Gemglow™
 Generic
Gemifloxacin
Therapeutic Area
Antibiotic
Composition and Strengths
Gemifloxacin is a synthetic broad spectrum
antibacterial agent for oral administration. Gemifloxacin is related to the
fluoroquinolone class of antibiotics, available as the mesylate salt in the
sesquihydrate form. Chemically, gemiloxacin is (R,S)-7-[(4Z)-3-(aminomethyl)-4-(methoxyimino)-1-pyrrolidinyl]-
1-cycloproplyl-6-fluoro-1, 4-dihydro-4-oxo-1,8-naphthyridine-3-carboxylic acid
(C18H20FN5O4CH4O3S)
Product Descriptions and Properties
Mechanism of Action
Gemifloxacin inhibits two specific enzymes, DNA gyrase and DNA topoisomerase IV,
which aid in bacterial DNA replication. Gemifloxacin displays strong binding
affinity at both of these target sites, which helps maintain high potency
against resistant S. pneumoniae. This dual targeting with Gemifloxacin is
achievable at therapeutic drug levels.
Pharmacokinetics
The pharmacokinetics
of Gemifloxacin are approximately linear over the dose range from 40mg to 640mg.
There was minimal accumulation of Gemifloxacin following multiple oral doses up
to 640mg a day for 7 days (mean accumulation <20%). Following repeat oral
administration of 320mg Gemifloxacin once daily, steady-state is achieved by the
third day of dosing.
Absorption
and Bioavailability
Gemifloxacin is rapidly absorbed from the
gastrointestinal tract. Peak plasma concentrations of Gemifloxacin were observed
between 0.5 and 2 hours following oral tablet administration and the absolute
bioavailability of the 320mg tablet averaged approximately 71% (95% CI 60%-84%).
Following repeat oral doses of 320mg to healthy subjects, the mean ± SD maximal
Gemifloxacin plasma concentrations (Cmax) and systemic drug exposure (AUC(0-24))
were 1.61 ± 0.51 µg/mL (range 0.70-2.62 µg/mL) and 9.93 ± 3.07 µg/mL (range
4.71-20.1 µg/mL), respectively. In patients with respiratory and urinary tract
infections (n=1423), similar estimates of systemic drug exposure were determined
using a population pharmacokinetics analysis (geometric mean AUC(0-24), 8.36 µg/mL;
range 3.2 - 47.7 µg/mL. The pharmacokinetics of Gemifloxacin were not
significantly altered when a 320mg dose was administered with a high-fat meal.
Therefore Gemifloxacin tablets may be administered without regard to meals.
Distribution
In vivo plasma protein binding in healthy elderly
and young subjects ranged from 55% to 73% and was unaffected by age. Renal
impairment does not significantly affect the protein binding of Gemifloxacin.
The blood-to-plasma concentration ratio of Gemifloxacin was 1.2:1. Gemifloxacin
is widely distributed throughout the body after oral administration.
Concentrations of Gemifloxacin in bronchoalveolar lavage fluid exceed those in
the plasma. Gemifloxacin penetrates well into lung tissue and fluids
Indications
Gemglow TM (Gemifloxacin)
tablets are indicated for the treatment of following bacterial infections. Acute
bacterial sinusitis. Acute bacterial exacerbation of chronic bronchitis.
Community acquired pneumonia. Un-complicated Urinary tract infection. Acute
pyelonephiritis
Warning and Precautions
General
Prescribing Gemifloxacin in the absence of a proven or strongly suspected
bacterial infection is unlikely to provide benefit to the patient and increases
the risk of the development of drug-resistant bacteria.
Rash
In clinical studies, the overall rate of drug-related rash was 2.8%. The most
common form of rash associated with Gemifloxacin was described as maculopapular
and mild to moderate in severity; 0.3% was described as urticarial in
appearance. There were no documented cases in the clinical trials of more
serious skin reactions known to be associated with significant morbidity or
mortality. Rash was observed in patients <40 years of age, especially females
and post-menopausal females taking hormone replacement therapy. Prolonging
duration of therapy beyond 7 days causes the incidence of rash to increase
significantly in all subgroups except men over the age of 40. Gemifloxacin
therapy should be discontinued in patients developing a rash while on treatment.
Phototoxicity
Photosensitivity reactions have been reported very rarely in clinical trials
with Gemifloxacin. However, as with all drugs of this class, it is recommended
that patients avoid unnecessary exposure to strong sunlight or artificial UV
rays (e.g., sunlamps, solariums), and should be advised of the appropriate use
of broad spectrum sun block if in bright sunlight. Treatment should be
discontinued if a photosensitivity reaction is suspected.
Hepatic Effects
There were no clinical symptoms associated with these liver enzyme elevations.
The recommended dose of Gemglow 320 mg daily should not be exceeded. Alteration
of the dosage regimen is necessary for patients with impairment of renal
function (creatinine clearance -40 mL/min). Adequate hydration of patients
receiving Gemifloxacin should be maintained to prevent the formation of a highly
concentrated urine.
Pregnancy
The safety of Gemifloxacin in pregnant women has not been established.
Gemifloxacin should not be used in pregnant women unless the potential benefit
to the mother outweighs the risk to the fetus. There are no adequate and
well-controlled studies in pregnant women.
Nursing Mothers
Gemifloxacin is excreted in the breast milk of rats. There is no information on
excretion of Gemifloxacin into human milk. Therefore, Gemifloxacin should not be
used in lactating women unless the potential benefit to the mother outweighs the
risk.
Drug Interactions
Administration of
repeat doses of Gemifloxacin had no effect on the repeat dose pharmacokinetics
of theophylline, digoxin or an ethinyiestradiol/levonorgestrol oral
contraceptive product in healthy subjects.
Concomitant administration of Gemifloxacin and calcium carbonate, cimetidine,
omeprazole, or an estrogen/progesterone oral contraceptive produced minor
changes in the pharmacokinetics of gemifloxacin, which were considered to be
without clinical significance.
Concomitant administration of Gemifloxacin with probenecid resulted in a 45%
increase in systemic exposure to Gemifloxacin.
Gemifloxacin had no significant effect on the anticoagulant effect of warfarin
in healthy subjects on stable warfarin therapy. However, because some quinolones
have been reported to enhance the anticoagulant effects of warfarin or its
derivatives in patients, the prothrombin time or other suitable coagulation test
should be closely monitored if a quinolone antimicrobial is administered
concomitantly with warfarin or its derivatives.
The absorption of oral Gemifloxacin is significantly reduced by the concomitant
administration of an antacid containing aluminum and magnesium. Magnesium and/or
aluminum-containing antacids, products containing ferrous sulfate, multivitamin
preparations containing zinc or other metal cations should not be taken within 3
hours before or 2 hours after Gemifloxacin. Sucralfate should not be taken
within 2 hours of Gemifloxacin.
Side Effects
Drug-related adverse
events, classified as possibly or probably related with a frequency of •1% for
patients receiving 320mg of Gemifloxacin versus comparator drug (beta-Iactam
antibiotics, macrolides or other fluoroquinolones) are as follows: diarrhoea
3.6% vs. 4.6%; rash 2.8% vs. 0.6%; nausea 2.7% vs. 3.2%; headache 1.2% vs. 1.5%;
abdominal pain 0.9% vs. 1.1%; vomiting 0.9% vs. 1.1%; dizziness 0.8% vs. 1.5%;
and taste perversion 0.3% vs. 1.9%. Gemifloxacin appears to have a low potential
for photosensitivity. In clinical trials, treatment-related photosensitivity
occurred in only 0.039% (3/7659) of patients. Additional drug-related adverse
events (possibly or probably related) in >0.1% to 1% of patients who received
320 mg of Gemifloxacin were: abdominal pain, anorexia, arthralgia, constipation,
dermatitis, dizziness, dry mouth, dyspepsia, fatigue, flatulence, fungal
infection, gastritis, genital moniliasis, hyperglycemia, insomnia, leukopenia,
moniliasis, pruritus, somnolence, taste perversion, thrombocythemia, urticaria,
vaginitis, and vomiting.
Dosage And Administration
One 320 mg tablet once daily
Presentations Available
Gemifloxacin
320mg tablets are available in alu-alu blister pack of 7's
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