• 제목/요약/키워드: terbinafine

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자연감염된 개에서 분리한 Microsporum gypseum을 인공감염시킨 기니픽에서 Terbinafine의 효과 II. 임상적 ald 진균학적 효과 (Efficacy of Terbinafine in Guinea Pigs Experimentally Infected with Microsporum gypseum Isolated from Naturally Infected Dog II. Clinical and Mycological Efficacy)

  • 임채형;이창우
    • 한국임상수의학회지
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    • 제17권1호
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    • pp.6-12
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    • 2000
  • 알비노 기니픽의 피부에 Microsporum gypseum을 접종한 후 체중 kg당 20, 40 및 80mg의 terbinafine을 접종 당일부터 9일간 연속 투여하였다. 대조군의 피부는 인설과 가피를 동반한 현저한 염증이 발생되었다. 이와 대조적으로 terbinafine을 경구투여한 처치군에서는 피부 증상이 현저하게 차도를 보였다. 진균학적인 평가를 위해 모근침범시험을 실시 하였다. 체중 kg 당 20∼80mg의 terbinafine을 경구투여한 처치군은 진균학적으로 97∼100%의 치료효과를 나타냈으며, 대주군에서는 치료효과가 전혀 없었다.

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Population Pharmacokinetic Characteristics of Levosulpiride and Terbinafine in Healthy Male Korean Volunteers

  • Lee, Yong-Bok
    • 대한약학회:학술대회논문집
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    • 대한약학회 2003년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.1
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    • pp.84-87
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    • 2003
  • The purposes of this study were to evaluate the population pharmacokinetics of levosulpiride and terbinafine according to several pharmacokinetic models and to investigate the influence of characteristics of subjects such as age, body weight, height and serum creatinine concentration on the pharmacokinetic parameters of levosulpiride and terbinafine, respectively. (omitted)

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자연감염된 개에서 분리한 Microsporum gypseum을 인공감염시킨 기니픽에서 Terbinafine의 효과 1. 인공감염된 기니픽에 있어서 Microsporum gypseum의 생물학적 주기 (Efficacy of Terbinafine in Guinea Pigs Experimentally Infected with Microsporum gypseum Isolated from Nturally Infected Dog 1. The Biological Cycle of M. gypseum in Experimentally Infected Guinea Pigs)

  • 임채형;이창우
    • 한국임상수의학회지
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    • 제17권1호
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    • pp.1-5
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    • 2000
  • Microsporum gypseum을 인공감염시킨 기니픽에서 terbinafine의 치료효과 실험을 위한 전단계 실험으로서 인공감염시킨 기니픽에서 M. gyspeum의 생물학적 주기를 조사하였는데, 이것은 인공감염된 후 효과적인 치료와 평가의 시기를 결정하기 위해 필요하였다. M. gypseum으로 인공감염된 기니픽의 생물학적 주기는 급성기 이후에 자연치유되는 것이 특징이었다. 증식기는 감염 후 5일부터 11일까지 지속되었다. 따라서 다음 번의 치료효과 실험에서 인공감염 당일부터 9일간 계속 terbinafine을 경구투구하고, 마지막 투여 다음 날 진균학적 및 임상적 평가를 하기로 결정하였다.

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라미실 정(테르비나핀 125 mg)에 대한 미코실 정의 생물학적 동등성 (Bioequivalence of Mycosil Tablet to Lamisil Tablet (Terbinafine 125 mg))

  • 조혜영;박현진;정경희;조행남;문재동;이용복
    • 한국임상약학회지
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    • 제10권2호
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    • pp.62-67
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    • 2000
  • Terbinafine has a primary fungicidal action mediated by squalene epoxidase inhibition. Treated fungi accumulate squalene while becoming deficient in ergosterol, an essential component of fungal cell membranes. Bioequivalence of two terbinafine tablets, $Lamisil^{TM}$ (Novartis Korea Ltd., Seoul, Korea) and $Mycosil^{TM}$ (Daewon Pharmaceutical Co., Ltd., Seoul, Korea), was evaluated according to the guidelines of Korea Food and Drug Administration (KFDA). Sixteen normal male volunteers ($20\sim29$ years old) were randomly divided into two groups and a randomized $2\times2$ cross-over study was employed. After oral administration of $Mycosil^{TM}\;or\;Lamisil^{TM}$ (125 mg terbinafine), blood samples were taken at predetermined time intervals and the serum terbinafine concentrations were determined using an HPLC method with UV/VIS detector. The pharmacokinetic parameters $(AUC_t,\;C_{max}\;and\;T_{max})$ were calculated and ANOVA was utilized for the statistical analysis. The results showed that the differences in $AUC_t,\;C_{max}\;and\;T_{max}$ between two tablets based on the $Lamisil^{TM}$ tablet were $-2.24\%,\;-7.68\%\;and\;2.92\%$, respectively. The powers %(1-\beta)\;for\;AVC_t,\;C_{max}\;and\;T_{max}\;were\;87.11\%,\;95.36\%\;and\;99.99\%$, respectively. Minimum detectable differences $(\Delta)\;and\;90\%$ confidence intervals were all less than $\pm20\%$. All these parameters met the criteria of KFDA for bioequivalence, indicating that $Mycosil^{TM}$ tablet is bioequivalent to $Lamisil^{TM}$ tablet.

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Systematic Target Screening Revealed That Tif302 Could Be an Off-Target of the Antifungal Terbinafine in Fission Yeast

  • Lee, Sol;Nam, Miyoung;Lee, Ah-Reum;Lee, Jaewoong;Woo, Jihye;Kang, Nam Sook;Balupuri, Anand;Lee, Minho;Kim, Seon-Young;Ro, Hyunju;Choi, Youn-Woong;Kim, Dong-Uk;Hoe, Kwang-Lae
    • Biomolecules & Therapeutics
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    • 제29권2호
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    • pp.234-247
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    • 2021
  • We used a heterozygous gene deletion library of fission yeasts comprising all essential and non-essential genes for a microarray screening of target genes of the antifungal terbinafine, which inhibits ergosterol synthesis via the Erg1 enzyme. We identified 14 heterozygous strains corresponding to 10 non-essential [7 ribosomal-protein (RP) coding genes, spt7, spt20, and elp2] and 4 essential genes (tif302, rpl2501, rpl31, and erg1). Expectedly, their erg1 mRNA and protein levels had decreased compared to the control strain SP286. When we studied the action mechanism of the non-essential target genes using cognate haploid deletion strains, knockout of SAGA-subunit genes caused a down-regulation in erg1 transcription compared to the control strain ED668. However, knockout of RP genes conferred no susceptibility to ergosterol-targeting antifungals. Surprisingly, the RP genes participated in the erg1 transcription as components of repressor complexes as observed in a comparison analysis of the experimental ratio of erg1 mRNA. To understand the action mechanism of the interaction between the drug and the novel essential target genes, we performed isobologram assays with terbinafine and econazole (or cycloheximide). Terbinafine susceptibility of the tif302 heterozygous strain was attributed to both decreased erg1 mRNA levels and inhibition of translation. Moreover, Tif302 was required for efficacy of both terbinafine and cycloheximide. Based on a molecular modeling analysis, terbinafine could directly bind to Tif302 in yeasts, suggesting Tif302 as a potential off-target of terbinafine. In conclusion, this genome-wide screening system can be harnessed for the identification and characterization of target genes under any condition of interest.

POPULATION PHARMACOKINETICS OF TERBINAFINE IN HEALTHY MALE KOREAN SUBJECTS USING NONMEM

  • Kang, Hyun-Ah;Cho, Hea-Youg;Lee, Suk;Lee, Yong-Bok
    • 대한약학회:학술대회논문집
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    • 대한약학회 2002년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2
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    • pp.421.1-421.1
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    • 2002
  • The purposes of this study were to evaluate the population pharmacokinetics of terbinafine according to two-compartment model will, lag time and to investigate the influence of characteristics or subjects such as body weight and age on the pharmacokinetic parameters of terbinatine. Serum data from 73 healthy male Korean subjects were used for this analysis. After overnight fast. each subject received a single 125 mg oral dose of terbinafine. (omitted)

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라미실 정(테르비나핀 125mg)에 대한 터비넥스 정의 생물학적동등성 (Bioequivalence of Terbinex Tablet to Lamisil Tablet (Terbinafine 125mg))

  • 고현철;홍정희;신인철
    • Biomolecules & Therapeutics
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    • 제11권1호
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    • pp.65-71
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    • 2003
  • Terbinafine is a synthetic allylamine that is available in an oral formulation and is used at a dosage of 250mg/day. It is used as an active antifungal agent and inhibits the fungal enzyme squalene epoxidase, which leads to the accumulation of the sterol squalene, which is toxic to the organism. The purpose of the present study was to evaluate the bioequivalence of two terbinafine tablets, Lamisil (Novartis Korea Ltd.) and Terbinex (C-TRI Ltd.), according to the guidelines of Korea Food and Drug Administration (KFDA). Eighteen normal male volunteers, 26.00$\pm$2.57 year in age and 70.51$\pm$9.36 kg in body weight, were divided into two groups and a randomized 2${\times}$2 cross-over study was employed. After one tablet containing 125 mg of terbinafine was orally administered, blood was taken at predetermined time intervals and the concentrations of terbinafine in plasma were determined using HPLC with UV detector. Pharmacokinetic parameters such as AUC, $C_{max}$ and $T_{max}$ were calculated and ANOVA test was utilized for the statistical analysis of the parameters. The results showed that the differences in AUC, $C_{max}$ and $T_{max}$ between two tablets were -4.191%, 5.223% and -25.720%, respectively when calculated against the Lamisil, tablet. The powers (1-$\beta$) for AUC, $C_{max}$ and $T_{max}$ were 81%, 87% and below 60%, respectively. Minimum detectable differences(.il) at alpha=O.1 and 1-/3=0.8 were less than 20% (e.g., 19.72% and 17.77% for AUC and $C_{max}$, respectively). But minimum detectable differences($\Delta$) at alpha=0.1 and 1-$\beta$=0.8 for $T_{max}$ were more than 20% (e.g., 26.25%). The 90% confidence intervals were within $\pm$20% (e.g., -17.440∼9.06 and -6.713∼17.160 for AUC and $C_{max}$ respectively). But 90% confidence intervals for $T_{max}$ were not within $\pm$20% (e.g., -43.346∼8.083). Another ANOVA test was conducted for logarithmically transformed AUC and $C_{max}$. These results showed that there are no significant differences in AUC and $C_{max}$ between the two formulations: The differences between the formulations in these log transformed parameters were all for less than 20% (e.g., -4.19% and 5.22% for AUC and $C_{max}$, respectively). The 90% confidence intervals for the log transformed data were not the acceptance range of log 0.8 to log 1.25 in AUC but the acceptance range of log 0.8 to log 1.25 in $C_{max}$ (e.g., log 1.13∼log 1.50 and log 0.94-log 1.22 for AUC and $C_{max}$ respectively). The major parameters, AUC and $C_{max}$ met the criteria of KFDA for bioequivalence although $T_{max}$ did not meet the criteria of KFDA (1998 year) for bioequivalence, indicating that Onfran tablet is bioequivalent to Zofran tablet. But in another ANOVA test AUC did not meet the criteria of KFDA (2002) for bioequivalence but $C_{max}$ met the criteria of KFDA (2002 year) for bioequivalence.or bioequivalence.equivalence.equivalence.equivalence.

라미실 정(테르비나핀 125 mg)에 대한 터비나 정의 생물학적 동등성 (Bioequivalence of Terbina Tablet to Lamisil Tablet (Terbinafine 125 mg))

  • 김수진;정인성;조혜영;심영순;정태진;오인준;문재동;이용복
    • Journal of Pharmaceutical Investigation
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    • 제30권2호
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    • pp.133-138
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    • 2000
  • Terbinafine is an orally active antifungal agent as it inhibits the fungal enzyme squalene epoxidase, which is important in the early biosynthetic pathway of ergosterol. This leads to abnormal development of the fungal cell membrane. Bioequivalence of two terbinafine tablets, $Lamisil^{TM}$ (Novartis Korea Ltd.) and $Terbina^{TM}$ (Korean Drug Co., Ltd.), was evaluated according to the guidelines of Korea Food and Drug Administration (KFDA). Sixteen normal male volunteers, $23.56{\pm}1.75$ years old and $65.60{\pm}8.54\;kg$ of body weight, were divided into two groups and a randomized $2{\times}2$ cross-over study was employed. After one tablet containing 125 mg of terbinafine was orally administered, blood was taken at predetermined time intervals and the serum concentrations of terbinafine were determined using an HPLC method with UV detector. The pharmacokinetic parameters $(AUC_t,\;C_{max}\;and\;T_{max})$ were calculated and ANOVA test was utilized for the statistical analysis of parameters. The results showed that the differences in $AUC_t,\;C_{max}\;and\;T_{max}$ between two tablets based on $Lamisil^{TM}$, tablet were -2.53%, -2.98% and 8.13%, respectively. The powers $(1-{\beta})$ for $AUC_t,\;C_{max}\;and\;T_{max}$ were 85.21%, 98.21% and 93.11%, respectively. Minimum detectable differences $({\Delta})$ at ${\alpha}=0.1\;and\;1-{\beta}=0.8$ were all less than 20%. The 90% confidence intervals were all within ${\pm}20%$. All the parameters above met the criteria of KFDA for bioequivalence, indicating that $Terbina^{TM}$ tablet is bioequivalent to $Lamisil^{TM}$ tablet.

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In vivo and in vitro efficacy of florfenicol, terbinafine, and mometasone furoate topical otic solution for the treatment of canine otitis externa

  • Bae, Seulgi;Jin, Yunseok;Oh, Taeho
    • 대한수의학회지
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    • 제61권4호
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    • pp.37.1-37.6
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    • 2021
  • This study evaluated the efficacy of a new, single-dose otic solution combining florfenicol, terbinafine, and mometasone furoate for the treatment of canine otitis externa (OE) in vitro and in vivo. Forty-one client-owned dogs with OE were included in the study and divided into a treatment group that received the test solution and a negative control group that received a normal saline solution. On day 0, the dogs were treated either with the test or the control solution and evaluated over 30 days. Clinical efficacy was evaluated by clinical signs and cytological organism counts. In vitro antimicrobial susceptibility was evaluated by the minimum inhibitory concentration (MIC). After treatment with the test solution, clinical signs continuously decreased and cytological scores were significantly reduced. The results of MIC testing showed that the test solution was potent against the common pathogenic causes of canine OE. In this study, the most common causative pathogens were Staphylococcus pseudintermedius, Pseudomonas spp. and Malassezia pachydermatis. No issues related to safety were identified. Based on these results, this new ototopical drug can be used as first line treatment for canine OE.