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Entecavir

 
Drug Info: Entecavir
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Brand names: Baraclude™



Entecavir tablets

What are Entecavir tablets?

ENTECAVIR (Baraclude™) is used to treat infections due to the hepatitis B virus. Entecavir can slow the liver damage caused by hepatitis B. It will not cure or prevent hepatitis B infection. Generic entecavir tablets are not yet available.

What should I tell my health care provider before I take this medicine?

They need to know if you have any of these conditions:
• kidney disease
• liver disease
• HIV infection or AIDS
• an unusual reaction to Entecavir, other medicines, foods, dyes, or preservatives
• pregnant or trying to get pregnant
• breast-feeding

How should this medicine be used?

Take entecavir tablets by mouth. Follow the directions on the prescription label. Take entecavir 2 hours before and at least 2 hours after eating. Swallow tablets with a drink of water. Try to take your dose at the same time each day. Do not take your medicine more often than directed. Do not stop taking this medicine except on your prescriber's advice.

Contact your pediatrician or health care professional regarding the use of this medicine in children. Special care may be needed.

What drug(s) may interact with Entecavir?

• amiloride
• amphotericin B
• antiinflammatory drugs (NSAIDs, such as ibuprofen)
• certain antibiotics given by injection
• cimetidine
• cisplatin
• cyclosporine
• ketoconazole
• megestrol
• metformin
• midodrine
• morphine
• pamidronate
• pancuronium
• quinine
• ranitidine
• some antibiotics such as trimethoprim and vancomycin
• some medicines for colds, hay fever, or allergies
• some medicines to control the heart rhythm such as digoxin, disopyramide, dofetilide, procainamide, and quinidine
• some medicines for mental depression or psychotic disorders
• some medicines used to control high blood pressure such as enalapril, lisinopril, and ramipril
• some medicines used to treat viral infections such as acyclovir, cidofovir, foscarnet, ganciclovir, valacyclovir, and valganciclovir
• tacrolimus
• triamterene
• trospium
• zoledronic acid

Tell your prescriber or health care professional about all other medicines you are taking, including non-prescription medicines, nutritional supplements, or herbal products. Also tell your prescriber or health care professional if you are a frequent user of drinks with caffeine or alcohol, if you smoke, or if you use illegal drugs. These may affect the way your medicine works. Check with your health care professional before stopping or starting any of your medicines.

What should I watch for while taking Entecavir?

You must visit your prescriber or health care professional for regular checks on your progress during and after treatment with entecavir. You will need regular blood tests to check for liver function and hepatitis B virus levels.

Discuss any new symptoms with your prescriber or health care professional. Tell your prescriber or health care professional at once if you have nausea and vomiting accompanied by severe stomach pain. Some people have worsening of hepatitis after stopping entecavir therapy. Do not stop taking entecavir unless your prescriber instructs you to.

Entecavir will not cure hepatitis B infection and you can still get other illnesses or complications associated with your disease. Taking entecavir does not reduce the risk of passing hepatitis B infection to others through sexual or blood contact. Do not have sexual contact without protection; talk to your health care professional about practicing 'safe sex', such as using condoms. Be careful about cuts, abrasions and other possible sources of blood contact. Do not share razors, toothbrushes or other personal items that might have contact with blood. Never share a needle or syringe with anyone.

What side effects may I notice from receiving Entecavir?

Side effects that you should report to your prescriber or health care professional as soon as possible:
• breathing difficulties or shortness of breath
• dark yellow or brown urine
• dizziness
• irregular heartbeat
• loss of appetite for several days or longer
• not passing urine as often as usual or blood in your urine
• passing out or fainting
• severe diarrhea
• unusual muscle pain
• unusual weakness, tiredness, or discomfort
• unusual stomach pain or discomfort
• vomiting
• yellowing of the eyes or skin

Side effects that usually do not require medical attention (report to your prescriber or health care professional if they continue or are bothersome):
• headache
• heartburn or indigestion
• insomnia or trouble sleeping
• mild diarrhea
• nausea
• sleepiness

Where can I keep my medicine?

Keep out of the reach of children in a container that small children cannot open.

Store between 15—30 degrees C (59—86 degrees F). Keep the container tightly closed. Throw away any unused medicine after the expiration date.

Last updated: 4/21/2005 10:46:00 AM

Important Disclaimer: The drug information provided here is for educational purposes only. It is intended to supplement, not substitute for, the diagnosis, treatment and advice of a medical professional. This drug information does not cover all possible uses, precautions, side effects and interactions. It should not be construed to indicate that this or any drug is safe for you. Consult your medical professional for guidance before using any prescription or over the counter drugs.

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Wikipedia: Entecavir
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Home > Library > Miscellaneous > Wikipedia
Entecavir
Systematic (IUPAC) name
2-Amino-9-[(1S,3R,4S)-4-hydroxy-3-(hydroxymethyl)-2-methylidenecyclopentyl]-6,9-dihydro-3H-purin-6-one
Identifiers
CAS number 142217-69-4
ATC code J05AF10
PubChem 153941
DrugBank APRD00948
Chemical data
Formula C12H15N5O3 
Mol. mass 277.279 g/mol
Pharmacokinetic data
Bioavailability  ?
Protein binding 13%
Metabolism  ?
Half life 128–149 hours
Excretion Renal 62–73%
Therapeutic considerations
Licence data

EU EMEA:link, US FDA:link
Pregnancy cat.

C(US)
Legal status

℞-only(US)
Routes Oral
 Yes check.svgY(what is this?)  (verify)

Entecavir (INN) (pronounced /ɛnˈtɛkəvɪr/) is an oral antiviral drug used in the treatment of hepatitis B infection. It is marketed under the trade name Baraclude (BMS).

Entecavir is a nucleoside analog[1] (more specifically, a guanine analogue) that inhibits reverse transcription, DNA replication and transcription in the viral replication process. The drug's manufacturer claims that entecavir is more efficacious than previous agents used to treat hepatitis B (lamivudine and adefovir). It also has a few problems as well there are studies out in 2007 that patients that have stopped entecavir for a month or more have created a resistant version of the virus and will have to switch to a different medication like Viread to fight the newly resistant infection.

Entecavir was approved by the U.S.FDA in March 2005.

History

  • 1992: SQ-34676 at Squibb as part of anti-herpes virus program[2]
  • 1997: BMS 200475 developed at BMS pharmaceutical research institute as antiviral nucleoside analogue à Activity demonstrated against HBV, HSV-1, HCMV, VZV in cell lines & no or little activity against HIV or influenza[3]
  • Superior activity observed against HBV pushed research towards BMS 200475, its base analogues and its enantiomer against HBV in HepG2.2.15 cell line[4]
  • Comparison to other NAs, proven more selective potent inhibitor of HBV by virtue of being Guanine NA[5]
  • 1998: Inhibition of hepadnaviral polymerases was demonstrated in vitro in comparison to a number of NAs-TP[6]
  • Metabolic studies showed more efficient phosphorylation to triphosphate active form[7]
  • 3 year treatment of woodchuck model of CHB  sustained antiviral efficacy and prolonged life spans without detectable emergence of resistance[8]
  • Efficacy # LVD resistant HBV replication in vitro[9]
  • Superior activity compared to LVD invivo for both HBeAg + & HBeAg- patients[10][11]
  • Efficacy in LVD refractory CHB patients[12]


References

  1. ^ Sims KA, Woodland AM (December 2006). "Entecavir: a new nucleoside analog for the treatment of chronic hepatitis B infection". Pharmacotherapy 26 (12): 1745–57. doi:10.1592/phco.26.12.1745. PMID 17125436. http://www.atypon-link.com/doi/abs/10.1592/phco.26.12.1745. 
  2. ^ Slusarchyk, W. A., A. K. Field, J. A. Greytok, P. Taunk, A. V. Tooumari, M. G. Young, and R. Zahler. 4-Hydroxy-3-(hydroxymethyl)-2-methylcyclopentyl purines and pyrimidines, a novel class of anti-herpesvirus agents. Abstract from the Fifth International Conference on Antiviral Research. Antivir Res 1992.17(Suppl. 1):98
  3. ^ Bisacchi, G. S., S. T. Chao, C. Bachard, J. P. Daris, S. F. Innaimo, J. A. Jacobs, O. Kocy, P. Lapointe, A. Martel, Z. Merchant, W. A. Slusarchyk, J. E. Sundeen, M. G. Young, R. Colonno, and R. Zahler. BMS-200475, a novel carbocyclic 29-deoxyguanosine analog with potent and selective antihepatitis B virus activity in vitro. Bioorg. Med. Chem. Lett. 1997. 7:127–132
  4. ^ Bisacchi, G. S., S. T. Chao, C. Bachard, J. P. Daris, S. F. Innaimo, J. A. Jacobs, O. Kocy, P. Lapointe, A. Martel, Z. Merchant, W. A. Slusarchyk, J. E. Sundeen, M. G. Young, R. Colonno, and R. Zahler. BMS-200475, a novel carbocyclic 29-deoxyguanosine analog with potent and selective antihepatitis B virus activity in vitro. Bioorg. Med. Chem. Lett. 1997. 7:127–132
  5. ^ Innaimo S F, Seifer M, Bisacchi G S, Standring D N, Zahler R, Colonno R J. Identification of BMS-200475 as a Potent and Selective Inhibitor of Hepatitis B Virus. Antimicrob. Agents Chemother. 1997. 41(7): 1444–1448
  6. ^ Seifer, M., R. K. Hamatake, R. J. Colonno, and D. N. Standring. In vitro inhibition of hepadnavirus polymerases by the triphosphates of BMS-200475 and lobucavir. Antimicrob. Agents Chemother. 1998. 42:3200–3208
  7. ^ Yamanaka, G., T. Wilson, S. Innaimo, G. S. Bisacchi, P. Egli, J. K. Rinehart, R. Zahler, and R. J. Colonno. Metabolic studies on BMS-200475, a new antiviral compound active against hepatitis B virus. Antimicrob. Agents Chemother. 1999. 43:190–193
  8. ^ Colonno, R. J., E. V. Genovesi, I. Medina, L. Lamb, S. K. Durham, M. L. Huang, L. Corey, M. Littlejohn, S. Locarnini, B. C. Tennant, B. Rose, and J. M. Clark. Long-term entecavir treatment results in sustained antiviral efficacy and prolonged life span in the woodchuck model of chronic hepatitis infection. J. Infect. Dis. 2001.184:1236–1245
  9. ^ Levine, S., D. Hernandez, G. Yamanaka, S. Zhang, R. Rose, S. Weinheimer, and R. J. Colonno. Efficacies of entecavir against lamivudine-resistant hepatitis B virus replication and recombinant polymerases in vitro. Antimicrob. Agents Chemother. 2002.46:2525–2532
  10. ^ Chang, T. T. A comparison of entecavir and lamivudine for HBeAg-positive chronic hepatitis B. N. Engl. J. Med. 2006. 354:1001–1010
  11. ^ Lai, C. L. et al. Entecavir versus lamivudine for patients with HBeAg-negative chronic hepatitis B. N. Engl. J.Med. 2006. 354:1011–1020.
  12. ^ Sherman, M., C. Yurdaydin, J. Sollano, M. Silva, Y. F. Liaw, J. Cianciara, A. Boron-Kaczmarska, P. Martin, Z. Goodman, R. J. Colonno, A. Cross, G. Denisky, B. Kreter, R. Hindes, and the AI463026 Behold Study Group. Entecavir for the treatment of lamivudine-refractory, HBeAg-positive chronic hepatitis B. Gastroenterology 2006. 130:2039–2049.

External links

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Hepatitis B (VII)
Multiple/general
Nucleic acid inhibitors
Multiple/unknown
ErbB2/PI3K Pathway
#WHO-EM. ‡Withdrawn from market. CLINICAL TRIALS: †Phase III. §Never to phase III

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