Paroxetine: Difference between revisions
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| generic | | generic = Paroxetine (HCl; mesylate as Pexeva) | ||
| brand | | brand = Paxil (IR), Paxil CR (controlled-release), Brisdelle (low-dose for menopausal vasomotor symptoms), Pexeva (paroxetine mesylate) | ||
| structure | | structure = | ||
| classes | | classes = [[:Category:SSRIs|Selective serotonin reuptake inhibitor (SSRI)]], [[:Category:Antidepressants|Antidepressant]], [[:Category:Anxiolytics|Anxiolytic]] | ||
| | | uses = <vote slug="major-depressive-disorder-use">Major depressive disorder (FDA)</vote>, <vote slug="generalized-anxiety-disorder-use">Generalized anxiety disorder (FDA)</vote>, <vote slug="social-anxiety-disorder-use">Social anxiety disorder (FDA)</vote>, <vote slug="panic-disorder-use">Panic disorder (FDA)</vote>, <vote slug="ocd-use">Obsessive-compulsive disorder (FDA)</vote>, <vote slug="ptsd-use">Posttraumatic stress disorder (FDA)</vote>, <vote slug="premenstrual-dysphoric-disorder-use">Premenstrual dysphoric disorder (Paxil CR; FDA)</vote>, <vote slug="menopausal-vasomotor-use">Menopausal vasomotor symptoms (Brisdelle 7.5 mg; FDA)</vote> | ||
| uses | | starting_dose = MDD/GAD: 20 mg PO once daily. Panic disorder: 10 mg titrating to 40 mg. OCD: 20 mg titrating to 40-60 mg. CR: 25 mg/day. Brisdelle: 7.5 mg at bedtime for hot flashes | ||
| starting_dose | | preparations = IR tablets 10, 20, 30, 40 mg; CR tablets 12.5, 25, 37.5 mg; oral suspension 10 mg/5 mL; Brisdelle capsules 7.5 mg | ||
| preparations | | fda_max = 50 mg/day (IR); 62.5 mg/day (CR); 60 mg/day (OCD) | ||
| fda_max = | | pill_id = | ||
| routes | | routes = Oral | ||
| onset | | onset = Antidepressant effect emerges over 1-2 weeks | ||
| duration | | duration = 24 hours (once-daily dosing) | ||
| halflife | | halflife = ~21 hours (with nonlinear pharmacokinetics from CYP2D6 autoinhibition)<ref name="paxil-label">FDA Prescribing Information, Paxil (paroxetine hydrochloride), GSK/Apotex, current revision. https://www.accessdata.fda.gov/drugsatfda_docs/label/2012/020031s067,020710s031.pdf</ref> | ||
| bioavailability = Highly variable due to saturable first-pass metabolism<ref name="paxil-label" /> | |||
| pregnancy = '''Among the least preferred SSRIs in pregnancy.''' Observational signal for cardiac malformations (atrial and ventricular septal defects) with first-trimester exposure, and the most severe neonatal adaptation syndrome of any SSRI with third-trimester exposure<ref name="paxil-label" /> | |||
| legal = [[USLegal:Prescription only|Rx-only]] in US. Carries the antidepressant '''Boxed Warning''' for suicidality in children, adolescents, and young adults<ref name="paxil-label" /> | |||
| mechanism = <vote slug="paroxetine-mech-claim">Selective serotonin reuptake inhibitor with additional mild norepinephrine reuptake inhibition and the most anticholinergic activity of any SSRI, which underlies the relatively greater burden of sedation, weight gain, dry mouth, constipation, and sexual dysfunction compared to other SSRIs.</vote> Paroxetine is a '''strong CYP2D6 inhibitor and autoinhibitor''', producing nonlinear pharmacokinetics and substantial interactions with CYP2D6 substrates (tricyclic antidepressants, certain β-blockers, tamoxifen, certain neuroleptics). The worst-in-class discontinuation syndrome among SSRIs follows from the short effective half-life combined with strong serotonin transporter occupancy; slow taper is essential after extended use<ref name="cpic-ssri">CPIC Guideline for CYP2D6 and CYP2C19 Genotypes and Dosing of Selective Serotonin Reuptake Inhibitors, 2023. https://cpicpgx.org/guidelines/guideline-for-selective-serotonin-reuptake-inhibitors-and-cyp2d6-and-cyp2c19/</ref>. | |||
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== References == | |||
<references /> | |||
[[Category:SSRIs]] | |||
[[Category:Antidepressants]] | [[Category:Antidepressants]] | ||
[[Category:Anxiolytics]] | |||