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Levaquin, Levofloxacin Review Article

 

LevofloxacinLevaquin, also known as levofloxacin, makes part of a group of antibiotics called flouroquinolones and it is used to treat bacterial infections of the sinuses, kidney, skin, bladder or prostate, but it is also used to treat bacterial infections that cause pneumonia and bronchitis, and also people who have been exposed to anthrax. While taking levofloxacin you should avoid exposure to sunlight, sun lamps or tanning beds because this can make your skin more sensitive to sunlight. Furthermore, this medicine can cause you to have unusual results on certain medical tests so you should inform your doctor that you are taking Levaquin. Levaquin is active against gram-negative aerobic bacteria such as those belonging to the Enterobacteriaceae group, (E. coli and Citrobacter, Enterobacter, Klebsiella, Proteus, Providencia, Salmonella, Serratia, Shigella, and Yersinia). It is also active against P. aeruginosa, N. gonorrhoeae and meningitidis, H. influenzae, M. catarrhalis, Gardnerella vaginalis, H. pylori, Legionella spp., Pasteurella multocida, and Vibrio spp. It is the treatment of choice for Legionella pneumophilia.

Levaquin, Levofloxacin generic (generic - what is it?)

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Levaquin also affects gram positive aerobic bacteria (an advantage over other drugs belonging to the same class), which includes staphylococci (both penicillinase-producing and penicillinase-nonproducing strains, as well as methicillin-resistant Staphylococcus aureus or MRSA). Levaquin belongs to a subset of fluoroquinolones which are active against Streptococci like S. pneumonia (Hooper, 2000) and enterococci (Sweetman, 2009).

LevaquinWith the said microbes, Levaquin is therefore effective in the treatment of a wide spectrum of diseases such as acute bacterial sinusitis, tuberculosis, both complicated and uncomplicated urinary tract infection (effective even against multi drug resistant Pseudomonas strains), acute pyelonephritis, chronic bacterial prostitis, complicated skin infections, hospital or community acquired pneumonia (HAP or CAP), and it is also used for the treatment and prevention of post exposure of anthrax disease. The Center for Disease Control (2002) also recommends Levaquin for uncomplicated gonococcal infections.

The World Health Organization has stated that Levaquin is a reserve second-line agent for multi-drug resistant tuberculosis, a type of tuberculosis that is very hard to cure because of its strong resistance against different antibacterial agents. It is also used for atypical mycobacterial infections.

Fluoroquinolones: Mechanism of Action

The fluoroquinolones, chemically, are fluorinated 4-quinolone compounds which contain a carboxylic moiety at position three of the primary ring, as well as a fluorine atom at position six and piperazine moiety at position 7. Levaquin, specifically, is a chiral fluorinated carboxyquinolone.

Fluoroquinolones are a class of antimicrobial drugs which act on DNA synthesis. These drugs target the bacterial enzyme DNA gyrase (for gram negative bacteria) and Topoisomerase IV (for gram positive bacteria). Both enzymes are important for DNA replication. For gram positive bacteria, topoisomerase IV separates molecules that are produced during replication. On the other hand, for gram negative bacteria, DNA gyrase is involved in the supercoiling of DNA. Thus, when either of the two enzymes is inhibited, DNA replication is inhibited.

Efficacy

Levaquin is one of the most trusted antibiotics when it comes to respiratory tract, urinary tract, and skin infections, possessing above 90% bioavailability in both extracellular and intracellular compartments and activity against a variety of clinically important pathogens (Noel, 2009).

The efficacy of Levaquin in respiratory tract infections such as acute bacterial exacerbations of chronic bronchitis, acute bacterial sinusitis, and both community and hospital pneumonia has been established in several studies. Levaquin’s ability to combat respiratory infections is largely attributable to its excellent penetration in pulmonary tissues, as well as to its remarkable activity towards typical and atypical bacteria that cause upper and lower respiratory tract infections. In one U.S. surveillance program entitled TRUST (Noel, 2009) the activity of Levaquin against 2.858 Streptococcus pneumoniae isolates was determined. It was found that regardless of the nature of the patient and location of the specimens collected, >99% were susceptible to Levaquin, with a minimum inhibitory concentration of 1 ?g/mL. Even more remarkable is the finding that while some of the isolates showed resistance to other drug classes such as penicillins and macrolides, the susceptibility to Levaquin remained unchanged. In other surveillance studies involving Haemophilus influenza and Moraxella catarrhalis, the susceptibility rates for Levaquin are >99% and 100%, respectively (Suzuki, Koguchi, Tanaka, et al., 1995).

Clinical studies have also supported the use of Levaquin in the treatment of community-acquired pneumonia (CAP), especially in patients with comorbidities such as diabetes. In a study by Fogarty, Sullivan, Chattman, et al. (1998), 94% of patients with mild to moderate CAP and 97% of patients with severe CAP were successfully treated with Levaquin. In another study by Fogarty, Siami, Kohler, et al. (2004), monotherapy using Levaquin was found to be comparable to combination therapy with a penicillin and macrolide in patients with severe CAP who require hospitalization and possess poor respiratory rate and hypotension. Likewise, in patients with hospital-acquired pneumonia, Levaquin therapy achieved a 59% success rate compared to a 63% cure rate with imipenem-cilastatin (Shorr, Zadeikis, Jackson, et al., 1998).

Levaquin is also highly recommended for the treatment of acute bacterial sinusitis and acute bacterial exacerbation of chronic bronchitis (ABECB). 7 published studies involving Levaquin therapy in acute bacterial sinusitis displayed a success rate of 86 to 96 percent using Levaquin 500 mg. treatment regimen once daily for 10-14 days (Noel, 2009). In addition, Levaquin at a dose of 500 or 750 mg. was shown to have comparable response rates to beta-lactams, macrolides, and other fluoroquinolones (Noel, 2009).

Fluoroquinolones such as Levaquin are regarded as the first line agents in treating complicated genitourinary tract infections because of their reliability against common uropathogens and their ability to achieve desirable concentrations in the urine and the genitourinary tract. In one study assessing the efficacy of 250 mg of Levaquin for complicated urinary tract infection and acute pyelonephritis (Shorr, Zadeikis, Jackson, et al., 2005), eradication rates of 99% was observed for E. coli, 93% for Klebsiella pneumoniae,100% for Proteus mirabilis, 86% for P. aeruginosa, and 67% for Streptococcus faecalis were observed.

Safety

Aside from its wide spectrum of activity, Levaquin has been extensively used for several infections due to its high safety level. Clinical trials which spanned for over 12 years have stated and proven that Levaquin is extremely well tolerated by patients. The most common side effect of Levaquin is GI disturbances, occurring about 3-17% of patients. These adverse effects include mild nausea and vomiting, abdominal discomfort, diarrhea. Other side effects include mild headache and dizziness, rashes, and photosensitivity (Kahn, 2001).

Patients taking antidiabetic drugs, as well insulin should monitor their blood glucose levels when using Levaquin. There have been reports of hyper- and hypo-glycemia when used among these patients.

QT prolongation has also been observed in patients taking Levaquin. Thus, it should used in caution with patients with known heart problem, uncorrected hypokalemia (low potassium stores affect heart rate), and for patients receiving class IA or class III antiarrhythmic agents (sotalol, ibutilide, amiodarone) and other drugss known to increase the QTc interval.

A dose reduction is recommended for patients with renal disease, since this drug is largely renally excreted. Renal impairment may cause a prolongation of its half life.

Levaquin is generally contraindicated in children and pregnant women, because of the lack of specific studies supporting their safety of use. However, some studies suggests that the adverse effects of Levaquin in children is reversible, and some diseases, such as cystic fibrosis, is safely managed/treated with Levaquin (Noel, Bradley, Kauffman, et al., 2007).

Chemotherapy: Antibacterials

Most people understand chemotherapy as drugs that are used for cancer. In a sense, this is correct. However, chemotherapeutic agents are a group of drugs that can be subdivided into two- first, the most commonly known antineoplastic agents (for cancer), and second, the antimicrobial agents. Antimicrobial agents can be further divided into four- the antibacterials (for bacterial infections), the antifungals (for fungal infections), the antiprotozoals (for ameobas and other parasites such as malaria), and the anthelminthic agents (for worms).

Antibacterials, or antibiotics, are a group of drugs used to treat, and sometimes prevent, bacterial infections. They have been considered a great gift to humanity ever since they were discovered; revolutionizing the field of medicine and the way people saw disease. The history of antibacterials began with salvarsan, which was synthesized in 1910 to provide a cure for syphilis. It was once theorized that a “magic bullet” could attack the causative agent of infections without doing much harm to the body of the host. Soon after the discovery of salvarsan, more natural and synthetic compounds emerged to give rise to the line of antibiotics we have today.

Bacteria are prokaryotic organisms that may be classified as pathogenic (can cause infection) and non pathogenic. They are ubiquitous - present everywhere, in close association with larger, multi-cellular organisms such as humans. Even if some bacteria are pathogenic, they do not always cause infection as the body’s natural defenses prevent this. But when the primary defenses of immune system are overcome, the infection begins. It is at this moment that antibacterial therapy is important.

An interesting note about the battle against bacteria – bacteria are capable of developing resistance. With resistance, bacteria are able to become “immune” to a particular bacterial agent – resulting to a failure of therapy for a patient, which leads to serious complications and sometimes death. Because of the serious threat of bacterial infections, several antibacterial agents have been developed, in hopes of eradicating the disease, or if not, at least prevent the morbidities and mortalities it brings. An important class of antibacterial drugs called the fluoroquinolones, from which Levaquin belongs.

Safety

Aside from its wide spectrum of activity, Levaquin has been extensively used for several infections due to its high safety level. Clinical trials which spanned for over 12 years have stated and proven that Levaquin is extremely well tolerated by patients. The most common side effect of Levaquin is GI disturbances, occurring about 3-17% of patients. These adverse effects include mild nausea and vomiting, abdominal discomfort, diarrhea. Other side effects include mild headache and dizziness, rashes, and photosensitivity (Kahn, 2001).

Patients taking antidiabetic drugs, as well insulin should monitor their blood glucose levels when using Levaquin. There have been reports of hyper- and hypo-glycemia when used among these patients.

QT prolongation has also been observed in patients taking Levaquin. Thus, it should used in caution with patients with known heart problem, uncorrected hypokalemia (low potassium stores affect heart rate), and for patients receiving class IA or class III antiarrhythmic agents (sotalol, ibutilide, amiodarone) and other drugss known to increase the QTc interval.

A dose reduction is recommended for patients with renal disease, since this drug is largely renally excreted. Renal impairment may cause a prolongation of its half life.

Levaquin is generally contraindicated in children and pregnant women, because of the lack of specific studies supporting their safety of use. However, some studies suggests that the adverse effects of Levaquin in children is reversible, and some diseases, such as cystic fibrosis, is safely managed/treated with Levaquin (Noel, Bradley, Kauffman, et al., 2007).

Chelation

All fluoroquinolones are known to have a reaction called chelation with essential metals in the body, such as calcium, chromium, manganese, iron, cobalt, nickel, copper, zinc and cadmium. Chelation with these metals retards the bioavailability of Levaquin (Sultana, Arayne and Sharif 2004).

Chelation is a chemical interaction between a ligand and a metal. A ligand is usually an organic compound that is polydentate in nature (possesses several atoms with several lone electron pairs). These electrons are capable of making a coordinate bond with a metal by acting as a lewis base (electron donors). The metal, on the other hand, is a multivalent compound that acts as a lewis acid (electron acceptor). Chelation occurs when the metal accepts several electron pairs from different atoms in the ligand, enclosing it inside the compound.

Because of the interaction of Levaquin with these metals, Levaquin does not reach the target. Therefore, its efficacy in treating an infection is reduced.

In a study made by Sultana, Arayne and Sharif (2004), they proved this phenomenon. In their study, they made a simple dissolution test following British Pharmacopeia standards using simulated gastric juice, intestinal fluid and blood pH, with dissolved metal ions in the medium. The results of their studies have shown that indeed, the bioavailability of Levaquin is markedly decreased in the presence of these metals- proving the occurrence of chelation.

Dosage

Levaquin is usually given orally or by intravenous infusion as a 5 mg/mL solution over 30 to 90 minutes. The usual oral dose ranges from 250 to 500 mg. once or twice daily for a period of 7-14 days, depending on the severity of the infection. For uncomplicated urinary tract infections, therapy lasts for only 3 days but for more serious conditions such as chronic bacterial prostatitis, a 28-day therapy is required. In the U.S., doses of up to 750 mg. daily for duration of 7-14 days may be used in cases of complicated skin infections and hospital-acquired pneumonia. In cases of community-acquired pneumonia, bacterial sinusitis, complicated urinary tract infections, and acute pyelonephritis, a therapy course of once daily for up to 5 days is used. A 500 mg. daily levaquin therapy for 60 days is also used in the U.S. for treatment of inhalation anthrax (Sweetman, 2009).

Bibliography

Centers for Disease Control and Prevention, 2002, Sexually transmitted diseases treatment guidelines, MMWR Recomm. Rpt., 51(RR6):1–78

Fogarty, C.M., Sullivan, J.G., Chattman, M.S., et al., 1998, Once a day levofloxacin in the treatment of mild to moderate and severe community-acquired pneumonia in adults

Fogarty, C., Siami, G., Kohler, R., et al., 2004, Multicenter, open-label, randomized study to compare the safety and efficacy of levofloxacin versus ceftriaxone sodium and erythromycin followed by clarithromycin and amoxicillin-clavulanate in the treatment of serious community-acquired pneumonia in adults

Hooper, D. C., Quinolones, In, Mandell, Douglas, and Bennett's Principles and Practice of Infectious Diseases, 5th ed. (Mandell, G.L., Bennett, J.E., and Dolin, R., eds.) Churchill Livingstone, New York, pp. 404–423

Kahn, J. B., 2001, Latest industry information on the safety profile of levofloxacin in the U.S

Noel, G. J., Bradley, J. S., Kauffman, R. E., et al., 2007, Comparative safety profile of levofloxacin in 2523 children with a focus on four specific musculoskeletal disorders

Shorr, A. F., Zadeikis, N., Jackson, W. L., et al., 2005, Levofloxacin for treatment of ventilator-associated pneumonia: a subgroup analysis from a randomized trial

Sultana, N., Arayne, M. S., Sharif, S., 2004, Levofloxacin interactions with essential and trace elements

Suzuki, Y., Koguchi, M., Tanaka, S., et al., 1995, Study of clinically isolated new quinolone-resistant Haemophilus influenzae

Sweetman, S. C. ed., 2009, Martindale, The complete drug reference 36th ed, London: Pharmaceutical Press, p. 158,292-293

World Health Organization, 2010, WHO Model list of essential medicine 16th list


 

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