency virus-infected patients receiving nucleoside analogue combination regimens." Clin Infect Dis 31 (2000): 162-6
  20. Kronenberg A, Riehle HM, Gunthard HF "Liver failure after long-term nucleoside antiretroviral therapy." Lancet 358 (2001): 759-601
  21. Boubaker K, Flepp M, Sudre P, et al. "Hyperlactatemia and Antiretroviral Therapy: The Swiss HIV Cohort Study." Clin Infect Dis 33 (2001): 1931-7
  22. Coghlan ME, Sommadossi JP, Jhala NC, Many WJ, Saag MS, Johnson VA "Symptomatic lactic acidosis in hospitalized antiretroviral-treated patients with human immunodeficiency virus infection: a report of 12 cases." Clin Infect Dis 33 (2001): 1914-21
  23. "Product Information. Viread (tenofovir)." Gilead Sciences (2001):
  24. "Product Information. Baraclude (entecavir)." Bristol-Myers Squibb (2005):

• Diseases requiring hemodialysis

  Moderate

  Entecavir is removed by hemodialysis. Following a single 1 mg dose of entecavir administered two hours before the hemodialysis session, approximately 13% of the dose was removed over four hours of hemodialysis. Entecavir should be administered after hemodialysis.

  1 source

  1. "Product Information. Baraclude (entecavir)." Bristol-Myers Squibb (2005):

• Kidney Diseases

  Moderate

  Entecavir is primarily eliminated by the kidney. Compared to patients with normal renal function (CrCl above 80 mL/min), peak plasma concentration (Cmax) and systemic exposure (AUC) of a single 1 mg dose of entecavir increased by 30% and 150%, respectively, in patients with moderate renal dysfunction (CrCl 30 to 49 mL/min), and 89% and 422%, respectively, in patients with severe renal dysfunction (CrCl below 30 mL/min). Systemic exposure was increased even further in patients with end-stage renal disease managed on dialysis. These patients had an approximately 8-fold increase in entecavir AUC compared to patients with normal renal function. Renal clearance of entecavir decreased by 65% and 89%, respectively, in patients with moderate and severe renal dysfunction. Dosage adjustment of entecavir is recommended for patients with CrCl below 50 mL/min, including patients on dialysis, in accordance with the manufacturer's product labeling.

  1 source

  1. "Product Information. Baraclude (entecavir)." Bristol-Myers Squibb (2005):