MECHANISM OF ACTION The actual mechanism of ssri are unknown They increase the extracellular level of serotonin by limiting its reabsoption in to the presynaptic receptor There will be large amount of serotonin in the synaptic cleft and available for postsynaptic receptor
PHARMACODYNAMICS SERT are glycoprotien with 12 membrane regions embded in axon terminaland cellbody membrane of seronergic neurons When extracellular serotonin binds to receptor on the transporter conformational changes occurs and moved to cell Combing with k+ results in release of serotonin SSRI’S inhibit the transport by binding with SERT receptor other than the serotonin binding site
FLOUXETINE Bicyclic compund First ssri Metabolised to norfluoxetine Inhibitor of CYP2D6 isoenzyme Plasma t ½ is 2 days Can’t be used in patients needed rapid effects Side effects are agitation and deramatological changes
FLUVOXAMINE Shorter acting T ½ of 18 hrs Used for OCD treatment Nausea, dyspepsia
PAROXETINE T ½ of 20 hours Short acting Sexual side effects and more of gasrtic side effects
SERTALINE Used in anxiety and post traumatic disoder T ½ is 20 hrs
CITALOPRAM T ½ is 33 hrs Death can occur in overdosage Used in mood changes in premenstrual syndrome
ESCITALOPRAM AND DAPOXETINE Esictalopam have same uses of citalopam Dapoxetine are ssri made to improve the sexual side effects of ssri’s