• Title/Summary/Keyword: 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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    • v.5 no.3
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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.

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

  • Cheon, Young Ju;Kim, Jung Tae;Lim, Sung Cil
    • Korean Journal of Clinical Pharmacy
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    • v.25 no.3
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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.

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

  • Nam, Hye-Seon;Nam, Kyong-Hee;Jung, Su-Hee;Lee, Jang-Woo;Kang, Jin-Yeong;Hong, Soon-Keun;Kim, Tae-Sung;Jung, Ki-Kyung;Kang, Tae-Seok;Yoon, Hae-Jung;Lee, Kwang-Ho;Rhee, Gyu-Seek
    • Analytical Science and Technology
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    • v.25 no.1
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    • pp.76-82
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    • 2012
  • The determination and confirmation of dutasteride in human serum was performed by a liquid chromatography-electrospray ionization tandem mass spectrometry (LC-ESI/MS/MS). Beclomethasone as an internal standard (I.S.) was added to the serum and the mixed sample was pretreated by liquid-liquid extraction (LLE) with methyl tert-butyl ether (MTBE). The mass transitions of dutasteride and I.S. monitored in multiple reaction monitoring (MRM) were m/z 529.6${\rightarrow}$461.5 and m/z 409.3${\rightarrow}$391.2, respectively, and the retention times were 6.45 and 5.46 min, respectively. The calibration curve was linear in the concentration range of 0.5~30.0 ng/mL ($R^2$= 0.9999) and the limit of quantitation (LOQ) was found to be 0.5 ng/mL. The recovery of dutasteride was shown to be 66~72%. The intra-day assay precision and accuracy were in the range 3.5~5.5% and 85.7~89.9%, respectively, and the interday assay precision and accuracy were in the range 4.2~5.8% and 90.8~95.8%, respectively.

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

  • Bak, Jia;Pyeon, Hae-In;So, Soojeong;Lee, Seunghyun;Lee, Seungmin;Suh, Hwa-Jin;Kang, Jae Seon;Choi, Yun-Sik;Chung, Il Kyung
    • Journal of Life Science
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    • v.28 no.4
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    • pp.465-471
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    • 2018
  • Bee pollen is one of many types of alternative remedies, and it has been used for a long time throughout the world. It has numerous health effects, including antifungal, antibacterial, and antioxidant properties, immune modulation, enhanced cell proliferation, and even anti-carcinogenic effects. This study was designed to elucidate the effects of bee pollen on benign prostatic hyperplasia in rodents. For this experiment, we used nano-sized bee pollen produced through wet-grinding technology, thereby the extraction efficiency of the active ingredients in the bee pollen was significantly enhanced. First, We found that nano-sized bee pollen significantly reduced the size of prostates enlarged by chronic testosterone administration. In addition, nano-sized bee pollen significantly reduced the plasma concentration of the prostate-specific antigen (PSA). Interestingly, nano-sized bee pollen did not reduce the testosterone-induced increase in the plasma concentration of prostaglandin $E_2$ ($PGE_2$). The beneficial effects of nano-sized bee pollen in reducing both the size of the prostate and the plasma concentration of PSA was comparable to that of dutasteride. Finally, nano-sized bee pollen did not cause damage in LNCaP cells which are androgen-sensitive human prostate adenocarcinoma cells. Together, these data indicate that nano-sized bee pollen may be able to be used as a good alternative remedy for the treatment of benign prostatic hyperplasia.

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

  • Baek, Ji-Won;Yang, Bo Ram;Choi, Subin;Shin, Kwang-Hee
    • Korean Journal of Clinical Pharmacy
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    • v.31 no.4
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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.

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

  • Park, Kwang-Il
    • The Journal of the Korean life insurance medical association
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    • v.29 no.1
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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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    • v.47 no.2
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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.