• The Korean Journal of Pharmacology
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• v.23 no.2
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• pp.113-121
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• 1987

Local anesthetics were investigated for their effects on mitochondrial electron transport system, production of superoxide radical from submitochondrial particles and malondialdehyde production through lipid per oxidation. Local anesthetics had various effects on activities of enzymes in electron transport chain. The activities of NADH dehydrogenase, NADH oxidase and NADH-ubiquinone oxidoreductase were effectively inhibited by lidocaine, procaine and dibucaine but slightly influenced by cocaine. The activities of succinate dehydrogenase, succinate-cytochrome c oxidoreductase and succinate-ubiquinone oxidoreductase were inhibited by lidocaine and dibucaine, but the succinate oxidase activity was stimulated by local anesthetics. Both dihydroubiquinone-cytochrome c oxidoreductase and cytochrome c oxidase activities were inhibited by local anesthetics. In these reactions, the response of Complex I segment to local anesthetics was greater than other Complex segments. Local anesthetics inhibited both the superoxide production from submitochondrial particles supplemented with succinate or NADH and the enhanced production of superoxide radicals by antimycin. The malondialdehyde production by oxygen free radicals was inhibited by local anesthetics. These results suggest that the inhibition of superoxide and malondialdehyde production caused by local anesthetics may be brought by suppression of the electron transport in mitochondria at sites in or near complex I segment.

• Journal of Dental Anesthesia and Pain Medicine
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• v.20 no.1
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• pp.29-37
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• 2020

Background: This study evaluated the efficacy of three intraoral topical anesthetics in reducing the injection needle prick pain from local anesthetic among children aged 7-11 years old. Methods: It is a prospective, Interventional, parallel design, single-blind, randomized clinical trial in which subjects (n=90) aged 7-11 years were included in the study based on an inclusion criteria. Subjects were divided into three groups based on computer-generated randomization with an allocation ratio of 1:1:1. Groups A, B, and C received benzocaine 20% jelly (Mucopain gel, ICPA health products Ltd, Ankleshwar, India), cetacaine anesthetic liquid (Cetylite Industries, Inc, Pennsauken, NJ), and EMLA cream (2% AstraZeneca UK Ltd, Luton, UK), respectively, according to manufacturer's instructions, for 1 minute prior to local anesthetic injection. After application of topical anesthetic agent, for all the groups, baseline pre-operative (prior to topical anesthetic administration) and post-operative scores (after local anesthetic administration) of pulse rate was recorded using Pulse oximeter (Gibson, Fingertip Pulse Oximeter, MD300C29, Beijing Choice Electronic). Peri-operative (i.e., during the administration of local anesthesia) scores were recorded using Face, Legs, Activity, Cry, Consolability (FLACC) Scale, Modified Children hospital of Eastern Ontario Pain Scale (CPS) behavior rating scale, and Faces Pain Scale (FPS-R) - Revised (For self-reported pain). Direct self-reported and physiological measures were ascertained using FPS-R - Revised and Pulse oximeter, respectively, whereas CPS and FLACC scales assessed behavioral measures. To test the mean difference between the three groups, a one way ANOVA with post hoc tests was used. For statistical significance, a two-tailed probability value of P < 0.05 was considered as significant. Results: The Cetacaine group had significantly lower pain scores for self-report (P < 0.001), behavioral, and physiological measures (P < 0.001) than the other two groups. However, there was no significant difference between the Benzocaine group and EMLA group during palatal injection prick. Conclusion: Cetacaine can be considered as an effective topical anesthetic agent compared to benzocaine 20% jelly (Mucopain gel) and EMLA cream.

• The Korean Journal of Pain
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• v.9 no.1
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• pp.200-205
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• 1996

Radiofrequency thermocoagulation(RF) techniques are safe and effective methods as compared to neurodestructive procedure. Other advantages are: ability to perform RF lesions under local or sedative anesthesia, rapid recovery period, low incidence of morbidity and mortality, ability to repeat RF lesions, and leaves no significant scarring. We performed C2 ganglionotomy by RF lesion generator on a patient, suffering post-traumatic occipital neuralgia, as the patient did not respond to conservative therapies such as: trigger point injection, TENS, cryotherapy and stretch, occipital nerve block, C2 ganglion block. Prognostic nerve block was performed usng local anesthetics. Excellent effect was conformed before C2 ganglionotomy. This procedure was performed under fluoroscopy. Type RCK-2A Rosomoff Cordotomy kit was used to stabilize the head and neck. Postoperatively, the patient was free of occipital pain and head motions no longer triggered pain. To date, the patient remains symptom free except for some cervical discomfort.

• YAKHAK HOEJI
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• v.47 no.2
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• pp.78-84
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• 2003

Local anesthetics are used to reduce pain, but they are so frequently injected to patients. So, we prepared lidocaine solid lipid microspheres (SLM) as long acting abdominal injection using spray drying method and evaluated drug entrapment, particle size, SEM, zeta potential and in vitro and in vivo drug release pattern, The particle sizes of SLM were 30∼100$\mu$m and it is enough to inject into abdominal tissue. The entrapment efficiency of SLM was over 95％ as spray drying method. Surfactant and PC decreased the burst effect by 20∼30％. In in vivo test, C-6 showed controlled release concentration profile in plasma for 8 days and C-5 sustained longer than we expected.

• The Korean Journal of Pain
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• v.9 no.1
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• pp.39-45
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• 1996

Tachyphylaxis to local anesthetics has shown to be promote longer interanalgesic intervals between injections. Previous study demonstrated thermal hyperalgesia accelerates development of tachyphylaxis to sciatic nerve blockade in rats, while MK-801 prevents development of tachyphylaxis. Dextromethorphan is one of NMDA receptor antagonist similar to MK-801. A hypothesis that dextromethorphan would prevent the development of tachyphylaxis was tested in this study. A catheter was surgically implanted along the sciatic nerve a in rat. After recovery from surgery, the animal received repeated injections of 3% 2-chloroprocaine followed by motor block testing with or without hot-plate testing at $56^{\circ}C$. In other experiments, dextromethorphan was administrered by intraperiotneal injection prior to an injection of local anesthetic therough the implanted catheter. Sensory and motor testing was then carried out. Rats injected with 2-chloroprocaine and subjected to hot-plate testing, developed tachyphylaxis to motor and sensory blockade. However, animals pretreated with dextromethorphan did not develop tachyphylaxis over series of three injections. Dextromethorphan seems to prevent development of tachyphylaxis to sciatic nerve blockade in this rat model. Dextromethorphan, one of N-Methyl-D-aspartate receptor antagonist, can be applied to prolong the effect of local anesthetic.

• Journal of Korean Neurosurgical Society
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• v.48 no.5
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• pp.429-433
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• 2010

Objective : This prospective study evaluated the use of continuous sedation using propofol and remifentanil when carpal tunnel release (CTR) was performed under local anesthesia. Methods : We sedated 60 patients undergoing CTR using local anesthesia with remifentanil at loading and continuous doses of $0.5\;{\mu}g\;kg^{-1}$ and $0.05\;{\mu}g\;kg^{-1}min^{-1}$, respectively, and propofol, using a target controlled infusion (TCI) pump set to a target of $2\;{\mu}g\;mL^{-1}$ (group A), or with the same drug doses except that the continuous remifentanil dose was $0.07\;{\mu}g\;kg^{-1}min^{-1}$ (group B) or $0.1\;{\mu}g\;kg^{-1}min^{-1}$ (group C). Results : In group B, the levels of pain when local anesthetics were administered (p = 0.001), intraoperative pain (p < 0.001) and anxiety (p = 0.001) were significantly lower than those of group A. Furthermore, the incidence of adverse events, including desaturation (p < 0.001) and vomiting (p = 0.043), was significantly lower in group B than in group C. Conclusion : Continuous sedation using an appropriate dose of remifentanil and propofol can be used as safe, efficacious ambulatory anesthesia in cases of CTR under local anesthesia, performed using only 2 mL of local anesthetic, with a high degree of patient satisfaction.

• Biomolecules & Therapeutics
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• v.19 no.3
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• pp.357-363
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• 2011

In relieving local pains, ropivacaine has been widely used. In case of their application such as ointments and creams, it is difficult to expect their effects for a significant period of time, because they are easily removed by wetting, movement and contacting. Therefore, the new formulations that have suitable bioadhesion were needed to enhance local anesthetic effects. The effect of drug concentration and temperature on drug release was studied from the prepared 1.5% Carboxymethyl cellulose (CMC) (150MC) gels using synthetic cellulose membrane at $37{\pm}0.5^{\circ}C$. As the drug concentration and temperature increased, the drug release increased. A linear relationship was observed between the logarithm of the permeability coefficient and the reciprocal temperature. The activation energy of drug permeation was 3.16 kcal/mol for a 1.5% loading dose. To increase the skin permeation of ropivacaine from CMC gel, enhancers such as saturated and unsaturated fatty acids, pyrrolidones, propylene glycol derivatives, glycerides, and non-ionic surfactants were incorporated into the ropivacaine-CMC gels. Among the enhancers used, polyoxyethylene 2-oleyl ether showed the highest enhancing effects. For the efficacy study, the anesthetic action of the formulated ropivacaine gel containing an enhancer and vasoconstrictor was evaluated with the tail-flick analgesimeter. According to the rat tail-flick test, 1.5% drug gels containing polyoxyethylene 2-oleyl ether and tetrahydrozoline showed the best prolonged local analgesic effects. In conclusion, the enhanced local anesthetic gels containing penetration enhancer and vasoconstrictor could be developed using the bioadhesive polymer.

• Journal of Korean Neurosurgical Society
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• v.52 no.3
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• pp.228-233
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• 2012

Objective : Chronic neck or back pain can be managed with various procedures. Although these procedures are usually well-tolerated, a variety of side effects have been reported. In this study we reviewed cases of unexpected temporary adverse events after blocks and suggest possible causes. Methods : We reviewed the records of patients treated with spinal pain blocks between December 2009 and January 2011. The types of blocks performed were medial branch blocks, interlaminar epidural blocks and transforaminal epidural blocks. During the first eight months of the study period (Group A), 2% mepivacaine HCL and triamcinolone was used, and during the last six months of the study period (Group B), mepivacaine was diluted to 1% with normal saline. Results : There were 704 procedures in 613 patients. Ten patients had 12 transient neurologic events. Nine patients were in Group A and one was in Group B. Transient complications occurred in four patients after cervical block and in eight patients after lumbar block. Side effects of lumbar spine blocks were associated with the concentration of mepivacaine (p<0.05). The likely causes were a high concentration of mepivacaine in five patients, inadvertent vascular injection in three patients, intrathecal leak of local anesthetics in one, and underlying conversion disorder in one. Conclusion : Spinal pain blocks are a good option for relieving pain, but clinicians should always keep in mind the potential for development of inevitable complications. Careful history-taking, appropriate selection of the anesthetics, and using real-time fluoroscopy could help reduce the occurrence of adverse events.

• The Korean Journal of Pain
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• v.14 no.2
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• pp.193-198
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• 2001

Background: Anterior atlantoaxial subluxation (AAS) is a frequent phenomenon in rheumatoid arthritis (RA). AAS compresses the C2 ganglion or nerve and is a cause of posterior neck pain or occipital headache. Methods: We selected RA patients that had developed posterior neck pain or occipital headache caused by AAS. AAS was diagnosed by an increase of ADI (atlantodental interval). A distance of 3 mm or more was considered significant. Patients with vertical subluxation or symptoms suggestive of myelopathy were excluded. Before C2 RF ganglionotomy, we proceeded with a C2 ganglion block or greater occipital nerve block used by local anesthetics. For C2 RF ganglionotomy, the patient was placed in the supine position on a fluoroscopic table. A 100 mm, 4 mm active tip electrode was chosen. Following sensory stimulation at 0.2 to 0.6 V, the lesion was performed at a temperature of $60^{\circ}C$ to $65^{\circ}C$ for 60 sec. We followed up the patient after 6 months later. Results: All cases were female and the average duration of RA was 8.5 years. The duration of posterior neck pain or occipital headache was 1-8 months. The average ADI was 4.2 mm and the McGregor index was 3.3 mm on the average. In all cases, the score on the 4 point Likert scale was 4 (pain free) during the follow-up period. Conclusions: We found that the occipital headache or posterior neck pain caused by AAS in rheumatoid arthritis patients was alleviated over a short term follow up. C2 RF ganglionotomy is suggested as an effective palliative treatment for AAS in RA patients.

• Clinics in Shoulder and Elbow
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• v.24 no.4
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• pp.224-230
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• 2021

Background: Local anesthetics often are used in rotator cuff tears as therapeutic tools, although some cases have reported that they have detrimental effects. Neurotropin (NTP) is used widely in Japan as a treatment for various chronic pain conditions and is shown to have protective effects on cartilage and nerve cells. In this study, we investigated the protective effect of NTP against lidocaine-induced cytotoxicity. Methods: Tenocytes from rotator cuff tendons were incubated with lidocaine, NTP, lidocaine with NTP, and a control medium. Cell viability was evaluated using the WST-8 assay. Cell apoptosis was detected via annexin V staining using flow cytometry. The expression of BCL-2 and cytochrome c, which are involved in the intrinsic mitochondrial pathway of apoptosis, was evaluated via Western blotting and immunohistochemical staining. Results: In the cell viability assay, lidocaine decreased cell viability in a dose-dependent manner, and NTP did not affect cell viability. Moreover, NTP significantly inhibited the cytotoxic effect of lidocaine. The flow cytometry analysis showed that lidocaine significantly induced apoptosis in tenocytes, and NTP considerably inhibited this lidocaine-induced apoptosis. Western blotting experiments showed that lidocaine decreased the protein expression of BCL-2, and that NTP conserved the expression of BCL-2, even when used with lidocaine. Immunohistochemical staining for cytochrome c showed that 0.1% lidocaine increased cytochrome c-positive cells, and NTP suppressed lidocaine-induced cytochrome c expression. Conclusions: NTP suppresses lidocaine-induced apoptosis of tenocytes by inhibiting the mitochondrial apoptotic pathway. Intra-articular/bursal injection of NTP with lidocaine could protect tenocytes in rotator cuff tendons against lidocaine-induced apoptosis.