• Title/Summary/Keyword: Theophylline

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Effects of Erythromycin and New Macrolides on the Serum Theophylline Level and Clearance (혈중 Theophylline 농도 및 청소율에 대한 Erythromycin과 New Macrolides 항생제의 영향)

  • Lee, Heung-Bum;Lee, Yong-Chul;Rhee, Yang-Keun
    • Tuberculosis and Respiratory Diseases
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    • v.45 no.3
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    • pp.546-552
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    • 1998
  • Background: Up to 90% of a theophylline dose is biotransformed, by interaction with one or more the variants of the cytochrome P-450 drug metabolism system. Macrolides affect the elimination of theophylline by influencing on the microsomal enzyme systems. We evaluate the effect of erythromycin and new macrolides on the serum theophylline level and clearance. Method : Subjects consisted of moderate asthmatic patients with normal renal and hepatic functions. All subjects were non-smokers and treated with oral theophylline 400 mg per day. We randomly assigned 53 patients into four groups. Each group was treated with one macrolides, the first group erythromycin(n:19, 500 mg bid), second roxithromycin (n:14. 150 mg bid), third clarithromycin (n:10, 250 mg bid) and fourth azithromycin(n:10, 250 mg bid). We measured the serum theophylline level and clearance at three intervals, at pretreatment, after the first and fourth week after receiving the following macrolides, erythromycin, roxithromycin and clarithromycin. When azithromycin was administered, the serum theophylline level was measured at pretreatment and after one week of treatment They were measured by a computerized program of Bayesian method. Results : When compared with control, erythromycin and roxithromycin-treated groups had a significantly elevated serum theophylline level and decreased clearance. However, there were no significant changes of the serum theophylline level and clearance in clarithromycin and azithromycin-treated groups. Conclusion : These results suggest that theophylline dose may need to be readjusted and have periodic drug monitoring when erythromycin or roxithromycin is administered concurrently.

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Effect of Cimetidine on Theophylline Disposition and Metabolic Pathways (Cimetidine의 Theophylline 약동학 및 대사과정에 미치는 효과에 관한 연구)

  • Jang, In-Jin;Lee, Sun-Hee;Shin, Jae-Gook;Shin, Sang-Goo;Park, Chan-Woong
    • The Korean Journal of Pharmacology
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    • v.26 no.1
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    • pp.83-90
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    • 1990
  • The effect of cimetidine on theophylline metabolism was examined in dogs. Single dose intravenous theophylline kinetic studies were performed in cross-over manner before and after one week intravenous cimetidine (30 mg/kg/day) treatment. Cimetidine decreased theophylline clearance by an average of 31% (p<0.05) and prolonged theophylline half-li fe by an average of 29% (p<0.01) compared to those in control peirods. However, steady-state volume of distribution and protein binding of theophylline were not changed significantly. Twenty-four hours urinary excretion of 3-methylxanthine, 1-methyluric acid and 1,3-dimethyluric acid, which are the major metabolites of theophylline, were all decreased after cimetidine treatment, whereas the excreted fractions of individual metabolites were unchanged by cimetidine. From the above data, it could be susggested that cimetidine decreases theophylline clearance and prolongs the half-life by non-specific inhibition of the demethylations and 8-hydroxylation pathways.

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Effect of Formoterol on the Plasma Levels of Theophylline after the Oral Administration to the Children with Respiratory Diseases (소아 호출기 환자에서 경구 투여된 Formoterol이 Theophylline의 혈중농도에 미치는 영향의 연구)

  • Jang, Jin Kyung;Jung, Nak Gyun;Lee, Sook Hyang;Cho, Hea Kyoung
    • Korean Journal of Clinical Pharmacy
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    • v.10 no.3
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    • pp.107-110
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    • 2000
  • Theophylline and $\beta$-adrenergic agonists are frequently used together in patients with respiratory diseases. However the clinical impact of $\beta_2$-adrenergic agonists on the blood concentration of theophylline is not fully evaluated. Formoterol, a newly available oral ${\beta}_2$-adrenergic agonist is frequently used in pediatric respiratory patients. The objective of this study was to investigate the effect of oral formoterol on theophylline's blood concentration. Randomized prospective study was conducted. Twenty-four children were enrolled on the study. Their age ranged 2 to 73 months (mean 35.8 months). Theophylline group (12 patients) received 10 mg/kg/day of for theophylline orally. Theophylline/formoterol group (12 patients) received 10 mg/kg/day of theophylline and $4\;{\mu}g/kg/day$ of formoterol orally. All medications were administered at least for 5 days starting on admission day. Theophylline's trough concentrations were obtained on days 3 and day 5. Pulse rates were recorded before the study medications were given on admission, and days 3 and day 5. Statistical significance was calculated by two-tailed Student's t-test. Theophylline's levels in children given theophylline and formoterol together were lower an those given theophylline alone ($6.38\pm0.90\;{\mu}g/ml\;vs\;7.43\pm0.77\;{\mu}g/ml$ on day 3(p<0.05), $5.62\pm0.56\;{\mu}g/ml\;vs.\;6.78\pm0.61\;{\mu}g/ml$ on day 5 (p<0.05)). In both groups, theophylline's trough concentration on day 5 were lower than day 3. There was no significant side effects in both groups. In conclusion, the new ${\beta}_2$ selective adrenergic agonist formoterol reduced serum theophylline levels in children with respiratory diseases. Further investigation is needed to clarify the long term effect of this drug interaction.

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Effect of Combination Therapy of Isoniazid, Rifampicin, Ethambutol, and Pyrazinamide on Theophylline Pharmacokinetics (Isoniazid, Rifampicin, Ethambutol, Pyrazinamide의 병용투여가 Theophylline의 약물동태에 미치는 영향)

  • Ahn, Hyo-Cho;Yang, Jae-Heaon;Kim, Gwang-Hun;Ahn, Heok-Soo;Jang, Jae-Ho;Lee, Heung-Bum;Lee, Yong-Chul;Rhee, Yang-Keun
    • Tuberculosis and Respiratory Diseases
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    • v.44 no.5
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    • pp.992-1000
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    • 1997
  • Background : Since up to 90% of a theophylline dose is biotransformed, probably by interaction with one or more the variants of the cytochrome P-450 drug metabolism system, anti-tuberculosis agents including drugs influencing microsomal enzyme systems, such as isoniazid and rifampicin. may be affect the elimination of theophylline. Method : The effect of combination therapy with isoniazid(INH), rifampicin(RFP), ethambutol(EMB) and pyrazinamide(PZA) on the pharmacokinetics of theophylline was evaluated by a computer program using Bayesian method. Three group were divided as follows. Group I is control, Group II is treated with INH. RFP, EMB and PZA and Group III is treated with INH, RFP and EMB. All of them were ilon-smoker who were normal in liver and renal functions, and not administered drugs affecting on the clearance of theophylline with exception of anti-tuberculous agents. Results : When it compared control with test groups, the clearance of theophylline in Group II and Group III was significantly decreased(p<0.001), and half life in Group II and Group III showed significant elevation(p<0.001). However there were no significant differences in clearance and half life between the Group II and Group III. Conclusion : These results suggest that theophylline dose may be need of readjustment in concurrent medication of anti-tuberculous agents including INH, RFP, and EMB.

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Effects of Enoxacin and Ciprofloxacin on the Theophylline Metabolism in Humans (Enoxacin과 Ciprofloxacin이 Theophylline 대사에 미치는 영향에 대한 연구)

  • Choi, Soo-Jeon;Lee, Bong-Choon;Kim, Dong-Soon
    • Tuberculosis and Respiratory Diseases
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    • v.38 no.4
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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.

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Pharmacokinetics of Theophylline in Rabbits with Hepatic Failure (간장장해에서 Theophylline의 체내동태)

  • Moon, Hong-Sub;Lee, Chong-Ki;Choi, Jun-Shik
    • Korean Journal of Clinical Pharmacy
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    • v.2 no.1
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    • pp.23-28
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    • 1992
  • This study was attempted to investigate the pharmacokinetics of theophylline(4mg/kg) in the rabbits of carbon tetrachloride induced hepatic Cailure, The plasma concentration and relative bioavailability of theophylline were increased significantly in hepatic railure rabbits compared with those of normal rabbits. There was significant relationship between SGOT value and bioavailability parameters of theophylline. From the results of this experiments, dosage regimen of theophylline is considered to be adjusted in dose size and dosing interval using SGOT values.

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Selective Adsorption of a Symmetrie Theophylline Imprinted Membrane Prepare by a Wet Phase Inversion Method (습식 상 전이법으로 제조된 Theophylline 각인 대칭 막의 선택적 흡착)

  • 박중곤;오창엽;서정일
    • KSBB Journal
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    • v.17 no.2
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    • pp.207-211
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    • 2002
  • The theophylline imprinted membrane was prepared by a wet phase inversion method. Theophylline was implanted during copolymerization of acrylonitrile with acrylic acid or implanted in the dimethyl sulfoxide solution containing10 wt% copolymer, p(AN-co-AA). Rolling the glass plate, on which the copolymer solution was cast, in water removed the sponge layer and thus made the membrane symmetric. The adsorption selectivity of the membrane toward template molecule was increased with the coagulation temperature of the membrane and the initial concentration of the theophylline and caffeine mixture.

Chromatographic Characterization of Pentoxifylline and a Mixture of Caffeine-theophylline Imprinted Polymer (Pentoxifylline과 Caffeine-theophylline Imprinted Polymers의 크로마토그래피 특성)

  • 홍승표;왕덕선;구윤모;노경호
    • KSBB Journal
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    • v.18 no.1
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    • pp.65-69
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    • 2003
  • Two molecular imprinted polymers (MIPs) were prepared by using pentoxifylline and a mixture of caffeine-theophylline (2:1, mole ratio) as the templates, MAA as the monomer, and EDMA as the crosslinker The obtained polymer particles (particle size 25-35 $\mu\textrm{m}$) were packed into a HPLC column (150$\times$3.9mm). The selectivity and chromatographic characterization of the imprinted polymers were studied using pentoxifylline, caffeine, theophylline, theobromine as samples and acetonitrile as the mobile phase, Both imprinted polymers showed increased affinity for structural analogues. By using a mixture of caffeine-theophylline templates MIPs, good separations of caffeine, theobromine and theophylline were obtained, and pentoxifylline and caffeine were partly separated.

Effect of Cimetidine on Pharmacokinetics of Theophylline in Healthy Korean Volunteers (건강한 한국인 자원자에서 theophylline 약동학에 미치는 Cimetidine의 효과)

  • Kwon, Jun-Tack;Chai, Seok;Sohn, Dong-Ryul;Yom, Yoon-Ki;Kim, Hyung-Ki
    • Korean Journal of Clinical Pharmacy
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    • v.17 no.1
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    • pp.13-18
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    • 2007
  • The purpose of the present study was to investigate the effect of cimetidine on theophylline pharmacokinetics in Korean healthy normal subjects. Eight subjects were enrolled and open label, two period cross-over study was conducted without significant drug related adverse reactions. Cimetidine seemed that significantly inhibited the metabolism of theophylline, oral clearance decreased significantly when cimetidine was coadministered. Coadministered cimetidine increased $AUC_t$ and $C_{max}$ of theophylline. All subjects were genotyped using PCR-RFLP methods to evaluate the differences in metabolic capacity in accordance with CYP1A2 genotypes, but no mutant genotype was found. This suggests that metabolic capacities were not significantly affected by CYP1A2 genotypes among subjects. In conclusion, disposition of theophylline was significantly affected by coadministered cimetidine. Further evaluation with well-designed drug interaction study in accordance with various genotype of CYP1A2 is needed.

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Studies on the Effects of Dibutyryl Cyclic AMP and Theophylline on RNA Synthesis in Mouse Follicular Oocytes in Vitro (Dibutyryl Cyclic AMP와 Theophylline이 培養중인 생쥐 濾胞卵子의 RNA合成에 미치는 영향에 관한 연구)

  • Cho, Wan-Kyoo;Yoo, Seung-Hyun
    • The Korean Journal of Zoology
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    • v.18 no.1
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    • pp.19-26
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    • 1975
  • 自記放射法을 이용하여 dbcAMP와 theophylline이 未成熟卵子의 RNA合成에 미치는 영향을 관찰하였다. 培養中인 未成熟卵子의 RNA合成은 dbcAMP와 theophylline에 의하여 抑制를 받았다. dbcAMP나 theophylline은 培養液(modified Krebs-Ringer bicarbonate solution)內에 100 $\\mu$g/ml 정도 들어 있으며 핵막(germinal vesicle)의 붕괴 되지 못하고 그대로 存在하며 그동안의 RNA合成은 극히 억제된 채로 남아 있다. 그러나 培養을 시작하여 2$\\sim$3時間後, 즉 핵막붕괴가 끝난 다음에 이들 억제물질을 배양액에 添加하면 正常卵子와 같이 성숙분열이나 RNA合成이 억제 됨이 없이 진행된다. 24時間동안 dbcAMP나 theophylline으로 성숙이 억제 되었던 卵子도 이들 억제물질을 제거하면 즉시 成熟分裂이 진행되며 RNA合成도 正常的으로 일어난다. 이런 結果로 미루어 dbcAMP등의 RNA合成 抑制機作에 한 가지 가능성을 추측할 수 있다. 즉 dbcAMP나 theophylline의 처리에 의해 細胞質內 cAMP의 농도가 높아지고 이 cAMP는 핵막붕괴나 染色質의 응집에 관여하는 단백질 合成을 誘導할 mRNA合成을 억제하며 이 때문에 卵子는 핵을 보유한채 그대로 남아 있는 것이다.

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