Each mL contains Ofloxacin 3 mg.
Pharmacology: Ofloxacin is considered to inhibit DNA synthesis of bacteria specifically. Its effect is bactericidal, and bacteriolysis is observed at the MICs.
Ofloxacin exerts a broad-spectrum potent antibacterial activity against organisms causing ophthamological infections, including gram-positive bacteria [Staphylococcus sp., Streptococcus sp., (including S. pneumoniae), etc.], gram-negative bacteria (Pseudomonas sp., [including P. aeruginosa], Haemophilus sp., Serratia sp., Proteus sp. etc.), and Anaerobic bacteria (Propionibacterium acnes, etc).
Pharmacokinetics: Blood concentrations: In healthy adult volunteers, the blood concentration of ofloxacin was measured following topical instillation of one drop of Tarivid ophthalmic solution to the eye 16 times every 30 minutes or 32 times every 15 minutes. Concentrations of ofloxacin at 30 minutes after the instillation were 0.019 μg/mL and 0.034 μg/mL, respectively, which gradually decreased thereafter.
Ocular distribution: Tarivid ophthalmic solution was given topically to the eyes of patients with cataract 5 times every 5 minutes before surgery, and concentration of ofloxacin in the aqueous humor was measured. The concentration reached the maximum (1.20 μg/mL) one hour after the last instillation.
Ocular penetration in animals (albino rabbits, dogs): After single instillation of Tarivid ophthalmic solution to the eye of normal albino rabbits, ofloxacin penetrated well into the cornea, bulbar conjunctiva, ocular muscle, sclera, iris/ciliary body and aqueous humor.
At 1 hour after instillation, the drug level in the cornea, sclera, ocular muscle, and iris/ciliary body reached their peaks of 3.32 μg/g, 1.62 μg/g, 2.62 μg/g and 0.95 μg/g, respectively. Peaks in the bulbar conjunctiva and the aqueous humor in the anterior chamber were 2.95 μg/g at 15 minutes and 0.71 μg/mL at 30 minutes, respectively.
Multiple instillation, 5 times at 5-min intervals, of Tarivid ophthalmic solution to the eye of normal albino rabbits allowed ofloxacin to penetrate into similar ocular tissues in which the drug penetration was evident with single instillation. At 5 minutes after the last instillation, the ofloxacin concentrations in the cornea, sclera, bulbar conjunctiva and vitreous body reached the highest levels of 7.78 μg/g, 7.66 μg/g, 34.98 μg/g, 0.95 μg/mL, respectively. In other ocular tissues, the peak concentration was 18.54 μg/g in the ocular muscle at 15 minutes, 3.12 μg/g in the iris/ciliary body at 30 minutes, and 3.56 μg/mL in the aqueous humor in the anterior chamber at 1 hour.
When one drop of 0.3% ophthalmic solution of levofloxacin, an optical isomer of ofloxacin (l-form), was applied to the eye of beagle dogs 4 times a day for 2 weeks, the concentration of the drug at 24 hours after the last administration were 39.4 μg/g in iris/ciliary body and 12.3 μg/g in the choroidal and retinal pigment epithelium, indicating that the concentrations were high in the melanin-containing ocular tissues. On the other hand, the transfer of this drug to the retinal tissues except the pigment epithelium was slight.
For the treatment of bacterial infections caused by susceptible strains of the designated microorganisms in corneal ulcers and conjunctivitis.
Usually, instill 1 drop a time 3 times daily. The dosage may be adjusted according to the patient's symptoms.
User instruction: Instruct the patient to be careful not to touch the tip of the bottle to the eye directly in order to avoid the contamination of the drug.
Route of administration: Ophthalmic use only.
Overdose is not known to have caused any symptoms.
Tarivid ophthalmic solution is contraindicated in patients with history of hypersensitivity to the active ingredient of this product or any quinolone antibiotics.
In order to avoid emergence of resistant bacteria, bacterial susceptibility should be confirmed and treatment with this drug should be limited to the minimum period required for the eradication of the infection.
Avoid long-term use.
This product should be used in pregnant women or women who may possibly be pregnant only if the expected therapeutic benefits are judged to outweigh the possible risks associated with treatment. [The safety of this product during pregnancy has not been established.]
Adverse reactions to this drug were reported in 44 of 13,329 patients evaluated before and after approval (0.33%). The major adverse reactions were eye irritation in 11 patients (0.08%), eyelid itching in 8 patients (0.06%), blepharitis in 6 patients (0.05%), conjunctival injection in 5 patients (0.04%), eye pain 5 patients (0.04%), swelling of eyelid in 5 patients (0.04%), etc. [At the end of the re-examination period].
Clinically significant adverse reactions ("rarely": <0.1%, occasionally: 5%> ≥0.1%, and no specific designation: ≥5% or incidence unknown): Shock, anaphylactoid reaction:
Since shock and anaphylactoid reaction may occur, patients should be carefully observed. If any symptoms such as erythema, rash, dyspnoea, decreased blood pressure, and eyelid oedema, etc. are observed, administration should be discontinued and appropriate measures should be taken.
Other adverse reactions:
If the following adverse reactions are observed, appropriate measures such as discontinuing administration should be taken. (See table.)
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S01AE01 - ofloxacin ; Belongs to the class of quinolone antiinfectives. Used in the treatment of eye infections.
Ophth soln 0.3% (clear, pale to light yellow, sterile aqueous) x 5 mL.