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Actions of Levofloxacin 0.5.% TOA in details
Pharmacology: Mechanism of Action: The main mechanism of action of Levofloxacin 0.5.% TOA is the inhibition of DNA gyrase. It is 2-fold stronger than that of ofloxacin. There is not much difference between the minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC). The activity of Levofloxacin 0.5.% TOA is bactericidal. In the observation of bacterial morphology, bacteriolysis can be seen in the concentration around MIC.
Orally administered Levofloxacin 0.5.% TOA is rapidly and almost completely absorbed with peak plasma concentrations being obtained within 1 hr. The absolute bioavailability is approximately 100%. Food has little effect on the absorption of Levofloxacin 0.5.% TOA.
Distribution in Plasma: Approximately 30-40% of Levofloxacin 0.5.% TOA is bound to serum protein. Multiple dosing with Levofloxacin 0.5.% TOA 500 mg once daily showed neglible accumulation. There is modest but predictable accumulation of Levofloxacin 0.5.% TOA after doses of 500 mg twice daily. Steady state is achieved within 3 days.
Penetration into Tissues and Body Fluids: Penetration into Bronchial Mucosa, Epithelial Lining Fluid (ELF): Maximum Levofloxacin 0.5.% TOA concentrations in bronchial mucosa and ELF were 8.3 mcg/mL and 10.8 mcg/mL, respectively. These were reached approximately 1 hr after administration.
Penetration into Lung Tissue: Maximum Levofloxacin 0.5.% TOA concentrations in lung tissues were approximately 11.3 mcg/mL and were reached between 4-6 hrs after administration.
Metabolism: Levofloxacin 0.5.% TOA is metabolised to a very small extent, the metabolites being desmethyl-Levofloxacin 0.5.% TOA and Levofloxacin 0.5.% TOA N-oxide. These metabolites account for <5% of the dose excretion in urine. Levofloxacin 0.5.% TOA is stereochemically stable and does not undergo chiral inversion.
Elimination: Following oral and IV administration, Levofloxacin 0.5.% TOA is eliminated relatively slowly from the plasma (half-life: 6-8 hrs). Excretion is primarily by the renal route (>85% of the administered dose).
Microbiology: Levofloxacin 0.5.% TOA is a broad-spectrum antibacterial agent against gram-positive and gram-negative bacteria including anaerobes. Levofloxacin 0.5.% TOA has shown strong antibacterial activities against Staphylococcus spp, Streptococcus pneumoniae, Streptococcus pyogenes, Streptococcus hemolyticus, Enterobacter spp, Escherichia coli, Klebsiella spp, Serratia spp, Enterococcus spp, Proteus spp and other glucose nonfermentative gram-negative rods, Pseudomonas aeruginosa, Haemophilus influenzae and Neisseria gonorrhoeae. Morever, Levofloxacin 0.5.% TOA has shown antibacterial activity against Chlamydia trachomatis. Levofloxacin 0.5.% TOA has an excellent protective and treatment effects in mice.
How should I take Levofloxacin 0.5.% TOA?
Take Levofloxacin 0.5.% TOA only as directed by your doctor. Do not take more of it, do not take it more often, and do not take it for a longer time than your doctor ordered.
Levofloxacin 0.5.% TOA comes with a Medication Guide. Read and follow the instructions carefully. Ask your doctor if you have any questions.
Levofloxacin 0.5.% TOA oral liquid should be taken 1 hour before or 2 hours after eating. You may measure your dose with a marked measuring spoon, oral syringe, or medicine cup.
Levofloxacin 0.5.% TOA tablets may be taken with meals or on an empty stomach.
Levofloxacin 0.5.% TOA is best taken with a full glass (8 ounces) of water. Several additional glasses of water should be taken every day, unless otherwise directed by your doctor. Drinking extra water will help to prevent some unwanted effects of Levofloxacin 0.5.% TOA.
Levofloxacin 0.5.% TOA works best when there is a constant amount in the blood. To help keep the amount constant, do not miss any doses. Also, it is best to take the doses at evenly spaced times, day and night. For example, if you are to take one dose a day, try to take it at the same time each day.
If you need to take Levofloxacin 0.5.% TOA for anthrax infection or plague, your doctor will want you to begin taking it as soon as possible after you are exposed to anthrax or bacteria causing the plague.
If you are taking aluminum or magnesium-containing antacids, iron supplements, multivitamins, didanosine (Videx®), sucralfate (Carafate®), or zinc, do not take them at the same time that you take Levofloxacin 0.5.% TOA. It is best to take these medicines at least 2 hours before or 2 hours after taking Levofloxacin 0.5.% TOA. These medicines may keep Levofloxacin 0.5.% TOA from working properly.
Keep using Levofloxacin 0.5.% TOA for the full treatment time, even if you feel better after the first few doses. Your infection may not clear up if you stop using the medicine too soon.
The dose of Levofloxacin 0.5.% TOA will be different for different patients. Follow your doctor's orders or the directions on the label. The following information includes only the average doses of Levofloxacin 0.5.% TOA. If your dose is different, do not change it unless your doctor tells you to do so.
The amount of medicine that you take depends on the strength of the medicine. Also, the number of doses you take each day, the time allowed between doses, and the length of time you take the medicine depend on the medical problem for which you are using the medicine.
- For oral dosage forms (oral solution or tablets):
- For treatment of an infection:
- Adults—250 to 750 milligrams (mg) once a day.
- Children—Use and dose must be determined by your doctor.
- For preventing anthrax infection:
- Adults—500 milligrams (mg) once a day.
- Children 6 months of age and older and weighing more than 50 kilograms (kg)—500 mg once a day.
- Children 6 months of age and older and weighing less than 50 kg—Dose is based on body weight and must be determined by your doctor. The dose is usually 8 mg per kg of body weight per dose, given two times a day. However, the dose is usually not more than 250 mg.
- Infants younger than 6 months of age—Use and dose must be determined by your doctor.
- For treatment and prevention of plague:
- Adults—500 milligrams (mg) once a day.
- Children 6 months of age and older, weighing more than 50 kilograms (kg)—500 mg once a day.
- Children 6 months of age and older, weighing less than 50 kg—Dose is based on body weight and must be determined by your doctor. The dose is usually 8 mg per kg of body weight per dose, given two times a day. However, the dose is usually not more than 250 mg.
- Infants younger than 6 months of age—Use and dose must be determined by your doctor.
- For treatment of an infection:
If you miss a dose of Levofloxacin 0.5.% TOA, take it as soon as possible. However, if it is almost time for your next dose, skip the missed dose and go back to your regular dosing schedule. Do not double doses.
Store the medicine in a closed container at room temperature, away from heat, moisture, and direct light. Keep from freezing.
Keep out of the reach of children.
Do not keep outdated medicine or medicine no longer needed.
Ask your healthcare professional how you should dispose of any medicine you do not use.
Levofloxacin 0.5.% TOA administration
Take exactly as prescribed by your doctor. Do not take in larger or smaller amounts or for longer than recommended. Follow the directions on your prescription label.
Take Levofloxacin 0.5.% TOA with a full glass of water (8 ounces). Drink several extra glasses of fluid each day while you are taking Levofloxacin 0.5.% TOA. You may take Levofloxacin 0.5.% TOA tablets with or without food.
Take Levofloxacin 0.5.% TOA oral solution (liquid) on an empty stomach 1 hour before or 2 hours after meals. Measure liquid medicine with a special dose-measuring spoon or cup, not a regular table spoon. If you do not have a dose-measuring device, ask your pharmacist for one.
Take this medication for the full prescribed length of time. Your symptoms may improve before the infection is completely cleared. Skipping doses may also increase your risk of further infection that is resistant to antibiotics. Levofloxacin 0.5.% TOA will not treat a viral infection such as the common cold or flu.
This medication can cause you to have a false positive drug screening test. If you provide a urine sample for drug screening, tell the laboratory staff that you are taking Levofloxacin 0.5.% TOA.
Store at room temperature away from moisture and heat. Do not allow the liquid medicine to freeze.
Levofloxacin 0.5.% TOA pharmacology
Mechanism Of Action
Levofloxacin 0.5.% TOA is a member of the fluoroquinolone class of antibacterial agents.
The mean ± SD pharmacokinetic parameters of Levofloxacin 0.5.% TOA determined under single and steady-state conditions following oral tablet, oral solution, or intravenous (IV) doses of Levofloxacin 0.5.% TOA are summarized in Table 8.
Table 8: Mean ± SD Levofloxacin 0.5.% TOA PK Parameters
Figure 3: Mean Levofloxacin 0.5.% TOA Plasma Concentration vs. Time Profile: 500 mg
The mean volume of distribution of Levofloxacin 0.5.% TOA generally ranges from 74 to 112 L after single and multiple 500 mg or 750 mg doses, indicating widespread distribution into body tissues. Levofloxacin 0.5.% TOA reaches its peak levels in skin tissues and in blister fluid of healthy subjects at approximately 3 hours after dosing. The skin tissue biopsy to plasma AUC ratio is approximately 2 and the blister fluid to plasma AUC ratio is approximately 1 following multiple once-daily oral administration of 750 mg and 500 mg doses of Levofloxacin 0.5.% TOA, respectively, to healthy subjects. Levofloxacin 0.5.% TOA also penetrates well into lung tissues. Lung tissue concentrations were generally 2- to 5-fold higher than plasma concentrations and ranged from approximately 2.4 to 11.3 mcg/g over a 24-hour period after a single 500 mg oral dose.
In vitro, over a clinically relevant range (1 to 10 mcg/mL) of serum/plasma Levofloxacin 0.5.% TOA concentrations, Levofloxacin 0.5.% TOA is approximately 24 to 38% bound to serum proteins across all species studied, as determined by the equilibrium dialysis method. Levofloxacin 0.5.% TOA is mainly bound to serum albumin in humans. Levofloxacin 0.5.% TOA binding to serum proteins is independent of the drug concentration.
Levofloxacin 0.5.% TOA is stereochemically stable in plasma and urine and does not invert metabolically to its enantiomer, D-ofloxacin. Levofloxacin 0.5.% TOA undergoes limited metabolism in humans and is primarily excreted as unchanged drug in the urine. Following oral administration, approximately 87% of an administered dose was recovered as unchanged drug in urine within 48 hours, whereas less than 4% of the dose was recovered in feces in 72 hours. Less than 5% of an administered dose was recovered in the urine as the desmethyl and N-oxide metabolites, the only metabolites identified in humans. These metabolites have little relevant pharmacological activity.
Levofloxacin 0.5.% TOA is excreted largely as unchanged drug in the urine. The mean terminal plasma elimination half-life of Levofloxacin 0.5.% TOA ranges from approximately 6 to 8 hours following single or multiple doses of Levofloxacin 0.5.% TOA given orally or intravenously. The mean apparent total body clearance and renal clearance range from approximately 144 to 226 mL/min and 96 to 142 mL/min, respectively. Renal clearance in excess of the glomerular filtration rate suggests that tubular secretion of Levofloxacin 0.5.% TOA occurs in addition to its glomerular filtration. Concomitant administration of either cimetidine or probenecid results in approximately 24% and 35% reduction in the Levofloxacin 0.5.% TOA renal clearance, respectively, indicating that secretion of Levofloxacin 0.5.% TOA occurs in the renal proximal tubule. No Levofloxacin 0.5.% TOA crystals were found in any of the urine samples freshly collected from subjects receiving Levofloxacin 0.5.% TOA.
There are no significant differences in Levofloxacin 0.5.% TOA pharmacokinetics between young and elderly subjects when the subjects' differences in creatinine clearance are taken into consideration. Following a 500 mg oral dose of Levofloxacin 0.5.% TOA to healthy elderly subjects (66–80 years of age), the mean terminal plasma elimination half-life of Levofloxacin 0.5.% TOA was about 7.6 hours, as compared to approximately 6 hours in younger adults. The difference was attributable to the variation in renal function status of the subjects and was not believed to be clinically significant. Drug absorption appears to be unaffected by age. Levofloxacin 0.5.% TOA dose adjustment based on age alone is not necessary.
The pharmacokinetics of Levofloxacin 0.5.% TOA following a single 7 mg/kg intravenous dose were investigated in pediatric patients ranging in age from 6 months to 16 years. Pediatric patients cleared Levofloxacin 0.5.% TOA faster than adult patients, resulting in lower plasma exposures than adults for a given mg/kg dose. Subsequent pharmacokinetic analyses predicted that a dosage regimen of 8 mg/kg every 12 hours (not to exceed 250 mg per dose) for pediatric patients 6 months to 17 years of age would achieve comparable steady state plasma exposures (AUC0-24 and Cmax) to those observed in adult patients administered 500 mg of Levofloxacin 0.5.% TOA once every 24 hours.
There are no significant differences in Levofloxacin 0.5.% TOA pharmacokinetics between male and female subjects when subjects' differences in creatinine clearance are taken into consideration. Following a 500 mg oral dose of Levofloxacin 0.5.% TOA to healthy male subjects, the mean terminal plasma elimination halflife of Levofloxacin 0.5.% TOA was about 7.5 hours, as compared to approximately 6.1 hours in female subjects. This difference was attributable to the variation in renal function status of the male and female subjects and was not believed to be clinically significant. Drug absorption appears to be unaffected by the gender of the subjects. Dose adjustment based on gender alone is not necessary.
The effect of race on Levofloxacin 0.5.% TOA pharmacokinetics was examined through a covariate analysis performed on data from 72 subjects: 48 white and 24 non-white. The apparent total body clearance and apparent volume of distribution were not affected by the race of the subjects.
Clearance of Levofloxacin 0.5.% TOA is substantially reduced and plasma elimination half-life is substantially prolonged in adult patients with impaired renal function (creatinine clearance < 50 mL/min), requiring dosage adjustment in such patients to avoid accumulation. Neither hemodialysis nor continuous ambulatory peritoneal dialysis (CAPD) is effective in removal of Levofloxacin 0.5.% TOA from the body, indicating that supplemental doses of Levofloxacin 0.5.% TOA are not required following hemodialysis or CAPD.
Pharmacokinetic studies in hepatically impaired patients have not been conducted. Due to the limited extent of Levofloxacin 0.5.% TOA metabolism, the pharmacokinetics of Levofloxacin 0.5.% TOA are not expected to be affected by hepatic impairment.
The pharmacokinetics of Levofloxacin 0.5.% TOA in patients with serious community-acquired bacterial infections are comparable to those observed in healthy subjects.
The potential for pharmacokinetic drug interactions between Levofloxacin 0.5.% TOA and antacids, warfarin, theophylline, cyclosporine, digoxin, probenecid, and cimetidine has been evaluated.
Mechanism Of Action
Levofloxacin 0.5.% TOA is the L-isomer of the racemate, ofloxacin, a quinolone antimicrobial agent. The antibacterial activity of ofloxacin resides primarily in the L-isomer. The mechanism of action of Levofloxacin 0.5.% TOA 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.
Mechanism of Resistance
Fluoroquinolone resistance can arise through mutations in defined regions of DNA gyrase or topoisomerase IV, termed the Quinolone-Resistance Determining Regions (QRDRs), or through altered efflux.
Fluoroquinolones, including Levofloxacin 0.5.% TOA, differ in chemical structure and mode of action from aminoglycosides, macrolides and β-lactam antibiotics, including penicillins. Fluoroquinolones may, therefore, be active against bacteria resistant to these antimicrobials.
Resistance to Levofloxacin 0.5.% TOA due to spontaneous mutation in vitro is a rare occurrence (range: 10 ed. CLSI Document M45-A2, 2010.
- DailyMed. "LEVOFLOXACIN: DailyMed provides trustworthy information about marketed drugs in the United States. DailyMed is the official provider of FDA label information (package inserts).". https://dailymed.nlm.nih.gov/dailyme... (accessed September 17, 2018).
- NCIt. "Levofloxacin: NCI Thesaurus (NCIt) provides reference terminology for many systems. It covers vocabulary for clinical care, translational and basic research, and public information and administrative activities.". https://ncit.nci.nih.gov/ncitbrowser... (accessed September 17, 2018).
- EPA DSStox. "Levofloxacin: DSSTox provides a high quality public chemistry resource for supporting improved predictive toxicology.". https://comptox.epa.gov/dashboard/ds... (accessed September 17, 2018).
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Information checked by Dr. Sachin Kumar, MD Pharmacology