英文药名：UNASYN-S KIT for Intravenous Use(Sulbactam Sodium/Ampicillin Sodium)

中文药名： 舒巴坦钠/氨苄西林钠注射剂

生产厂家：辉瑞日本公司

ユナシン-Sキット静注用1.5g／ユナシン-Sキット静注用3g

治疗类别名称
β-内酰胺酶抑制剂制定抗生素制剂
商標名
UNASYN-S KIT for Intravenous Use
一般名
スルバクタムナトリウム（Sulbactam Sodium）
略号
SBT
化学名
Monosodium(2S,5R)-3,3-dimethyl-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylate 4,4-dioxide
分子式
C8H10NNaO5S
分子量
255.22
構造式

滴度
舒巴坦钠的滴度，表示为舒巴坦（C8H11NO5S）的质量（效价）的数量。
性状
舒巴坦钠为白色至淡黄色结晶性粉末。它易溶于水，稍少溶于甲醇，极微溶于乙醇（99.5），并在乙腈中几乎不溶。
一般名
アンピシリンナトリウム（Ampicillin Sodium）
略号
ABPC
化学名
Monosodium(2S,5R,6R)-6-[(2R)-2-amino-2-phenylacetylamino]-3,3-dimethyl-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylate
分子式
C16H18N3NaO4S
分子量
371.39
構造式

性状
滴度
氨苄青霉素钠的滴度，表示氨苄青霉素（C16H19N3O4S）的质量（效价）的数量。
氨苄西林钠为白色结晶或结晶性粉末，以淡黄白色。这是非常易溶于水，稍少溶于乙醇（99.5）。
操作注意事项
1.为了保持产品的质量，外面包包围此产品不能打开，直到使用。
2.不要在下列情况下使用。
（1）
当和解决方案时，外袋破损泄漏。
（2）当药物隔壁的开口之前溶解。
（3）在溶液或当药物变色着色。
3.容器液体规模被用作粗略指导。
药效药理
1. 抗菌作用
(1) 本剤药物，葡萄球菌，大肠杆菌，变形杆菌，对于β-内酰胺酶产生的氨苄青霉素抗性菌和肺炎球菌流感嗜血杆菌，呈现出强大的抗菌活性）。
(2) 本剤药物，β-内酰胺酶先进的生产葡萄球菌，大肠杆菌，或由变形杆菌属，18一个单一的鼠标感染模型显示比氨苄西林强大的治疗效果）。此外，显示了较强的利治疗效果β-内酰胺酶先进的生产氨苄西林耐药流感嗜血杆菌和氨苄西林敏感肺炎小鼠混合感染模型氨苄青霉素
2. 作用机序
本剤药，舒巴坦IC是β-内酰胺酶，II，III强和IV型，不可逆转地灭活轻轻的IA和V型），氨苄西林由这些酶水解为了防止，它显示了抗菌活性也氨苄西林耐药菌。氨苄青霉素与细胞壁合成可能干扰强烈细菌抑制肽聚糖的交联，动作杀菌。
适应病症
<适应物种>
金黄色葡萄球菌敏感性这种药物，大肠杆菌，变形杆菌，流感嗜血杆菌
<主治>
肺炎，肺脓肿，膀胱炎，腹膜炎
用法与用量
[肺炎，肺脓肿，腹膜炎的情况下]
像往常一样舒巴坦钠，氨苄西林钠为成人，每日分6克（效价）两次，溶解在使用时连接解决方案，并注入静脉注射。顺便提及，可适当增加，根据需要在严重感染的情况下，一个3克（效价）（12克（效价作为每日剂量））每天四次是上限。
[如果膀胱炎]
像往常一样舒巴坦钠，氨苄西林钠为成人，每日分3G（效价）两次，溶解在使用时连接解决方案，并注入静脉注射。
如在儿童正常舒巴坦钠氨苄西林钠，是每人每天60〜150毫克（效价）/ kg的三到四倍的时间分割，溶解在使用的附溶液中，滴注入静脉。
（溶解操作方法）
见原处方
包装规格
UNASYN-S 套件 静脉 1.5克：10包
UNASYN-S 套件 静脉 3G：    10包

生产和销售
辉瑞日本公司
提示：以上中文处方资料不够完整，使用者以原处方资金料为准。
完整说明书附件：http://www.info.pmda.go.jp/go/pack/6139504G1028_2_06/.
Unasyn (Ampicillin Sodium / Sulbactam Sodium)
INDICATIONS AND USAGE
UNASYN is indicated for the treatment of infections due to susceptible strains of the designated microorganisms in the conditions listed below.
Skin and Skin Structure Infections caused by beta-lactamase producing strains of Staphylococcus aureus, Escherichia coli, [ Efficacy for this organism in this organ system was studied in fewer than 10 infections.] Klebsiella spp. (including K. pneumoniae ), Proteus mirabilis, Bacteroides fragilis,  Enterobacter spp., and Acinetobacter calcoaceticus.
NOTE: For information on use in pediatric patients see PRECAUTIONS–Pediatric Use and CLINICAL STUDIES sections.
Intra-Abdominal Infections caused by beta-lactamase producing strains of Escherichia coli, Klebsiella spp. (including K. pneumoniae ), Bacteroides spp. (including B. fragilis), and Enterobacter spp.
Gynecological Infections caused by beta-lactamase producing strains of Escherichia coli, and Bacteroides spp. (including B. fragilis ).
While UNASYN is indicated only for the conditions listed above, infections caused by ampicillin-susceptible organisms are also amenable to treatment with UNASYN due to its ampicillin content. Therefore, mixed infections caused by ampicillin-susceptible organisms and beta-lactamase producing organisms susceptible to UNASYN should not require the addition of another antibiotic.
Appropriate culture and susceptibility tests should be performed before treatment in order to isolate and identify the organisms causing infection and to determine their susceptibility to UNASYN.
Therapy may be instituted prior to obtaining the results from bacteriological and susceptibility studies when there is reason to believe the infection may involve any of the beta-lactamase producing organisms listed above in the indicated organ systems. Once the results are known, therapy should be adjusted if appropriate.
To reduce the development of drug-resistant bacteria and maintain effectiveness of UNASYN and other antibacterial drugs, UNASYN 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.
DOSAGE AND ADMINISTRATION
UNASYN may be administered by either the IV or the IM routes (following dilution). However, the intent of the pharmacy bulk package is for preparation of solutions for IV infusion only.
For IV administration, the dose can be given by slow intravenous injection over at least 10–15 minutes or can also be delivered in greater dilutions with 50–100 mL of a compatible diluent as an intravenous infusion over 15–30 minutes.
UNASYN may be administered by deep intramuscular injection. (see DIRECTIONS FOR USE-Preparation for Intramuscular Injection section).
The recommended adult dosage of UNASYN is 1.5 g (1 g ampicillin as the sodium salt plus 0.5 g sulbactam as the sodium salt) to 3 g (2 g ampicillin as the sodium salt plus 1 g sulbactam as the sodium salt) every six hours. This 1.5 to 3 g range represents the total of ampicillin content plus the sulbactam content of UNASYN, and corresponds to a range of 1 g ampicillin/0.5 g sulbactam to 2 g ampicillin/1 g sulbactam. The total dose of sulbactam should not exceed 4 grams per day.
Pediatric Patients 1 Year of Age or Older
The recommended daily dose of UNASYN in pediatric patients is 300 mg per kg of body weight administered via intravenous infusion in equally divided doses every 6 hours. This 300 mg/kg/day dosage represents the total ampicillin content plus the sulbactam content of UNASYN, and corresponds to 200 mg ampicillin/100 mg sulbactam per kg per day. The safety and efficacy of UNASYN administered via intramuscular injection in pediatric patients have not been established. Pediatric patients weighing 40 kg or more should be dosed according to adult recommendations, and the total dose of sulbactam should not exceed 4 grams per day. The course of intravenous therapy should not routinely exceed 14 days. In clinical trials, most children received a course of oral antimicrobials following initial treatment with intravenous UNASYN. (see CLINICAL STUDIES section).
Impaired Renal Function
In patients with impairment of renal function the elimination kinetics of ampicillin and sulbactam are similarly affected, hence the ratio of one to the other will remain constant whatever the renal function. The dose of UNASYN in such patients should be administered less frequently in accordance with the usual practice for ampicillin and according to the following recommendations:
TABLE 5 UNASYN Dosage Guide for Patients with Renal Impairment
When only serum creatinine is available, the following formula (based on sex, weight, and age of the patient) may be used to convert this value into creatinine clearance. The serum creatinine should represent a steady state of renal function.

     Males         weight (kg) × 140 – age)
                         72 × serum creatinine

     Females     0.85 × above value
COMPATIBILITY, RECONSTITUTION AND STABILITY
When concomitant therapy with aminoglycosides is indicated, UNASYN and aminoglycosides should be reconstituted and administered separately, due to the in vitro inactivation of aminoglycosides by any of the aminopenicillins.
DIRECTIONS FOR USE
General Dissolution Procedures
UNASYN sterile powder for intravenous and intramuscular use may be reconstituted with any of the compatible diluents described in this insert. Solutions should be allowed to stand after dissolution to allow any foaming to dissipate in order to permit visual inspection for complete solubilization.
Preparation for Intravenous Use
UNASYN concentrations between 3 and 45 mg (2 to 30 mg ampicillin/1 to 15 mg sulbactam/mL) are recommended for intravenous use.
Directions For Proper Use of Pharmacy Bulk Package
The 15 gram vial may be reconstituted with either 92 mL Sterile Water for Injection or 0.9% Sodium Chloride Injection. The diluent should be added in two separate aliquots in a suitable work area, such as a laminar flow hood. Add 50 mL of solution, shake to dissolve. Then add an additional 42 mL and shake. The solution should be allowed to stand after dissolution to allow any foaming to dissipate in order to permit visual inspection for complete solubilization. The resultant solution will have a final concentration of approximately 100 mg/mL ampicillin and 50 mg/mL sulbactam. The closure may be penetrated only one time after reconstitution, if needed, using a suitable sterile transfer device or dispensing set that allows for measured dispensing of the contents.
After reconstitution, use within two hours if stored at room temperature, or within four hours if stored under refrigeration.
Reconstituted Bulk Solution Should Not be Used For Direct Infusion
If the reconstituted bulk solution is stored for less than one hour at room temperature (20°C/68°F) prior to further dilution, the use periods indicated in Table 6 apply for the diluted solutions.
If the bulk solution is stored for one to two hours at room temperature (20°C/68°F) and then diluted with Sterile Water for Injection or 0.9% Sodium Chloride Injection to the following concentrations, the use periods indicated in Table 7 apply.
Any unused portions of solution that remain after the indicated time periods should be discarded.
http://www.info.pmda.go.jp/go/pack/6139504G1028_2_05/