Enter drug's generic or brand name below. Results will appear here. Note: all drug related information obtained on this page is provided by RX List.
Using the RX LIST database:
(1) Enter the drug name in the search box below and hit ENTER
(2) The rx list web site will open here with the drug search completed. Next, scroll down the page to locate the link to the drug you are searching for and then click on the link.
Gatifloxacin
(gatifloxacin) Ophthalmic Solution, 0.5%
Gatifloxacin sterile ophthalmic solution is an 8-methoxyfluoroquinolone anti-infective for the treatment of bacterial conjunctivitis. Its chemical name is (±)-1-Cyclopropyl-6-fluoro-1,4-dihydro-8-methoxy-7(3-methyl-1-piperazinyl)-4-oxo-3-quinolinecarboxylic acid, anhydrous. Its molecular formula is C19H22FN3O4, and its molecular weight is 375.4. Its chemical structure is:
 |
Gatifloxacin ophthalmic solution, 0.5% is a clear, pale yellow, sterile, preserved aqueous solution with an osmolality of 260-330 mOsm/kg and a pH of 5.1-5.7.
Gatifloxacin ophthalmic solution, 0.5% contains Active: gatifloxacin 0.5% (5 mg/mL); Inactives: benzalkonium chloride 0.005%; edetate disodium; hydrochloric acid; purified water; and sodium chloride. Hydrochloric acid and/or sodium hydroxide may be used to adjust pH to approximatelt 6.
TEQUIN®
(gatifloxacin) Tablets
(gatifloxacin) Injection
(gatifloxacin in 5% dextrose) Injection
TEQUIN® is available as TEQUIN (gatifloxacin) Tablets for oral administration and TEQUIN (gatifloxacin) Injection and TEQUIN (gatifloxacin in 5% dextrose) Injection for intravenous administration.
To reduce the development of drug-resistant bacteria and maintain the effectiveness of TEQUIN (gatifloxacin removed from us market - may 2006) and other antibacterial drugs, TEQUIN (gatifloxacin removed from us market - may 2006) should be used only to treat or prevent infections that are proven or strongly suspected to be caused by bacteria.
TEQUIN contains gatifloxacin, a synthetic broad-spectrum 8-methoxyfluoroquinolone antibacterial agent for oral or intravenous administration. Chemically, gatifloxacin is (±)-1-cyclopropyl-6-fluoro-1, 4-dihydro-8-methoxy-7-(3-methyl-1-piperazinyl)-4-oxo-3-quinolinecarboxylic acid sesquihydrate.
The chemical structure is:
Its empirical formula is C19H22FN3O4·1.5 H2O and its molecular weight is 402.42. Gatifloxacin is a sesquihydrate crystalline powder and is white to pale yellow in color. It exists as a racemate, with no net optical rotation. The solubility of the compound is pH dependent. The maximum aqueous solubility (40-60 mg/mL) occurs at a pH range of 2 to 5.
TEQUIN (gatifloxacin removed from us market - may 2006) Tablets
TEQUIN (gatifloxacin removed from us market - may 2006) Tablets are available as 200-mg and 400-mg white, film-coated tablets and contain the following inactive ingredients: hypromellose, magnesium stearate, methylcellulose, microcrystalline cellulose, polyethylene glycol, polysorbate 80, simethicone, sodium starch glycolate, sorbic acid, and titanium dioxide.
TEQUIN (gatifloxacin removed from us market - may 2006) Injection for Intravenous Administration
TEQUIN (gatifloxacin removed from us market - may 2006) Injection is available in 40-mL (400-mg) single-use vials as a sterile, preservative-free aqueous solution of gatifloxacin with pH ranging from 3.5 to 5.5. TEQUIN (gatifloxacin in 5% dextrose) Injection is also available in ready-to-use 100-mL (200-mg) and 200-mL (400-mg) flexible bags as a sterile, preservative-free aqueous solution of gatifloxacin with pH ranging from 3.5 to 5.5. The appearance of the intravenous solution may range from light yellow to greenish-yellow in color. The color does not affect nor is it indicative of product stability.
The intravenous formulation contains dextrose, anhydrous, USP or dextrose, monohydrate, USP and Water for Injection, USP, and may contain hydrochloric acid and/or sodium hydroxide for pH adjustment.
Gatifloxacin ophthalmic solution, 0.5% is indicated for the treatment of bacterial conjunctivitis caused by susceptible strains of the following organisms:
Staphylococcus aureus
Staphylococcus epidermidis
Streptococcus mitis group*
Streptococcus oralis*
Streptococcus pneumoniae
Haemophilus influenzae
*Efficacy for this organism was studied in fewer than 10 infections.
Patients 1 year of age or older: Instill one drop every two hours in the affected eye(s) while awake, up to 8 times on Day 1. Instill one drop two to four times daily in the affected eye(s) while awake on Days 2 through 7.
Six (6) mL bottle containing 2.5 mL of a 0.5% sterile topical ophthalmic solution.
Gatifloxacin ophthalmic solution, 0.5% is supplied sterile in a white, low density polyethylene (LDPE) bottle with a controlled dropper tip, and a tan cap in the following sizes:
2.5 mL in 6 mL bottle
Storage: Store at 20°-25°C (68°-77°F) [see USP Controlled Room Temperature]. Protect from freezing.
Manufactured by: Hi-Tech Pharmacal Co., Inc. Amityville, NY 11701, Revised: July 2013
TEQUIN (gatifloxacin) is indicated for the treatment of infections due to susceptible strains of the designated microorganisms in the conditions listed below (see DOSAGE AND ADMINISTRATION).
Acute bacterial exacerbation of chronic bronchitis due to Streptococcus pneumoniae, Haemophilus influenzae, Haemophilus parainfluenzae, Moraxella catarrhalis, or Staphylococcus aureus.
Acute sinusitis due to Streptococcus pneumoniae or Haemophilus influenzae.
Community-acquired pneumonia due to Streptococcus pneumoniae (including multidrug-resistant strains [MDRSP])*, Haemophilus influenzae, Haemophilus parainfluenzae, Moraxella catarrhalis, Staphylococcus aureus, Mycoplasma pneumoniae, Chlamydia pneumoniae, or Legionella pneumophila. (See Clinical Studies.)
Uncomplicated skin and skin structure infections (ie, simple abscesses, furuncles, folliculitis, wound infections, and cellulitis) due to Staphylococcus aureus (methicillin-susceptible strains only) or Streptococcus pyogenes.
NOTE: An insufficient number of patients with the diagnosis of impetiginous lesions were available for evaluation.
Uncomplicated urinary tract infections (cystitis) due to Escherichia coli, Klebsiella pneumoniae, or Proteus mirabilis.
Complicated urinary tract infections due to Escherichia coli, Klebsiella pneumoniae, or Proteus mirabilis.
Pyelonephritis due to Escherichia coli.
Uncomplicated urethral and cervical gonorrhea due to Neisseria gonorrhoeae. Acute, uncomplicated rectal infections in women due to Neisseria gonorrhoeae (see WARNINGS).
To reduce the development of drug-resistant bacteria and maintain the effectiveness of TEQUIN (gatifloxacin (removed from us market - may 2006)) and other antibacterial drugs, TEQUIN (gatifloxacin (removed from us market - may 2006)) 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.
*Multidrug-resistant Streptococcus pneumoniae (MDRSP) includes isolates previously known as PRSP (penicillin-resistant Streptococcus pneumoniae), and are strains resistant to two or more of the following antibiotics: penicillin (MIC 2 µg/mL), 2nd generation cephalosporins (eg, cefuroxime), macrolides, tetracyclines, and trimethoprim/ sulfamethoxazole.
The recommended dosage for TEQUIN (gatifloxacin (removed from us market - may 2006)) Tablets or TEQUIN (gatifloxacin (removed from us market - may 2006)) Injection is described in Table 4. Doses of TEQUIN (gatifloxacin (removed from us market - may 2006)) are administered once every 24 hours. These recommendations apply to all patients with a creatinine clearance ³40 mL/min. For patients with a creatinine clearance
THE SAFETY AND EFFECTIVENESS OF GATIFLOXACIN IN PEDIATRIC PATIENTS, ADOLESCENTS (LESS THAN 18 YEARS OF AGE), PREGNANT WOMEN, AND LACTATING WOMEN HAVE NOT BEEN ESTABLISHED (see PRECAUTIONS: Pediatric Use, Pregnancy, and Nursing Mothers).
QTc Interval Prolongation
Gatifloxacin has the potential to prolong the QTc interval of the electrocardiogram in some patients. QTc prolongation may lead to an increased risk for ventricular arrhythmias including torsades de pointes. Rare cases of torsades de pointes have been spontaneously reported during postmarketing surveillance in patients receiving quinolones, including gatifloxacin. Nearly all of these rare cases were associated with one or more of the following factors: age over 60, female gender, underlying cardiac disease, and/or use of multiple medications. No cardiovascular morbidity or mortality attributable to QTc prolongation has occurred in over 44,000 patients treated with gatifloxacin in clinical trials; these include 118 patients concurrently receiving drugs known to prolong the QTc interval and 139 patients known to have uncorrected hypokalemia (ECG monitoring was not performed). Gatifloxacin should be avoided in patients with known prolongation of the QTc interval, patients with uncorrected hypokalemia, and patients receiving class IA (quinidine, procainamide), or class III (amiodarone, sotalol) antiarrhythmic agents. (See CLINICAL PHARMACOLOGY: Electrocardiogram.)
Pharmacokinetic and pharmacodynamic studies between gatifloxacin and drugs that prolong the QTc interval such as cisapride, erythromycin, antipsychotics, and tricyclic antidepressants have not been performed. Gatifloxacin should be used with caution when given concurrently with these drugs, as well as in patients with ongoing proarrhythmic conditions, such as clinically significant bradycardia or acute myocardial ischemia.
The magnitude of QTc prolongation increases with increasing concentrations of the drug (see CLINICAL PHARMACOLOGY: Electrocardiogram); therefore, the recommended dose and the recommended intravenous infusion rate should not be exceeded (see DOSAGE AND ADMINISTRATION for dosing recommendations for patients with or without renal impairment).
Disturbances in Blood Glucose
Disturbances of blood glucose, including symptomatic hyper- and hypoglycemia, have been reported with TEQUIN (gatifloxacin (removed from us market - may 2006)) , usually in diabetic patients. Therefore, careful monitoring of blood glucose is recommended when TEQUIN (gatifloxacin (removed from us market - may 2006)) is administered to patients with diabetes (see CLINICAL PHARMACOLOGY, PRECAUTIONS: Information for Patients and Drug Interactions, and ANIMAL PHARMACOLOGY).
Studies conducted in non-infected patients with type 2 diabetes mellitus controlled on oral hypoglycemic agents have demonstrated that TEQUIN (gatifloxacin (removed from us market - may 2006)) is associated with disturbances in glucose homeostasis including an increase in serum insulin and decrease in serum glucose usually following administration of initial doses (ie, first 2 days of treatment), and sometimes associated with symptomatic hypoglycemia. Increases in fasting serum glucose were also observed, usually after the third day of TEQUIN (gatifloxacin (removed from us market - may 2006)) administration, continuing throughout the duration of treatment, and returning to baseline by 28 days after the cessation of gatifloxacin treatment in most patients.
During the postmarketing period, there have been reports of serious disturbances of glucose homeostasis in patients being treated with TEQUIN (gatifloxacin (removed from us market - may 2006)) . Hypoglycemic episodes, in some cases severe, have been reported in patients with diabetes mellitus treated with either sulfonylurea or non-sulfonylurea oral hypoglycemic medications. These events frequently occurred on the first day of therapy and usually within 3 days following the initiation of TEQUIN (gatifloxacin (removed from us market - may 2006)) . Hyperglycemic episodes, in some cases severe and associated with hyperosmolar non-ketotic hyperglycemic coma, were reported in diabetic patients, mostly between 4 and 10 days following the initiation of TEQUIN (gatifloxacin (removed from us market - may 2006)) therapy. Some of the hyperglycemic and hypoglycemic events were life-threatening and many required hospitalization, although these events were reversible when appropriately managed. Many of these patients had other underlying medical problems and were receiving concomitant medications that may have contributed to the glucose abnormality. Episodes of hyperglycemia, including hyperosmolar non-ketotic hyperglycemic coma, also occurred in patients not previously diagnosed with diabetes mellitus. Elderly patients who may have unrecognized diabetes, age-related decrease in renal function, underlying medical problems, and/or are taking concomitant medications associated with hyperglycemia may be at particular risk for serious hyperglycemia.
The dose of TEQUIN should be adjusted based on underlying renal function (see DOSAGE AND ADMINISTRATION). When TEQUIN (gatifloxacin (removed from us market - may 2006)) is used in diabetic patients, blood glucose should be closely monitored. Signs and symptoms of hypoglycemia should be monitored, especially during the first 3 days of therapy, and signs and symptoms of hyperglycemia should be monitored in diabetics and patients who may be at risk for hyperglycemia, especially with continued treatment with TEQUIN (gatifloxacin (removed from us market - may 2006)) beyond 3 days. If signs and symptoms of either hypoglycemia or hyperglycemia occur in any patient being treated with TEQUIN (gatifloxacin (removed from us market - may 2006)) , appropriate therapy must be initiated immediately and TEQUIN (gatifloxacin (removed from us market - may 2006)) should be discontinued.
Tendon Effects
Ruptures of the shoulder, hand, and Achilles tendon or other tendons that required surgical repair or resulted in prolonged disability have been reported in patients receiving quinolones, including gatifloxacin. Postmarketing surveillance reports indicate that this risk may be increased in patients receiving concomitant corticosteroids, especially the elderly. Gatifloxacin 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 excluded. Tendon rupture can occur during or after therapy with quinolones, including gatifloxacin.
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.
Other
As with other members of the quinolone class, gatifloxacin has caused arthropathy and/or chondrodysplasia in immature dogs. The relevance of these findings to the clinical use of gatifloxacin is unknown (see ANIMAL PHARMACOLOGY).
Convulsions, increased intracranial pressure, and psychosis have been reported in patients receiving quinolones. Quinolones may also cause central nervous system (CNS) stimulation, which may lead to tremors, restlessness, lightheadedness, confusion, hallucinations, paranoia, depression, nightmares, and insomnia. These reactions may occur following the first dose. If these reactions occur in patients receiving gatifloxacin, the drug should be discontinued and appropriate measures instituted (see ADVERSE REACTIONS).
As with other quinolones, TEQUIN (gatifloxacin (removed from us market - may 2006)) should be used with caution in patients with known or suspected CNS disorders, such as severe cerebral atherosclerosis, epilepsy, and other factors that predispose to seizures.
Serious and occasionally fatal hypersensitivity and/or anaphylactic reactions have been reported in patients receiving therapy with quinolones. These reactions may 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.
TEQUIN (gatifloxacin (removed from us market - may 2006)) should be discontinued 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).
Serious and sometimes fatal events, some due to hypersensitivity and some due to uncertain etiology, have been reported in patients receiving antibacterial therapy. These events may be severe and generally occur following the administration of multiple doses. Clinical manifestations may include one or more of the following: fever, rash or severe dermatologic reactions (eg, toxic epidermal necrolysis, Stevens-Johnson syndrome); vasculitis, arthralgia, myalgia, serum sickness; allergic pneumonitis, interstitial nephritis; acute renal insufficiency or failure; hepatitis, jaundice, acute hepatic necrosis or failure; anemia, including hemolytic and aplastic; thrombocytopenia, including thrombotic thrombocytopenic purpura; leukopenia; agranulocytosis; pancytopenia; and/or other hematologic abnormalities.
Pseudomembranous colitis has been reported with nearly all antibacterial agents, including TEQUIN (gatifloxacin (removed from us market - may 2006)) , and may range in severity from mild to life-threatening. It is important, therefore, to consider this diagnosis in patients who present with diarrhea subsequent to the administration of any antibacterial agent.
Treatment with antibacterial agents alters the flora of the colon and may permit overgrowth of clostridia. Studies indicate that a toxin produced by Clostridium difficile is the primary cause of "antibiotic-associated colitis."
After the diagnosis of pseudomembranous colitis has been established, therapeutic measures should be initiated. Mild cases of pseudomembranous colitis usually respond to drug discontinuation alone. In moderate to severe cases, consideration should be given to management with fluids and electrolytes, protein supplementation, and treatment with an antibacterial drug clinically effective against C. difficile colitis.
Gatifloxacin 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.
General
Prescribing TEQUIN (gatifloxacin (removed from us market - may 2006)) in the absence of 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.
Quinolones may cause central nervous system (CNS) events including nervousness, agitation, insomnia, anxiety, nightmares, or paranoia (see WARNINGS and PRECAUTIONS: Information for Patients).
Administer gatifloxacin with caution in the presence of renal insufficiency. Careful clinical observation and appropriate laboratory studies should be performed prior to and during therapy since elimination of gatifloxacin may be reduced. In patients with impaired renal function (creatinine clearance
Gatifloxacin is a fluoroquinolone antibacterial (see Microbiology).
Gatifloxacin ophthalmic solution 0.3% or 0.5% was administered to one eye of 6 healthy male subjects each in an escalated dosing regimen starting with a single 2 drop dose, then 2 drops 4 times daily for 7 days, and finally 2 drops 8 times daily for 3 days. At all time points, serum gatifloxacin levels were below the lower limit of quantification (5 ng/mL) in all subjects.
Gatifloxacin is an 8-methoxyfluoroquinolone with a 3-methylpiperazinyl substituent at C7. The antibacterial action of gatifloxacin results from inhibition of DNA gyrase and topoisomerase IV. DNA gyrase is an essential enzyme that is involved in the replication, transcription, and repair of bacterial DNA. Topoisomerase IV is an enzyme known to play a key role in the partitioning of the chromosomal DNA during bacterial cell division. The mechanism of action of fluoroquinolones including gatifloxacin is different from that of aminoglycoside, macrolide, and tetracycline antibiotics.
Therefore, gatifloxacin may be active against pathogens that are resistant to these antibiotics and these antibiotics may be active against pathogens that are resistant to gatifloxacin. There is no crossresistance between gatifloxacin and the aforementioned classes of antibiotics. Cross resistance has been observed between systemic gatifloxacin and some other fluoroquinolones.
Resistance to gatifloxacin in vitro develops via multiple-step mutations. Resistance to gatifloxacin in vitro occurs at a general frequency of 1 x 10-7 to 10-10.
Gatifloxacin has been shown to be active against most isolates of the following organisms both microbiologically and clinically, in conjunctival infections as described in the INDICATIONS AND USAGE section.
Staphylococcus aureus
Staphylococcus epidermidis
Streptococcus mitis group*
Streptococcus oralis*
Streptococcus pneumoniae
Haemophilus influenzae
*Efficacy for this organism was studied in fewer than 10 infections.
In two randomized, double-masked, multicenter clinical trials, where patients 1-89 years of age were dosed for 5 days, gatifloxacin ophthalmic solution was clinically superior to its vehicle on day 6 in patients with conjunctivitis and positive conjunctival cultures. Clinical outcomes for the trials demonstrated clinical success (resolution of conjunctival hyperaemia and conjunctival discharge) of 58% (193/333) for the gatifloxacin-treated groups versus 45% (148/325) for the vehicle-treated groups. Microbiological outcomes for the same clinical trials demonstrated a statistically superior eradication rate for causative pathogens of 90% (301/333) for gatifloxacin vs. 70% (228/325) for vehicle. Please note that microbiological eradication does not always correlate with clinical outcome in anti-infective trials.
Gatifloxacin is administered as a racemate, with the disposition and antibacterial activity of the R- and S-enantiomers virtually identical.
Absorption
Gatifloxacin is well absorbed from the gastrointestinal tract after oral administration and can be given without regard to food. The absolute bioavailability of gatifloxacin is 96%. Peak plasma concentrations of gatifloxacin usually occur 1-2 hours after oral dosing.
The oral and intravenous routes of administration for TEQUIN can be considered interchangeable, since the pharmacokinetics of gatifloxacin after 1-hour intravenous administration are similar to those observed for orally administered gatifloxacin when equal doses are administered (Figure 1) (see DOSAGE AND ADMINISTRATION).
Figure 1: Mean Plasma Concentration-Time Profiles of Gatifloxacin Following Intravenous (IV) and Oral (PO) Administration of a Single 400-mg Dose to Healthy Subjects.
Pharmacokinetics
The mean (SD) pharmacokinetic parameters of gatifloxacin following oral administration to healthy subjects with bacterial infections and subjects with renal insufficiency are listed in Table 1. The mean (SD) pharmacokinetic parameters of gatifloxacin following intravenous administration to healthy subjects are listed in Table 2.
| Table 1: Gatifloxacin Pharmacokinetic Parameters- Oral Administration | |||||||
Cmax (mg/mL) | Tmaxa (h) | AUCb (mg.h/mL) | T ½ (h) | Cl/F (mL/min) | C1R (mL/min) | UR (%) | |
200 mg - Healthy Volunteers | |||||||
Single dose (n=12) | 2.0 ±0.4 | 1.00 (0.50, 2.50) | 14.2 ± 0.4 | - | 241 ±40 | - | 73.8 ± 10.9 |
400 mg - Healthy Volunteers | |||||||
Single dose (n=202)c | 3.8 ±1.0 | 1.00 (0.50, 6.00) | 33.0 ± 6.2 | 7.8±1.3 | 210 ±44 | 151 ±46 | 72.4 ± 18.1 |
Multiple dose (n=18) | 4.2 ±1.3 | 1.50 (0.50, 4.00) | 34.4 ± 5.7 | 7.1±0.6 | 199 ±31 | 159 ±34 | 80.2 ±12.1 |
400 mg - Patients with Infection | |||||||
Multiple dose (n=140)d | 4.2 ±1.9 | - | 51.3±20.4 | - | 147 ±48 | - | - |
400 mg - Single Dose Subjects with Renal Insufficiency | |||||||
Clcr50 - 89 mL/min (n=8) | 4.4 ±1.1 | 1.13 (0.75-2.00) | 48.0 ± 12.7 | 11.2±2.8 | 148 ±41 | 124 ± 38 | 83.7±7.8 |
Clcr 30 - 49 mL/min (n=8) | 5.1 ±1.8 | 0.75 (0.50, 6.00) | 74.9 ± 12.6 | 17.2±8.5 | 92 ±17 | 67 ±24 | 71.1 ±17.4 |
Clcr 0.5 | Resistant (R) | ||||||
c These interpretive standards are applicable to agar dilution tests with GC agar base and 1% defined growth supplement.
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 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 gatifloxacin powder should provide the following MIC values:
Microorganism | MIC Range (µg/mL) |
|
Enterococcus faecalis ATCC 29212 | 0.12 - 1.0 |
|
Escherichia coli ATCC 25922 | 0.008 - 0.03 |
|
Haemophilus influenzae ATCC 49247d | 0.004 - 0.03 |
|
Neisseria gonorrhoeae ATCC 49226e | 0.002 - 0.016 |
|
Pseudomonas aeruginosa ATCC 27853 | 0.5 - 2.0 |
|
Staphylococcus aureus ATCC 29213 | 0.03 - 0.12 |
|
Streptococcus pneumoniae ATCC 49619f | 0.12 - 0.5 |
d This quality control range is applicable to only H. influenzae ATCC 49247 tested by a broth microdilution procedure using HTM. 1
e This quality control range is applicable to only N. gonorrhoeae ATCC 49226 tested by an agar dilution procedure using GC agar base with 1% defined growth supplement. 1
f This quality control range is applicable to only S. pneumoniae ATCC 49619 tested by a microdilution procedure using cation-adjusted Mueller-Hinton broth with 2-5% lysed horse blood. 1
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 procedure2 requires the use of standardized inoculum concentrations. This procedure uses paper disks impregnated with 5 µg gatifloxacin to test the susceptibility of microorganisms to gatifloxacin.
Reports from the laboratory providing results of the standard single-disk susceptibility test with a 5-µg gatifloxacin disk should be interpreted according to the following criteria:
The following zone diameter interpretive criteria should be used for testing
Enterobacteriaceae and Staphylococcus species:
Zone Diameter (mm) | Interpretation |
³18 | Susceptible (S) |
15 - 17 | Intermediate (I) |
£14 | Resistant (R) |
For testing Haemophilus influenzae and Hemophilus parainfluenzaeg:
Zone Diameter (mm) | Interpretation |
³18 | Susceptible (S) |
g This zone diameter standard is applicable only to tests with Haemophilus influenzae and Haemophilus parainfluenzae using Haemophilus Test Medium (HTM).2
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.
For testing Streptococcus pneumoniaeh:
Zone Diameter (mm) | Interpretation |
³21 | Susceptible (S) |
18 - 20 | Intermediate (I) |
£17 | Resistant (R) |
For testing Streptococcus species other than Streptococcus pneumoniaeh:
Zone Diameter (mm) | Interpretation |
³18 | Susceptible (S) |
15 - 17 | Intermediate (I) |
£14 | Resistant (R) |
h These zone diameter standards only apply to tests performed using Mueller-Hinton agar
supplemented with 5% sheep blood incubated in 5% CO2.2
For testing Neisseria gonorrhoeae i:
Zone Diameter (mm) | Interpretation |
³38 | Susceptible (S) |
34 - 37 | Intermediate (I) |
£33 | Resistant (R) |
i These interpretive standards are applicable to disk diffusion tests with GC agar base and 1% defined growth supplement incubated in 5% CO2.
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 gatifloxacin.2
As with standardized dilution techniques, 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-µg gatifloxacin disk should provide the following zone diameters in these laboratory quality control strains:
Microorganism | Zone Diameter Range (mm) |
|
Escherichia coli ATCC 25922 | 30-37 |
|
Haemophilus influenzae ATCC 49247j | 33-41 |
|
Neisseria gonorrhoeae ATCC 49226k | 45-56 |
|
Pseudomonas aeruginosa ATCC 27853 | 20-28 |
|
Staphylococcus aureus ATCC 25923 | 27-33 |
|
Streptococcus pneumoniae ATCC 49619l | 24-31 |
j This quality control range applies to tests conducted with Haemophilus influenzae ATCC 49247 using Haemophilus Test Medium (HTM)2.
k This quality control range is only applicable to tests conducted with N. gonorrhoeae ATCC 49226 performed by disk diffusion using GC agar base and 1% defined growth supplement2.
l This quality control range is applicable only to tests conducted with S. pneumoniae ATCC 49619 performed by disk diffusion using Mueller-Hinton agar supplemented with 5% defibrinated sheep blood.
CLINICAL STUDIES
Community-Acquired Bacterial Pneumonia and Community-Acquired Pneumonia Due to Multi-Drug Resistant Streptococcus pneumoniae (MDRSP)*
Clinical efficacy of gatifloxacin in the treatment of community-acquired bacterial pneumonia (CAP) was evaluated in two non-comparative Phase II/III studies and three Phase III studies comparing oral TEQUIN (gatifloxacin (removed from us market - may 2006)) to oral clarithromycin, TEQUIN (gatifloxacin (removed from us market - may 2006)) IV/oral to levofloxacin IV/oral, and TEQUIN (gatifloxacin (removed from us market - may 2006)) IV/oral to ceftriaxone IV (+/- erythromycin IV) with step-down to oral clarithromycin. Success rates for clinically evaluable patients with a bacterial pathogen isolated at baseline (see INDICATIONS AND USAGE) ranged from 88% to 90% for TEQUIN (gatifloxacin (removed from us market - may 2006)) -treated patients. Success rates were not statistically different from comparator therapy.
Gatifloxacin was also effective for the treatment of community-acquired pneumonia caused by multi-drug resistant Streptococcus pneumoniae (MDRSP) isolates. Of 27 clinically and microbiologically evaluable patients with MDRSP isolates obtained primarily from post-marketing studies of patients with CAP, 100% achieved clinical and bacteriological success post-therapy. The clinical cure rates and bacteriological success rates are shown in the table below.
*Multidrug-resistant Streptococcus pneumoniae (MDRSP) includes isolates previously known as PRSP (penicillin-resistant Streptococcus pneumoniae), and are strains resistant to two or more of the following antibiotics: penicillin (MIC 2 µg/mL), 2nd generation cephalosporins (eg, cefuroxime), macrolides, tetracyclines, and trimethoprim/ sulfamethoxazole.
Table 6: Clinical and Bacteriological Success Rates for Gatifloxacin- Treated MDRSP CAP Patients (Population: Valid for Efficacy) | |||
Screening Susceptibility | Clinical Success n/Na | Bacteriological Success n/Nb | |
|
Penicillin-resistant | 10/10 (100%) | 10/10 (100%) | |
|
2nd generation cephalosporin-resistant* | 13/13 (100%) | 13/13 (100%) | |
|
Macrolide-resistant** | 24/24 (100%) | 24/24 (100%) | |
|
Trimethoprim/sulfamethoxazole-resistant | 12/12 (100%) | 12/12 (100%) | |
|
Tetracylcine-resistant | 14/14 (100%) | 14/14 (100%) | |
|
a n = number of patients successfully treated; N = number of clinically evaluable patients with MDRSP (froma total of 27 patients). | |||
|
b n = number of patients successfully treated (presumed eradication or eradication); N = number of microbiologically evaluable patients with MDRSP (from a total of 27 patients). | |||
|
* 2nd generation cephalosporin tested was cefuroxime. | |||
|
** Clarithromycin and erythromycin were the macrolide antimicrobials tested. | |||
Not all isolates were resistant to all antimicrobial classes tested. Success and eradication rates are summarized in the table below.
Table 7: Clinical Success and Bacteriological Eradication Rates for Gatifloxacin-Treated MDRSP CAP Patients (Population: Valid for Efficacy) | ||
Streptococcus pneumoniae with MDRSP | Clinical Success Rate | Bacteriological Eradication Rate |
|
Resistant to at least 2 antimicrobials | 12/12 (100%) | 12/12 (100%) |
|
Resistant to at least 3 antimicrobials | 12/12 (100%) | 12/12 (100%) |
|
Resistant to at least 4 antimicrobials | 2/2 (100%) | 2/2 (100%) |
|
Resistant to at least 5 antimicrobials | 1/1 (100%) | 1/1 (100%) |
|
Bacteremias with MDRSP | 3/3 (100%) | 3/3 (100%) |
REFERENCES
1. National Committee for Clinical Laboratory Standards. Methods for Dilution Antimicrobial Susceptibility Tests for Bacteria That Grows Aerobically - Fifth Edition; Approved Standard, NCCLS Document M7-A5, Vol. 20, No. 2, NCCLS, Wayne, PA, January 2000.
2. National Committee for Clinical Laboratory Standards. Performance Standards for Antimicrobial Disk Susceptibility Tests - Seventh Edition; Approved Standard, NCCLS Document M2-A7, Vol. 20, No. 1, NCCLS, Wayne, PA, January 2000.
Patients should be instructed to avoid contaminating the applicator tip with material from the eye, fingers, or other source.
Patients should be advised not to wear contact lenses if they have signs and symptoms of bacterial conjunctivitis.
TEQGUIN®
(gatifloxacin)
200 mg and 400 mg Tablets
This section contains important information about TEQUIN (gatifloxacin) that you should read before you begin treatment. This section does not list all the benefits and risks of TEQUIN (gatifloxacin (removed from us market - may 2006)) and does not take the place of discussions with your doctor or healthcare professional about your medical condition or your treatment. If you have questions, talk with your healthcare professional. The medicine described here can only be prescribed by a licensed healthcare professional. Only your healthcare professional can determine if TEQUIN (gatifloxacin (removed from us market - may 2006)) is right for you.
What is TEQUIN (gatifloxacin (removed from us market - may 2006)) ?
TEQUIN (gatifloxacin (removed from us market - may 2006)) (pronounced TEK win) is an antibiotic used to treat lung, sinus, skin, or urinary tract infections, and also to treat certain sexually transmitted diseases caused by germs called bacteria. TEQUIN (gatifloxacin (removed from us market - may 2006)) kills many of the kinds of bacteria that can infect the lungs, sinus, skin, and urinary tract and that cause certain sexually transmitted diseases. TEQUIN (gatifloxacin (removed from us market - may 2006)) has been shown in a large number of clinical trials to be safe and effective for the treatment of bacterial infections.
Sometimes viruses, rather than bacteria, may infect the lungs and sinuses (for example, the common cold). TEQUIN (gatifloxacin (removed from us market - may 2006)) , like all other antibiotics, does not kill viruses.
The sexually transmitted disease called gonorrhea is treated by TEQUIN (gatifloxacin (removed from us market - may 2006)) . Other diseases called syphilis or non-gonococcal disease are not treated by TEQUIN (gatifloxacin (removed from us market - may 2006)) .
You should contact your doctor if you think your condition is not improving while taking TEQUIN (gatifloxacin (removed from us market - may 2006)) . TEQUIN (gatifloxacin (removed from us market - may 2006)) Tablets are white and contain either 200 mg or 400 mg of active drug.
How and when should I take TEQUIN (gatifloxacin (removed from us market - may 2006)) ?
TEQUIN (gatifloxacin (removed from us market - may 2006)) should be taken once a day for 1 to 14 days depending on your prescription. It should be swallowed whole and may be taken with or without food. Try to take the tablet at the same time each day.
You may begin to feel better quickly; however, in order to make sure that all bacteria are killed, you should complete the full course of medication. Do not take more than the prescribed dose of TEQUIN (gatifloxacin (removed from us market - may 2006)) . Try not to miss a dose, but if you do, take it as soon as possible. If it is almost time for the next dose, skip the missed dose and continue your regular dose.
Who should not take TEQUIN (gatifloxacin (removed from us market - may 2006)) ?
You should avoid TEQUIN (gatifloxacin (removed from us market - may 2006)) if you have ever had a severe allergic reaction to any medicine in the group of antibiotics known as "quinolones" such as CIPRO® (ciprofloxacin) or LEVAQUIN®(levofloxacin).
You should avoid TEQUIN (gatifloxacin (removed from us market - may 2006)) if you have a rare condition known as congenital prolongation of the QTc interval. If any of your family members have this condition, you should inform your healthcare professional.
You should avoid TEQUIN (gatifloxacin (removed from us market - may 2006)) if you are being treated for heart rhythm disturbances with certain medicines such as quinidine, procainamide, amiodarone, or sotalol. Inform your healthcare professional if you are taking a heart rhythm drug.
You should avoid TEQUIN (gatifloxacin (removed from us market - may 2006)) if you have a condition known as hypokalemia (low blood potassium). Hypokalemia may be caused by medicines called diuretics such as furosemide and hydrochlorothiazide. If you are taking a diuretic you should speak with your healthcare professional.
If you are pregnant or planning to become pregnant while taking TEQUIN (gatifloxacin (removed from us market - may 2006)) , talk to your doctor before taking this medication. TEQUIN (gatifloxacin (removed from us market - may 2006)) is not recommended for use during pregnancy or nursing, as the effects on the unborn child or nursing infant are unknown.
TEQUIN (gatifloxacin (removed from us market - may 2006)) is not recommended for children.
What about other medications I am taking?
It is important to let your healthcare provider know all of the medicines that you are using.
· It is important to let your healthcare provider know if you are taking certain medicines that can have an effect on an electrocardiogram test, such as cisapride, erythromycin, some antidepressants, and some antipsychotic drugs.
· You should tell your healthcare professional if you are taking medicines called diuretics (also sometimes called water pills) such as furosemide and hydrochlorothiazide, because diuretics can sometimes cause low potassium.
· If you have diabetes, it is important to let your healthcare provider know that you have this condition and what medications you are taking for it.
· Many antacids and multivitamins may interfere with the absorption of TEQUIN (gatifloxacin (removed from us market - may 2006)) and may prevent it from working properly. You should take TEQUIN (gatifloxacin (removed from us market - may 2006)) 4 hours before taking these products.
What are the possible side effects of TEQUIN (gatifloxacin (removed from us market - may 2006)) ?
TEQUIN (gatifloxacin (removed from us market - may 2006)) is generally well tolerated. The most common side effects that can occur when taking TEQUIN (gatifloxacin (removed from us market - may 2006)) are usually mild and include nausea, vomiting, stomach pain, diarrhea, dizziness, and headache. You should be careful about driving or operating machinery until you are sure TEQUIN (gatifloxacin (removed from us market - may 2006)) does not cause dizziness. If you notice any side effects not mentioned in this section or if you have any question or concerns about the side effects you are experiencing, please discuss them with your healthcare professional.
In a few people, TEQUIN (gatifloxacin (removed from us market - may 2006)) , like some other antibiotics, may produce a small effect on the heart that is seen on an electrocardiogram test. Although this did not cause any problems in patients who took TEQUIN (gatifloxacin (removed from us market - may 2006)) in premarketing clinical trials, in theory, it could result in extremely rare cases of abnormal heartbeat, which may be dangerous. Contact your healthcare professional if you develop heart palpitations (fast beating) or have fainting spells.
Disturbances of blood sugar, including symptoms of high blood sugar (hyperglycemia) and low blood sugar (hypoglycemia), have been reported with TEQUIN (gatifloxacin (removed from us market - may 2006)) in diabetic patients. Elderly patients with additional medical problems or taking additional medications may also be at risk for high blood sugar. If you develop low blood sugar while on TEQUIN (gatifloxacin (removed from us market - may 2006)) , you should take immediate measures to increase your blood sugar, stop taking TEQUIN (gatifloxacin (removed from us market - may 2006)) , and contact your healthcare professional at once. If you develop high blood sugar while on TEQUIN (gatifloxacin (removed from us market - may 2006)) , you should contact your healthcare professional at once before taking additional TEQUIN (gatifloxacin (removed from us market - may 2006)) . If you have diabetes or suspect that you may have diabetes, discuss how to detect changes in your blood sugar with your healthcare professional at once before taking additional TEQUIN (gatifloxacin (removed from us market - may 2006)) .
Where can I get more information about TEQUIN (gatifloxacin (removed from us market - may 2006)) ?
This section is a summary of the most important information about TEQUIN (gatifloxacin (removed from us market - may 2006)) . It does not include everything there is to know about TEQUIN (gatifloxacin (removed from us market - may 2006)) . If you have any questions or problems, you should talk to your doctor or healthcare provider. There is also a leaflet (Package Insert) written for healthcare professionals that your pharmacist can let you read. You may want to read this information and discuss it with your doctor or other healthcare professional. Remember, no written information can replace careful discussion with your doctor.
Remember
· Take your dose of TEQUIN (gatifloxacin (removed from us market - may 2006)) once a day.
· Complete the course of medication (take all of the pills) even if you are feeling better.
· Do not use TEQUIN (gatifloxacin (removed from us market - may 2006)) for another condition or give it to others.
· Store TEQUIN (gatifloxacin (removed from us market - may 2006)) tablets at room temperature in a tightly sealed container.
· Throw away TEQUIN (gatifloxacin (removed from us market - may 2006)) when it is outdated or no longer needed by flushing it down the toilet.
· Keep this and all medications out of reach of children.
