LEVOFLOXACIN (Levaquin): What is used for?

What is Levofloxacin?

Levofloxacin is an active ingredient used for the treatment of various infections: acute bacterial sinusitis, acute exacerbation of chronic bronchitis, community-acquired pneumonia, complicated skin infection, cystitis, prostatitis…
The product ingredient of Levofloxacin is Levofloxacin hemihydrate.

The brand names of Levofloxacin in the United States are: Levaquin and Levaquin Leva-Pak.

Mechanism of action (MOA) of Levofloxacin

Fluoroquinolonic antibacterial agent, levofloxacin acts on the DNA-DNA girase complex and on topoisomerase IV.

Therapeutic indications, uses and benefits of Levofloxacin

Adults, treatment of: pyelonephritis and complicated urinary tract infections, chronic bacterial prostatitis, uncomplicated cystitis, inhalational anthrax (treatment and post-exposure prophylaxis).

Treatment, when the recommended antibacterials are inappropriate, of: acute bacterial sinusitis, acute exacerbation of chronic bronchitis, community-acquired pneumonia, complicated infection of skin and soft tissues.

Dosage of Levofloxacin

Adults.

Acute bacterial sinusitis: 500 mg, 1 time/day orally, 10-14 days. Acute exacerbation of chronic bronchitis: 500 mg, 1 time/day orally, 7-10 days.
Community acquired pneumonia: 500 mg once/day or 500 mg twice/day, 7-14 days oral or slow intravenous perfusion.
Pyelonephritis: 500 mg, 1 time/day orally or slow intravenous perfusion, 7-10 days.

Complicated urinary tract infection: 500 mg 1 time/day, 7-14 days oral or slow intravenous perfusion.
Uncomplicated urinary tract infections, cystitis: 250 mg once/day orally, 3 days.
Chronic bacterial prostatitis: 500 mg once/day, 28 days oral or slow intravenous perfusion.
Complicated skin and soft tissue infections: 500 mg 1 time/day orally or 500 mg 2 times/day orally or slow intravenous infusion, 7-14 days.
Inhalation anthrax: 500 mg once/day orally or slow intravenous infusion, 8 weeks.

Duration of treatment should be continued at least 48-72 hours after the patient remains fever-free or bacterial eradication has been demonstrated.

Method of administration

Oral use:
The tablets should be swallowed without chewing and with a sufficient amount of liquid. They can be divided by slot to adjust dosage and taken during or between meals.
They should be taken at least 2 hours before or after the administration of salts of Fe or Zn, antacids containing Mg or Al, didanosine formulations with Al or Mg containing buffering agents and sucralfate.

Intravenous (IV) use:
The infusion is slow of minimum 30 minutes for 250 mg and 60 minutes for 500 mg.

Contraindications with Levofloxacin

• Hypersensitivity to levofloxacin or other quinolones.
• Patients with epilepsy.
• Patients with a history of tendon disorders related to the administration of fluoroquinolones.
• Children or adolescents in growth phase.
• Pregnancy and lactation.

Levofloxacin Warnings and Cautions

Warnings

• Kidney failure, adjust dosage.
• Methicillin-resistant S. aureus is probably resistant to levofloxacin.
• Consider local resistance to E. coli.
• Inhalational anthrax, consult national and/or international consensus documents on its treatment.
• Risk of tendinitis and tendon rupture (greater in > 60 years, those who receive doses > 1000 mg/day and treated with corticosteroids), discontinue treatment at any sign of tendinitis and keep the affected limb at rest.
• Risk of: pseudomembranous colitis (discontinuation of treatment), haemolytic reactions in patients with G6PDH deficiency, severe and life-threatening hypersensitivity reactions (e.g. angioedema, anaphylactic shock) after administration of the first dose, severe skin reactions (s.). of Stevens Johnson or toxic epidermal necrolysis), hyper or hypoglycaemia in diabetics (glucose monitoring), bleeding and increased clotting tests in vitamin K antagonists (control), psychotic reactions and superinfection by non-sensitive microorganisms in prolonged treatment.

Cautions

• Caution in: patients predisposed to seizures or treatment with drugs that lower the seizure threshold (e.g. theophylline), psychotic patients or patients with a history of psychiatric illness, patients at risk of prolongation of QT interval: congenital syndrome with long QT interval, uncorrected electrolyte imbalance (e.g. hypokalemia, hypomagnesaemia), heart disease (e.g., hypognesaemia). heart failure, myocardial infarction, bradycardia), concomitance with QT interval extenders (class IA and III antiarrhythmics, tricyclic antidepressants, macrolides, antipsychotics), elderly, women; reported cases of sensory or sensory-motor polyneuropathy leading to paresthesia, hypoesthesia, dysesthesia or weakness and liver necrosis to fulminant liver failure.
• Not recommended with myasthenia gravis.
• Consult an ophthalmologist if vision deteriorates.
• Avoid UV/solar exposure.
• Do not prescribe quinolones or fluoroquinolones for: treatment of self-limited or mild infections (such as pharyngitis, tonsillitis and acute bronchitis), prophylaxis of traveler’s diarrhea or recurrent lower urinary tract infections, non-bacterial infections or for mild to moderate infections (including uncomplicated cystitis), acute exacerbations of chronic bronchitis and chronic obstructive pulmonary disease, acute bacterial rhinosinusitis and acute otitis media), unless other antibiotics commonly recommended for these infections are considered inadequate and should not be prescribed in patients with a history of serious adverse reactions following administration of this type of antibiotics; Very rare cases of serious disabling, long-lasting (persistent for months or years), and potentially irreversible adverse reactions affecting different and sometimes multiple body systems (musculoskeletal, nervous, psychiatric, and sensory) have been reported in patients receiving quinolones and fluoroquinolones, regardless of their age and pre-existing risk factors (discontinuation of treatment if they occur).
• Increased risk of aneurysm and aortic dissection (especially in the elderly).
• Assess risk/benefit in: patients with a family history of aneurysm, diagnosed with pre-existing aortic aneurysm and/or aortic dissection, or in the presence of other risk factors or disorders predisposing to aortic aneurysm and dissection (Marfan syndrome, Ehlers- Danlos vascular syndrome, Takayasu arteritis, giant cell arteritis, BehÇet disease, hypertension, known atherosclerosis).Avoid in patients who have previously experienced serious adverse reactions with the use of medications containing quinolones or fluoroquinolones.
• Also Intravenous: respect recommended perfusion time and interrupt in case of sudden drop in blood pressure.

Renal insufficiency

Caution. Adjust dose if Clcr ≤ 50 ml/min:

– 250 mg/24 h guideline, initial: 250 mg, then Clcr 50-20 ml/min: 125 mg/24 h; Clcr 19 – 10 ml/min: 125 mg/48 h; Clcr < 10 ml/min, haemodialysis and DPCA: 125 mg/48 h.

– 500 mg/24 h guideline, initial: 500 mg, then Clcr 50-20 ml/min: 250 mg/24 h; Clcr 19 – 10 ml/min: 125 mg/24 h; Clcr < 10 ml/min, haemodialysis and DPCA: 125 mg/24 h.

– 500 mg/12 h guideline, initial: 500 mg, then Clcr 50-20 ml/min: 250 mg/12 h; Clcr 19 – 10 ml/min: 125 mg/12 h; Clcr < 10 ml/min, haemodialysis and DPCA: 125 mg/24 h.

Interactions with Levofloxacin

• Decreased absorption by: salts of Fe or zinc, antacids with Al and Mg, didanosine formulations with Al or Mg containing buffering agents (space 2 h).
• Bioavailability decreased by: sucralfate, to administer it 2 h later.
• Caution with: drugs that lower convulsive threshold (theophylline, fenbufen, NSAIDs); drugs that prolong the QT interval (e.g. class IA and III antiarrhythmics, tricyclic antidepressants, macrolides, antipsychotics).
• Renal clearance decreased by: probenecid, cimetidine.
• Increase in half-life of: cyclosporine.
• Increase in coagulation tests (PT/INR) and/or bleeding with: vit K antagonists (e.g. warfarin).
• Do not mix perfusion IV with: heparin, alkaline solution (e.g. sodium bicarbonate).
• Lab: fake + opiates in urine. False – in bacteriological diagnosis of tuberculosis.

Pregnancy and Levofloxacin

Contraindicated. Animal studies show no harmful effects. Absence of data in humans, experimental risk of injury to weight-bearing cartilage of developing organisms.

Breastfeeding

Levofloxacin is contraindicated in breastfeeding women. Not enough information is available regarding the excretion of levofloxacin in human milk; however, other fluoroquinolones are excreted in breast milk.

Levofloxacin should not be used in lactating women due to the absence of human data and experimental data suggesting the risk of fluoroquinolone injury to weight-bearing cartilage of developing organisms.

Effects on driving ability

Some adverse reactions (e.g. dizziness/vertigo, drowsiness, visual disturbances) may alter the ability of patients to concentrate and react and therefore constitute a risk in situations where these abilities are particularly important (e.g. when driving a vehicle or using machinery).

Adverse reactions and side effects of Levofloxacin

Insomnia; headache, dizziness; diarrhea, vomiting, nausea; increased liver enzymes (ALT/AST, alkaline phosphatase, GGT).

Intravenous: phlebitis, reaction at the site of administration (pain, redness).

Levofloxacin systemic use: severe skin adverse reactions, inflammation and tendon rupture, inadequate secretion of antidiuretic hormone (SIADH).

⭐⭐⭐⭐⭐ VIDEO OF LEVOFLOXACIN/LEVAQUIN (DRUG)

Source: The content of this active ingredient has been written taking into account the clinical and molecular information of all medicines authorised and marketed in the United States under the Unique Ingredient Identifier (UNII) by the Substance Registration System (SRS) of the Food and Drug Administration (FDA) and the United States Pharmacopeia (USP).

In order to know in detail the information authorized by the FDA for each drug, you should consult the corresponding medication guide authorized by the FDA.

Resources:

UNII: 6GNT3Y5LMF
ChemIDplus
DrugPortal
PubChem CID: 3033924
NCI Thesaurus: C1586