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For the treatment of depression, depression accompanied by anxiety, obsessive compulsive disorder and panic attacks
Paroxetine is a potent and highly selective inhibitor of neuronal serotonin reuptake. Paroxetine likely inhibits the reuptake of serotonin at the neuronal membrane, enhances serotonergic neurotransmission by reducing turnover of the neurotransmitter, therefore it prolongs its activity at synaptic receptor sites and potentiates 5-HT in the CNS; paroxetine is more potent than both sertraline and fluoxetine in its ability to inhibit 5-HT reuptake. Compared to the tricyclic antidepressants, SSRIs have dramatically decreased binding to histamine, acetylcholine, and norepinephrine receptors.
LD<sub>50</sub>=500mg/kg (orally in mice); Coma, dizziness, drowsiness, facial flushing, nausea, sweating, tremor, vomiting
completely absorbed after oral dosing
24 hours
Paroxetine is extensively metabolized and the metabolites are considered to be inactive. Paroxetine metabolism is mediated in part by CYP2D6, and the metabolites are primarily excreted in the urine and to some extent in the feces.