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替卡西林:其药理特性与治疗效果综述

Ticarcillin: a review of its pharmacological properties and therapeutic efficacy.

作者信息

Brogden R N, Heel R C, Speight T M, Avery G S

出版信息

Drugs. 1980 Nov;20(5):325-52. doi: 10.2165/00003495-198020050-00001.

DOI:10.2165/00003495-198020050-00001
PMID:7002527
Abstract

Ticarcillin is a semisynthetic penicillin for parenteral administration. The antibacterial activity of ticarcillin is similar to that of carbenicillin except that it is two to four times more active in vitro against Pseudomonas aeruginosa, generally less active against Gram-positive cocci and more active against most Gram-negative bacilli. As the pharmacokinetics of ticarcillin and carbenicillin are also similar, ticarcillin should theoretically be clinically effective when administered at a lower dosage than carbenicillin. There is some evidence that ticarcillin is comparable in efficacy with carbenicillin when given in half to two-thirds the dosage, when the drugs are given in combination with an aminoglycoside and in clinical situations where these drugs are agents of choice. Ticarcillin has been used successfully in the treatment of complicated urinary tract infection, pulmonary infection in cystic fibrosis and bacteraemia and is effective when combined with an aminoglycoside in severe infections in patients with granulocytopenia. The efficacy in anaerobic infections is at present poorly documented, although preliminary results are promising. Tolerability has generally been good with hypokalaemia being the most frequently reported side effect. At the dosages used, bleeding and fluid overload have seldom occurred.

摘要

替卡西林是一种供注射用的半合成青霉素。替卡西林的抗菌活性与羧苄西林相似,不同的是它对铜绿假单胞菌的体外活性比羧苄西林强2至4倍,对革兰氏阳性球菌的活性一般较弱,对大多数革兰氏阴性杆菌的活性较强。由于替卡西林和羧苄西林的药代动力学也相似,理论上替卡西林以低于羧苄西林的剂量给药时应具有临床疗效。有证据表明,当替卡西林与氨基糖苷类药物联合使用时,以及在这些药物为首选药物的临床情况下,以羧苄西林一半至三分之二的剂量给药时,其疗效与羧苄西林相当。替卡西林已成功用于治疗复杂性尿路感染、囊性纤维化患者的肺部感染和菌血症,并且在粒细胞减少症患者的严重感染中与氨基糖苷类药物联合使用时有效。尽管初步结果很有前景,但目前替卡西林在厌氧菌感染中的疗效记录不足。总体耐受性良好,低钾血症是最常报告的副作用。在所用剂量下,很少发生出血和液体超负荷。

相似文献

1
Ticarcillin: a review of its pharmacological properties and therapeutic efficacy.替卡西林:其药理特性与治疗效果综述
Drugs. 1980 Nov;20(5):325-52. doi: 10.2165/00003495-198020050-00001.
2
Carbenicillin and ticarcillin.羧苄青霉素和替卡西林。
Med Clin North Am. 1982 Jan;66(1):61-77. doi: 10.1016/s0025-7125(16)31442-0.
3
Comparative in vitro activity and clinical pharmacology of ticarcillin and carbenicillin.替卡西林和羧苄西林的体外活性及临床药理学比较
Antimicrob Agents Chemother. 1975 Oct;8(4):457-62. doi: 10.1128/AAC.8.4.457.
4
In vitro activity of ticarcillin, carbenicillin and ampicillin against some gram-negative bacilli.替卡西林、羧苄西林和氨苄西林对某些革兰氏阴性杆菌的体外活性。
J Antibiot (Tokyo). 1975 Nov;28(11):912-9. doi: 10.7164/antibiotics.28.912.
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Ticarcillin: a collaborative in vitro comparison with carbenicillin against over 9,000 clinical bacterial isolates.替卡西林:与羧苄西林针对9000多株临床分离细菌的体外协同比较
Am J Med Sci. 1977 Nov-Dec;274(3):255-63.
6
Clinical pharmacology and efficacy of ticarcillin in infants and children.替卡西林在婴幼儿中的临床药理学及疗效
Pediatrics. 1978 Jun;61(6):858-63.
7
Ticarcillin for treatment of serious infections with gram-negative bacteria.替卡西林用于治疗革兰氏阴性菌引起的严重感染。
J Infect Dis. 1976 Nov;134(5):476-85. doi: 10.1093/infdis/134.5.476.
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In vitro activity of ticarcillin against anaerobic bacteria compared with that of carbenicillin and penicillin.替卡西林对厌氧菌的体外活性与羧苄西林和青霉素的比较。
Antimicrob Agents Chemother. 1977 Feb;11(2):258-61. doi: 10.1128/AAC.11.2.258.
9
Interactions of carbenicillin and ticarcillin with gentamicin.羧苄西林和替卡西林与庆大霉素的相互作用。
Antimicrob Agents Chemother. 1975 Apr;7(4):431-4. doi: 10.1128/AAC.7.4.431.
10
Clinical and pharmacological studies of ticarcillin in gram-negative infections.替卡西林治疗革兰氏阴性菌感染的临床及药理学研究。
Antimicrob Agents Chemother. 1976 Jan;9(1):94-101. doi: 10.1128/AAC.9.1.94.

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Drugs. 2015 Dec;75(18):2097-117. doi: 10.1007/s40265-015-0506-7.
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Susceptibility of gram-negative bacteria and Staphylococcus aureus to combinations of ticarcillin and clavulanic acid.革兰氏阴性菌和金黄色葡萄球菌对替卡西林与克拉维酸联合用药的敏感性。
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本文引用的文献

1
Prospective, randomized comparative study of clindamycin, chloramphenicol, and ticarcillin, each in combination with gentamicin, in therapy for intraabdominal and female genital tract sepsis.克林霉素、氯霉素及替卡西林分别与庆大霉素联合用于治疗腹腔内感染和女性生殖道败血症的前瞻性随机对照研究。
J Infect Dis. 1980 Sep;142(3):384-93. doi: 10.1093/infdis/142.3.384.
2
-carboxy-3-thienylmethylpenicillin (BRL 2288), a new semisynthetic penicillin: absorption and excretion in man.羧基-3-噻吩甲基青霉素(BRL 2288),一种新型半合成青霉素:人体中的吸收与排泄
Antimicrob Agents Chemother (Bethesda). 1970;10:402-6. doi: 10.1128/AAC.10.3.402.
3
磺胺二甲氧嘧啶、阿莫西林、克拉维酸分别与阿莫西林或替卡西林联用、替莫西林及氯唑西林对脐血血清中胆红素的置换作用。
Br J Clin Pharmacol. 1985 Oct;20(4):345-8. doi: 10.1111/j.1365-2125.1985.tb05075.x.
4
In vitro susceptibility of Mycobacterium tuberculosis, Mycobacterium africanum, Mycobacterium bovis, Mycobacterium avium, Mycobacterium fortuitum, and Mycobacterium chelonae to ticarcillin in combination with clavulanic acid.结核分枝杆菌、非洲分枝杆菌、牛分枝杆菌、鸟分枝杆菌、偶然分枝杆菌和龟分枝杆菌对替卡西林联合克拉维酸的体外敏感性。
Antimicrob Agents Chemother. 1987 Jan;31(1):132-3. doi: 10.1128/AAC.31.1.132.
5
Clinical pharmacokinetics of enzyme inhibitors in antimicrobial chemotherapy.抗菌化疗中酶抑制剂的临床药代动力学
Clin Pharmacokinet. 1988 Sep;15(3):133-64. doi: 10.2165/00003088-198815030-00001.
Susceptibility of Proteus species and Pseudomonas aeruginosa to penicillins and cephalosporins.
Antimicrob Agents Chemother (Bethesda). 1970;10:63-7.
4
-carboxy-3-thienylmethylpenicillin (BRL 2288), a new semisynthetic penicillin: in vivo evaluation.羧基-3-噻吩甲基青霉素(BRL 2288),一种新型半合成青霉素:体内评价
Antimicrob Agents Chemother (Bethesda). 1970;10:396-401.
5
-carboxy-3-thienylmethylpenicillin (BRL 2288), a new semisynthetic penicillin: in vitro evaluation.羧基-3-噻吩甲基青霉素(BRL 2288),一种新型半合成青霉素:体外评价
Antimicrob Agents Chemother (Bethesda). 1970;10:390-5.
6
In vitro studies of a semisynthetic penicillin, 6-(D(-)- -carboxy-3-thienylacetamido) penicillanic acid (BRL 2288), active against Pseudomonas.对一种半合成青霉素6-(D(-)-α-羧基-3-噻吩乙酰氨基)青霉烷酸(BRL 2288)进行的体外研究,该青霉素对铜绿假单胞菌有活性。
Antimicrob Agents Chemother (Bethesda). 1970;10:385-9.
7
Semisynthetic penicillin 6-(D(--)-alpha-carboxy-3-thienylacetamido) penicillanic acid active against Pseudomonas in vitro.半合成青霉素6 -(D(-)-α-羧基-3-噻吩基乙酰胺基)青霉烷酸在体外对假单胞菌有活性。
Appl Microbiol. 1971 Jan;21(1):66-70. doi: 10.1128/am.21.1.66-70.1971.
8
In vitro studies of alpha-carboxyl-3-thienylmethyl penicillin, a new semisynthetic penicillin.新型半合成青霉素α-羧基-3-噻吩甲基青霉素的体外研究
Appl Microbiol. 1971 Jan;21(1):61-5. doi: 10.1128/am.21.1.61-65.1971.
9
Administration of ticarcillin, a new antipseudomonal antibiotic, in patients undergoing dialysis.在接受透析的患者中使用替卡西林(一种新型抗假单胞菌抗生素)。
Antimicrob Agents Chemother. 1974 Feb;5(2):119-20. doi: 10.1128/AAC.5.2.119.
10
Clinical pharmacology of ticarcillin (alpha-carboxyl-3-thienylmethyl penicillin, BRL-2288).替卡西林(α-羧基-3-噻吩甲基青霉素,BRL-2288)的临床药理学
Antimicrob Agents Chemother. 1973 Jul;4(1):31-6. doi: 10.1128/AAC.4.1.31.