Overview
11 DESCRIPTION Levofloxacin tablets are synthetic antibacterial agents for oral administration. Chemically, levofloxacin, a chiral fluorinated carboxyquinolone, is the pure (-)-(S)-enantiomer of the racemic drug substance ofloxacin. The chemical name is (-)-(S)-9-fluoro-2,3-dihydro-3-methyl-10-(4-methyl-1-piperazinyl)-7-oxo-7H-pyrido[1,2,3-de]-1,4-benzoxazine-6-carboxylic acid hemihydrate.
Mechanism of Action
12 CLINICAL PHARMACOLOGY 12.1 Mechanism of Action Levofloxacin is a member of the fluoroquinolone class of antibacterial agents [see Microbiology ( 12.4 )] . 12.3 Pharmacokinetics The mean ±SD pharmacokinetic parameters of levofloxacin determined under single and steady-state conditions following administration of the oral tablets, are summarized in Table 8. Table 8 Mean ±SD Levofloxacin PK Parameters 1 clearance/bioavailability 2 volume of distribution/bioavailability 3 healthy males 18 to 53 years of age 4 healthy male and female subjects 18 to 54 years of age 5 healthy males 22 to 75 years of age 6 healthy females 18 to 80 years of age 7 young healthy male and female subjects 18 to 36 years of age 8 healthy elderly male and female subjects 66 to 80 years of age * Absolute...
Indications
- 1 INDICATIONS AND USAGE Levofloxacin is a fluoroquinolone antibacterial indicated in adults (18 years of age and older) with infections caused by designated, susceptible bacteria and in pediatric patients where indicated ( 1 , 12.4 ). Pneumonia: Nosocomial ( 1.1 ) and Community Acquired ( 1.2 , 1.3 ) Skin and Skin Structure Infections (SSSI): Complicated ( 1.4 ) and Uncomplicated ( 1.5 ) Chronic bacterial prostatitis ( 1.6 ) Inhalational Anthrax, Post-Exposure in adult and pediatric patients ( 1.7 ) Plague in adult and pediatric patients ( 1.8 ) Urinary Tract Infections (UTI): Complicated ( 1.
Common Doses
- 50 mL
- 750 mg
- 500 mg
- 250 mg
Dosage
2 DOSAGE AND ADMINISTRATION Administer levofloxacin tablets to pediatric patients weighing 30 kg and greater only ( 2.1 , 2.2 ). Levofloxacin tablets cannot be administered to pediatric patients who weigh less than 30 kg because of the limitations of the available strengths. Alternative formulations of levofloxacin may be considered for pediatric patients who weigh less than 30 kg ( 2.2 ). Dosage in Adult and Pediatric Patients with Creatinine Clearance greater than or equal to 50 mL/minute ( 2.1 , 2.2 ) Type of Infection Dose Every 24 hours Duration (days) Nosocomial Pneumonia ( 1.
Black Box Warning
WARNING: SERIOUS ADVERSE REACTIONS INCLUDING TENDINITIS, TENDON RUPTURE, PERIPHERAL NEUROPATHY, CENTRAL NERVOUS SYSTEM EFFECTS AND EXACERBATION OF MYASTHENIA GRAVIS WARNING: SERIOUS ADVERSE REACTIONS INCLUDING TENDINITIS, TENDON RUPTURE, PERIPHERAL NEUROPATHY, CENTRAL NERVOUS SYSTEM EFFECTS AND EXACERBATION OF MYASTHENIA GRAVIS See full prescribing information for complete boxed warning. Fluoroquinolones, including levofloxacin, have been associated with disabling and potentially irreversible serious adverse reactions that have occurred together ( 5.
Contraindications
- 4 CONTRAINDICATIONS Known hypersensitivity to levofloxacin or other quinolones ( 4 , 5.7 ) Levofloxacin tablet is contraindicated in persons with known hypersensitivity to levofloxacin, or other quinolone antibacterials [see Warnings and Precautions ( 5.3 )].
Side Effects
- 6 ADVERSE REACTIONS The following serious and otherwise important adverse drug reactions are discussed in greater detail in other sections of labeling: Disabling and Potentially Irreversible Serious Adverse Reactions [see Warnings and Precautions ( 5.1 )] Tendinitis and Tendon Rupture [see Warnings and Precautions ( 5.2 )] Peripheral Neuropathy [see Warnings and Precautions ( 5.3 )] Central Nervous System Effects [see Warnings and Precautions ( 5.4 )] Exacerbation of Myasthenia Gravis [see Warnings and Precautions ( 5.
Interactions
- 7 DRUG INTERACTIONS Interacting Drug Interaction Multivalent cation-containing products including antacids, metal cations or didanosine Absorption of levofloxacin is decreased when the tablets are taken within 2 hours of these products. ( 2.4 , 7.1 ) Warfarin Effect may be enhanced. Monitor prothrombin time, INR and watch for bleeding ( 7.2 ) Antidiabetic agents Carefully monitor blood glucose ( 5.13 , 7.3 ) 7.1 Chelation Agents: Antacids, Sucralfate, Metal Cations, Multivitamins While the chelation by divalent cations is less marked than with other fluoroquinolones, concurrent administration...