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|Storage:||Shading, Confined Preservation||Usage:||Increase Woman Sex Desire|
Flibanserin White Raw Powder 167933-07-5 for Increasing Woman Sex Desire
Product name: Flibanserin
Appearance: white powder
Purity: over 99%
Usage: Female libido booster
|CAS No.||167933-07-5||Outer Packing||1Kg|
|Production date||2016.03.07||Shelf life||2018.03.06|
|Standard adopted||In-house quality standard|
|Items of analysis||Specification||Results|
|Appearance||White to off-white powder||White powder|
|Loss on drying||Less than 0.5%||0.13%|
|Heavy metals||Less than10ppm||Conforms|
|Other impurity||Any other impurity: Less than 0.3%||0.081%|
|Other impurity||Total of all other impurity: Less than 1.0%||0.14%|
|Assay (HPLC)||More than 99.0%||99.86%|
|Residual solvents(GC)||Ethanol: Less than 500ppm||42ppm|
|Residual solvents(GC)||Ethyl acetate: Less than 500ppm||ND|
This medication is used to treat women who have not gone through menopause who have low sexual desire and are concerned about it.
Flibanserin should not be used to treat low sexual desire caused by: a medical or mental/mood disorder, problems in the relationship, or the effects of other drugs. This medication should not be used by women who have gone through menopause, or by men. Flibanserin is not used to enhance sexual performance.
Mechanism of action:
Flibanserin acts as a full agonist in the frontal cortex and the raphe dorsalis, but only as a partial agonist in the CA3 region of the hippocampus of the 5-HT1A receptor (Ki = 1 nM in CHO cells, but only 15–50 nM in cortex, hippocampus and dorsal raphe) and, with lower affinity, as an antagonist of the 5-HT2A receptor (Ki = 49 nM) and antagonist or very weak partial agonist of the D4 receptor (Ki = 4–24 nM).Despite the much greater affinity of flibanserin for the 5-HT1A receptor, and for reasons that are unknown (although it might be caused by the competition with endogenous serotonin), flibanserin occupies the 5-HT1A and 5-HT2A receptors in vivo with similar percentages.Flibanserin also has low affinity for the 5-HT2B receptor (Ki = 89.3 nM) and the 5-HT2C receptor (Ki = 88.3 nM), both of which it behaves as an antagonist of.Flibanserin preferentially activates 5-HT1A receptors in the prefrontal cortex, demonstrating regional selectivity, and has been found to increase dopamine and norepinephrine levels and decrease serotonin levels in the rat prefrontal cortex, actions that were determined to be mediated by activation of the 5-HT1A receptor.As such, flibanserin has been described as a norepinephrine–dopamine disinhibitor (NDDI).
The proposed mechanism of action refers to the Kinsey dual control model of sexual response.Various neurotransmitters, sex steroids, and other hormones have important excitatory or inhibitory effects on the sexual response. Among neurotransmitters, excitatory activity is driven by dopamine and norepinephrine, while inhibitory activity is driven by serotonin. The balance between these systems is of significance for a normal sexual response. By modulating serotonin and dopamine activity in certain parts of the brain, flibanserin may improve the balance between these neurotransmitter systems in the regulation of sexual response.
DOSAGE AND ADMINISTRATION:
The recommended dosage of ADDYI is 100 mg administered orally once per day at bedtime. ADDYI is dosed at bedtime because administration during waking hours increases the risks of hypotension, syncope, accidental injury, and central nervous system (CNS) depression (such as somnolence and sedation).
If a dose of ADDYI 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.
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