Description
Fluoxetine Hcl is the hydrochloride salt form of fluoxetine, a diphenhydramine derivative and selective serotonin reuptake inhibitor with antidepressant, anti-anxiety, antiobsessional and antibulimic activity and with potential immunomodulating activity.
Biological Activity
Fluoxetine Hcl is a selective serotonin reuptake inhibitor. Binds to the human 5-HT transporter with a Ki of 0.9 nmol/l and is between 150- and 900-fold selective over 5-HT1A, 5-HT2A, H1, α1, α2-adrenergic, and muscarinic receptors. Fluoxetine also inhibits assembly and activation of the NLRP3-ASC inflammasome and prevents degeneration of retinal pigmented epithelium (RPE) cells in an animal model of dry age-related macular degeneration (AMD).
Mechanism of action
Upon administration, fluoxetine binds to the presynaptic serotonin (5-HT) receptor resulting in negative allosteric modulation of the receptor complex, thereby blocking recycling of serotonin by the presynaptic receptor. Inhibition of serotonin reuptake by fluoxetine enhances serotonergic function through serotonin accumulation in the synaptic space, resulting in long-term desensitization and downregulation of 5-HT receptors, preventing 5-HT-mediated signaling and leading to antidepressant, anti-anxiety, antiobsessional and antibulimic effects.
Side effects
Common effects include: agitation, hallucinations, fever, sweating, shivering, fast heart rate, muscle stiffness, twitching, loss of coordination, nausea, vomiting, or diarrhea.
