Exalgo（盐酸二氢吗啡酮）缓释片，这是一种利用OROS®Push-Pull™渗透输送系统以可控速率释放阿片样药物的制剂。

Covidien公司（纽约证券交易所：COV）是全球领先的卫生保健产品供应商，今天推出EXALGO（盐酸二氢吗啡酮）缓释片（基），唯一的缓释吗啡酮治疗在美国上市。这种治疗证明，以创新的输送系统相结合，提供了阿片类药物耐受患者中度至重度慢性疼痛的痛苦为每剂24小时。

“慢性疼痛的病人经历的痛苦如此严重，它常常被削弱”

由美国食品和药物管理局（FDA）批准在2010年3月1日，EXALGO片盐酸二氢吗啡酮提供一个众所周知的治疗 - 在慢性疼痛的治疗使用了超过80年。对于EXALGO指示每日一次为中度至重度疼痛的阿片类药物耐受需要持续，昼夜为长时间阿片类镇痛的病人管理机关。
EXALGO是8毫克，12毫克和16毫克片剂。
“慢性疼痛的病人经历的痛苦所以它往往被严重削弱，说：”疼痛治疗专家指出，韦伯斯特博士琳，医学临床研究Lifetree疼痛门诊主任在盐湖城，犹他州。
“这种疼痛可以使患者几乎不可能举行一次工作，或做简单的活动，如去杂货店或到他们的孩子练习足球。喜欢EXALGO缓释制剂可以帮助疼痛的日常管理由避免了高峰和低谷的痛苦可能发生的短效阿片类药物。“

目前有一个更持久的治疗未满足需要管理慢性疼痛。在2006年美国疼痛基金会的调查之声慢性疼痛，只有23个患者的百分之慢性疼痛的报道他们的药物是“非常有效。”
一从历史上看，患者谁痛患有慢性可能已订明短效阿片类药物或其他一些扩展，阿片类药物的释放，这将引起他们接管一天中的止痛药多剂量。
“作为通用在美国的控制疼痛的药物的处方数，最大的供应商，Covidien是提供可以访问，扩大与创新相结合，证明药物运载系统的先进的疼痛治疗药物的患者的限制重点”之称提摩太赖特河主席，制药，Covidien公司。
“随着EXALGO片的推出，阿片类药物耐受的慢性疼痛患者将可以选择采取每天一剂，可提供24小时救援，并保持等待的痛苦。这是一个疼痛管理的突破。”
EXALGO利用翁山;推挽;渗透压运送系统，旨在控制率的阿片类药物释放在。通过提供一个全日的氢吗啡酮持续释放，药物配方有助于减少高峰和有时是由慢性疼痛的病人谁上，而这些更频繁的间隔剂量提供止痛产品依赖经验的低谷。

缓释阿片类药物除了治疗疼痛景观，医生对病人的另一种工具来帮助管理往往是什么削弱中度至重度慢性疼痛。
 
根据这一方案，医疗保健提供者教育需要作为一项重要内容，以确保安全使用，以适当的病人的选择和剂量的焦点。

作为Covidien公司的持续承诺要为患者负责倡导的一部分，公司还制定了一项自愿安全使用的EXALGO将提供给医护人员，药剂师，病人及照顾者的工具，范围广泛。这些材料包括病人/处方药物的协议，耐心辅导，指导和更多的安全使用的工具。所有材料将不断审查和更新的基础上，从病人和开处方的反馈。

EXALGO

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

Manufacturer:
Mallinckrodt, Inc.

Pharmacological Class:
Opioid analgesic

Active Ingredient(s):
Hydromorphone HCl 8mg, 12mg, 16mg; ext-rel tabs; contains sulfites.