A Clinical Review on Paroxetine and Emerging Therapies for the Treatment of Vasomotor Symptoms

Figures & data

Table 1 SSRI/SNRI and CYP2D6 Activity

Potent Inhibitors	Moderate Inhibitors	Weak Inhibitors	No Activity CYP2D6
Fluoxetine	Sertraline	Citalopram	Venlafaxine
Paroxetine	Duloxetine	Escitalopram	Desvenlafaxine
Bupropion	Fluvoxetine		Mirtazapine

Table 2 Comparison of Non-Hormonal Options for Vasomotor Symptoms^{4,39,41,42,46,57,58}

Medication Name and Dose	Vasomotor Symptom Effect	Common Side Effects (%)	Additional concerns
SSRI Paroxetine mesylate 7.5 mg/d* Paroxetine HCl 10-25 mg/d** Citalopram 10-20 mg/d** Escitalopram 10-20 mg/d** SNRI Desvenlafaxine100-150 mg/d** Venlafaxine 37.5-150 mg/d**	Hot flash reduction from 25 – 69% Composite hot flash frequency and severity improved from 27 – 61%	Nausea or dizziness, which usually improves after 1 to 2 weeks	Avoid potent CYP2D6 inhibitors in Tamoxifen users Patients with bipolar disease, uncontrolled seizures, liver or kidney insufficiency, uncontrolled hyponatremia or poorly controlled hypertension, concurrent use of other SSRIs or SNRIs Black box warnings: uncommon suicidal thoughts within first few months
Gabapentinoids Gabapentin 900-2,400 mg/d** Pregabalin 150-300 mg/d**	31 – 89.5% reductions in VMS	Dizziness, unsteadiness, and drowsiness which usually improves by week 4	Lower doses often effective. Start with 100-300 mg at night and up titrate until effective dose Since drowsiness is a common adverse side effect of gabapentin, it may be a good choice for women with disruptive sleep from VMS
Emerging Options
Oxybutynin 5-15 mg/d**	50-77% reduction in hot flash frequency	Dry mouth, urinary issues, constipation	Anticholinergic side effects best tolerated at lower doses
Estetrol ** ‡	Reduction of weekly hot flashes: 66% at 4 weeks; 82% at 12 weeks	Further study needed	Further study needed to establish effective dose and safety
(NK3R) antagonists ** ‡	45% to 93% reduction in number of hot flashes	Further study needed	Further study needed to establish effective dose and safety

Abbreviations: SSRI = Selective Reuptake Inhibitor; SNRI = Selective Norepinephrine Reuptake Inhibitor; NK3R = Neurokinin 3 Receptor

Notes: *FDA approved for the treatment of VMS. **Off label. ‡Further study needed to establish dose

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