• Biomolecules & Therapeutics
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• 제17권4호
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• pp.388-394
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• 2009

The cytokines which is produced by allergen-specific T helper (Th) cells play a pivotal role in the pathogenesis of asthma. Asthma is caused by exaggerated T-helper 2 (Th2)-based immune responses. It is suggested that controlling such Th2-based response is necessary for asthma therapy. The current therapies for asthma focus primarily on control of symptoms and suppression of inflammation, without affecting the underlying cause. So, we examined that anti-asthmatic drugs might have play a certain role in Th2/Th1 balance. Splenocytes isolated from ovalbumin (OVA)-sensitized mice cultured with anti-asthmatic drugs. It is well known that Th2 and Th1 immune responses can balance one another, as Th2 mediators suppress Th1 responses and Th1 mediators similarly inhibit Th2 responses. But salmeterol inhibits both of Th1 and Th2 mediators, which salmeterol is a suppressor of immune responses not only a suppressor of Th2-based immune responses. Aminophylline is a weak suppressor of immune responses. But ipratropium and cromoglycate don't have any suppressor effect to Th2-driven responses. They only have suppressor effect to Th1 immune responses. Salmeterol, ipratropium, aminophylline, and cromoglycate augmented mRNA levels of CRTH2, EP2, and IP2 receptors in OVA-sensitized splenocytes. It is well known that the up-regulation of CRTH2 - $PGD_2$ receptor - results in restraint of eosinophil recruitment and that the increment of IP and EP2 - $PGI_2$ and $PGE_2$ receptor, respectively - may induce the accumulation of cAMP that decrease the effector function of T cells. Moreover salmeterol and cromoglycate increase the mRNA expression of $PGD_2$ synthase. These findings indicate that anti-asthma agents may alleviate the immunological responses that cause the asthmatic diseases.

• Toxicological Research
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• 제4권1호
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• pp.1-12
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• 1988

In order to evaluate the effect of cigarette smoking on the pharmacokinetics of theophylline in Koreans, doses of 4.5 to 5.0 mg/kg of theophylline, as injectable aminophylline, were administered to 12 normal young volunteers (male, 22 to 35 yrs;mean, 26 yrs) through intravenous infusion over 30 minutes, and pharmacokinetics of theophylline were tested. Among subjects, six were nonsmokers and the other were smokers (range 1 to 2 packs/day). Also the correlations between plasma and saliva theophylline concentrations were investigated by determining the concentrations of theophylline in saliva simultaneously at each plasma sampling time. The total body clearances of theophylline in smokers (Mean${\pm}$SD, 0.0578${\pm}$0.0092 L/hr/kg)were appreciably higher than thoxe of nonsmokers (Mean${\pm}$SD, 0.0359${\pm}$0.0063 L/hr/kg), and the half-lives of theophylline in smokers averaged 5.36${\pm}$1.22hr, and significantly shorter than those of nonsmokers which averaged 9.14${\pm}$1.73hrs(p<0.005). But the apparent volumes of distribution of theophylline did not show any significant difference between smokers (Mean${\pm}$SD,0.44 ${\pm}$0.05L/kg) and nonsmokers (Mean${\pm}$SD, 0.46${\pm}$0.05L/kg). The average concentration ratios in saliva and plasma were 0.61 in smokers and 0.56 in nonsmokers after 2 hrs following drug administrations, and the smoker group had a slightly higher value of ratio(S/P) than the nonsmoker group (p<0.05). The correlations between saliva and plasma theophylline concentration in smokers were r=0.852(p<0.0005) within 2 hr and r=0.985(p<0.0005) after 2 hrs and also those of nonsmokers were r=0.729(p<0.0005) within 2 hrs and r=0.957(p<0.0005) after 2 hrs starting the infusion. From the results, it was found that smoking cigarettes had significantly increased the clearance of theophylline and that the relationships between saliva and plasma theophylline concentrations in all subjects were better after 2 hrs than within 2 hrs starting the infusion of aminophlline.

• 한국임상수의학회지
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• 제29권6호
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• pp.483-487
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• 2012

심장에 발생하는 원발성 그리고 전이성 종양은 개에서는 흔치 않다. 우리는 본 연구에서 심장초음파적 진단을 이용하여 요크셔테리어 2마리에서 발생한 심장내 종괴를 확인하였다. 첫째 증례에서의 종괴는 상행 대동맥과 폐동맥 사이에 위치하고 있었으며, 중증도의 대동맥 역류와 좌심실의 확장을 유발하고 있었다. 이 증례의 환자등급은 ISACHC II 등급의 심부전으로 분류되었다. 환자에 대한 심장처방으로는 furosemide, enalapril, pimobendan 그리고 경구적인 화학요법으로는 lomustine가 처방되었다. 둘째 증례에서의 종괴는 좌심방의 2/3를 차지하고 있었으며, 좌심방의 확연한 확장과 심각한 이첨판 역류 (~5 m/s) 를 유발하고 있었으나, 환자의 심부전 등급은 ISACHC Ib 등급으로 심각한 울혈성 심부전은 나타나지 않았다. 종괴의 성상은 cardiac myxoma로 추정되었으나, 조직생검검사는 보호자의 거절로 인하여 수행되지 않았다. 환자에 대한 심장처방으로는 ramipril, clopidogrel 그리고 기관지 확장제는 aminophylline이 처방되었다. 본 증례의 두 환자들은 여전히 생존해 있으며, 정기적인 검진을 받고 있다.

• 한국임상약학회지
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• 제17권1호
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• pp.13-18
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• 2007

Theophylline은 methylxanthine계열 기관지확장제중 가장 강력하며 기관지 천식이나 만성 폐쇄성 호흡기 질환환자에서 사용된다. Theophylline은 치료지수가 5-20 mg/L로 매우 좁은 치료지수를 갖는 약물이다. Cimetidine과 theophylline은 주로 간에 존재하는 cytochrome P450 (CYP) 효소에 의해 대사되며 theophylline은 유전적 다형성이 보고된 바있는 CYP1A2에 의해 대부분 대사된다. 본 연구는 theophylline의 약동학에 미치는 cimetidine의 영향을 평가하고 CYP1A2 유전적 다형성의 영향유무를 검증하였다. 8명의 건강한 비흡연자인 한국인 자원자를 모집하여 공개, 2기 교차시험을 실시하였다. 8명의 자원자에게 1기 시험의 첫날 100 mg의 aminophylline을 경구로 단회 투여하였으며 약물투여 후 36시간까지 채혈하여 혈장을 보관하였다. 공혈장 채취를 위해 채혈한 혈액중 일부를 가지고 유전자형 검색을 실시하였다. 1주일의 휴약기를 거친 후 2기 시험을 진행하였다. 2기 시험의 첫날 같은 용량의 aminophylline과 200 mg의 cimetidine을 같이 경구로 단회 투여하였다. 혈장 중 theophylline농도는 고성능 액체 크로마토그래피를 이용하여 측정하였으며 1기와 2기 시험에서 각종 약동학적 경수를 컴퓨터를 이용하여 계산하였다. 8명의 자원자에서 PCR-RFLP를 이용하여 유전자형 검색을 실시하였다. 8명(남자 4명, 여자 4명)의 자원자에서 약물과 관련한 약물이상 반응은 시험기간동안 발생하지 않았다. 약동학적 분석에서 theophylline의 혈장 농도 곡선하 면적(AUC)와 최고혈중농도($C_{max}$)가 cimetidine과 theophylline을 동시에 투여하였을 때 통계적으로 유의하게 증가하였으며 경구 청소율(CL/F)은 유의하게 감소하였다. 8명의 CYP1A2 유전자형 검색에서 돌연변이 유전자형은 발견하지 못하였으며 CYP1A2*1C 유전자형 검색에서 모두 (G/G) homozygote였으며 CYP1A2*1F 유전자형 검색에서는 5명이 (A/A) homozygote이고 3명이 (A/C) heterozygote였다. 따라서 theophylline대사에 CYP1A2유전자형에 따른 대사능의 차이는 관찰할 수 없었다. 이상의 결과를 요약하면 theophylline의 약동학은 cimetidine에 의해 유의한 차이를 보였으며 CYP1A2유전자형에 따른 영향은 관찰할 수 없었다. CYP1A2유전자형에 따른 생체내 대사능을 관찰하는 실험이 향후 이루어 져야 할 것으로 사료된다.

• 대한핵의학회지
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• 제32권3호
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• pp.250-258
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• 1998

목적 : ATP는 작용 시간이 빠르고 반감기가 짧은 효과적인 관상동맥 확장제로 알려져 있어 이를 심근관류 SPECT의 부하 약물로 사용 할 때에 부작용의 빈도와 안전성, 그 진단적 가치에 대해 알아 보고자하였다. 대상 및 방법: 관상동맥 질환이 의심되는 319명의 환자를 대상으로 ATP 부하(0.08 mg/kg/ min for 6min) T1-201 심근관류 SPECT를 실시하여 그 부작용을 조사하고 관상동맥 조영술과 비교하였다. 결과: 76.5%의 환자에서 부작용이 발생하였으나 일시적이고 경미하였으며, 모든 환자에서 ATP 주입을 끝낼 수 있었고 aminophylline이 필요했던 환자는 2명이었다. 관상동맥 조영술과 비교한 결과, 예민도 80%, 특이도 90% 였다. 결론: 6분간 0.08mg/kg/min의 ATP 주입 용량을 사용한 본 연구 결과에서 ATP 부하 심근관류 SPECT는 관상동맥 질환의 진단에서 adenosine이나 dipyridamole을 이용했을 때보다 부작용의 발생 빈도 및 부작용의 정도가 낮아 안전하게 사용될 수 있으며 진단 성능도 동등한 것으로 생각된다.

• 한국기계가공학회지
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• 제19권1호
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• pp.11-18
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• 2020

The emergence of the flow-through cell (FTC) method has made up for the limitations of previous dissolution test methods, but the high cost of the FTC dissolution devices have seriously hindered the progression of research and application of the FTC. This new design uses a peristaltic pump to simulate the sinusoidal flow rate of a piston pump. The flow profile of each peristaltic pump was sinusoidal with a pulsation of 120 ± 1 pulses per minute, and the flow rate ranged from 1.0 - 36.0 mL/min. The flow control of each channel was adjusted independently so the flow errors of the seven channels were close to 2%. The structure of the system was simplified, and the cost was reduced through manual sampling and immersing the FTC in a water bath. The dissolution rate of the theophylline and aminophylline films was determined, and good experimental results were obtained.

• 생약학회지
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• 제9권2호
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• pp.99-102
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• 1978

Several kinds of medicinal plants are used as diuretics in folk medicines and oriental drugs. The diuretic action of water extracts of the ten kinds of crude drugs, such as Pachyma hoelen $R_{UMPHIUS}$ Zea mays L., Akebia quinata $D_{ECAISNE}$, Alisma orientale Juzepezuk, Atractylodes koreana $N_{AKAI}$, phytolacca americana L., Achyranthes japo-nica $N_{AKAI}$, Juncus decipiens $N_{AKAI}$, Prunella asiatica $N_{AKAI}$ and Artemisia capillaris $T_{HUNBERG}$ was examined in mouse and compared with aminophylline as a control the following results were obtained. The urine volume was found to be remarkably increased by the Pachyma hoelen RUMPHIUS, Phytolacca americana L., Prunella asiatica $N_{AKAI}$ and Artemisia capillaris $T_{HUNBERG}$, moderately increased by the Akebia quinata $D_{ECAISNE}$, Achyranthes japonica $N_{AKAI}$ and Juncus decipiens $N_{AKAI}$, and slightly increased by Zea mays $L_{ENNE}$, Alisma orientale $J_{UZFPEZUK}$ and Atractylodes koreana $N_{AKAI}$.

• 대한두개안면성형외과학회지
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• 제12권1호
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• pp.22-27
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• 2011

Purpose: Packing the nose is a common procedure after the closed reduction of a nasal bone fracture to prevent postoperative complications, such as bleeding and adhesion formation as well as to stabilize the framework of the nasal bone. On the other hand, it is difficult for a patient to endure nasal packing because of breathing difficulties, headaches, chest discomfort, insomnia, general weakness and hypoxia. This study examined the availability of a bronchodilator to improve the decreased oxygen saturation and postoperative symptoms on nasal packing. Methods: From February, 2010 to July, 2010, a prospective randomized comparison of the incidence of a range of postoperative signs and symptoms was conducted on 60 patients, who did (n=30) and did not (n=30) undergo bronchodilator infusion (aminophylline 250 mg/10 mL + normal saline 100 mL IV qd) following nasal packing. The postoperative symptoms and oxygen saturation in the two groups were compared. Results: Patients who had infused the bronchodilator showed improved oxygen saturation. Nevertheless, there were no significant differences in the postoperative uncomfortable symptoms (dyspnea, headache, chest discomfort, insomnia, general weakness) between the two groups. Conclusion: A bronchodilator after nasal packing improves oxygen saturation by dilating the airway tract but it cannot reduce the uncomfortable symptoms caused by nasal obstruction. Overall, the bronchodilator is a useful medication for improving the level of oxygen saturation.

• 한국임상약학회지
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• 제9권1호
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• pp.55-61
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• 1999

The object of this work was to study the pharmacokinetic differences and the cause of these differences in cirrhotic rats induced by N,N-dimethylnitrosamine or carbon tetrachloride treatment when aminophylline (8 mg/kg as theophylline, i.v.) was injected. The concentrations of theophylline and its major metabolite (1,3-dimethyluric acid) in plasma were determined by HPLC. In addition, formation of 1,3-dimethyluric acid from theophylline in microsomes was determined. In cirrhotic rats, the systemic clearance of theophylline was reduced to $17\%$ of the control value while AUC (area under the plasma concentration-time curve) and $(t_{1/2})_{\beta}$ were increased to about 6 fold and 10 fold, respectively. The formation of 1,3-dimethyluric acid was decreased to $33-41\%$ of the control value in microsomes of cirrhotic rat liver. From these results, it can be concluded that in cirrhotic rats induced by N,N-dimethylnitrosamine or carbon tetrachloride the total body clearance of theophylline is markedly reduced due to a reduced hepatic metabolism.

• Tuberculosis and Respiratory Diseases
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• 제38권4호
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• pp.372-378
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• 1991

Some kinds of newer fluoroquinolone antibiotics are known to interact with theophylline, which is widely used as a potent bronchodilator in asthma or chronic obstructive lung disease. To evaluate the effect of enoxacin and ciprofloxacin on the metabolism of theophylline, aminophylline was administered intravenously in bolus (6 mg/kg) over 30 minutes to 6 healthy volunteers (age: $23.3{\pm}4.2$ year, body weight: $63.2{\pm}9.0\;kg$, height: $169.0{\pm}6.5\;cm$, female 3, male 3) before and after per oral 5-day medication of enoxacin and ciprofloxacin, respectively and we measured the level of theophylline in serum. The results were as follows: 1) Enoxacin and ciprofloxacin did not influence the volume of distribution significantly. 2) Enoxacin decreased the clearance of theophylline significantly (from $42.9{\pm}14.6\;ml/min$ to $30.1{\pm}6.3\;ml/min$: p<0.05), but ciprofloxacin did not cause significant decrease (to $32.8{\pm}6.2\;ml/min$: p>0.005). 3) Enoxacin increased the elimination half life of theophylline significantly (from $496{\pm}83\;min$ to $693{\pm}32\;min$: p<0.001), but ciprofloxacin did not cause significant increase (to $687{\pm}222\;min$: p>0.05). These results suggested that enoxacin influenced clearance and elimination half life significantly and thorough monitoring of the level of theophylline in patients with coadminstration of enoxacin and theophylline was necessary. In case of ciprofloxacin, the influence on the metabolism of theophylline was not statistically significant, but one exceptionally large decrease of the clearance and increase of the elimination halflife of theophylline suggested the necessity of monitoring of theophylline level during coadministration of ciprofloxacin and theophylline.