• Title/Summary/Keyword: 약물상호작용

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Synthetic studies of 2,2'-(ethylenediimino) and 2,2'-(thioureido)-di-1-carboxylic acids as the antitubercular and the other bacteriostatic agents (2,2'-(ethylenediimino) and 2,2'-(thioureido)-di-1-carboxylic acids의 항결핵성및 항균성화합물로서의 합성연구)

  • Chough, Yun-Sung
    • YAKHAK HOEJI
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    • v.10 no.2_3
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    • pp.8-11
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    • 1966
  • 항인결핵균성및 streptomycin, isoniazid및 para-aminosalicylic acid에 대한 내성인결핵균주에 현저한 항균작용 있는 dextro-2,2'-(ethylenediimino)-di-1- butanol(Ethambutol) 계열 및 thioureido(-NHCSNH-) 함유화 합물 계열인 2,2'-(ethylenediimino)-di-1-butyric acid및 2,2'-(thioureido)-di-1-butyric acid를 합성했으며 이들 약물의 구조와 작용간의 상호관계를 설명코저 이들 화합물과 류사한 구조인 2,2'-(thioureido)-di-acetic acid를 합성했기에 보고함.

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Effects of Ticlopidine on the Bioavailability and Pharmacokinetics of Nicardipine after Oral and Intravenous Administration (티크로피딘이 니칼디핀의 생체이용률 및 약물동태에 미치는 영향)

  • Moon, Hong-Seop;Choi, Jun-Shik;Bang, Joon-Seok
    • Korean Journal of Clinical Pharmacy
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    • v.22 no.1
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    • pp.1-8
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    • 2012
  • 항혈소판제인 티크로피딘과 항고혈압제인 니칼디핀과의 약동학적 상호작용 연구를 위하여 티크로피딘 (3 또는 10 mg/kg)과 니칼디핀의 경구 (4 mg/kg) 및 정맥 (12 mg/kg) 투여하여 본 연구를 시행하였다. 연구방법: 티크로피딘이 cytochrome P450 (CYP) 3A4 활성과 P-glycoprotein (P-gp)의 활성에 미치는 영향도 평가하였다. 결 과: 티크로피딘과 니칼디핀의 병용투여 시 티크로피딘이 니칼디핀의 약물동태 파라미터에 미치는 결과는 다음과 같다. 티크로피딘은 CYP3A4 효소의 활성을 저해 하였으나 P-gp활성에는 영향을 미치지 못하였다. 니칼디핀의 혈중농도곡선하면적 (AUC)는 대조군에 비해 티크로피딘 10 mg/kg 병용투여군에서 유의성 (p < 0.05)있게 증가되었다. 상대적 생체이용률 (RB)은 티크로피딘 병용투여군에서 115-143%로 증가하였다. 결 론: 본 논문에서 흰쥐에 티크로피딘과 니칼디핀을 병용경구투여 시 니칼디핀의 생체이용률 (bioavailability)이 유의성 (p < 0.05)있게 증가된 것은 티크로피딘이 대사효소인 CYP3A4를 억제하여 소장과 간장에서 초회통과효과 (first-pass metabolism)를 감소 시켰기 때문인 것으로 사료된다. 본 실험결과를 토대로 인체에서 티크로피딘과 니칼디핀의 상호작용을 검토한 후 투여용량을 조절하는 것이 바람직하다고 사료된다.

다환상 방향족 화합물이 자궁성장에 미치는 영향

  • 신윤용;류재천;문창규
    • Proceedings of the Korean Society of Applied Pharmacology
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    • 1992.05a
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    • pp.55-55
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    • 1992
  • 다환상 방향족탄화수소류인 3-methylcholanthrene 이 자궁에 미치는 영향을 연구하고자 자궁의 성장에 미치는 영향과 에스트로겐 수용채와의 상호작용을 조사하였다. 3-Methylcholanthrene 단독 투여군은 대조군에 비해 투여 용량에 관계없이 유의성있는 자궁 무게의 변화를 나타내지 않았으나 diethylstilbesterol과 3-methylcholanthrene 병용 투여군에서는 diethylstilbesterol 단독 투여군에 비해 자궁 무게가 병용 투여한 3-methylcholanthrene 용량에 의존적으로 감소하였다. 안티에스트로갠인 tamoxifen이 자궁 성장에 미치는 영향을 관찰하기 위하여 tamoxifen단독 투여시에는 자궁 무게가 대조군에 비해 약간 증가하여 (p<0.05)부분 효능 작용을 나타냈으나 diethylstilbesterol과 동시 투여시에는 diethylstilbesterol에 의한 자궁 무게 증가가 감소되었으며 그 감소 정도는 병용한 tamoxifen 용량에 의존적이었다. Diethylstilbesterol과 3-methylcholanthrene 및 tamoxifen을 병용 투여했을때 diethylstilbesterol에 3-methylcholanthrene만을 병용 부여하였을 때보다 diethylstilbesterol에 의한 자궁 성장이 유의적으로 (P<0.01)감소되었다. Diethylstilbesterol과 3-methylcholanthrene의 병용 투여군에서는 투여한 후 시간이 경과함에 따라 diethylstilbesterol 단독 투여군에 비해 일정한 비율(23.6=3.9%)로 자궁 무게 증가가 억제되었다.

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Drug Interaction Studies-Effects of Prazosin on Furosemide Kinetics and Diuretic Action- (약물상호작용(藥物相互作用)에 관(關)한 연구(硏究) -Furosemide의 동력학(動力學) 및 이뇨작용(利尿作用)에 미치는 Prazosin의 영향(影響)-)

  • Kang, Young-Sook;Yong, Jae-Ick
    • Journal of Pharmaceutical Investigation
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    • v.13 no.4
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    • pp.173-182
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    • 1983
  • The influence of prazosin (0.1 mg/kg i.v.) on the excretion and diuretic action of furosemide (2mg/kg i.v.) in rabbits was studied to investigate an interaction between ${\alpha}-adrenergic$ blocking agent, prazosin and furosemide. The results were as follows; 1) With the combined administration of prazosin and furosemide, the plasma concentration of furosemide was increased, the urinary excretion rate and renal clearance of furosemide were reduced, and tile biological half-life of furosemide was increased. 2) The diuretic action of furosemide was significantly reduced with the combined administration of prazosin: maximal decrease in urine volume, urinary electrolytes, clearance of $Na^+$ and $Cl^-$, and GFR and RPF, as well as maximal increase in $Na^+$ reabsorption rate were noted 10 minutes after administration of furosemide (2mg/kg i.v.)

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Suspected Upper Gastrointestinal Bleeding by Interaction of Clozapine and Buspirone (상부위장관 출혈이 의심되는 클로자핀과 부스피론의 상호작용)

  • Sung, Yu-Mi;Kim, Soo-In;Yun, Kyu-Wol;Lim, Weon-Jeong
    • Korean Journal of Psychosomatic Medicine
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    • v.14 no.1
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    • pp.62-66
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    • 2006
  • Introduction: Unexpected serious and lethal drug interactions can be occurred by polypharmacy for treatment-resistant psychiatric disorders. We report a case who has suspected upper gastrointestinal bleeding after the combination of clozapine and buspirone. Case : A 69-year-old woman with DSM-IV schizophrenia who was admitted to our hospital had no previous medical problems. Findings on physical exam, laboratory values, EEG, and a magnetic reso-nance imaging scans were no abnormality, except for slightly low level of hemoglobin at admission. Because of aggravating anxiety symptom, a trial of buspirone was begun from 15mg, in addition to olanzapine 30mg. And then olanzapine was switched to clozapine due to her treatment-refractory his-tory and poor response on this admission. Moreover, At the admission 11 weeks later, after 4 weeks of starting buspirone and clozapine, she was placed on a regimen of clozapine 300mg and buspirone 60mg. At this point, she started to complaint nonspecific abdominal pain for 4 days and then hematemesis, melena and hypotension were developed suddenly with negative findings in gastroduodenoscopy. After stopping all medication, the suspected upper gastrointestinal bleeding was subsided. After the regimen was switched back to clozapine only, psychotic symptoms were improved without the recurrence of the adverse events. Conclusion : We concluded that the upper gastrointestinal bleeding in this case was attributed to the drug interaction with clozapine and buspirone, although the definite mechanism is not clear. The clini-cians should be very cautious to prescribe the combination of clozapine and buspirone due to a possible lethal adverse effect.

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Evaluation of Cytotoxic Properties of Tea Polyphenols in Intestinal Cells Treated with Over-the-counter Drugs (녹차 폴리페놀 성분과 일반 의약품의 상호작용에 의한 장관계 세포 독성 평가)

  • Choi, Hyun-A;Kim, Mi-Ri;Hong, Jung-Il
    • Korean Journal of Food Science and Technology
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    • v.43 no.5
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    • pp.641-647
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    • 2011
  • Polyphenols in green tea are biologically active and may interact with commonly-consumed over-the-counter (OTC) drugs in the body. In this study, modulation of cytotoxicity of polyphenon 60 (PPE, tea polyphenol mixture) with co-treatment of several OTC drugs, including ibuprofen (Ibu), acetaminophen (AAP), and aspirin was investigated in intestinal cells. PPE showed more potent cytotoxic effects on colon cancer HCT 116 cells than on normal intestinal INT 407 cells. Ibu had the strongest cytotoxic effects on both cell types. Cytotoxicity of PPE on HCT 116 and INT 407 cells was not markedly altered by co-treated OTC drugs. Cytotoxicity of the OTC drugs was not affected by PPE. When HCT 116 cells were incubated with AAP before or after PPE treatment, cytotoxicity was slightly enhanced more than their additive effect. The present study may provide basic information of possible toxicity due to interaction of the polyphenols and the OTC drugs.

Modulatory Effects of Korean Red Ginseng Extract (Panax ginseng C.A. Meyer) on Cytochrome P450 after Oral Administration to Mice for 14 Days (마우스에 홍삼추출물의 14일간 경구 투여에 따른 약물대사효소 조절능 평가)

  • Kim, Hee-Yeon;Nam, Woong-Shik;Kim, Seong-Hee;Jang, Hye-Ryang;Lee, Mi-Kyoung;Kim, Tae-Wan;Lee, Sang-Kyu
    • Journal of Life Science
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    • v.22 no.8
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    • pp.991-998
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    • 2012
  • Ginseng is one of the most commonly used herbal medicines and health foods. Korean red ginseng (KRG; Panax ginseng C.A. Meyer) extract is known to have potential therapeutic activities, such as anti-viral effects, the amelioration of food allergies, anti-oxidant effects, and obesity reduction. Nevertheless, no reports have been issued the modulatory effects of KRG extract on the activity of cytochrome P450 (CYP). In the present study, we investigated the modulatory effect of KRG extract in vitro and in vivo by using pooled human liver microsomes and male ICR mice. When human liver microsomes were incubated with KRG extract at 0.01-10 mg/ml, CYP1A2, 2B6, 2C19, 2D6, and 3A were not significantly inhibited by KRG extract, although CYP2B6 was slightly inhibited. Mice were orally administered KRG extract at 50, 250, or 500 mg/kg daily for 3, 7, or 14 days. However, the activities of CYPs in mouse livers were not significantly different from those of vehicle-treated controls. In conclusion, no significant ginseng-drug interaction was observed. KRG extract did not significantly modulate the activities of CYPs in vitro or in vivo.

Screening for inhibitory effect on nine CYP isoforms by 20 herbal medications (고속 스크리닝 기법을 이용한 한약제제의 cytochrome P45O 저해능 탐색)

  • Kim, Hyun-Mi;Liu, Kwang-Hyeon
    • Journal of Life Science
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    • v.17 no.3 s.83
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    • pp.334-339
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    • 2007
  • We evaluated the potential of 20 herbal medications (HMs), commonly used in Korea, to inhibit the catalytic activities of several cytochrome P450 (CYP) isoforms. The abilities of 500 ${\mu}g/ml$ of aqueous extracts of 20 HMs to inhibit phenacetin O-deethylation (CYP1A2), coumarin 6-hydroxylation (CYP2A6), bupropion hydroxylation (CYP2B6), rosiglitazone hydroxylation (CYP2C8), tolbutamide 4-methylhydroxylation (CYP2C9), S-mephenytoin 4'-hydroxylation (CYP2C19), dextromethorphan O-demethylation (CYP2D6), chlorzoxazone 6-hydroxylation (CYP2E1), and midazolam 1'-hydroxylation (CYP3A) were tested using human liver microsomes. The HMs Woohwangcheongsimwon suspension and Hwanglyeonhaedok-Tang strongly inhibited CYP2B6 and CYP2D6 isoform activity, respectively. These results suggest that some of the HMs used in Korea have potential to inhibit CYP isoforms in vitro. Although the plasma concentrations of the active constituents of the HMs were not determined, some herbs could cause clinically significant interactions because the usual doses of those individual herbs are several grams of freeze-dried extracts.

Pharmacokinetics Interaction between Cardiotonic Pills and Cilostazol in Rats (렛트를 이용한 심적환과 cilostazol에 관한 상호작용 연구)

  • Kim, Ekyune
    • Journal of Life Science
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    • v.26 no.1
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    • pp.123-128
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    • 2016
  • The object of this study was to obtain accurate information about the co-administration effects of cardiotonic pills on the pharmacokinetics of cilostazol were observed as a process of the comprehensive and integrative medicine. Cilostazol is a synthetic anti-platelet and vasodilator agent developed for the treatment of intermittent claudication resulting from peripheral arterial disease. By increasing intracellular cyclic adenosine monophosphate (cAMP), cilostazol induces the activation of protein kinase A, which activates endothelial nitric oxide synthase. In order to evaluate the effect of a single or repeated cardiotonic pill dose on the pharmacokinetics of cilostazol, a single dose of pure_distilled water or a colloidal suspension of distilled water and cardiotonic pills were administered to the control and test groups, respectively. After 30 min, both groups were administered cilostazol. Plasma was collected 30min before administration, and 0.25, 0.5, 0.45, 1, 2, 4, 6, 8, and 24h after the end of cilostazol treatment. We then evaluated the pharmacokinetic changes observed with cilostazol between the control and test groups. No statistically significant differences were observed. These findings demonstrated that a single dose of cardiotonic pills did not affect the pharmacokinetics of cilostazol. The results obtained in this study suggest that co-administration of cardiotonic pills and cilostazol may not affect the bioavailability of cilostazol as a potential drug interaction.