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Flibanserin; Uses, Dosage, Side Effects, Interactions, Pregnancy

Flibanserin is the first drug to be approved for hypoactive sexual desire disorder (HSDD) in premenopausal women by the FDA in August 2015. It was originally developed as an antidepressant medication by Boehringer Ingelheim, but showed lack of efficacy in trials and was further developed as a hypoactive sexual disorder drug is a medication approved for the treatment of pre-menopausal women with hypoactive sexual desire disorder (HSDD). The medication increases the number of satisfying sexual events per month by about one half over placebo from a starting point of about two to three. The certainty of the estimate is low. The side effects of dizziness, sleepiness, and nausea occur about three to four times more often.

Mechanism of Action of Flibanserin

Flibanserin’s mechanism of action is attributed to its high affinity for 5-HTA1 and 5-HTA2 receptors, displaying agonist activity on 5-HTA1 and antagonist on 5-HTA2, resulting in lowering of serotonin in the brain as well as an effect on increasing norepinephrine and dopamine neurotransmitters. Flibansetrin has a high affinity for serotonin receptors in the brain: it acts as an agonist on 5-HT1A and an antagonist on 5-HT2A. In vivo, flibanserin binds equally to 5-HT1A and 5-HT2A receptors. However, under higher levels of brain 5-HT (i.e., under stress), flibanserin may occupy 5-HT2A receptors in higher proportion than 5-HT(1A) receptors. It may also moderately antagonize D4 (dopamine) receptors and 5-HT2B and 5-HTB2C. Its action on neurotransmitter receptors may contribute to the reduction in serotonin levels and an increase in dopamine and norepinephrine levels, all of which may play part in reward processing.

Indications of Flibanserin

It is called the female viagra

Treatment of HSDD in postmenopausal women or in men.
To enhance sexual performance.
A co-existing medical or psychiatric condition,
Problems within the relationship, or
The effects of a medication or other drug substance
Poor control over intercourse
Sexual Dysfunction,
Persistent or recurrent ejaculation with minimal sexual stimulation before, on, or shortly after penetration and before the patient wishes; and
Marked personal distress or interpersonal difficulty as a consequence of PE; and
Poor control over ejaculation;
A history of premature ejaculation in the majority of intercourse attempts over the prior 6 months.
Sexual erectile dysfunction
Inability to sustain a satisfactory erection to complete intercourse

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Contra indications of Flibanserin

The habit of Drinking Too Much Alcohol
abnormally low blood pressure
Liver Problems
A Mother who is Producing Milk and Breastfeeding

Dosage of Flibanserin

Strengths : 100 mg

Hypoactive Sexual Desire Disorder

Indicated for premenopausal women with acquired, generalized hypoactive sexual desire disorder (HSDD) as characterized by the low sexual desire that causes marked distress or interpersonal difficulty and is not caused by a coexisting medical or psychiatric condition, problems within the relationship, or the effects of a medication or other drug substance
100 mg orally once daily at bedtime
Dosed at bedtime because administration during waking hours increases risks of hypotension, syncope, accidental injury, and central nervous system depression
Discontinued after 8 weeks if no improvement

Missed dose
- If a dose is missed at bedtime, instruct the patient to take the next dose at bedtime on the next day
- Instruct the patient to not double the next dose
CYP3A4 inhibitors
- Coadministration with moderate or strong CYP3A4 inhibitors is contraindicated
- If initiating flibanserin following moderate or strong CYP3A4 inhibitor use, start flibanserin 2 weeks after the last dose of the CYP3A4 inhibitor
- If initiating a moderate or strong CYP3A4 inhibitor following flibanserin use, start the moderate or strong CYP3A4 inhibitor 2 days after the last dose of flibanserin

Pediatric:

Not indicated for pediatric use

Dosing Considerations

Acquired HSDD refers to HSDD that develops in a patient who previously had no problems with sexual desire
Generalized HSDD refers to HSDD that occurs regardless of the type of stimulation, situation, or partner
Limitations of use

Side Effects of Flibanserin

The Most common

Constipation
sleepiness or unusual drowsiness
clumsiness or unsteadiness
dizziness
drowsiness
dry mouth
false sense of well-being
increased watering of mouth
lightheadedness
constipation;
vision changes;
breast swelling (in men or women); or
decreased sex drive, impotence, or difficulty having an orgasm.
blurred vision, tunnel vision, eye pain or swelling, or seeing halos around lights;
restless muscle movements in your eyes, tongue, jaw, or neck;
a light-headed feeling, like you might pass out;

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Common

Drowsiness and lightheadedness the day after taking the medicine.
Confusion.
Numbed emotions.
Visual disturbances such as blurred vision or double vision.
Shaky movements and unsteady walk (ataxia).
Loss of memory (amnesia).
Muscle weakness.
Dizziness.
A headache.
Skin rashes.
Disturbances of the gut such as diarrhea, c onstipation, nausea, vomiting or abdominal pain.
Difficulty in passing urine (urinary retention).
Changes in sex drive.
Low blood pressure (hypotension).
Blood disorders.
Jaundice.
Unexpected aggression, restlessness or irritability (tell your doctor if you experience this).
Nightmares or hallucinations (tell your doctor if you experience this).

Serious

agitation
anxiety
behavioral changes, including aggressiveness, angry outbursts, bizarre behavior, or decreased inhibitions
confusion
increased trouble sleeping
memory problems
muscle spasms
shortness of breath
signs of depression (e.g., poor concentration, changes in weight, changes in sleep, decreased interest in activities, thoughts of suicide)
sleepwalking

Drug Interactions of Flibanserin

Flibanserin may interact with following drugs, supplements & may change the efficacy of drugs

general anesthetics
antihistamines (e.g., cetirizine, doxylamine, diphenhydramine, hydroxyzine, loratadine)
antipsychotics (e.g., chlorpromazine, clozapine, haloperidol, olanzapine, quetiapine, risperidone)
aripiprazole
baclofen
barbiturates (e.g., butalbital, pentobarbital, phenobarbital)
benzodiazepines (e.g., alprazolam, diazepam, lorazepam)
bupropion
celecoxib
cilostazol
clopidogrel
cyclosporine
diabetes medications (e.g., chlorpropamide, metformin, nateglinide, rosiglitazone)
diltiazem
estrogens (e.g., conjugated estrogen, )
glucosamine
heparin
low molecular weight heparins
mirtazapine
monoamine oxidase inhibitors (MAOIs; e.g. rasagiline, selegiline, )
multivitamins
muscle relaxants
nifedipine
non-steroidal anti-inflammatory medications (NSAIDs; e.g., diclofenac, ibuprofen, naproxen)
omega-3 fatty acids
pentoxifylline
propranolol
quinolone antibiotics (e.g., ciprofloxacin, norfloxacin, ofloxacin)
rasagiline
seizure medications ( phenobarbital, phenytoin, valproic acid, )
selective serotonin reuptake inhibitors (SSRIs; e.g., citalopram, duloxetine, fluoxetine, paroxetine, sertraline)
serotonin antagonists (anti-emetic medications; e.g., granisetron, ondansetron)
tapentadol
theophyllines (e.g., aminophylline, oxtriphylline, theophylline)
thiazide diuretics (water pills; e.g., hydrochlorothiazide, )
thyroid replacements (e.g., dessicated thyroid, levothyroxine)
tizanidine
tramadol
tricyclic antidepressants (e.g., desipramine, nortriptyline)
triptans (e.g., sumatriptan, rizatriptan)

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Pregnancy & Lactation of Flibanserin

Pregnancy

It is not known if flibanserin will harm your unborn baby. There are no well-done studies that have been done in humans with flibanserin. In animal studies, pregnant animals were given flibanserin, and some babies had problems but were given high doses of flibanserin. Animal studies cannot rule out the potential for fetal harm.

Lactation

Tell your doctor if you are breastfeeding or plan to breastfeed.

It is not known if flibanserin crosses into human milk. Because many medications can cross into human milk and because of the possibility for serious adverse reactions in nursing infants with the use of this medication, breastfeeding is not recommended during treatment with flibanserin.