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Flibanserin
Systematic (IUPAC) name
1-[2-[4-(3-trifluoromethyl phenyl) piperazin-1-yl] ethyl] benzimidazol- [1H]-2-one
Identifiers
CAS number 167933-07-5
ATC code none
PubChem 6918248
Chemical data
Formula C20H21F3N4O 
Mol. mass 390.40 g/mol
Therapeutic considerations
Pregnancy cat.  ?
Legal status

Flibanserin (BIMT-17) is a drug produced by Boehringer Ingelheim.[1] It is currently being investigated as a drug for women with decreased sexual desire.[2] It is a 5-HT1A serotonin receptor agonist, a 5-HT2A serotonin receptor antagonist, and a dopamine D4 receptor partial agonist that had initially been developed as an anti-depressant.[3][4] As with Viagra, the effects of flibanserin were discovered serendipitously after it was trialled as an antidepressant.[5]. Although touted as "Female Viagra"[6] flibanserin does not work like any PDE5 inhibitors. Flibanserin does not play a part in transferring increased amounts of blood to the female genital region as PDE5 inhibitors do to the male genital region. Female HSDD (Hypoactive Sexual Desire Disorder) is not similar to its male counterpart Erectile Dysfunction in the way it is treated. Some have argued that Female Sexual Dysfunction is merely Disease Mongering [7] and a ploy to expand a market for sex drugs for women and to medicalization women's sexuality. [8]

Contents

Early results

On November 16, 2009, Boehringer Ingelheim reported that late-stage trials showed that the drug promoted sexual desire and increased the number of "satisfying sexual events" in women suffering from abnormally low libido.

The results of four Phase III studies involving more than 2,000 pre-menopausal women suffering from Hypoactive Sexual Desire Disorder (HSDD) were presented at the congress of the European Society for Sexual Medicine in Lyon, France. Women with the drug said that the average number of times they had "satisfying sexual experiences" rose from 2.8 to 4.5 times a month. However, women with the placebo said the number of times rose to 3.7 times a month. Flibanserin must be taken once a day and takes up to 4 weeks to have an effect. In animals, flibanserin increases dopamine and noradrenalin and decreases serotonin.[9] Flibanserin does not display consistent effects in animal models of anxiety and seems to exert potential antipsychotic effects. Flibanserin may induce some sedation but does not induce observable toxic effects at pharmacologically relevant doses. [10]

Mechanism of action

Flibanserin directly manipulates the chain of chemical reactions in the brain believed to trigger sexual desire[11]. This is unlike Procter & Gamble's hormone patch Intrinsa, which is targeted at post-menopausal women. However it is not precisely known how flibanserin enhances sexual desire.

Clinical trials

As of November 2009, Phase III clinical trials are assessing safety and efficacy in pre- and post-menopausal women.[12][13] These trials are based on a self-evaluation of sexual satisfaction experiences which is subjective and difficult to measure accurately.

See also

References

  1. ^ Borsini F, Evans K, Jason K, Rohde F, Alexander B, Pollentier S (summer 2002). "Pharmacology of flibanserin". CNS Drug Rev. 8 (2): 117–142. PMID 12177684. 
  2. ^ Jolly E, Clayton A, Thorp J, Lewis-D’Agostino D, Wunderlich G, Lesko L. Design of Phase III pivotal trials of flibanserin in female Hypoactive Sexual Desire Disorder (HSDD). Sexologies. Volume 17, Supplement 1, April 2008, Pages S133-S134. doi:10.1016/S1158-1360(08)72886-X
  3. ^ D'Aquila P, Monleon S, Borsini F, Brain P, Willner P (December 1997). "Anti-anhedonic actions of the novel serotonergic agent flibanserin, a potential rapidly-acting antidepressant". European Journal of Pharmacology 340 (2-3): 121–32. doi:10.1016/S0014-2999(97)01412-X. PMID 9537806. 
  4. ^ Invernizzi RW, Sacchetti G, Parini S, Acconcia S, Samanin R (August 2003). "Flibanserin, a potential antidepressant drug, lowers 5-HT and raises dopamine and noradrenaline in the rat prefrontal cortex dialysate: role of 5-HT(1A) receptors.". Br J Pharmacol. 139 (7): 1281–8. doi:10.1038/sj.bjp.0705341. PMID 12890707. PMC 1573953. http://www.nature.com/bjp/journal/v139/n7/full/0705341a.html. 
  5. ^ 'Female Viagra' discovery claim. BBC News, Tuesday, 17 November 2009
  6. ^ 'Female Viagra' discovery claim. BBC News, Tuesday, 17 November 2009
  7. ^ Female Sexual Dysfunction: A Case Study of Disease Mongering and Activist Resistance
  8. ^ [ http://sexualities.sagepub.com/cgi/content/abstract/9/3/363 The ‘Pinking’ of Viagra Culture: Drug Industry Efforts to Create and Repackage Sex Drugs for Women]
  9. ^ Limp reception for female 'libido booster,' Clare Wilson, New Scientist, 21 November 2009, p. 11
  10. ^ Pharmacology of flibanserin
  11. ^ "Boehringer Drug Shown to Kindle Female Sex Drive". ABC News. November 16, 2009. http://abcnews.go.com/Health/wireStory?id=9093634. Retrieved November 16, 2009. 
  12. ^ ClinicalTrials.gov NCT00996164
  13. ^ ClinicalTrials.gov NCT00996372

External links








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