ELSALOX

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ELSALOX

Chemical Name:

Moxifloxacin
Therapeutic Category:

Antimicrobial
Pharmacologic Category:

Antibiotic, Fluoroquinolone 4th
Pharmaceutical Form:

Tablets
Composition:

Moxifloxacin 400mg

ELSALOX

Vial & Film Coated Tablets

Moxifloxacin (Hydrochloride)

1-CHEMICAL COMPOSITION:
ELSALOX - Film Coated Tablets: Each film coated tablets contains Moxifloxacin (Hydrochloride) 400mg.

ELSALOX – Vial: Each Vial contains Moxifloxacin (HCl) 400 mg/250ml.

Excipients

ELSALOX - Film Coated Tablets

Microcrystalline Cellulose, Lactose Monohydrate, Croscarmellose Sodium, Magnesium Stearate, Hypromellose, Titanium Dioxide, Polyethylene Glycol, Brilliant Blue.

ELSALOX – Vial

Mannitol, Water for injection

2-MECHANISM OF ACTION:
ELSALOX is a synthetic broad spectrum antibacterial agent , it 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.
The mechanism of action for quinolones, including moxifloxacin, is different from that of macrolides, beta-lactams, aminoglycosides, or tetracyclines; therefore, microorganisms resistant to these classes of drugs may be susceptible to moxifloxacin and other quinolones .

3-PHARMACOKINETICS:

Absorption: Moxifloxacin, given as an oral tablet, is well absorbed from the gastrointestinal tract.
The absolute bioavailability of moxifloxacin is approximately 90 percent.
Co-administration with a high fat meal does not affect the absorption of moxifloxacin.

Cmax values after administration of single oral and I.V dose was found to be

3.1mg/L and 3.9mg/L in healthy volunteers.

Distribution : Moxifloxacin is approximately 30-50% bound to serum proteins, independent of drug concentration .

Moxifloxacin is widely distributed throughout the body, with tissue concentrations often exceeding plasma concentrations.

Metabolism : Approximately 52% of an oral or intravenous dose of moxifloxacin is metabolized via glucuronide and sulfate conjugation.

Elimination : The mean elimination half-life from plasma is 12 hours. Approximately 45% of an oral or intravenous dose of moxifloxacin is excreted as unchanged drug (~20% in urine and ~25% in feces).

4-INDICATIONS:

ELSALOX is indicated for the treatment of adults (>/= 18 years of age) with infections caused by susceptible strains in the following conditions:

- Acute Bacterial Sinusitis caused by Streptococcus pneumoniae, Haemophilus influenzae, or Moraxella catarrhalis.

- Acute Bacterial Exacerbation of Chronic Bronchitis caused by Streptococcus pneumoniae, Haemophilus influenzae, Haemophilus parainfluenzae, Klebsiella pneumoniae, methicillin-susceptible Staphylococcus aureus, or Moraxella catarrhalis.

- Community Acquired Pneumonia caused by Streptococcus pneumoniae (including multi-drug resistant strains), Haemophilus influenzae, Moraxella catarrhalis, methicillin-susceptible Staphylococcus aureus, Klebsiella pneumoniae, Mycoplasma pneumoniae, or Chlamydia pneumoniae.

- Uncomplicated Skin and Skin Structure Infections caused by methicillin-susceptible Staphylococcus aureus or Streptococcus pyogenes.

- Complicated Intra-Abdominal Infections including polymicrobial infections such as abscess caused by Escherichia coli , Bacteroides fragilis , Streptococcus anginosus , Streptococcus constellatus , Enterococcus faecalis , Proteus mirabilis , Clostridium perfringens , Bacteroides thetaiotaomicron , or Peptostreptococcus species.

- Complicated Skin and Skin Structure Infections caused by methicillin-susceptible Staphylococcus aureus , Escherichia coli , Klebsiella pneumoniae , or Enterobacter cloacae .
Appropriate culture and susceptibility tests should be performed before treatment in order to isolate and identify organisms causing infection and to determine their susceptibility to moxifloxacin .

5-DOSAGE AND ADMINISTRATION:

The dose of Moxifloxacin is 400 mg ( orally or as intravenous infusion ) as an intravenous infusion once every 24 hours. The duration of therapy depends on the type of infection as described below.

Infection	Daily Dose	Duration

Acute Bacterial Sinusitis	400 mg	10 days
Acute Bacterial Exacerbation of Chronic Bronchitis	400 mg	5 days
Community Acquired Pneumonia	400 mg	7-14 days
Uncomplicated Skin and Skin Structure Infections	400 mg	7 days
Complicated Skin and Skin Structure Infections	400 mg	7-21 days
Complicated Intra-Abdominal Infections	400 mg	5-14 days

For Complicated Intra-Abdominal Infections, therapy should be initiated with the intravenous formulation .
When switching from intravenous to oral dosage administration, no dosage adjustment is necessary. Patients whose therapy is started with moxifloxacin I.V. may be switched to moxifloxacin Tablets when clinically indicated at the discretion of the physician.

Moxifloxacin I.V. is compatible with the following intravenous solutions at ratios from 1:10 to 10:1

0.9% Sodium Chloride Injection, USP	Sterile Water for Injection, USP
1M Sodium Chloride Injection	10% Dextrose for Injection, USP
5% Dextrose Injection, USP	Lactated Ringer`s for Injection

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

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

6-CONTRAINDICATIONS:

ELSALOX is contraindicated in persons with a history of hypersensitivity to moxifloxacin or any member of the quinolone class of antimicrobial agents.

7-DRUG INTERACTIONS:

Antacids, Sucralfate, Metal Cations, and Multivitamins :

Oral administration of quinolones with antacids containing aluminum or magnesium,

with sucralfate, with metal cations such as iron, or with multivitamins containing

iron or zinc may substantially interfere with the absorption of quinolones, resulting in systemic concentrations considerably lower than desired. Therefore, moxifloxacin should be taken at least 4 hours before or 8 hours after these agents.

Warfarin

Quinolones, including moxifloxacin, have been reported to enhance the

anticoagulant effects of warfarin or its derivatives in the patient population .

Therefore the prothrombin time, International Normalized Ratio (INR), or

other suitable anticoagulation tests should be closely monitored if a quinolone is

administered concomitantly with warfarin or its derivatives.

Drugs metabolized by Cytochrome P450 enzymes

Moxifloxacin is unlikely to alter the pharmacokinetics of drugs metabolized by these enzymes (e.g. midazolam, cyclosporine, warfarin, theophylline).

Nonsteroidal anti-inflammatory drugs (NSAIDs)

Although not observed with moxifloxacin in preclinical and clinical trials, the concomitant administration of a nonsteroidal anti-inflammatory drug with a quinolone may increase the risks of CNS stimulation and convulsions.
Drugs that Prolong QT
prolongation of the QTc interval in the ECG has been observed in some patients receiving moxifloxacin . Sotalol, a Class III antiarrhythmic, has been shown to further increase the QTc interval when combined with high doses of intravenous (IV) moxifloxacin in dogs. Therefore, moxifloxacin should be avoided with Class IA and Class III antiarrhythmics.

Note : No clinically significant drug-drug interactions between itraconazole, theophylline, 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.

8-ADVERSE REACTIONS:

The most common undesirable effects include:

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, anorexia, stomatitis,

glossitis

Hemic And Lymphatic: leukopenia, eosinophilia, prothrombin decrease, thrombocythemia

Metabolic And Nutritional: lactic dehydrogenase increased, amylase increased

Musculoskeletal: arthralgia, myalgia

Nervous System: insomnia, nervousness, vertigo, somnolence, anxiety

Skin/Appendages: rash (maculopapular, purpuric, pustular), pruritus, sweating,

urticaria

Urogenital: vaginal moniliasis, vaginitis

9-WARNINGS & PRECAUTIONS:

- Moxifloxacin I.V. should be administered by intravenous infusion only. It is not intended for intra-arterial, intramuscular, intrathecal, intraperitoneal, or subcutaneous administration.
- Moxifloxacin I.V. should be administered by intravenous infusion over a period of 60 minutes by direct infusion or through a Y-type intravenous infusion set which may already be in place (Rapid or bolus intravenous infusion must be avoided)
- Additives or other medications should not be added to moxifloxacin I.V. or infused simultaneously through the same intravenous line. If the same intravenous line or a Y-type line is used for sequential infusion of other drugs, the line should be flushed before and after infusion of moxifloxacin I.V. with an infusion solution compatible with moxifloxacin I.V. as well as with other drug(s) administered via this common line.

- QT Prolongation : Moxifloxacin should be used with caution in patients with ongoing proarrhythmic conditions. The magnitude of QT prolongation may increase with increasing concentrations of the drug or increasing rates of infusion of the intravenous formulation. Therefore the recommended dose or infusion rate should not be exceeded.

- Central Nervous System Effects : Convulsions and increased intracranial pressure have been reported in patients receiving fluoroquinolones. Fluoroquinolones may also cause central nervous system (CNS) events including: dizziness, confusion, tremors, depression. These reactions may occur following the first dose. If these reactions occur in patients receiving Moxifloxacin, the drug should be discontinued

- Hypersensitivity Reactions : anaphylactic reactions, some following the first dose, have been reported in patients receiving quinolone therapy, including moxifloxacin . The drug should be discontinued at the first appearance of a skin rash or any other sign of hypersensitivity. Oxygen, intravenous steroids, and airway management, including intubation, may be administered as indicated.

- Clostridium Difficile-Associated Diarrhea : Clostridium difficile-associated diarrhea (CDAD) has been reported with use of nearly all antibacterial agents, including moxifloxacin.

- Tendon Rupture : Rupture of the shoulder , hand , achilles tendon or other tendons have been reported in patients receiving quinolone therapy, including moxifloxacin

10-PREGNANCY & LACTATION:
Pregnancy category C : Moxifloxacin should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.

Lactation : Moxifloxacin may also be excreted in human 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.

11-Pediatric Use:

Safety and effectiveness in pediatric patients and adolescents less than 18 years

of age have not been studied.

12-OVERDOSE:

Single oral overdoses up to 2.8 g were not associated with any serious adverse events. 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.

13-PACKAGING :

ELSALOX F.C. Tablets : Carton package of 5 film coated tablets.

ELSALOX – Vial: Carton package of 1 Vial of 250 ml.

14-STORAGE CONDITIONS:
Store ELSALOX at temperature below 25°C. Protect from light.