Usage
Ofloxacin + Prednisolone is prescribed for bacterial infections accompanied by inflammation. It is particularly useful in conditions like conjunctivitis, corneal ulcers, and uveitis. This combination is also used in other inflammatory conditions where bacterial infection is a concern, such as otitis externa.
Pharmacological Classification:
- Ofloxacin: Fluoroquinolone antibiotic
- Prednisolone: Corticosteroid
Mechanism of Action:
Ofloxacin inhibits bacterial DNA gyrase and topoisomerase IV, enzymes essential for bacterial DNA replication, leading to bacterial cell death. Prednisolone, a synthetic glucocorticoid, exerts anti-inflammatory and immunosuppressive effects by binding to glucocorticoid receptors and modulating gene expression, suppressing the production of inflammatory mediators.
Alternate Names
While the generic name “Ofloxacin + Prednisolone” is widely recognized, there may be regional variations. This combination is typically not referred to by a single international nonproprietary name (INN) since it is a fixed-dose combination of two separate active ingredients.
Brand Names: Examples of brand names this combination may be marketed under include Oflozee P, and other regional and local variations may also exist.
How It Works
Pharmacodynamics: Ofloxacin exerts a bactericidal effect by inhibiting bacterial DNA replication. Prednisolone reduces inflammation and suppresses the immune response by modulating the expression of multiple genes involved in inflammation.
Pharmacokinetics:
- Ofloxacin: Well-absorbed orally, reaching peak plasma concentrations in 1-2 hours. Metabolized in the liver and excreted primarily through the kidneys.
- Prednisolone: Absorbed well orally. Metabolized in the liver and excreted in urine.
Mode of Action: Ofloxacin inhibits DNA gyrase and topoisomerase IV. Prednisolone binds to glucocorticoid receptors in the cytoplasm, translocates to the nucleus, and interacts with DNA to modify gene transcription, resulting in reduced inflammation.
Receptor Binding, Enzyme Inhibition, or Neurotransmitter Modulation: Ofloxacin inhibits bacterial DNA gyrase and topoisomerase IV. Prednisolone binds to glucocorticoid receptors.
Elimination Pathways: Ofloxacin is primarily eliminated renally. Prednisolone is metabolized in the liver and excreted in the urine.
Dosage
Standard Dosage
Adults:
- Ophthalmic: 1-2 drops in the affected eye(s) every 2-4 hours for the first two days, then four times daily for 8 days. Dosage strength usually contains Ofloxacin 0.3% and Prednisolone 1%.
Children: Pediatric ophthalmic use should follow the same regimen as adults unless otherwise directed by a physician. Consider age and weight for adjustments in certain situations.
Special Cases:
- Elderly Patients: Similar to adults, but close monitoring for adverse effects, particularly tendon rupture, is warranted.
- Patients with Renal Impairment: Dose adjustment may be needed for severe renal impairment.
- Patients with Hepatic Dysfunction: Caution advised; dosage adjustment may be required in severe liver dysfunction.
- Patients with Comorbid Conditions: Patients with diabetes should be monitored for increased blood glucose levels. Caution in patients with hypertension due to potential fluid retention from prednisolone. Close monitoring of patients with a history of tendon disorders, particularly if they are also taking systemic corticosteroids.
Clinical Use Cases
Dosing for clinical scenarios other than standard eye infections is not recommended with the Ofloxacin + Prednisolone combination. These use cases would be managed with other forms of ofloxacin or prednisolone.
Dosage Adjustments
Dosage adjustments should be made on a patient-specific basis, taking into account age, weight, renal function, hepatic function, and concomitant medications.
Side Effects
Common Side Effects
- Ocular: Transient burning, stinging, itching, discomfort, blurred vision, foreign body sensation, photophobia, tearing, dry eyes.
- Systemic: Headache, nausea, dizziness.
Rare but Serious Side Effects
- Tendon rupture (especially Achilles tendon)
- Peripheral neuropathy
- Seizures
- Pseudomembranous colitis
Long-Term Effects
- Cataracts
- Glaucoma
- Increased intraocular pressure
- Secondary ocular infections (fungal or viral)
Adverse Drug Reactions (ADR)
- Hypersensitivity reactions (e.g., rash, itching, swelling, severe dizziness, difficulty breathing)
- Stevens-Johnson syndrome
- Toxic epidermal necrolysis
Contraindications
- Hypersensitivity to ofloxacin, prednisolone, or any component of the formulation.
- Viral or fungal infections of the eye.
- Mycobacterial eye infections (tuberculosis).
- Untreated purulent eye infections.
Drug Interactions
- Nonsteroidal anti-inflammatory drugs (NSAIDs): Increased risk of tendon rupture.
- Anticoagulants (e.g., warfarin): Prednisolone may enhance or decrease anticoagulant effect; monitor INR.
- Oral hypoglycemics: Prednisolone may increase blood glucose levels; monitor blood glucose.
- Antacids, iron, zinc: Reduced absorption of ofloxacin.
Pregnancy and Breastfeeding
- Pregnancy: Prednisolone is generally considered safe during pregnancy. Ofloxacin safety data is limited; use only if potential benefit outweighs the risk.
- Breastfeeding: Both ofloxacin and prednisolone are present in breast milk; potential risks to the infant should be considered.
Drug Profile Summary
- Mechanism of Action: Ofloxacin inhibits bacterial DNA replication. Prednisolone provides anti-inflammatory and immunosuppressive effects.
- Side Effects: Common: Transient ocular discomfort, headache. Serious: Tendon rupture, peripheral neuropathy.
- Contraindications: Hypersensitivity, viral/fungal eye infections.
- Drug Interactions: NSAIDs, anticoagulants, oral hypoglycemics.
- Pregnancy & Breastfeeding: Use with caution; consider risk/benefit ratio.
- Dosage: Ophthalmic: 1-2 drops in the affected eye every 2-4 hours initially, then four times a day.
- Monitoring Parameters: Monitor for signs of tendonitis/rupture, increased intraocular pressure, blood glucose levels (diabetics), INR (if on warfarin).
Popular Combinations
While ofloxacin and prednisolone are commonly combined ophthalmically, systemic combinations of other fluoroquinolones and corticosteroids might be used in certain clinical contexts, but this is not common practice due to the increased risk of serious side effects like tendon rupture.
Precautions
- General Precautions: Avoid contact lenses during treatment. Monitor for adverse effects, especially tendon inflammation or pain.
- Specific Populations: As described in the Dosage section.
- Lifestyle Considerations: Avoid driving or operating machinery if blurred vision occurs.
FAQs (Frequently Asked Questions)
Q1: What is the recommended dosage for Ofloxacin + Prednisolone eye drops?
A: The typical dosage is 1-2 drops in the affected eye(s) every 2-4 hours for the initial two days, followed by four times a day for a total of 8 days.
Q2: What are the most common side effects of Ofloxacin + Prednisolone eye drops?
A: Common side effects include transient burning, stinging, itching, foreign body sensation, and blurred vision.
Q3: What are the serious side effects of Ofloxacin + Prednisolone?
A: Tendon rupture (especially Achilles tendon), peripheral neuropathy, seizures, and severe allergic reactions.
Q4: Can Ofloxacin + Prednisolone be used in children?
A: Yes, similar dosage regimen as adults, but careful monitoring is crucial, especially in younger children.
Q5: What are the contraindications for Ofloxacin + Prednisolone?
A: Hypersensitivity to either drug, viral/fungal eye infections, mycobacterial infections, and untreated purulent eye infections.
Q6: Can Ofloxacin + Prednisolone be used during pregnancy or breastfeeding?
A: Use with caution. Consult with a specialist to weigh the benefits against the potential risks.
Q7: What are the drug interactions to be aware of with Ofloxacin + Prednisolone?
A: NSAIDs, anticoagulants (e.g., warfarin), and oral hypoglycemics. Antacids, iron and zinc can reduce absorption of ofloxacin.
Q8: What should patients be advised regarding the use of Ofloxacin + Prednisolone eye drops?
A: Avoid contact lenses during treatment. Report any vision changes, tendon pain, or signs of allergic reaction immediately. Shake well before use. Do not touch the tip of the bottle to any surface.
Q9: How does Ofloxacin + Prednisolone work in treating eye infections?
A: Ofloxacin eliminates bacteria while prednisolone reduces inflammation, promoting faster healing and symptom relief.
