Product Elements:
Nafcillin nafcillin sodium nafcillin sodium nafcillin
Drug Interactions:
Drug interactions tetracycline, a bacteriostatic antibiotic, may antagonize the bactericidal effect of penicillin, and concurrent use of these drugs should be avoided. nafcillin in high dosage regimens, i.e., 2 grams every 4 hours, has been reported to decrease the effects of warfarin. when nafcillin and warfarin are used concomitantly, the prothrombin time should be closely monitored and the dose of warfarin adjusted as necessary. this effect may persist for up to 30 days after nafcillin has been discontinued. nafcillin when administered concomitantly with cyclosporine has been reported to result in subtherapeutic cyclosporine levels. the nafcillin-cyclosporine interaction was documented in a patient during two separate courses of therapy. when cyclosporine and nafcillin are used concomitantly in organ transplant patients, the cyclosporine levels should be monitored.
Indications and Usage:
Indications and usage nafcillin is indicated in the treatment of infections caused by penicillinase-producing staphylococci which have demonstrated susceptibility to the drug. culture and susceptibility tests should be performed initially to determine the causative organism and its susceptibility to the drug (see clinical pharmacology - susceptibility test methods ). nafcillin should not be used in infections caused by organisms susceptible to penicillin g. if the susceptibility tests indicate that the infection is due to a methicillin-resistant staphylococcus spp., therapy with nafcillin for injection, usp should be discontinued and alternative therapy provided. to reduce the development of drug-resistant bacteria and maintain the effectiveness of nafcillin for injection, usp and other antibacterial drugs, nafcillin 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 suscepti
Read more...bility 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.
Warnings:
Warnings serious and occasionally fatal hypersensitivity (anaphylactic) reactions have been reported in patients on penicillin therapy. these reactions are more likely to occur in individuals with a history of penicillin hypersensitivity and/or a history of sensitivity to multiple allergens. there have been reports of individuals with a history of penicillin hypersensitivity who have experienced severe reactions when treated with cephalosporins. before initiating therapy with nafcillin, careful inquiry should be made concerning previous hypersensitivity reactions to penicillins, cephalosporins, or other allergens. if an allergic reaction occurs, nafcillin should be discontinued and appropriate therapy instituted. serious anaphylactic reactions require immediate emergency treatment with epinephrine. oxygen, intravenous steroids, and airway management, including intubation, should also be administered as indicated. clostridium difficile associated diarrhea (cdad) has been reported with u
Read more...se of nearly all antibacterial agents, including nafcillin 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.
General Precautions:
General nafcillin 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 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. the liver/biliary tract is the primary route of nafcillin clearance. caution should be exercised when patients with concomitant hepatic insufficiency and renal dysfunction are treated with nafcillin. serum levels should be measured and the dosage adjusted appropriately to avoid possible neurotoxic reactions associated with very high concentrations (see dosage and administration ). pres
Read more...cribing nafcillin 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.
Dosage and Administration:
Dosage and administration nafcillin for injection, in the pharmacy bulk package bottle is for intravenous injection only. the usual iv dosage for adults is 500 mg every 4 hours. for severe infections, 1 gram every 4 hours is recommended. administer slowly over at least 30 to 60 minutes to minimize the risk of vein irritation and extravasation. bacteriologic studies to determine the causative organisms and their susceptibility to nafcillin 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 nafcillin 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 duration of ther
Read more...apy. nafcillin-probenecid therapy is generally limited to those infections where very high serum levels of nafcillin are necessary. no dosage alterations are necessary for patients with renal dysfunction, including those on hemodialysis. hemodialysis does not accelerate nafcillin clearance from the blood. for patients with hepatic insufficiency and renal failure, measurement of nafcillin serum levels should be performed and dosage adjusted accordingly. with intravenous administration, particularly in elderly patients, care should be taken because of the possibility of thrombophlebitis. parenteral drug products should be inspected visually for particulate matter and discoloration prior to administration whenever solution and container permit. do not add supplementary medication to nafcillin for injection, usp.
Contraindications:
Contraindications a history of a hypersensitivity (anaphylactic) reaction to any penicillin is a contraindication.
Adverse Reactions:
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 or vaccines. two types of allergic reactions to penicillins 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 administrat
Read more...ion 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. local reactions pain, swelling, inflammation, phlebitis, thrombophlebitis, and occasional skin sloughing at the injection site have occurred with intravenous administration of nafcillin (see dosage and administration ). severe tissue necrosis with sloughing secondary to subcutaneous extravasation of nafcillin has been reported. nervous system reactions neurotoxic reactions similar to those observed with penicillin g could occur with large intravenous or intraventricular doses of nafcillin especially in patients with concomitant hepatic insufficiency and renal dysfunction (see precautions ). urogenital reactions renal tubular damage and interstitial nephritis have been associated infrequently with the administration of nafcillin. 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 nafcillin. 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 nafcillin. to report suspected adverse reactions, contact athenex pharmaceutical division, llc. at 1-855-273-0154 or fda at 1-800-fda-1088 or www.fda.gov/medwatch .
Drug Interactions:
Drug interactions tetracycline, a bacteriostatic antibiotic, may antagonize the bactericidal effect of penicillin, and concurrent use of these drugs should be avoided. nafcillin in high dosage regimens, i.e., 2 grams every 4 hours, has been reported to decrease the effects of warfarin. when nafcillin and warfarin are used concomitantly, the prothrombin time should be closely monitored and the dose of warfarin adjusted as necessary. this effect may persist for up to 30 days after nafcillin has been discontinued. nafcillin when administered concomitantly with cyclosporine has been reported to result in subtherapeutic cyclosporine levels. the nafcillin-cyclosporine interaction was documented in a patient during two separate courses of therapy. when cyclosporine and nafcillin are used concomitantly in organ transplant patients, the cyclosporine levels should be monitored.
Use in Pregnancy:
Pregnancy: teratogenic effects pregnancy category b reproduction studies have been performed in the mouse with oral doses up to 20 times the human dose and orally in the rat at doses up to 40 times the human dose and have revealed no evidence of impaired fertility or harm to the rodent fetus due to nafcillin. there are, however, no adequate or well-controlled studies in pregnant women. because animal reproduction studies are not always predictive of human response, nafcillin should be used during pregnancy only if clearly needed.
Pediatric Use:
Pediatric use the liver/biliary tract is the principal route of nafcillin elimination. because of immature hepatic and renal function in pediatric patients, nafcillin excretion may be impaired, with abnormally high serum levels resulting. serum levels should be monitored and the dosage adjusted appropriately. there are no approved pediatric patient dosage regimens for intravenous nafcillin. safety and effectiveness in pediatric patients have not been established.
Geriatric Use:
Geriatric use clinical studies of nafcillin for injection did not include sufficient numbers 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. each pharmacy bulk package bottle contains nafcillin sodium, as the monohydrate equivalent to 10 grams of nafcillin. the sodium content is 65.8 mg [2.9 meq] per gram of nafcillin. the product is buffered with 40 mg sodium citrate per gram. at the usual recommended doses, patients would receive between 197.4 and 394.8 mg/day (8.7 and 17.4 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.
Overdosage:
Overdosage neurotoxic reactions similar to those observed with penicillin g may arise with intravenous doses of nafcillin especially in patients with concomitant hepatic insufficiency and renal dysfunction (see precautions ). in the case of overdosage, discontinue nafcillin, treat symptomatically and institute supportive measures as required. hemodialysis does not increase the rate of clearance of nafcillin from the blood.
Description:
Description nafcillin for injection, usp is a semisynthetic antibiotic penicillin derived from the penicillin nucleus 6-aminopenicillanic acid. it is the sodium salt in a parenteral dosage form. the chemical name is 4-thia-1-azabicyclo [3.2.0]heptane-2-carboxylic acid, 6-[[(2-ethoxy-1-naphthalenyl)carbonyl]amino]-3,3-dimethyl-7-oxo-monosodium salt, monohydrate [2 s (2α,5α,6β)]. it is resistant to inactivation by the enzyme penicillinase (beta-lactamase). the structural formula of nafcillin sodium is as follows: c 21 h 21 n 2 nao 5 sâ¢h 2 o m.w. 454.48 each nafcillin for injection, usp pharmacy bulk package is supplied as a dry powder in bottles containing nafcillin sodium and is intended for intravenous use only. it is soluble in water. the ph of the aqueous solution is 6.0 to 8.5. each pharmacy bulk package bottle contains nafcillin sodium, as the monohydrate equivalent to 10 grams of nafcillin. the sodium content is 65.8 mg [2.9 meq] per gram of nafcillin. the product is buffered with 40 mg sodium citrate per gram. a pharmacy bulk package is a container of sterile dosage form which contains many single doses. the contents are intended for use in a pharmacy admixture program and are restricted to the preparation of admixtures for intravenous infusion. further dilution is required after reconstitution, (see dosage and administration and directions for proper use of pharmacy bulk package ). not to be dispensed as a unit . structural formula
Clinical Pharmacology:
Clinical pharmacology in a study of five healthy adults administered a single 500 mg dose of nafcillin by intravenous injection over seven minutes, the mean plasma concentration of the drug was approximately 30 mcg/ml at 5 minutes after injection. the mean area under the plasma concentration-versus-time curve (auc) for nafcillin in this study was 18.06 mcg ⢠h/ml. the serum half-life of nafcillin administered by the intravenous route ranged from 33 to 61 minutes as measured in three separate studies. in contrast to the other penicillinase-resistant penicillins, only about 30% of nafcillin is excreted as unchanged drug in the urine of normal volunteers, and most within the first six hours. nafcillin is primarily eliminated by nonrenal routes, namely hepatic inactivation and excretion in the bile. nafcillin binds to serum proteins, mainly albumin. the degree of protein binding reported for nafcillin is 89.9 ± 1.5%. reported values vary with the method of study and the investigato
Read more...r. the concurrent administration of probenecid with nafcillin increases and prolongs plasma concentrations of nafcillin. probenecid significantly reduces the total body clearance of nafcillin with renal clearance being decreased to a greater extent than nonrenal clearance. the penicillinase-resistant penicillins are widely distributed in various body fluids, including bile, pleural, amniotic and synovial fluids. with normal doses insignificant concentrations are found in the aqueous humor of the eye. high nafcillin csf levels have been obtained in the presence of inflamed meninges. renal failure does not appreciably affect the serum half-life of nafcillin; therefore, no modification of the usual nafcillin dosage is necessary in renal failure with or without hemodialysis. hemodialysis does not accelerate the rate of clearance of nafcillin from the blood. a study which assessed the effects of cirrhosis and extrahepatic biliary obstruction in man demonstrated that the plasma clearance of nafcillin was significantly decreased in patients with hepatic dysfunction. in these patients with cirrhosis and extrahepatic obstruction, nafcillin excretion in the urine was significantly increased from about 30 to 50% of the administered dose, suggesting that renal disease superimposed on hepatic disease could further decrease nafcillin clearance. 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 strains of staphylococcus aureus . the penicillinase-resistant penicillins are active in vitro against a variety of other bacteria. susceptibility test methods for specific information regarding susceptibility test interpretive criteria and associated test methods and quality control standards recognized by fda for this drug, please see: https://www.fda.gov/stic .
Carcinogenesis and Mutagenesis and Impairment of Fertility:
Carcinogenesis, mutagenesis, impairment of fertility no long-term animal studies have been conducted with these drugs. studies on reproduction (nafcillin) in rats and mice reveal no fetal or maternal abnormalities before conception and continuously through weaning (one generation).
How Supplied:
How supplied nafcillin for injection, usp is supplied as follows: ndc nafcillin for injection, usp package factor 70860-119-99 10 gram pharmacy bulk bottle 1 bottle per carton each nafcillin for injection, usp pharmacy bulk package bottle contains nafcillin sodium equivalent to 10 grams of nafcillin. storage conditions prior to reconstitution: store at 20º to 25ºc (68º to 77ºf). [see usp controlled room temperature.] sterile, nonpyrogenic, preservative-free. the container closure is not made with natural rubber latex. athenex mfd. for athenex schaumburg, il 60173 (usa) mfd. by istituto biochimico italiano made in italy ©2018 athenex. revised: september 2018
Information for Patients:
Information for patients patients should be counseled that antibacterial drugs including nafcillin for injection should only be used to treat bacterial infections. they do not treat viral infections (e.g. the common cold). when nafcillin 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 nafcillin 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 a
Read more...s 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.
Package Label Principal Display Panel:
Package label - principal display panel - bottle label ndc 70860-119-99 nafcillin for injection, usp 10 grams per pharmacy bulk package pharmacy bulk package - not for direct infusion this pharmacy bulk package is not to be dispensed as a unit rx only buffered - for intravenous use package label - principal display panel - bottle label