• Journal of the korean academy of Pediatric Dentistry
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• v.38 no.1
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• pp.1-8
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• 2011

The objective of this study was to determine the effectiveness of topical 5% EMLA cream versus 20% Benzocaine gel in reducing pain from intra oral needle insertion alone as well as injection of anesthetic. The 2 topical anesthetics were tested against each other bilaterally using a randomized, controlled, single blinded, split mouth design. Phase I was conducted to find out the rapidity of onset action of the two agents on anterior/posterior vestibules and anterior/posterior palatal mucosa. Phase II was conducted to evaluate the efficacy of the two topical anaesthetic agents in reducing the pain of intraoral injections. The agents were left in anterior/posterior vestibules and anterior/posterior palatal mucosa for the amount of time recorded in phase I. Subjects recorded pain on a 100-mm modified visual analog scale(VAS). A pulse oximeter was used to recorded the preoperative and postoperative pulse rates. In phase I of the study, two topical agents showed the longer onset of action at anterior part and vestibules than posterior part and palatal mucosa. EMLA cream showed the rapidest onset of action compared to benzocaine gel except on anterior palatal mucosa. In phase II of the study, the VAS grading of the pain for anesthetic administration showed EMLA cream was significantly(P<.05) better in elimination or reducing the pain on the anterior/posterior palatal mucosa. In conclusion, EMLA cream showed the rapidest onset of action compared to benzocaine gel except on anterior palatal mucosa. EMLA cream was found to be superior to Benzocaine gel with regards to pain reduction for anesthetic administration especially on anterior and posterior palatal mucosa.

• Archives of Plastic Surgery
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• v.36 no.1
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• pp.113-117
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• 2009

Purpose: Although Hydrofluoric acid(HF) is not a strong acid when compared to other hydrogen halides, it is a feared corrosive and is particularly dangerous at higher concentrations. HF burns are characterized by symptoms, often delayed and localized with diluted HF solutions, to include erythema, edema and severe pain. Pain, a well known symptom following exposure to calcium binding. And, EMLA$^{(R)}$ cream is a topical formulation based upon the eutectic mixture of lidocaine and prilocaine and is used in clinical settings to provide pain relief undergoing superficial surgical procedures. The aim of this study is to evaluate effects of EMLA$^{(R)}$ cream, pain - control dressing on the treatment for HF injury wound. Methods: From June 2007 to June 2008, this study was carried out with 10 patients who had HF partial thickness burns. We were applied topically EMLA$^{(R)}$ cream to injured wound with vaseline gauze and 10% calcium gluconate wet gauze dressings. As a principle, in the emergency treatment, partial or complete removal of the bullae along with copious washing with normal saline was done, depending on the degree of HF invasion of the distal digital extremities. The effect of dressing was investigated by visual analogue pain scale. Results: We therefore reviewed 10 cases of HF - induced pain and pain relief treatment principle. The 10 cases who came to the hospital nearly immediately after the injury healed completely without sequelae and EMLA$^{(R)}$ related complications. Conclusion: Proper initial treatment of HF burns are important, if not promptly recognized and properly treated, for produce serious injury. Topical EMLA$^{(R)}$ cream remain a powerful, new advancement for minimizing HF - related pain during dressing procedures. When used appropriately, topical EMLA$^{(R)}$ cream can provide a safe and effective alternative to other forms of HF - pain control treatment.

• Proceedings of the PSK Conference
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• 2000.04a
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• pp.70-81
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• 2000

DA-5018 is a synthetic capsaicin derivative under development as a non-narcotic a analgesic ag$\varepsilon$nt. DA-50 18 showed a potent analgesic activity against acute and chronic pain m model(Tablel, 2.), but it had a narrow margin of safety. DA-5018 did not bind to opioid(${\kappa}, {\delta}, {\mu}$), NKl, CGRP receptors in vitro and its analgesic effect was not antagonized by naloxone, a and it did not develop analgesic tolerance. In addition DA-5018 had no inhibitory effects against c cyclooxygenase and 5-lipooxygenase activities. DA-5018 significantly increased the relcase of substance P from the slices of the rat spinal cord. These results suggest that DA-50 18 is not a narcotic nor aspirin-like analgesic and the release of substance P is one of analgesic mechanism of action of DA-5018. We found that DA-5018 was almost ten times more potent and was at l least IOO-times less irritable compared to capsaicin. Accordingly development of topical formula was adopted. Topical formula was desiged and screened by flux test of DA-5018 using hairless mouse skin and several formulas were selected. With these topical formulas we a assessed the analgesic efficacy and carried out the toxicity, skin irritation and pharmacokinetic studies. In streptozotocin-induced hyperalgesic rat and 50 % galactose-fed hyperalgesic rat as diabetic pain models, DA-5018 cream increased the pain thresh이ds up to 77.0% and 24.4% respectively, while Zostrix-HP(capsaicin cream) incr$\varepsilon$as cd by 65.9% and 21.0%. DA-5018 c cream showed a good analgesic effect as welI in FCA-induced arthritic rat. DA-5018 cream did not show any toxicological signs in acute and chronic toxicity test and had little skin irritation in car swclIing and scratching t$\varepsilon$st. Pharmacokinetics of DA-50 18 were studied after topical application of ${14}^C$-Iabelled or unlabelIed DA-5018 cream. Plasma and skin concentrations c except applied skin wcre below the dctection limit and after 7-day cummulative application, plasma concentrations were also below detection limit DA-50 18 may have an advantag$\varepsilon$ ov$\varepsilon$r c capsaicin and is now being developed as a topical agent for the treatment of pains. DA-50 18 cream was approved for Korean IND and is now under a Phase II clinical study for arthritic pain a after finising Phase I study. DA-50 18 was also liscensed out to Stiefel Company in America in

• Journal of Veterinary Clinics
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• v.38 no.2
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• pp.56-62
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• 2021

Madecassoside, an active ingredient extracted from Centella asiatica, is used for treatment of various skin disorders in humans. However, the effect of madecassoside on the skin of dogs and cats has not been studied yet. The purpose of this study was to evaluate clinical efficacy of topical madecassoside cream in dogs and cats with skin diseases. A total of twenty-one dogs and ten cats with various skin diseases were included in the study. The 1% topical madecassoside cream was applied to the animal's skin lesion at least once a day for 7 days, and the skin condition was evaluated before the application of madecassoside cream (day 0) and 7 days after the application (day 7). The skin condition was scored by five clinical indices: canine atopic dermatitis extent and severity index-4 (CADESI-4), coat condition, pruritus, scale, and general condition. In dogs, all five clinical indices (CADESI-4, coat condition, pruritus, scale, and general condition) were significantly decreased on day 7 compared to those on day 0 (p < 0.0001, p < 0.05, p < 0.001, p < 0.01, and p < 0.05, respectively). In cats, the CADESI-4 and scale were significantly decreased on day 7 compared to those on day 0 (p < 0.01 and p < 0.05, respectively). No adverse effects were observed during the trial period in the dogs and cats included in this study. The results of this study demonstrate that the topical madecassoside cream is applicable to skin lesions in dogs and cats.

• Biomolecules & Therapeutics
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• v.5 no.2
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• pp.117-124
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• 1997

The analgesic effects of DA-5018, a new caosaucin derivative, were evaluated in various experimental pain models. Drugs were administered subcutaneously or topically. When drugs were administered subcutaneously, 1) the $ED_{50}$ of DA-5018, morphine . HCI, capsaicin and acetaminophen were 0.091-2.0, 0.3-4.3, 1.4-26.5 and 45.4-643 mg/kg, respectively in various pain or inflammatory models including acetic acid writhing, formalin, tail flick, Randall-Selitto, hot plate and crouton oil-induced ear edema test, 2) the AD2 values (the dose for doubling of pain threshold of vehicle control) of DA-5018, capsaicin and ketoprpgin were 1.07 $\pm$ 0. 18, 23.47$\pm$4.46 and 2.97$\pm$0.43 mg/kg in Freund's complete adjuvant (FCA)-induced arthritic pain model. And by topical application, 1) neither DA-5018 0.3% cream nor Zostrix-HP (capsaicin 0.075%) were effective in formalin test, 2) although DA-5018 0.3% cream significantly inhibited the croton oil-induced ear edema being better than Zostrix-HP and Kenofen (ketoprofen 3%). 3) In FCA model, DA-5018 0.3% cream reversed the decreased pain threshold of arthritic rat from 136.4 g (day 0) to 289.0 g (day 5) and 250.1 g (day 10), which was similar to Zostrix-HP. These results suggest that DA-5018 administered subcutaneously has a potent and broad analgesic spectrum than nonsteroidal antiinflammatory drugs against acute and chronic pain, and by topical application it exerts comparable analgesic and antiinglammaatory effects to capsaicin cream.

• CELLMED
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• v.9 no.3
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• pp.7.1-7.4
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• 2019

In this study, we investigated an inhibitory effect of AST cream on atopic dermatitis (AD) using a 2,4-dinitrochlorobenzene-induced AD murine model. Topical treatment with AST cream ameliorated the severity of AD-like lesional skin through decreases in infiltration of inflammatory cells and time of scratching behaviors. Also, AST cream reduced histamine and IgE levels in serum. The protein levels of IL-4 and IL-6 in AD-like lesional skin were suppressed by AST cream. These findings suggest that AST cream would be an alternative therapeutic agent for AD-like skin diseases.

• Korean journal of dermatology
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• v.56 no.10
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• pp.609-613
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• 2018

Background: Psoriasis is a chronic inflammatory skin disease with an incidence of 0.5~3% of the worldwide population. The pathogenesis of psoriasis is related to dysregulated keratinocyte function and immune reactions. Notably, genetic factors are considered important etiological contributors. Globally, several researchers have recently performed genome-wide association studies (GWAS) to identify the genes related with psoriasis. Objective: We aimed to investigate the expression pattern of 2 candidate genes that were identified by GWAS. These include interleukin 28 receptor alpha (IL28RA) and CUB and Sushi multiple domains 1 (CSMD1). Methods: We applied imiquimod cream to develop a psoriasis-like mouse model and obtained skin tissue. We performed immunohistochemistry to detect the expression of IL-28A and CSMD1. Results: IL28RA expression increased at an early time point such as 1 day after the topical application of 5% imiquimod cream. However, its expression returned to baseline levels 2 weeks after the topical application of imiquimod cream. CSMD1 expression also increased after the topical application of imiquimod, with increased expression particularly observed in the upper epidermal layer. Notably, CSMD1 expression decreased 7 days after imiquimod cream application. Conclusion: These results suggest that IL28RA and CSMD1 may play key roles in the pathogenesis of psoriasis.

• Journal of Dental Anesthesia and Pain Medicine
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• v.16 no.4
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• pp.237-244
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• 2016

Topical anesthetics act on the peripheral nerves and reduce the sensation of pain at the site of application. In dentistry, they are used to control local pain caused by needling, placement of orthodontic bands, the vomiting reflex, oral mucositis, and rubber-dam clamp placement. Traditional topical anesthetics contain lidocaine or benzocaine as active ingredients and are used in the form of solutions, creams, gels, and sprays. Eutectic mixtures of local anesthesia cream, a mixture of various topical anesthetics, has been reported to be more potent than other anesthetics. Recently, new products with modified ingredients and application methods have been introduced into the market. These products may be used for mild pain during periodontal treatment, such as scaling. Dentists should be aware that topical anesthetics, although rare, might induce allergic reactions or side effects as a result of an overdose. Topical anesthetics are useful aids during dental treatment, as they reduce dental phobia, especially in children, by mitigating discomfort and pain.

• Journal of Pharmaceutical Investigation
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• v.28 no.3
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• pp.177-183
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• 1998

Low toxicity, reverse thermal gelation and high drug loading capabilities suggest that poloxamer 407 gels have great potential as a topical drug delivery system. Kojic acid (KA) is an antimelanogenic agent which has been widely used in cosmetics to whiten the skin color. However, it has the drawbacks of skin irritancy due to its acidic pH. Poloxamer gels of different polymer contents were formulated to overcome the problem and compared to the cream type formulations of either w/o/w multiple emulsion cream or o/w type emulsion cream. Using Franz diffusion cells mounted with a synthetic cellulose membrane (MWCO 12,000), drug release characteristics of the formulations were evaluated by the HPLC assay of KA concentration in the receptor compartment of pH 7.4 phosphate buffered saline solutions. Drug release from w/o/w multiple emulsion cream was controlled by oil membrane, showing the apparent zero order release kinetics. The KA release from the poloxamer gels was also controlled by the gel matrix, showing that drug release increased linearly as KA contents increase, but decreased exponentially as the polymer contents increase. In the skin irritancy test, the primary irritancy index(PII) of poloxamer gel base was lower than those of multiple emulsion cream base and o/w cream. Depending on KA contents or polymer contents in the gel. PH values in poloxamer gels were ranged from 1.3 to 2.0, which are interpreted as low or negligible irritation on skin. There was a good correlation between the log value of flux in drug release and PII value in skin irritation. It was possible to conclude that the poloxamer gels containing KA might be a good candidate for an antimelanogenic topical delivery system by virtue of the controlled release of the drug and the reduced skin irritancy.

• 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.