Ofloxacin Ophthalmic Solution - Indications, Contraindications, Dosage, Side Effects, and Precautions

Overview

Ofloxacin ophthalmic solution drug, is prescribed for the treatment of eye infections. Ofloxacin belongs to the class of antibiotics known as Quinolones. It acts by inhibiting bacterial growth. This drug is exclusively effective against bacterial eye infections. It is ineffective against other types of eye infections. The ineffectiveness of any antibiotic can be diminished by its misuse or overuse.

Drug Development and Approval

Ofloxacin was first licensed for medical use in 1985 after being patented in 1980. It is on the World Health Organization's Essential Medicines List. A generic version of ofloxacin is available. With over 1 million prescriptions in 2020, it was the 242nd most widely prescribed drug in the United States.

Composition:

• The active ingredient is 0.3 % Ofloxacin (3 mg/mL).

• Benzalkonium chloride (0.005%) as a preservative.

• Sodium chloride and purified water are inactive ingredients.

• It may also contain hydrochloric acid and sodium hydroxide to modify the pH (potential of hydrogen).

Dosage Form:

Ophthalmic solution (0.3 %).

Drug Class:

Ophthalmic anti-infectives.

What Are the Indications of the Drug?

This drug indicated in the conditions specified below, the ophthalmic solution is recommended for the treatment of infections caused by the strains of the following bacteria:

Gram-positive Bacteria:

Staphylococcus aureus.

Staphylococcus epidermidis.

Streptococcus pneumoniae.

Gram-negative Bacteria:

Enterobacter cloacae.

Haemophilus influenzae.

Pseudomonas aeruginosa.

Proteus mirabilis.

What Are the Contraindications of the Drug?

Hypersensitivity to Ofloxacin or other quinolone antibacterials. History of tendon disorders associated with Quinolone use, epilepsy, or lowered seizure threshold.

Dosage:

The following dosing schedule is indicated for the treatment of

Bacterial Conjunctivitis:

• Day one and day two, every two to four hours, administer one to two drops to the affected eyes.

• From day three to seven, one to two drops should be instilled four times daily.

Bacterial Corneal Ulcer:

• Day one and day two, while awake, administer one to two drops to the affected eye every 30 minutes.

• Approximately four to six hours after bedtime, administer one to two drops of the medication.

• Three through seven to nine days, instill one to two drops per hour while awake.

• Days seven through nine and during the duration of treatment, instill one to two drops four times daily.

Storage:

Store between 15 to 25°C. Protect from light and heat.

For Patients:

What Is This Ofloxacin Ophthalmic Solution?

Ofloxacin is used to treat eye infections that are caused by bacteria. It is an antibiotic in the Quinolone class of drugs, a group of antibiotics. Infections brought on by viruses will not be cured with this medication.

How to Use This Medicine?

• Always make sure to follow all of the instructions on the label of the medication. This medicine should not be taken in more or prominent or lesser dosages, nor should it be taken longer than indicated.
• Do not use this medication if one is using a pair of contact lenses. The preservative in Ofloxacin solution may cause soft contact lenses to turn yellow. After administering this medication, one should refrain from putting the contact lenses in for at least fifteen minutes.
• Always administer the eye drops with clean hands, and remember to wash hands before instilling the eye drops.

The Eye Drops Should Be Administered in the Following Manner:

• Create a little pocket under the lower eyelid by tilting the head back slightly and pulling down on the lower eyelid. Keep the tip of the dropper pointed away from the eye as one holds it. Turn the head away from the bottle as one squeezes a drop while looking upward.

• Keep the head down and close the eyes for two or three minutes without blinking or squinting. Keep the eyes closed. To prevent the liquid from flowing into the tear duct, place the tip of the finger on the inside corner of the eye and gently push it there for approximately one minute.

• Take only the amount of drops recommended by your healthcare provider. Wait approximately five minutes between each drop if using more than one drop.

• Before applying any additional eye drops recommended by the doctor, wait at least ten minutes.

What Dietary Instructions Should Be Followed?

Consult the doctor before consuming coffee or other caffeinated beverages while taking this medication.

What Is the Dosing and Usage of This Medication?

Adult Dosage for Bacterial Conjunctivitis and Corneal Ulcers:

Typical Dosage for Children with Bacterial Conjunctivitis and Corneal Ulcers:

Use:

To treat bacterial corneal ulcers caused by strains of S. aureus, S. epidermidis, S. pneumoniae, P. aeruginosa, S. marcescens, and P. acnes that are susceptible to the drug.

Storage and Disposal Instructions:

• Keep this medication in its original container, properly closed, and out of the reach of children.

• Keep it at ambient temperature and away from sources of extreme heat and moisture (not in the bathroom).

• Unwanted medications should be disposed of in a certain manner so that pets, children, and other people cannot swallow them.

• Do not dump this drug down the toilet. Instead, a medicine take-back program is an ideal approach to dispose of your medicines. Learn about take-back initiatives in your neighborhood by speaking with the pharmacist or contacting the local garbage/recycling department.

Keeping all medication out of children's sight and access is critical because many containers, such as weekly pill minders and those for creams, eye drops, and inhalers, are not child-resistant and are readily opened by young children. To keep small children safe from poisoning, always lock the safety caps and immediately place the medication in a secure location out of their sight and reach.

Other Information:

• Attend all of the doctor's appointments.

• Do not share this medication with anyone else.

• You must keep a written record of all prescription and nonprescription (over-the-counter) medications and any vitamins, minerals, or other dietary supplements.

• One should bring this list along when they go to the doctor or are admitted to the hospital. It is also crucial to have this information on hand in an emergency.

For Doctors:

Drug Description:

Ofloxacin 0.3 % ophthalmic solution is a sterile solution. It is an anti-infective fluorinated carboxyquinolone for topical ophthalmic application. Chemical name is ()-9-Fluoro-2,3-dihydro ()-9-Fluoro-2,3-dihydro ()-9-Flu-3-methyl

-10-(4-methyl-1-piperazinyl)[1,2,3-de]-7-oxo-7H pyrido-1,4-benzoxazine-6-carboxylic acid.

Contains: Ofloxacin 0.3 % (3 mg/mL) is the active ingredient. Benzalkonium chloride (0.005%) as a preservative.

Inactive Ingredients: Sodium chloride in suspension. It may also contain hydrochloric acid and sodium hydroxide to modify the pH.

The pH of the ofloxacin ophthalmic solution is 6.4 and is unbuffered (range 6.0 to 6.8). Its osmolality is 300 mOsm/kg. Ofloxacin is a fluorinated 4-Quinolone that varies from others in that it has a six-member (pyrido benzoxazine) ring from positions of the fundamental ring structure.

Composition:

One ml of solution contains 3.0 mg of ofloxacin (0.3 % w/v).

Excipients:

Benzalkonium chloride weighs 0.05 mg per milliliter of solution (0.005 % w/v).

Pharmaceutical Form:

The solution is clear and pale to a light yellow-green solution that is almost completely free of particles that can be seen.

Pharmacokinetics:

Ofloxacin concentrations in serum, urine, and tears were tested in 30 healthy women at various points over a ten-day course of therapy with Ofloxacin ophthalmic solution. The mean serum of Ofloxacin levels ranged between 0.4 and 1.9 ng/mL. After 10 1/2 days of QID (four times a day), the maximum concentration of Ofloxacin is increased from 1.1 ng/mL on the first day to 1.9 ng/mL on day eleven. After ten days of topical ophthalmic treatment, maximum blood Ofloxacin concentrations were more than 1000 times lower than those reported after typical oral dosages of Ofloxacin.

During the 40 minutes following the last treatment on day 11, tear Ofloxacin concentrations ranged from 5.7 to 31 mcg/g. The mean tear content was 9.2 mcg/g four hours after topical ophthalmic treatment.

Four hours after starting topical ocular treatment of two drops of Ofloxacin ophthalmic solution instilled every 30 minutes, corneal tissue concentrations of 4.4 mcg/mL were found. Ofloxacin was mostly excreted in the urine unaltered.

Dosage and Use:

The Typical Adult Dosage for Bacterial Conjunctivitis:

First and Second Day: One to two drops every 2 to 4 hours to the afflicted eye(s).

Days Three Through Seven: Apply 1 to 2 drops four times per day to the afflicted eye(s).

Use:

To treat bacterial conjunctivitis by strains of Staphylococcus aureus, S. epidermidis, Streptococcus pneumoniae, Enterobacter cloacae, Haemophilus influenzae, Proteus mirabilis, and Pseudomonas aeruginosa.

Corneal Ulcers Common Adult Dosage:

Days 1 and 2: Every 30 minutes while awake and between 4 and 6 hours after retiring, apply 1 to 2 drops to the afflicted eye(s).

Days 3 to 7 to 9: Apply 1 to 2 drops, when awake, to the afflicted eye(s).

Instill one to two drops into the afflicted eye(s) four times per day from days seven to nine until the end of the treatment.

Use:

To treat bacterial corneal ulcers by Serratia marcescens, Propionibacterium acnes, S. aureus, S. epidermidis, S. pneumoniae, P. aeruginosa, and other sensitive strains.

Common dosage for children with bacterial conjunctivitis:

Age One Year or Older:

Days One and Two: Every two to four hours, put one to two drops in the afflicted eye(s).

Days Three Through Seven: Apply one to two drops four times per day to the afflicted eye(s).

Use:

To treat bacterial conjunctivitis brought on by strains of S. aureus, S epidermidis, S pneumoniae, E. cloacae, H. influenzae, P. mirabilis, and P. aeruginosa that are susceptible to the drug.

Common Dosage for Children with Corneal Ulcers:

Age One Year or Older:

Days One and Two: Every 30 minutes while awake and between four and six hours after bed, apply one to two drops to the afflicted eye(s).

Days Three Through Seven to Nine: While awake, place one to two drops in the afflicted eye(s).

Days seven to nine and up until the end of treatment: Apply one to two drops four times per day to the afflicted eye(s).

Use:

To treat bacterial corneal ulcers caused by strains of S. aureus, S. epidermidis, S. pneumoniae, P. aeruginosa, S. marcescens, and P. acnes that are susceptible to the drug.

Warning:

Do Not Use for Injection. Ofloxacin ophthalmic solution should never be injected subconjunctivally or directly into the eye's anterior chamber.

There have been a few instances of anaphylactic reactions, shock, and fatal hypersensitivity reactions in individuals receiving systemic quinolones, including Ofloxacin, with some occurring after the first dose. Cardiovascular collapse, dyspnea, loss of consciousness, angioedema (including laryngeal, pharyngeal, or facial edema), airway obstruction, angioedema, and itching were all reported in some instances. A patient receiving topical ophthalmic ofloxacin experienced a rare case of Stevens-Johnson syndrome that proceeded to severe epidermal necrolysis. If you have an allergic reaction to ofloxacin, stop taking it. Severe acute hypersensitivity reactions may necessitate immediate emergency care. As clinically indicated, oxygen and airway care, including intubation, should be delivered.

Precautions:

On taking with other anti-infectives, prolonged use may result in the overgrowth of non-susceptible organisms, particularly fungi. If superinfection occurs, discontinue use and seek further treatment. Whenever clinical judgment demands, the patient should be examined under magnification using techniques such as slit lamp biomicroscopy and, when applicable, fluorescein staining. Ofloxacin should be stopped as soon as a skin rash or other evidence of a hypersensitive reaction appears.

Systemic administration of Quinolones, including Ofloxacin, has resulted in cartilage lesions or erosions in weight-bearing joints, as well as other indicators of arthropathy in juvenile animals of diverse species. Ofloxacin has been linked to these side effects in young dogs when treated systemically at 10 mg/kg/day (equal to 110 times the maximum permitted daily adult ophthalmic dose).

Supply:

Ofloxacin ophthalmic solution 0.3 % is supplied as a sterile solution in opaque white low-density polyethylene plastic containers and white dropper tips with beige high-impact polystyrene (HIPS) caps.

Contains 5 ml in a 10 ml bottle. Store at a temperature of 15° to 25 °C (59° to 77°F).

Drug Interactions:

There have been no specific medication interaction investigations with Ofloxacin ophthalmic solution. However, systemic administration of some Quinolones has been shown to increase plasma theophylline concentrations, interfere with caffeine metabolism, and enhance the effects of the oral anticoagulant warfarin and its derivatives, as well as be associated with transient increases in serum creatinine in patients receiving cyclosporine concurrently.

Pregnancy:

In pregnant women, no sufficient and well-controlled trials have been conducted. Ofloxacin should not be used in pregnant women since systemic Quinolones have been reported to cause arthropathy in immature animals.

Teratogenic Potential:

When given at levels of 810 mg/kg/day (equal to 9000 times the maximum permitted daily ocular dose) and 160 mg/kg/day, Ofloxacin has been proven to have an embryocidal impact in rats and rabbits (equivalent to 1800 times the maximum recommended daily ophthalmic dose). In rats and rabbits, these doses resulted in lower fetal body weight and higher fetal death. Minor fetal skeletal changes were observed in rats given 810 mg/kg/day. When given to pregnant rats and rabbits at a dosage as high as 810 mg/kg/day and 160 mg/kg/day, respectively, Ofloxacin is not teratogenic.

Nursing Moms:

A single 200 mg oral dose was found in breast milk giving mothers comparable to those seen in plasma in nursing mothers. Ofloxacin is not known to be excreted in human milk after topical ophthalmic treatment. Because Ofloxacin can produce significant adverse reactions in nursing infants, a choice should be made whether to quit breastfeeding or discontinue the medicine, taking into account the drug's importance to the mother.

Pediatric Use:

It has not been shown to be safe or beneficial in infants under one year. Quinolones, including Ofloxacin, have been reported in immature animals to cause arthropathy following oral treatment. However, topical administration of Ofloxacin to juvenile animals has not exhibited any arthropathy. There is no indication that the Ofloxacin ophthalmic dose affects weight-bearing joints.

Use in Elderly:

No overall variations in safety or efficacy between older persons have been reported.

What Are the Adverse Reactions Caused by the Drug?

Temporary eye burning or discomfort was the most often reported drug-related side event. Stinging, redness, itching, chemical conjunctivitis or keratitis, ocular/periocular/facial edema, foreign body sensation, photophobia, impaired vision, tears, dryness, and eye pain have all been recorded. There have been a few reports of dizziness and nausea.

Carcinogenesis, Mutagenesis, Impairment of Fertility:

Long-term investigations to assess Ofloxacin's carcinogenic potential have yet to be done. The Ames test showed that in vitro and in vivo cytogenetic assay, sister chromatid exchange assay unscheduled DNA synthesis (UDS) assay utilizing human fibroblasts, the dominant lethal assay, and the mouse micronucleus assay all revealed that ofloxacin was not mutagenic. Ofloxacin was active in the UDS test using rat hepatocytes and the mouse lymphoma assay.

Ofloxacin did not have any effect on male or female fertility, morphological or reproductive performance in rats given Ofloxacin doses up to 360 mg/kg/day, which is equivalent to 4000 times the maximum recommended daily dose.

Nonteratogenic Effects :

Additional research in rats with dosages up to 360 mg/kg/day during late gestation revealed no harmful effects on late fetal development, labor, delivery, breastfeeding, neonatal viability, or infant growth. However, no sound and well-controlled studies on pregnant women exist. Only if the possible benefit outweighs the potential risk to the fetus should Ofloxacin ophthalmic solution be used during pregnancy.

Patient Education Instructions:

• Avoid getting material on the applicator tip from the eye, fingers, or other sources.

• Systemic quinolones, such as Ofloxacin, have been linked to hypersensitivity reactions, even after a single dose. If a rash or an adverse reaction is seen, stop using it immediately and consult the doctor.

• Use Ofloxacin ophthalmic solution precisely as directed by your doctor.

• If using other topically applied ophthalmic drugs, give them at least ten minutes before or after using Ofloxacin ophthalmic solution.

• Wash hands before each use.

• Check that the dust cover seal is intact before using the medication for the first time.