2009年12月14日，美国食品药品管理局(FDA)已批准yprexa Relprevv (奥氮平)用于治疗精神分裂症成人患者。该长效抗精神病药通过肌注给药，可持续释放奥氮平达4周。

应用长效药物Zyprexa Relprevv治疗精神分裂症的优势在于，可使精神科医生准确知道患者接受治疗的时间，并且如果患者未复诊接受预定注射的话，可立即发现患者对治疗不依从。
 
FDA批准Zyprexa Relprevv是基于涉及2,054例患者的临床数据。应用该药治疗后，精神分裂症患者的下列症状得到了控制，包括幻觉、妄想、情感淡漠和社交退缩。礼来公司表示，该药疗效明确，不需要口服补充治疗。
 
在研究中，Zyprexa Relprevv的给药剂量为150mg、210mg、300mg和405mg。根据剂量的不同，治疗性奥氮平暴露时间可维持2周或4周。
 
研究发现，除了注射相关事件(如注射后谵妄/镇静综合征，PDSS)之外，Zyprexa Relprevv的安全性与口服奥氮平相似。PDSS事件包括许多镇静体征和症状，从轻度镇静到昏迷和(或)谵妄，包括精神错乱、定向障碍、激越、焦虑或其他认知功能障碍。
 
截至2009年11月30日，在所有临床试验中，因注射Zyprexa Relprevv 而出现PDSS事件的几率<0.1%，约2%患者出现PDSS事件。注射后最初1h内出现事件的可能性最大。多数事件在注射后最初3h内出现；然而，也有事件在3h后才出现。所有出现PDSS事件的患者基本上可在72h内恢复，多数患者选择继续接受Zyprexa Relprevv治疗。

短期安慰剂对照试验报告的最常见治疗中出现的不良事件(treatment-emergent adverse events)(至少1个 Zyprexa Relprevv治疗组的发生率>5%，并高于安慰剂组)为头痛、镇静、体重增加、咳嗽、腹泻、腰痛、恶心、嗜睡、口干、鼻咽炎、食欲增加和呕吐。

FDA approves Zyprexa RelPrevv, a long-acting injectable, ensuring happy holidays for Eli Lilly

Pharmaceutical giant Eli Lilly & Co. got a nice gift under the tree this year. It came from the FDA, which approved a long-acting injectable version of their top-selling Zyprexa, to be marketed as Zyprexa RelPrevv.

Zyprexa (olanzapine) can help ease symptoms of schizophrenia, such as hallucinations and delusions. Unfortunately, as with many psychiatric drugs, relief goes hand in hand with risk.

The drug’s serious side effects can include weight gain, diabetes and heart problems. And the new, injectable version adds another risk: “post-injection delirum/sedation syndrome” (PDSS).

PDSS develops in about 2 percent of patients. Patients with PDSS have become confused, walked into walls, and fallen asleep in public places. Since PDSS usually occurs soon after the injection, Zyprexa RelPrevv will have prescribing restrictions, including a requirement that patients stay under observation at a health care facility for three hours, and leave with an escort.

The risk of PDSS concerned the FDA enough to reject the drug’s first application in 2008, but Lilly’s “mitigation program” won them over.

The new drug’s approval will help Lilly fight off generic competition next year, when the patent runs out on regular Zyprexa. It will be hard to match the oral drug’s sales, but Lilly plans an aggressive marketing push, hoping they can talk psychiatrists into prescribing more long-acting injectables, known as “depot” drugs.

Observers expect Lilly to push the “relapse prevention” angle - after all, the drug itself is tagged Rel(apse) Prevv(ention). The key here will be talking to docs about the extreme dangers of “non-compliance.”

A person who swallows a pill each day can choose to skip it. One injection of a “depot” drug, though, lasts for weeks.

And Lilly’s concern over generic olanzapine? It’s understandable: the company’s third-quarter financial results, released Oct. 21, 2009, show Zyprexa was one of their “Revenue Highlights,” raking in $3.5 billion since January.