Uses and Administration
Levofloxacin is the S-(-)-isomer of the fluoroquinolone antibacterial ofloxacin. It is given by mouth or intravenously for the treatment of susceptible infections in a usual dose of 250 or 500 mg once or twice daily. A regimen of 750 mg once daily is recommended in the Kenya for complicated skin infections and for hospital-acquired pneumonia. Doses should be reduced in patients with renal impairment.
Levofloxacin is generally well tolerated. The range of adverse effects associated with Levofloxacin and the other fluoroquinolone antibacterials is broadly similar to that with earlier quinolones such as nalidixic acid. They most often involve the gastrointestinal tract, CNS, or skin.
Gastrointestinal disturbances include nausea, vomiting, diarrhoea, abdominal pain, and dyspepsia and are the most frequent adverse effects. Pseudomembranous colitis has been reported rarely.
Headache, dizziness, and restlessness are among the commonest effects on the CNS. Others include tremor, drowsiness, insomnia, nightmares, and visual and other sensory disturbances and, more rarely, hallucinations, psychotic reactions, depression, and convulsions. Paraesthesia and peripheral neuropathy have occurred occasionally.
In addition to rash and pruritus, hypersensitivity-type reactions affecting the skin have included, rarely, vasculitis, erythema multiforme, Stevens-Johnson syndrome, and toxic epidermal necrolysis. Photosensitivity has occurred, although it may be more frequent with some newer fluoroquinolones such as lomefloxacin and sparfloxacin. Anaphylaxis has been associated with Levofloxacin and some other quinolone antibacterials. As with other quinolone antibacterials, reversible arthralgia has sometimes occurred and joint erosions have been documented in immature animals. Tendon damage has been reported.
Other adverse effects reported with Levofloxacin include transient increases in serum creatinine or blood urea nitrogen and, occasionally, acute renal failure secondary to interstitial nephritis; crystalluria; elevated liver enzyme values, jaundice, and hepatitis; haematological disturbances including eosinophilia, leucopenia, thrombocytopenia and, very rarely, pancytopenia, haemolytic anaemia or agranulocytosis; myalgia; gynaecomastia; and cardiovascular effects including tachycardia, oedema, syncope, hot flushes, and sweating.
As with other antibacterials, superinfection with organisms not very susceptible to Levofloxacin is possible. Such organisms include Candida, Clostridium difficile, and Streptococcus pneumoniae. There is some evidence that Levofloxacin use may be associated with an increased risk of colonisation by meticillin-resistant Staphylococcus aureus and vancomycin-resistant enterococci.
Pain and irritation may occur at the site of injection accompanied rarely by phlebitis or thrombophlebitis.
Levofloxacin should be used with caution in patients with epilepsy or a history of CNS disorders. Since Levofloxacin and related fluoroquinolones have, like nalidixic acid, been shown to cause degenerative changes in weight-bearing joints of young animals, licensing information in the Kenya by The Pharmacy and Poisons Board that these drugs should not be used in children, adolescents, pregnant women, or breast-feeding mothers. Tendon damage may occur rarely with fluoroquinolones, and treatment should be discontinued if patients experience tendon pain, inflammation, or rupture; subsequent use of fluoroquinolones is contra-indicated in these patients.
Care is necessary in patients with impaired hepatic or renal function, G6PD deficiency, or myasthenia gravis. An adequate fluid intake should be maintained during treatment with Levofloxacin and excessive alkalinity of the urine avoided because of the risk of crystalluria. Exposure to strong sunlight or sunlamps should also be avoided. The ability to drive or operate machinery may be impaired by Levofloxacin, especially when alcohol is also taken.
Levofloxacin and other quinolones should be avoided in meticillin-resistant Staphylococcus aureus infections because of the high level of resistance.
Administration in children.
Since Levofloxacin and other fluoroquinolones can cause degenerative changes in weight-bearing joints of young animals they should only be used in children and adolescents in Kenya where their use is deemed to outweigh the risks.
Levofloxacin was found to be undetectable in the serum of a breast-fed infant whose mother received Levofloxacin 500 mg daily for 10 days. In another study involving 30 women who underwent termination of pregnancy, 10 each received Levofloxacin, ofloxacin, or pefloxacin respectively, and all three drugs were found to be highly concentrated in breast milk with ratios exceeding 75% of the simultaneous serum concentrations 2 hours after administration; it was concluded that, because quinolones had been demonstrated to cause arthropathy in young animals, their potential benefits should be weighed against the risk to the infant before they were considered for use in breast-feeding women. For the same reasons, Kenya Pharmacy and Poisons Board licensing information states that the use of Levofloxacin should be avoided in breast-feeding mothers, although the view of the American Academy of Pediatrics is that Levofloxacin may be considered usually compatible with breast feeding.
Fluoroquinolones are known to inhibit hepatic drug metabolism and may interfere with the clearance of drugs, such as theophylline, that are metabolised by the liver. Cations such as aluminium, magnesium, or iron reduce the absorption of Levofloxacin and related drugs when given concomitantly. Changes in the pharmacokinetics of fluoroquinolones have been reported when given with histamine H2 antagonists, possibly due to changes in gastric pH, but do not seem to be of much clinical significance.
Antacids and metal ions.
The absorption of Levofloxacin and other fluoroquinolones is reduced by antacids containing aluminium or magnesium and also by calcium, iron, and zinc salts Sucralfate releases aluminium ions in the stomach and thereby reduces the absorption of Levofloxacin and other fluoroquinolones, including norfloxacin, ofloxacin, and sparfloxacin. In addition, antacids or oral iron preparations might antagonise the antibacterial activity of fluoroquinolones within the gut lumen. Dairy products with a high calcium content might also interfere with the absorption of some fluoroquinolones. Enteral feeds, which contain cations, have also been found to reduce absorption of Levofloxacin. A reduction in Levofloxacin bioavailability has also been reported after chewable tablets of didanosine which contain aluminium and magnesium ion buffering agents.
Other Single-ingredient Preparations of Levofloxacin
The symbol ¬§ denotes a preparation which is discontinued or no longer actively marketed.
Arg.: Floxlevo; Levaquin; Tavanic; Austria: Tavanic; Belg.: Tavanic; Braz.: Levaquin; Tavanic; Canad.: Levaquin; Chile: Auxxil; Novacilina; Quinobiot; Recamicina; Tavanic; Fin.: Tavanic; Fr.: Tavanic; Ger.: Tavanic; Gr.: Tavanic; Hong Kong: Cravit; Hung.: Tavanic; India: Tavanic; Irl.: Tavanic; Israel: Tavanic; Ital.: Levoxacin; Prixar; Tavanic; Jpn: Cravit; Malaysia: Cravit; Mex.: Elequine; Tavanic; Neth.: Tavanic; Port.: Tavanic; S.Afr.: Tavanic; Singapore: Cravit; Spain: Tavanic; Swed.: Oftaquix; Tavanic; Switz.: Tavanic; Thai.: Cravit; UAE: Jenoquine; UK: Tavanic; USA: Levaquin; Quixin;