Bupropion/naltrexone

Bupropion/naltrexone
Bupropion/naltrexone
Combination of
Bupropion norepinephrine/dopamine reuptake inhibitor
Naltrexone opioid receptor antagonist
Clinical data
Pregnancy cat.  ?
Legal status  ?
Identifiers
ATC code  ?
 YesY(what is this?)  (verify)

Bupropion/naltrexone (proposed trade name Contrave) is an experimental treatment for obesity in phase III clinical trials.[1] Currently being developed by Orexigen[2] in a sustained-release formulation, it is a combination of two approved drugs, bupropion and naltrexone. Both drugs have individually shown some evidence of effectiveness in weight loss, and the combination is expected to have a synergistic effect.[3] In clinical trials, patients taking Contrave combined with diet and exercise lost more weight than patients taking a placebo and following the same diet and exercise program.[4] On 31 March 2010, Orexigen submitted a New Drug Application (NDA) to the U.S. Food and Drug Administration (FDA) for this drug combination.[5] On 7 December 2010, an FDA Advisory Committee voted 13-7 for the approval of Contrave, and voted 11-8 for the conduct of a post-marketing cardiovascular outcomes study.[6] Contrave's PDUFA date is 31 January 2011. Subsequently, on 2 February 2011, the FDA rejected the drug and it was decided that an extremely large-scale study of the long-term cardiovascular effects of Contrave would be needed, before approval could be considered.[7] The recommended daily dose of Contrave is two (8 mg naltrexone/90 mg bupropion) tablets taken twice daily (4 tablets total - 32 mg naltrexone, 360 mg bupropion). Upon initiation, the drug will be started with a quarter-dose (or one tablet) for one week and a pill will be added to the regimen each week until the full recommended dose is reached on Week 4.

During phase 2 testing, different dosages were used in a once daily formula. These include:

  • 16 mg naltrexone - 400 mg bupropion
  • 32 mg naltrexone - 400 mg bupropion
  • 48 mg naltrexone - 400 mg bupropion

The second dosage (32 mg-400 mg) on average showed the best benefit-to-risk ratio.

Treatment is designed to influence the hypothalamus in order to decrease food intake over an extended period of time. Studies of almost 700 patients, 90% female, ran up to 56 weeks. The control group, overall, lost 5% of their initial body weight, or 11-16 lbs. The experimental (medicated) group lost 20-23 lbs during the same amount of time. The average starting weight for participants was 223 lbs.[8] Current medical weight loss medications average 5-22 lbs lost in 6 months.[9][unreliable source?]

References

  1. ^ Plodkowski, Raymond A.; Nguyen, Quang; Sundaram, Umasankari; Nguyen, Loida; Chau, Diane L.; St. Jeor, Sachiko (2009). "Bupropion and naltrexone: a review of their use individually and in combination for the treatment of obesity". Expert Opinion on Pharmacotherapy 10 (6): 1069–1081. doi:10.1517/14656560902775750. PMID 19364254. 
  2. ^ Obesity expert named Life Scientist of the Year
  3. ^ Sinnayah P, Wallingford N, Evans A, Crowley MA (2007). "Bupropion and naltrexone interact synergistically to decrease food intake in mice". Obesity 15 (9): A179. 
  4. ^ Positive 24-week Results For Contrave Phase III Obesity Treatment Study Reported By Orexigen, Medical News Today, 28 Sep 2006
  5. ^ Orexigen(R) Therapeutics Submits Contrave(R) New Drug Application to FDA for the Treatment of Obesity
  6. ^ www.orexigen.com
  7. ^ [1]
  8. ^ WebMD.com
  9. ^ WeightLossNYC.com, About Weight Loss Medications

Wikimedia Foundation. 2010.

Игры ⚽ Нужна курсовая?

Look at other dictionaries:

  • Naltrexone — Not to be confused with the related chemical naloxone. Naltrexone Systematic (IUPAC) name …   Wikipedia

  • Anti-obesity medication — Orlistat (Xenic …   Wikipedia

  • Anti-obesity drug — Anti obesity drugs or weight loss drugs refer to all pharmacological agents that reduce or control weight. These drugs alter one of the fundamental processes of the human body, weight regulation, by either altering appetite or metabolism.The main …   Wikipedia

  • Methadone — Phy redirects here. For the abbreviation for the physical layer of the OSI Model, see PHY. Not to be confused with Methedrine, Methedrone, Mephedrone, or Methylone. Methadone …   Wikipedia

  • Acamprosate — Systematic (IUPAC) name 3 Acetamidopropane 1 sulfonic acid Clinical data Pregnancy cat. C …   Wikipedia

  • Disulfiram — Systematic (IUPAC) name 1,1 ,1 ,1 [disulfanediylb …   Wikipedia

  • Management of obesity — The main treatment for obesity consists of dieting and physical exercise.[1] Diet programs may produce weight loss over the short term,[2] but maintaining this weight loss is frequently difficult and often requires making exercise and a lower… …   Wikipedia

  • Varenicline — Systematic (IUPAC) name 7,8,9,10 tetrahydro 6,10 methano 6H pyrazino (2,3 h)(3) benzazepine Clinical data Trade names …   Wikipedia

  • Psychoactive drug — An assortment of psychoactive drugs A psychoactive drug, psychopharmaceutical, or psychotropic is a chemical substance that crosses the blood–brain barrier and acts primarily upon the central nervous system where it affects brain function,… …   Wikipedia

  • Methamphetamine — Meth and Tik redirect here. For other uses, see Meth (disambiguation) and Tik (disambiguation). This article is about the psychostimulant drug, methamphetamine, in both racemic and dextrorotatory forms. For the CNS inactive OTC nasal decongestant …   Wikipedia

Share the article and excerpts

Direct link
Do a right-click on the link above
and select “Copy Link”