更年期潮热被认为是一种血管张力症状，困扰着多达75%的更年期女性，且可能持续5年甚至更长时间。其本身并不致命，但症状相当麻烦，常给患者造成诸多不适。6月28日，美国食品药品管理局(FDA)正式批准Brisdelle(帕罗西汀)用于治疗中至重度更年期相关潮热。这是迄今FDA所批准的惟一一种针对更年期潮热的非激素疗法，其他所有已经获准的治疗药物均含有雌二醇或雌二醇+孕酮。

Brisdell(帕罗西汀)中含有7.5mg帕罗西汀，每日1次，睡前服用，其安全性及有效性在两项随机、双盲、安慰剂对照临床研究中得到了证实。在这两项研究共有1175名中度至重度存在潮热症状（最少每天七到八次或每周50-60次）的绝经后妇女参与。其中一项研究的治疗周期为12周，另一项研究则持续了24周。结果显示，与安慰剂相比，Brisdelle减少了潮热的次数，其机制尚不清楚。
Brisdelle(帕罗西汀)治疗过程中最常见的副作用包括头痛、疲劳、恶心或呕吐。
其它药物如Paxil和Pexeva含有更高剂量的帕罗西汀，这些药物被批准用于治疗诸如重度抑郁症、强迫症、惊恐障碍和广泛性焦虑障碍。所有被批准用于治疗抑郁症的药物，包括Paxil和Pexeva在内均有一项黑框警告，提示儿童和年轻人服用后自杀风险升高的可能。由于Brisdelle与Paxil、Pexeva所含的活性成分相同，故Brisdelle(帕罗西汀)的标签上也有关于自杀风险的黑框警告。
Brisdelle(帕罗西汀)的说明书中还警告，若与他莫昔芬同服，其有效性可能会降低，出血风险可能增加，并且有发生5-羟色胺综合征的风险。该药将附一份患者用药指导。
研究者指出：有相当多的女性受到更年期潮热的困扰，她们不能或不想接受激素治疗。如今FDA批准的首款非激素药物为患者提供了新的治疗选择，可以帮助她们缓解更年期常见的潮热症状。
Pharmacological Class:
SSRI.
 
Active Ingredient(s):
Paroxetine (as mesylate) 7.5mg; capsules.
 
Company
Noven Therapeutics
 
 
Indication(s):
 
Moderate to severe vasomotor symptoms associated with menopause. Limitation of use: not indicated for treatment of any psychiatric condition.
 
Pharmacology:
 
Brisdelle is an oral selective serotonin reuptake inhibitor (SSRI) and its mechanism of action for the treatment of vasomotor symptoms is unknown.
 
Clinical Trials:
 
The efficacy of Brisdelle was established in two Phase 3 studies in 1174 postmenopausal women with a minimum of 7–8 moderate to severe vasomotor symptoms (VMS) per day at baseline (≥50 per week) for 30 days prior to receiving study drug. Participants received Brisdelle 7.5mg once daily at bedtime.
 
Study 1 was a 12-week, randomized, double-blind, placebo-controlled clinical trial with a total of 606 postmenopausal women. Study 2 was a 24-week, randomized, double-blind, placebo-controlled clinical trial with a total of 568 postmenopausal women. The co-primary efficacy endpoints for both studies were the reduction from baseline in VMS frequency and severity at Weeks 4 and 12.
 
Study 1 results demonstrated a statistically significant reduction from baseline in the frequency of moderate to severe vasomotor symptoms at Week 4 and Week 12 and a statistically significant reduction in the severity of moderate to severe VMS at Week 4 for Brisdelle compared to placebo. Results from Study 2 showed a statistically significant reduction from baseline in the frequency and severity of moderate to severe vasomotor symptoms at Week 4 and Week 12 for Brisdelle compared to placebo.
 
Persistence of benefit at 24 weeks in Study 2 was eva luated with a responder analysis where responders were defined as those patients who achieved ≥50% reduction from baseline in the frequency of moderate to severe VMS at Week 24. The proportion of patients achieving a ≥50% reduction in the frequency of moderate to severe VMS from baseline to Week 24 was 48% in the Brisdelle group and 36% in the placebo group at Week 24.
 
 
Legal Classification:
 
Rx
 
Adults:
 
7.5mg once daily at bedtime.
 
Children:
 
Not established.
 
Contraindication(s):
 
During or within 14 days of MAOIs. Concomitant linezolid or IV methylene blue. Concomitant pimozide, thioridazine (may cause QTc prolongation). Pregnancy (Category X).
 
Warnings/Precautions:
 
Increased risk of suicidal thinking and behavior in children and young adults when used to treat depressive or other psychiatric disorders; monitor all patients for clinical worsening or unusual changes; consider discontinuing if occurs. Monitor for serotonin syndrome; discontinue if occurs. Risk of hyponatremia. Volume-depleted. Screen for risk of bipolar disorder prior to initiating therapy; monitor for mania/hypomania. History of seizures or with conditions that lower the seizure threshold; eva luate and consider discontinuing if occurs. Discontinue if akathisia occurs. Narrow angle glaucoma. Elderly. Nursing mothers: not recommended.
 
Interaction(s)
 
See Contraindications. Concomitant other paroxetine-containing products: not recommended. Do not start MAOIs until at least 2 weeks after discontinuing paroxetine. Increased risk of serotonin syndrome with other serotonergic drugs (eg, triptans, tricyclic antidepressants, fentanyl, lithium, tramadol, tryptophan, buspirone, St. John's Wort) or with drugs that impair serotonin metabolism (eg, MAOIs, linezolid, IV methylene blue). Avoid concomitant tamoxifen. May affect, or be affected by, drugs metabolized by CYP2D6, including nortriptyline, amitriptyline, imipramine, desipramine, fluoxetine, phenothiazines, risperidone, atomoxetine, digoxin, theophylline, Class 1C antiarrhythmics (eg, propafenone, flecainide, encainide), quinidine. May potentiate protein-bound drugs (eg, warfarin). Potentiated by cimetidine; monitor. Antagonized by phenobarbital, phenytoin, fosamprenavir/ritonavir; monitor. Increased risk of bleeding with NSAIDs, aspirin, warfarin, or others that affect coagulation. Risk of hyponatremia with diuretics.
 
Adverse Reaction(s)
 
Headache, fatigue, nausea/vomiting; potential for bone fracture.
 
How Supplied:
 
Caps—30
 
LAST UPDATED:
 
12/6/2013