近日，美国食品和药物管理局（FDA）批准了1.62％的透明，无味的凝胶制剂AndroGel（睾酮凝胶）显示恢复性腺功能减退男性的睾酮水平，与AndroGel 1％相比，起始剂量的凝胶体积减半。 在起始剂量下，新的AndroGel 1.62％在两台泵压机中含有40.5mg睾酮，而AndroGel 1％在四台泵压机中含有50mg睾酮。AndroGel的剂量和给药1.62％与AndroGel 1％不同，两者不可互换。AndroGel 1.62％和AndroGel 1％都是处方药，用于治疗低睾酮或无睾酮的成年男性，也称为性腺功能减退症。 批准日期：2011年4月29日 公司：AbbVie Inc AndroGel（睾酮[testosterone]）凝胶1.62％用于局部使用CIII 最初的美国批准：1953年 警告： 对于完整的BOXED警告，对TESTOSTERONE的二次接触请参阅完整的预定信息。 据报道，二次接触睾酮凝胶的儿童进行了病毒化。 儿童应避免接触使用睾酮凝胶的男性未洗过或未穿衣的应用部位。 医疗保健提供者应建议患者严格遵守建议的使用说明。 最近的重大变化 警告和注意事项：10/2016 作用机制 内源性雄激素，包括睾酮和二氢睾酮（DHT），负责男性性器官的正常生长和发育以及维持第二性征。 这些影响包括前列腺，精囊，阴茎和阴囊的生长和成熟; 男性头发分布的发展，如面部，耻骨，胸部和腋毛; 喉扩大; 声带增厚; 和身体肌肉组织和脂肪分布的改变。 睾酮和DHT是第二性征正常发育所必需的。 男性性腺功能减退症是由睾酮分泌不足引起的临床综合症，有两个主要病因。 原发性性腺功能减退症是由性腺缺陷引起的，如Klinefelter综合征或Leydig细胞发育不全，而继发性性腺功能减退症是下丘脑（或垂体）未能产生足够的促性腺激素（FSH，LH）。 适应症和用法 AndroGel 1.62％适用于与缺乏或缺乏内源性睾酮相关的病症的男性替代疗法： 原发性性腺功能减退症（先天性或后天性） 低促性腺功能减退症（先天性或后天性） 使用限制： AndroGel的安全性和有效性1.62％的男性患有“与年龄相关的性腺功能减退症”尚未建立。 AndroGel的安全性和有效性在18岁以下的男性中尚未确定1.62％。 局部睾酮产品可能具有不同的剂量，强度或应用说明，可能导致不同的全身暴露。 剂量和给药 AndroGel的剂量和用量1.62％与AndroGel的1％不同。对于AndroGel 1％的剂量和给药，请参考其完整的处方信息。 在启动AndroGel 1.62％之前，通过确保在早晨至少两天测量血清睾酮并且这些浓度低于正常范围来确认性腺功能减退症的诊断。 AndroGel 1.62％的起始剂量是40.5mg睾酮（2个泵启动或单个40.5mg包），每天在早晨局部施用一次。 适用于肩部和上臂清洁，干燥，完整的皮肤。不要将AndroGel 1.62％涂抹在身体的任何其他部位，包括腹部，生殖器，胸部，腋窝（腋窝）或膝盖。 剂量调整：AndroGel 1.62％可在最低20.25毫克睾酮（1个泵驱动或单个20.25毫克包）和最多81毫克睾酮（4个泵启动或两个40.5毫克包）之间进行剂量调整。应在开始治疗后约14天和28天或剂量调整后，根据给药前早晨血清睾酮浓度滴定剂量。此外，此后应定期评估血清睾酮浓度。 患者应在施用AndroGel 1.62％后立即用肥皂和水洗手，并在凝胶干燥后用衣服覆盖施用部位。在任何预期应用场所与他人皮肤接触的情况之前，用肥皂和水彻底清洗应用部位。 剂量形式和强度 AndroGel（睾酮凝胶）1.62％局部使用可用如下： 计量泵，每次驱动可提供20.25mg睾酮。 包含20.25毫克睾酮的小包。 包含40.5毫克睾酮的小包。 禁忌症 男性患有乳腺癌或已知或疑似前列腺癌。 孕妇或哺乳期妇女。睾丸激素可能会导致胎儿受到伤害。 警告和注意事项 监测患有良性前列腺增生（BPH）的患者，以改善BPH的体征和症状。 避免女性或儿童无意中接触AndroGel 1.62％。二次接触睾酮可产生男性化的迹象。 AndroGel 1.62％应该停止，直到确定男性化的原因。 已经报道了使用睾酮产品的患者的静脉血栓栓塞（VTE），包括深静脉血栓形成（DVT）和肺栓塞（PE）。评估符合DVT或PE的体征或症状的患者。 一些上市后研究显示，与使用睾酮替代疗法相关的心肌梗塞和中风风险增加。 外源性雄激素给药可能导致无精子症。 有或没有充血性心力衰竭（CHF）的水肿可能是患有先前存在的心脏，肾脏或肝脏疾病的患者的并发症。 睡眠呼吸暂停可能发生在有风险因素的人群中。 定期监测血清睾酮，前列腺特异性抗原（PSA），血红蛋白，血细胞比容，肝功能检查和脂质浓度。 AndroGel 1.62％易燃，直至干燥。 不良反应 最常见的不良反应（发生率≥5％）是前列腺特异性抗原（PSA）的增加。 药物相互作用 雄激素可降低血糖，因此可降低糖尿病患者的胰岛素需求。 雄激素可见抗凝血活性的变化。建议更频繁地监测国际标准化比率（INR）和凝血酶原时间。 使用睾酮与促肾上腺皮质激素（ACTH）或皮质类固醇可导致液体潴留增加。谨慎使用，尤其是患有心脏病，肾病或肝病的患者。 用于特定人群 老年患者的长期安全性数据不足，使用AndroGel 1.62％来评估心血管疾病和前列腺癌的潜在风险。 包装提供/存储和处理 AndroGel 1.62％用于非气雾剂计量泵，每次完成泵驱动可提供20.25mg睾酮。泵由塑料和不锈钢制成，LDPE/铝箔内衬由硬质塑料制成，带有聚丙烯盖。每个88g计量泵可以分配75g凝胶或60计量泵启动;每个泵驱动分配1.25克凝胶。 AndroGel 1.62％还提供单位剂量铝箔包装，每包30个。每包1.25克或2.5克凝胶分别含有20.25毫克或40.5毫克睾酮。 NDC号码包大小 0051-8462-33 88g泵（每个泵分配60个计量泵启动，每个泵启动含有20.25mg睾酮，在1.25g凝胶中） 0051-8462-12每个单位剂量小包含有1.25g凝胶中提供的20.25mg睾酮 0051-8462-31 30包（每个单位剂量包含1.25克凝胶中提供的20.25毫克睾酮） 0051-8462-01每个单位剂量小包含有2.5g凝胶中提供的40.5mg睾酮 0051-8462-30 30包（每个单位剂量包含2.5g凝胶中提供的40.5毫克睾酮） 在受控的室温下储存20°-25°C（68°-77°F）;允许偏移15° - 30°C（59°- 86°F）[见USP受控室温]。 使用过的AndroGel 1.62％泵或使用过的AndroGel 1.62％的包装应该以防止儿童或宠物意外使用或摄入的方式丢弃在家庭垃圾中。 完整资料附件：https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=8677ba5b-8374-46cb-854c-403972e9ddf3 AndroGel(testosterone gel) 1% and 1.62% IMPORTANT SAFETY INFORMATION USE: AndroGel(testosterone gel) 1% and 1.62% AndroGel® (testosterone gel) 1% and 1.62% are controlled substances, available by prescription, used to treat adult males who have low or no testosterone due to certain medical conditions. It is not known if AndroGel is safe or effective to treat men who have low testosterone due to aging. It is not known if AndroGel is safe or effective in children younger than 18 years old. Testosterone products that are applied to the skin may have different doses, strengths, or application instructions that may lead to different levels of testosterone in your body. IMPORTANT SAFETY INFORMATION AndroGel can transfer from your body to others. This can happen if other people come into contact with the area where AndroGel was applied. Signs of puberty that are not expected have happened in young children who were accidentally exposed to testosterone through skin-to-skin contact with men using topical testosterone products like AndroGel. Women and children should avoid contact with the unwashed or unclothed area where AndroGel has been applied. If a woman or child makes contact with the AndroGel application area, the contact area on the woman or child should be washed well with soap and water right away. To lower the risk of transfer of AndroGel 1.62%, you should apply it only to your shoulders and upper arms, areas that will be covered by a short-sleeve T-shirt. Do not apply AndroGel 1.62% to any other parts of your body, such as your stomach area (abdomen), penis, scrotum, chest, armpits (axillae), or knees. Wash your hands right away with soap and water after applying. After the gel has dried, cover the application area with clothing until you have washed the application area well or have showered. If you expect another person to have skin-to-skin contact with your shoulders or upper arms, first wash the application area well with soap and water. To lower the risk of transfer of AndroGel 1%, you should apply it only to areas that will be covered by a short-sleeve T-shirt. These areas include shoulders, upper arms, and stomach area. Do not apply AndroGel 1% to any other parts of your body, such as your penis, scrotum, chest, armpits (axillae), knees, or back. Wash your hands right away with soap and water after applying AndroGel. After the gel has dried, cover the application area with clothing. If you expect to have skin-to-skin contact with another person, first wash the application area well with soap and water. Stop using AndroGel and call your healthcare provider right away if you see any signs and symptoms of puberty in a child, or changes in body hair or increased acne in a woman, that may have occurred through accidental exposure to AndroGel. Do not use AndroGel if you have breast cancer or have or might have prostate cancer. AndroGel is not meant for use in women and must not be used in women who are or may become pregnant or are breastfeeding. AndroGel may harm the unborn or breastfeeding baby. Women who are pregnant or who may become pregnant should avoid contact with the area of skin where AndroGel has been applied. Before you use AndroGel, tell your healthcare provider if you have breast cancer; prostate cancer; urinary problems due to enlarged prostate; heart, kidney, or liver problems; problems breathing while you sleep (sleep apnea); or have any other medical conditions.  AndroGel can cause serious side effects, including: If you already have enlargement of your prostate gland, your signs and symptoms can get worse while using AndroGel (including changes in urination) Possible increased risk of prostate cancer Blood clots in the legs or lungs. Signs and symptoms of a blood clot in your leg can include leg pain, swelling, or redness. Signs and symptoms of a blood clot in your lungs can include difficulty breathing or chest pain. Possible increased risk of heart attack or stroke AndroGel is a controlled substance (CIII) because it contains testosterone that can be a target for people who abuse prescription medicines. Keep it in a safe place to protect it and never give it to anyone else. Selling or giving away this medicine may harm others and is against the law. In large doses, AndroGel may lower your sperm count Swelling of your ankles, feet, or body, with or without heart failure. This may cause serious problems for people who have heart, kidney, or liver disease Enlarged or painful breasts Having problems breathing while you sleep (sleep apnea) Tell your healthcare provider about all the medicines you take, including prescription and non-prescription medicines, vitamins, and herbal supplements. Especially tell your healthcare provider if you take insulin, medicines that decrease blood clotting, or corticosteroids. AndroGel is flammable until dry. Let AndroGel dry before smoking or going near an open flame. The most common side effects of AndroGel 1.62% are increased prostate specific antigen (a test used to screen for prostate cancer), mood swings, high blood pressure, increased red blood cell count, and skin irritation where the gel is applied. The most common side effects of AndroGel 1% are acne, skin irritation where the gel is applied, increased cholesterol levels, increased prostate specific antigen, increased red blood cell count, and increased liver function tests. AndroGel 1% and 1.62% application sites and dosages are not interchangeable with each other or with other topical testosterone products. This is the most important information to know about AndroGel. For further information, talk with your healthcare provider. 什么是睾固酮, 为什么要补充睾固酮？ 男性荷尔蒙中，最重要的一种就是睾固酮。其作用包括增进肌肉量与强度、改变体脂肪的比率与分布、维持骨密度、促进红血球制造、刺激体毛生长、调节男性生殖功能等。同时它也会影响情绪，睾固酮过低时容易郁闷、提不起劲、丧失性欲，过高时则容易冲动、具有攻击性倾向等。但因为人体有自动调控荷尔蒙量的恒定机制，如果血中睾固酮长时间高于正常生理范围时，会使下视丘的“促性腺激素”减少分泌。补充过多时，反而会压抑自身生产的荷尔蒙量，将来一旦停用，会使血中睾固酮值掉得更厉害。 补充睾固酮可改善因缺乏睾固酮所致的倦怠、情绪低落等症状，但补充过量不但无法得到超乎常人的体能，反而会出现攻击性等负面的作用。 本品初次使用, 有什么感觉？ 涂抺完毕后, 涂抹部位会于2分钟左右恢复干爽, 30分钟即可感觉药效, 除了勃起容易外, 精神活力会比从前大增, 但仍建议连续使用一星期, 让体内荷尔蒙调整适应, 疗程结束后, 可停药评估。 哪些人需考虑补充睾固酮 出现男性更年期症状，影响生活品质。 勃起功能障碍，以PDE5抑制剂(威而钢、犀利士、乐威壮)单独治疗效果不佳。 有中央性肥胖、第二型糖尿病，或代谢症候群，且睾固酮值偏低者。 什么是肝脏首渡效应(first-pass effect) 其他型式如口服等荷尔蒙投予由于吸收后第一关会先到肝脏，大部份的睾固酮会在此被分解，这就是肝脏首渡效应(first-pass effect)。首渡效应使得口服剂形的生物可利用率低(只有服用的一小部份发挥作用)，所以肝功能不佳的患者须慎用, 而Androgel昂斯妥凝胶并不会产生肝脏首渡效应。 Androgel昂斯妥凝胶与其他产品最大的不同 Androgel昂斯妥凝胶可长效吸收, 不伤肝脏, 更重要可维持稳定血中浓度, 药效持续, 使用极方便, 安全系数高, 不影响前列腺功能。