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FLUOROQUINOLONES; A WOLF IN SHEEP'S CLOTHING

   ARE FLUOROQUINOLONES SAFE ? 

HOW DO FLUOROQUINOLONES WORK?

Fluoroquinolones are a broad spectrum of antibiotics which has been prescribed for many common conditions such as anthrax, urinary tract infections, acute sinusitis, bronchitis, meningococcal meningitis, etc. 

Fluoroquinolones include norfloxacin, Lomefloxacin, ciprofloxacin, ofloxacin, gatifloxacin, levofloxacin, sparfloxacin, fleroxacin, moxifloxacin, gemifloxacin, garenofloxacin, and trovafloxacin. 

Fluoroquinolones are bactericidal and act by inhibiting DNA gyrase (topoisomerase II) and topoisomerase IV, resulting in inhibition of DNA replication of the bacteria. However, the risks of fluoroquinolones outweigh the benefits. 

FDA has updated warnings for fluoroquinolones about the risks of mental health side effects and dysglycemic effects.

 https://www.fda.gov/news-events/press-announcements/fda-updates-warnings-fluoroquinolone-antibiotics-risks-mental-health-and-low-blood-sugar-adverse

Due to these controversies, some of these drugs have been withdrawn from the markets of the United States as well as India. 


 

SIDE EFFECTS OF FLUOROQUINOLONES

What are the side effects of fluoroquinolones? Well, there are many. Gastrointestinal distress is the most common side effect followed by CNS adverse effects. Clinicians had been always warned about the side effects of fluoroquinolones, but recently these warnings have been reinforced. Fluoroquinolones have been causing disabling and potentially permanent side effects to the patient. There have also been many increased cases of drug resistance to fluoroquinolones.

 The two main adverse effects of fluoroquinolones that have been found out recently are the change in the blood sugar level and mental health issues. The clinicians can easily recognize high or low blood sugar but mental health issues can be more subtle, hence, difficult to prove that they are being caused due to fluoroquinolone administration. 

GI distress being one of the most common side effects of fluoroquinolones manifests as anorexia, vomiting, nausea, and abdominal discomfort. Fluoroquinolones may also be responsible for Clostridium-difficile associated diarrhea. 

In the United States, there has been increased resistance of fluoroquinolones with Methicillin-resistant Staphylococcus aureus (MRSA) and Pseudomonas aeruginosa.

 It is very important to keep in mind that if a patient had previously encountered any of the side effects of fluoroquinolones, he or she shouldn't be administered the drug ever again.

 The next most frequent adverse effect which has been found recently is that the fluoroquinolones affect the central nervous system, but it is seen only in 10% of the patients. The CNS symptoms could be manifested as headache, dizziness, and insomnia. The serious implications of fluoroquinolones are seizures, delirium, and frank hallucinations. Some incidence of clinical neuropathies such as burning and tingling sensation, weakness, etc has also been noticed in patients treated with fluoroquinolones. 

Clinical neuropathy can result within a few days of use of the drug and there is no specific treatment for it, whereas, peripheral neuropathy can occur at any time during the course of the treatment and it may last for years which proves to be very problematic for the patients.

 Fluoroquinolones also worsen muscle weakness in patients suffering from myasthenia gravis. They may also cause cartilage problems, hence are not advocated in children less than 18 years of age and in pregnancy. The most common tendon injury resulting due to fluoroquinolones is Achilles tendinitis which results due to tendon rupture and can lead to the need for surgery. Achilles tendinitis can occur in the initial phase of the treatment and are completely unpredictable. There have been many cases of patients on fluoroquinolones developing Achilles tendinitis. 

Some fluoroquinolones, for example, Sparfloxacin and Gatifloxacin have been linked with prolonging QT interval and arrhythmia (torsades de pointes) Owing to these reasons, these drugs have been withdrawn from the market. Gatifloxacin has also been linked to hypo or hyperglycemia. 

Trovafloxacin has the potential to lead to hepatotoxicity. 

When NSAIDs are combined with fluoroquinolones, it increases CNS toxicity (seizures). Fluoroquinolones are strictly contraindicated in epilepsy, as they decrease the seizure threshold. 

The fluoroquinolones which have been withdrawn from the market are :

  1. Temafloxacin for causing immune hemolytic anemia.
  2. Trovafloxacin for causing hepatoxicity.
  3. Grepafloxacin for causing cardiotoxicity and increased QT interval.
  4. Clinafloxacin for causing phototoxicity. 


 

WHEN TO AVOID FLUROQUINOLONES?

If you’re on fluoroquinolones, keep a keen eye on yourself and in case you encounter any of the following signs such as, the sign of tendon injury or if you feel pins and needles, tingling or burning sensation in your legs and arms, or if there is any swelling in your shoulder, legs or arms, don’t hesitate to consult your doctor. The patients on these drugs can also ask their physicians to change their drugs if there are other options available. If you’re an epileptic patient, you must strictly avoid fluoroquinolones. If you are taking a corticosteroid such as hydrocortisone or prednisolone, you may be at a higher risk of developing tendinitis. Hence, both the patient and the physician need to avoid fluoroquinolones, as much as they can.

 

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