Pharmacology
Paroxetine is the most potent and one of the most specific selective serotonin (5-hydroxytryptamine, 5-HT) reuptake inhibitors (SSRI). This activity of the drug on brain neurons is thought to be responsible for its antidepressant effects.
Its affinities are as follows:
- SERT (Ki = 0.04nM)
- NET (Ki = 90nM)
- DAT (Ki = 400nM)
Paroxetine is a phenylpiperidine derivative, chemically unrelated to the tricyclic or tetracyclic antidepressants. In receptor binding studies, paroxetine did not exhibit significant affinity for the adrenergic (α1, α2, β), dopaminergic, serotonergic (5HT1, 5HT2), or histamine receptors of rat brain membrane. A weak affinity for the muscarinic acetylcholine and noradrenaline receptors was evident. The predominant metabolites of paroxetine are approximately 1/50th the strength of paroxetine and are essentially inactive.
Paroxetine has been shown to have antimicrobial activity against several groups of microorganisms. This is mainly against Gram positive microorganisms. It also shows synergistic activity when combined with some antibiotics against several bacteria. Paroxetine has also been demonstrated to have antifungal activity being most potent against the hypersusceptible Candida albicans strain DSY1204.
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