Hydroxypropylmethylcellulose + Ofloxacin + Prednisolone

Usage

This combination medication is primarily used to treat bacterial infections of the eye, particularly where inflammation is a significant component. It is commonly prescribed for conditions such as bacterial conjunctivitis, corneal ulcers (bacterial), and other inflammatory ocular conditions susceptible to or complicated by bacterial infection.

• Pharmacological Classification: This is a combination product containing:

  • Ofloxacin: Fluoroquinolone antibiotic
  • Prednisolone: Corticosteroid, anti-inflammatory
  • Hydroxypropylmethylcellulose (HPMC): Lubricant, artificial tears

• Mechanism of Action:

  • Ofloxacin: Inhibits bacterial DNA gyrase and topoisomerase IV, enzymes essential for bacterial DNA replication and repair, leading to bacterial cell death.
  • Prednisolone: Suppresses the inflammatory cascade by binding to glucocorticoid receptors, reducing redness, swelling, and pain.
  • HPMC: Increases tear film viscosity, providing lubrication and reducing eye irritation.

Alternate Names

While the generic name is Hydroxypropylmethylcellulose + Ofloxacin + Prednisolone, variations may exist internationally. This combination is not commonly found under a single international nonproprietary name (INN). Brand names vary depending on the manufacturer and region. One example is Oflotrex P

How It Works

• Pharmacodynamics: Ofloxacin exerts bactericidal effects, while prednisolone reduces inflammation and associated symptoms like pain and swelling. HPMC provides soothing lubrication.

• Pharmacokinetics:

  • Ofloxacin: After topical ocular administration, it achieves therapeutic concentrations in ocular tissues with minimal systemic absorption. It is primarily eliminated renally.
  • Prednisolone: Topical administration results in local anti-inflammatory action with limited systemic absorption. Systemic absorption is metabolized primarily in the liver and excreted in the urine.
  • HPMC: Acts locally and is not systemically absorbed.

• Mode of Action:

  • Ofloxacin: Targets bacterial DNA gyrase and topoisomerase IV, inhibiting DNA replication and transcription, leading to bacterial death.
  • Prednisolone: Binds to glucocorticoid receptors in the cytoplasm, translocates to the nucleus, and modulates gene expression of inflammatory mediators, reducing inflammation.
  • HPMC: Physically lubricates the ocular surface, providing a protective coating and reducing friction.

• Elimination Pathways:

  • Ofloxacin: Primarily renal excretion.
  • Prednisolone: Hepatic metabolism and renal excretion.

Dosage

Standard Dosage

Adults:

Instill 1-2 drops into the affected eye(s) every 2 to 4 hours, or as directed by the physician. The frequency may be increased to every hour initially for severe infections. As the infection improves, the frequency should be gradually reduced.

Children:

Dosage should be determined by the physician based on the child’s age, weight, and the severity of the infection.

Special Cases:

• Elderly Patients: No specific dosage adjustment is generally required, but close monitoring for adverse effects is recommended.

• Patients with Renal Impairment: Dosage adjustment may be necessary in severe renal impairment due to the renal excretion of ofloxacin.

• Patients with Hepatic Dysfunction: While prednisolone is primarily metabolized in the liver, topical ocular administration results in minimal systemic absorption, reducing the need for dosage adjustments.

• Patients with Comorbid Conditions: Patients with glaucoma or a history of herpes simplex keratitis require close monitoring.

Clinical Use Cases

The primary clinical use cases are bacterial conjunctivitis and corneal ulcers. This combination is not indicated for use in other clinical settings such as intubation, surgical procedures, mechanical ventilation, or ICU use. Emergency situations such as status epilepticus or cardiac arrest are outside the scope of this medication’s usage.

Dosage Adjustments

Dosage adjustments should be individualized based on the patient’s response to treatment and the severity of the infection. Renal impairment may necessitate dose reduction.

Side Effects

Common Side Effects:

• Transient ocular burning or stinging
• Blurred vision
• Eye discomfort or irritation
• Redness
• Watering of the eyes

Rare but Serious Side Effects:

• Allergic reactions (e.g., rash, itching, swelling, difficulty breathing)
• Severe skin reactions (e.g., Stevens-Johnson syndrome, toxic epidermal necrolysis)
• Tendinitis or tendon rupture, particularly Achilles tendon (with systemic fluoroquinolones)
• Peripheral neuropathy
• Seizures (especially in patients with CNS disorders)
• Increased intraocular pressure, glaucoma, cataract formation (with prolonged corticosteroid use)

Long-Term Effects:

• Prolonged corticosteroid use can lead to glaucoma, cataracts, and delayed wound healing.

Adverse Drug Reactions (ADR):

• Hypersensitivity reactions (e.g., anaphylaxis) requiring immediate medical attention

Contraindications

• Hypersensitivity to ofloxacin, other quinolones, prednisolone, or any component of the formulation.
• Viral or fungal infections of the eye, particularly herpes simplex keratitis.
• Mycobacterial eye infections.

Drug Interactions

• Systemic quinolones can interact with certain medications, such as warfarin, theophylline, and some antidiabetic agents. However, the interaction potential with topical ocular ofloxacin is minimal due to low systemic absorption.
• Concomitant use of other topical ophthalmic medications should be spaced out to avoid dilution and reduced efficacy.

Pregnancy and Breastfeeding

• Pregnancy: Safety Category C. Use only if potential benefit outweighs the risk to the fetus.

• Breastfeeding: Limited information available. Exercise caution. Consider the benefit of breastfeeding alongside the potential risk to the infant.

Drug Profile Summary

• Mechanism of Action: Ofloxacin inhibits bacterial DNA synthesis; prednisolone reduces inflammation; HPMC lubricates.

• Side Effects: Burning/stinging, blurred vision, discomfort, redness, tearing. Rarely: allergic reactions, skin reactions, tendon issues, neuropathy, seizures.

• Contraindications: Hypersensitivity, viral/fungal eye infections.

• Drug Interactions: Minimal with topical administration. Monitor for tendon rupture with concomitant systemic corticosteroids or quinolones.

• Pregnancy & Breastfeeding: Caution advised.

• Dosage: 1-2 drops every 2-4 hours, or as directed.

• Monitoring Parameters: Monitor for allergic reactions, increased intraocular pressure, signs of infection, or worsening symptoms.

Popular Combinations

This particular triple combination is itself a common combination. There are no established further combinations with it.

Precautions

• Ensure proper hygiene during administration to avoid contamination.
• Monitor for adverse reactions, including allergic reactions.
• Avoid prolonged or excessive use of topical corticosteroids.

FAQs (Frequently Asked Questions)

Q1: What is the recommended dosage for Hydroxypropylmethylcellulose + Ofloxacin + Prednisolone?

A: The usual dose is 1-2 drops in the affected eye(s) every 2-4 hours. Initial frequency can be higher for severe infections.

Q2: Can this combination be used for ear infections?

A: No, this formulation is specifically designed for ophthalmic use.

Q3: How long can this medication be used?

A: The duration of treatment should be determined by the physician and is typically limited to the duration of the infection and resolution of inflammation. Prolonged use of topical corticosteroids should be avoided.

Q4: What are the common side effects?

A: Common side effects include transient burning/stinging, blurred vision, eye discomfort, redness, and tearing.

Q5: Can contact lenses be worn while using this medication?

A: Contact lens wear should generally be avoided during treatment of eye infections. Consult the prescribing physician for guidance.

Q6: What should be done if symptoms worsen or do not improve?

A: Patients should contact their doctor immediately if symptoms worsen or do not improve after a few days of treatment.

Q7: Are there any serious side effects I should be aware of?

A: Although rare, serious side effects include allergic reactions, severe skin reactions, and increased intraocular pressure with prolonged corticosteroid use.

Q8: Can pregnant or breastfeeding women use this medication?

A: Pregnant or breastfeeding women should consult their physician before using this medication. Use only if potential benefit outweighs the risk.

Q9: Can this combination be used in children?

A: Yes, but the dosage should be determined by a physician.

Q10: What are the contraindications to using this combination?

A: Contraindications include hypersensitivity to any of the components and viral/fungal infections of the eye, particularly herpes simplex keratitis.