• 제목/요약/키워드: Dutasteride

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A Method to Monitor Dutasteride in Rat Plasma Using Liquid-Liquid Extraction and Multiple Reaction Monitoring: Comparisons and Validation

  • Kang, Myung Joo;Cho, Ha Ra;Lee, Dong Hoon;Yeom, Dong Woo;Choi, Young Wook;Choi, Yong Seok
    • Mass Spectrometry Letters
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    • 제5권3호
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    • pp.79-83
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    • 2014
  • Three different dutasteride extraction methods were compared and a method based on liquid-liquid extraction (LLE) using methyl tert-butyl ether and methylene chloride was proved to be more effective than others for the extraction of dutasteride and finasteride, the internal standard (IS), from rat plasma. Additionally, a method composed of the LLE extraction, liquid chromatography, and multiple reaction monitoring (MRM) to target dutasteride and IS was validated by assessing specificity, linearity ($r^2$ = 0.9993, 5 - 400 ng/mL), sensitivity (the limit of detection: 4.03 ng/mL; the limit of quantitation: 12.10 ng/mL), accuracy (intra-day: 89.4 - 105.9%; inter-day: 84.9 - 100.9%), precision (intra-day: 0.8 - 6.9%; inter-day: 2.9 - 15.9%), and recovery (84.7 - 107.8%). Since the validated method was successfully applied to a pharmacokinetic study of dutasteride, it can be useful for the pharmacokinetic evaluation of newly developed dutasteride formulations.

미국 식품의약국 미승인 두타스테라이드의 국내 남성형 탈모증 약물요법 적용에대한 후향적 평가 (Retrospective Pharmacotherapeutic Evaluation of Dutasteride not Approved by US FDA for Androgenetic Alopecia in Korea)

  • 천영주;김정태;임성실
    • 한국임상약학회지
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    • 제25권3호
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    • pp.171-177
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    • 2015
  • Background: Androgenetic alopecia (AGA), one of alopecias, requires continuous treatment in order to prevent or stop it, and patient's compliance is very important. Currently, only two drugs (finasteride, minoxidil) have been approved for AGA by Food and Drug Administration of United States (US FDA). However, another ${\alpha}-2$ reductase inhibitor, dutasteride, is approved by Korea Ministry of Food and Drug Safety (MFDS) through a phase III trial. For treatment, pharmacotherapy of AGA usually combines topical minoxidil 7% with one of oral <${\alpha}-2$ reductase inhibitor. Objectives: We evaluated the comparative efficacy and adverse effect between topical minoxidil 7%/finasteride 1 mg and topical minoxidil 7%/dutasteride 0.5 mg pharmacotherapy for outpatients with AGA. Also we evaluated the relationship between therapeutic effect and regular hospital visit. Method: This study was performed retrospectively based on electronic medical record (EMR) data of total 98 patients (topical minoxidil 7% with dutasteride 0.5 mg ($Avodart^{(R)}$) or finasteride 1 mg ($Alopecia^{(R)}$, $Propecia^{(R)}$) with diagnosis of AGA from department of dermatology at a secondary hospital from January $1^{st}$, to May $31^{st}$, 2014. Results: The efficacy and adverse event of topical minoxidil 7%/dutasteride 0.5 mg (DUTA group) were 100% and 45.7%, and of topical minoxidil 7%/finasteride 1 mg (FINA group) were 92.1% and 33.3%, respectively. The mean onset time of responses and adverse events in the FINA group were 3.86 months and 4.43 months. Those in the DUTA group were 3.97 months and 5.06 months. Conclusion: Both FINA and DUTA group were highly effective, but the DUTA group showed higher efficacy and adverse effects than those in the FINA group. Dutasteride may be another alternative in AGA treatment.

LC-MS/MS를 이용한 혈청 중 dutasteride 분석 (Analysis of dutasteride in human serum by LC-MS/MS)

  • 남혜선;남경희;정수희;이장우;강진영;홍순근;김태성;정기경;강태석;윤혜정;이광호;이규식
    • 분석과학
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    • 제25권1호
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    • pp.76-82
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    • 2012
  • 본 연구는 혈청 중 두타스테라이드의 확인과 정량을 위하여 LC-ESI-MS/MS를 이용한 신뢰성 있는 분석법을 개발하고, 분석방법의 타당도를 검증하고자 수행하였다. 내부표준물질인 베클로메타손을 첨가한 혈청을 methyl tert-butyl ether (MTBE)를 사용하여 액체상추출법(liquid-liquid extraction, LLE)으로 추출하였다. LC-MS/MS의 양이온 모드에서 MRM(multiple reaction monitoring)방법으로 확인한 두타스테라이드와 베클로메타손의 mass transition은 각각 m/z 529.6${\rightarrow}$461.5, m/z 409.3${\rightarrow}$391.2 이었으며, 머무름 시간은 각각 6.45분, 5.46분이었다. 검량선은 0.5~30.0 ng/mL의 농도 범위에서 $R^2$=0.9999의 높은 직선성을 나타내었으며, 정량한계와 회수율은 각각 0.5 ng/mL와 66~72% 이었다. 일내에 대한 정밀도는 3.5~5.5%, 정확도는 85.7~89.9% 범위이었으며, 연속 3일간 수행한 일간 정밀도는 4.2~5.8%, 정확도는 90.8~95.8% 이었다.

테스토스테론-유도 양성전립선비대증에서 나노화 벌 화분의 효능 연구 (Beneficial Effects of Nano-sized Bee Pollen on Testosterone-induced Benign Prostatic Hyperplasia in Rodents)

  • 박지아;편해인;소수정;이승현;이승민;서화진;강재선;최윤식;정일경
    • 생명과학회지
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    • 제28권4호
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    • pp.465-471
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    • 2018
  • 벌 화분은 오랫동안 전 세계적으로 이용되어 온 대체요법 중 하나이다. 벌 화분은 항진균 및 항균작용, 항암작용, 면역조절, 그리고 세포의 증식 등 다양한 생리활성을 갖고 있는 것으로 알려져 있다. 본 연구는 설치류를 이용하여 벌 화분의 양성전립선비대증의 개선 효과를 밝히기 위해 진행되었다. 벌 화분은 활성 성분의 추출률을 극대화하고, 생체 흡수율을 높이기 위하여 나노 크기로 분쇄하여 이용하였다. 먼저, 나노 크기의 벌 화분은 만성 testosterone 투여에 의한 전립선 크기 증가를 유의하게 완화하였다. 게다가 나노 크기의 벌 화분은 혈중 전립선 특이 항원의 농도를 뚜렷하게 감소시켰다. 흥미롭게도 나노 크기의 벌 화분은 testosterone에 의한 혈중 prostaglandin $E_2$ 증가에는 유의한 영향을 미치지 않았다. 이러한 나노 크기 벌 화분의 약리 효능은 dutasteride의 효과와 유사하였다. 마지막으로 나노 크기의 벌 화분은 androgen-반응성 인간 전립선 샘암종 세포인 LNCaP 세포의 손상을 유도하지 않았다. 이러한 결과를 종합하면, 나노화 된 벌 화분은 양성전립선비대증의 치료에 대체요법으로 이용될 수 있을 것으로 기대된다.

의약품이상사례보고시스템 데이터베이스를 이용한 피나스테리드의 약물유해반응 실마리 정보 탐색 (Signal Detection for Adverse Events of Finasteride Using Korea Adverse Event Reporting System (KAERS) Database)

  • 백지원;양보람;최수빈;신광희
    • 한국임상약학회지
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    • 제31권4호
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    • pp.324-331
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    • 2021
  • To investigate signals of adverse drug reactions of finasteride by using the Korea Adverse Events Reporting System (KAERS) database. This pharmacovigilance was based on the database of the drug-related adverse reactions reported spontaneously to the KAERS from 2013 to 2017. This study was conducted by disproportionality analysis. Data mining analysis was performed to detect signals of finasteride. The signal was defined by three criteria as proportional reporting ratio (PRR), reporting odds ratio (ROR), and information component (IC). The signals of finasteride were compared with those of the other drugs; dutasteride (similar mechanism of action), minoxidil (different mechanism but similar indications for alopecia), silodosin (different mechanism but similar indications for BPH). It was examined whether the detected signals exist in drug labels in Korea. The total number of adverse event-drug pairs was reported 2,665,429 from 2013 to 2017, of which 1,426 were associated with finasteride. The number of investigated signals of finasteride was 42. The signals that did not include in the drug label were 29 signals, including mouth dry, hypotension, dysuria etc. The signal of finasteride was similar to that of dutasteride and silodosin but was different to that of minoxidil. Early detection of signals through pharmacovigilance is important to patient safety. We investigated 29 signals of finasteride that do not exist in drug labels in Korea. Further pharmacoepidemiological studies should be needed to evaluate the signal causality with finasteride.

전립선암 선별을 위한 PSA 측정의 보험의학적 의미 (Review of measurement of prostate specific antigen: in the aspect of insurance medicine)

  • 박광일
    • 보험의학회지
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    • 제29권1호
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    • pp.16-21
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    • 2010
  • The measurement of prostate specific antigen (PSA) in screening for prostate cancer is recently performed as a routine check-up in clinical medicine and insurance medicine. Several factors may affect serum PSA levels. As prostate size increases with increasing age, the PSA concentration also rises. Increasing body mass index (BMI) is associated with a lower mean PSA concentration. Inhibitors of 5-alpha-reductase such as finasteride and dutasteride produce a 50 percent or greater decrease in serum PSA during the first three months of therapy, which persists as long as the drug is continued. Men who are regularly taking non-steroidal antiinflammatory drugs (NSAIDs) or acetaminophen have lower PSA levels. Emerging concepts regarding PSA testing that may help refine the interpretation of an elevated concentration include: PSA density, PSA velocity, and Free versus complexed or bound PSA. With many insurance companies, PSA level has become part of a standard battery of blood tests, along with HIV, cholesterol, liver enzymes, and other predictors of premature death. But, there is no clear proof of benefit, so we have to monitor the value of PSA test as a prostate cancer screening test in insurance medicine.

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Effects of Oxya chinensis sinuosa hot water extract on benign prostatic hyperplasia in LNCaP cells

  • Hyun Jung Lim;Sohyun Park;Ra-Yeong Choi;In-Woo Kim;Minchul Seo;Hae Yong Kweon;Joon Ha Lee
    • International Journal of Industrial Entomology and Biomaterials
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    • 제47권2호
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    • pp.140-146
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    • 2023
  • In recent years, the number of patients with benign prostatic hyperplasia (BPH), a condition that commonly occurs in elderly men, has increased due to aging and the adoption of western dietary habits. Treatment with chemical drugs, such as finasteride or dutasteride, can cause side effects such as erectile dysfunction or sexual problems. This necessitates the development of remedies using natural substances derived from food ingredients. In this study, we investigated the inhibitory effects of Oxya chinensis sinuosa hot water extract (OCH) on BPH production in LNCaP cells, a hormone-dependent prostate cancer cell line. We found that the mRNA expression of androgen receptor (AR), prostate specific antigen (PSA), and, 5α-reductases 1, and 2 decreased following treatment with OCH. Furthermore, OCH treatment resulted in reduced protein expression of BPH regulators, such as AR. Collectively, these results suggest that OCH exerts a beneficial effect on BPH by inhibiting the AR signaling pathway, indicating the potential of OCH as a therapeutic agent for the prevention and treatment of BPH.