Description:
Moxifloxacin is a synthetic broad spectrum antibacterial agent available in tablet.

Pharmacological Action:
Pharmacodynamic properties
Moxifloxacin has in vitro activity against a wide range of Gram-Positive and Gram-negative microorganisms. The bactericidal action of moxifloxacin results from inhibition of the topoisomerase II (DNA gyrase) and topoisomerase IV required for bacterial DNA replication, transcription, repair and recombination. It appears that the C8-methoxy moiety contributes to enhanced activity and lower selection of resistant mutants of Gram-positive bacteria compared to the C8-H moiety. The presence of the bulky bicycloamine substituent at the C-7 position prevents active efflux, associated with the NorA or pmr A genes seen in certain Gram-positive bacteria.

Pharmacokinetic properties:
Absorption
Moxifloxacin, given as an oral tablet, is well absorbed from the gastrointestinal tract. The absolute bioavailability of moxifloxacin is approximately 90%.Co-administration with a high fat meal (i.e., 500 calories from fat) does not affect the absorption of moxifloxacin.
Distribution
Moxifloxacin is approximately 30-50% bound to serum proteins, independent of drug concentration. The volume of distribution of moxifloxacin ranges from 1.7 to 2.7 L/kg. Moxifloxacin is widely distributed throughout the body, with tissue concentrations often exceeding plasma concentrations. The rates of elimination of moxifloxacin from tissues generally parallel the elimination from plasma.
Metabolism
Approximately 52% of an oral or intravenous dose of moxifloxacin is metabolized via glucuronide and sulfate conjugation. The cytochrome P450 system is not involved in moxifloxacin metabolism and is not affected by moxifloxacin.
Excretion
Approximately 45 % of an oral or intravenous dose of moxifloxacin is excreted as unchanged drug (~ 20% in urine and ~ 25% in feces). A total of 96% ± 4% of an oral dose is excreted as either unchanged drug or known metabolites.

Indication and Usage:
Moxifloxacin is indicated for the treatment of adults (> 18 years of age) with infections caused by susceptible strains of the designated microorganisms in the conditions listed below
Acute Bacterial Sinusitis.
Acute Bacterial Exacerbation of Chronic Bronchitis
Community Acquired Pneumonia
Complicated & Uncomplicated Skin and Skin Structure Infections
Complicated Intra-Abdominal Infections

Moxifloxacin has been shown to be active against most strains of the following microganisms, both in vitro and in clinical infections.

Gram-positive microorganisms:
Staphylococcus aureus (including methicillin-sensitive strains)
Streptococcus pneumoniae (including penicillin and macrolide resistant strains)
Streptococcus pyogenes (Group A)

Gram-negative microorganisms:
Haemophilus influenzae (including ß-lactamase negative and positive strains)
Haemophilus parainfluenzae
Klebsiella pneumoniae
Moraxella catarrhalis (including ß-lactamase negative and positive strains)
Escherichia coli
Enterobacter cloacae

Atypicals:
Chlamydia pneumoniae
Mycoplasma pneumoniae

According to in vitro studies, the following organisms are sensitive to moxifloxacin, however, the safety and effectiveness of moxifloxacin in treating clinical infections due to these microorganisms has not been established in adequate and well-controlled clinical trials.

Gram-positive microorganisms:
Streptococcus milleri
Streptococcus mitior
Streptococcus agalactiae
Staphylococcus cohnii
Staphylococcus epidermidis(including methicillin sensitive strains)
Staphylococcus haemolyticus
Staphylococcus hominis
Staphylococcus saprophyticus
Staphylococcus simulant
Corynebacterium diptheriae

Gram-negative microorganisms:
Bordetella pertussis
Klebsiella oxytoca
Enterobacter aerogenes
Enterobacter agglomerans
Enterobacter intermedius
Enterobacter sakazaki
Proteus mirabilis
Proteus vulgaris
Morganella morganii
Providencia rettgeri
Providencia stuartii

Anaerobes:
Bacteroides distasonis
Bacteroides eggerthii
Bacteroides fragilis
Bacteroides ovatus
Bacteroides thetaiotaomicron
Bacteroides uniformis
Fusobacterium spp.
Porphyromonas spp.
Porphyromonas anaerobius
Porphyromonas asaccharolyticus
Porphyromonas magnus
Prevotella spp.
Propionibacterium spp.
Clostridium perfringens
Clostridium ramosum

Atypicals:
Legionella pneumophila
Caxiella burnettii

Dosage & Administration:
The oral dose of moxifloxacin is 400mg once in a day. The duration of therapy depends on the type of infection given below.

Impaired Renal Function:
No dosage adjustment is required in renally impaired patients, including those on either hemodialysis or continuous ambulatory peritoneal dialysis.

Impaired Hepatic Function:
No dose adjustment is required in patients with mild or moderate hepatic insufficiency. The pharmacokinetics of moxifloxacin in patients with severe hepatic insufficiency have not been established.

Contraindications:
Moxifloxacin is contraindicated in patients with a history of hypersensitivity to moxifloxacin or any member of the quinolone class of antimicrobial agents.

Warnings & Special Precautions:
The safety and effectiveness of moxifloxacin in paediatric patients, adolescents (Less than 18 years of age), pregnant women and lactating women have not been established.
Pregnancy: Teratogenic Effects. Pregnancy Category C
Since there are no adequate or well-controlled studies in pregnant women, moxifloxacin should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.
Quinolones may cause central nervous system (CNS) event, including: nervousness, agitation, insomnia, anxiety, nightmares or paranoia.
Nursing Mothers
Moxifloxacin is excreted in the breast milk. Because of the potential for serious adverse reactions in infants who are nursing from mothers taking moxifloxacin, 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.

Adverse Effects:
Most adverse events reported in moxifloxacin trials were described as mild to moderate in severity and required no treatment. Additional clinically relevant uncommon events that occurred in greater than or equal to 0.1% and less than 2% of moxifloxacin treated patients were:
Body as a whole: abdominal pain, headache, asthenia. Injection site reaction (including phlebitis), malaise, moniliasis, pain, allergic reaction.
Cardiovascular: tachycardia, palpitation, vasodilation, QT interval prolonged.
Digestive: vomiting abnormal liver function test, dyspepsia, dry mouth, flatulence, oral moniliasis, constipation, GGTP increased, anorexia, stomatitis, glossitis
Hemic and Lymphatic: leukopenia, eosinophilia, prothrombin decrease.
Metabolic and Nutritional: lactic dehydrogenase increased, amylase increased
Musculoskeletal: arthralgia, myalgia
Nervous System: insomnia, nervousness, vertigo, somnolence, anxiety, tremor
Skin/ Appendages: rash (maculopapular, purpuric, pustular), pruritis, sweating, urticaria
Special Senses: taste perversion
Urogenital: vaginal moniliasis, vaginitis

Interactions:
No clinically significant drug interactions between itraconazole, theophylline, warfarin, digoxin, atenolol, oral contraceptives or glyburide have been observed with moxifloxacin. Itraconazole, theophylline, digoxin, probenecid, morphine, ranitidine, and calcium have been shown not to significantly alter the pharmacokinetics of moxifloxacin.

Overdose:
Limited data on overdoses are available. In the event of acute overdose, the stomach should be emptied and adequate hydration maintained. ECG monitoring is recommended due to the possibility of QT interval prolongation. The patient should be carefully observed and given supportive treatment. The administration of activated charcoal as soon as possible after oral overdose may prevent excessive increase of systemic moxifloxacin exposure.

Presentation:
Pack of 5 film coated tablets in a blister.