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苯唑西林钠（OXACILLIN SODIUM）

2012-11-17 11:57:01 作者：新特药房来源：互联网浏览次数：240 文字大小：【大】【中】【小】

简介： 部分中文苯唑西林钠处方资料（仅供参考）中文品名：苯唑西林钠通用药名：Oxacillin Sodium 别名：Prostaphlin, Bactocill, P 12 CA名称：4-Thia-1-azabicyclo[3.2.0]heptane-2-carboxylic acid, ...

关键字：苯唑西林钠

部分中文苯唑西林钠处方资料（仅供参考）

中文品名：苯唑西林钠

通用药名：Oxacillin Sodium

别名：Prostaphlin, Bactocill, P 12

CA名称：4-Thia-1-azabicyclo[3.2.0]heptane-2-carboxylic acid, 3,3-dimethyl-6-[[(5-methyl-3-phenyl-4-isoxazolyl]carbonyl]amino]-7-oxo-, monosodium salt, (2S,5R,6R)-
苯唑西林;新青霉素Ⅱ;苯唑青霉素;苯唑西林钠;苯唑青霉素钠;苯甲异唑青霉素;苯唑西林/苯唑青霉素;(2S,5R,6R)-3,3-二甲基-6-[(5-甲基-3-苯基-1,2-恶唑-4-甲酰)氨基]-7-氧代-4-硫杂-1-氮杂双环[3.2.0]庚烷-2-羧酸钠盐

药理及应用
本品为半合成、耐青霉素酶、耐酸青霉素，可口服与注射给药。作用机制同青霉素，但对青霉素敏感阳性球菌的抗菌作用不如青霉素，比青霉素差10倍,本品不为金黄色葡萄球菌产生的青霉素酶所破坏，对产酶金黄色葡萄球菌有效，对不产酶菌株的抗菌作用不如青霉素G。用于耐青霉素G的金黄色葡萄球菌和表皮葡萄球菌的周围感染，对中枢感染一般不适用。主要用于耐青霉素葡萄球菌所致的各种感染，如败血症、心内膜炎、烧伤、骨髓炎、呼吸道感染、脑膜炎、软组织感染等，也可用于化脓性链球菌或肺炎球菌与耐青霉素葡萄球菌所致的混合感染[2]。

药理药动
药效学
参阅青霉素。苯唑西林为耐青霉素酶青霉素，其抗菌作用方式与青霉素相仿。本品对革兰阳性菌和奈瑟菌属有抗菌活性，对耐青霉素金葡菌的最低抑菌浓度为0.4μg/ml，但对青霉素敏感葡萄球菌和各种链球菌的抗菌作用则较青霉素为弱。
药动学
肌内注射苯唑西林 0.5g，半小时血药浓度达峰值，为16.7μg/ml。剂量加倍，血药浓度亦倍增。本品耐酸稳定，口服后吸收良好，30～33％可在肠道吸收；空腹口服本品1g，血药峰浓度于0.5～l小时到达，为11.7μg/ml。食物可影响本品在胃肠道的吸收。3小时内静脉滴注苯唑西林钠 250mg，滴注结束时的平均血浆浓度为9.7μg/ml，2小时后0.16μg/ml。新生儿肌注本品20mg/kg后，8～15天和20～21天新生儿血药峰浓度(平均)分别为51.5和47.0μg/ml。　　
苯唑西林在肝、肾、肠、脾、胸腔积液和关节腔液均可达有效治疗浓度，腹水中浓度低，痰中的浓度为 0.3～14.5μg/g(平均为2.1μg/g)。本品难以透过正常血脑屏障。蛋白结合率很高，约93％。正常健康人Ｔ1/2为 0.5～0.7小时；8～15天和 20～21天新生儿的Ｔ1/2分别为 1.6和1.2天。本品约 49％(500mg)由肝脏代谢，通过肾小球滤过和肾小管分泌，自肾脏排出体外。肌内注射和口服给药在尿中排出量分别为 40％和 23～30％，10～23％尿中排出的药物为代谢产物。　　
囊肿性纤维化病人的肾小管分泌功能增强，其清除双氯西林的速率较正常人快 3倍，因此其血药浓度相当低。以苯唑西林等异恶唑组青霉素治疗此种病人时，剂量应加大，而且需监测血药浓度。　　
苯唑西林可经胆汁排泄，苯唑西林的胆汁排泄量较其他异恶唑组青霉素者为多。血液透析和腹膜透析皆不能消除苯唑西林。

用量用法
1.静脉滴注：每次１－２g,溶于100ml输液中滴注0.5-1h,每日3-4次。小儿按体重每日50-100mg/kg,分次给予。肌注：每次1g,每日3-4次。　　
2.肌内注射或静脉滴注。成人每次0.5～1.0g，每4～6小时一次，病情严重者剂量可增加。小儿体重在40kg以下者，每6小时按体重12.5～25mg/kg，体重超过40kg者给以成人剂量。

不良反应
①过敏反应:与青霉素G有交叉过敏反应；
②肝毒性:转氨酶升高或引起非特异性肝炎；
③大剂量静脉给药可引起惊厥；
④血液学异常:如中性白细胞下降。　　
更多信息参阅青霉素钠。青霉素引起的各种过敏反应皆可发生于苯唑西林。　　
静脉注射苯唑西林偶可产生发热、恶心、呕吐和血清转氨酶升高，肝活检显示非特异性肝炎；停药后症状消失，可能属过敏反应。静脉注射大剂量苯唑西林(每日达 18g)可引起抽搐等神经毒性反应，此反应尤易见于肾功能减退病人。偶见有中性粒细胞减少症或粒细胞缺乏症，急性间质性肾炎伴肾功能衰竭也有报告，婴儿应用大剂量苯唑青霉素后有发生血尿、蛋白尿和尿毒症者。　　
苯唑西林毒性极微，临床应用发生反应者较少。口服给药时约15％病人出现胃肠道反应，以轻度中上腹不适、腹胀、食欲减退等为多见。个别病人也可出现恶心、呕吐、腹痛、腹泻等。有时可出现中性细胞减少，但多伴有白细胞减少。有的病人出现肌肉紧张、抽搐、神志不清、头痛、心悸、血清ALT升高、药疹、药热，偶可发生白色念珠菌继发感染，一般较轻，不致影响治疗，对特异质者，可致出血倾向，个别人氨基转移酶升高。肌内注射后，少数病人主诉局部疼痛，且有出现局部硬结者。静脉给药如用量大于10.g／日，最好分两次静滴，浓度不宜过高，速度宜慢。偶见肝炎及胆汁郁滞之病例。大剂量可有神经系统反应，如神志不清，抽搐，惊厥。

注意事项
1.本品可致过敏性休克，用药前应作过敏试验。　　
2.可出现药疹、药物热、胃肠道反应等。　　
3.对婴儿大量投用可致血尿、蛋白尿甚至尿毒症。　　　　
禁用慎用：对青霉素过敏者禁用。肝病患者及新生儿慎用。

处方须知
①连续大剂量静脉滴注可出现痉挛、神志不清、头痛甚至惊厥等神经系统反应。　　
②特异质患者可致出血倾向。　　
③溶解后冷藏不宜超过24h。

适应症
主要用于耐青霉素葡萄球菌所致的各种感染，如败血症、呼吸道感染、脑膜炎、软组织感染等，也可用于化脓性链球菌或肺炎球菌与耐青霉素葡萄球菌所致的混合感染。

药物相互作用
参阅青霉素钠。在静脉注射液中苯唑西林与庆大霉素、士霉素、四环素、新生霉素、多粘菌素 B、磺胺嘧啶、呋喃妥因、去甲肾上腺素、间羟胺、苯巴比妥、戊巴比妥、水解蛋白、维生素B族、维生素C、琥珀胆碱等呈配伍禁忌。　　
苯唑西林在 5％葡萄糖氯化钠注射液中放置 12小时后，其效价减少 12％；当本品加入 5％葡萄糖注射液或氯化钠注射液中，同时有磷酸盐缓冲液存在，则在 21～25℃放置24小时效价无变化。　　
阿司匹林、磺胺药在体内外皆可抑制苯唑西林对血清蛋白的结合，磺胺药可减少苯唑西林在胃肠道的吸收。丙磺舒可延长和增高本品的血药浓度。二盐酸奎宁在体外减弱苯唑西林对金葡菌的抗菌活性；苯唑西林与西索米星或奈替米星联合应用可增强苯唑西林对金葡菌的抗菌作用。氨苄西林或庆大霉素与苯唑西林联合后可互相增强对肠球菌的作用。苯唑西林与其他β-内酰胺类抗生素一样，与氨基糖苷类混合后，两者的抗菌活性明显减弱，因此不能在同一容器内给药。

OXACILLIN injection, powder, for solution
[Sandoz Inc]
To reduce the development of drug-resistant bacteria and maintain the effectiveness of Oxacillin for Injection and other antibacterial drugs, Oxacillin for Injection should be used only to treat or prevent infections that are proven or strongly suspected to be caused by bacteria.
DESCRIPTION
Oxacillin for Injection, USP is a semisynthetic antibiotic substance derived from 6-amino-penicillanic acid. It is the sodium salt in a parenteral dosage form. The pharmacy bulk package contains oxacillin sodium monohydrate equivalent to 10 grams oxacillin. It also contains approximately 2.5 mEq of sodium and 20 mg dibasic sodium phosphate (as a buffer) per gram of oxacillin.

4-Thia-1-azabicyclo [3.2.0]heptane-2-carboxylic acid, 3,3-dimethyl-6-[[(5-methyl-3-phenyl-4-isoxazolyl) carbonyl] amino]-7-oxo-,monosodium salt, monohydrate, [2S(2α,5α,6β)].

A pharmacy bulk package bottle is a container of a sterile preparation for intravenous use that contains many single doses. The contents of this pharmacy bulk package bottle are intended for use by a pharmacy admixture service for addition to suitable parenteral fluids in the preparation of admixtures for intravenous infusion. (See DOSAGE AND ADMINISTRATION: Directions For Proper Use of Pharmacy Bulk Package).

FURTHER DILUTION IS REQUIRED. NOT FOR DIRECT INFUSION.

CLINICAL PHARMACOLOGY

Intravenous administration provides peak serum levels approximately 5 minutes after the injection is completed. Slow I.V. administration of 500 mg gives a peak serum level of 43 µg/mL after 5 minutes with a half-life of 20-30 minutes.

The penicillinase-resistant penicillins bind to serum protein, mainly albumin. The degree of protein binding reported for oxacillin is 94.2% ± 2.1%. Reported values vary with the method of study and the investigator.

The penicillinase-resistant penicillins vary in the extent to which they are distributed in the body fluids. With normal doses, insignificant concentrations are found in the cerebrospinal fluid and aqueous humor. All the drugs in this class are found in therapeutic concentrations in the pleural, bile, and amniotic fluids.

The penicillinase-resistant penicillins are rapidly excreted primarily as unchanged drug in the urine by glomerular filtration and active tubular secretion. The elimination half-life for oxacillin is about 0.5 hours. Nonrenal elimination includes hepatic inactivation and excretion in bile.

Probenecid blocks the renal tubular secretion of penicillins. Therefore, the concurrent administration of probenecid prolongs the elimination of oxacillin and, consequently, increases the serum concentration.

Microbiology

Penicillinase-resistant penicillins exert a bactericidal action against penicillin-susceptible microorganisms during the state of active multiplication. All penicillins inhibit the biosynthesis of the bacterial cell wall.

The drugs in this class are highly resistant to inactivation by staphylococcal penicillinase and are active against penicillinase-producing and nonpenicillinase-producing strains of Staphylococcus aureus.

The penicillinase-resistant penicillins are active in vitro against a variety of other bacteria.

Susceptibility Plate Testing

Quantitative methods of susceptibility testing that require measurement of zone diameters or minimal inhibitory concentrations (MIC’s) give the most precise estimates of antibiotic susceptibility. One such procedure has been recommended for use with discs to test susceptibility to this class of drugs. Interpretations correlate diameters on the disc test with MIC values. A penicillinase-resistant class disc may be used to determine microbial susceptibility to cloxacillin, dicloxacillin, methicillin, nafcillin, and oxacillin. With this procedure, employing a 5 microgram methicillin sodium disc, a report from the laboratory of “susceptible” (zone of at least 14 mm) indicates that the infecting organism is likely to respond to therapy. A report of “resistant” (zone of less than 10 mm) indicates that the infecting organism is not likely to respond to therapy. A report of “intermediate susceptibility” (zone of 10 to 13 mm) suggests that the organism might be susceptible if high doses of the antibiotic are used, or if the infection is confined to tissues and fluids (e.g. urine), in which high antibiotic levels are attained.

In general, all staphylococci should be tested against the penicillin G disc and against the methicillin disc. Routine methods of antibiotic susceptibility testing may fail to detect strains of organisms resistant to the penicillinase-resistant penicillins. For this reason, the use of large inocula and 48-hour incubation periods may be necessary to obtain accurate susceptibility studies with these antibiotics. Bacterial strains which are resistant to one of the penicillinase-resistant penicillins should be considered resistant to all of the drugs in the class.

Pharmacokinetics

Oxacillin Sodium, with normal doses, has insignificant concentrations in the cerebrospinal and ascitic fluids. It is found in therapeutic concentrations in the pleural, bile, and amniotic fluids. Oxacillin Sodium is rapidly excreted as unchanged drug in the urine by glomerular filtration and active tubular secretion.

Oxacillin Sodium binds to serum protein, mainly albumin. The degree of protein binding reported varies with the method of study and the investigator, but generally has been found to be 94.2 ± 2.1%.

Intravenous injection gives a peak serum level about 5 minutes after the injection is completed. Slow IV dosing with 500 mg gives a 5 minute peak of 43 mcg/mL with a half-life of 20 to 30 minutes.

INDICATIONS AND USAGE

Oxacillin is indicated in the treatment of infections caused by penicillinase producing staphylococci which have demonstrated susceptibility to the drug. Cultures and susceptibility tests should be performed initially to determine the causative organism and its susceptibility to the drug. (See CLINICAL PHARMACOLOGY: Susceptibility Plate Testing).

Oxacillin may be used to initiate therapy in suspected cases of resistant staphylococcal infections prior to the availability of susceptibility test results. Oxacillin should not be used in infections caused by organisms susceptible to penicillin G. If the susceptibility tests indicate that the infection is due to an organism other than a resistant Staphylococcus, therapy should not be continued with oxacillin.

To reduce the development of drug-resistant bacteria and maintain the effectiveness of Oxacillin for Injection, USP and other antibacterial drugs, Oxacillin for Injection, USP 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.

CONTRAINDICATIONS

A history of a hypersensitivity (anaphylactic) reaction to any penicillin is a contraindication.

WARNINGS

SERIOUS AND OCCASIONALLY FATAL HYPERSENSITIVITY (ANAPHYLACTIC SHOCK WITH COLLAPSE) REACTIONS HAVE OCCURRED IN PATIENTS RECEIVING PENICILLIN. THE INCIDENCE OF ANAPHYLACTIC SHOCK IN ALL PENICILLIN-TREATED PATIENTS IS BETWEEN 0.015 AND 0.04 PERCENT. ANAPHYLACTIC SHOCK RESULTING IN DEATH HAS OCCURRED IN APPROXIMATELY 0.002 PERCENT OF THE PATIENTS TREATED. ALTHOUGH ANAPHYLAXIS IS MORE FREQUENT FOLLOWING PARENTERAL ADMINISTRATION, IT HAS OCCURRED IN PATIENTS RECEIVING ORAL PENICILLINS.

WHEN PENICILLIN THERAPY IS INDICATED, IT SHOULD BE INITIATED ONLY AFTER A COMPREHENSIVE PATIENT DRUG AND ALLERGY HISTORY HAS BEEN OBTAINED. IF AN ALLERGIC REACTION OCCURS, THE DRUG SHOULD BE DISCONTINUED AND THE PATIENT SHOULD RECEIVE SUPPORTIVE TREATMENT, E.G., ARTIFICIAL MAINTENANCE OF VENTILATION, PRESSOR AMINES, ANTIHISTAMINES, AND CORTICOSTEROIDS. INDIVIDUALS WITH A HISTORY OF PENICILLIN HYPERSENSITIVITY MAY ALSO EXPERIENCE ALLERGIC REACTIONS WHEN TREATED WITH A CEPHALOSPORIN.

Clostridium difficile associated diarrhea (CDAD) has been reported with use of nearly all antibacterial agents, including oxacillin for injection, and may range in severity from mild diarrhea to fatal colitis. Treatment with antibacterial agents alters the normal flora of the colon leading to overgrowth of C. difficile.

C. difficile produces toxins A and B which contribute to the development of CDAD. Hypertoxin producing strains of C. difficile cause increased morbidity and mortality, as these infections can be refractory to antimicrobial therapy and may require colectomy. CDAD must be considered in all patients who present with diarrhea following antibiotic use. Careful medical history is necessary since CDAD has been reported to occur over two months after the administration of antibacterial agents.

If CDAD is suspected or confirmed, ongoing antibiotic use not directed against C. difficile may need to be discontinued. Appropriate fluid and electrolyte management, protein supplementation, antibiotic treatment of C. difficile, and surgical evaluation should be instituted as clinically indicated.

PRECAUTIONS

General

Oxacillin should generally not be administered to patients with a history of sensitivity to any penicillin.

Penicillin should be used with caution in individuals with histories of significant allergies and/or asthma. Whenever allergic reactions occur, penicillin should be withdrawn unless, in the opinion of the physician, the condition being treated is life-threatening and amenable only to penicillin therapy.

The oral route of administration should not be relied upon in patients with severe illness, or with nausea, vomiting, gastric dilation, cardiospasm, or intestinal hypermotility. Occasionally patients will not absorb therapeutic amounts of orally administered penicillin.

The use of antibiotics may result in overgrowth of nonsusceptible organisms. If new infections due to bacteria or fungi occur, the drug should be discontinued and appropriate measures taken.

Prescribing Oxacillin for Injection 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

Information for Patients

Patients should be counseled that antibacterial drugs including Oxacillin for Injection should only be used to treat bacterial infections. They do not treat viral infections (e.g., the common cold). When Oxacillin for Injection is prescribed to treat a bacterial infection, patients should be told that although it is common to feel better early in the course of therapy, the medication should be taken exactly as directed. Skipping doses or not completing the full course of therapy may: (1) decrease the effectiveness of the immediate treatment, and (2) increase the likelihood that bacteria will develop resistance and will not be treatable by Oxacillin for Injection or other antibacterial drugs in the future.

Diarrhea is a common problem caused by antibiotics which usually ends when the antibiotic is discontinued. Sometimes after starting treatment with antibiotics, patients can develop watery and bloody stools (with or without stomach cramps and fever) even as late as two or more months after having taken the last dose of the antibiotic. If this occurs, patients should contact their physician as soon as possible.

Laboratory Tests

Bacteriologic studies to determine the causative organisms and their susceptibility to oxacillin should be performed (See CLINICAL PHARMACOLOGY: Microbiology). In the treatment of suspected staphylococcal infections, therapy should be changed to another active agent if culture tests fail to demonstrate the presence of staphylococci.

Periodic assessment of organ system function including renal, hepatic, and hematopoietic should be made during prolonged therapy with oxacillin.

Blood cultures, white blood cell, and differential cell counts should be obtained prior to initiation of therapy and at least weekly during therapy with oxacillin.

Periodic urinalysis, blood urea nitrogen, and creatinine determinations should be performed during therapy with oxacillin and dosage alterations should be considered if these values become elevated. If any impairment of renal function is suspected or known to exist, a reduction in the total dosage should be considered and blood levels monitored to avoid possible neurotoxic reactions.

AST (SGOT) and ALT (SGPT) values should be obtained periodically during therapy to monitor for possible liver function abnormalities.

Drug Interactions

Tetracycline, a bacteriostatic antibiotic, may antagonize the bactericidal effect of penicillin and concurrent use of these drugs should be avoided.

Oxacillin blood levels may be prolonged by concurrent administration of probenecid which blocks the renal tubular secretion of penicillins.

Carcinogenesis, Mutagenesis, Impairment of Fertility

No long-term animal studies have been conducted with these drugs.

Studies on reproduction (nafcillin) in rats and rabbits reveal no fetal or maternal abnormalities before conception and continuously through weaning (one generation).

Teratogenic Effects

Pregnancy Category B

Reproduction studies performed in the mouse, rat, and rabbit have revealed no evidence of impaired fertility or harm to the fetus due to the penicillinase-resistant penicillins. Human experience with the penicillins during pregnancy has not shown any positive evidence of adverse effects on the fetus. There are, however, no adequate or well-controlled studies in pregnant women showing conclusively that harmful effects of these drugs on the fetus can be excluded. Because animal reproduction studies are not always predictive of human response, this drug should be used during pregnancy only if clearly needed.

Nursing Mothers

Penicillins are excreted in breast milk. Caution should be exercised when penicillins are administered to a nursing woman.

Pediatric Use

Because of incompletely developed renal function in pediatric patients, oxacillin may not be completely excreted, with abnormally high blood levels resulting. Frequent blood levels are advisable in this group with dosage adjustments when necessary. All pediatric patients treated with penicillins should be monitored closely for clinical and laboratory evidence of toxic or adverse effects. Safety and effectiveness in pediatric patients have not been established.

Geriatric Use

Clinical studies of oxacillin did not include sufficient number of subjects aged 65 and over to determine whether they respond differently from younger subjects. Other reported clinical experience has not identified differences in responses between the elderly and younger patients. In general, dose selection for an elderly patient should be cautious, usually starting at the low end of the dosing range, reflecting the greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant disease or other drug therapy.

This drug is known to be substantially excreted by the kidney, and the risk of toxic reactions to this drug may be greater in patients with impaired renal function. Because elderly patients are more likely to have decreased renal function, care should be taken in dose selection, and it may be useful to monitor renal function.

Oxacillin for Injection contains 57 mg (2.5 mEq) of sodium per gram. At the usual recommended doses, patients would receive between 57 and 342 mg/day (2.5 and 15 mEq) of sodium. The geriatric population may respond with a blunted natriuresis to salt loading. This may be clinically important with regard to such diseases as congestive heart failure.

ADVERSE REACTIONS

Body as a Whole

The reported incidence of allergic reactions to penicillin ranges from 0.7 to 10 percent (See WARNINGS). Sensitization is usually the result of treatment but some individuals have had immediate reactions to penicillin when first treated. In such cases, it is thought that the patients may have had prior exposure to the drug via trace amounts present in milk and vaccines.

Two types of allergic reactions to penicillin are noted clinically, immediate and delayed.

Immediate reactions usually occur within 20 minutes of administration and range in severity from urticaria and pruritus to angioneurotic edema, laryngospasm, bronchospasm, hypotension, vascular collapse, and death.

Such immediate anaphylactic reactions are very rare (See WARNINGS) and usually occur after parenteral therapy but have occurred in patients receiving oral therapy. Another type of immediate reaction, an accelerated reaction, may occur between 20 minutes and 48 hours after administration and may include urticaria, pruritus, and fever. Although laryngeal edema, laryngospasm, and hypotension occasionally occur, fatality is uncommon.

Delayed allergic reactions to penicillin therapy usually occur after 48 hours and sometimes as late as 2 to 4 weeks after initiation of therapy. Manifestations of this type of reaction include serum sickness-like symptoms (i.e., fever, malaise, urticaria, myalgia, arthralgia, abdominal pain) and various skin rashes. Nausea, vomiting, diarrhea, stomatitis, black or hairy tongue, and other symptoms of gastrointestinal irritation may occur, especially during oral penicillin therapy.

Nervous System Reactions

Neurotoxic reactions similar to those observed with penicillin G may occur with large intravenous doses of oxacillin especially in patients with renal insufficiency.

Urogenital Reactions

Renal tubular damage and interstitial nephritis have been associated infrequently with the administration of oxacillin. Manifestations of this reaction may include rash, fever, eosinophilia, hematuria, proteinuria, and renal insufficiency.

Gastrointestinal Reactions

Pseudomembranous colitis has been reported with the use of oxacillin. The onset of pseudomembranous colitis symptoms may occur during or after antibiotic treatment (see WARNINGS).

Metabolic Reactions

Agranulocytosis, neutropenia, and bone marrow depression have been associated with the use of methicillin sodium, nafcillin, oxacillin, and cloxacillin. Hepatotoxicity, characterized by fever, nausea, and vomiting associated with abnormal liver function tests, mainly elevated SGOT levels, has been associated with the use of oxacillin and cloxacillin.

To report SUSPECTED ADVERSE EVENTS, contact FDA at 1-800-FDA-1088 or www.fda.gov.

OVERDOSAGE

The signs and symptoms of oxacillin overdosage are those described in the ADVERSE REACTIONS section. If signs or symptoms occur, discontinue use of the medication, treat symptomatically, and institute appropriate supportive measures.

DOSAGE AND ADMINISTRATION

The intent of the pharmacy bulk package for this product is for preparation of solutions for IV infusion only.

The penicillinase-resistant penicillins are available for oral administration and for intramuscular and intravenous injection. The sodium salts of methicillin, oxacillin, and nafcillin may be administered parenterally and the sodium salts of cloxacillin, dicloxacillin, oxacillin, and nafcillin are available for oral use.

Bacteriologic studies to determine the causative organisms and their susceptibility to oxacillin should always be performed. Duration of therapy varies with the type and severity of infection as well as the overall condition of the patient, therefore it should be determined by the clinical and bacteriological response of the patient. In severe staphylococcal infections, therapy with oxacillin should be continued for at least 14 days. Therapy should be continued for at least 48 hours after the patient has become afebrile, asymptomatic, and cultures are negative. The treatment of endocarditis and osteomyelitis may require a longer term of therapy.

Concurrent administration of oxacillin and probenecid increases and prolongs serum penicillin levels. Probenecid decreases the apparent volume of distribution and slows the rate of excretion by competitively inhibiting renal tubular secretion of penicillin. Penicillin-probenecid therapy is generally limited to those infections where very high serum levels of penicillin are necessary.

Oral preparations of the penicillinase-resistant penicillins should not be used as initial therapy in serious, life-threatening infections (See PRECAUTIONS: General). Oral therapy with the penicillinase-resistant penicillins may be used to follow-up the previous use of a parenteral agent as soon as the clinical condition warrants. With intravenous administration, particularly in elderly patients, care should be taken because of the possibility of thrombophlebitis.

RECOMMENDED DOSAGES FOR OXACILLIN FOR INJECTION, USP
Drug	Adults	Infants and Children <40 kg (88 lbs)	Other Recommendations
Oxacillin	250 to 500 mg IV every 4 to 6 hours (mild to moderate infections)	50 mg/kg/day IV in equally divided doses every 6 hours (mild to moderate infections)
Oxacillin	1 gram IV every 4 to 6 hours (severe infections)	100 mg/kg/day IV in equally divided doses every 4 to 6 hours (severe infections)	Premature and Neonates 25 mg/kg/day IV

Directions for use

For Administration by Intravenous Drip

Reconstitute as directed below (Pharmacy Bulk Package) prior to further dilution.

STABILITY PERIODS FOR OXACILLIN FOR INJECTION, USP*
* IMPORTANT: This chemical stability information in no way indicates that it would be acceptable practice to use this product well after the preparation time. Good professional practice suggests that a product should be used as soon after preparation as feasible.
Concentration mg/mL	Sterile Water for Injection, USP	0.9% Sodium Chloride Injection, USP	Sodium Lactate Injection, USP (M/6 Sodium Lactate)	5% Dextrose Injection, USP	5% Dextrose and 0.45% Sodium Chloride Injection, USP	10% Invert Sugar Injection, USP	Lactated Ringers Injection, USP
ROOM TEMPERATURE (25°C)
10-100	4 Days	4 Days
10-30			24 Hrs		24 Hrs
0.5-2				6 Hrs		6 Hrs	6 Hrs
REFRIGERATION (4°C)
10-100	7 Days	7 Days
10-30			4 Days	4 Days	4 Days	4 Days	4 Days
FROZEN (-15°C)
50-100	30 Days
250/1.5 mL	30 Days
100		30 Days
10-100			30 Days	30 Days	30 Days	30 Days	30 Days

Stability

Studies on Oxacillin Sodium at concentrations of 0.5 mg/mL and 2 mg/mL in various intravenous solutions listed below indicate the drug will lose less than 10% activity at room temperature (70° F) during a 6-hour period.

IV Solution

5% Dextrose in Normal Saline

10% D-Fructose in Water

10% D-Fructose in Normal Saline

Lactated Potassic Saline Injection

10% Invert Sugar in Normal Saline

10% Invert Sugar Plus 0.3% Potassium Chloride in Water

Travert 10% Electrolyte #1

Travert 10% Electrolyte #2

Travert 10% Electrolyte #3

Only those solutions listed above should be used for the intravenous infusion of Oxacillin Sodium. The concentration of the antibiotic should fall within the range specified. The drug concentration and the rate and volume of the infusion should be adjusted so that the total dose of oxacillin is administered before the drug loses its stability in the solution in use.

If another agent is used in conjunction with oxacillin therapy, it should not be physically mixed with oxacillin but should be administered separately.

Pharmacy Bulk Package

This glass Pharmacy Bulk Package bottle contains 10 grams Oxacillin Sodium and is designed for use in the pharmacy in preparing IV admixtures. Add 93 mL Sterile Water for Injection, USP or Sodium Chloride Injection, USP 0.9%. The resulting solution will contain 100 mg oxacillin per mL and will require further dilution.

CAUTION: NOT TO BE DISPENSED AS A UNIT.

Directions For Proper Use of Pharmacy Bulk Package

The container closure may be penetrated only one time after reconstitution, utilizing a suitable sterile dispensing set which allows measured distribution of the contents.
Use of this product is restricted to a suitable work area, such as a laminar flow hood.
Once this container closure has been punctured, withdrawal of the contents should be completed without delay. If prompt fluid transfer cannot be accomplished, discard the contents no later than 4 hours after initial closure puncture. This time limit should begin with the introduction of solvent or diluent into the Pharmacy Bulk Package bottle.
A plastic ball attached to the pharmacy bulk package provides a suitable hanging device while dispensing contents.

Parenteral drug products should be inspected visually for particulate matter and discoloration prior to administration, whenever solution and container permit.

HOW SUPPLIED

Oxacillin for Injection, USP, is available in a Pharmacy Bulk Package bottle which contains oxacillin sodium monohydrate equivalent to 10 grams oxacillin.

NDC 0781-3103-95 10 grams Pharmacy Bulk Package bottle, Packaged in carton of ten Pharmacy Bulk Package bottles.

Storage

Store the dry powder at 20°-25°C (68°-77°F) [See USP Controlled Room Temperature].
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产地国家: 美国
原产地英文商品名:
OXACILLIN 2g/vial 10vials/box
原产地英文药品名:
OXACILLIN SODIUM
原产地英文化合物名称:
4-Thia-1-azabicyclo[3.2.0]heptane-2-carboxylic acid, 3,3-dimethyl-6-[[(5-methyl-3-phenyl-4-isoxazolyl]carbonyl]amino]-7-oxo-, monosodium salt, (2S,5R,6R)-
中文参考商品译名:
苯唑西林 2克/瓶 10瓶/盒
中文参考药品译名:
苯唑西林钠
中文参考化合物名称:
;(2S,5R,6R)-3,3-二甲基-6-[(5-甲基-3-苯基-1,2-恶唑-4-甲酰)氨基]-7-氧代-4-硫杂-1-氮杂双环[3.2.0]庚烷-2-羧酸钠盐
生产厂家中文参考译名:
山德士-NOVAPLUS
生产厂家英文名:
SANDOZ-NOVAPLUS

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产地国家: 美国
原产地英文商品名:
OXACILLIN 1g/vial 10vials/box
原产地英文药品名:
OXACILLIN SODIUM
原产地英文化合物名称:
4-Thia-1-azabicyclo[3.2.0]heptane-2-carboxylic acid, 3,3-dimethyl-6-[[(5-methyl-3-phenyl-4-isoxazolyl]carbonyl]amino]-7-oxo-, monosodium salt, (2S,5R,6R)-
中文参考商品译名:
苯唑西林 1克/瓶 10瓶/盒
中文参考药品译名:
苯唑西林钠
中文参考化合物名称:
;(2S,5R,6R)-3,3-二甲基-6-[(5-甲基-3-苯基-1,2-恶唑-4-甲酰)氨基]-7-氧代-4-硫杂-1-氮杂双环[3.2.0]庚烷-2-羧酸钠盐
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http://www.drugs.com/cons/bactocill.html
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http://www.rxlist.com/oxacillin-drug.htm