Source:http://www4.wiwiss.fu-berlin.de/dailymed/resource/drugs/3504
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Nafcillin (Injection, Solution)
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Nafcillin
Injection, USP supplied as a premixed frozen solution is to be
administered as an intravenous infusion. The usual I.V. dosage for
adults is 500 mg every 4 hours. For severe infections, 1 g 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 oftherapy 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 therapy. 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 Injection, USP. Store in a freezer
capable of maintaining a temperature of -20��C (-4��F) or
less.
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dailymed-instance:descripti... |
Nafcillin
Injection, USP is a sterile injectable product containing nafcillin
which is added as Nafcillin Sodium, USP, a semisynthetic penicillin
derived from the penicillin nucleus, 6-aminopenicillanic acid. The
chemical name of nafcillin sodium is Monosodium (2S,5R,6R)-6-(2-ethoxy-1-naphthamido)-3,3-dimethyl-7-oxo-4-thia-1-
azabicyclo[3.2.0]heptane-2-carboxylate monohydrate. It is resistant to
inactivation by the enzyme penicillinase (beta-lactamase). The molecular
formula of Nafcillin Sodium, USP is
CHNNaOS��HO.
The molecular weight is 454.48. The structural formula of nafcillin
sodium is as follows: Nafcillin
Injection, USP is a frozen, iso-osmotic, sterile, nonpyrogenic premixed
50 mL or 100 mL solution containing 1 g or 2 g of nafcillin,
respectively, added as Nafcillin Sodium, USP. Dextrose, USP has been
added to the above dosages to adjust osmolality (approximately 1.8 g and
3.6 g as dextrose hydrous to the 1 g and 2 g dosages, respectively).
Sodium Citrate Hydrous, USP has been added as a buffer (approximately 90
mg and 180 mg to the 1 g and 2 g dosages, respectively). The pH has been
adjusted with hydrochloric acid and may have been adjusted with sodium
hydroxide. The pH is 6.5 (6.0 to 8.5). The solution is intended for
intravenous use after thawing to room temperature. This GALAXY
container is fabricated from a specially designed multilayer plastic (PL
2040). Solutions are in contact with the polyethylene layer of this
container and can leach out certain chemical components of the plastic
in very small amounts within the expiration period. The suitability of
the plastic has been confirmed in tests in animals according to the USP
biological tests for plastic containers, as well as by tissue culture
toxicity studies.
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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��g/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��g��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 investigator. 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.<br/>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.<br/>Susceptibility
Tests:<br/>Diffusion
Techniques: Quantitative methods that require measurement of zone
diameters provide reproducible estimates of the
susceptibility of bacteria to antimicrobial compounds.
One such standardized procedurethat has
been recommended for use with disks to test the
susceptibility of microorganisms to nafcillin uses the
1-��g nafcillin disk. Interpretation involves correlation
of the diameter obtained in the disk test with the MIC
for nafcillin. Reports from the laboratory providing
results of the standard single-disk susceptibility test
with a 1-��g nafcillin disk should be interpreted
according to the following criteria: A
report of���Susceptible���indicates that the pathogen is
likely to be inhibited by usually achievable
concentrations of the antimicrobial compound in blood. A
report of���Intermediate���indicates that the result
should be considered equivocal, and, if the
microorganism is not fully susceptible to alternative,
clinically feasible drugs, the test should be repeated.
This category implies possible clinical applicability in
body sites where the drug is physiologically
concentrated or in situations where high dosage of drug
can be used. This category also provides a buffer zone
that prevents small uncontrolled technical factors from
causing major discrepancies in interpretation. A report
of���Resistant���indicates that usually achievable
concentrations of the antimicrobial compound in the
blood are unlikely to be inhibitory and that other
therapy should be selected. Measurement of MIC or MBC and achieved antimicrobial
compound concentrations may be appropriate to guide
therapy in some infections. (See CLINICAL PHARMACOLOGY section for
further information on drug concentrations achieved in
infected body sites and other pharmacokinetic properties
of this antimicrobial drug product.) Standardized susceptibility test procedures require the
use of laboratory control microorganisms. The 1��g
nafcillin disk should provide the following zone
diameters in these laboratory test quality control
strains:<br/>Dilution
techniques: Quantitative methods that are used to determine minimum
inhibitory concentrations provide reproducible estimates
of the susceptibility of bacteria to antimicrobial
compounds. One such standardized procedure uses a
standardized dilution method(broth, agar,
or microdilution) or equivalent with nafcillin powder.
The MIC values obtained should be interpreted according
to the following criteria: Interpretation should be as stated above for results
using diffusion techniques. As with standard diffusion
techniques, dilution methods require the use of
laboratory control microorganisms. Standard nafcillin powder should provide the following MIC values:
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Nafcillin
Injection, USP is supplied as a premixed frozen iso-osmotic solution in
50 mL and 100 mL single dose GALAXY containers (PL 2040 Plastic) as follows: 2G3540 NDC
0338-1017-41 1 gram nafcillin in 50 mL 2G3556 NDC
0338-1019-48 2 grams nafcillin in 100 mL Store at or below
-20��C/-4��F. See DIRECTIONS FOR USE OF GALAXY CONTAINER (PL 2040 PLASTIC).
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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). Prescribing
Nafcillin Injection, USP 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.<br/>Laboratory Tests: Bacteriologic studies to determine the causative organisms and
their susceptibility to nafcillin should be performed. (SeeCLINICAL
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
nafcillin. White blood cell and differential cell counts should
be obtained prior to initiation of therapy and periodically
during therapy with nafcillin. Periodic urinalysis, blood urea nitrogen, and creatinine determinations should be performed
during therapy with nafcillin. SGOT and SGPT values should be
obtained periodically during therapy to monitor for possible
liver function abnormalities.<br/>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.<br/>Drug/Laboratory
Test Interactions: Nafcillin
in the urine can cause a false-positive urine reaction for
protein when the sulfosalicyclic acid test is used, but not with the dipstick.<br/>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).<br/>Pregnancy:<br/>Teratogenic
Effects:<br/>Nursing Mothers: Penicillins
are excreted in human milk. Caution should be exercised when
penicillins are administered to a nursing woman.<br/>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. The
potential for toxic effects in pediatric patients from chemicals
that may leach from the single dose premixed intravenous
preparation in plastic containers has not been
determined.<br/>Geriatric Use: Clinical
studies of Nafcillin Injection, USP 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. Nafcillin
Injection, USP contains 76.6 mg (3.33 mEq) of sodium per gram.
At the usual recommended doses, patients would receive between
230 and 460 mg/day (10.0 and 20.0 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.<br/>Information for
Patients: Patients
should be counseled that antibacterial drugs including Nafcillin
Injection, USP should only be used to treat bacterial
infections. They do not treat viral infections (e.g., the common
cold). When Nafcillin Injection, USP 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) decreasethe effectiveness of the immediate treatment and (2) increase
the likelihood that bacteria will develop resistance and will
not be treatable by Nafcillin Injection, USP 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.
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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 . 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.
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Nafcillin sodium
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Nafcillin (Injection, Solution)
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Body as a Whole: The
reported incidence of allergic reactions to penicillin ranges
from 0.7 to 10 percent . 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
reactionsto 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 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.<br/>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.<br/>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. .<br/>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.<br/>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 .<br/>Metabolic Reactions: Agranulocytosis, neutropenia, and bone marrow depression have
been associated with the use of nafcillin.
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dailymed-instance:warning |
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 use of nearly all antibacterial
agents, including Nafcillin Injection, USP, 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 againstC. 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.
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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 Tests). Nafcillin may be
used to initiate therapy in suspected cases of resistant staphylococcal
infections prior to the availability of susceptibility test results.
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 an organism other than a resistant
Staphylococcus, therapy should not be continued with Nafcillin
Injection, USP. To reduce the
development of drug-resistant bacteria and maintain the effectiveness of
Nafcillin Injection, USP and other antibacterial drugs, Nafcillin
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.
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Nafcillin
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