TEMPE: Topical Eutectic-Like Mixture for Premature Ejaculation

Background: Premature ejaculation (also known as rapid or early ejaculation) is the most common form of sexual dysfunction experienced by men, but there is presently an unmet need for a licensed pharmaceutical product that can be used on demand and that is effective from the first dose. Objective: TEMPE^® (Topical Eutectic-Like Mixture for Premature Ejaculation; Plethora Solutions Plc.) is a proprietary metered-dose aerosol containing a combination of the well-known local anaesthetics lidocaine and prilocaine in a novel formulation. The authors evaluate here the progress that has been made towards the reformulation of these local anaesthetic agents into a unique eutectic-like formulation for use as a desensitising agent in the treatment of premature ejaculation, as well as examining other potential uses for the spray, such as pain relief at skin-graft donor sites. Methods: Both lidocaine and prilocaine are soluble in the hydrofluoroalkane (HFA-134a) propellant, providing a unique formulation in which the pressurised liquid propellant is used as the solvent. Deployment of the metered-dose chamber vaporises the propellant, spraying lidocaine and prilocaine, now forced into a eutectic-like combination that remains in liquid form at temperatures well below their individual melting points, onto the target surface. The site is thus easily covered in a controlled dose of pure local anaesthetic in base form, providing ideal circumstances for optimised absorption through non- or poorly-keratinised skin, mucus membranes and wound surfaces. Results/conclusion: TEMPE has been developed for use in premature ejaculation and preliminary results show promising improvements in intravaginal ejaculatory latency, as well as patient-reported outcomes.     

双氯芬酸钠利多卡因联合长效止痛剂用于肛肠病术后疼痛的临床研究

目的：探讨肛肠疾病术后有效镇痛的方法。方法：将肛肠病术后86例随机单盲分为A组（双氯芬酸钠利多卡因加长效止痛剂）56例、B组（长效止痛剂）30例。观察记录术后6、24、48h镇痛评分（VAS）、不良反应发生情况。结果：术后6、24hVAS评分A组显著低于B组（P〈0．01），两组48hVAS差异无统计学意义（P〉0．05），A组不良反应明显少于B组（P〈0．01）。结论：双氯芬酸钠利多卡因与长效止痛剂联合应用于肛肠术后镇痛效果良好，可持续长效镇痛，不良反应少，是一经济适用简便的术后多模式镇痛方法。     

Normal Resting and Exercising Muscle Blood Flow during Acute Ethanol Infusion

A 2 year-old drank from a bottle of viscous lidocaine. Coughing and choking were prompt, and seizures began within 10 to 15 seconds. Intraosseous phenobarbital 40?mg/kg stopped seizures temporarily, 30?mg/kg more plus lorazepam 20?mg/kg were needed for complete control. Suctioning of the airway revealed viscous material compatible with the drug. Bilateral hilar pneumonia ensued rapidly. The syndrome of inappropriate antidiuretic hormone secretion occurred and was countered appropriately. Intubation, performed on admission, could not be discontinued. The adult respiratory distress syndrome, characterized by a typical diffuse X-ray pattern and poor oxygenation, developed. Bilateral pneumothoraces complicated care. The patient required 14 days of extracorporeal membrane oxygenation before recovery. A lidocaine level was obtained at 4?h post-ingestion and was 0.5 μg/mL (2 μmol/L). The rapid onset of seizures suggests that the drug was absorbed from the pulmonary bed. This possibility is supported by the finding of viscous-lidocaine-like material in the trachea, the rapid development of aspiration pneumonia, and the development of adult respiratory distress syndrome, which has been observed in adults when lidocaine was used in the trachea for procedures.     

A Prospective,Randomized, Double-Blind Study of the Anesthetic Efficacy of Sodium Bicarbonate Buffered 2% Lidocaine With 1?:?100,000 Epinephrine in Inferior Alveolar Nerve Blocks

The authors, using a crossover design, randomly administered, in a double-blind manner, inferior alveolar nerve (IAN) blocks using a buffered 2% lidocaine with 1 : 100,000 epinephrine/sodium bicarbonate formulation and an unbuffered 2% lidocaine with 1 : 100,000 epinephrine formulation at 2 separate appointments spaced at least 1 week apart. An electric pulp tester was used in 4-minute cycles for 60 minutes to test for anesthesia of the first and second molars, premolars, and lateral and central incisors. Anesthesia was considered successful when 2 consecutive 80 readings were obtained within 15 minutes, and the 80 reading was continuously sustained for 60 minutes. For the buffered 2% lidocaine with 1 : 100,000 epinephrine/sodium bicarbonate formulation, successful pulpal anesthesia ranged from 10–71%. For the unbuffered 2% lidocaine with 1 : 100,000 epinephrine formulation, successful pulpal anesthesia ranged from 10–72%. No significant differences between the 2 anesthetic formulations were noted. The buffered lidocaine formulation did not statistically result in faster onset of pulpal anesthesia or less pain during injection than did the unbuffered lidocaine formulation. We concluded that buffering a 2% lidocaine with 1 : 100,000 epinephrine with sodium bicarbonate, as was formulated in the current study, did not statistically increase anesthetic success, provide faster onset, or result in less pain of injection when compared with unbuffered 2% lidocaine with 1 : 100,000 epinephrine for an IAN block.     

芬太尼与利多卡因宫旁阻滞麻醉用于人工流产的疗效比较

目的：比较芬太尼与利多卡因宫旁阻滞麻醉在人工流产术中的疗效。方法：选择我院2009年3月～2009年5月门诊终止妊娠早孕妇女100例,分为两组。芬太尼组50例,利多卡因组50例。比较两组宫旁阻滞麻醉镇痛效果及人流综合征发生率。结果：芬太尼组的镇痛效果明显优于利多卡因组,人流综合征的发生率明显低于利多卡因组。结论：芬太尼宫旁阻滞麻醉具有镇痛效果明显,人流综合征发生率低等优点,优于利多卡因麻醉效果。     

盐酸利多卡因注射液碱化后稳定性试验

目的：考察盐酸利多卡因注射液碱化后的稳定性。方法：盐酸利多卡因注射液配制成4种浓度的溶液,每个浓度分别加入不同量的5％NaHCO3溶液,测定碱化前后4种溶液不同时间的pH值及利多卡因的含量。结果：4种浓度的溶液碱化后随着加入的NaHCO3量的增加,其pH值也逐渐增加,与碱化前相比较均有明显升高,百分含量随着时间的延长,均有显著上升,但随着加入NaHCO3量的增加含量显著下降,放置24h有针状结晶析出,结论：碱化时加NaHCO3量最好在0．5－2．0ml之间,碱化后放置时间不宜过长。     

Effect of lidocaine on retinal aquaporin-4 expression after ischemia/reperfusion injury in the rat★

BACKGROUND: Several studies have demonstrated that high doses of lidocaine can reduce edema in rats with brain injury by down-regulating aquaporin-4 (AQP4) expression. The hypothesis for the present study is that lidocaine could retinal edema that is associated with AQP4 expression. OBJECTIVE: This study was designed to investigate the interventional effects of lidocaine on retinal AQP4 expression and retinal edema following ischemia/reperfusion injury in the rat. DESIGN, TIME AND SETTING: This study, a randomized, controlled, animal experiment, was performed at the Basic Research Institute, Chongqing Medical University from September 2006 to May 2007. MATERIALS: Seventy-five, healthy, adult, female, Sprague-Dawley rats were included. A total of 50 rats were used to establish a retinal ischemia/reperfusion injury model using an anterior chamber enhancing perfusion unit. Rabbit anti-rat AQP4 antibody was purchased from Santa Cruz Biotechnology, USA. METHODS: All 75 rats were randomly divided into three groups, with 25 rats in each: control, model, and lidocaine. At each time point (1, 6, 12, 24, and 48 hours after modeling, five rats for each time point), each rat in the lidocaine group was intraperitoneally administered lidocaine with an initial dose of 30 mg/kg, followed by subsequent doses of 15 mg/kg every six hours. The entire treatment process lasted three days for each rat. At each above-mentioned time point, rats in the model group were modeled, but not administered any substances. Rats in the control group received the same treatments as in the lidocaine group except that lidocaine was replaceld by physiological saline. MAIN OUTCOME MEASURES: Following hematoxylin-eosin staining, rat retinal tissue was observed to investigate retinal edema degree through the use of an optical microscope and transmission electron microscope. Retinal AQP4 expression was determined by immunohistochemistry. RESULTS: At each above-mentioned time point, AQP4 expression was significantly increased in the model group compared to the control group (P < 0.05); this change was consistent with the degree of retinal edema. In the lidocaine group, retinal AQP4 expression was significantly decreased (P < 0.05), and retinal edema was reduced, compared with the model group. CONCLUSION: Lidocaine inhibits rat retinal AQP4 expression following ischemia/reperfusion injury, leading to a reduction of retinal edema. Key Words: ischemia/reperfusion; lidocaine; aquaporin-4     

Infusions of Lidocaine into the Amygdala, but not the Preoptic Area, Block Pseudopregnancy in the Rat

In the rat, vaginocervical stimulation (VCS) received during mating is required for the subsequent expression of 10–12 days of twice-daily prolactin surges that are necessary for pregnancy or pseudopregnancy (PSP). This temporal separation of sensory stimulus and neuroendocrine response suggests that a mnemonic of the vaginocervical stimulation is created in the brain that triggers and sustains the daily prolactin surges. We investigated the possible involvement of the medial preoptic area (mPOA) and the medial amygdala (mAMYG) as potential neural sites involved in the processing of this neuroendocrine arc. Cycling female rats were bilaterally implanted with intracerebral cannulae in either the mPOA or mAMYG. On proestrus, females were manually palpated to confirm sexual receptivity and then received bilateral infusions of either the local anesthetic lidocaine, the Ca⁺⁺ channel blocker, verapamil, or phosphate-buffered saline (PBS) into either brain site before or both before and after receipt of 15 intromissions from an experienced male. Unmated control females received comparable infusions of lidocaine or verapamil, and were placed in the empty test arena for 10 min. Infusions consisted of either a single bilateral infusion 15 min before mating (Expt. 1), bilateral infusions both 15 min before and after mating (Expt. 2) or eight bilateral infusions separated by 30 min intervals spanning a period beginning 45 min before and ending 2 h 45 min after mating (Expt. 3). None of the lidocaine infusions into the mPOA prevented the establishment of PSP, and neither verapamil infusions into the mAMYG nor the shorter-term neural block (i.e. single or double lidocaine infusions) of the mAMYG prevented mating-induced PSP. However, the longer-term neural block (i.e. multiple lidocaine infusions) of the mAMYG significantly reduced the incidence of PSP. These data support previous findings that the mAMYG receives sensory input from VCS, and suggest that the mAMYG is a site at which a mnemonic of VCS is established.     

利多卡因膀胱灌洗治疗耻骨上前列腺切除术后膀胱痉挛

目的观察利多卡因膀胱灌洗对耻骨上前列腺切除术后膀胱痉挛的治疗作用。方法选择耻骨上经膀胱前列腺切除术 36例 ,治疗组用利多卡因行膀胱持续灌洗 (每 5 0 0ml生理盐水加入 2 %利多卡因 10 0mg) ,对照组用生理盐水灌洗。结果利多卡因治疗组的膀胱灌洗液转清时间明显短于对照组 (P <0 .0 5 ) ,术后膀胱痉挛发生例数、每日发生次数、持续天数均明显少于对照组 (P <0 .0 5 )。结论利多卡因膀胱灌洗可显著降低耻骨上前列腺切除术后膀胱痉挛的发生率