Each Targofloxin tablet contains 150 mg levofloxacin(as hemihydrate)
Excipients: Hydroxypropyl methylcellulose, crospovidone, microcrystalline cellulose, magnesium stearate, croscarmellose sodium, aerosil 200, talc.
Targofloxln, levofloxacin, is the L-isomer of the racemate, cflcxacin, a fluoroquinolone antimicrobial agent. The antibacterial activity of ofloxacin resides primarily in the Leisomer, It! mechanism of action involves inhibition of bacterial topoisomerase IV and DNA gyrase (both of which are type IT topoisomerase), enzymes required for bacterial DNA replication, transcription, repair and recombination.
Levofloxacin is a concentration-dependent antimicrobial agent, taken in a dose of 750 mg daily, could shorten the duration of treatment without compromising efficacy, as well. prevents the emergence of resistance.
Levofloascin is active against a wide range of gram negative , gram positive microorganisms, atypttal and some anaerobcs.
It is bactericidal at concentrations equal to or slightly greater than inhibitory concentrations. It is generally considered to be about twice as active as its isomer, ofloxacin.
It is active against:
Aerobic gram-positive microorganisms: Staphylococcus aureus. Staphylococcus epidermidis. Streptococcus pneumoniae, Streptococcus pyogenes, Staphylococcus saprophyticus, Enterococcusfaecalis (many strains arc only moderately susceptible). Aerobic gram-negative microorganisms: Escherichia coli, Haemophilus influenzae, Haemophilur parainfiuenzae, Klebsiella pneumoniae, Legionella pneumoniae, Moraxelra catarmalis, Proteus mirabilis, Pseudomonas aeruginosa, Serratia
marcescens, Enserobacter cloacae
Atypical microorganisms such as: Chlamydia pneumoniae, Mycoplasma pneumoniae.
Levoflcxacin is rapidly and almost completely absorbed following oral administration with peak plasma concentrations achieved within 1 or 2 hours after oral dose.
It can be administered without regard to food.
It is distributed into body tissues including the bronchial mucosa, lungs and prostate, but penetration into the CSF is relatively poor. It is approximately 30 to 4()Oh bound to plasma proteins.
It is only metabolized to a small degree to inactive metabolites. The elimination half- life oflevofloxacin is 6 to 8 hours, although this may be prolonged in patients with renal impainnent. It is excreted largely unchanged, primarily in the urine. Due to the limited extent of levcfloxacin metabolism, the phannacokinetics of levofloxacin are not expected to be affected by hepatic impainnem.
1- Upper respiratory tract infections such as: acute bacterial sinusitis, acute maxillary sinusitis, otitis media, otitis externa, laryngitis and pharyngitis.
2- Lower respiratory tract infections such as: community-acquired pneumonia, nosocomial pneumonia and acute bacterial exacerbation of chronic bronchitis.
3- Complicated and uncomplicated skin and skin structure infections.
4- Complicated and uncomplicated urinary tract infections.
5- Acute pyelonephritis, gonorrhoea.
6- Chronic bacterial prostatitis.
7- Gastrointestinal tract infections such as typhoid fever.
Side effects :
It is generally well tolerated. As with other quinolones, the most common side effects are mild including nausea, diarrhoea, itching, abdominal pain, dizziness, headache, sleep disorders, rash, and pruritus. Less frequent side effects include anorexia, dyspepsia, vomiting, constipation,bearing and smell; vaginitis, chest pain, back pain, genital moniliasis, oedema. fatigue, increased sweating, malaise, tremor, urticaria, leucorrhea. Isolated reports of tendon inflammation and damage.
In persons with a history of hypersensitivity to tevcfloxecin, qi:dholone antimicrobial agents, or any other components of the product.
Pregnancy: Adequate and well-controlled studies tn..pregnant women have not been established, use in pregnancy only if the potential beeefirjustifies the potential risk to
lactation: Because of the potential for serious adverse reactions from levofloxacin 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.
Children: Safety and efficacy in paediatric patients and adolescents below the age of .
18 years have not been established.
Adequate hydration of patients should be maintained to prevent the formation of highly concentrated urine. As with other quinolones:
– Caution in driving as it may impair performance of skilled tasks .
– Administer levotloxacin with caution in the presence of renal insufficiency. – Excessive exposure to sunlight should be avoided.
– Levofloxacin 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.
– Careful monitoring of blood glucose is recommended.
– (Use of levofloxacin in the presence of risk factors for torsedes de pointes such as hypokalaemia, significant bradycardia, and cardiomyopathy should be avoided). Levofloxecia should be avoided in patients with known prolongation of the QT interval, patients with uncorrected hypokalemia. and patients receiving class lA
(quinidine, procainamidc), or class m antiarrhythmic agents.
– Discontinue treatment if patients experience tendon pain, inflammation, or rupture.
– As with other potent antimicrobial drugs, periodic assessment of organ system function including bepatic, renal, full blood picture is advisable.
Drug-drug interactions :
Antacids, sueralfate, metal cations, multivitamin: While the chelation by divalent cations is less marked than with other quinolones, concurrent administration of levofloxacin tablets with antacids containing magnesium, or aluminum, as well as sucralfate, metal cations such as iron, and multivitamin preparations with zinc may interfere with the gastrcintestinat absorption of levofloxacin. resulting in systemic levels considerably lower than desired. These agents should be taken at least two hours before or two hours after levofloxacin administration.
Theophylline: No significant effect of levofloxacin on the plasma concentrations, AUC, and other disition parameters for-theophylline was detected in a clinical study involving 14 healthy volunteers. Similarly, DO apparent effect of theophylline on
levofloxacin absorption and disposition was observed. However, concomitant administration of other quinolones with theophylline has resulted in prolonged elimination half-life, elevated serum theophylline levels, and a subsequent increase in the risk ofthcophyllinc-relatcd adversc reactions in the patient population. Thcrefore, theophylline levels should be closely monitored and appropriate dosage adjustments made when levoflcxacia is eo-administered.
Warfarin: No significant effect oflevofloxacin on the peak plasma concentrations, AUC, and other disposition parameters for warfarin was detected. Similarly, no apparent effect of warfarin on levofloxacin absorption and disposition was observed. Elevations of the prothrombin time in the setting of concurrent warfarin and
levcflcxacin use have been associated with episodes of bleeding. Prothrombin time, International Normalized Ratio (INR), or other suitable anticoagulation tests should be closely monitored i~ levofloxacin is administat concomitantly with warfarin. Patients
should also be monitored for evidence of bleeding.
AUC, and other disposition parameters for cyclosporine was detected. However, elevated serum levels of cyclosporine have been reponed. in the patient population when co-administered with some other quinolones. Therefore, no dosage adjustment is required for levofloxecin or cyclosporine when administered concomitantly.
Digoxin: No significant effect oflevofloxacin on the peak plasma concentrations, AVe, and other disposition parameters for digoxin was detected. Levofloxacin absorption and disposition kinetics were similar in the presence or absence of digoxin. Therefore, no
dosage adjustment for levofloxacin or digoxin is required when administered concomitantly.
Probenecid and Cimetidine: No significant effect of probenecid or cimetidine on the rate and extent of levofloxacin absorption was observed. Although these differences were statistically significant. the changes were not high enough to warrant dosage adjustment for levofloxacin when probenecid or cimetidine is eo-administered.
Non-steroidalanti-inflammatory drugs: The concomitant adrnimstration ofa non- steroidal anti-inflammatory drug with a quinolone, including levoflcxacin, may increase the risk ofCNS stimulation and convulsive seizures.
Antidiabetic agents: Disturbances of blood glucose, including hyperglycemia and hypoglycemia, have been reported in patients treated concomitantly with quinolones and an antidiabetic agent. Therefore, careful monitoring of blood glucose is recommended when these agents are eo-administered
Dosage and administration :
Oral doses should be administered more or equal to 2 hours before or 2 hours after antacids containing magnesium and/or alwninium, iron. and multivitamin preparations with zinc.
Targofloxin should be taken as one tablet daily every 24 hours.
The duration of treatment is depending on the type of infection and the direction of the physician.
Patients with impaired renal function:
Targofloxin 150 mg tablets are supplied in boxes of 5 tablets each.
Store at a temperature not exceeding 30’C.
I Keep out of reach of children I
Produced by :
GLOBAl NAPI PHARMACEUTICALS
Industrial Zone, 6·0f October City – Egypt