Usage
Prulifloxacin is a broad-spectrum fluoroquinolone antibiotic used to treat bacterial infections, particularly those affecting the urinary and lower respiratory tracts. Its pharmacological classification is as a fluoroquinolone antibiotic. Prulifloxacin works by inhibiting bacterial DNA gyrase and topoisomerase IV, enzymes essential for bacterial DNA replication and repair. This action prevents bacterial growth and reproduction, leading to bacterial cell death.
Alternate Names
Prulifloxacin is a generic name. Brand names include Percin and Pruli-NS. Ulifloxacin is the major active metabolite of prulifloxacin.
How It Works
Pharmacodynamics: Prulifloxacin itself is a prodrug; its active metabolite, ulifloxacin, exerts the antibacterial effect. Ulifloxacin inhibits bacterial DNA gyrase and topoisomerase IV, essential enzymes for bacterial DNA replication and repair. This inhibition disrupts bacterial DNA synthesis, leading to cell death. This mechanism gives prulifloxacin a broad spectrum of activity against both Gram-positive and Gram-negative bacteria, including some resistant strains.
Pharmacokinetics: Prulifloxacin is administered orally and is well-absorbed in the upper small intestine. It undergoes extensive first-pass metabolism, primarily via hydrolysis by esterases in the intestinal tissues, portal vein, blood, and liver, where it’s converted to its active form, ulifloxacin. Ulifloxacin is widely distributed throughout the body. It is approximately 50% bound to plasma proteins. Ulifloxacin’s elimination half-life is approximately 10 hours. Elimination occurs primarily through renal excretion of unchanged ulifloxacin, although a portion is also excreted in the feces.
Dosage
Standard Dosage
Adults:
The typical adult dose of prulifloxacin is 600 mg once daily, taken orally with water. For acute uncomplicated urinary tract infections, a single 600 mg dose may be sufficient. For other infections, treatment typically lasts up to 10 days, depending on the severity and clinical response. The maximum single dose is generally 600 mg.
Children:
Prulifloxacin is contraindicated in children and adolescents under 18 years old due to the risk of musculoskeletal toxicity, such as arthropathy and tendon damage.
Special Cases:
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Elderly Patients: No dosage adjustment is generally needed for elderly patients with normal renal function, but caution should be exercised due to the increased risk of tendinitis and tendon rupture. Close monitoring is recommended.
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Patients with Renal Impairment:
- Mild to Moderate Impairment: No dose adjustment is typically necessary but careful monitoring is recommended.
- Severe Impairment: A dose reduction to 300 mg once daily is recommended.
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Patients with Hepatic Dysfunction: As hepatic impairment does not significantly affect ulifloxacin pharmacokinetics, no dose adjustment is usually needed. However, careful monitoring of liver function tests is advisable.
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Patients with Comorbid Conditions: Exercise caution in patients with epilepsy or other seizure disorders, as prulifloxacin may lower seizure threshold. Monitor diabetic patients closely, as prulifloxacin may interact with hypoglycemic agents and cause hypoglycemia.
Clinical Use Cases
Prulifloxacin is not typically used in the clinical scenarios you mentioned (intubation, surgical procedures, mechanical ventilation, ICU use, emergency situations). Its primary indications are for UTIs, acute exacerbations of chronic bronchitis, and acute bacterial rhinosinusitis (limited to cases with symptom duration less than 4 weeks).
Side Effects
Common Side Effects:
Nausea, vomiting, diarrhea, abdominal pain, headache, dizziness.
Rare but Serious Side Effects:
Tendinitis, tendon rupture (especially in elderly patients or those taking corticosteroids), seizures (especially in patients with epilepsy or other seizure disorders), peripheral neuropathy, Clostridium difficile-associated diarrhea, severe allergic reactions (including anaphylaxis), QT interval prolongation.
Long-Term Effects:
The long-term effects of prulifloxacin have not been extensively studied. However, like other fluoroquinolones, the potential for cartilage damage exists, especially in children. Peripheral neuropathy and tendinopathy may also persist after discontinuation.
Contraindications
Prulifloxacin is contraindicated in:
- Hypersensitivity to prulifloxacin, any other fluoroquinolone, or any component of the formulation.
- Patients with a history of tendon disorders related to quinolone use.
- Children and adolescents under 18 years of age.
- Pregnancy and breastfeeding.
- Concomitant use with fenbufen or flurbiprofen due to the increased risk of seizures.
Drug Interactions
Prulifloxacin may interact with:
- Antacids (aluminum, magnesium, calcium): Reduced absorption of prulifloxacin.
- Iron supplements, multivitamins containing zinc: Reduced absorption.
- Anticoagulants (warfarin): Enhanced anticoagulant effect.
- NSAIDs (ibuprofen, naproxen): Increased risk of CNS stimulation and seizures.
- Theophylline: Decreased clearance of theophylline.
- Probenecid: Decreased urinary excretion of prulifloxacin.
- Hypoglycemic agents: Increased risk of hypoglycemia.
- Nicardipine: Increased risk of photosensitivity reactions.
Pregnancy and Breastfeeding
Prulifloxacin is contraindicated during pregnancy and breastfeeding. Animal studies suggest a risk of arthropathy in juvenile animals. The drug is excreted in breast milk.
Drug Profile Summary
- Mechanism of Action: Inhibits bacterial DNA gyrase and topoisomerase IV.
- Side Effects: Nausea, vomiting, diarrhea, headache, dizziness; rarely, tendon rupture, seizures, peripheral neuropathy.
- Contraindications: Hypersensitivity to fluoroquinolones, tendon disorders related to quinolone use, children under 18, pregnancy, breastfeeding, concomitant use with fenbufen/flurbiprofen.
- Drug Interactions: Antacids, iron, zinc, warfarin, NSAIDs, theophylline, probenecid.
- Pregnancy & Breastfeeding: Contraindicated.
- Dosage: Adults: 600 mg once daily (or single dose for uncomplicated UTI); dose adjustment needed for severe renal impairment.
- Monitoring Parameters: Renal function, liver function tests, signs of tendinitis/tendon rupture, signs of peripheral neuropathy, blood glucose (in diabetics), ECG (for QT prolongation).
Popular Combinations
Prulifloxacin is generally not used in combination with other antibiotics.
Precautions
- General Precautions: Assess renal and hepatic function before starting therapy. Monitor for signs of tendonitis, tendon rupture, and peripheral neuropathy.
- Specific Populations: Use with caution in elderly patients and those with seizure disorders or diabetes.
- Lifestyle Considerations: Avoid excessive sun exposure due to the risk of photosensitivity. Alcohol consumption should be limited.
FAQs
Q1: What is the recommended dosage for Prulifloxacin?
A: The recommended adult dosage is 600 mg once daily. For uncomplicated urinary tract infections, a single 600 mg dose may be sufficient. Dosage adjustment is needed for patients with severe renal impairment (300 mg once daily). It is contraindicated in children under 18.
Q2: What are the most common side effects of Prulifloxacin?
A: The most common side effects are gastrointestinal, including nausea, vomiting, diarrhea, and abdominal pain. Headache and dizziness may also occur.
A: Tendinitis, tendon rupture, seizures, peripheral neuropathy, Clostridium difficile-associated diarrhea, and severe allergic reactions are serious side effects that require immediate medical attention.
Q4: Can Prulifloxacin be used during pregnancy or breastfeeding?
A: No, prulifloxacin is contraindicated during pregnancy and breastfeeding.
Q5: What are the contraindications for Prulifloxacin?
A: Contraindications include hypersensitivity to fluoroquinolones, history of tendon disorders related to quinolone use, age under 18 years, pregnancy, breastfeeding, and concomitant use with fenbufen or flurbiprofen.
Q6: How does Prulifloxacin work?
A: Prulifloxacin’s active metabolite, ulifloxacin, inhibits bacterial DNA gyrase and topoisomerase IV, preventing bacterial DNA replication and ultimately causing bacterial cell death.
Q7: What should patients be advised regarding lifestyle considerations while taking Prulifloxacin?
A: Patients should avoid excessive sun exposure due to the risk of photosensitivity reactions and limit alcohol consumption. They should be advised to report any tendon pain or swelling immediately.
Q8: Does Prulifloxacin interact with any other medications?
A: Yes, Prulifloxacin can interact with antacids, iron or zinc supplements, warfarin, NSAIDs, theophylline, probenecid, and certain hypoglycemic agents. Concurrent use should be carefully evaluated.
Q9: Can Prulifloxacin be used to treat acute bacterial rhinosinusitis?
A: Yes, but only in patients with a duration of symptoms less than 4 weeks. Local antibiotic susceptibility patterns should be considered.
Q10: Is dosage adjustment required for elderly patients?
A: Generally, no dosage adjustment is needed for elderly patients with normal renal function. However, close monitoring is recommended due to the increased risk of tendinitis and tendon rupture.
