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Ростовский Государственный Медицинский Университет

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Primary Care Ophthalmology_Palay, Krachmer_2005

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Therapeutic Medications	375

abnormalities and experience symptoms related to “dry eyes” (burning, itching, reﬂex tearing, and foreign body sensation). Patients with ocular surface abnormalities usually respond well to the “artiﬁcial tears” type of lubricant, although the symptomatic relief may be only temporary.

Restasis (cyclosporine 0.05% emulsion) is a newer agent for the topical treatment of severe dry eye associated with ocular inﬂammatory disorders.

Table 17–3 Artiﬁcial Tear Preparations

Generic Name	Trade Name	Preservative*

Carboxymethyl cellulose	Refresh Plus	None
	Celluvisc	None
Hydroxyethyl cellulose	Comfort Tears	Benzalkonium chloride,
		EDTA
Hydroxyethyl cellulose, polyvinyl	TearGard	Sorbic acid, EDTA
alcohol
Hydroxyethyl cellulose, povidone	Adsorbotear	Thimerosal, EDTA
Hydroxypropyl cellulose	Lacrisert	None
Hydroxypropyl methylcellulose	Isopto Plain	Benzalkonium chloride
	Isopto Tears	Benzalkonium chloride
	Tearisol	Benzalkonium chloride,
		EDTA
	Ultra Tears	Benzalkonium chloride
Hydroxypropyl methylcellulose,	Bion Tears	None
dextran 70	Tear Naturale II	Polyquad
	Tears Naturale Free	None
	Tears Renewed	Benzalkonium chloride,
		EDTA
Polycarbophil, PEG-400, dextran 70	AquaSite	EDTA
	AquaSite (multidose)	EDTA, ascorbic acid
Polyvinyl alcohol, PEG-400,	HypoTears	Benzalkonium chloride,
dextrose		EDTA
	HypoTears PF	EDTA
Polyvinyl alcohol, povidone	Murine	Benzalkonium chloride,
		EDTA
	Refresh	None
	Tears Plus	Chlorobutanol

*Preparations containing preservatives should be used no more than 6 to 8 times a day, to prevent toxicity to the ocular surface.

EDTA, ethylenediaminetetra-acetic acid.

Antibiotics

The most common ocular pathogens usually are staphylococci, streptococci, and Haemophilus species. Empirical treatment generally is successful in eradicating most surface infections; however, resistant organisms are becoming more common. Appropriate culture and susceptibility testing should be addressed before the initiation of therapy when clinically indicated.

376 CHAPTER 17 • Guide to Ophthalmic Medications

In general, topical antibiotics are given 4 to 6 times a day for simple infections and during the postoperative period. Severe infections, however, may require the use of multiple fortiﬁed antibiotics or an appropriate topical ﬂuoroquinolone every hour around the clock.

Fortiﬁed Antibiotics. Used by ophthalmologists for serious anterior segment and corneal infections when higher concentrations of drug are needed to ﬁght unusually virulent pathogens, fortiﬁed antibiotics are easily prepared by most pharmacies. The most common examples are fortiﬁed tobramycin or gentamicin, fortiﬁed vancomycin, and fortiﬁed cefazolin.

Table 17–4 Antibiotics

Generic Name	Trade Name	Bacterial Coverage

Bacitracin zinc	AK-Tracin	Most gram-positive organisms,
		diphtheroids, Haemophilus, and
		Actinomyces
Chloramphenicol	AK-Chlor	Many gram-positive and gram-negative
	Chloramphenicol	organisms, especially Haemophilus,
	(generic)	Moraxella species, Staphylococcus aureus,
	Chloromycetin	beta-hemolytic streptococci, and
	Chloroptic	diphtheroids
	Ocu-Chlor
Ciproﬂoxacin	Ciloxan	Broad spectrum, particularly targeting
hydrochloride		staphylococci, streptococci, and
		Pseudomonas aeruginosa
Erythromycin	AK-Mycin	Most gram-positive organisms,
	Erythromycin (generic)	diphtheroids, Haemophilus, Actinomyces,
	Ilotycin	and Neisseria species
Gatiﬂoxacin	Zymar	Fourth-generation ﬂuoroquinolone with
		broader spectrum of coverage, but not
		as good for Pseudomonas species
Gentamicin sulfate	Garamycin	Broad spectrum, particularly targeting
	Genoptic	staphylococci (when drug used in high
	Gentacidin	concentrations), and P. aeruginosa
	Gentak
	Gentamicin (generic)
Levoﬂoxacin	Quixin	Broad spectrum, particularly targeting
		staphylococci, streptococci, and
		Haemophilus inﬂuenzae
Moxiﬂoxacin	Vigamox	Fourth-generation ﬂuoroquinolone with
		broader spectrum of coverage, but not
		as good for Pseudomonas species
Oﬂoxacin	Ocuﬂox	Broad spectrum, particularly targeting
		staphylococci, streptococci, Haemophilus,
		and P. aeruginosa
Polymyxin B/bacitracin	AK-Poly-Bac	Some gram-negative organisms and most
	Polysporin	gram-positive organisms, diphtheroids,
		Haemophilus, and Actinomyces

Therapeutic Medications	377

Table 17–4 Antibiotics—cont’d

Generic Name	Trade Name	Bacterial Coverage

Polymyxin B/	AK-Spore Neosporin	Gram-negative organisms and broad
neomycin/bacitracin	Neotal	spectrum for gram-positive organisms,
	Polymyxin B (generic)	particularly targeting staphylococci,
		pseudomonads, diphtheroids,
		Haemophilus, and Actinomyces
Polymyxin B/	Terramycin	Most staphylococci, streptococci,
oxytetracycline		gonococci, Chlamydia species, and few
		gram-negative organisms
Polymyxin B/	Polytrim	Most staphylococci, streptococci, and
trimethoprim		Haemophilus
Sulfacetamide sodium	AK-Sulf	Wide range of gram-positive and gram-
	Bleph-10	negative organisms; some staphylococci,
	Cetamide	pneumococci, Haemophilus, Moraxella
	Isopto Cetamide	and Chlamydia species
	Ophthacet
	Sodium Sulamyd
	Sulf-10
	Sulfacetamide (generic)
Sulﬁsoxazole diolamine	Gantrisin	Wide range of gram-positive and gram-
		negative organisms; some staphylococci,
		pneumococci, Haemophilus, Moraxella
		and Chlamydia species
Tobramycin sulfate	Defy	Broad spectrum, including staphylococci,
	Tobrex	streptococci, Haemophilus, and
	Tobramycin (generic)	P. aeruginosa

Table 17–5 Antibiotic Concentrations

		Concentration of	Concentration of
Generic Name	Trade Name	Solution	Ointment

Bacitracin zinc	AK-Tracin	NA	50 units/g
Chloramphenicol	AK-Chlor	0.5%	1.0%
	Chloromycetin	0.5%	1.0%
	Chloroptic	0.5%	1.0%
	Ocu-Chlor	0.5%	1.0%
Ciproﬂoxacin	Ciloxan	0.3%	0.3%
hydrochloride
Erythromycin	AK-Mycin	NA	0.5%
	Erythromycin (generic)	NA	0.5%
	Ilotycin	NA	0.5%
Gatiﬂoxacin	Zymar	0.3%	NA
Gentamicin sulfate	Garamycin	0.3%	0.3%
	Genoptic	0.3%	0.3%
	Gentacidin	0.3%	0.3%
	Gentak	0.3%	0.3%
	Gentamicin (generic)	0.3%	0.3%

378 CHAPTER 17 • Guide to Ophthalmic Medications

Table 17–5 Antibiotic Concentrations—cont’d

		Concentration of	Concentration of
Generic Name	Trade Name	Solution	Ointment

Levoﬂoxacin	Quixin	0.5%	NA
Moxiﬂoxacin	Vigamox	0.5%	NA
Oﬂoxacin	Ocuﬂox	0.3%	NA
Polymyxin B/bacitracin	AK-Poly-Bac	NA	10,000 units,
			500 units/g
	Polysporin	NA	10,000 units,
			500 units/g
Polymyxin B/neomycin	Statrol	16,250 units,	10,000 units,
		3.5 mg/mL	3.5 mg/g
Polymyxin B/neomycin/	Neotal	NA	5000 units, 5 mg,
bacitracin			400 units/g
	Neosporin	NA	NA
	Polymyxin B (generic)	NA	NA
Polymyxin B/neomycin/	AK-Spore	10,000 units in 1.75 mg	NA
gramicidin	Neosporin	10,000 units in 1.75 mg	NA
gramicidin	Neosporin	or 0.025 mg/mL	NA
	Polymyxin B (generic) }	or 0.025 mg/mL	NA
	Polymyxin B (generic) }		NA
Polymyxin B/oxytetracycline	Terramycin	NA	10,000 units, 5 mg/g
Polymyxin B/trimethoprim	Polytrim	10,000 units, 1 mg/mL	NA
Sulfacetamide sodium	AK-Sulf	10.0%	10.0%
	Bleph-10	10.0%	10.0%
	Cetamide	NA	10.0%
	Isopto Cetamide	15.0%	NA
	Ophthacet	10.0%	NA
	Sodium Sulamyd	10%, 30%	10.0%
	Sulf-10	10.0%	NA
	Sulfacetamide (generic)	10%, 15%, 30%	10.0%
Sulﬁsoxazole diolamine	Gantrisin	4.0%	4.0%
Tobramycin sulfate	Defy	0.3%	0.3%
	Tobrex	0.3%	NA
	Tobramycin (generic)	0.3%	0.3%

NA, not applicable.

Antivirals

Advances in the pharmacology of chemotherapeutic agents used to ﬁght viral diseases have progressed rather slowly compared with those in other areas of medicine, in part because of the more complex mechanisms of viral infection that must be addressed in developing such agents. Viruses are obligate intracellular pathogens that use the host’s metabolic processes for their survival and replication. Thus, antiviral agents need to target the pathogen while leaving uninfected host cells essentially unaffected from their toxic side effects. To date, the most effective antiviral agents target viral enzymes and proteins that are essential for viral assembly.

Therapeutic Medications	379

Table 17–6 Antiviral Agents

Generic Name	Trade Name	Concentration	Indication

Idoxuridine	Herplex	0.1% solution	HSV infection
	Stoxil	0.5% ointment	HSV infection
Triﬂuridine	Viroptic	1.0% solution	HSV infection
Vidarabine	Vira-A	3.0% ointment	HSV infection
monohydrate
Acyclovir sodium	Zovirax	Systemic preparation only	HSV, HZV infection
Foscarnet sodium	Foscavir	Systemic preparation only	CMV infection in immunocompromised
			patients
Famciclovir	Famvir	Systemic preparation only	HZV infection
Ganciclovir sodium	Cytovene	Systemic preparation only	CMV infection in immunocompromised
	Vitrasert	Intraocular implant	patients
	Vitrasert	Intraocular implant
Valacyclovir	Valtrex	Systemic preparation only	HSV, HZV infection
hydrochloride

CMV, cytomegalovirus; HSV, herpes simplex virus; HZV, herpes zoster virus.

Antifungal Agents

Deciding on the appropriate ophthalmic antifungal usually depends on several variables, including the site of primary infection, route of administration, organism involved, and drug sensitivities. Currently, Diﬂucan (ﬂuconazole) and Sporanox (itraconazole) are oral/systemic agents that show good ocular penetration as an adjunct in these difﬁcult to treat infections.

Table 17–7 Antifungal Agents

Generic Name	Trade Name	Topical Concentration	Spectrum

Amphotericin B	Amphotericin B	0.1-0.5% solution	Blastomycetes; Candida, Coccidioides, and
			Histoplasma species
Flucytosine	Ancobon	1.0% solution	Candida species
Natamycin*	Natacyn	5% suspension	Candida species, aspergilli, and Cephalosporium,
			Fusarium, and Penicillium species
Miconazole nitrate	Monistat	1% solution	Candida and Cryptococcus species, aspergilli

*Often the drug of choice for most mycotic corneal infections and the only ocular formulation commercially available. The others need to be prepared by the pharmacy.

380 CHAPTER 17 • Guide to Ophthalmic Medications

Anti-inﬂammatory Agents

Anti-inﬂammatory agents are used most frequently to suppress immunologic mechanisms of all types, both externally and within the eye. Suppression of severe external inﬂammation is necessary to prevent corneal scarring and permanent tear ﬁlm abnormalities. Within the eye, these agents help prevent synechiae (scarring), some forms of glaucoma, and postoperative inﬂammation. Topical administration allows excellent penetration into the anterior chamber. Some agents penetrate easier (e.g., suspensions) than others depending on the chemical composition. Topical corticosteroids should be used with caution because they can cause cataracts and glaucoma used chronically and may acutely potentiate herpes simplex viral replication or microbial infection.

Table 17–8 Anti-inﬂammatory Agents

			Topical
Generic Name	Trade Name	Formulation	Concentration

Dexamethasone	Maxidex	Suspension*	0.1%
Dexamethasone sodium	AK-Dex	Ointment	0.05%
phosphate	Decadron	Ointment	0.05%
	Maxidex	Ointment	0.05%
	Dexamethasone (generic)	Ointment	0.05%
Dexamethasone sodium	AK-Dex	Solution	0.1%
phosphate	Decadron	Solution	0.1%
	Dexamethasone (generic)	Solution	0.1%
Fluorometholone	Fluor-OP	Suspension*	0.1%
	FML	Suspension*	0.1%
	FML Forte	Suspension*	0.25%
	FML S.O.P.	Ointment	0.1%
Fluorometholone acetate	Flarex	Suspension*	0.1%
Loteprednol etabonate	Alrex	Suspension*	0.2%
	Lotemax	Suspension*	0.5%
Medrysone	HMS	Suspension*	1.0%
Prednisolone acetate	Econopred	Suspension*	0.125%
	Econopred Plus	Suspension*	1.0%
	Pred-Forte	Suspension*	1.0%
	Pred Mild	Suspension*	0.125%
Prednisolone sodium	AK-Pred	Solution	0.125%, 1.0%
phosphate	Inﬂamase	Solution	0.125%
	Inﬂamase Forte	Solution	1.0%
	Prednisolone (generic)	Solution	0.125%, 1.0%
Rimexolone	Vexol	Suspension*	1.0%

*Suspensions need to be shaken before instillation.

Therapeutic Medications	381

Anti-inﬂammatory and Antibiotic Combinations. Generally, anti-inﬂammatory medications are indicated for steroid-responsive inﬂammatory ocular conditions for which a corticosteroid is indicated and bacterial infection or risk of bacterial ocular infection exists. These medications may be contraindicated in any condition in which an epithelial defect exists, including patients with epithelial herpes simplex keratitis and those who have recently undergone uncomplicated removal of a corneal foreign body.

Table 17–9 Anti-inﬂammatory and Antibiotic Combinations

			Formulation and
Generic Name	Trade Name		Amount	Typical Dosage

Gentamicin sulfate/	Pred-G		Suspension (5 mL)	1 drop 4 times a day
prednisolone acetate			Ointment (3.5 g)	Up to 4 times a day
Neomycin/polymyxin B/	Dexacidin	}	Suspension (5 mL)	1 drop 4 times a day
dexamethasone	Maxitrol	}	Ointment (3.5 g)	Up to 4 times a day
Neomycin/dexamethasone	NeoDecadron		Suspension (5 mL)	1 drop 4 times a day
			Ointment (3.5 g)	Up to 4 times a day
Oxytetracycline/dexamethasone	Terra-Cortril		Suspension (5 mL)	1 drop 3 times a day
Sulfacetamide sodium/	AK-Cide		Suspension (5 mL)	1 drop 4 times a day
prednisolone acetate	VasocidinBlephamide }		Suspension (5 mL)	1 drop 4 times a day
prednisolone acetate	VasocidinBlephamide }		Ointment (3.5 g)	Up to 4 times a day
Tobramycin/dexamethasone	Tobradex		Suspension (5 mL)	1 drop 4 times a day
			Ointment (3.5 g)	Up to 4 times a day

Nonsteroidal Anti-inﬂammatory Agents. Nonsteroidal anti-inﬂammatory drugs (NSAIDs) also are used to suppress inﬂammatory mechanisms, both externally and within the eye. They differ from corticosteroids in their mechanisms of action and effectiveness; however, they do not cause cataracts or glaucoma or potentiate herpes simplex viral replication.

Table 17–10 Nonsteroidal Anti-inﬂammatory Agents

Generic Name	Trade Name	Formulation	Topical Concentration

Diclofenac	Voltaren	Solution	0.1%
Flurbiprofen	Ocufen	Solution	0.03%
Ketorolac	Acular	Solution	0.5%
Suprofen	Profenal	Solution	1.0%

382 CHAPTER 17 • Guide to Ophthalmic Medications

Table 17–11 Comparison of Selected Anti-inﬂammatory Agents

Generic Name	Trade Name	Comment

NSAIDs	Ocufen	Interference with prostaglandin-induced operative
	Voltaren	miosis, other inﬂammations (e.g., iritis, cystoid
	Acular	macular edema), and allergy-related irritation; no
		causation of cataracts or glaucoma; no potentiation of
		herpes simplex infection
Loteprednol	Alrex	Used for ocular surface allergy control
	Lotemax	Higher strength, better for intraocular inﬂammation
		Fewer side effects than with prednisolone and
		dexamethasone
Medrysone	HMS	Weak steroid, useful for surface allergy, very few side
		effects
Fluorometholone	FML	More potent than medrysone, excellent for external
		inﬂammation, fewer side effects than with
		prednisolone and dexamethasone
Prednisolone	Pred-Forte	Potent steroid, highly effective for anterior segment
acetate		inﬂammation, higher risk of side effects (IOP
		elevation, infection, HSV activation)
Dexamethasone	Decadron	Highly potent and effective, very high risk of side
sodium		effects
phosphate
Rimexolone	Vexol	Potent steroid, with somewhat fewer ocular side effects
		(similar to those with FML)

HSV, herpes simplex virus; IOP, intraocular pressure; NSAIDs, nonsteroidal anti-inﬂammatory drugs.

Antiglaucoma Medications

Antiglaucoma medications are used to reduce optic nerve damage and visual loss associated with elevated introcular pressure. The seven classes of these medications, which differ in their mechanisms of action, are as follows:

1.Beta-blocking agents (Table 17–12)

2.Adrenergic agonists (Table 17–13)

3.Cholinergic agonists (Table 17–14)

4.Sympathomimetics (Table 17–15)

5.Carbonic anhydrase inhibitors (Table 17–16)

6.Prostaglandins (Table 17–17)

7.Hyperosmotic agents (Table 17–18)

Beta Blockers. A class of drugs commonly used as ﬁrst-line agents for treatment of open-angle glaucoma and ocular hypertension, beta blockers work mostly by reducing aqueous humor secretion by the ciliary body. Because of some systemic absorption, they may be contraindicated in some patients with heart and respiratory conditions. More selective beta blockers appear to have less severe side effects, but are not as efﬁcacious. Ocular side effects include stinging and burning.

Therapeutic Medications	383

Table 17–12 Antiglaucoma Medications: Beta Blockers

Generic Name	Trade Name	Typical Dosage	Comments

Betaxolol hydrochloride	Betoptic-S (0.25%) 1 drop	Generic (0.5%) 1 drop	Beta-2 selective; use cautiously
	2 times a day	2 times a day	in patients with respiratory
			conditions
Carteolol hydrochloride	Ocupress (1.0%)	1 drop 2 times a day	Nonselective beta blocker
Levobunolol	Betagan (0.25%, 0.5%)	1 drop 2 times a day	Nonselective beta blocker
hydrochloride	Generic (0.25%, 0.5%)	1 drop 2 times a day
Metipranolol	Optipranolol (0.3%)	1 drop 2 times a day	Nonselective beta blocker
Timolol maleate	Timoptic (0.25%, 0.5%)	1 drop 2 times a day	Nonselective beta blocker
Timolol maleate	Timoptic XE (0.25%, 0.5%)	Once a day	Nonselective beta blocker;
			solution becomes a gel
			once in contact with the
			eye, increasing period of
			drug delivery
Timolol hemihydrate	Betimol (0.25%, 0.5%)	1 drop 2 times a day	Nonselective beta blocker

Alpha Agonists. Alpha agonists reduce intraocular pressure by decreasing aqueous production and increasing uveoscleral outﬂow. This class may prove to be effective at reducing intraocular pressure without the cardiac side effects of beta blockers. Currently, two drugs are on the market. The most common side effect is an allergic reaction developing with long-term use.

Table 17–13 Antiglaucoma Medications: Alpha Agonists

Generic Name	Trade Name	Typical Dosage	Comments

Apraclonidine	Iopidine (0.5%, 1%)	1 drop 3 times a day	Short-term adjuvant for patients on
			maximal medical therapy; approximately
			1 month to be effective
Brimonide tartrate	Alphagan-P (0.15%)	1 drop 3 times a day	Agent with seemingly better toleration
			than its predecessor; less tachyphylaxis
			noted
	Generic (0.2%)	1 drop 3 times a day	High allergy incidence

Cholinergics. Parasympathomimetic agents are divided into direct-acting (cholinergic) and indirect-acting (anticholinesterase) agents. Used primarily for glaucoma and control of accommodative esotropia, they reduce intraocular pressure by causing contraction on the ciliary muscle. This contraction pulls on the trabecular meshwork and facilitates aqueous outﬂow. Acute poisoning with these agents (unusual with topical application) can produce the cholinergic crisis syndrome, which includes sweating, gastrointestinal disturbances, bradycardia, and paralysis of the respiratory muscles.

384 CHAPTER 17 • Guide to Ophthalmic Medications

Table 17–14 Antiglaucoma Medications: Cholinergic Agents

Generic Name	Trade Name	Typical Dosage	Concentrations

Cholinergic Agents
Carbachol	Isopto Carbachol	1 drop 3 times a day	1.5%, 3%
Pilocarpine	Akarpine	1 drop 4 times a day	1%, 2%, 4%
hydrochloride	Isopto Carpine	1 drop 4 times a day	0.5%, 1%-6%, 8%, 10%
	Ocusert-Pilo	1 insert a week	20-40 mg/hr/week
	Pilocar	1 drop 4 times a day	0.5%, 1%-4%, 6%
	Pilopine HS Gel	1/2 inch at bedtime	4%
	Piloptic	1 drop 4 times a day	0.5%, 1%-4%, 6%
	Pilostat	1 drop 4 times a day	1%, 2%, 4%
	Storzine	1 drop 4 times a day	1%, 2%, 4%
	Generic	1 drop 4 times a day	0.5%, 1%-4%, 6%
Pilocarpine nitrate	Pilagan	1 drop 4 times a day	1%, 2%, 4%
Anticholinesterase Agents
Physostigmine	Eserine	1 drop 4 times a day	0.25%
	Generic (ointment)	1/2 inch 3 times a day	0.25%
Demecarium	Humorsol	1 drop 2 times a day	0.125%, 0.25%
		to 1 drop a week
Echothiophate iodide	Phospholine iodide	1 drop 2 times a day	0.125%, 0.25%

Sympathomimetics. Sympathomimetics have been of limited usefulness in the general population due to the numerous side effects (surface allergy, tolerance) associated with their use. However, a certain subset of the population tolerates these medications. These agents reduce intraocular pressure by mostly increasing aqueous outﬂow.

Table 17–15 Antiglaucoma Medications: Sympathomimetics

Generic Name	Trade Name	Typical Dosage	Concentration

Epinephrine bitartrate	Epitrate	1 drop every day or 2	2%
		times a day
Epinephrine borate	Epinal	1 drop 2 times a day	0.5%, 1%
	Eppy/n	1 drop 2 times a day	0.5%, 1%, 2%
Epinephrine hydrochloride	Epifrin	1 drop every day or 2	0.5%, 1%, 2%
	Glaucon	times a day	1%, 2%
Dipivefrin hydrochloride	Propine	1 drop 2 times a day	0.10%

Carbonic Anhydrase Inhibitors. Carbonic anhydrase inhibitors (CAIs) reduce aqueous formation by direct inhibition of carbonic anhydrase within the ciliary body. Oral CAIs are highly effective but can also result in serious side effects such as paresthesias, anorexia, gastrointestinal disturbances, headaches, altered taste and smell, and sodium and potassium depletion. Kidney stone formation may be facilitated in certain patients. Topical CAIs appear to be much better tolerated, with a lower side-effect proﬁle, but are not as effective.

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