英文药名：Osphena(Ospemifene Tablets) 中文药名：奥培米芬片 生产厂家：盐野义公司 药品介绍 2013年2月26日美国食品药品监督管理局(FDA)批准Osphena(ospemifene)治疗 妇女经受中度至严重性交痛[dyspareunia]，一种由于绝经外阴和阴道萎缩的症状。 性交痛是一种绝经期间雌激素的激素水平下降伴随情况。雌激素较低可能使阴道组织变薄，变干和更加脆弱，导致性交时疼痛。 Osphena，一种每天1次与食物口服的药物，其作用如同雌激素作用于阴道组织使它们变厚，和不那么脆弱，导致妇女经受性交疼痛量减低。 FDA药物评价和研究中心的药物评价III副室主任Victoria Kusiak，M.D.说：“性交痛是绝经后妇女最频发报道的问题，”“Osphena对寻求缓解的妇女提供另一种治疗选择。” 在1,889例有外阴和阴道萎缩症状的绝经后妇女的三项临床研究确定Osphena的安全性和有效性。妇女 被随机地赋予接受Osphena或一种安慰剂。在12周治疗后，来自前两项试验的结果显示Osphena-治疗妇女与接受安慰剂妇女比较性交疼痛 统计显著改善。来自第三项研究结果支持在性交痛治疗的长期安全性。 正在被批准Osphena有一个黑框警告提醒妇女和卫生保健专业人员该药其作用像雌激素对阴道组织，曾被显示可刺激子宫衬里(子宫内膜)和致之变厚。在有生育力妇女中，在绝经前，每月发生子宫内膜的这种变厚。绝经后妇女永远不再有月经，而被刺激的子宫内膜不是正常的。妇女如经常经历不寻常出血应找她们的卫生保健专业人员因为可能是子宫内膜癌征象或一种情况导致子宫内膜癌。Osphena处方应符合个别妇女最短的时间与治疗目标和风险。 黑框警告还陈述血栓性和出血性卒中的发生率(分别为每一千妇女0.72和1.45)和深静脉血栓形成发生率(每一千妇女1.45)。这些发生率代表低风险相反单独雌激素治疗见到卒中和深静脉血栓形成风险增加。 在临床试验期间最常报道的副作用包括潮热，阴道排泄物，肌肉痉挛，生殖器排泄物和出汗过多。 Osphena由总部在新泽西的盐野义制药公司Shionogi Inc上市。 Generic Name: ospemifene Dosage Form: tablet, film coated Medication Class: Selective Estrogen Receptor Modulator FDA Approval Date: February 2013 Pharmacological Class: Estrogen (agonist/antagonist). Active Ingredient(s): Ospemifene 60mg; tabs. Company Shionogi, Inc. Indication(s): Treatment of moderate-to-severe dyspareunia due to menopause. Pharmacology: The mechanism of action of Ospemifene is mediated through binding to estrogen receptors. This binding results in activation of estrogenic pathways in some tissues (agonism) and blockade of estrogenic pathways in others (antagonism). Clinical Trials: The safety and effectiveness of Osphena on moderate-to-severe symptoms of vulvar and vaginal atrophy in postmenopausal women were assessed in three placebo-controlled clinical trials. The first trial was a 12-week, randomized, double-blind, placebo-controlled, parallel-group study that enrolled 826 postmenopausal women (41–81 years old) who at baseline had ≤5% superficial cells on a vaginal smear, a vaginal pH >5.0, and who identified at least one moderate-to-severe vaginal symptom that was considered the most bothersome to her (vaginal dryness, pain during intercourse [dyspareunia], or vaginal irritation/itching). Treatment groups included Osphena 30mg (n=282), Osphena 60mg (n=276), and placebo (n=268). Improvement in the mean change from baseline to Week 12 was assessed for the co-primary efficacy variables of the most bothersome symptom (MBS) of vulvar and vaginal atrophy (defined as the individual moderate-to-severe symptom that was identified by the woman as most bothersome at baseline), percentage of vaginal superficial and vaginal parabasal cells on a vaginal smear, and vaginal pH. Following completion of 12-weeks, women with an intact uterus were allowed to enroll in a 40-week double-blind extension study, and women without an intact uterus were allowed to enroll in a 52-week open-label extension study. The second trial was a 12-week, randomized, double-blind, placebo-controlled, parallel-group study that enrolled 919 postmenopausal women (41–79 years old) who at baseline had ≤5% superficial cells on a vaginal smear, a vaginal pH >5.0, and who identified either moderate-to-severe vaginal dryness (dryness cohort) or moderate-to-severe dyspareunia (dyspareunia cohort) as most bothersome to her at baseline. Treatment groups included Osphena 60mg (n=463) and placebo (n=456). Primary endpoints were similar to those in Trial 1. The third trial was a 52-week, randomized, double-blind, placebo-controlled, long-term safety study that enrolled 426 postmenopausal women (49–79 years old) with an intact uterus. Treatment groups included Osphena 60mg (n=363) and placebo (n=63). In the first and second trial, the modified intent-to-treat population of women treated with Osphena demonstrated a statistically significant improvement (least square mean change from baseline to Week 12) in moderate-to-severe bothersome symptoms (MBS) of dyspareunia (Trial 1: [-1.39 (0.11); P=0.0012]; Trial 2: [-1.55 (0.06); P<0.0001] when compared to placebo. A statistically significant increase in the proportion of superficial cells and a corresponding statistically significant decrease in the proportion of parabasal cells on a vaginal smear was also demonstrated (P <0.0001 for both). The mean reduction in vaginal pH between baseline and Week 12 was also statistically significant (P <0.0001). Legal Classification: Rx Adults: 60mg once daily with food. Children: Not studied. Contraindication(s): Undiagnosed abnormal genital bleeding. Known or suspected estrogen-dependent neoplasia. Active DVT, pulmonary embolism, or history of. Active arterial thromboembolism (eg, stroke, MI, or history of). Known or suspected pregnancy (Category X). Warnings/Precautions: Use for shortest duration consistent with treatment goals and risks. Increased risk of cardiovascular disorders, arterial vascular disease, and/or venous thromboembolism. Discontinue if thromboembolic or hemorrhagic stroke is suspected or occur. Discontinue at least 4–6 weeks before surgery type associated with increased risk of thromboembolism or during prolonged immobilization. Increased risk of endometrial cancer. Consider the addition of a progestin in patients with an intact uterus to reduce endometrial hyperplasia risk. Known, suspected, or history of breast cancer: do not use. Severe hepatic impairment: not recommended. Reevaluate periodically. Nursing mothers. Interaction(s) Avoid concomitant other estrogens or estrogen agonists/antagonists. Antagonized by rifampin. Potentiated by fluconazole (avoid), ketoconazole. May affect or be affected by highly protein-bound drugs. May increase risk of adverse reactions with concomitant CYP3A4 and CYP2C9 inhibitors. Adverse Reaction(s) Hot flush, vaginal or genital discharge, muscle spasms, hyperhidrosis. How Supplied: Tabs—100 Blister pack—30 (2 X 15) LAST UPDATED: 7/22/2013 https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=8462d6ab-e3cd-4efa-a360-75bf8f917287