|
制造商：
辉凌制药公司
药理分类：
抗纤溶
活性成分（补）：
氨甲环酸650mg;标签。
指示（补）：
循环月经出血。
药理作用：
相较于正常月经出血的妇女，月经出血妇女子宫内膜，子宫，月经血浓度升高组织纤溶酶原激活物（tPA）的。
氨甲环酸是一种氨基酸赖氨酸削弱了止血纤维蛋白溶解的纤维蛋白溶酶的衍生物。氨甲环酸占赖氨酸的纤维蛋白溶酶的结合位点，阻止纤维蛋白单体结合，从而保持和稳定纤维蛋白的矩阵结构。赖氨酸的高亲和力结合位点饱和纤溶酶原取代从表面纤溶酶原纤维蛋白。
此药主要通过肾小球滤过消除超过95％，淘汰不变。肾功能不全患者，因此需要在减少剂量。
临床试验：
一个3个周期的治疗研究和6周期治疗进行研究，建立在重月经出血治疗的安全性和氨甲环酸的疗效。在这些随机，双盲，安慰剂对照研究，主要结果测量是月经失血量（MBL）的，而终点是凝集素从基线的变化。
在3个周期的研究中，二氨甲环酸（1950mg/day或3900mg/day为每个周期长达5天）相比，不同剂量的安慰剂。评估的294例，115人被随机分派到3900mg/day剂量，这些患者显着减少凝集素相比，那些服用安慰剂。
在6周期的研究中，氨甲环酸3900mg/day给予长达5天/周期进行比较安慰剂。本研究已评估的187例，115人被随机接受研究药物。凝集素的一个显着减少因与研究药物治疗相比，服用安慰剂。研究的成功也需要实现在MBL的减少这是临床上有意义的课题。
在这两项研究，与氨甲环酸3900mg/day治疗与对社会，休闲减少限制和体力活动。
法律分类：
接收
成人：
治疗长达5天月经期间。燕子的整体。 ≥18yrs：肾功能正常（血清肌酐≤1.4mg/dL）：1300mg每日三次;训练班> 1.4-2.8mg/dL：1300mg，每天两次;训练班> 2.8-5.7mg/dL：每天一次1300mg;训练班> 5.7毫克/升：650mg每日一次。
儿童：
“18yrs：不影响。
禁忌（补）：
主动血栓栓塞性疾病（如深静脉血栓，肺栓塞，脑栓塞）。历史或血栓形成或栓塞（例如，视网膜静脉或动脉阻塞;血栓瓣膜病，心脏节律疾病血栓形成，hypercoagulopathy）的风险。
警告/注意事项：
排除子宫内膜病理第一。肾功能损害。蛛网膜下腔出血（脑水肿/梗塞可能发生）。急性早幼粒细胞白血病治疗的口服维甲酸（增加凝血效果）。妊娠（Cat.B）。哺乳的母亲。
互动（补）：
增加血栓事件（如中风，心肌梗塞）的荷尔蒙避孕药，因子IX的产品，抗凝血剂浓缩液，口服维A酸的风险。组织型纤溶酶原激活剂可降低氨甲环酸和第三方协议双方疗效。
不良反应（补）：
头痛，鼻窦/鼻部症状，疼痛（背部，腹部，肌肉骨骼，关节），肌肉痉挛，偏头痛，贫血，乏力，视觉/眼部活动（视网膜阻塞;停止，如果发生），严重过敏性反应。
如何提供：
制表- 30，100，500
最后更新：
2010年6月10号
Ferring acquires LYSTEDA™ from Xanodyne Pharmaceuticals, Inc.
Global Acquisition Expands Ferring's Role in Women's Health
Ferring Pharmaceuticals today announced an agreement that will expand its Women's Health product portfolio with the acquisition of the global rights to Xanodyne Pharmaceutical’s LYSTEDA™ (tranexamic acid), a first-in-class, non-hormonal therapy indicated specifically for treatment of women with cyclic heavy menstrual bleeding (HMB). The company will initially market LYSTEDA in the U.S., and is evaluating opportunities in other markets. LYSTEDA oral tablets received approval on November 13, 2009 following a Priority Review by the U.S. Food and Drug Administration (FDA). It is estimated that up to 22 million women suffer from HMB in the U.S.1,2
"Ferring, as a global, privately held biopharmaceutical company, has a long-standing commitment to the health of women worldwide," said Michel L. Pettigrew, President of the Executive Board, and President and CEO, Ferring Holding Inc. "The acquisition of LYSTEDA, in addition to our ongoing support of research and medical education in the field of Reproductive Health, demonstrates this significant commitment and represents an important addition to our Women’s Health portfolio."
Added Olivier Delannoy, Vice President, U.S. Infertility Business Unit, "In the U.S., the acquisition of LYSTEDA enables us to expand into the field of obstetrics and gynecology. Ferring is a well-established leader in reproductive endocrinology with the broadest portfolio of infertility treatments in the U.S., including MENOPUR®, BRAVELLE® and ENDOMETRIN®. The addition of LYSTEDA furthers our goal of providing treatments for every stage of a woman's reproductive health, including before, during and after pregnancy."
Ferring will introduce LYSTEDA to the Obstetric and Gynecology community at the upcoming American College of Obstetricians and Gynecologists (ACOG) 58th Annual Clinical Meeting, May 15-19, 2010 in San Francisco. For more information, visit www.lysteda.com.
About LYSTEDA™
LYSTEDATM (tranexamic acid) tablets are indicated for the treatment of cyclic heavy menstrual bleeding. Prior to prescribing LYSTEDA, exclude endometrial pathology that can be associated with heavy menstrual bleeding.
Important Safety Information
Do not prescribe LYSTEDA to women who are known to have: active thromboembolic disease, a history of thrombosis or thromboembolism, including retinal vein or artery occlusion, an intrinsic risk of thrombosis or thromboembolism. Venous and arterial thrombosis or thromboembolism, and retinal artery and retinal vein occlusions, have been reported with tranexamic acid.
Do not prescribe LYSTEDA to women with known hypersensitivity to tranexamic acid.
Because LYSTEDA is antifibrinolytic, concomitant use with hormonal contraception may exacerbate the increased thrombotic risk (blood clots, stroke, and myocardial infarction) associated with combination hormonal contraceptives. Women using hormonal contraception should use LYSTEDA only if there is a strong medical need and the treatment benefit will outweigh the potential increased risk of a thrombotic event.
In case of severe allergic reaction, discontinue LYSTEDA and seek immediate medical attention. A case of severe allergic reaction (dyspnea, tightening of the throat, and facial flushing) to LYSTEDA was reported in clinical trials and a case of anaphylactic shock was reported in the literature, involving a patient who received an intravenous bolus of tranexamic acid.
Retinal venous and arterial occlusion has been reported in patients using tranexamic acid. Immediately discontinue LYSTEDA if visual or ocular symptoms occur. Ligneous conjunctivitis also has been reported in patients taking tranexamic acid which resolved with drug discontinuation.
LYSTEDA is not recommended for women taking either Factor IX complex concentrates or antiinhibitor coagulant concentrates because the risk of thrombosis may be increased.
Exercise caution when prescribing LYSTEDA to women with acute promyelocytic leukemia taking all-trans retinoic acid for remission induction because of possible exacerbation of the procoagulant effect of all-trans retinoic acid.
Cerebral edema and cerebral infarction may be caused by use of LYSTEDA in women with subarachnoid hemorrhage.
The most common adverse reactions in clinical trials (> 5%, and more frequent in LYSTEDA subjects compared to placebo subjects) were: headache, sinus and nasal symptoms, back pain, abdominal pain, musculoskeletal pain, arthralgia, muscle cramps and spasms, migraine, anemia and fatigue.
About Ferring Pharmaceuticals
Ferring Pharmaceuticals, headquartered in Switzerland, is a privately owned, research driven specialty biopharmaceutical group active in global markets. The company identifies, develops and markets innovative products in the areas of endocrinology, gastroenterology, gynaecology, fertility and urology. Ferring Pharmaceuticals Inc. offers a line of products in the U.S. market. They include: BRAVELLE® (urofollitropin for injection, purified), MENOPUR® (menotropins for injection, USP) and REPRONEX® (menotropins for injection, USP), NOVAREL® (chorionic gonadotropin for injection, USP), ENDOMETRIN® (progesterone) Vaginal Insert, 100 mg, FIRMAGON® (degarelix for injection), PROSED® DS (methenamine, phenyl salicylate, methylene blue, benzoic acid, hyoscyamine sulfate), DESMOPRESSIN, and EUFLEXXA® (1% sodium hyaluronate).
11月13日，FDA批准Lysteda片（tranexamic acid，氨甲环酸）作为首个非激素类产品用于治疗月经大出血（月经过多）。Lysteda通过使一种有助于血液凝固的蛋白质加以稳定而起效。该药由位于美国肯塔基州Newport市的Xanodyne制药公司生产。
LYSTEDA
Indication(s):
Cyclic heavy menstrual bleeding.
Pharmacology:
Compared to women with normal menstrual bleeding, women with heavy menstrual bleeding have elevated concentrations of endometrial, uterine, and menstrual blood tissue plasminogen activator (tPA).
Tranexamic acid is a derivative of the amino acid lysine that diminishes the dissolution of hemostatic fibrin by plasmin. Tranexamic acid occupies the binding sites for lysine on plasmin, preventing binding to fibrin monomers, thus preserving and stabilizing fibrin’s matrix structure. Saturation of the high affinity lysine binding site on plasminogen displaces plasminogen from the surface of fibrin.
This drug is eliminated primarily by glomerular filtration, with more than 95% eliminated unchanged. Patients with renal dysfunction therefore require a reduction in dose.
Clinical Trials:
A 3-cycle treatment study and a 6-cycle treatment study were conducted to establish the safety and efficacy of tranexamic acid in the treatment of heavy menstrual bleeding. In these randomized, double-blind, placebo-controlled studies, the primary outcome measure was menstrual blood loss (MBL), and the endpoint was the change from baseline in MBL.
In the 3-cycle study, two different doses of tranexamic acid (1950mg/day or 3900mg/day for up to 5 days per cycle) were compared to placebo. Of 294 evaluable patients, 115 were randomized to the 3900mg/day dose; these patients had significantly reduced MBL, compared to those given placebo.
In the 6-cycle study, tranexamic acid 3900mg/day given for up to 5 days/cycle was compared to placebo. This study had 187 evaluable patients, 115 of whom were randomized to receive the study drug. A significant reduction in MBL resulted from treatment with the study drug, compared to placebo. Study success also required achieving a reduction in MBL that was clinically meaningful for the subjects.
In both studies, treatment with tranexamic acid 3900mg/day was associated with a reduction in limitations on social, leisure, and physical activities.
Legal Classification:
Rx
Adults:
Treat for up to 5 days during menses. Swallow whole. ≥18yrs: Normal renal function (serum creatinine ≤1.4mg/dL): 1300mg three times daily; Cr >1.4–2.8mg/dL: 1300mg twice daily; Cr >2.8–5.7mg/dL: 1300mg once daily; Cr >5.7mg/dL: 650mg once daily.
Children:
<18yrs: not studied.
Contraindication(s):
Active thromboembolic disease (eg, DVT, pulmonary embolism, cerebral thrombosis). History or risk of thrombosis or thromboembolism (eg, retinal vein or artery occlusion; thrombogenic valvular disease, thrombogenic cardiac rhythm disease, hypercoagulopathy).
Warnings/Precautions:
Exclude endometrial pathology first. Renal impairment. Subarachnoid hemorrhage (cerebral edema/infarction may occur). Acute promyelocytic leukemia treated with oral tretinoin (increased procoagulant effect). Pregnancy (Cat.B). Nursing mothers.
Interaction(s):
Increased risk of thrombotic events (eg, stroke, MI) with hormonal contraceptives, Factor IX products, anti-inhibitor coagulant concentrates, oral tretinoin. Tissue plasminogen activators may decrease efficacy of both tranexamic acid and tPAs.
Adverse Reaction(s):
Headache, sinus/nasal symptoms, pain (back, abdomen, musculoskeletal, joint), muscle cramps, migraine, anemia, fatigue; visual/ocular events (retinal occlusion; discontinue if occurs), severe allergic reaction.
How Supplied:
Tabs—30, 100, 500
Last Updated:
6/10/2010
|
