Experiement: Flibanserin

[anacleta]

If approved by the FDA, Flibanserin will be the first drug on the market for women who report to have a lack of sexual drive. Soon will be presented a new proposal for approval to the FDA.


Flibanserin is a 5-HT1A receptor agonist and 5-HT2A receptor antagonist that had initially been investigated as an antidepressant.

Evidence from a variety of sources suggests that the neurotransmitter serotonin may have a role in Hypoactive sexual desire disorder by acting excessively as a sexual satiety signal. Serotonergic agents such as the selective serotonin reuptake inhibitors (SSRIs) inhibit all phases of sex including desire, arousal, and orgasm.
Addition of the 5-HT1A receptor partial agonist, buspirone, to SSRI treatment has been shown to counteract these negative sexual side effects. The 5-HT1A receptor mediates inhibitory neurotransmission.
Flibanserin, as a full 5-HT1A receptor agonist, is presumed to have similar or even more pronounced pro-sexual effects as buspirone.
Stimulation of the serotonin 5-HT2A receptor in male rodents has been associated with decreased sexual behavior. Thus, 5-HT2A antagonism is theorized to have pro-sexual effects.
Supporting this notion is the fact that nefazodone, an SSRI with inherent 5-HT2A receptor antagonist activity,
has fewer negative sexual side effects than other SSRIs without such activity.
Flibanserin has been shown to block central 5-HT2A receptors, and thus might reverse sexual inhibition caused by an excess of serotonin activity in the brain.
Although flibanserin’s effect is believed to be related to its activity at the 5-HT1A and 5-HT2A receptors, its mechanism of action in the treatment of HSDD is unknown.


http://www.fda.gov/downloads/Advisor.../UCM215437.pdf

[cyrus91]

i tried this drug, although i don't know if it was unadulterated or not, as i ordered it as a research chemical some odd years ago. it made me quite ill. i took it for about a week and i spent that week as a dizzied gastrointestinal mess and that's when i realized that i shouldn't order research chemicals. hah. that, or the drug just wasn't for me. oh, and no sexual benefits. that said, buspirone, which has a related mechanism of action, exerts a similar, albeit much more mild effect on me and also provides for no sexual benefits.

Sounds like you've tried a few different things Catalunya. What if anything has restored some sexual benefits for YOU since PSSD?

[brian6211]

i've tried a whole damn lot but stopped experimenting quite a while ago -- perhaps two years ago. i totally turned myself into a lab rat while i was desperate for a period of time some years ago.

what has restored a lot of sexual functioning? time.

i take zinc here and there before sex and that seems to help a bit, but i don't take anything to help sexually because everything that i've tried has wound up making things worse in some way or another.

worth mentioning that perhaps preventing full sexual healing is that i have to take a low dose of pregabalin (50mg/day) that i'm attempting to taper off of, although it's incredibly difficult, and a moderate dose of clonazepam daily to control panic disorder. i've been taking both for years and i, unfortunately, cannot function without an anxiolytic.

I hear you Catalunya about not being able to function without an anti-anxiety med. But have you tried Mirtazapine or Tradozone? My family doctor told me that he's willing to prescribe Lyrica(pregabalin) if the Mirtazapine, which I'm experimenting at the moment(3.5mg cutting the pill in 4), doesn't work and it doesn't. But at first Mirtazapine seemed to significantly increase libido but after 3-4 days, nothing.

And Catalunya, how long have you been dealing with PSSD?

[Ghost]

hey brian -- i actually have tried mirtazapine and trazodone and both of them produced the exact same response that you described, although for me the effect lasted only for about 1-2 days and not 3-4, and after that i was left off worse than before. same with cyproheptadine, nefazodone, and mianserin so i think the antagonization of one (or more) serotonin subtype just doesn't go over well with my penis. hah. they also aren't effective in controlling anxiety well enough for me. if by 'nothing' you mean that remeron is neutral for you, though, then you could very well up the dose and see what happens because you're on a really low dose of the drug.

careful with lyrica -- the drug can produce profound sexual dysfunction in higher doses and can cause sexual problems at even quite low doses for a whole lot of people. some of the most common side effects are sexual in nature with that drug. also, if you notice sexual side effects, reduce or get off the drug as quickly as possibly because physical dependency and withdrawal are very real with the substance. it's been incredibly difficult for me to try to wean off this drug and i'm not entirely sure that i'll be successful -- i have to be super careful not to relapse into a state of dysfunction.

i think that i've been dealing with pssd for either four or five years now, although my symptoms are much, much milder than they were at the start when i cold-turkeyed off of paroxetine after more than a decade of use. in retrospect, i should have tapered off of the drug to both prevent sexual problems and more importantly to have avoided an unnecessary relapse. i primarily suffer now from very low libido in terms of sexual maladies.

When did things start getting better, Catalunya?

[brian6211]

hey brian -- i actually have tried mirtazapine and trazodone and both of them produced the exact same response that you described, although for me the effect lasted only for about 1-2 days and not 3-4, and after that i was left off worse than before. same with cyproheptadine, nefazodone, and mianserin so i think the antagonization of one (or more) serotonin subtype just doesn't go over well with my penis. hah. they also aren't effective in controlling anxiety well enough for me. if by 'nothing' you mean that remeron is neutral for you, though, then you could very well up the dose and see what happens because you're on a really low dose of the drug.

careful with lyrica -- the drug can produce profound sexual dysfunction in higher doses and can cause sexual problems at even quite low doses for a whole lot of people. some of the most common side effects are sexual in nature with that drug. also, if you notice sexual side effects, reduce or get off the drug as quickly as possibly because physical dependency and withdrawal are very real with the substance. it's been incredibly difficult for me to try to wean off this drug and i'm not entirely sure that i'll be successful -- i have to be super careful not to relapse into a state of dysfunction.

i think that i've been dealing with pssd for either four or five years now, although my symptoms are much, much milder than they were at the start when i cold-turkeyed off of paroxetine after more than a decade of use. in retrospect, i should have tapered off of the drug to both prevent sexual problems and more importantly to have avoided an unnecessary relapse. i primarily suffer now from very low libido in terms of sexual maladies.

Well that's F***ing interesting for me and the effect of 3.75mg(cutting the pill of Mirt in 4 {15mg}) curing my anxiety 90-95% and feel that I don't need more than that(probably having serotonin receptors Fu**ed UP). Even today after 5 days on that dose, I feel it is too much for me, feeling numb'ish from head to toe. This weekend I will not take anything* and will update if you guys are interested.

Catalunya, you say it's hard for you to get off lyrica, because if you don't take it, you become severely anxious and can't function? I think I will hold off going on it for the reasons you mentioned and keep experimenting Mirtazapine for my anxiety.

When you mention relapse, do you mean OCD and Anxiety?

[brian6211]

oh, i thought that you meant that 3.75mg of mirtazapine wasn't working to control your anxiety very well at all.

and that's right about the lyrica taper being very difficult. as for relapse, i mean relapsing into a state of panic. i suffer from panic disorder. i do not suffer from ocd.

Oh I see, you got the other "monster"

[brian6211]

oh, i thought that you meant that 3.75mg of mirtazapine wasn't working to control your anxiety very well at all.

and that's right about the lyrica taper being very difficult. as for relapse, i mean relapsing into a state of panic. i suffer from panic disorder. i do not suffer from ocd.

Oh I see, you got the other "monster"

yup.

Well I have this girl from work that has been sharing with me that she has Panic Disorder as well. She takes Magnesium-Calcium (bla bla wtv natural product) and says that it cured it for her60-70%). Have you been blood tested for any deficiencies in your body(vitamin/mineral) wise?

[brian6211]

Have you tried all the benzodiazepines available on the market? Cuz from what I read(I've never taken any btw), there are many different types. Maybe some of them are less acting on the serotonin system..

[brian6211]

Have you tried all the benzodiazepines available on the market? Cuz from what I read(I've never taken any btw), there are many different types. Maybe some of them are less acting on the serotonin system..

they're all less-acting on the serotonergic system -- i don't think any of the commonly prescribed benzos touch serotonin save for klonopin. the problem is that i'm taking 3mg/day of klonopin (fda and ema max recommended dose for panic disorder is 4mg/day, so my dose is not insignificant, although at least it's within reasonable limits), thus a switch to valium/diazepam isn't doable bc the equivalent dose would be insanely high -- same for tranxene/clorazepate. i would double my dose if i were to switch to ativan/lorazepam or xanax xr/alprazolam because their half-lives are much shorter and would require bid or tid dosing schedules (i'm currently taking all 3mg of klonopin at once in the morning which keeps me steady enough and lets the serum level drop a bit by evening which allows for sex -- i'm usually ready to go in the middle of the day, though things are much more fun at night).

that said, i kinda think the serotonergic properties that klonopin possesses are really helping keep me stable. when i was switched over to equivalent doses of xanax xr and ativan i fell ill and never recovered until i placed back on klonopin. my sexual functioning totally worsened as well, but that could have been due to the insanely high levels of anxiety i was experiencing. when i experimented and tried to take xanax xr as well as ativan once daily, i experienced interdose rebound anxiety.

i'm kinda in a shitty situation with the benzodiazepines, but the drug has allowed me to have a social life, work my way through graduate school, and hold down a full-time career. i'm now 29 and trying to wean off of pregabalin without compromising stability as i've been on that drug for years as well. ugh.

thanks for your suggestions, man -- i really appreciate them. i've thought everything through, though, it seems. at the very least i can't complain that the sexual maladies i suffer from are as intense or life-changing as those that some others have to live with.

I see that you have tried all options, hehe. And I'm impressed that you were able to go to gradute school! Like Damn, how were you able to study while anxious like that?! I mean I tried University but had to drop out due to Anxiety and OCD. I'm thankful that I have a very stable job in a Bank and make a decent income and have all kinds of social benefits(insurance, stock options, etc...).

[brian6211]

re: studying through grad school -- well, because i wasn't anxious as i was / am in remission.

i'm glad that you have a really stable job, though, and that that job has a number of benefits that are there for you should you need them, particularly medical insurance.

is remeron sexually neutral for you or are there negative sexual side effects (not counting the initial libido boost when you first began the med)? if remeron is too sedating for you, another option if you live in the united states that *usually* is devoid or at least minimal on the sexual-side-effect front is nefazodone.

Well the initial libido increase has kind of faded away. The sexual side effect I get from remeron is some anesthesia, although not severe but still significant. I live in Canada and nefazodone is illegal here. Anyway, I thought of trying Trazodone if Mirtazapine is causing to much problems sexually. And I'm still experimenting and I'm not taking anything this weekend. So I'll see what happens..