Marketed by: Pacira Pharmaceuticals (Parsippany, NJ)
Indication: The FDA approved Exparel (bupivacaine liposome injectable suspension) for single-dose infiltration into surgical sites to produce postsurgical analgesia. Exparel uses DepoFoam technology to provide pain relief over time. The recommended dosage of Exparel, which is slowly injected into soft tissue via infiltration, is dependent upon the surgical site and the volume required to cover the surgical area. The product is contraindicated for obstetrical paracervical block anesthesia. Although it should not be administered with lidocaine or other non–bupivacaine-based local anesthetics, Exparel may be used after at least 20 minutes have elapsed following the local administration of lidocaine.
Dosage Form: Injectable suspension: 10- and 20-mL single-use vials containing 13.3 mg bupivacaine liposome per mL
EXPAREL
Manufacturer:
Pacira Pharmaceuticals

Pharmacological Class:
Local anesthetic (amide-type).

Active Ingredient(s):
Bupivacaine 13.3mg/mL; liposome injectable suspension; preservative-free.

Indication(s):
For administration into the surgical site to produce postsurgical analgesia.

Pharmacology:
Exparel is an aqueous suspension of multivesicular liposomes containing bupivacaine. After injection of Exparel into soft tissue, bupivacaine is released from the multivesicular liposomes over a period of time.

Bupivacaine is related chemically and pharmacologically to the amide-type local anesthetics. Local anesthetics block the generation and the conduction of nerve impulses presumably by increasing the threshold for electrical excitation in the nerve, by slowing the propagation of the nerve impulse, and by reducing the rate of rise of the action potential.

Clinical Trials:
A multicenter, randomized, double-blind, placebo-controlled, parallel-group study evaluated the safety and efficacy of Exparel 106mg in 193 patients undergoing bunionectomy. Study medication was administered directly into the wound at the conclusion of the surgery, prior to wound closure. Pain intensity was rated by the patients on a 0 to 10 numeric rating scale (NRS) out to 72 hours. The primary outcome measure was the area under the curve (AUC) of the NRS pain intensity scores (cumulative pain scores) collected over the first 24 hour period. There was a significant treatment effect for Exparel compared to placebo. In this clinical study, Exparel demonstrated a significant reduction in pain intensity compared to placebo for up to 24 hours. The difference in mean pain intensity between treatment groups occurred only during the first 24 hours following study drug administration. Between 24 and 72 hours after study drug administration, there was minimal to no difference between Exparel and placebo treatments on mean pain intensity.

A multicenter, randomized, double-blind, placebo-controlled, parallel-group study evaluated the safety and efficacy of Exparel 266mg in 189 patients undergoing hemorrhoidectomy. Study medication was administered directly into the wound (greater than or equal to 3 cm) at the conclusion of the surgery. Pain intensity was rated by the patients on a 0 to 10 NRS at multiple time points up to 72 hours. The primary outcome measure was the AUC of the NRS pain intensity scores (cumulative pain scores) collected over the first 72 hour period. There was a significant treatment effect for Exparel compared to placebo. In this clinical study, Exparel demonstrated a significant reduction in pain intensity compared to placebo for up to 24 hours. The difference in mean pain intensity between treatment groups occurred only during the first 24 hours following study drug administration. Between 24 and 72 hours after study drug administration, there was minimal to no difference between Exparel and placebo treatments on mean pain intensity; however, there was an attendant decrease in opioid consumption, the clinical benefit of which was not demonstrated.

Exparel has not been demonstrated to be safe and effective in other procedures.

Legal Classification:
Rx

Adults:
For single-dose administration only. Base dose on surgical site and volume required to cover area. Inject slowly into soft tissue via infiltration. Bunionectomy: 106mg (volume: 8mL). Hemorrhoidectomy: 266mg (volume: 20mL). See literature for administration.

Children:
<18yrs: not recommended.

Contraindication(s):
Obstetrical paracervical block.

Warnings/Precautions:
Not interchangeable with other forms of bupivacaine. Avoid intravascular inj. To be administered under the supervision of experienced clinicians. Cardiovascular disease. Hepatic or renal impairment. Monitor cardiovascular and respiratory vital signs. Pregnancy (Cat.C), nursing mothers: not recommended.

Interaction(s):
Do not dilute with water or hypotonic agents (may result in disruption of liposomal particles). Do not mix with lidocaine or other non-bupivacaine-based local anesthetics. Do not administer other forms of bupivacaine within 96hrs following administration of Exparel. May administer after at least 20 minutes following local administration of lidocaine.

Adverse Reaction(s):
Nausea, constipation, vomiting, pyrexia, dizziness, edema peripheral, anemia, hypotension, pruritus, tachycardia, headache, insomnia, anemia postoperative, muscle spasms, hemorrhagic anemia, back pain, somnolence, and procedural pain; CNS effects (eg, excitation, depression, restlessness, anxiety, dizziness, tremors), cardiovascular effects (eg, myocardium depression, decreased cardiac output, heart block, hypotension, bradycardia, ventricular arrhythmias, cardiac arrest), allergic-type reactions, neurologic effects (eg, spinal block, urinary retention, paresthesia, weakness, headache, paralysis of lower extremities).

How Supplied:
Single-use vial (10mL, 20mL)—10

EXPAREL
制造商：
pacira制药

类药物：
局部麻醉剂（酰胺型）。

活性成分（S）：
布比卡因13.3mg/mL;脂质体注射悬挂;不含防腐剂。

指示（S）：
到手术部位的管理产生术后镇痛。

药理作用：
exparel是一个含有布比卡因多囊脂质体的水悬浮液。后注入软组织Exparel，布比卡因过了一段时间的多囊脂质体被释放。

布比卡因与化学和药理的酰胺型局部麻醉剂。局部麻醉药阻止增加减缓传播神经冲动，神经阈值电励磁发电和大概的神经冲动的传导，降低动作电位的上升率。

临床试验：
一个多中心，随机，双盲，安慰剂对照，平行组研究评估在193接受bunionectomy患者的Exparel 106mg的安全性和疗效。研究药物直接管理到伤口在手术结束前，伤口愈合。评分由0至10的数字评定量表（NRS），72小时患者的疼痛强度。主要的测量结果是该地区的网络实名制的疼痛强度超过前24小时内收集的分数（累积疼痛评分）曲线下面积（AUC）。有显着的治疗效果与安慰剂相比，为Exparel。在此临床研究中，Exparel表现在疼痛强度显着减少，比安慰剂长达24小时。研究给药后的第一个24小时期间，只发生在治​​疗组之间的平均疼痛强度的差异。研究给药后24和72小时之间，有没有平均疼痛强度Exparel和安慰剂治疗之间的差异是最小的。

一个多中心，随机，双盲，安慰剂对照，平行组研究评估Exparel 266mg 189发生痔疮患者的疗效和安全。研究药物直接进入伤口管理（大于或等于3厘米），手术结束。疼痛强度被评为上一个0到10（NRS）在多个时间点多达72小时的患者。主要结果测量是网络实名制的疼痛强度在第72小时内收集的分数（累积疼痛评分）的AUC。有显着的治疗效果与安慰剂相比，为Exparel。在此临床研究中，Exparel表现在疼痛强度显着减少，比安慰剂长达24小时。研究给药后的第一个24小时期间，只发生在治​​疗组之间的平均疼痛强度的差异。研究给药后24和72小时之间，有没有平均疼痛强度Exparel和安慰剂治疗之间的差异是最小的，然而，在随之而来的阿片类药物用量减少，没有表现出临床获益。

exparel还没有被证明是安全和有效，在其他程序。

法律分类：
RX

成人：
只用于单剂量给药。手术部位及体积剂量的基础上需要覆盖面积。注入软组织通过渗透缓慢。 bunionectomy：106mg（体积：8ML）。痔疮：266mg（体积：20毫升）。看到行政的文学。

儿童：
<18yrs：不推荐。

禁忌症（S）：
产科宫颈旁阻滞。

警告/注意事项：
不与其他形式的布比卡因互换。避免血管损伤。要管理经验丰富的医生的监督下。心血管疾病。肝或肾功能损害。监测心血管和呼吸系统的重要标志。 （Cat.C）怀孕，哺乳母亲：不推荐。

互动（补）：
不要稀释水或低渗代理（可能导致中断脂质体颗粒）。不要混合使用利多卡因或其他非基于布比卡因局部麻醉。不要在96小时以下的Exparel管理管理布比卡因的其他形式。可以管理后至少20分钟后，地方行政利多卡因。

不良反应（S）：
恶心，便秘，呕吐，发烧，头晕，周边水肿，贫血，低血压，皮肤瘙痒，心动过速，头痛，失眠，贫血术后，肌肉痉挛，失血性贫血，背部疼痛，嗜睡，和程序疼痛;中枢神经系统的影响（例如，激励，忧郁，烦躁，焦虑，头晕，震颤），（例如，心肌抑郁症，心血管的影响降低心输出量，心脏传导阻滞，低血压，心动过缓，室性心律失常，心脏骤停），过敏性反应，神经系统的影响（例如，椎管内阻滞，尿潴留，感觉异常，无力，头痛，下肢瘫痪）。

如何提供：
单用小瓶（10ML，20ML）-10

最后更新：
2012年4月23日