Ophthalmic Therapeutics M. Gohari MD. Topical Anesthetics. useful for diagnostic and therapeutic procedures, including tonometry, removal of foreign bodies or sutures, gonioscopy, conjunctival scraping, and minor surgical operations on the cornea and conjunctiva.
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Topical anesthetics should never be prescribed for home use, since prolonged application may cause corneal complications
Preparation: Solution, 0.5%.
Dosage: 1 drop and repeat as necessary. Onset and duration of action: Anesthesia begins within 20 seconds and lasts 10–15 minutes.
Comment:Least irritating of the topical anesthetics.
Preparations: Solution, 0.5%, and ointment, 0.5%.
Onset and duration of action: Anesthesia occurs within 1 minute and lasts for 15–20 minutes.
Comment: Stings considerably on instillation
Preparation (as Fluress): Solution, 0.4%.
Onset and duration of action: Anesthesia begins within 1 or 2 minutes and lasts for 10–15 minutes.
Local Anesthetics for Injection
Duration of action: 45–60 minutes.
Duration of action: Approximately 2 hours. Comment: Carbocaine is similar to lidocaine in potency.
It is usually used in patients who are allergic to lidocaine.
Atropine drops must be used with caution to avoid toxic reactions resulting from systemic absorption. Restlessness and excited behavior with dryness and flushing of the skin of the face, dry mouth, fever, inhibition of sweating, and tachycardia are prominent toxic symptoms, particularly in young children.
Comment:Pilocarpine was introduced in 1876 and is still a commonly used antiglaucoma drug.
Comment:Carbachol is poorly absorbed through the cornea and usually is used if pilocarpine is ineffective.
Comment: A high incidence of allergic reactions has limited the use of this old and seldom-used antiglaucoma drug. The miosis produced is extreme; ciliary spasm and myopia are common. Local irritation is common, and phospholine iodide is believed to be cataractogenic in some patients. Pupillary block may occur.
Echothiophate Iodide (Phospholine Iodide)
Systemic toxicity may occur in the form of cholinergic stimulation, including salivation, nausea, vomiting, and diarrhea. Ocular side effects include cataract formation, spasm of accommodation, and iris cyst formation.
Preparation: Solution, 0.5% and 1%. Dosage: 1 drop of 1% solution before anterior segment laser treatment and a second drop upon completion of the procedure. One drop of 0.5% solution two or three times a day as short-term adjunctive treatment in glaucoma patients receiving other medications.
Comment: applied topically for prevention and management of intraocular pressure elevations after anterior segment laser procedures. It is also used as adjunctive therapy in patients on maximally tolerated medical therapy who need further reduction of intraocular pressure.
Apraclonidine lowers intraocular pressure by decreasing aqueous humor formation. It may also improve aqueous outflow. Unlike clonidine, apraclonidine does not appear to penetrate blood-tissue barriers easily and produces few side effects. The reported systemic side effects include occasional decreases in diastolic blood pressure, bradycardia, and central nervous system symptoms of insomnia, irritability, and decreased libido.
Ocular side effects include conjunctival blanching, upper lid elevation, mydriasis, and burning.
relatively specific alpha 2 adrenergic agonist that lowers intraocular pressure by decreasing aqueous production and perhaps also by increasing outflow through the uveoscleral pathway. It has only minimal effect on heart rate and blood pressure.
Preparation: Solution, 0.15%. Dosage: 1 drop two or three times daily. Frequently used as a replacement drug in patients unable to tolerate beta-blockers.
Toxicity: Dry mouth, stinging, and redness are the most common side reactions.
Systemic Side Effects of Timolol
Comment: Its relative 1 receptor selectivity reduces the risk of pulmonary side effects, particularly in patients with reactive airway disease.
Comment:Levobunolol is a nonselective 1 and 2 blocker.
Comment:Metipranolol is a nonselective 1 and 2 blocker .
Preparations and dosages:Oral: Tablets, 125 mg and 250 mg; give 125–250 mg two to four times a day (dosage not to exceed 1 g in 24 hours). Sustained-release capsules, 500 mg; give 1 capsule once or twice a day. Parenteral: May give 500-mg ampules intramuscularly or intravenously for short periods in patients who cannot tolerate the drug orally.
Preparation: Solution, 2%. Dosage: 1 drop two to four times daily.
Toxicity: Local reactions include burning and stinging, superficial punctatekeratopathy, and allergic reactions of the conjunctiva. Bitter after-taste is common. Systemic side reactions associated with oral carbonic anhydrase agents are rare.
Preparation: Suspension, 1%.
Preparations and dosage: Glycerin is usually given orally as 50% solution with water, orange juice, or flavored normal saline solution over ice .
Onset and duration of action: Maximum hypotensive effect occurs in 1 hour and lasts 4–5 hours. Toxicity: Nausea, vomiting, and headache occasionally occur.
Comment: Oral administration and the absence of diuretic effect are significant advantages of glycerin over the other hyperosmotic agents.
Comment: Unlike glycerin, isosorbide does not produce calories or elevated blood sugar.
Preparation: 5–25% solution for injection. Dosage: 1.5–2 g/kg intravenously, usually in 20% concentration.
Onset and duration of action:Maximum hypotensive effect occurs in about 1 hour and lasts 5–6 hours.
Comment:Problems with cardiovascular overload and pulmonary edema are more common with this agent because of the large fluid volumes required.
Nonsteroidal Anti-Inflammatory Agents
Other Drugs Used
in the Treatment of
Preparation: Solution, 4%. Dosage: 1 drop four to six times a day.
Comment:Cromolyn is useful in the treatment of many types of allergic conjunctivitis. Response to therapy usually occurs within a few days but sometimes not until treatment is continued for several weeks.
Cromolyn acts by inhibiting the release of histamine and slow-reacting substance of anaphylaxis (SRS-A) from mast cells. It is not useful in the treatment of acute symptoms.
Dosage: Twice daily.
Comment:Ketotifen has antihistamine and mast cell–stabilizing activity.
Dosage: 1 drop four times a day.
Comment:Lodoxamide is a mast cell stabilizer . It is indicated in the treatment of allergic reactions of the external ocular tissues, including vernal conjunctivitis and vernal keratitis. As with cromolyn, a therapeutic response does not usually occur until after a few days of treatment.
Comment: rapid onset of an antihistamine and true mast cell–stabilizing activity.
Olapadine Hydrochloride (Patanol)
Comment:Olapatadine has both antihistamine and mast cell–stabilizing actions.
Levocabastine Hydrochloride (Livostin)
Comment:selective, potent histamine H1-receptor antagonist. It is useful in reducing acute symptoms of allergic conjunctivitis. Relief of symptoms occurs within minutes after application and lasts up to 2 hours.
only cyclooxygenase inhibitor approved for allergy by the FDA.
Vasoconstrictors & Decongestants
Topical Antibiotic Solutions & Ointments
Most gram-positive organisms are sensitive to bacitracin.
It is not used systemically because of its nephrotoxicity.
particularly in staphylococcal conjunctivitis.
It may be used instead of silver nitrate in prophylaxis of
It is best known in ophthalmologic practice as Neosporin, in which it is combined with polymyxin and bacitracin.
Contact skin sensitivity develops in 5% of patients if the drug is continued for longer than a week.
Effective against many gram-negative organisms.
Topical Preparationsof Systemic Antibiotics
limited uses in ophthalmology because their effectiveness is so often impaired by the development of resistant strains. Ointment may be used for prophylaxis of ophthalmianeonatorum.
Gentamicin (Garamycin, Genoptic, Gentacidin, Gentak)
corneal ulcers caused by gram-negative organisms. It is also effective against many gram-positive staphylococci but is not effective against streptococci.
Tobramycin (Tobrex, Aktop)
Similar antimicrobial activity to gentamicin but more effective against streptococci. Best reserved for treatment of pseudomonas keratitis, for which it is more effective.
Chloramphenicol (Chloromycetin, Chloroptic)
effective against a wide variety of gram-positive and gram-negative organisms.
aplastic anemia have been associated with long-term therapy.
For treatment of conjunctivitis, 1 drop every 2–4 hours. For treatment of corneal ulcers, 1 drop every 15–30 minutes for the first day, 1 drop every hour the second day, and 1 drop every 4 hours thereafter.
This fourth-generation fluoroquinolone is more effective against a broader spectrum of gram-positive bacteria and atypical mycobacteria than earlier fluoroquinolones.
most commonly used drugs in the treatment of bacterial conjunctivitis. Their advantages include (1) activity against both gram-positive and gram-negative organisms, (2) relatively low cost, (3) low allergenicity, and (4) the fact that their use is not complicated by secondary fungal infections
Initial drug of choice for most mycotic corneal ulcers.
more effective than nystatin but not available in ophthalmic ointment form. Many patients have extreme ocular discomfort following application of this drug.
in the form of an intravenous preparation that may be instilled directly into the eye.
Used in the treatment of herpes simplex keratitis.
In herpetic epithelial keratitis, apply four times daily for 7–10 days. It is effective in some patients unresponsive to idoxuridine. interferes with viral DNA synthesis. The drug is effective against herpetic corneal epithelial disease and has limited efficacy in stromalkeratitis or uveitis. It may cause cellular toxicity and delay corneal regeneration. The cellular toxicity is less than that of idoxuridine.
Acts by interfering with viral DNA synthesis. More soluble than either idoxuridine or vidarabine and probably more effective in stromal disease.
Preparations: 200, 400, and 800 mg. Comment: Acyclovir is an antiviral agent with inhibitory activity against herpes simplex types 1 and 2, varicella-zoster virus, Epstein-Barr virus, and cytomegalovirus. which inhibits viral DNA polymerase.
Acyclovir has low toxicity.
Preparation: Intravitreal implant, 4.5 mg. Comment: treatment of cytomegalovirus retinitis without the adverse effects of systemic therapy.
for detection of corneal epithelial defects, in applanation tonometry, and in fitting contact lenses.
Used in diagnosis of keratoconjunctivitis sicca; the mucous shreds and devitalized corneal epithelium stain with rose bengal.
Ocular & Systemic
Side Effects of