topical anesthetics useful for diagnostic and therapeutic procedures, including tonometry, removal...

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Page 1: Topical Anesthetics  useful for diagnostic and therapeutic procedures, including tonometry, removal of foreign bodies or sutures, gonioscopy, conjunctival
Page 2: Topical Anesthetics  useful for diagnostic and therapeutic procedures, including tonometry, removal of foreign bodies or sutures, gonioscopy, conjunctival
Page 3: Topical Anesthetics  useful for diagnostic and therapeutic procedures, including tonometry, removal of foreign bodies or sutures, gonioscopy, conjunctival

Topical Anesthetics

Page 4: Topical Anesthetics  useful for diagnostic and therapeutic procedures, including tonometry, removal of foreign bodies or sutures, gonioscopy, conjunctival

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

Page 5: Topical Anesthetics  useful for diagnostic and therapeutic procedures, including tonometry, removal of foreign bodies or sutures, gonioscopy, conjunctival

Proparacaine, tetracaine, and benoxinate are the most commonly used topical anesthetics.

equivalent anesthetic potency

Page 6: Topical Anesthetics  useful for diagnostic and therapeutic procedures, including tonometry, removal of foreign bodies or sutures, gonioscopy, conjunctival

Note: Topical anesthetics should never be

prescribed for home use, since prolonged application may cause corneal complications

Page 7: Topical Anesthetics  useful for diagnostic and therapeutic procedures, including tonometry, removal of foreign bodies or sutures, gonioscopy, conjunctival

Proparacaine Hydrochloride (Ophthaine) 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.

Page 8: Topical Anesthetics  useful for diagnostic and therapeutic procedures, including tonometry, removal of foreign bodies or sutures, gonioscopy, conjunctival

Tetracaine Hydrochloride (Pontocaine) 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

Page 9: Topical Anesthetics  useful for diagnostic and therapeutic procedures, including tonometry, removal of foreign bodies or sutures, gonioscopy, conjunctival

Benoxinate Hydrochloride Preparation (as Fluress): Solution, 0.4%. Onset and duration of action: Anesthesia

begins within 1 or 2 minutes and lasts for 10–15 minutes.

Page 10: Topical Anesthetics  useful for diagnostic and therapeutic procedures, including tonometry, removal of foreign bodies or sutures, gonioscopy, conjunctival

Local Anesthetics for Injection

Page 11: Topical Anesthetics  useful for diagnostic and therapeutic procedures, including tonometry, removal of foreign bodies or sutures, gonioscopy, conjunctival

Lidocaine, procaine, and mepivacaine are commonly used local anesthetics for eye surgery.

Longer-acting agents such as bupivacaine and etidocaine are often mixed with other local anesthetics to prolong the duration of effect.

the physician must be aware of the potential systemic toxic action when rapid absorption occurs from the site of the injection, with excessive dosage, or following inadvertent intravascular injection

Page 12: Topical Anesthetics  useful for diagnostic and therapeutic procedures, including tonometry, removal of foreign bodies or sutures, gonioscopy, conjunctival

The addition of hyaluronidase encourages spreading of the anesthetic and shortens the onset to as little as 1 minute. For these reasons, hyaluronidase is commonly used in retrobulbar and peribulbar injections prior to cataract extraction.

Injectable anesthetics are used by ophthalmologists most commonly in older patients, who may be susceptible to cardiac arrhythmias; therefore, l-epinephrine should not be used in concentrations greater than 1:200,000

Page 13: Topical Anesthetics  useful for diagnostic and therapeutic procedures, including tonometry, removal of foreign bodies or sutures, gonioscopy, conjunctival

Lidocaine Hydrochloride (Xylocaine)

Owing to its rapid onset and longer action (1–2 hours), lidocaine has become the most commonly used local anesthetic. It is approximately twice as potent as procaine.

Up to 30 mL of 1% solution, without epinephrine, may be used safely. In cataract surgery, 15–20 mL is usually more than adequate. The maximum safe dose is 4.5 mg/kg without epinephrine and 7 mg/kg with epinephrine.

Intracameral lidocaine in a 1% solution without preservatives is employed for anesthesia in cataract surgery.

Page 14: Topical Anesthetics  useful for diagnostic and therapeutic procedures, including tonometry, removal of foreign bodies or sutures, gonioscopy, conjunctival

Procaine Hydrochloride (Novocaine)

Duration of action: 45–60 minutes.

Page 15: Topical Anesthetics  useful for diagnostic and therapeutic procedures, including tonometry, removal of foreign bodies or sutures, gonioscopy, conjunctival

Mepivacaine Hydrochloride (Carbocaine) 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.

Page 16: Topical Anesthetics  useful for diagnostic and therapeutic procedures, including tonometry, removal of foreign bodies or sutures, gonioscopy, conjunctival

Bupivacaine Hydrochloride (Marcaine, Sensorcaine)

Onset and duration of action: The onset of action is slower than that of lidocaine, but it persists much longer (up to 6–10 hours).

Page 17: Topical Anesthetics  useful for diagnostic and therapeutic procedures, including tonometry, removal of foreign bodies or sutures, gonioscopy, conjunctival

Etidocaine Hydrochloride (Duranest)

Onset and duration of action: The onset of action is slower than that of lidocaine but more rapid than that of bupivacaine. The duration of action is approximately twice as long as that of lidocaine (4–8 hours).

Page 18: Topical Anesthetics  useful for diagnostic and therapeutic procedures, including tonometry, removal of foreign bodies or sutures, gonioscopy, conjunctival
Page 19: Topical Anesthetics  useful for diagnostic and therapeutic procedures, including tonometry, removal of foreign bodies or sutures, gonioscopy, conjunctival

Mydriatics & Cycloplegics

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Mydriatics and cycloplegics both dilate the pupil. In addition, cycloplegics cause paralysis of accommodation .

Their prime uses are (1) for dilating the pupils to facilitate ophthalmoscopy; (2) for paralyzing the muscles of accommodation, particularly in young patients, as an aid in refraction; and (3) for dilating the pupil and paralyzing the muscles of accommodation in uveitis to prevent synechia formation and relieve pain and photophobia.

Page 21: Topical Anesthetics  useful for diagnostic and therapeutic procedures, including tonometry, removal of foreign bodies or sutures, gonioscopy, conjunctival

Since mydriatics and cycloplegics both dilate the pupil, they should be used with extreme caution in eyes with narrow anterior chamber angles since cause angle-closure glaucoma .

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Phenylephrine Hydrochloride (Neo-Synephrine)

Preparations: Solution, 0.12%, 2.5%, and 10%. Onset and duration of action: The effect usually occurs

within 30 minutes after instillation and lasts 2–3 hours. Comment: facilitate ophthalmoscopy, in treatment of

uveitis, and to dilate the pupil prior to cataract surgery. The 10% solution should not be used in newborn infants,

in cardiac patients, or in patients receiving reserpine, guanethidine, or tricyclic antidepressants, because of increased susceptibility to the vasopressor effects

Phenylephrine is a mydriatic with no cycloplegic effect

Page 23: Topical Anesthetics  useful for diagnostic and therapeutic procedures, including tonometry, removal of foreign bodies or sutures, gonioscopy, conjunctival

Cycloplegics (Parasympatholytics)

Page 24: Topical Anesthetics  useful for diagnostic and therapeutic procedures, including tonometry, removal of foreign bodies or sutures, gonioscopy, conjunctival

Preparations: Solution, 0.5–3%; ointment, 0.5% and 1%.

Dosage: For refraction in children, instill 1 drop of 0.25–0.5% solution in each eye twice a day for 1 or 2 days before the examination and then 1 hour before the examination;

Onset and duration of action: The onset of action is within 30–40 minutes. A maximum effect is reached in about 2 hours. The effect lasts for up to 2 weeks .

cycloplegia in children, treatment of iritis. It is also used to maintain a dilated pupil after intraocular surgical procedures.

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Toxicity: 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.

Page 26: Topical Anesthetics  useful for diagnostic and therapeutic procedures, including tonometry, removal of foreign bodies or sutures, gonioscopy, conjunctival

Preparation: Solution, 0.25%. Dosage: 1 drop two or three times daily. Onset and duration of action: Cycloplegia

occurs in about 40 minutes and lasts for 3–5 days when scopolamine is used as an aid to refraction .

Toxicity: dizziness and disorientation, mainly in older people.

Page 27: Topical Anesthetics  useful for diagnostic and therapeutic procedures, including tonometry, removal of foreign bodies or sutures, gonioscopy, conjunctival

Preparations: Solution, 2% and 5%. Dosage: For refraction, 1 drop in each eye

and repeat two or three times at intervals of 10–15 minutes.

Onset and duration of action: Maximal cycloplegic effect lasts for about 3 hours, but complete recovery time is about 36–48 hours. In certain cases, the shorter action is an advantage over scopolamine and atropine.

Toxicity: Sensitivity and side effects associated with the topical instillation of homatropine are rare.

Page 28: Topical Anesthetics  useful for diagnostic and therapeutic procedures, including tonometry, removal of foreign bodies or sutures, gonioscopy, conjunctival

Preparations: Solution, 0.5%, 1%, and 2%. Dosage: For refraction, 1 drop in each eye and

repeat after 10 minutes. Onset and duration of action: The onset of

dilatation and cycloplegia is within 30–60 minutes. The duration of action is less than 24 hours.

Comment: Cyclopentolate is more popular than homatropine and scopolamine in refraction because of its shorter duration of action

Occasionally, neurotoxicity may occur, manifested by incoherence, visual hallucinations, slurred speech, and ataxia. These reactions are more common in children.

Page 29: Topical Anesthetics  useful for diagnostic and therapeutic procedures, including tonometry, removal of foreign bodies or sutures, gonioscopy, conjunctival

Preparations: Solution, 0.5% and 1%; 0.25% with 1% hydroxamphetamine hydrobromide (Paremyd).

Dosage: 1 drop of 1% solution two or three times at 5-minute intervals.

Onset and duration of action: The time required to reach the maximum cycloplegic effect is usually 20–25 minutes, and the duration of this effect is only 15–20 minutes; therefore, the timing of the examination after instilling tropicamide is important. Complete recovery requires 5–6 hours.

Comment: Tropicamide is an effective mydriatic with weak cycloplegic action and is therefore most useful for ophthalmoscopy.

Page 30: Topical Anesthetics  useful for diagnostic and therapeutic procedures, including tonometry, removal of foreign bodies or sutures, gonioscopy, conjunctival

Preparations: Solution, 0.2% cyclopentolate hydrochloride and 1% phenylephrine hydrochloride.

Dosage: 1 drop every 5–10 minutes for two or three doses.

Onset and duration of action: Mydriasis and some cycloplegia occur within the first 3–6 minutes. The duration of action is usually less than 24 hours.

This drug combination is of particular value for pupillary dilation in examination of premature and small infants

Page 31: Topical Anesthetics  useful for diagnostic and therapeutic procedures, including tonometry, removal of foreign bodies or sutures, gonioscopy, conjunctival

Glaucoma

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Page 34: Topical Anesthetics  useful for diagnostic and therapeutic procedures, including tonometry, removal of foreign bodies or sutures, gonioscopy, conjunctival
Page 35: Topical Anesthetics  useful for diagnostic and therapeutic procedures, including tonometry, removal of foreign bodies or sutures, gonioscopy, conjunctival
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Page 37: Topical Anesthetics  useful for diagnostic and therapeutic procedures, including tonometry, removal of foreign bodies or sutures, gonioscopy, conjunctival

The concentration used and the frequency of instillation should be individualized on the basis of tonometric measurements. Use the smallest dosage that effectively controls the intraocular pressure and prevents optic nerve damage.

All parasympathomimetics decrease intraocular pressure by increasing the outflow of aqueous humor through the trabecular meshwork.

Page 38: Topical Anesthetics  useful for diagnostic and therapeutic procedures, including tonometry, removal of foreign bodies or sutures, gonioscopy, conjunctival

Pilocarpine Hydrochloride & Nitrate Comment: Pilocarpine was introduced in

1876 and is still a commonly used antiglaucoma drug.

Carbachol, Topical Comment: Carbachol is poorly absorbed

through the cornea and usually is used if pilocarpine is ineffective.

Page 39: Topical Anesthetics  useful for diagnostic and therapeutic procedures, including tonometry, removal of foreign bodies or sutures, gonioscopy, conjunctival

Physostigmine Salicylate & Sulfate (Eserine) 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.

Demecarium Bromide (Humorsol)

Page 40: Topical Anesthetics  useful for diagnostic and therapeutic procedures, including tonometry, removal of foreign bodies or sutures, gonioscopy, conjunctival

Epinephrine has the advantages of long duration of action (12–72 hours) and no miosis, which is especially important in patients with incipient cataracts (effect on vision not accentuated).

effects on both alpha and beta receptor sites.

primarily acts by increasing outflow of aqueous humor. However, it also has an ability to decrease production of aqueous humor following long-term use.

Page 41: Topical Anesthetics  useful for diagnostic and therapeutic procedures, including tonometry, removal of foreign bodies or sutures, gonioscopy, conjunctival

Apraclonidine Hydrochloride (Iopidine) 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.

Page 42: Topical Anesthetics  useful for diagnostic and therapeutic procedures, including tonometry, removal of foreign bodies or sutures, gonioscopy, conjunctival

Brimonidine Tartrate (Alphagan-P)

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.

Page 43: Topical Anesthetics  useful for diagnostic and therapeutic procedures, including tonometry, removal of foreign bodies or sutures, gonioscopy, conjunctival

Timolol Maleate (Timoptic; Timoptic XE, Betimol)

Preparations: Solution, 0.25% and 0.5%; gel, 0.25% and 0.5%.

Dosage: 1 drop of 0.25% or 0.5% in each eye once or twice daily if needed. One drop of gel once daily.

Comment: nonselective beta-adrenergic blocking agent applied topically for treatment of open-angle glaucoma, aphakic glaucoma, and some types of secondary glaucoma. A single application can lower the intraocular pressure for 12–24 hours. Timolol has been found to be effective in some patients with severe glaucoma inadequately controlled by maximum tolerated antiglaucoma therapy with other drugs. The drug does not affect pupillary size or visual acuity.

Although timolol is usually well tolerated, it should be prescribed cautiously for patients with known contraindications to systemic use of beta-adrenergic blocking drugs (eg, asthma, heart failure).

Page 44: Topical Anesthetics  useful for diagnostic and therapeutic procedures, including tonometry, removal of foreign bodies or sutures, gonioscopy, conjunctival

Systemic Side Effects of Timolol

Page 45: Topical Anesthetics  useful for diagnostic and therapeutic procedures, including tonometry, removal of foreign bodies or sutures, gonioscopy, conjunctival

If the lacrimal outflow system is functioning, an estimated 80% of a timolol eye drop is absorbed from the nasal mucosa and passes almost directly into the vascular system. This is called the first-order pass effect and is true for all drugs that can be easily absorbed through mucosal tissue in the head.

whereas if given orally, its first pass includes absorption

via the gastrointestinal tract and then the liver, where 80–90% is detoxified before reaching the right atrium.

Cardiopulmonary histories should be taken for candidates of beta-blocker glaucoma therapy. Pulmonary function studies should be considered in patients with bronchoconstrictive disease, and electrocardiograms should be ordered on selected patients with cardiac disease. Patients with known bronchial asthma, chronic respiratory or cardiovascular disease, or sinus bradycardia may need screening before using timolol.

The drug should be used with caution in patients receiving other systemic beta-blocking agents.

Page 46: Topical Anesthetics  useful for diagnostic and therapeutic procedures, including tonometry, removal of foreign bodies or sutures, gonioscopy, conjunctival

Betaxolol Hydrochloride (Betoptic; Betoptic S)

Comment: Its relative 1 receptor selectivity reduces the risk of pulmonary side effects, particularly in patients with reactive airway disease.

Levobunolol Hydrochloride (Betagan) Comment: Levobunolol is a nonselective 1 and 2

blocker.

Metipranolol Hydrochloride (Optipranolol) Comment: Metipranolol is a nonselective 1 and 2

blocker .

Carteolol Hydrochloride (Ocupress)

Page 47: Topical Anesthetics  useful for diagnostic and therapeutic procedures, including tonometry, removal of foreign bodies or sutures, gonioscopy, conjunctival

Inhibition of carbonic anhydrase in the ciliary body reduces the secretion of aqueous.

useful in reducing the intraocular pressure in selected cases of open-angle glaucoma and can be used with some effect in angle-closure glaucoma.

sulfonamide derivatives. Oral administration produces the maximum effect in approximately 2 hours; intravenous administration, in 20 minutes. The duration of maximal effect is 4–6 hours following oral administration.

in patients whose intraocular pressure cannot be controlled with eye drops.

They are valuable for this purpose but have many undesirable side effects, including potassium depletion, gastric distress, diarrhea, exfoliative dermatitis, renal stone formation, shortness of breath, fatigue, acidosis, and tingling of the extremities.

Since the advent of timolol, topical carbonic anhydrase inhibitors, other newer glaucoma medications, and laser therapy, systemic carbonic anhydrase inhibitors are being used less frequently.

Page 48: Topical Anesthetics  useful for diagnostic and therapeutic procedures, including tonometry, removal of foreign bodies or sutures, gonioscopy, conjunctival

Acetazolamide (Diamox) 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.

Methazolamide (Neptazane)

Dichlorphenamide (Daranide)

Page 49: Topical Anesthetics  useful for diagnostic and therapeutic procedures, including tonometry, removal of foreign bodies or sutures, gonioscopy, conjunctival

Dorzolamide Hydrochloride (Trusopt) Preparation: Solution, 2%. Dosage: 1 drop two to

four times daily. Toxicity: Local reactions include burning and stinging,

superficial punctate keratopathy, and allergic reactions of the conjunctiva. Bitter after-taste is common. Systemic side reactions associated with oral carbonic anhydrase agents are rare.

Brinzolamide Ophthalmic Suspension (Azopt) Preparation: Suspension, 1%.

Page 50: Topical Anesthetics  useful for diagnostic and therapeutic procedures, including tonometry, removal of foreign bodies or sutures, gonioscopy, conjunctival

increasing outflow of aqueous humor, mainly via the uveoscleral pathway.

Latanoprost (Xalatan) Dosage: 1 drop daily.

Travoprost (Travatan)

Bimatoprost (Lumigan)

Unoprostone Isopropyl (Rescula) Dosage: Two drops daily.

Toxicity: All four preparations are associated with increased brown pigmentation of the iris, conjunctival hyperemia, punctate epithelial keratopathy, and a foreign body sensation.

In addition, they may aggravate ocular inflammation and have been associated with the development of cystoid macular edema.

Page 51: Topical Anesthetics  useful for diagnostic and therapeutic procedures, including tonometry, removal of foreign bodies or sutures, gonioscopy, conjunctival

improve compliance but not necessarily resulting in as large a reduction in intraocular pressure as expected from summation of the effects of the individual agents administered separately.

Xalacom (latanoprost 0.005% and timolol 0.5%) once daily in the morning,

Cosopt (dorzolamide 2% and timolol 0.5%) twice daily , Combigan (brimonidine 0.2% and timolol 0.5%) twice

daily, Duotrav (travoprost 0.004% and timolol 0.5%) once

daily, Ganfort (bimatoprost 0.03% and timolol 0.5%) once

daily

Page 52: Topical Anesthetics  useful for diagnostic and therapeutic procedures, including tonometry, removal of foreign bodies or sutures, gonioscopy, conjunctival

reduce intraocular pressure by making the plasma hypertonic to aqueous humor.

in the management of acute (angle-closure) glaucoma and occasionally in preoperative or postoperative surgery when reduction of intraocular pressure is indicated. The dosage for all is approximately 1.5 g/kg.

Glycerin (Osmoglyn) 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.

Isosorbide (Ismotic) Comment: Unlike glycerin, isosorbide does not produce calories or elevated

blood sugar. Mannitol (Osmitrol) 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.

Urea (Ureaphil) Toxicity: Accidental extravasation at the injection site may cause local reactions

ranging from mild irritation to tissue necrosis.

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Page 54: Topical Anesthetics  useful for diagnostic and therapeutic procedures, including tonometry, removal of foreign bodies or sutures, gonioscopy, conjunctival

Topical Corticosteroids

Page 55: Topical Anesthetics  useful for diagnostic and therapeutic procedures, including tonometry, removal of foreign bodies or sutures, gonioscopy, conjunctival

Indications inflammatory conditions of the anterior segment of the globe: allergic

conjunctivitis, uveitis, episcleritis, scleritis, phlyctenulosis, superficial punctate keratitis, interstitial keratitis, and vernal conjunctivitis.

Administration & Dosage The corticosteroids and certain derivatives vary in their anti-inflammatory

activity. The relative potency of prednisolone to hydrocortisone is 4 times; of dexamethasone and betamethasone, 25 times.

The duration of treatment will vary with the type of lesion and may extend from a few days to several months.

Initial therapy for a severely inflamed eye consists of instilling drops every 1 or 2 hours while awake. When a favorable response is observed, gradually reduce the dosage and discontinue as soon as possible.

Caution: Side effects of local steroid therapy are exacerbation of herpes simplex keratitis, fungal keratitis, cataract formation (unusual), and open-angle glaucoma (common). These effects are produced to a lesser degree with systemic steroid therapy. Any patient receiving topical ocular corticosteroid therapy or long-term systemic corticosteroid therapy should be under the care of an ophthalmologist

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Nonsteroidal Anti-Inflammatory Agents

(NSAIDs)

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Oral NSAIDs—indomethacin 75 mg daily, flurbiprofen 150 mg daily, or ibuprofen 600 mg daily—are the first-line treatment for scleritis. Gastric irritation and hemorrhage are a risk.

Topical ophthalmic preparations of several NSAIDs provide ocular bioavailability with little toxicity. These agents act primarily by blocking prostaglandin synthesis through inhibition of cyclooxygenas.

flurbiprofen (Ocufen), and suprofen (Profenal) : for inhibition of miosis during cataract surgery.

Ketorolac (Acular): seasonal allergic conjunctivitis. Diclofenac (Voltaren) and ketorolac (Acular) were the first

topically applied NSAIDs approved for treatment of postoperative inflammation following cataract surgery and for relief of pain and photophobia in patients undergoing laser corneal refractive surgery.

In addition, two new topically applied NSAIDs, nepafenac suspension (Nevanac) and Bromfenac solution (Xibrom), are now commercially available.

topically applied NSAIDs are often used to prevent and treat cystoid macular edema following cataract surgery.

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Other Drugs Used in the Treatment of Allergic

Conjunctivitis

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Cromolyn Sodium (Crolom) 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.

Ketotifen Fumarate (Zaditor) Dosage: Twice daily. Comment: Ketotifen has antihistamine and mast cell–stabilizing activity.

Lodoxamide Tromethamine (Alomide) 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.

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Nedocromil Sodium (Alocril) 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.

Emedastine Difumarate (Emadine) H1-antagonist Ketorolac Tromethamine (Acular) only cyclooxygenase inhibitor approved for allergy by the FDA.

Vasoconstrictors & Decongestants

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Anti-Infective Ophthalmic Drugs

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Topical Antibiotic Solutions & Ointments

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Bacitracin Most gram-positive organisms are sensitive to

bacitracin. It is not used systemically because of its nephrotoxicity.

Erythromycin particularly in staphylococcal conjunctivitis. It may be used instead of silver nitrate in prophylaxis of ophthalmia neonatorum. Neomycin 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. Polymyxin B Effective against many gram-negative organisms.

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Topical Preparationsof Systemic Antibiotics

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Topical use of the antibiotics commonly used systemically should be avoided if possible because sensitization of the patient may interfere with future systemic use.

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Tetracyclines limited uses in ophthalmology because their effectiveness is so

often impaired by the development of resistant strains. Ointment may be used for prophylaxis of ophthalmia neonatorum.

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.

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Ciprofloxacin (Ciloxan) 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.

Gatifloxacin (Zymar) This fourth-generation fluoroquinolone is more

effective against a broader spectrum of gram-positive bacteria and atypical mycobacteria than earlier fluoroquinolones.

Moxifloxacin (Vigamox) fourth-generation fluoroquinolone

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mixture of antibiotics and bacteriostatic agents

Sulfonamides 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

Sulfacetamide Sodium

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Topical Antifungal Agents

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Natamycin (Natacyn) Initial drug of choice for most mycotic corneal ulcers.

Nystatin (Mycostatin) Nystatin is not available in ophthalmic ointment form, but the

dermatologic preparation (100,000 U/g) is not irritating to ocular tissues and can be used in the treatment of fungal infection of the eye.

Amphotericin B (Fungizone) more effective than nystatin but not available in ophthalmic

ointment form. Many patients have extreme ocular discomfort following application of this drug.

Miconazole (Monistat) in the form of an intravenous preparation that may be instilled

directly into the eye. Fluconazole (Diflucan)

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Antiviral Agents

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Idoxuridine (Herplex) Used in the treatment of herpes simplex keratitis. Vidarabine (Vira-A) 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 stromal keratitis or uveitis. It may cause cellular toxicity and delay corneal regeneration. The cellular toxicity is less than that of idoxuridine.

Trifluridine (Viroptic) Acts by interfering with viral DNA synthesis. More soluble than

either idoxuridine or vidarabine and probably more effective in stromal disease.

Acyclovir (Zovirax) 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.

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Ganciclovir (Vitrasert)

Preparation: Intravitreal implant, 4.5 mg. Comment: treatment of cytomegalovirus retinitis without the adverse effects of systemic therapy.

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Fluorescein Sodium for detection of corneal epithelial defects,

in applanation tonometry, and in fitting contact lenses.

Rose Bengal Used in diagnosis of keratoconjunctivitis

sicca; the mucous shreds and devitalized corneal epithelium stain with rose bengal.

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Methylcellulose and related chemicals, polyvinyl alcohol and related chemicals, and gelatin are used in the formulation of artificial tears, ophthalmic lubricants, contact lens solutions, and gonioscopic lens solutions. These agents are particularly useful in the treatment of keratoconjunctivitis sicca

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The active ingredients in these agents usually are either ephedrine , naphazoline , phenylephrine

constrict the superficial vessels of the

conjunctiva and relieve redness. They also relieve minor surface irritation

and itching of the conjunctiva, which can represent a response to noxious or irritating agents such as smog, swimming pool chlorine, etc.

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reduce corneal edema by creating an osmotic gradient in which the tear film is made hypertonic to the corneal tissues. Temporary clearing of corneal edema results.

Preparations: Anhydrous glycerin solution (Ophthalgan); hypertonic sodium chloride 2% and 5% ointment and solution (Absorbonac, Ak-NaCl, Hypersal, Muro-128).

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Ocular & Systemic Side Effects of Drugs

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One important principle in avoiding systemic side effects from topical ophthalmic medications is to prevent overdosing. The physician should prescribe the lowest concentration of medication that will be therapeutically effective

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The eyelids should be kept closed for 3 minutes to prevent blinking.

The patient receiving multiple topical medications should wait 10 minutes between doses so that the first drug will not be washed out of the eye by the second.

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