中文名称： 亚胺培南-西司他丁钠
英文名称： Imipenem-Cilastatin sodium hydrate
英文别名： Sodium (Z)-7-[(2R)-2-amino-3-hydroxy-3-oxopropyl]sulfanyl-2-[[(1S)-2,2-dimethylcyclopropanecarbonyl]amino]hept-2-enoate (5R,6S)-3-[2-(aminomethylideneamino)ethylsulfanyl]-6-(1-hydroxyethyl)-7-oxo-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid hydrate; (2Z)-7-{[(2S)-2-amino-2-carboxyethyl]sulfanyl}-2-({[(1S)-2,2-dimethylcyclopropyl]carbonyl}amino)hept-2-enoic acid - (5R,6S)-3-[(2-{[(E)-aminomethylidene]amino}ethyl)sulfanyl]-6-[(1R)-1-hydroxyethyl]-7-oxo-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid hydrate (1:1:1); (2Z)-7-{[(2S)-2-amino-2-carboxyethyl]sulfanyl}-2-({[(1S)-2,2-dimethylcyclopropyl]carbonyl}amino)hept-2-enoic acid - (5R,6S)-3-[(2-{[(1E)-aminomethylidene]amino}ethyl)sulfanyl]-6-[(1R)-1-hydroxyethyl]-7-oxo-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid (1:1)
CAS号： 92309-29-0
分子式： C28H43N5O9S2
分子量： 657.7991 
InChI： InChI=1/C16H26N2O5S.C12H17N3O4S/c1-16(2)8-10(16)13(19)18-12(15(22)23)6-4-3-5-7-24-9-11(17)14(20)21;1-6(16)9-7-4-8(20-3-2-14-5-13)10(12(18)19)15(7)11(9)17/h6,10-11H,3-5,7-9,17H2,1-2H3,(H,18,19)(H,20,21)(H,22,23);5-7,9,16H,2-4H2,1H3,(H2,13,14)(H,18,19)/b12-6-;/t10-,11-;6-,7-,9-/m11/s1 
分子结构： 

分类名称
一级分类：抗生素 二级分类：其他β内酰胺类 三级分类： 
 
药品英文名
Imipenem
 
药品别名
伊米配能/西司他丁钠、亚胺硫霉素/西拉司丁、泰宁、泰能、Imipenem/Cilastatin、Primaxin、Tienam
 
药物剂型
注射剂。 每支0.25g；0.5g；1g（以亚胺培南计量）。其中含有等量的西拉司丁钠。
 
药理作用
本品为具有碳青霉烯环的甲砜霉素类抗生素，通过抑制细菌细胞壁的合成而杀灭革兰阳性菌、阴性菌及厌氧菌，其中包括对其他抗生素不敏感或易耐药的铜绿假单胞菌、金黄色葡萄球菌、粪肠球菌和脆弱拟杆菌。由于亚胺培南可在肾内被肾肽酶破坏，临床应用制剂中加入了西司他丁钠特异性酶抑制剂，它可阻断亚胺培南在肾脏的代谢，继而增加尿道中未经改变的亚胺培南的浓度，以保证药物的有效性。本品对细菌产生的β-内酰胺酶的稳定性强，抗菌谱广，抗菌活性强。链球菌属(产酶、不产酶)、大肠埃希菌属、克雷伯菌属、流感嗜血杆菌、变形梭杆菌、沙雷菌属、产气杆菌、阴沟肠杆菌、铜绿假单胞菌、不动杆菌及脆弱拟杆菌等致病菌均对本品高度敏感。
 
药动学
本品为亚胺培南和西司他丁钠的复合物，二者的比例为1∶1。静脉注射本品1g(静注时间不可少于40～60min)，Cmax为65mg/L，有效抗菌浓度可维持4～6h。本品t1/2β为1h，主要经肾排出体外，24h尿中排出给药量的70%。
 
适应证
临床由于敏感菌引起的各类感染。尤其适用于多种菌混合感染和需氧/厌氧菌的混合感染，如败血症、感染性心内膜炎，腹腔内感染、下呼吸道感染、泌尿生殖器感染、妇科感染、骨关节感染、皮肤和软组织感染等，还适用于污染的手术或可能污染之手术的术前预防、及防止已存在的手术后感染向严重发展。有效率均在85%以上。
 
禁忌证
对本品任何成分有过敏的患者禁用；严重休克或有心脏传导阻滞的患者禁用。
 
注意事项
本品与β-内酰胺抗生素、青霉素和头孢菌素有局部交叉过敏反应，因此，在使用本品前，应详细询问患者有无过敏史，使用后若有过敏反应，应立即停药并做相应处理。孕妇和哺乳期妇女慎用。有癫痫病的患者在应用本品期间应继续采用抗惊厥疗法。一旦出现局部性震颤，则应减量或停药。 本品静滴时不能与其他抗生素混合使用。且应现用现配，用生理盐水溶解的药液室温下存放不能超过12h，用葡萄糖溶液溶解的药液只能保存4h。
 
不良反应
超剂量使用本品可能出现神经系统毒性反应，如肌肉痉挛、精神错乱或癫痫发作，尤其是肾功能损害严重伴有癫痫病史的患者。局部红斑、疼痛，有可能发生血栓性静脉炎。过敏反应：皮疹、瘙痒、荨麻疹、多形性红斑、约翰逊综合征血管性水肿、念珠菌病、发热，牙齿色斑。罕见中毒性表皮坏死、表皮脱落性皮炎。胃肠道反应：恶心、呕吐、腹泻、严重者可发生伪膜性肠炎。血液：嗜酸细胞增多症、白细胞减少症、中性白细胞减少症、血小板减少症、血小板增多症和血红蛋白降低，以及延长凝血酶原时间，部分患者Coombs试验呈阳性反应。肝肾功能：可出现ALT、AST、胆红素和碱性磷酸酶升高、罕见肝炎。对肾功能不良的患者，有可能引起肾功能损伤。
 
用法用量
静脉滴注，稀释液可用0.9%氯化钠溶液、5% (10%)葡萄糖溶液、5%(10%)甘露醇溶液。成人，一般感染：每天1～2g，分3或4次静脉滴注；重症感染：每天2g，分2次静脉滴注，最大剂量不能超过每天4g，静脉点滴速度30min500mg为宜。儿童，每天30～80mg/kg；严重感染每天100mg/kg，每6～8小时1次。
 
药物相应作用
丙磺舒可使本品的血药浓度和T1/2延长，故不推荐并用。与乳酸钠制剂产生配伍变化。本品虽可与氨基糖苷类抗生素联用，但两种药物不可混合注射。

【原产地英文商品名】PRIMAXIN I.V. 500mg/vial 25vials/box
【原产地英文药品名】IMIPENEM/CILASTATIN SODIUM
【中文参考商品译名】
注：以下产品不同规格和不同价格，购买时请以电话咨询为准
·PRIMAXIN I.V. 500毫克/瓶 25瓶/盒
·PRIMAXIN I.V. 250毫克/瓶 25瓶/盒
【中文参考药品译名】亚胺培南-西拉司丁钠
【生产厂家中文参考译名】默克
【生产厂家英文名】MERCK

Although clinical improvement has been observed in patients with cystic fibrosis, chronic pulmonary disease, and lower respiratory tract infections caused by P aeruginosa, bacterial eradication may not necessarily be achieved.

As with other beta-lactam antibiotics, some strains of P aeruginosa may develop resistance fairly rapidly during treatment with PRIMAXIN I.V. During therapy of P aeruginosa infections, periodic susceptibility testing should be done when clinically appropriate.

To reduce the development of drug-resistant bacteria and maintain the effectiveness of PRIMAXIN I.V. and other antibacterial drugs, PRIMAXIN I.V. should be used only to treat or prevent infections that are proven or strongly suspected to be caused by susceptible bacteria. When culture and susceptibility information are available, they should be considered in selecting or modifying antibacterial therapy. In the absence of such data, local epidemiology and susceptibility patterns may contribute to the empiric selection of therapy.

Selected Important Safety Information
PRIMAXIN I.V. is contraindicated in patients who have shown hypersensitivity to any component of this product.

SERIOUS AND OCCASIONALLY FATAL HYPERSENSITIVITY (ANAPHYLACTIC) REACTIONS HAVE BEEN REPORTED IN PATIENTS RECEIVING THERAPY WITH BETA-LACTAMS. THESE REACTIONS ARE MORE LIKELY TO OCCUR IN PERSONS WITH A HISTORY OF SENSITIVITY TO MULTIPLE ALLERGENS.

BEFORE INITIATING THERAPY WITH PRIMAXIN I.V., CAREFUL INQUIRY SHOULD BE MADE CONCERNING PREVIOUS HYPERSENSITIVITY REACTIONS TO PENICILLINS, CEPHALOSPORINS, OTHER BETA-LACTAMS, AND OTHER ALLERGENS. IF AN ALLERGIC REACTION TO PRIMAXIN I.V. OCCURS, DISCONTINUE THE DRUG. SEIZURES AND OTHER CNS ADVERSE EVENTS HAVE BEEN REPORTED DURING TREATMENT WITH PRIMAXIN I.V.

Co-administration of carbapenems, including PRIMAXIN I.V., to patients receiving valproic acid or divalproex sodium results in a reduction of valproic acid concentrations, which may drop below the therapeutic range and increase the risk of breakthrough seizures. Increasing the dose of valproic acid or divalproex sodium may not be sufficient. Concomitant use of PRIMAXIN I.V. and valproic acid/divalproex sodium is generally not recommended. Consider other anti-bacterials in patients whose seizures are well controlled on valproic acid or divalproex sodium. If PRIMAXIN I.V. is necessary, consider supplemental anticonvulsant therapy.

Clostridium difficile-associated diarrhea (CDAD) has been reported with use of nearly all antibacterial agents, including PRIMAXIN I.V., and may range in severity from mild diarrhea to fatal colitis. CDAD must be considered in all patients who present with diarrhea following antibiotic use. CDAD has been reported to occur over 2 months after administration of antibacterial agents. If CDAD is suspected or confirmed, ongoing antibiotic use not directed against C difficile may need to be discontinued.

Central nervous system (CNS) adverse experiences such as confusional states, myoclonic activity, and seizures have been reported during treatment with PRIMAXIN I.V., especially when recommended dosages were exceeded. These experiences have occurred most commonly in patients with CNS disorders (eg, brain lesions or history of seizures) and/or compromised renal function. However, there have been reports of CNS adverse experiences in patients who had no recognized or documented underlying CNS disorder or compromised renal function.

The most frequently reported systemic adverse clinical reactions that were reported as possibly, probably, or definitely related to PRIMAXIN I.V. were nausea (2.0%), diarrhea (1.8%), vomiting (1.5%), rash (0.9%), fever (0.5%), hypotension (0.4%), seizures (0.4%), dizziness (0.3%), pruritus (0.3%), urticaria (0.2%), and somnolence (0.2%).

Prescribing PRIMAXIN I.V. in the absence of a proven or strongly suspected bacterial infection or a prophylactic indication is unlikely to provide benefit to the patient and increases the risk of the development of drug-resistant bacteria.