制造商：
Mallinckrodt公司
药理分类：
阿片类镇痛药
活性成分（补）：
盐酸二氢吗啡酮8mg，12mg，16mg;分机- REL的标签;含有亚硫酸盐。
指示（补）：
中度至重度疼痛的阿片类镇痛时需要不断在相当长的一段时间。不适用于视需要使用或治疗急性或后运痛苦。对于阿片类药物耐受患者只使用。
药理作用：
氢吗啡酮是吗啡的衍生物，作品主要通过与中枢神经系统μ-阿片受体相互作用。其主要治疗作用是镇痛，其范围是由如呼吸抑制，镇静，恶心呕吐，它的副作用限制。
Exalgo是每天服用一次的口服制剂的二氢表示的情况下使用其中一种长效阿片类镇痛药是恰当的。为类似产品，适当选择病人是至关重要的这种药物的合理使用。它应该只用于阿片类药物耐受的病人，也就是说，谁的病人已采取重大剂量的阿片类药物（如口服吗啡60mg/day，透皮芬太尼25mcg/hr，羟考酮30mg/day，口服酮8mg/day，口腔羟25mg/day）至少一个星期。经过单次口服剂量，血药浓度逐渐增加了6-8小时。在此之后，浓度持续24小时。稳态水平后达到3-4年一次，服药天。约3 / 4的药物是通过肾脏排除，主要为肝代谢物。肾功能损害的延误消除。对于严重肾功能不全的患者，短效阿片类药物可能是一个更合适的选择。
临床试验：
随机提取研究进行评估治疗阿片类药物耐受患者腰背疼痛的Exalgo疗效。
经过公开标签转换和调整期，病人转换为Exalgo开始剂量约为75的每日总剂量吗啡当量％。经过充分的疼痛控制与每日一次给药实现，患者进入了一个为期12周的安慰剂对照治疗阶段。在这个阶段，患者随机接受了Exalgo，或Exalgo相同剂量和从在滴定阶段（立即减免允许救援剂量产品）达到稳定剂量逐渐减少剂量匹配的安慰剂。相较于安慰剂，Exalgo提供卓越的镇痛效果。平均每周数字疼痛强度量表的分数，有一个从基线到12周，两组之间最后一次访问的平均变化显着差异。
法律分类：
印度工业联合会
成人：
没有为初次使用。燕子的整体。 > 17yrs：个别化。正常范围：8 - 64mg，每日一次。见其他阿片类药物转换文献。逐步撤出。中度/重度肝或中度肾功能损害：减少剂量，密切监测。
儿童：
≤17yrs：不推荐。
禁忌（补）：
非阿片类药物的宽容。显着的呼吸障碍。哮喘（急性或严重）。亚硫酸盐过敏。麻痹性肠梗阻。胃肠道阻塞或狭窄或顾。
警告/注意事项：
严重肾功能不全：不推荐。头部受伤。颅内压增高。急腹症。胃肠手术。受损的肾，肝，甲状腺，肾上腺皮质，或肺的功能。胆囊疾病。胆道疾病或手术。痉挛症。震颤性谵妄。中毒性精神病。循环性休克。吸毒者。避免突然停止。老人。虚弱。产科镇痛，分娩，哺乳母亲：不推荐。妊娠（Cat.C）。
互动（补）：
不推荐单胺氧化抑制剂后14天。电位与酒精（不受剂量倾销），中枢神经系统抑制剂，三环类，吩噻嗪。混合激动剂/拮抗剂阿片类药物可减少戒断症状的影响和沉淀。添加剂的抗胆碱作用（例如，尿潴留，便秘）与其他抗胆碱能药物。
不良反应（补）：
便秘，胃肠不适，嗜睡，头痛，无力，头晕，皮疹，体位性低血压，尿潴留，呼吸或循环系统抑郁症，晕厥。
如何提供：
制表- 100
最后更新：
2010年5月14日
Manufacturer:
Mallinckrodt, Inc.
Pharmacological Class:
Opioid analgesic
Active Ingredient(s):
Hydromorphone HCl 8mg, 12mg, 16mg; ext-rel tabs; contains sulfites.
Indication(s):
Moderate to severe pain when continuous opioid analgesia is needed for an extended time period. Not for as-needed use or to treat acute or post-op pain. For use in opioid-tolerant patients only.
Pharmacology:
Hydromorphone is a morphine derivative that works primarily by interacting with mu-opioid receptors in the CNS. Its principal therapeutic effect is analgesia, the extent of which is limited by its side effects such as respiratory depression, sedation, and nausea.
Exalgo is a once-daily oral formulation of hydromorphone indicated for use in situations where a long-acting opioid analgesic is appropriate. As for similar products, proper patient selection is critical to the appropriate use of this medication. It should be used only in opioid-tolerant patients; that is, patients who have been taking significant doses of opioids (eg, oral morphine 60mg/day, transdermal fentanyl 25mcg/hr, oxycodone 30mg/day, oral hydromorphone 8mg/day, oral oxymorphone 25mg/day) for at least one week. After a single oral dose, plasma levels gradually increase over 6–8 hrs. After that, the concentration is sustained for 24 hrs. Steady-state levels are reached after 3–4 days of once-daily dosing. About 3/4 of the drug is eliminated via the kidneys, mostly as hepatic metabolites. Renal impairment delays their elimination. For patients with severe renal dysfunction, a shorter-acting opioid may be a more appropriate choice.
Clinical Trials:
A randomized withdrawal study was conducted to assess the efficacy of Exalgo in treating lower back pain in opioid-tolerant patients.
After an open-label conversion and titration phase, patients were converted to a starting dose of Exalgo that was about 75% of their total daily morphine equivalent dose. After adequate pain control was achieved with once-daily dosing, patients entered a 12-week, placebo-controlled treatment phase. In this phase, patients were randomized to receive either the same dose of Exalgo, or Exalgo and matched placebo in doses tapering from the stable dose achieved during the titration phase (rescue doses of an immediate-relief product allowed). Compared to placebo, Exalgo provided superior analgesia. In average weekly pain intensity Numeric Rating Scale scores, there was a significant difference in the mean changes from baseline to week 12 or final visit between the two groups.
Legal Classification:
CII
Adults:
Not for initial use. Swallow whole. >17yrs: Individualize. Usual range: 8–64mg once daily. See literature for converting from other opioids. Withdraw gradually. Moderate/severe hepatic or moderate renal impairment: reduce dose, monitor closely.
Children:
≤17yrs: not recommended.
Contraindication(s):
Non-opioid tolerant. Significant respiratory impairment. Asthma (acute or severe). Sulfite allergy. Paralytic ileus. GI or GU obstruction or stricture.
Warnings/Precautions:
Severe renal dysfunction: not recommended. Head injury. Increased intracranial pressure. Acute abdomen. GI surgery. Impaired renal, hepatic, thyroid, adrenocortical, or pulmonary function. Gallbladder disease. Biliary disease or surgery. Convulsive disorders. Delirium tremens. Toxic psychosis. Circulatory shock. Drug abusers. Avoid abrupt cessation. Elderly. Debilitated. Obstetrical analgesia, labor and delivery, nursing mothers: not recommended. Pregnancy (Cat.C).
Interaction(s):
Not recommended within 14 days of MAOIs. Potentiation with alcohol (not subject to dose-dumping), CNS depressants, tricyclics, phenothiazines. Mixed agonist/antagonist opioids may reduce effects and precipitate withdrawal symptoms. Additive anticholinergic effects (eg, urinary retention, constipation) with other anticholinergics.
Adverse Reaction(s):
Constipation, GI upset, somnolence, headache, asthenia, dizziness, rash, orthostatic hypotension, urinary retention, respiratory or circulatory depression, syncope.
How Supplied:
Tabs—100
Last Updated:
5/14/2010