美国FDA批准Novalar Pharmaceuticals公司的牙科麻醉反转药甲磺酸酚妥拉明注射液（phentolamine mesylate，OraVerse）。本品是首个适用于软组织（唇和舌）局麻的反转药品，加速恢复至正常感觉和功能。
OraVerse（甲磺酸酚妥拉明）为注射使用
美国最初批准：1952
适应症和用法
OraVerse被指示为软组织麻醉，即唇及舌麻醉的逆转，以及相关的功能缺损从口腔内粘膜下注射含血管收缩剂的局部麻醉剂的所得。 OraVerse不推荐用于儿童不到6岁或体重不足15公斤（33磅）。
【用法用量】
麻药用量给药OraVerse剂量
½墨盒硒鼓½（0.2毫克）
1盒1盒（0.4毫克）
2墨盒2墨盒（0.8毫克）
OraVerse使用用于局部麻醉的施用相同的位置（S）和同样的技术（S）（浸润或嵌段注射）给药。
剂型和规格
每盒0.4毫克/毫升1.7解决方案
禁忌
无
警告和注意事项
心肌梗塞，脑血管痉挛，脑血管闭塞已经报道发生酚妥拉明的静脉内或肌肉内给药之后，通常与标记低血压发作或休克样状态偶尔遵循肠胃外给药的关联。
心动过速和心脏arrhythmiasmay发生与使用酚妥拉明或其它α-肾上腺素能阻断剂。
不良反应
与OraVerse最常见的不良反应（发生率5％和>控制）是注射部位疼痛。
特殊人群中使用
使用儿童患者小于6岁或<15千克（33磅）不推荐。
在儿科患者体重不到30公斤（66磅），最大剂量OraVerse的建议是1/2柱（0.2毫克）。
Generic Name: phentolamine mesylate
Date of Approval: May 9, 2008
Company: Novalar Pharmaceuticals, Inc.
Treatment for: Reversal of Dental Anesthesia
FDA Approves OraVerse
The United States Food and Drug Administration (FDA) has approved OraVerse (phentolamine mesylate) for the reversal of soft-tissue anesthesia and the associated functional deficits resulting from a local dental anesthetic.
Clinical Studies
The approval of OraVerse for use in adults and children is based on data from several clinical studies, including two Phase 3 studies in adults and adolescents age 12 and older and a Phase 2 pediatric study. The two Phase 3 studies were conducted in 18 centers across the United States, including leading dental schools, clinical research organizations and private clinics. There were 484 dental patients enrolled across the two studies.
In the randomized, double-blinded, controlled Phase 3 studies, following the administration of local anesthetics and completion of the dental procedure, patients were administered either OraVerse or control. OraVerse reduced the median time to recovery of normal sensation in the lower lip (as measured by standardized lip tapping procedures) by 85 minutes compared to control. OraVerse reduced the median time to recovery of normal sensation in the upper lip by 83 minutes. Within one hour after administration of OraVerse, 41% of patients reported normal lower lip sensation as compared to 7% in the control group, and 59% of patients in the OraVerse group reported normal upper lip sensation as compared to 12% in the control group. In both Phase 3 studies, the primary endpoint showed that OraVerse was statistically different compared to control (p<0.0001).
The multi-center, randomized, double-blinded, controlled Phase 2 pediatric study eva luated the safety and efficacy of OraVerse in the reversal of soft tissue anesthesia in patients undergoing dental procedures after receiving local anesthetic. This study enrolled 152 patients: 96 patients in the OraVerse group and 56 patients in the control group. Of the 152 patients enrolled, 115 were trainable in the assessment method: 72 patients in the OraVerse group and 43 patients in the control group. The study assessed the efficacy of OraVerse through the measurement of time to normal lip sensation for those trainable in the assessment. The median time to normal sensation in patients age 6-11 was reduced by 75 minutes for the OraVerse treated group, a 56% acceleration of the time to normal sensation.
In all OraVerse clinical trials, there were no serious adverse events reported and the most common adverse reaction that was greater than control was transient injection site pain. Although tachycardia and cardiac arrhythmia may occur with the parenteral use of alpha-adrenergic blocking agents, such events are uncommon after submucosal administration of OraVerse.
About OraVerse
OraVerse (phentolamine mesylate) Injection is the only local anesthetic reversal agent that accelerates the return to normal sensation and function following restorative and periodontal maintenance procedures. OraVerse is indicated for the reversal of soft-tissue anesthesia, i.e., anesthesia of the lip and tongue, and the associated functional deficits resulting from an intraoral submucosal injection of a local anesthetic containing a vasoconstrictor. OraVerse is not recommended for use in children less than six years of age or weighing less than 15 kg (33 lbs).
About Prolonged Soft-Tissue Anesthesia
Prolonged soft-tissue anesthesia is an unnecessary and unwanted side effect of local dental anesthesia, especially in routine, restorative or hygienic dental procedures.
Absorption of the local anesthetic into the cardiovascular system is passive and the local anesthetic remains in and around the nerves in the lips, cheek, and tongue causing the unwanted side effect of lingering numbness.
This numbness can last up to five hours following treatment. This results in difficulty in speaking, eating, and drinking, and prevents patients from returning to their daily activities. Prolonged numbness, especially in children, can result in injury due to accidental biting of the lip and/or tongue.
OraVerse is a novel formulation of phentolamine, an alpha-adrenergic antagonist. The hypothesis for the mechanism of action is that OraVerse acts as a vasodilator and the result is faster diffusion of anesthetic into the cardiovascular system and away from the site, thereby reducing the unwanted side effects of lingering lip and tongue numbness.