中文品名】替莫西林
【药效类别】抗生素>青霉素类
【通用药名】TEMOCILLIN
【别　　名】Temopen，BRL 17421, ISF-09338, Negaspec, Negoban
【CA 名 称】
4-Thia-1-azabicyclo[3.2.0]heptane-2-carboxylic acid, 6-[(carboxy-3-thienylacetyl)amino]-6-methoxy-3,3-dimethyl-7-oxo-, (2S,5R,6R)-
【CA登记号】[66148-78-5]
【结 构 式】

【分 子 式】C16H18N2O7S2
【分 子 量】
【收录药典】

Principes actifs	Témocilline
Statut	Médicament soumis à prescription médicale
Laboratoire	Eumedica Sa

NEGABAN : ses autres formes替莫西林(替莫西林二钠)

　　Temocillin (Temopen, Negaban)

　　本品为耐β 内酰胺酶的半合成青霉素。对革兰阴性菌有高度抗菌活性，对β?内酰胺酶高度稳定，某些第三代头孢菌素耐药的革兰阴性菌应用本品有效。对肠杆菌属细菌、溶血性链球菌等抗菌活性好；但对绿脓杆菌活性差。临床应用于敏感菌所致的败血症、呼吸道感染腹膜炎、胆道感染、尿路感染及软组织感染等。常用剂量，1g～2g/次，1次/12小时，肌注或静注；对单纯性尿路感染0.5g/次，2次/日。对有肾功能损害的病人，用药间隔可延长。

　　替莫西林;别名:羧噻吩甲氧青霉素、坦莫西林、青霉素P12、Temopen;替莫西林适应症:临床用于治疗敏感菌所致尿路、皮肤和软组织感染等。;替莫西林药理学作用:本品为半合成广谱青霉素，口服不吸收。本品对β-内酰胺酶稳定，对革兰阴性菌有高度的抗菌活性，对某些对第三代头孢菌素耐药的革兰阴性菌敏感，对肠球菌、溶血性链球菌等活性较高，但对铜绿假单胞菌活性差。分类名称

　　一级分类：抗生素二级分类：青霉素类三级分类：

　　药品英文名

　　Temocillin

　　药品别名

　　羧噻吩甲氧青霉素、坦莫西林、青霉素P12、Temopen

　　药物剂型

　　注射剂(粉)：1g，2g。

　　药理作用

　　本品为半合成广谱青霉素，口服不吸收。本品对β-内酰胺酶稳定，对革兰阴性菌有高度的抗菌活性，对某些对第三代头孢菌素耐药的革兰阴性菌敏感，对肠球菌、溶血性链球菌等活性较高，但对铜绿假单胞菌活性差。

　　药动学

　　本品在胃酸中不稳定，口服不吸收。肌内注射后约1h达到血药峰浓度，胆汁中有分泌，但脑脊液中浓度较低，血浆蛋白结合率为85%，主要由肾脏排出，半衰期较长，为4.5～5.4h，肾功能损害者可达18h以上。

　　适应证

　　临床用于治疗敏感菌所致尿路、皮肤和软组织感染等。

　　禁忌证

　　1.对本品及青霉素过敏者禁用。2.产妇和哺乳期妇女禁用。

　　注意事项

　　不良反应

　　见青霉素。本品能被血液透析所清除。

　　用法用量

　　肌内注射或缓慢静脉注射给药：成人：每天1～4g，分2次给予。

　　药物相应作用

　　本品与氨基糖苷类药物(如庆大霉素、妥布霉素、阿米卡星等)合用对铜绿假单胞菌有协同作用。但不宜在同一容器中给予，以免两者失活。

　　专家点评

　　国外曾报道本品为半合成青霉素，对革兰阴性菌感染有效，包括尿道、呼吸系统和胆道的感染。另外对医院内感染、菌血症、腹膜炎、手术后创面感染和淋病亦有效。对大多数革兰阴性菌有抗菌活性，能高度抵抗β-内酰胺酶。应用本品治疗肾盂肾炎、膀胱炎，每天0.5～1g，每天2次，连续5天，结果痊愈率为97.0%
NEGABAN 2 g Poudre pour solution injectable Boîte de 1 Flacon
Drug Description
1 g of temocillin as temocillin sodium.
Presentation
Powder for solution for injection/infusion. Vial containing a white to pale yellow sterile solid.
Indications
Negaban is indicated for the treatment of septicaemia, urinary tract infection and lower respiratory tract infection where susceptible gram-negative bacilli are suspected or confirmed. In mixed infections where gram-positive or anaerobic bacteria are also liable to be implicated, co-administration with other appropriate antibacterial agents should be considered. Consideration should be given to official guidance on the appropriate use of antibacterial agents.
Adult Dosage

Adults (including the elderly): The usual dosage is 1-2 g every 12 hours.
 
Children: Insufficient data are available to recommend an appropriate dosage regime.
 
Dosage in patients with impaired renal or hepatic functions (adults): Temocillin is mainly excreted renally and unchanged. Excretion is reduced in renal impairment and half-life is increased according to the severity of renal failure. In moderate and severe renal failure, dose adjustments are necessary in accordance with the following regimen:

Creatinine clearance (ml/min)

Dosage per administration

Interval between administrations
 
More than 60

1 to 2 g
12 h

60 to 30

1 g

12 h

30 to 10
 
1 g
 
24 h
 
Less than 10

1 g or 500 mg
 
48 h or 24 h

In case of hemodialysis: as a rule, the I.M. route should be avoided, considering the patient's treatment with heparin. I.V. injection of Negaban is recommended, using water for injection as solvent: 1 g (I.V.) every 48 hours, preferably at the end of the hemodialysis. In case of daily hemodialysis: 500 mg (I.V.) after each hemodialysis.
 
In case of continuous peritoneal dialysis in ambulatory patients: 1 g Negaban I.M. every 48 hours.
 
These data are based on studies where creatinine clearance was used to estimate the degree of renal impairment.
 
Limited experience in patients with impaired hepatic function has not indicated a need for a reduction in dosage.

Method of administration:
 
Negaban may be administered by intravenous injection, intermittent intravenous infusion or intramuscular injection.
 
Intravenous solutions: Negaban solutions should be administered by slow injection into the vein (3-4 minutes) or as an intravenous infusion over a period of 30-40 minutes.
 
Intramuscular injection: Negaban may be given intramuscularly after reconstitution. If pain is experienced at the site of I.M. injection, a sterile solution of lidocaine hydrochloride 0.5-1% may be used in place of Water for Injections.
 
Contra Indications

The use of Negaban is contraindicated in patients with a history of allergic reactions to any of the penicillins or any other type of beta-lactam drug.
 
Special Precautions

Serious and occasionally fatal anaphylactic reactions have been reported in patients receiving therapy with penicillins. If an allergic reaction occurs during therapy with Negaban, the drug must be discontinued.
 
Cross-allergy with cephalosporins is frequent (10 to 15%).
 
In patients with kidney failure, the posology must be adapted to the degree of insufficiency. Posology and Method of Administration.
 
Bleeding manifestations have occurred in some patients receiving beta-lactam antibiotics. These reactions have sometimes been assessed with abnormalities of coagulation tests and are more likely to occur in patients with renal failure. If bleeding manifestations occur, the antibiotic should be discontinued and appropriate therapy instituted.
 
As with any antibiotic, temocillin may be associated with induced pseudomembranous colitis, although animal studies have never shown any induction of Clostridium difficile infection. In case of severe, persistent diarrhoea, caution is recommended, Negaban must be discontinued and suitable therapy be initiated (eg oral metronidazole or oral vancomycin). Preparations which inhibit peristalsis are contra-indicated.
 
As with other antibiotics, the possibility of emergence of resistant organisms which might cause superinfections should be kept in mind, particularly during prolonged treatment. Microbiological follow-up may be required to detect any important superinfection. If this occurs, appropriate measures should be taken.
 
As with other penicillins, patients may experience neuromuscular excitability or convulsions if higher than recommended doses are given intravenously.
 
Periodic electrolyte determinations should be made in patients with low potassium reserves and the possibility of hypokalaemia should be kept in mind with patients who have potentially low potassium reserves and who are receiving cytotoxic therapy or diuretics. Modest elevations of indices of liver function may be observed.
 
1 vial of Negaban 1 g contains 5 mmol of sodium.
 
Interactions

None known.
 
Adverse Reactions

Undesirable effects are typical of the injectable penicillins: they may include diarrhoea, pain at the site of I.M. injection, occasionally rash, either urticarial or erythematous.
 
Certain reactions such as fever, arthralgia or myalgia, sometimes develop more than 48 hours after the start of the treatment. In any case, discontinuance of treatment and recourse to another appropriate antibiotic therapy are essential.
 
In common with other ß-lactam antibiotics angioedema and anaphylaxis have been reported.
 
There is also a risk of phlebitis and thrombophlebitis with intravenous administration of β-lactam antibiotics, although to a lesser extent in the case of Negaban.
 
In patients suffering from renal failure, neurological disorders with convulsions have been reported following the I.V. injection of high doses of penicillin.
 
Manufacturer
EUMEDICA SA
Drug Availability
 POM – Prescription Only Medicine
Updated
05 March 2010