Source:http://www4.wiwiss.fu-berlin.de/dailymed/resource/drugs/689
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Floxin (Tablet, Coated)
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The usual dose of FLOXIN (ofloxacin tablets)
Tablets is 200 mg to 400 mg orally every 12 h as described in the following
dosing chart. These recommendations apply to patients with normal renal function
(i.e., creatinine clearance>50 mL/min). For patients with altered renal function
(i.e., creatinine clearance���50 mL/min), see the Patients with Impaired Renal Function subsection.<br/>Patients with Normal Renal Function: Antacids containing calcium, magnesium, or aluminum; sucralfate;
divalent or trivalent cations such as iron; or multivitamins containing zinc;
or Videx (didanosine) should not be taken within the two-hour
period before or within the two-hour period after taking ofloxacin.<br/>Patients with Impaired Renal Function: Dosage should be adjusted for patients with a creatinine
clearance���50 mL/min. After a normal initial
dose, dosage should be adjusted as follows: When only the serum creatinine is known, the following
formula may be used to estimate creatinine clearance. Men:
Creatinine clearance (mL/min) = Weight (kg)��(140-age) 72��serum creatinine (mg/dL) Women: 0.85��the value
calculated for men. The serum creatinine should represent
a steady-state of renal function.<br/>Patients with Cirrhosis: The excretion of ofloxacin may be reduced in patients with
severe liver function disorders (e.g., cirrhosis with or without ascites).
A maximum dose of 400 mg of ofloxacin per day should therefore not be exceeded.
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| dailymed-instance:descripti... |
FLOXIN (ofloxacin tablets) Tablets is a
synthetic broad-spectrum antimicrobial agent for oral administration. Chemically,
ofloxacin, a fluorinated carboxyquinolone, is the racemate, (��)-9-fluoro-2,3-dihydro-3-methyl-10-(4-methyl-1-piperazinyl)-7-oxo-7H-pyrido[1,2,3-de]-1,4-benzoxazin-6-carboxylic
acid. The chemical structure is: Its empirical formula is CHFNO,
and its molecular weight is 361.4. Ofloxacin is an off-white to pale yellow
crystalline powder. The molecule exists as a zwitterion at the pH conditions
in the small intestine. The relative solubility characteristics of ofloxacin
at room temperature, as defined by USP nomenclature, indicate that ofloxacin
is considered to be soluble in aqueous
solutions with pH between 2 and 5. It is sparingly to slightly soluble in aqueous
solutions with pH 7 (solubility falls to 4 mg/mL) and freely
soluble in aqueous solutions with pH above 9. Ofloxacin has the
potential to form stable coordination compounds with many metal ions. This in vitro chelation potential has the following
formation order: Fe>Al>Cu>Ni>Pb>Zn>Mg>Ca>Ba. FLOXIN Tablets
contain the following inactive ingredients: anhydrous lactose, modified corn
starch, hydroxypropyl cellulose, hypromellose, magnesium stearate, polyethylene
glycol, polysorbate 80, sodium starch glycolate, titanium dioxide and may
also contain synthetic yellow iron oxide.
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Following oral administration, the bioavailability of ofloxacin
in the tablet formulation is approximately 98%. Maximum serum concentrations
are achieved one to two hours after an oral dose. Absorption of ofloxacin
after single or multiple doses of 200 to 400 mg is predictable, and the amount
of drug absorbed increases proportionately with the dose. Ofloxacin has biphasic
elimination. Following multiple oral doses at steady-state administration,
the half-lives are approximately 4���5 hours and 20���25 hours.
However, the longer half-life represents less than 5% of the total AUC. Accumulation
at Steady-state can be estimated using a half-life of 9 hours. The total clearance
and volume of distribution are approximately similar after single or multiple
doses. Elimination is mainly by renal excretion. The following are mean peak
serum concentrations in healthy 70���80 kg male volunteers after single
oral doses of 200, 300, or 400 mg of ofloxacin or after multiple oral doses
of 400 mg. Steady-state concentrations were attained after four oral
doses, and the area under the curve (AUC) was approximately 40% higher than
the AUC after single doses. Therefore, after multiple-dose administration
of 200 mg and 300 mg doses, peak serum levels of 2.2��g/mL and 3.6��g/mL,
respectively, are predicted at steady-state. In vitro, approximately 32% of the drug in plasma
is protein bound. The single dose and steady-state plasma
profiles of ofloxacin injection were comparable in extent of exposure (AUC)
to those of ofloxacin tablets when the injectable and tablet formulations
of ofloxacin were administered in equal doses (mg/mg) to the same group of
subjects. The mean steady-state AUCattained after
the intravenous administration of 400 mg over 60 min was 43.5��g���h/mL;
the mean steady-state AUCattained after the oral
administration of 400 mg was 41.2��g���h/mL (two one-sided t-test,
90% confidence interval was 103���109). (See following chart.) Between 0
and 6 h following the administration of a single 200 mg oral dose of ofloxacin
to 12 healthy volunteers, the average urine ofloxacin concentration was approximately
220��g/mL. Between 12 and 24 hours after administration, the average
urine ofloxacin level was approximately 34��g/mL. Following
oral administration of recommended therapeutic doses, ofloxacin has been detected
in blister fluid, cervix, lung tissue, ovary, prostatic fluid, prostatic tissue,
skin, and sputum. The mean concentration of ofloxacin in each of these various
body fluids and tissues after one or more doses was 0.8 to 1.5 times the concurrentplasma level. Inadequate data are presently available on the distribution
or levels of ofloxacin in the cerebrospinal fluid or brain tissue. Ofloxacin
has a pyridobenzoxazine ring that appears to decrease the extent of parent
compound metabolism. Between 65% and 80% of an administered oral dose of ofloxacin
is excreted unchanged via the kidneys within 48 hours of dosing. Studies indicate
that less than 5% of an administered dose is recovered in the urine as the
desmethyl or N-oxide metabolites. Four to eight percent of an ofloxacin dose
is excreted in the feces. This indicates a small degree of biliary excretion
of ofloxacin. The administration of FLOXIN with
food does not affect the Cand AUCof the
drug, but Tis prolonged. Clearance of
ofloxacin is reduced in patients with impaired renal function (creatinine
clearance rate���50 mL/min), and dosage adjustment is necessary. Following oral administration
to healthy elderly subjects (65���81 years of age), maximum plasma concentrations
are usually achieved one to two hours after single and multiple twice-daily
doses, indicating that the rate of oral absorption is unaffected by age or
gender. Mean peak plasma concentrations in elderly subjects were 9���21%
higher than those observed in younger subjects. Gender differences in the
pharmacokinetic properties of elderly subjects have been observed. Peak plasma
concentrations were 114% and 54% higher in elderly females compared to elderly
males following single and multiple twice-daily doses. [This interpretation
was based on study results collected from two separate studies.] Plasma concentrations
increase dose-dependently with the increase in doses after single oral dose
and at steady state. No differences were observed in the volume of distribution
values between elderly and younger subjects. As in younger subjects, elimination
is mainly by renal excretion as unchanged drug in elderly subjects, although
less drug is recovered from renal excretion in elderly subjects. Consistent
with younger subjects, less than 5% of an administered dose was recovered
in the urine as the desmethyl and N-oxide metabolites in the elderly. A longer
plasma half-life of approximately 6.4 to 7.4 hours was observed in elderly
subjects, compared with 4 to 5 hours for young subjects. Slower elimination
of ofloxacin is observed in elderly subjects as compared with younger subjects
which may be attributable to the reduced renal function and renal clearance
observed in the elderly subjects. Because ofloxacin is known to be substantially
excreted by the kidney, and elderly patients are more likely to have decreased
renal function, dosage adjustment is necessary for elderly patients with impaired
renal function as recommended for all patients.<br/>MICROBIOLOGY: Ofloxacin is a quinolone antimicrobial agent. The mechanism
of action of ofloxacin and other fluoroquinolone antimicrobials involves inhibition
of bacterial topoisomerase IV and DNA gyrase (both of which are type II topoisomerases),
enzymes required for DNA replication, transcription, repair and recombination. Ofloxacin
has in vitro activity against a wide
range of gram-negative and gram-positive microorganisms. Ofloxacin is often
bactericidal at concentrations equal to or slightly greater than inhibitory
concentrations. Fluoroquinolones, including ofloxacin,
differ in chemical structure and mode of action from aminoglycosides, macrolides
and��-lactam antibiotics, including penicillins. Fluoroquinolones may,
therefore, be active against bacteria resistant to these antimicrobials. Resistance
to ofloxacin due to spontaneous mutation in vitro
is a rare occurrence (range: 10to 10).
Although cross-resistance has been observed between ofloxacin and some other
fluoroquinolones, some microorganisms resistant to other fluoroquinolones
may be susceptible to ofloxacin. Ofloxacin has been
shown to be active against most strains of the following microorganisms both in vitro and in clinical infections as described
in the INDICATIONS AND USAGE section: Aerobic
Gram-positive microorganisms Staphylococcus
aureus (methicillin-susceptible strains)Streptococcus pneumoniae (penicillin-susceptible
strains)Streptococcus
pyogenes Aerobic
Gram-negative microorganisms Citrobacter
(diversus) koseriEnterobacter aerogenesEscherichia coliHaemophilus influenzaeKlebsiella pneumoniaeNeisseria gonorrhoeaeProteus mirabilisPseudomonas aeruginosa As with other
drugs in this class, some strains of Pseudomonas
aeruginosa may develop resistance fairly rapidly during treatment
with ofloxacin. Other microorganisms Chlamydia trachomatis The following in
vitro data are available, but their clinical
significance is unknown. Ofloxacin exhibits in vitro minimum inhibitory concentrations (MIC
values) of 2��g/mL or less against most (���90%) strains of the
following microorganisms; however, the safety and effectiveness of ofloxacin
in treating clinical infections due to these microorganisms have not been
established in adequate and well-controlled trials. Aerobic Gram-positive microorganisms Staphylococcus epidermidis (methicillin-susceptible strains)Staphylococcus saprophyticusStreptococcus pneumoniae (penicillin-resistant strains) Aerobic Gram-negative microorganisms Acinetobacter calcoaceticusBordetella pertussisCitrobacter freundiiEnterobacter cloacaeHaemophilus ducreyiKlebsiella oxytocaMoraxella catarrhalisMorganella morganiiProteus vulgarisProvidencia rettgeriProvidencia stuartiiSerratia marcescens Anaerobic
microorganisms Clostridium
perfringes Other
microorganisms Chlamydia
pneumoniaeGardnerella vaginalisLegionella pneumophilaMycoplasma hominisMycoplasma pneumoniaeUreaplasma urealyticum Ofloxacin is not
active against Treponema pallidum Many
strains of other streptococcal species, Enterococcus
species, and anaerobes are resistant to ofloxacin.<br/>Susceptibility Tests:<br/>Dilution techniques: Quantitative methods are used to determine antimicrobial
minimum inhibitory concentrations (MIC values). These MIC values provide estimates
of the susceptibility of bacteria to antimicrobial compounds. The MIC values
should be determined using a standardized procedure. Standardized procedures
are based on a dilution method(broth or agar) or equivalent with
standardized inoculum concentrations and standardized concentrations of ofloxacin
powder. The MIC values should be interpreted according to the following criteria: The current absence of data on resistant strains precludes
defining any results other than "Susceptible". Strains yielding MIC results
suggestive of a "nonsusceptible" category should be submitted to a reference
laboratory for further testing. A report of "Susceptible" indicates that the pathogen is
likely to be inhibited if the antimicrobial compound in the blood reaches
the concentration usually achievable. 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 a high dosage of drug can be used. This category also provides a buffer
zone which prevents small uncontrolled technical factors from causing major
discrepancies in interpretation. A report of "Resistant" indicates that the
pathogen is not likely to be inhibited if the antimicrobial compound in the
blood reaches the concentration usually achievable; other therapy should be
selected. Standardized susceptibility test procedures
require the use of laboratory control microorganisms to control the technical
aspects of the laboratory procedures. Standard ofloxacin powder should provide
the following MIC values:<br/>Diffusion techniques: Quantitative methods that require measurement of zone diameters
also provide reproducible estimates of the susceptibility of bacteria to antimicrobial
compounds. One such standardized procedurerequires the use of
standardized inoculum concentrations. This procedure uses paper disks impregnated
with 5-��g ofloxacin to test the susceptibility of microorganisms to ofloxacin. Reports
from the laboratory providing results of the standard single-disk susceptibility
test with a 5-��g ofloxacin disk should be interpreted according to the
following criteria: The current absence of data on resistant strains precludes
defining any results other than "Susceptible". Strains yielding zone diameter
results suggestive of a "nonsusceptible" category should be submitted to a
reference laboratory for further testing. Interpretation should be as stated above for results using
dilution techniques. Interpretation involves correlation of the diameter obtained
in the disk test with the MIC for ofloxacin. As with
standardized dilution techniques, diffusion methods require the use of laboratory
control microorganisms that are used to control the technical aspects of the
laboratory procedures. For the diffusion technique, the 5-��g ofloxacin
disk should provide the following zone diameters in these laboratory quality
control strains:
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FLOXIN (ofloxacin tablets) Tablets is contraindicated
in persons with a history of hypersensitivity associated with the use of ofloxacin
or any member of the quinolone group of antimicrobial agents.
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FLOXIN (ofloxacin tablets) Tablets are supplied
as 200 mg light yellow, 300 mg white, and 400 mg pale gold oval, straight-edged,
coated tablets. Each tablet is distinguished by an imprint of "FLOXIN" and
the appropriate strength. FLOXIN Tablets are packaged in bottles in the following
configurations: 200 mg tablets - bottles of 50 (NDC
0062-1540-02) 300 mg tablets - bottles of 50 (NDC 0062
-1541-02) 400 mg tablets - bottles of 100 (NDC 0062-1542-01) FLOXIN
Tablets should be stored in well-closed containers. Store at 25��C (77��F);
excursions permitted to 15���30��C (59���86��F). Keep
out of the reach of children.
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dailymed-ingredient:anhydrous_lactose,
dailymed-ingredient:hydroxypropyl_cellulose,
dailymed-ingredient:hypromellose,
dailymed-ingredient:magnesium_stearate,
dailymed-ingredient:modified_corn_starch,
dailymed-ingredient:polyethylene_glycol,
dailymed-ingredient:polysorbate_80,
dailymed-ingredient:sodium_starch_glycolate,
dailymed-ingredient:synthetic_yellow_iron_oxide,
dailymed-ingredient:titanium_dioxide
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General: Prescribing FLOXIN (ofloxacin tablets) Tablets
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. Adequate
hydration of patients receiving ofloxacin should be maintained to prevent
the formation of a highly concentrated urine. Administer
ofloxacin with caution in the presence of renal or hepatic insufficiency/impairment.
In patients with known or suspected renal or hepatic insufficiency/impairment,
careful clinical observation and appropriate laboratory studies should be
performed prior to and during therapy since elimination of ofloxacin may be
reduced. In patients with impaired renal function (creatinine clearance���50
mg/mL), alteration of the dosage regimen is necessary. Moderate to severe photosensitivity/phototoxicity
reactions, the latter of which may manifest as exaggerated sunburn reactions
(e.g., burning, erythema, exudation, vesicles, blistering, edema) involving
areas exposed to light (typically the face,���V���area of the
neck, extensor surfaces of the forearms, dorsa of the hands), can be associated
with the use of quinolones after sun or UV light exposure. Therefore, excessive
exposure to these sources of light should be avoided. Drug therapy should
be discontinued if photosensitivity/phototoxicity occurs (See ADVERSE REACTIONS/Post-Marketing Adverse
Events). As with other quinolones,
ofloxacin should be used with caution in any patient with a known or suspected
CNS disorder that may predispose to seizures or lower the seizure threshold
(e.g., severe cerebral arteriosclerosis, epilepsy) or in the presence of other
risk factors that may predispose to seizures or lower the seizure threshold
(e.g., certain drug therapy, renal dysfunction). A
possible interaction between oral hypoglycemic drugs (e.g., glyburide/glibenclamide)
or with insulin and fluoroquinolone antimicrobial agents have been reported
resulting in a potentiation of the hypoglycemic action of these drugs. The
mechanism for this interaction is not known. If a hypoglycemic reaction occurs
in a patient being treated with ofloxacin, discontinue ofloxacin immediately
and consult a physician. (See Drug
Interactions and ADVERSE REACTIONS.) As
with any potent drug, periodic assessment of organ system functions, including
renal, hepatic, and hematopoietic, is advisable during prolonged therapy.
(See WARNINGS
and ADVERSE
REACTIONS.)<br/>Torsades
de pointes: Some quinolones, including ofloxacin, have been associated
with prolongation of the QT interval on the electrocardiogram and infrequent
cases of arrhythmia. Rare cases of torsades de pointes have been spontaneously
reported during post-marketing surveillance in patients receiving quinolones,
including ofloxacin. Ofloxacin should be avoided in patients with known prolongation
of the QT interval, patients with uncorrected hypokalemia, and patients receiving
Class IA (quinidine, procainamide), or Class III (amiodarone, sotalol) antiarrhythmic
agents.<br/>Information for Patients: Patients should be advised:<br/>Drug Interactions:<br/>Antacids, Sucralfate, Metal Cations,
Multivitamins: Quinolones form chelates with alkaline earth and transition
metal cations. Administration of quinolones with antacids containing calcium,
magnesium, or aluminum, with sucralfate, with divalent or trivalent cations
such as iron, or with multivitamins containing zinc or with Videx (didanosine)
may substantially interfere with the absorption of quinolones resulting in
systemic levels considerably lower than desired. These agents should not be
taken within the two-hour period before or within the two-hour period after
ofloxacin administration. (See DOSAGE
AND ADMINISTRATION.)<br/>Caffeine: Interactions between ofloxacin and caffeine have not been
detected.<br/>Cimetidine: Cimetidine has demonstrated interference with the elimination
of some quinolones. This interference has resulted in significant increases
in half-life and AUC of some quinolones. The potential for interaction between
ofloxacin and cimetidine has not been studied.<br/>Cyclosporine: Elevated serum levels of cyclosporine have been reported
with concomitant use of cyclosporine with some other quinolones. The potential
for interaction between ofloxacin and cyclosporine has not been studied.<br/>Drugs metabolized by Cytochrome P450
enzymes: Most quinolone antimicrobial drugs inhibit cytochrome P450
enzyme activity. This may result in a prolonged half-life for some drugs that
are also metabolized by this system (e.g., cyclosporine, theophylline/methylxanthines,
warfarin) when co-administered with quinolones. The extent of this inhibition
varies among different quinolones. (See other Drug Interactions.)<br/>Non-steroidal anti-inflammatory drugs:: The concomitant administration of a non-steroidal anti-inflammatory
drug with a quinolone, including ofloxacin, may increase the risk of CNS stimulation
and convulsive seizures. (See WARNINGS and PRECAUTIONS:
General.)<br/>Probenecid: The concomitant use of probenecid with certain other quinolones
has been reported to affect renal tubular secretion. The effect of probenecid
on the elimination of ofloxacin has not been studied.<br/>Theophylline: Steady-state theophylline levels may increase when ofloxacin
and theophylline are administered concurrently. As with other quinolones,
concomitant administration of ofloxacin may prolong the half-life of theophylline,
elevate serum theophylline levels, and increase the risk of theophylline-related
adverse reactions. Theophylline levels should be closely monitored and theophylline
dosage adjustments made, if appropriate, when ofloxacin is co-administered.
Adverse reactions (including seizures) may occur with or without an elevation
in the serum theophylline level.<br/>Warfarin: Some quinolones have been reported to enhance the effects
of the oral anticoagulant warfarin or its derivatives. Therefore, if a quinolone
antimicrobial is administered concomitantly with warfarin or its derivatives,
the prothrombin time or other suitable coagulation test should be closely
monitored.<br/>Antidiabetic agents (e.g., insulin,
glyburide/glibenclamide): Since disturbances of blood glucose, including
hyperglycemia and hypoglycemia, have been reported in patients treated concurrently
with quinolones and an antidiabetic agent, careful monitoring of blood glucose
is recommended when these agents are used concomitantly.<br/>Interaction with Laboratory or Diagnostic
Testing:: Some quinolones, including ofloxacin, may produce false-positive
urine screening results for opiates using commercially available immunoassay
kits. Confirmation of positive opiate screens by more specific methods may
be necessary.<br/>Carcinogenesis, Mutagenesis, Impairment
of Fertility: Long-term studies to determine the carcinogenic potential
of ofloxacin have not been conducted. Ofloxacin was
not mutagenic in the Ames bacterial test, in
vitro and in vivo cytogenetic
assay, sister chromatid exchange (Chinese Hamster and Human Cell Lines), unscheduled
DNA Repair (UDS) using human fibroblasts, dominant lethal assays, or mouse
micronucleus assay. Ofloxacin was positive in the UDS test using rat hepatocytes
and Mouse Lymphoma Assay.<br/>Pregnancy: Teratogenic Effects. Pregnancy Category C. Ofloxacin
has not been shown to have any teratogenic effects at oral doses as high as
810 mg/kg/day (11 times the recommended maximum human dose based on mg/mor
50 times based on mg/kg) and 160 mg/kg/day (4 times the recommended maximum
human dose based on mg/mor 10 times based on mg/kg) when administered
to pregnant rats and rabbits, respectively. Additional studies in rats with
oral doses up to 360 mg/kg/day (5 times the recommended maximum human dose
based on mg/mor 23 times based on mg/kg) demonstrated no adverse
effect on late fetal development, labor, delivery, lactation, neonatal viability,
or growth of the newborn. Doses equivalent to 50 and 10 times the recommended
maximum human dose of ofloxacin (based on mg/kg) were fetotoxic (i.e., decreased
fetal body weight and increased fetal mortality) in rats and rabbits, respectively.
Minor skeletal variations were reported in rats receiving doses of 810 mg/kg/day,
which is more than 10 times higher than the recommended maximum human dose
based on mg/m. There are, however, no adequate
and well-controlled studies in pregnant women. Ofloxacin should be used during
pregnancy only if the potential benefit justifies the potential risk to the
fetus.<br/>Nursing Mothers: In lactating females, a single oral 200-mg dose of ofloxacin
resulted in concentrations of ofloxacin in milk that were similar to those
found in plasma. Because of the potential for serious adverse reactions from
ofloxacin in nursing infants, a decision should be made whether to discontinue
nursing or to discontinue the drug, taking into account the importance of
the drug to the mother. (See WARNINGS and ADVERSE
REACTIONS.)<br/>Pediatric Use: Safety and effectiveness in pediatric patients and adolescents
below the age of 18 years have not been established. Ofloxacin causes arthropathy
(arthrosis) and osteochondrosis in juvenile animals of several species.<br/>Geriatric Use: In phase 2/3 clinical trials with ofloxacin, 688 patients
(14.2%) were���65 years of age. Of these, 436 patients (9.0%) were
between the ages of 65 and 74 and 252 patients (5.2%) were 75 years or older.
There was no apparent difference in the frequency or severity of adverse reactions
in elderly adults compared with younger adults. The pharmacokinetic properties
of ofloxacin in elderly subjects are similar to those in younger subjects.
Drug absorption appears to be unaffected by age. Dosage adjustment is necessary
for elderly patients with impaired renal function (creatinine clearance rate���50 mL/min) due to reduced clearance of ofloxacin. In comparative
studies, the frequency and severity of most drug-related nervous system events
in patients���65 years of age were comparable for ofloxacin and control
drugs. The only differences identified were an increase in reports of insomnia
(3.9% vs 1.5%) and headache (4.7% vs 1.8%) with ofloxacin. It is important
to note that these geriatric safety data are extracted from 44 comparative
studies where the adverse reaction information from 20 different controls
(other antibiotics or placebo) were pooled for comparison with ofloxacin.
The clinical significance of such a comparison is not clear. (See CLINICAL PHARMACOLOGY and DOSAGE AND
ADMINISTRATION.) Elderly patients
may be more sensitive to drug-associated effects on the QT interval. Therefore,
precaution should be taken when using ofloxacin with concomitant drugs that
can result in prolongation of the QT interval (e.g. class IA or class III
antiarrhythmics) or in patients with risk factors for Torsade de pointes (e.g.
known QT prolongation, uncorrected hypokalemia). Patients over 65 are at increased risk for
developing severe tendon disorders including tendon rupture when being treated
with a fluoroquinolone such as FLOXIN. This risk is further
increased with concomitant steroid therapy. Tendon rupture usually involves
the Achilles, hand or shoulder tendons and can occur during therapy or up
to a few months post completion of therapy. Caution should be used when prescribing
FLOXIN to elderly patients especially those on corticosteroids.
Patients should be informed of this potential side effect and advised to discontinue
therapy and inform their physicians if any tendon symptoms occur.
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| dailymed-instance:overdosag... |
Information on overdosage with ofloxacin is limited. One
incident of accidental overdosage has been reported. In this case, an adult
female received 3 grams of ofloxacin intravenously over 45 minutes. A blood
sample obtained 15 minutes after the completion of the infusion revealed an
ofloxacin level of 39.3��g/mL. In 7 h, the level had fallen to 16.2��g/mL,
and by 24 h to 2.7��g/mL. During the infusion, the patient developed
drowsiness, nausea, dizziness, hot and cold flushes, subjective facial swelling
and numbness, slurring of speech, and mild to moderate disorientation. All
complaints except the dizziness subsided within 1 h after discontinuation
of the infusion. The dizziness, most bothersomewhile standing, resolved in
approximately 9 h. Laboratory testing reportedly revealed no clinically significant
changes in routine parameters in this patient. In the
event of an acute overdose, the stomach should be emptied. The patient should
be observed and appropriate hydration maintained. Ofloxacin is not efficiently
removed by hemodialysis or peritoneal dialysis.
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ofloxacin
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Floxin (Tablet, Coated)
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| dailymed-instance:adverseRe... |
The following is a compilation of the data for ofloxacin
based on clinical experience with both the oral and intravenous formulations.
The incidence of drug-related adverse reactions in patients during Phase 2
and 3 clinical trials was 11%. Among patients receiving multiple-dose therapy,
4% discontinued ofloxacin due to adverse experiences. In
clinical trials, the following events were considered likely to be drug-related
in patients receiving multiple doses of ofloxacin: In clinical trials, the most frequently reported adverse
events, regardless of relationship to drug, were: In clinical trials, the following events, regardless of
relationship to drug, occurred in 1 to 3% of patients: Additional events, occurring in clinical trials at a rate
of less than 1%, regardless of relationship to drug, were: The following laboratory abnormalities appeared in���1.0%
of patients receiving multiple doses of ofloxacin. It is not known whether
these abnormalities were caused by the drug or the underlying conditions being
treated.<br/>Post-Marketing Adverse Events: Additional adverse events, regardless of relationship to
drug, reported from worldwide marketing experience with quinolones, including
ofloxacin: In clinical trials using multiple-dose therapy, ophthalmologic
abnormalities, including cataracts and multiple punctate lenticular opacities,
have been noted in patients undergoing treatment with other quinolones. The
relationship of the drugs to these events is not presently established. CRYSTALLURIA
and CYLINDRURIA HAVE BEEN REPORTED with other quinolones.
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| dailymed-instance:warning |
In
the immature rat, the oral administration of ofloxacin at 5 to 16 times the
recommended maximum human dose based on mg/kg or 1���3 times based on
mg/mincreased the incidence and severity of osteochondrosis.
The lesions did not regress after 13 weeks of drug withdrawal. Other quinolones
also produce similar erosions in the weight-bearing joints and other signs
of arthropathy in immature animals of various species. Convulsions,
increased intracranial pressure, and toxic psychosis have been reported in
patients receiving quinolones, including ofloxacin. Quinolones, including
ofloxacin, may also cause central nervous system stimulation which may lead
to: tremors, restlessness/agitation, nervousness/anxiety, lightheadedness,
confusion, hallucinations, paranoia and depression, nightmares, insomnia,
and rarely suicidal thoughts or acts. These reactions may occur following
the first dose. If these reactions occur in patients receiving ofloxacin,
the drug should be discontinued and appropriatemeasures instituted. Insomnia
may be more common with ofloxacin than some other products in the quinolone
class. As with all quinolones, ofloxacin should be used with caution in patients
with a known or suspected CNS disorder that may predispose to seizures or
lower the seizure threshold (e.g., severe cerebral arteriosclerosis, epilepsy)
or in the presence of other risk factors that may predispose to seizures or
lower the seizure threshold (e.g., certain drug therapy, renal dysfunction).
(See PRECAUTIONS: General, Information
for Patients, Drug
Interactions and ADVERSE REACTIONS.) Hypersensitivity Reactions: Serious
and occasionally fatal hypersensitivity and/or anaphylactic reactions have
been reported in patients receiving therapy with quinolones, including ofloxacin.
These reactions often occur following the first dose. Some reactions have
been accompanied by cardiovascular collapse, hypotension/shock, seizure, loss
of consciousness, tingling, angioedema (including tongue, laryngeal, throat,
or facial edema/swelling), airway obstruction (including bronchospasm, shortness
of breath, and acute respiratory distress), dyspnea, urticaria, itching, and
other serious skin reactions. This drug should be discontinued immediately
at the first appearance of a skin rash or any other sign of hypersensitivity.
Serious acute hypersensitivity reactions may require treatment with epinephrine
and other resuscitative measures, including oxygen, intravenous fluids, antihistamines,
corticosteroids, pressor amines, and airway management, as clinically indicated.
(See PRECAUTIONS and ADVERSE
REACTIONS.) Other serious and sometimes
fatal events, some due to hypersensitivity, and some due to uncertain etiology,
have been reported rarely in patients receiving therapy with quinolones, including
ofloxacin. These events may be severe and generally occur following the administration
of multiple doses. Clinical manifestations may include one or more of the
following: The drug should be discontinued immediately at the first
appearance of skin rash, jaundice, or any other sign of hypersensitivity and
supportive measures instituted (See PRECAUTIONS:
Information for Patients and ADVERSE REACTIONS.)<br/>Peripheral neuropathy: Rare cases of sensory or sensorimotor axonal polyneuropathy
affecting small and/or large axons resulting in paresthesias, hypoesthesias,
dysesthesias and weakness have been reported in patients receiving quinolones,
including ofloxacin. Ofloxacin should be discontinued if the patient experiences
symptoms of neuropathy including pain, burning, tingling, numbness, and/or
weakness or other alterations of sensation including light touch, pain, temperature,
position sense, and vibratory sensation in order to prevent the development
of an irreversible condition. Clostridium
difficile associated diarrhea (CDAD) has been reported with use
of nearly all antibacterial agents, including FLOXIN 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.<br/>Tendon effects: Ruptures of the shoulder, hand, Achilles tendon or other
tendons that required surgical repair or resulted in prolonged disability
have been reported in patients receiving quinolones, including ofloxacin.
Post-marketing surveillance reports indicate that the risk is increased in
patients receiving corticosteroids, especially the elderly . Ofloxacin should
be discontinued if the patient experiences pain, inflammation, or rupture
of a tendon. Patients should rest and refrain from exercise until the diagnosis
of tendonitis or tendon rupture has been confidently excluded. Tendon rupture
can occur during or after therapy with quinolones, including ofloxacin. Ofloxacin has not been shown to be effective in the treatment
of syphilis. Antimicrobial agents used in high doses for short periods
of time to treat gonorrhea may mask or delay the symptoms of incubating syphilis.
All patients with gonorrhea should have a serologic test for syphilis at the
time of diagnosis. Patients treated with ofloxacin for gonorrhea should have
a follow-up serologic test for syphilis after three months and, if positive,
treatment with an appropriate antimicrobial should be instituted .
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To reduce the development of drug-resistant bacteria and
maintain the effectiveness of FLOXIN' (ofloxacin tablets) Tablets and
other antibacterial drugs, FLOXIN (ofloxacin tablets) Tablets
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. FLOXIN (ofloxacin
tablets) Tablets are indicated for the treatment of adults with mild to moderate
infections (unless otherwise indicated) caused by susceptible strains of the
designated microorganisms in the infections listed below. Please see DOSAGE AND ADMINISTRATION for specific recommendations. Acute
bacterial exacerbations of chronic bronchitis due to Haemophilus
influenzae or Streptococcus pneumoniae
. Community-acquired
Pneumonia due to Haemophilus influenzae
or Streptococcus pneumoniae. Uncomplicated skin and skin structure infections due
to Staphylococcus aureus, Streptococcus pyogenes,
or Proteus mirabilis. Acute, uncomplicated urethral and cervical gonorrhea due
to Neisseria gonorrhoeae. Nongonococcal urethritis and cervicitis due to Chlamydia trachomatis. Mixed Infections of the urethra and cervix due
to Chlamydia trachomatis and Neisseria gonorrhoeae. Acute pelvic inflammatory disease (including severe
infection) due to Chlamydia trachomatis and/or Neisseria gonorrhoeae. NOTE:
If anaerobic microorganisms are suspected of contributing to the infection,
appropriate therapy for anaerobic pathogens should be administered. Uncomplicated cystitis due to Citrobacter
diversus, Enterobacter aerogenes, Escherichia coli, Klebsiella pneumoniae,
Proteus mirabilis, or Pseudomonas aeruginosa
. Complicated urinary
tract infections due to Escherichia
coli, Klebsiella pneumoniae, Proteus mirabilis, Citrobacter diversusor Pseudomonas
aeruginosa. Prostatitis due to Escherichia
coli. Appropriate culture and susceptibility
tests should be performed before treatment in order to isolate and identify
organisms causing the infection and to determine their susceptibility to ofloxacin.
Therapy with ofloxacin may be initiated before results of these tests are
known; once results become available, appropriate therapy should be continued. As
with other drugs in this class, some strains of Pseudomonas
aeruginosa may develop resistance fairly rapidly during treatment
with ofloxacin. Culture and susceptibility testing performed periodically
during therapy will provide information not only on the therapeutic effect
of the antimicrobial agent but also on the possible emergence of bacterial
resistance.
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Floxin
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