What it's for (Indications)
- Pefloxacin is indicated for urinary tract infections, respiratory tract infections, ear, nose, and throat infections, gynecological infections (infections and inflammations occurring in the vagina and genital tract), abdominal and hepatobiliary (liver plus gallbladder) infection, bone and joint infections, septicemia (blood poisoning due to invasion of bacteria in the bloodstream), endocarditis (inflammation of the heart’s inner lining), and meningitis (inflammation of the meninges, membranous layers covering the brain and spinal cord).
Dosage Information
| Type | Guideline |
|---|---|
| Standard | N/A - Specific dosage and administration guidelines are not provided in the available data. Consult local prescribing information and clinical judgment. |
Safety & Warnings
Common Side Effects
- Pefloxacin, like other fluoroquinolone antibiotics, is associated with a spectrum of potential adverse effects that range from mild to severe, impacting multiple organ systems.
- Common side effects frequently involve the gastrointestinal tract, manifesting as nausea, vomiting, diarrhea, abdominal pain, and dyspepsia.
- Central nervous system (CNS) disturbances are also prevalent, including headache, dizziness, insomnia, nervousness, and, less commonly, confusion, hallucinations, or seizures.
- Dermatological reactions such such as rash, pruritus, and photosensitivity are reported, necessitating advice to avoid excessive sun exposure.
- Of significant concern are musculo-skeletal adverse effects, particularly tendinitis and tendon rupture (most notably Achilles tendon), which can occur during or up to several months post-treatment and may be permanent.
- Other serious adverse events encompass prolongation of the QT interval on an electrocardiogram, peripheral neuropathy that can be irreversible, Clostridioides difficile-associated diarrhea (CDAD), dysglycemia (both hypoglycemia and hyperglycemia), psychiatric adverse reactions, hepatotoxicity, and crystalluria.
- Patients should be counselled to report any unusual or severe symptoms promptly to their prescribing physician for immediate evaluation.
Serious Warnings
- Black Box Warning: As a member of the fluoroquinolone class of antibiotics, pefloxacin is associated with several serious adverse reactions, some of which can be disabling and potentially irreversible. While pefloxacin is not FDA-approved in the United States and thus does not carry a formal FDA Black Box Warning, the following serious warnings, consistent with the fluoroquinolone class, apply and warrant careful consideration before prescription. Pefloxacin should generally be reserved for use in patients who have no alternative treatment options for specific infections. **Serious Warnings Associated with Fluoroquinolone Use:** 1. **Tendinopathy and Tendon Rupture:** Pefloxacin is associated with an increased risk of tendinitis and tendon rupture in all age groups. This risk is notably higher in patients over 60 years of age, individuals concurrently receiving corticosteroid therapy, and transplant recipients (kidney, heart, or lung). Tendon rupture can occur during or after therapy, sometimes several months post-treatment, and can affect the Achilles, shoulder, hand, or other tendons. Patients should be advised to discontinue pefloxacin immediately at the first sign of tendon pain, swelling, or inflammation. 2. **Peripheral Neuropathy:** Cases of sensory or sensorimotor axonal polyneuropathy, characterized by paresthesias, hypoesthesias, dysesthesias, and weakness, have been reported with fluoroquinolone use. These symptoms can manifest soon after initiation of pefloxacin and may become irreversible in some patients. Pefloxacin should be discontinued at once if symptoms of peripheral neuropathy develop. 3. **Central Nervous System (CNS) Effects:** Fluoroquinolones can precipitate a range of serious psychiatric adverse reactions, including hallucinations, anxiety, depression, insomnia, severe nightmares, confusion, and, rarely, psychotic reactions that can progress to suicidal ideations or attempts. Additionally, they can cause seizures, increased intracranial pressure, lightheadedness, and tremors. Pefloxacin should be used with extreme caution in patients with known or suspected CNS disorders that may predispose them to seizures or lower their seizure threshold. 4. **Exacerbation of Myasthenia Gravis:** Fluoroquinolones possess neuromuscular blocking activity and can exacerbate muscle weakness in individuals with myasthenia gravis, potentially leading to severe respiratory compromise and death. Pefloxacin should be avoided in patients with a history of this condition. 5. **Aortic Aneurysm and Dissection:** Epidemiological studies indicate an elevated risk of aortic aneurysm and dissection with fluoroquinolone use, particularly in older patients. This risk is further heightened in patients with pre-existing aortic aneurysmal disease, hypertension, or certain genetic disorders. Use with extreme caution and consider alternative treatments in these high-risk individuals. 6. **Dysglycemia:** Disturbances in blood glucose homeostasis, including symptomatic hypoglycemia and hyperglycemia, have been reported with fluoroquinolone administration. These effects can occur in both diabetic and non-diabetic patients, and in severe cases, hypoglycemia can lead to coma. Close monitoring of blood glucose levels is recommended during pefloxacin therapy.
- Patients should avoid exposure to sun or ultraviolet light during treatment.
- There is a risk of severe hepatic insufficiency (loss of liver functions).
- Streptococci and pneumococci (bacteria) show only immediate susceptibility, and as such, pefloxacin should not be prescribed as a first-line treatment in respiratory tract infections when a bacteriological examination has not been carried out.
How it Works (Mechanism of Action)
Pefloxacin, a synthetic broad-spectrum fluoroquinolone antibiotic, exerts its potent bactericidal activity primarily by inhibiting two crucial bacterial enzymes: DNA gyrase (topoisomerase II) and topoisomerase IV. DNA gyrase is essential for maintaining the superhelical structure of bacterial DNA, facilitating processes such as replication, transcription, and repair. It introduces negative supercoils into DNA, which is vital for DNA unwinding. Topoisomerase IV, on the other hand, is critical for the decatenation (separation) of replicated chromosomal DNA during bacterial cell division. Pefloxacin binds to the DNA-enzyme complex, stabilizing the cleavable complex and preventing the re-ligation of DNA strands after they have been cleaved. This leads to an accumulation of irreversible double-strand DNA breaks, ultimately disrupting vital bacterial DNA processes and triggering a cascade of events that result in bacterial cell death. This precise and targeted interference with bacterial DNA management underscores its effectiveness against a wide spectrum of susceptible pathogenic bacteria, while exhibiting selectivity for prokaryotic topoisomerases over eukaryotic counterparts.
Commercial Brands (Alternatives)
No other brands found for this formula.