Drug intelligence / Profile preview

drospirenone + ethinylestradiol + fluoxetine

Development stage
Unknown
Lead developer
Cairo University
Modality
Small Molecules
Administration
Oral
01

Overview

Drospirenone + ethinylestradiol + fluoxetine is a combination therapy being investigated by Cairo University for the treatment of severe premenstrual syndrome (PMS). This regimen combines a fourth-generation combined oral contraceptive (COC), specifically Yasmin (containing the progestin drospirenone and the estrogen ethinylestradiol), with the selective serotonin reuptake inhibitor (SSRI) fluoxetine. Drospirenone acts as a progesterone receptor agonist to inhibit ovulation and a mineralocorticoid receptor antagonist to reduce water retention, while ethinylestradiol provides estrogenic support. Fluoxetine targets the serotonin transporter (SERT) to increase synaptic serotonin levels, addressing the neuropsychiatric symptoms of PMS. The trial evaluates whether the synergistic effect of hormonal stabilization and serotonergic modulation provides superior relief compared to monotherapy or placebo.

Brand names
YasminProzacSarafem
Other names
Yasmin + fluoxetineCombined oral contraceptives + fluoxetine
02

Targets

MR (Mineralocorticoid receptor)SERT (Sodium-dependent serotonin transporter)ER (Estrogen receptor)CYP3A4 (Cytochrome P450 3A4)PR (Progesterone receptor)AR (Adrenergic receptors)

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