静脉注射甲氧苄啶-磺胺甲恶唑的临床药理学
Clinical pharmacology of intravenously administered trimethoprim-sulfamethoxazole.
作者信息
Grose W E, Bodey G P, Loo T L
出版信息
Antimicrob Agents Chemother. 1979 Mar;15(3):447-51. doi: 10.1128/AAC.15.3.447.
Abstract
Pharmacokinetic studies of intravenously administered trimethoprim-sulfamethoxazole (TMP-SMX) were conducted in 11 patients with cancer while they received therapy with this drug combination for infection. Each patient received 160 mg of TMP and 800 mg of SMX every 8 h. The highest plasma concentrations of both agents were attained at the end of a 1-h infusion period, and the levels were maintained above 38 mug of free SMX and 2 mug of TMP per ml for 2 to 4 h on day 1. On day 4, these concentrations were exceeded at all time intervals of blood sampling. High concentrations of TMP and free SMX were recovered in the urine during the 8-h period. The plasma half-lives of TMP and free SMX, as determined during the first 8-h period, were 7.6 and 8.6 h, respectively. Compared with SMX, TMP had an approximately 2.5 times higher volume of distribution. This drug combination was well tolerated by the patients and unaccompanied by drug-related toxicity.
摘要
对11例癌症患者进行了静脉注射甲氧苄啶-磺胺甲恶唑（TMP-SMX）的药代动力学研究，这些患者在接受该药物组合治疗感染期间。每位患者每8小时接受160毫克TMP和800毫克SMX。两种药物的最高血浆浓度在1小时输注期结束时达到，在第1天，每毫升游离SMX浓度维持在38微克以上，TMP浓度维持在2微克以上达2至4小时。在第4天，所有采血时间间隔的浓度均超过上述水平。在8小时期间尿液中回收了高浓度的TMP和游离SMX。在前8小时期间测定的TMP和游离SMX的血浆半衰期分别为7.6小时和8.6小时。与SMX相比，TMP的分布容积约高2.5倍。患者对该药物组合耐受性良好，未出现与药物相关的毒性反应。
相似文献
1
Clinical pharmacology of intravenously administered trimethoprim-sulfamethoxazole.静脉注射甲氧苄啶-磺胺甲恶唑的临床药理学
Antimicrob Agents Chemother. 1979 Mar;15(3):447-51. doi: 10.1128/AAC.15.3.447.
2
Intravenous trimethoprim-sulfamethoxazole alone or combined with tobramycin for infections in cancer patients.
Am J Med Sci. 1980 Jan-Feb;279(1):4-13. doi: 10.1097/00000441-198001000-00001.
3
Pharmacokinetics of sulfadimethoxine and sulfamethoxazole in combination with trimethoprim after intravenous administration to healthy and pneumonic pigs.磺胺二甲氧嘧啶和磺胺甲恶唑与甲氧苄啶联合静脉注射给健康猪和患肺炎猪后的药代动力学
J Vet Pharmacol Ther. 1995 Aug;18(4):243-53. doi: 10.1111/j.1365-2885.1995.tb00588.x.
4
Trimethoprim-sulfamethoxazole pharmacokinetics during continuous ambulatory peritoneal dialysis.
Clin Nephrol. 1984 Nov;22(5):239-43.
5
Pharmacokinetics of trimethoprim and sulfamethoxazole in serum and cerebrospinal fluid of adult patients with normal meninges.甲氧苄啶和磺胺甲恶唑在脑膜正常的成年患者血清和脑脊液中的药代动力学。
Antimicrob Agents Chemother. 1984 Dec;26(6):811-4. doi: 10.1128/AAC.26.6.811.
6
Use of trimethoprim-sulfamethoxazole to prevent bacterial infections in children with acute lymphoblastic leukemia.使用甲氧苄啶-磺胺甲恶唑预防急性淋巴细胞白血病患儿的细菌感染。
Pediatr Infect Dis. 1985 May-Jun;4(3):265-9. doi: 10.1097/00006454-198505000-00012.
7
A comparison of trimethorprim-sulfamethoxazole with sulfamethoxazole alone in infections localized to the kidneys.甲氧苄啶-磺胺甲恶唑与单用磺胺甲恶唑治疗局限性肾脏感染的比较。
Can Med Assoc J. 1975 Jun 14;112(13 Spec No):9-12.
8
Effect of trimethoprim and trimethoprim-sulfamethoxazole on development of drug-resistant vaginal and fecal floras.甲氧苄啶及甲氧苄啶-磺胺甲恶唑对耐药性阴道和粪便菌群形成的影响。
Antimicrob Agents Chemother. 1980 Feb;17(2):263-8. doi: 10.1128/AAC.17.2.263.
9
Therapeutic failure of trimethoprim/sulfamethoxazole in the treatment of Pneumocystis carinii pneumonia.甲氧苄啶/磺胺甲恶唑治疗卡氏肺孢子虫肺炎的治疗失败
Ann Pharmacother. 1999 Apr;33(4):413-5. doi: 10.1345/aph.18225.
10
Plasma levels of trimethoprim and sulfonamide after administration of trimethoprim-sulfamethoxazole and trimethoprim-sulfamoxole.服用复方新诺明和复方磺胺甲恶唑后甲氧苄啶和磺胺类药物的血浆水平。
Int J Clin Pharmacol Ther Toxicol. 1980 Dec;18(12):536-7.
引用本文的文献
1
Population Pharmacokinetics of Trimethoprim/Sulfamethoxazole: Dosage Optimization for Patients with Renal Insufficiency or Receiving Continuous Renal Replacement Therapy.甲氧苄啶/磺胺甲恶唑的群体药代动力学：肾功能不全患者或接受持续肾脏替代治疗患者的剂量优化
Clin Pharmacol Ther. 2025 Jan;117(1):184-192. doi: 10.1002/cpt.3421. Epub 2024 Aug 15.
2
Lessons from Multiple Infections Such as Lymphoma Complicated with Pneumocystis Infection: A Case Report.淋巴瘤合并肺孢子菌感染等多重感染的经验教训：一例报告
Infect Drug Resist. 2024 Apr 22;17:1583-1588. doi: 10.2147/IDR.S461607. eCollection 2024.
3
Uropathogenic Escherichia coli Shows Antibiotic Tolerance and Growth Heterogeneity in an Model of Intracellular Infection.尿路致病性大肠杆菌在细胞内感染模型中表现出抗生素耐受和生长异质性。
Antimicrob Agents Chemother. 2021 Nov 17;65(12):e0146821. doi: 10.1128/AAC.01468-21. Epub 2021 Sep 27.
4
A trimethoprim derivative impedes antibiotic resistance evolution.一种三甲氧苄氨嘧啶衍生物能阻碍抗生素耐药性的进化。
Nat Commun. 2021 May 19;12(1):2949. doi: 10.1038/s41467-021-23191-z.
5
Activity of Cefiderocol Alone and in Combination with Levofloxacin, Minocycline, Polymyxin B, or Trimethoprim-Sulfamethoxazole against Multidrug-Resistant Stenotrophomonas maltophilia.头孢地尔单独及与左氧氟沙星、米诺环素、多粘菌素B或复方磺胺甲恶唑联合使用对多重耐药嗜麦芽窄食单胞菌的活性。
Antimicrob Agents Chemother. 2020 Aug 20;64(9). doi: 10.1128/AAC.00559-20.
6
Cotrimoxazole - optimal dosing in the critically ill.复方新诺明——危重症患者的最佳给药剂量
Ann Intensive Care. 2014 Apr 28;4:13. doi: 10.1186/2110-5820-4-13. eCollection 2014.
7
Trimethoprim- sulfamethoxazole: pharmacokinetics, clinical uses, and adverse reactions.甲氧苄啶-磺胺甲恶唑：药代动力学、临床应用及不良反应。
Tex Heart Inst J. 1990;17(2):86-93.
8
Pharmacokinetic optimisation in the treatment of Pneumocystis carinii pneumonia.卡氏肺孢子虫肺炎治疗中的药代动力学优化
Clin Pharmacokinet. 1993 May;24(5):388-412. doi: 10.2165/00003088-199324050-00004.
9
Treatment of experimental endocarditis due to methicillin-susceptible or methicillin-resistant Staphylococcus aureus with trimethoprim-sulfamethoxazole and antibiotics that inhibit cell wall synthesis.用甲氧苄啶-磺胺甲恶唑和抑制细胞壁合成的抗生素治疗由甲氧西林敏感或耐甲氧西林金黄色葡萄球菌引起的实验性心内膜炎。
Antimicrob Agents Chemother. 1995 Apr;39(4):953-7. doi: 10.1128/AAC.39.4.953.
10
Clinical pharmacokinetics of co-trimoxazole (trimethoprim-sulphamethoxazole).复方新诺明（甲氧苄啶-磺胺甲恶唑）的临床药代动力学
Clin Pharmacokinet. 1980 Sep-Oct;5(5):405-23. doi: 10.2165/00003088-198005050-00001.
本文引用的文献
1
Potentiation of sulfonamides and antibiotics by trimethoprim [2,4-diamino-5-(3,4,5-trimethoxybenzyl) pyrimidine].甲氧苄啶[2,4-二氨基-5-(3,4,5-三甲氧基苄基)嘧啶]对磺胺类药物和抗生素的增效作用
Antimicrob Agents Chemother (Bethesda). 1966;6:430-3.
2
Pharmacokinetics of sulfamethoxazole plus trimethoprim in man and their distribution in the rat.磺胺甲恶唑加甲氧苄啶在人体中的药代动力学及其在大鼠体内的分布。
Chemotherapy. 1970;15(6):337-55. doi: 10.1159/000220701.
3
Spectrofluorimetric method for the determination of trimethoprim in body fluids.体液中甲氧苄啶测定的荧光分光光度法。
Chemotherapy. 1969;14:Suppl:22-9. doi: 10.1159/000220652.
4
Species differences among dihydrofolate reductases as a basis for chemotherapy.二氢叶酸还原酶的种属差异作为化疗的基础。
Postgrad Med J. 1969 Nov;45:Suppl:7-10.
5
Trimethoprim, a sulphonamide potentiator.甲氧苄啶，一种磺胺增效剂。
Br J Pharmacol Chemother. 1968 May;33(1):72-90. doi: 10.1111/j.1476-5381.1968.tb00475.x.
6
Single-blind comparative trial of trimethoprim-sulphamethoxazole and ampicillin in the treatment of exacerbations of chronic bronchitis.甲氧苄啶-磺胺甲恶唑与氨苄西林治疗慢性支气管炎急性加重期的单盲对照试验
Br Med J. 1969 Nov 22;4(5681):470-3. doi: 10.1136/bmj.4.5681.470.
7
Absorption and urinary execretion of trimethoprim, sulfamethoxazole, and trimethoprim-sulfamethoxazole: results with single doses in normal young adults and preliminary observations during therapy with trimethoprim-sulfamethoxazole.甲氧苄啶、磺胺甲恶唑及甲氧苄啶-磺胺甲恶唑的吸收与尿排泄：正常年轻成年人单剂量用药结果及甲氧苄啶-磺胺甲恶唑治疗期间的初步观察
J Infect Dis. 1973 Nov;128:Suppl:584-99 p. doi: 10.1093/infdis/128.supplement_3.s584.
8
Excretion of sulfamethoxazole and trimethoprim into human bile.磺胺甲恶唑和甲氧苄啶向人胆汁中的排泄。
J Infect Dis. 1973 Nov;128:Suppl:574 p. doi: 10.1093/infdis/128.supplement_3.s574.
9
Pharmacokinetics of trimethoprim and sulfamethoxazole in normal subjects and in patients with renal failure.甲氧苄啶和磺胺甲恶唑在正常受试者及肾衰竭患者中的药代动力学。
J Infect Dis. 1973 Nov;128:Suppl:556-66 p. doi: 10.1093/infdis/128.supplement_3.s556.
10
Pharmacokinetic profile of trimethoprim-sulfamethoxazole in man.甲氧苄啶-磺胺甲恶唑在人体中的药代动力学特征。
J Infect Dis. 1973 Nov;128:Suppl:547-55 p. doi: 10.1093/infdis/128.supplement_3.s547.
Zotero 插件