Levofloxacin

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Levofloxacin is a broad-spectrum bactericidal agents of the fluoroquinolone class used to treat infections of the: Sinuses, Lungs, Urinary tract, Prostate gland, and Skin and underneath the skin including muscles.

Contents

[edit] BRAND NAMES

[edit] STRUCTURE

Levofloxacin.jpg

[edit] MECHANISM OF ACTION

Levofloxacin is a broad-spectrum bactericidal agents of the fluoroquinolone class (Levofloxacin is a 3rd generation quinolone) with a wide range activity against gram-negative and gram-positive organisms. It is the L-isomer of the racemate, ofloxacin (the antibacterial activity of ofloxacin resides primarily in the L-isomer).

Levofloxacin inhibits bacterial enzymes DNA gyrase and topoisomerase IV. DNA gyrase catalyzes the negative supercoiling of the circular DNA found in bacteria and Topoisomerase IV, on the other hand, is involved in the separation process of the DNA daughter chains after bacterial DNA duplication.

Depending on the type of bacterium, these enzymes represent either the primary or secondary target of antimicrobial action. In Gram-negative bacteria, such as E.coli, fluoroquinolones predominantly inhibit DNA gyrase, whereas for Gram-positive organisms like Staph.aureus, Topoisomerase IV is the principle target.

Ultimately, the action of Levofloxacin on DNA gyrase or on topoisomerase IV, results in damage to bacterial DNA and bacterial cell death.

[edit] INDICATIONS

Infections caused by bacteria susceptible to Levofloxacin like respiratory, urinary tract, gastrointestinal, abdominal, and skin infections:

  • Pneumonia: nosocomial and community acquired
  • Acute bacterial sinusitis
  • Acute bacterial exacerbation of chronic bronchitis
  • Skin and skin structure infections: complicated and uncomplicated
  • Chronic bacterial prostatitis
  • Urinary tract infections: complicated and uncomplicated (Attention: Resistance to fluoroquinolones, has become increasingly common in Escherichia coli infections of the urinary tract) [1]
  • Acute pyelonephritis
  • Inhalational anthrax, post-exposure
  • Plague

[edit] DOSAGE

Dosage in patients with normal renal function:

Type of Infection Dose every

24 hours

Duration

(days)

Nosocomial Pneumonia 750 mg 7–14
Community Acquired Pneumonia 500 mg 7–14
Community Acquired Pneumonia 750 mg 5
Acute Bacterial Sinusitis 750 mg 5
Acute Bacterial Sinusitis 500 mg 10–14
Acute Bacterial Exacerbation of Chronic Bronchitis 500 mg 7
Complicated Skin and Skin Structure Infections (SSSI) 750 mg 7–14
Uncomplicated SSSI 500 mg 7–10
Chronic Bacterial Prostatitis 500 mg 28
Complicated Urinary Tract Infection  or Acute Pyelonephritis  750 mg 5
Complicated Urinary Tract Infection  or Acute Pyelonephritis  250 mg 10
Uncomplicated Urinary Tract Infection 250 mg 3

Inhalational Anthrax (Post-Exposure)

Adult and pediatric patients > 50 kg 

Pediatric patients < 50 kg and ≥ 6 months of age

500 mg

8 mg/kg BID
(not to exceed
250 mg/dose)


60

60

Plague

Adult and pediatric patients > 50 kg 

Pediatric patients < 50 kg and ≥ 6 months of age

500 mg
8 mg/kg BID
(not to exceed
250 mg/dose)


10 to 14

10 to 14

[edit] CONTRAINDICATIONS

  • Known hypersensitivity to Levofloxacin or other quinolones
  • Patients who are pregnant or lactating
  • Patients with epilepsy or other seizure disorders
  • Patients below 18 years of age (exept FDA approved in pediatric patients (6 months of age and older) only for the prevention of inhalational anthrax (post-exposure) and for plague. An increased incidence of musculoskeletal disorders (arthralgia, arthritis, tendinopathy, and gait abnormality) has been observed in pediatric patients receiving Levofloxacin

[edit] WARNINGS AND PRECAUTIONS

  • Tendinitis may rarely occur. It most frequently involves the Achilles tendon and may lead to tendon rupture. This risk is further increased in older patients usually over 60 years of age, in patients taking corticosteroids, in patients receiving daily doses of 1000 mg and in patients with kidney, heart or lung transplants. Discontinue if pain or inflammation in a tendon occurs
  • Clostridium difficile-associated colitis: evaluate if diarrhea, particularly if severe, persistent and/or bloody, during or after treatment with levofloxacin.
  • Quinolones may lower the seizure threshold and may trigger seizures. Levofloxacin is contraindicated in patients with a history of epilepsy.
  • Photosensitisation: It is recommended that patients should not expose themselves unnecessarily to strong sunlight or to artificial UV rays (e.g. solarium), during treatment and for 48 hours following treatment discontinuation in order to prevent photosensitisation
  • Renal impairment: dose should be adjusted
  • Hypersensitivity reactions: Anaphylactic reactions and allergic skin reactions, serious, occasionally fatal, may occur after first dose
  • Peripheral neuropathy (Rare cases): discontinue if symptoms occur in order to prevent irreversibility (symptoms of neuropathy include pain, burning, tingling, numbness, and/or weakness or other alterations of sensation including light touch, pain, temperature, position sense, and vibratory sensation)
  • Hepatotoxicity: Severe, and sometimes fatal, hepatoxicity has been reported. Discontinue immediately if signs and symptoms of hepatitis occur (jaundice, dark urine, pruritus or tender abdomen)
  • May exacerbate muscle weakness in persons with myasthenia gravis. Levofloxacin is not recommended in patients with a known history of Myasthenia gravis.

[edit] INTERACTIONS

  • Multivalent cation containing products including iron salts, zinc salts, magnesium or aluminium-containing antacids or didanosine decrease the absorption of levofloxacin .These products or drugs should not be taken 2 hours before or after levofloxacin tablet administration. Calcium salts have a minimal effect on the oral absorption of levofloxacin.
  • Sucralfate: The bioavailability of Levofloxacin tablets is significantly reduced when administered together with sucralfate. Administer sucralfate 2 hours after the levofloxacin tablet administration.
  • Use with caution in patients receiving drugs known to prolong the QT (See WARNINGS AND PRECAUTIONS)
  • Antidiabetic agents (with oral hypoglycemic agent (e.g., glibenclamide) or with insulin): Cases of hypoglycemic coma have been reported. Monitor carefully blood glucose.

[edit] PREGNANCY AND LACTATION

  • Pregnancy Category C (US). Levofloxacin should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.
  • Nursing mothers: 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.

[edit] SIDE EFFECTS

Most common adverse reactions are nausea, headache, diarrhea, insomnia, constipation and dizziness.

For More serious adverse reactions see WARNINGS AND PRECAUTIONS

[edit] RELATED LINKS

[edit] BIBLIOGRAPHY

[edit] REFERENCES

  1. http://www.ncbi.nlm.nih.gov/pubmed/23388361