Flibanserin

Vallejos, Ximena; Wu, Christine Xia

doi:10.1177/0897190016630409

Cited by 8 publications

(3 citation statements)

References 10 publications

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“…Flibanserin (FLB; 2H-benzimidazol-2-one, 1,3-dihydro-1-[2-[4-[3(tri-fluoromethyl) phenyl]-1-piperazinyl]ethyl] was approved by US FDA in August 2015 under the trade name of Addyi ® for treating premenopausal woman with generalized hypoactive sexual desire disorder (HSDD), which is the most common form of female sexual dysfunction that is associated with emotional distress and relationship problems [ 1 , 2 ]. FLB is a non-hormonal drug that selectively binds to serotonin receptors in the central nervous system (CNS).…”

Section: Introductionmentioning

confidence: 99%

RETRACTED: Intranasal Niosomal In Situ Gel as a Promising Approach for Enhancing Flibanserin Bioavailability and Brain Delivery: In Vitro Optimization and Ex Vivo/In Vivo Evaluation

et al. 2020

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Flibanserin (FLB) is a multifunctional serotonergic agent that was recently approved by the FDA for the oral treatment of premenopausal women with hypoactive sexual desire disorder. FLB is a centrally acting drug that has a low oral bioavailability of 33% owing to its exposure to the hepatic first-pass effect, as well as its pH-dependent solubility, which could be an obstacle hindering the drug dissolution and absorption via mucosal barriers. Thus, this work aimed at overcoming the aforementioned drawbacks and promoting the nose-to-brain delivery of FLB via the formulation of an intra-nasal in situ niosomal gel. The Box–Behnken design was employed to study the impact of Span® 85 concentration (X1), hydration time (X2), and pH of the hydrating buffer (X3) on the vesicle size and drug entrapment. The optimized formulation exhibited a spherical shape with a vesicular size of 46.35 nm and entrapment efficiency of 92.48%. The optimized FLB niosomes integrated into gellan gum-based in situ gel exhibited enhanced ex vivo permeation and improved plasma and brain concentrations after nasal administration in rats compared to raw FLB. These findings highlight the capability of the proposed intra-nasal FLB niosomal in situ gel to boost the drug bioavailability and to promote its direct delivery to the brain.

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Section: Introductionmentioning

confidence: 99%

RETRACTED: Intranasal Niosomal In Situ Gel as a Promising Approach for Enhancing Flibanserin Bioavailability and Brain Delivery: In Vitro Optimization and Ex Vivo/In Vivo Evaluation

et al. 2020

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“…Інформація щодо використання фармакологічних засобів , які були б ефективними при лікуванні жіночих оргазмічних розладів, накопичується та вдосконалюється, і буде представлена в подальших публікаціях [105,106,107].…”

Section: варіанти лікуванняunclassified

Порушення Оргазму У Жінок

Ромащенко

2023

UJMH

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В статті Ромащенко О.В. «Порушення оргазму у жінок» представлено аналіз літературних даних щодо оцінки жіночого оргазму з різних точок зору (клінічної, етіологічної, фізіологічної, психологічної, соціологічної), в тому числі з урахуванням дефініцій, типів оргазму.Проаналізовано передумови розладу оргазму у жінок у відповідності до сучасної класифікації жіночих сексуальних дисфункцій, особливостей механізмів формування порушень оргазму у жінок з урахуванням психосоціальних факторів, нейрофізіологічних розладів, гормонального гомеостазу.Представлено механізми формування розладів оргазму у жінок у відповідності до їх різновидності, вікових етапів життя жінки.Висвітлено роль жіночого оргазму у збереженні фертильної функції.Представлено клінічні алгоритми ведення пацієнток з оргазмічними розладами та підходи до вибору та проведення терапії за таких умов.

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“…Flibanserin is a N-alkylpiperazine compound chemically known as 1-(2-(4-(3-trifluoromethylphenyl) piperazin-1-yl)ethyl)benzimidazol(1H)-2-one as a P-Glycoprotein inhibitor 25 . It works as a 5-hydroxytryptamine 1A (5-HT 1A ) agonist and 5-hydroxytryptamine 2A (5-HT 2A ) antagonist 26 .…”

Section: Flibanserin-a Wonder Drugmentioning

confidence: 99%

Flibanserin: A Miracle Drug in Management of Hypoactive Sexual Desire Disorder in Female

2020

IJFMT

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Female sensuality encircles wide range of behaviours and activities, including female sexual identity and etiquette. Many dimensions of female sexuality have been addressed by various societies and religions of the world, pertaining to biological sex, orientations and attitudes. A sufficient sexual appetite and libido in adults are essential for continuation of race. It also nurtures psychological health and immune functions. In case of hypoactive sexual desire, there will be recurrent deficiency or absence of interest and receptivity to sexual activities which causes distress and many interpersonal difficulties in fledged adult life. Flibanserin is the latest approved drug for the treatment of hypoactive sexual desire disorder in female. It generally functions on the activity and the role of neurotransmitters affecting mood and drives. Flibanserin has affinity with serotonin autoreceptor (5-HT 1A ) and dopamine receptor (D 4 ). It is a full-fledged agonist of 5-HT 1A in prefrontal cortex region and partial agonist in the CA3 region of hippocampus. It also acts as partial agonist of dopamine receptor (D 4 ) but it has poor antagonist property with 5-HT 2A , 5-HT 2B and 5-HT 2C receptors. Flibanserin declines neuronal firing rate generally in the cells of hippocampus, dorsal raphe and cortex region of brain. Hence, it can assist to improve the brain activation pattern and drives of hypoactive women.

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Flibanserin

Abstract: Flibanserin, a novel, nonhormonal agent that modulates excitatory and inhibitory neurotransmitters was studied in premenopausal women and has shown efficacy in improving sexual desire and SSEs.

Cited by 8 publications

References 10 publications

RETRACTED: Intranasal Niosomal In Situ Gel as a Promising Approach for Enhancing Flibanserin Bioavailability and Brain Delivery: In Vitro Optimization and Ex Vivo/In Vivo Evaluation

RETRACTED: Intranasal Niosomal In Situ Gel as a Promising Approach for Enhancing Flibanserin Bioavailability and Brain Delivery: In Vitro Optimization and Ex Vivo/In Vivo Evaluation

Порушення Оргазму У Жінок

Flibanserin: A Miracle Drug in Management of Hypoactive Sexual Desire Disorder in Female

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