• 제목/요약/키워드: Administration route

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Stability of 5-FU and Tegafur in Biological Fluids of Rats (흰쥐 생체시료 중 5-플루오로우라실 및 테가푸르의 안정성)

  • Jang, Ji-Hyun;Park, Jong-Kook;Kang, Jin-Hyoung;Chung, Suk-Jae;Shim, Chang-Koo;Kuh, Hyo-Jeong
    • Journal of Pharmaceutical Investigation
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    • v.34 no.3
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    • pp.161-168
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    • 2004
  • 5-Fluorouracil (5-FU) is an antimetabolite anticancer agent active against many types of solid tumors. Tegafur (TF), a prodrug of 5-FU, is frequently used in combination with uracil as dihydropyrimidine dehydrogenase (DPD) inhibitory fluoropyrimidine. We studied the stability of 5-FU and TF in biological fluids of rats and determined their bioavailability (BA) and excretion into bile, and urine. The drug concentrations were analyzed by an HPLC method. At room temperature, there was a 14-30% decrease in the concentration of 5-FU and TF in bile, urine, and plasma specimen at 10 and $100\;{\mu}g/ml$ over 240 min. No significant difference was noted among the sample types or between two different concentrations of 10 and $100{\mu}g/ml$. The decrease in drug concentration was significantly less in samples kept on ice (6-12%) for both drugs. These data indicate that biological fluid samples containing 5-FU or TF in plasma, urine, or bile should be placed on ice during the sample collection. Following these storage guidelines, samples were collected after administration 50 mg/kg of each drug via i.v. or oral route. BA was 1.5 folds greater for TF (60%) than that of 5-FU (42%). Approximately 0.52 and 3.3% of the i.v. doses of 5-FU and TF was excreted into bile, respectively. Renal clearance of 5-FU was about 16% of its total body clearance. These results suggest that instability of 5-FU and TF in biological fluids should be considered in pharmacokinetic or pharmacogenomic studies.

Evaluation of Pharmacist Intervention Program for Dosage Adjustment and IV-to-PO Conversion for $H_2$-Receptor Antagonist (신기능을 고려한 $H_2$-receptor antagonist의 용량, 용법 및 투여경로의 적절성 및 약사자문의 수용성)

  • Hwang, Bo Young;Oh, Jung Mi
    • Quality Improvement in Health Care
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    • v.9 no.2
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    • pp.230-240
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    • 2002
  • Background : The purpose of this study was to develop, implement and evaluate the pharmacist intervention program designed to identify and correctly adjust the dosage of $H_2$-receptor antagonists ($H_2RA$) in renally impaired patients and promote timely conversion of $H_2RA$ from IV to PO therapy. Methods : The study population consisted of renally impaired patients who received $H_2RA$ therapy from April 9 to May 8, 2001 at Hallym Medical Center. Each morning a specifically developed software program identified patients with serum creatinine (Scr) greater than 1.2 mg/dl or age greater than 65 years. The pharmacist, then screened the pharmacy profiles of the identified patients to determine if the patient was on $H_2RA$. For these patients on $H_2RA$ with renal impairement the creatinine clearance (CrCl) was calculated using Cockroft & Gault equation. The pharmacist determined the proper dosage for each identified patients based on the calculated CrCl and the oral dosage that would be appropriate for whom IV therapy was no longer indicated. Result : A total of 149 cases (101 patients) were monitored during the study period. The dosage was inappropriately prescribed for renal function in 61 of 149 cases (41%), and of those, pharmacist made recommendations for 58 cases of which 33 cases (57%) were accepted by the physicians. The administration route of H2RA was inappropriately used as IV in 22 of 53 cases (42%), and pharmacist made recommendations for those 22 cases of which 15 cases (68%) were accepted. Conclusion : Monitoring of patients with renal dysfunction by a pharmacist improved the dosing of $H_2RA$ and a dosing program of patients with renal impairment would be of benefit to other clinicians and institutions seeking to optimize patient care.

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Effects of General Anesthetic Agents on the Renal Function of Rabbits (신장기능(腎臟機能)에 미치는 몇가지 전신마취제(全身麻醉劑)의 영향(影響))

  • Kim, Suhn-H.;Cho, Kyung-W.;Song, He-S.
    • The Korean Journal of Physiology
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    • v.17 no.1
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    • pp.29-35
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    • 1983
  • The most popular way to get the animal to be co-operative for the animal experimentation is by using some kinds of general anesthetic agents. One of the most important point to take care of is, however, whether the agent(s) to be used is hinder the experimentation itself. There have been many contradictory reports of the general anesthetic agents on the renal function. Moreover, little information on the changes of the renal function by anesthesia has been available. We have done experiments to clarify and compare the effects of anesthesia induced by several general anesthetic agents on renal function in unanesthetized rabbits. Nembutal anesthesia(30 mg/kg, iv.) caused a decrease in free-water clearance, and increase in sodium and chloride excretion without significance. Thiopental anesthesia$(20{\sim}30\;mg/kg,\;iv.)$ suppressed all renal parameters tested. Chloralose(50 mg/kg, iv.) and chloral hydrate(75 mg/kg, iv.) did not change renal functions except for glomerular filtration rate, which parameter was suppressed only for a short period just after agent administration. Urethane(1 g/kg), administered by the route of either subcutaneously or intraperitoneally, suppressed renal functions lasted for the duration of experimental anesthesia. The above data suggest that it is very important to chose an appropriate anesthetic agents for a given experiment, especially experiment involved with renal function, and to interprete the data obtained from the anesthetized animal model for the expected results.

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Absorption, Distribution, Metabolism, and Excretion of CKD-732, a Novel Antiangiogenic Fumagillin Derivative, in Rats, Mice, and Dogs

  • Lee, Ho-Sup;Park, Won-Kyu;Son, Hoe-Joo;Lee, Sung-Sook;Kim, Joon-Kyum;Ahn, Soon-Kil;Hong, Chung-Il;Min, Hye-Ki;Kim, Myung-Soo;Myung, Seung-Woon
    • Archives of Pharmacal Research
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    • v.27 no.2
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    • pp.265-272
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    • 2004
  • The pharmacokinetics of CKD-732 (6-0-4-[dimethyl-aminoethoxy)cinnamoyl]-fumagillolㆍhemioxalate) was investigated in male SD rats and beagle dogs after bolus intravenous administration. The parent compound and metabolites obtained from in vitro and in vivo samples were determined by LC/MS. The main metabolite was isolated and identified as an N-oxide form of CKD-732 by NMR and LC/MS/MS. CKD-732 was metabolized into either M11 or others by rapid hydroxylation, demethylation, and hydrolysis. The blood level following the intravenous route declined in first-order kinetics with $T_{1}$2/$\beta$ values of 0.72-0.78 h for CKD-732 and 0.92-1.09 h for M11 in rats at a dose of 7.5-30 mg/kg. In dogs, $T_{1}$2/$\beta$ values of CKD-732 and M11 were 1.54 and 1.79 h, respectively. Moreover, AUC values increased dose dependently for CKD-732 and M11 in rats and dogs. The CLtot and Vdss did not change significantly with increasing dose, indicating linear pharmacokinetic patterns. The excretion patterns through the urine, bile, and feces were also examined in the animals. The total amount excreted in urine, bile, and feces was 2.13% for CKD-732 and 1.29% for M11 in rats, and 1.58% for CKD-732 and 2.28% for M11 in dogs.

Initial experience with intra-articular 188Re-tin colloid as a "radiation synovectomy" agent in various joints

  • Shinto, Ajit S;Indira, VU;Kamaleshwaran, KK;Banka, Vinay Kumar;Aswathy, KK;Thirumalaisamy, SG;Rajamani, V;Mallia, Madhav;Banerjee, Sharmila
    • Journal of Radiopharmaceuticals and Molecular Probes
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    • v.1 no.2
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    • pp.109-117
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    • 2015
  • Radiation synovectomy has been proposed as a promising palliative therapy for recurrent joint effusions for the last two or three decades. Ionizing radiations emitted by intrarticularly administered radiolabelled colloids. The aim of this study was to assess the effectiveness of radiation synovectomy (RSV) using $^{188}Re$-tin colloid in the treatment of recurrent joint effusions and chronic synovitis of knee joints. Three phase bone scan was acquired for the concerned joint prior to radiosynovectomy. $^{188}Re$-tin colloid was prepared as per the reported protocol. 9 patients, diagnosed with rheumatoid arthritis and suffering from chronic resistant synovitis of the knee, ankle or elbow joints were administered the radiopharmaceuticals, checked for radiochemical purity >95% by intraarticular route. A whole body scan was acquired 2 h post-radiosynovectomy. In all the 9 treatments, no leakage to non-target organs was visible in the whole body scan. Static scans of the joint revealed complete retention of $^{188}Re$-tin colloid in the joints post administration of the agent. Clinically all patients exhibited a complete or partial response. RSV with $^{188}Re$-tin colloid was safe and effective in patients with chronic synovitis of rheumatoid origin.

Evaluation of Trail Facility and Operation-Management for Walking Tour Revitalization - focus on Ganghwa Nadeul-gil - (도보여행 활성화를 위한 탐방로 시설 및 운영 관리 실태 평가 - 강화 나들길을 중심으로 -)

  • Shin, Sunmi;Byun, Byungseol
    • Journal of Wetlands Research
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    • v.17 no.2
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    • pp.176-183
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    • 2015
  • This study is aimed at deducting the evaluation standard of the walking tour trail and evaluating the real condition of trail facilities and operation & management. On the basis of the research on the walking tour, this study deducted the evaluation index of the trail facilities and administrative control, and divided it into visit resources, visit facilities and trail operation-management. This study selected the course of high use satisfaction among the Ganghwa Nadeul-gil section, and evaluated the real condition of Ganghwa Nadeul-gil trail by classifying the route as nature-oriented trail and culture-oriented trail. In case of nature-oriented trail, it's necessary to discover living culture resources of the village linked with the trail, and to develop amenities using bus stations and supermarket. In case of culture-oriented trail, it's required that economic regeneration plan should be arranged using the declining facilities.

In vitro inhibitory effects of Yangguksanhwa-tang and Taeumjowi-tang on CYP450 isozymes (양격산화탕과 태음조위탕 추출물의 in vitro CYP450 효소 활성 억제 효과)

  • Ha, Hye-Kyung;Jin, Seong-Eun;Shin, Hyeun-Kyoo
    • Journal of Society of Preventive Korean Medicine
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    • v.16 no.3
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    • pp.129-137
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    • 2012
  • Objective : Herb-drug interactions have become an important issue because of the consumption of herbal remedies has increased in the world. Yangguksanhaw-tang (Liang ge san huo-tang) and Taeumjowi-tang (Tai yin tiao wei-tang) are typical herbal formulas on Sasang constitution medicine (four-constitution medicine). This study was aimed at evaluating the effects of Yangguksanhaw-tang and Taeumjowi-tang on drug metabolizing enzymes, cytochrome P450 (CYP450) isozymes. Methods : Vivid$^{(R)}$ CYP450 Screening Kits were used to measure of CYP3A4, CYP2C19, CYP2D6 and CYP2E1 activities. This method is based on the use of fluorescent CYP450 substrates that are efficiently metabolized by specific CYP450 isozymes to yield a product with altered fluorescent properties. The percent inhibitions of CYP450s by herbal formulas were calculated. Results : Yangguksanhaw-tang inhibited CYP2C19 and CYP2E1 activities higher than that other CYP450 isozymes. The $IC_{50}$ values of CYP2C19 and CYP2E1 were 159.83 ${\mu}g/mL$ and 261.40 ${\mu}g/mL$, respectively. The CYP2E1 activity was inhibited ($IC_{50}=215.17{\mu}g/mL$) higher than that other CYP450 isozymes by Taeumjowi-tang. Conclusions : These results suggest that Yangguksanhaw-tang may inhibit the metabolism of co-administered drugs whose primary route of metabolism is via CYP2C19 or CYP2E1. Taeumjowi-tang could inhibit the metabolism of co-administered drugs, which are substrates for CYP2E1. Therefore, co-administration of the herbal formulas and other conventional drugs should be undertaken with care.

Immunological Activity and Immunotoxicity of Pine Tree Pollen in Mice (마우스를 이용한 송화분 섭취의 면역원성 및 안전성 탐색)

  • Kim, Young-Ok;Kim, Kwang-Ho;Park, Hyun-Ji;Park, Yeong-Chul;Park, Sung-Wook;Heo, Yong
    • Toxicological Research
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    • v.21 no.3
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    • pp.235-240
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    • 2005
  • Pollen has been used for prevention or treatment of certain diseases such as diabetes arthritis or cancer in traditional medicine. Among various pollens, pine tree pollen is known to relieve hypertension, suppress fatty liver progression, and facilitate the digestion, but its immunological activities are less known. To evaluate immunological reactivities and immunotoxicities of pine tree pollen, BALB/c mice were administered to the poller through oral route. Pine tree pollen suspended in distilled water or extracted with methanol has been administered at the concentration of 0, 10, or 100 mg/kg five days per week for four weeks. Polyclonal activation of splenic T cells with phytohemagglutinins did not induce a significant difference in IL-4 and $IFN_{\gamma}$ production between the pollen-administered mice groups and the control mice. Furthermore, polyclonal activation of splenic B cells with lipopolysaccharides did not result a significant difference in IgG1 and IgG2a production among the groups. These findings imply that the intake of pine tree pollen does not bring any humoral and cellular immune-dysrequlation. Whereas, viability of Listeria monocytogenes was suppressed in the mice administered with 100 mg/kg bw methanol extract, indicating the potential ability of pine tree pollen to enhance cell-mediated immunity mediated by type-1 helper T cells. In addition, aberrant upregulation of plasma IgG1 level was observed in the pollen-administered mice, which suggests a possibility of allergic response induction through the pine tree pollen uptake. Overall, pine tree pollen-mediated modulation of humoral or cellular immunity is worthy of further systematic investigation.

Geographic and Energy Aware Geocasting in Ad-Hoc Networks (Ad-Hoc 네트워크에서 위치와 에너지를 고려한 지오캐스팅 알고리즘)

  • Lee Ju-Young
    • Journal of Internet Computing and Services
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    • v.5 no.2
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    • pp.75-84
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    • 2004
  • Geocasting, a variant of the conventional multicasting problem, is one of communication type in which the data packets are delivered to a group of all nodes within a specified geographical region (i.e., the geocasting region) and is called location-based multicasting(LBM)(l). An Ad-hoc network is a dynamically reconfigurable and temporary wireless network where all mobile devices using batteries as energy resources cooperatively maintain network connectivity without central administration or the assistance of base stations. Consequently, the technique to efficiently consume the limited amounts of energy resources is an important problem so that the system lifetime is maximized. In this paper, we propose a LBPA(Location-Based Power Aware) geocasting algorithm that selects energy-aware neighbor to route a packet towards the target region In Ad-hoc network environments. The method Is such that the energy consumption is balanced among the nodes in proportion to their energy reserves. Through the simulations, the proposed LBPA algorithm shows better results, that is, as good as 40% on the average over the conventional LBM algorithm in terms of the network lifetime.

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An Enhanced Routing Protocol for Supporting Node Mobility in Multi-hop Ad-hoc Networks (다중 홉 Ad-hoc 네트워크에서 노드이동성을 고려한 라우팅 프로토콜에 관한 연구)

  • Kim, Kwan-Woong;Kim, Byun-Gon;Kim, Yong-Kab
    • Journal of the Korea Institute of Information and Communication Engineering
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    • v.11 no.9
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    • pp.1665-1671
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    • 2007
  • Mobile Ad hoc Networks (MANETs) refer to autonomous networks in which wireless data communications are established between multiple nodes in a given coverage area without a base station or centralized administration. Because of node mobility and limited battery life, the network topology may changes frequently. Selecting the most reliable path during route discovery process is important to improve performance in ad-hoc networks. In this study, we proposed an enhanced routing protocol based on AODV by monitoring variation of receiving signal strength. New metric function that consists of node mobility and hops of path is used for routing decision. From extensive experiments by using NS-2, The performance of the proposed routing scheme has been imp개ved by comparison to AODV protocol.