氨苄西林钠舒巴坦钠 Ampicillin Sodium and Sulbactam Sodium
【分类】抗生素/β-内酰胺类/β-内酰胺酶抑制剂
【别名】舒他西林、优力新、舒氨新、优立新、舒氨西林、氨苄西林-舒巴坦
【外文名】AmpicillinandSulbactam,Sultamicillin,Unasyn
【药理作用及用途】是氨苄西林与舒巴坦的混合物,重量(效价)比为2:1,片剂为1:1.舒巴坦为β-内酰胺酶抑制剂,对耐药菌产生的β-内酰胺酶有广谱抑酶作用,从而保护了氨苄西林不被酶灭活,而发挥其杀菌作用。本品可用于一般产酶耐药的革兰阴性需氧细菌引起的感染,对高度耐药的肠杆菌属引起的感染、绿脓杆菌感染与MRSA感染无效。用于由敏感细菌引起的感染如鼻窦炎、中耳炎、呼吸道感染、细菌性肺炎、尿道感染、肾盂肾炎、腹膜炎、胆囊炎、子宫内膜炎、盆腔蜂窝组织炎、细菌性败血症、脑膜炎、皮肤和软组织感染、骨和关节感染等。
【用法及用量】临用前加适量灭菌注射用水或生理盐水使其溶解。肌内注射,每日2~4g,分4次;静脉注射,每天4~12g,分2~4次;新生儿与婴幼儿用量为每天150mg/kg,6~8小时一次;口服,每次375mg,每日2~4次,饭前1小时或饭后2小时服用。
【不良反应】①可发生氨苄西林的各种不良反应;②舒巴坦每次剂量不得超过lg,每日剂量不得超过4g,静脉滴注未见与氨苄西林静脉滴注不同的反应;③肌内注射局部有疼痛反应。③偶见消化道反应。④常见有皮疹、瘙痒及其他皮肤反应。
【注意事项】①本联合制剂与青霉素有交叉过敏反应,应询问青霉素过敏史,青霉素过敏者禁用;②使用前应做皮肤过敏试验。③新生儿特别是早产儿慎用。
Ampicillin Sodium / Sulbactam Sodium
Pronunciation: (am-pih-SILL-in SO-dee-uhm/sull-BAK-tam SO-dee-uhm) Class: Aminopenicillin
Pharmacology Ampicillin inhibits bacterial cell wall mucopeptide synthesis. Sulbactam inhibits plasmid-medicated beta-lactamase enzymes commonly found in microorganisms resistant to ampicillin.
Indications and Usage Treatment of infections of skin and skin structure, intra-abdominal and gynecologic infections caused by susceptible microorganisms, and mixed infections caused by ampicillin-susceptible organisms and beta-lactamase–producing organisms.
Contraindications Hypersensitivity to penicillins, cephalosporins, or imipenem.
Dosage and Administration Adults IV/IM 1.5 to 3 g every 6 h, not to exceed 4 g/day sulbactam (1.5 g of product contains 0.5 g sulbactam).
Children 1 yr of age or older (less than 40 kg) IV 300 mg/kg/day (200 mg ampicillin/100 mg sulbactam) in divided doses every 6 h.
Children at least 40 kg IV Dose according to adult recommended doses; do not exceed total sulbactam dose of 4 g/day.
Storage/Stability Keep refrigerated after reconstitution. Medication is stable for 2 h at room temperature, 72 h if refrigerated. Store at or below 86°F prior to reconstitution
Drug Interactions Allopurinol Increases potential for ampicillin-induced skin rash.
Contraceptives, oral May reduce efficacy of oral contraceptives.
Tetracyclines May impair bactericidal effects of ampicillin/sulbactam.
Incompatibility Do not mix with aminoglycosides (eg, gentamicin).
Laboratory Test Interactions May cause false-positive urine glucose test results with Benedict solution, Fehling solution, or Clinitest tablets (enzyme-based tests; eg, Clinistix , Tes-tape , are recommended); false-positive direct Coombs test result in certain patient groups; false-positive protein reactions with sulfosalicylic acid and boiling test, acetic acid test, biuret reaction and nitric acid test (the bromphenol blue test, Multistix , is recommended).
Adverse Reactions Cardiovascular Thrombophlebitis at injection site.
CNS Dizziness; fatigue; insomnia; reversible hyperactivity.
Dermatologic Urticaria; maculopapular to exfoliative dermatitis; vesicular eruptions; erythema multiforme; skin rashes.
EENT Itchy eyes; laryngospasm; laryngeal edema.
GI Diarrhea; pseudomembranous colitis.
Genitourinary Interstitial nephritis (eg, oliguria, proteinuria, hematuria, hyaline casts, pyuria); nephropathy; increased BUN and creatinine; vaginitis.
Hematologic Decreased Hgb, Hct, RBC, WBC, neutrophils, lymphocytes, platelets; increased lymphocytes, monocytes, basophils, eosinophils, and platelets.
Metabolic Elevated serum alkaline phosphatase, glutamic oxaloacetic transaminase, ALT, AST, and LDH; reduced serum albumin and total proteins.
Miscellaneous Pain at injection site; hyperthermia
Precautions Pregnancy Category B .
Lactation Excreted in breast milk.
Children Safety and efficacy not established.
Hypersensitivity Reactions range from mild to life-threatening. Use cautiously in cephalosporin-sensitive patients because of possible cross-allergenicity.
Renal Function Use cautiously with altered dosing interval.
Superinfection May result in overgrowth of nonsusceptible bacterial or fungal organisms.
Overdosage Symptoms Hyperexcitability, convulsive seizures.
Patient Information Explain rationale for hospitalization during course of therapy. Inform patient of potential adverse reactions, and encourage a report of any problems. Encourage patient to increase fluid intake to 2,000 to 3,000 mL/day, unless contraindicated. Inform diabetic patients that this medication may cause false-positive glucose urine test results, and identify types that will be more reliable. If therapy is changed because of allergic reaction, explain significance of penicillin allergy, and inform of potential sensitivity to cephalosporins |