BRISDELLE
Clinical safety rating
cautionComprehensive clinical and safety monograph for BRISDELLE (BRISDELLE).
Selective serotonin reuptake inhibitor (SSRI); paroxetine is the active ingredient. Enhances serotonergic activity by blocking serotonin reuptake into presynaptic neurons, augmenting serotonin levels in the synaptic cleft.
| Metabolism | Extensively metabolized in the liver via cytochrome P450 enzymes, primarily CYP2D6. Metabolites are glucuronidated and excreted renally. |
| Excretion | Primarily renal excretion as metabolites; approximately 60% of a radiolabeled dose is recovered in urine and 30% in feces over 10 days. Less than 1% excreted unchanged. |
| Half-life | Terminal elimination half-life is approximately 9-11 hours for paroxetine (the active ingredient in Brisdelle). This supports once-daily dosing; steady-state is achieved within 7-14 days. |
| Protein binding | Approximately 95% bound to plasma proteins, primarily to albumin and alpha-1 acid glycoprotein. |
| Volume of Distribution | Volume of distribution is about 3-28 L/kg (mean ~13 L/kg), indicating extensive tissue distribution. |
| Bioavailability | Oral bioavailability is approximately 50-100% due to extensive first-pass metabolism; absolute bioavailability is about 50% for the immediate-release formulation. |
| Onset of Action | Onset of clinical effect for vasomotor symptoms is typically observed within 2-4 weeks of daily oral dosing. |
| Duration of Action | Duration of action approximately 24 hours with once-daily dosing due to the half-life; continuous administration is required for sustained effect. |
| Molecular Weight | 329.37 |
8 mg orally once daily, taken at bedtime.
| Dosage form | CAPSULE |
| Renal impairment | No dose adjustment required for mild-to-moderate renal impairment (CrCl ≥ 30 mL/min). For severe renal impairment (CrCl < 30 mL/min) or end-stage renal disease, not recommended due to lack of data. |
| Liver impairment | Mild hepatic impairment (Child-Pugh A): no adjustment. Moderate hepatic impairment (Child-Pugh B): maximum dose 4 mg orally once daily. Severe hepatic impairment (Child-Pugh C): contraindicated. |
| Pediatric use | Not approved for use in pediatric patients; safety and efficacy not established. |
| Geriatric use | For patients >65 years, start with 4 mg orally once daily at bedtime; may increase to 8 mg once daily based on response and tolerability. Monitor closely for sedation and falls. |
| 1st trimester | Paroxetine is classified as Pregnancy Category D. Studies have shown an increased risk of congenital malformations, particularly cardiovascular defects, when used during the first trimester. Use is contraindicated unless no safer alternative exists. |
| 2nd trimester | Second trimester exposure carries a risk of persistent pulmonary hypertension of the newborn (PPHN) and other adverse effects. Limited data suggest possible neurodevelopmental effects. |
| 3rd trimester | Third trimester use is associated with risk of neonatal adaptation syndrome (including respiratory distress, feeding difficulties, and irritability) and persistent pulmonary hypertension. Avoid if possible; if necessary, monitor neonate closely. |
Clinical note
Comprehensive clinical and safety monograph for BRISDELLE (BRISDELLE).
| Placental transfer | Paroxetine crosses the placenta with fetal serum concentrations approximately 70-80% of maternal levels, indicating moderate transfer. |
| Breastfeeding | Paroxetine is excreted into human breast milk in small amounts. Relative infant dose is estimated at 1-2% of maternal weight-adjusted dose. Reports of irritability, poor feeding, and drowsiness in breastfed infants exist. The American Academy of Pediatrics recommends cautious use, usually compatible with breastfeeding, but monitor infant for adverse effects. Avoid in preterm or compromised infants. |
| Lactation Rating | L2 (Safer) |
| Teratogenic Risk | Pregnancy Category C. In animal studies, paroxetine (active ingredient of Brisdelle) has been associated with increased fetal malformations (including cardiovascular) at doses greater than human therapeutic doses. In humans, retrospective studies suggest a small increased risk of congenital heart defects (primarily ventricular septal defects) with first-trimester exposure. Third-trimester exposure may increase risk for persistent pulmonary hypertension of the newborn (PPHN) and neonatal withdrawal syndrome (respiratory distress, feeding difficulties, jitteriness). |
| Fetal Monitoring | Monitor pregnant women for emergence or worsening of depression/anxiety. For neonates exposed in third trimester, monitor for signs of withdrawal (respiratory distress, feeding difficulties, irritability) and PPHN. Routine fetal ultrasound may be considered for first-trimester exposure due to possible cardiac malformation risk. |
| Fertility Effects | Paroxetine has been associated with sexual dysfunction (decreased libido, ejaculatory delay) in both men and women, which may affect fertility. Animal studies have shown no major impairment of fertility, but human data are limited. Consider potential impact on conception. |
■ FDA Black Box Warning
Increased risk of suicidal thinking and behavior in children, adolescents, and young adults with major depressive disorder and other psychiatric disorders.
| Serious Effects |
Concomitant use with monoamine oxidase inhibitors (MAOIs) or within 14 days of discontinuing MAOI treatmentConcomitant use with pimozideConcomitant use with thioridazineKnown hypersensitivity to paroxetine or any excipientsPregnancy (especially first trimester) due to teratogenicity
| Precautions | Suicidality risk in young adults, Serotonin syndrome with concurrent serotonergic drugs, Bone fractures risk, Sexual dysfunction, Abnormal bleeding risk, Angle-closure glaucoma risk, Hyponatremia in elderly or volume-depleted patients, Discontinuation syndrome upon abrupt withdrawal, Pregnancy: Potential harm to neonates (persistent pulmonary hypertension, serotonin syndrome), Lactation: Excreted in breast milk |
| Food/Dietary | Avoid alcohol due to additive central nervous system depression. No specific food interactions; take without regard to meals. |
| Clinical Pearls | BRISDELLE (paroxetine mesylate) is a selective serotonin reuptake inhibitor (SSRI) indicated for vasomotor symptoms (VMS) in menopause. It is the only non-hormonal therapy FDA-approved for moderate to severe VMS. Dosing starts at 7.5 mg once daily, typically at bedtime to minimize daytime sedation. Avoid concurrent use with MAOIs, other SSRIs/SNRIs, or strong CYP2D6 inhibitors (e.g., paroxetine itself). Monitor for serotonin syndrome, especially with triptans or linezolid. Discontinue gradually to avoid withdrawal symptoms. Note that paroxetine is pregnancy category D; use effective contraception. |
| Patient Advice | Take BRISDELLE at bedtime to reduce daytime drowsiness. · Do not crush or chew the capsule; swallow whole. · It may take 2–4 weeks to see full benefit for hot flashes. · Avoid alcohol as it can increase sedation. · Do not stop suddenly; taper under medical guidance. · Report any suicidal thoughts, worsening depression, or unusual behavior changes. · Contact doctor if you experience severe headache, nausea, or rapid heartbeat (serotonin syndrome). · Store at room temperature away from moisture and heat. |
Loading safety data…