By Lorne Yudcovitch, O.D., M.S., F.A.A.O.
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INTRODUCTION
Most optometrists who have practiced with therapeutic privileges are comfortable prescribing topical medications for ocular conditions such as conjunctivitis and glaucoma. However, when topical drops or ointments are not enough to treat a particular condition, oral agents may be necessary. This article reviews some of the most commonly prescribed oral medications used to manage infections, allergies, pain and inflammation, elevated IOP, and age-related macular degeneration (ARMD).
TREATMENT OF BACTERIAL INFECTIONS
There are five main categories of antibiotics used in the treatment of bacterial infections. These categories are based on how the drugs affect the target organism. Table 1 summarizes these categories, with examples of specific antibiotics in each category
Table 1. Antibiotic Drugs
|
Category
|
Mode of Action
|
Example Oral Drugs
|
|
1
|
Inhibit bacterial cell wall formation | Penicillins, Cephalosporins, Vancomycin |
|
2
|
Disrupt the bacterial cytoplasmic membrane | There are no oral antibiotics in this category |
|
3
|
Inhibit bacterial folic acid synthesis | Sulfonamides, Trimethoprim, Pyrimethamine |
|
4
|
Inhibit bacterial protein synthesis | Erythromycin, Clarithromycin, Azithromycin, Tetracycline, Doxycycline, Clindamycin, Chloramphenicol |
|
5
|
Inhibit bacterial DNA synthesis | Fluoroquinolones (e.g., Norfloxacin, Ofloxacin, Ciprofloxacin) |
Many antibiotics (in particular, the penicillins) can reduce the effect of oral contraceptives, so women who take birth control pills should be warned of this possibility.
Here are some of the more popular antibiotics prescribed with the typical adult dosages.
Antibiotics That Inhibit Bacterial Cell Wall Formation

Figure 1. Augmentin (amoxicillin with clavulanic acid)
Augmentin is useful treatment for such ocular infections such as preseptal cellulitis, canaliculitis, dacryocystitis, or dacryoadenitis. This combination of the penicillin, amoxicillin (available in 250 mg, 500 mg, or 875 mg doses) and beta-lactamase inhibitor clavulanic acid (125 mg dose) is typically prescribed as 500 mg/125 mg PO q8 hours or 875 mg/125 mg PO q12 hours for a week to ten days. This medication is best taken with meals.
Clavulanic acid inactivates the penicillinase or beta-lactamase that organisms such as Staphylococcus, Haemophilus, and Neisseria gonorrheae produce, making the amoxicillin more efficacious in inhibiting cell wall formation for these bacteria.
Dicloxacillin is another popular penicillin antibiotic. Its structure renders it resistant to penicillinases but not to beta lactamases. It is useful for treating staphylococcal infections because these organisms produce penicillinase.
Ask the patient about any penicillin allergies such as rash, hives, itching, or difficulty breathing before prescribing either Augmentin or Dicloxacillin.
The most severe side-effects include anaphylaxis, anemia, pseudomembranous colitis, and Stevens-Johnson syndrome, as well as risk of secondary infection by non-susceptible bacteria or fungi. Any digestive problems such as diarrhea or unusual bleeding should be reported by the patient promptly.

Figure 2. Cephalosporins: Keflex (cephalexin) and cefaclor
Cephalexin (trade name: Keflex) and cefaclor (trade name: Ceclor) are first and second-generation cephalosporins, respectively, that share similar ocular indications with Augmentin. Like the penicillins, they inhibit bacterial cell wall formation.
Both Keflex and Ceclor come in 250 mg and 500 mg doses. Keflex is typically prescribed 500 mg PO q12 hour for a week to ten days. Ceclor is typically prescribed 250-500 mg PO q8 hours for ten days.
Although Keflex is a popular workhorse antibiotic, the second-generation Ceclor may be a better choice because its spectrum of activity includes many beta-lactamase producing bacteria. Ceclor is also approved for children as young as 1 month.
Cefadroxil (trade name: Duracef) is another popular, but more expensive, cephalosporin antibiotic.
Potential serious side-effects associated with these drugs include hypersensitivity reactions, pseudomembranous colitis, hypoprothrombinemia, and reversible renal impairment. Elderly individuals who have decreased renal function should be prescribed an alternative medication if possible.
Patients who are allergic to penicillins may also react to cephalosporins (the incidence of cross allergies is estimated between 5-16%), so an alternative antibiotic class may be required.
Antibiotics That Inhibit Folic Acid Synthesis

Figure 3. Bactrim (trimethoprim/sulfamethoxazole)
Trimethoprim/sulfamethoxazole (trade name: Bactrim) is considered a second-choice antibiotic for cases of preseptal cellulitis or lacrimal infections in patients who have contraindications to other antibiotics. It is a combination of two antibiotics that each inhibit the bacterias intermediary metabolism of folic acid synthesis.
This medication is typically less effective against gram-negative organisms. Bactrim is available as Bactrim DS (160 mg trimethoprim/800 mg sulfamethoxazole) and Bactrim SS (half the amounts of DS) forms. Typical dosage is 160 mg/800 mg PO q12 hour.
Serious side effects of Bactrim are comparable to the penicillins and cephalosporins. Folinic acid supplement may need to be co-prescribed to prevent the patient from developing folate deficient megaloblastic anemia.
Also, as this antibiotic contains a sulfonamide (sulfamethoxazole), it is contraindicated in patients with sulfa allergies. Sulfonamides are also less effective in purulent infections because the pus contains breakdown products that reduce the bacterias need for folic acid.

Figure 4. Daraprim (pyrimethamine) for malaria
Pyrimethamine is prescribed for cases of active ocular toxoplasmosis retinochoroiditis. It is typically used in conjunction with sulfadiazine, and like sulfadiazine it is a folic-acid inhibitor.
Pyrimethamine is prescribed as a 100 to 200 mg PO loading dose on day one, followed by 25 to 50 mg PO per day for four to five weeks (sulfadiazene is co-prescribed with a loading dose of 2 to 4 g PO on day one, followed by 1 g PO per day.) Administer with folinic acid to prevent folate deficiency.
Serious side effects are comparable to Bactrim, the penicillins, and cephalosporins, but might also include seizures. This medication is also used for malaria treatment and prophylaxis.
Antibiotics That Inhibit Bacterial Protein Synthesis

Figure 5. Doxycycline
Doxycycline (trade names: Doryx, Periostat, Vibramycin, generic) is a long-acting tetracycline antibiotic commonly used for ocular rosacea, blepharitis, hordeola and meibomian gland dysfunction. It is also used in cases of ocular Chlamydia and certain protozoal infections such as toxoplasmosis.
This class of antibiotic inhibits protein synthesis by binding to the organisms ribosomes. Interestingly, there is also an anticollagenolytic activity in this class that may be useful in certain cases of sterile corneal ulcers or stromal melt. It comes in 20 mg, 50 mg, and 100 mg tablets. Typical dosage is 100 mg PO q12 hour for two weeks then, if needed, tapered to 100 mg PO qd for up to six months.
Doxycycline is prescribed much more often than tetracycline because there are usually fewer dosages per day and doxycycline can be taken with meals. Tetracycline must be taken in higher dosages and on an empty stomach to allow absorption. There are usually fewer side effects with doxycycline than tetracycline.
Tetracycline-type antibiotics, such as doxycycline, can cause photophobia, pseudotumor cerebri, and blood dyscrasias, as well as decreased bone growth and teeth discoloration in children under 8 years of age, so avoid it with children, nursing mothers, or pregnant women.

Figure 6. Erythromycin
Erythromycin (numerous trade names, generic), and similar drugs such as azithromycin and clarithromycin, is a macrolide antibiotic. This class, like the tetracyclines, inhibits protein synthesis by ribosomal binding they simply bind to the larger ribosomal subunits while the tetracyclines bind to the smaller ribosomal subunit.
Erythromycin is typically indicted as a second-choice treatment in Staphylococcus and other gram-positive eyelid infections, as well as for chlamydial infections such as ophthalmia neonatorum and adult inclusion conjunctivitis.
Dosage and formulas are varied although 250 mg and 500 mg tablets are common (suspension syrup is also available). The typical adult dosage is 250-500 mg PO q6-12 hours for two to three weeks.
Although erythromycin has a limited antibacterial spectrum (mainly gram-positive bacteria), it is one of the safest antibiotics to use. As such, it may be used more frequently with children and pregnant women, because side-effects are infrequent.
Serious side-effects can include anaphylaxis, pseudomembranous colitis, and hepatotoxicity when the estolate form of erythromycin is prescribed.

Figure 7. Zithromax (azithromycin)
Azithromycin (Zithromax) is another macrolide antibiotic popular with optometrists. It is used primarily for chlamydial conjunctivitis, prescribed in a dose-pack as four 250 mg tablets PO in one day. It can also be prescribed for skin infections as two 250 mg tablets PO on day one, followed by 250 mg PO qd for four more days. There is also a 1000 mg suspension form that is diluted with water and drunk.
Zithromax has become known as the big gun in treating chlamydial infection, and has been used worldwide in an effort to eradicate Chlamydia caused trachoma. Because of this, tetracyclines are considered a second-line chlamydial treatment at this time.
Serious side effects of azithromycin include anaphylaxis, Stevens-Johnson syndrome, pseudomembranous colitis, cholestatic jaundice. Fortunately, the short duration use of this medication may help reduce many side-effects that can occur with long-term antibiotic treatment.
As an side note, the antibiotic Chloramphenicol should be avoided due to the rare risk of potentially fatal bone marrow depression such as aplastic anemia (even with topical use), as well as numerous potential neurological complications. It is mentioned here simply to alert the practitioner.
Antibiotics That Inhibit Bacterial DNA Synthesis
Unlike other antibiotics that are bacteriostatic (bacteria-inhibiting) such as macrolides, the fluoroquinolones are bactericidal (bacteria-killing). The fluoroquinolones blockage of bacterial DNA gyrase to produce more DNA causes bacterial death. As such, this drug may be preferred when other drugs are ineffective or are contraindicated.

Figure 8. Cipro (ciprofloxacin)
Ciprofloxacin is a common fluoroquinolone (trade names: Cipro, Cipro XR, generic), which is prescribed for numerous bacterial and urinary tract infections, gonorrhea, and anthrax. It comes in 100 mg, 250 mg, 500 mg, 750 mg, and 1000 mg tablets. Typical dosage is 500 mg PO q12hour, although a higher dosage may be indicated depending on infection severity.
Milk or any calcium-fortified products should be avoided when taking fluoroquinolones.
Serious side-effects include seizures, psychosis, allergy, pseudomembranous colitis, and phototoxicity.
Resistance to fluoroquinolones, particularly by staphylococci, has been growing in recent years, so newer-generation fluoroquinolones or other class antibiotics may need to be considered if the patient's infection is not resolving.
TREATMENT OF VIRAL INFECTIONS

Figure 9. Zovirax (acyclovir) pills
In 1989, Acyclovir (trade name: Zovirax) was the first oral antiviral approved for herpetic infections. Acyclovir disrupts viral DNA synthesis in infected host cells while leaving uninfected host DNA replication alone.
It is indicated for varicella zoster virus (VZV) and certain herpes simplex virus (HSV) infections, and is available in 200, 400 and 800 mg tablets, as well as a 200 mg/5 ml suspension, as well as in generic form. Because of acyclovirs short half-life, it must be taken five times a day for initial infections.
Typical dosages are 400 mg PO 5x/day for seven days for herpes simplex infections, and 800 mg PO 5x/day for ten days for varicella/zoster infections. In addition, it has been found that a 400 mg PO BID dosage for up to two years may reduce the risk of recurrent herpes simplex corneal epithelial and stromal infections by almost 50%.
Before prescribing determine if a patient has hypersensitivity to acyclovir, or if there are any renal or hepatic problems, neurological problems (rare seizures have been reported), or hypoxia. However, this medication is relatively safe to use, and is recommended for children (at pediatric dosages) who develop herpetic infections including chicken pox. One study suggests that children with epithelial herpetic infection may be better treated with oral acyclovir than topical antivirals.

Figure 10. Valtrex (valcyclovir) and Famvir (famciclovir)
Famciclovir (trade name: Famvir) and valcyclovir (trade name: Valtrex) are newer anti-herpetic drugs that have a longer half-life than acyclovir. As such, they are typically prescribed on a TID dosage. Famvir comes in 125, 250, and 500 mg tablets, while Valtrex comes in 500 and 1000 mg tablets.
Famvir is usually prescribed 250 mg PO TID for one week for herpes simplex infections and 500 mg PO TID for 10 days for varicella/zoster infections. Valtrex is typically prescribed TID at double the dosage of Famvir.
Use caution with these medications, just as you would with acyclovir.
TREATMENT OF ALLERGIES
If a patient presents with an allergic response that has both systemic and ocular symptoms, or if a patient is not adequately responding to ocular allergy topical treatment, oral antihistamines should be considered. These drugs may also be used to help control Type I hypersensitivity reactions such as anaphylaxis.

Figure 11. First generation oral antihistamines: Benadryl (diphenhydramine), Chlor-Trimetron (chlorpheniramine), and Dimetapp (brompheniramine)
The first generation antihistamines (e.g., trade names Benadryl, Chlor-Trimetron, and Dimetapp) bind to histamine receptors, preventing the allergic response. Dosages vary depending on the medication.
Benadryl is available in 25 and 50 mg tablets as well as a 12.5 mg/5 ml elixir, while Chlor-Trimetron is available in 4, 8, and 12 mg tablets. Dimetapp comes only in a 1:15/5 ml elixir form in combination with pseudoephedrine.
Benadryl is prescribed typically 4-12 mg PO 4-12 hours, Chlor-Trimetron 25-50 mg PO 4-12 hours, and Dimetapp is given 5-10 ml PO TID/QID.
Quite frequently the first generation antihistamines tend to cause sedation, so patients should be warned of this effect. These antihistamines also tend to dry the throat and bronchi.
Caution should be used when prescribing Dimetapp to hypertensive patients due to the vasoconstrictor pseudoephedrine present in the elixir.
Second-generation, or non-sedating, antihistamines have become popular among consumers for allergic treatment. These antihistamines have fewer anti-cholinergic side-effects and are longer acting than their first-generation cousins.

Figure 12. Second generation oral antihistamines: Allegra (fexofenadine), Claritin (loratidine), and Zyrtec (cetrizine)
Loratidine (trade name: Claritin) comes in 10 mg tablets or 1 mg/ml syrup, fexofenadine (trade name: Allegra) comes in 30, 60, and 180 mg tablets, and cetrazine (trade name: Zyrtec) comes in 5 mg, 10 mg, and 1 g/ml syrup.
Allegra and Zyrtec also come in combination tablets (called Allegra-D and Zyrtec-D) with pseudoephedrine.
Claritin is now available as an OTC product.
A newer antihistamine desloratidine (trade name: Clarinex) comes in a 5 mg tablet form as well as a 5 mg sublingual form (trade name: Clarinex Reditabs). Because these drugs are longer acting, the dosage is once or twice a day.
Typical dosage for Claritin is 10 mg PO qd, for Allegra 60 mg PO BID (or 180 mg PO qd), Zyrtec 10 mg PO BID, and Clarinex 5 mg PO qd.
There may be possible drug interactions of second-generation antihistamines with erythromycin and anti-fungals, so the practitioner should be cautious. Food may affect antihistamine absorption as well.
TREATMENT OF OCULAR PAIN AND INFLAMMATION
Ocular conditions such as corneal abrasions, burns or erosions, ultraviolet keratopathy, uveitis, post-surgery symptoms, lid lacerations or other injuries, and zoster infections can cause significant pain. The optometrist may need to prescribe an oral analgesic in combination with other treatment when managing these conditions.
Based on their mechanisms of action, analgesics can be divided into peripherally acting and centrally acting. In general, peripherally acting analgesics work to inhibit peripheral pain receptors (through metabolic pathways such as the cyclo-oxygenase route), while centrally acting drugs affect the central nervous systems opioid receptors that are involved in pain perception.
Independent of the type of drug prescribed, the goal of therapy is to prescribe the least amount of medication required to adequately control the patient's pain. However, the doctor should also be aggressive enough when prescribing pain medication to ensure that the patient's discomfort is satisfactorily relieved.

Figure 13. Common OTC pain drugs: Tylenol (acetaminophen) and Advil (ibuprofen)
Sometimes peripheral-acting, over-the-counter medications are enough to quell the pain symptoms. Acetaminophen (trade name: Tylenol) is very popular in this regard, and comes in 325 and 500 mg tablets, as well as 160 or 325 mg/5 ml syrups. A generic form is available. Typical dosage is 325-1000 mg PO q4-6 hours. It is also combined with many central-acting painkillers, some of which will be discussed below.
Ibuprofen (trade names: Advil, Motrin, and Nuprin) is also popular and comes in 100 to 800 mg tablets, typically prescribed 300-800 mg PO q4-6 hours. It is also available in generic forms.
Acetaminophen is regarded as the safest pain medication in terms of systemic side-effects. Ibuprofen has a few relatively severe side-effects including kidney and liver toxicity, but the incidence of these side-effects is low.
As a side note, acetylsalicylic acid (ASA or aspirin) also serves in pain management, but its blood-thinning properties can create problems for some patients, and it has a higher risk of causing gastro-intestinal bleeds. Aspirin can also cause Reyes syndrome, a life-threatening brain disease, and lipid abnormality, if used with children and teenagers with chicken pox or flu symptoms. It should be avoided in these cases. Diflusinal (trade name: Dolobid) is a derivative of ASA, and should be regarded similarly.
Painkillers such as ibuprofen block both the cyclo-oxygenase-1 (COX-1) and cyclo-oxygenase-2 (COX-2) inflammatory pathways in the body. COX-1 mediates the production of the normal prostaglandins that benefit renal function, maintenance of the gastric mucosa, and blood coagulation. COX-2 mediates the production of the pathological prostaglandins that cause inflammation and pain.
COX-2 inhibiting drugs, therefore, inhibit the pathological prostaglandins while leaving the normal prostaglandins alone. This may offer a new level of safety as compared to the non-selective peripheral-acting analgesics such as ibuprofen.

Figure 14. COX-2 inhibiting drugs: Celebrex (celecoxib).
Celecoxib (trade name: Celebrex) is an example of a COX-2 inhibiting painkiller. Celebrex comes in 100, 200 and 400 mg tablets, and is typically prescribed 100 to 200 mg PO BID.
Side-effects of the COX-2 analgesics include hypertension along with heart and blood abnormalities, as well as liver and renal problems. These medications should not be used in conjunction with any other peripheral-acting painkillers for extended time periods.

Figure 15. Dual-action NSAID: Ultram (tramadol)
Tramadol (trade name: Ultram) is a good choice when pain is not responding to peripheral-acting analgesics, but there is concern over using a stronger, centrally-acting narcotic painkiller. Ultram has a dual central-acting mechanism, in that it weakly binds opioid receptors while also weakly inhibiting serotonin and norepinephrine reuptake. It comes in 50 mg tablets. Typical dosage is 50-100 mg PO q4-6 hours.
Due to its weaker effect, there may be less narcotic side effects than with other opiate analgesics, although the practitioner should still be wary of adverse reactions.
When the pain is severe enough that a stronger analgesic is necessary, the optometrist may need to prescribe a central-acting narcotic agent.

Figure 16. Narcotic analgesics: Tylenol #3 (acetaminophen + codeine), Vicodin (acetaminophen + hydrocodone)
Tylenol comes in several 300 mg acetaminophen:codeine combinations, designated by number (Tylenol #2 includes 15mg codeine, #3 includes 30mg, and #4 includes 40mg).
Typical dosage is 300 mg:30 mg PO q4 hours, maximum to 12 tablets in 24 hours.
Hydrocodone (with acetaminophen in Vicodin) is available in 500 mg:5 mg tablets, typically prescribed as 1-2 tablets PO q 4-6 hours. It also comes in stronger 660:10 mg (Vicodin HP) and 750:7.5 mg form (Vicodin ES) forms as well as in combination with ibuprofen (Vicoprofen).
Narcotic analgesics should be used for short duration therapy only because addiction can occur with these central-acting agents. The optometrist should determine if there is a patient history of narcotics dependency, and prescribe carefully. Specific prescription documentation, such as indicating no refills and spelling out the quantities rather than writing a number (i.e., Twenty tablets rather than 20 tablets) as well as communicating verbally with the patients pharmacist will help to prevent any potential forgery and abuse.
Respiratory depression is a serious potential side-effect of narcotic medications, as are sedation and gastrointestinal problems. Although hydrocodone is several times more potent than codeine, it tends to cause less sedation and gastro-intestinal problems than codeine does.
Many analgesics fall into federal Drug Enforcement Agency (DEA) Controlled Substances classifications, so it is useful to be familiar with these classifications.
Table 2. DEA Controlled Substances Classifications With Example Drugs
|
Schedule
|
Description
|
Examples
|
Prescribing Guidelines
|
|
I
|
High abuse potential | Heroin, marijuana, LSD | Not available therapeutically |
|
II
|
High abuse potential, severe dependence risk | Codeine, cocaine, Demerol, morphine, amphetamines, barbiturates, methadone | Written, signed prescription required |
|
III
|
Moderate-low physical dependence or high psychological dependence | Tylenol #3, Vicodin, Fiorinal, Phenergan + codeine, Tussionix, Empirin #3 | No more than 5 refills or dispensed more than 6 months after Rx date |
|
IV
|
Less abuse potential, limited dependence | Valium, Xanax, Librium, Darvon, Phenobarbitol | Same as Schedule III |
|
V
|
Limited abuse potential | Tylenol + codeine elixir, Phenergan + codeine syrup, Robitussin DAC syrup | Some over-the-counter sales allowed if 18 years of age or older; otherwise Rx needed |
Management of several ocular inflammatory conditions, including uveitis, scleritis, AION, orbital pseudotumor, and optic neuritis may require use of an oral corticosteroid. Steroids act to inhibit the cyclo-oxygenase pathway, and significantly reduce inflammation, as well as pain in many cases.

Figure 17. Oral steroids. Prednisone and Methylprednisolone Dosepak
Prednisone (Orasone, Deltasone, generic) comes in 1, 2.5, 5, 10, 20, and 50 mg tablets as well as 5 mg /5 ml solution form. It is the most commonly prescribed form of oral steroid.
Typical daily dosage is 40 to 60 mg PO qd initially with tapering over a one to two week period. Dosages up to 60 mg can be taken at one time, and it is recommended that prednisone be taken with meals to reduce gastric distress.
In acute situations when only a short-term therapy is needed, 40 to 60mg PO qd may be taken for two days, then discontinued without taper.
Methylprednisolone should be mentioned here as an alternative steroid in the treatment of ocular conditions. It is available in 2, 4, 8, 16, 24, and 32 mg tablets generically and as the Medrol dosepak blister packages. Dosepaks have six 4 mg tablets (total 24 mg) that the patient takes on day one, with the number of tablets taken reduced by one each day over six days in a tapering schedule. Many practitioners prefer using prednisolone as opposed to the lower dosage methylprednisolone but the dosepak is a convenient way to manage the patient's tapering sequence.
Oral steroids can provide significant analgesic effect in combination with their anti-inflammatory component. However, they should not be used in place of pain medication for conditions that require only analgesia. Steroids have numerous adverse side-effects that can be potentially be life threatening, including adrenal insufficiency, Cushingoid syndrome, steroid-induced diabetes, menstrual changes, reduced immunity, delayed wound healing, and mood swings. The practitioner should consider prescribing oral steroids only if there is no safer alternative treatment, and consultation with the patients primary care provider is suggested before starting a patient on oral steroids.
For a more information on treating pain and inflammation, the reader is encouraged to visit the On-Line CE courses titled Treating Pain and Inflammation Using Oral Medications" by Michael Grover, D.O., and "The Role of Steroids in Optometric Practice" by Lorne B. Yudcovitch, O.D.
TREATMENT OF ELEVATED INTRAOCULAR PRESSURE
Most optometrists are familiar with the topical carbonic anhydrase inhibitors (CAIs) used in treating various forms of glaucoma and ocular hypertension. However, in certain cases of extreme elevated intraocular pressure (such as angle closure glaucoma), and in cases of pseudotumour cerebri from increased intracranial hypertension, oral CAIs may be useful in significantly reducing fluid pressure. CAIs inhibit the aqueous-producing enzyme carbonic anhydrase, and subsequently have a large effect on reducing pressure in extra-cellular spaces, such as the aqueous and cerebral spinal fluid. Interestingly but not surprisingly, these medications are also used for cases of cerebral edema from high-altitude mountain sickness.

Figure 18. Carbonic anhydrase inhibitors: Diamox (acetazolamide) and Neptazane (methazolamide) pills
The most common CAI is acetazolamide (trade name: Diamox, generic), which comes in 125 and 250 mg tablets, as well as a 500 mg enteric-coated Sequels form. For angle closure glaucoma, typical dosage is two 250 mg tablets PO, followed by an additional 250 mg in 3 to 4 hours if needed. The Diamox Sequels are preferred for longer duration therapy, as the tablet has a slow release due to the coating. Methazolamide (trade name: Neptazane, generic) comes in 25 and 50mg tablets, with a typical dosing of 25-50 mg PO BID.
Oral carbonic anhydrase inhibitors can reduce intraocular pressure by as much as 50%, however their chronic use is not recommended due to the potential for adverse reactions.
Like steroids, CAIs have numerous serious side-effects that the optometrist should be aware of. They are closely related to sulfonamides, so patients with sulfa allergies should not take them. They also can cause renal calculi (kidney stones), acute respiratory failure, depression, fatigue, paresthesia of the extremities, acid-base imbalances, and blood dyscrasias such as aplastic anemia. Patients who have sickle cell anemia or carry the sickle cell trait may be at risk for increased sickling of red blood cells when taking CAIs.
Although more expensive, methazolamide tends to have fewer systemic side-effects than acetazolamide, but the risks are still present.
Another class of oral medications that can reduce intraocular pressure is the hyperosmotics. These drugs create an osmotic gradient that pulls water from the vitreous into the now hyperosmotic blood, lowering eye pressure as a result. Hyperosmotics have a short duration of effect only about 60 to 90 minutes. Currently, only Osmoglyn (Glycerin 50% solution) is available. Typically, the patient drinks Osmoglyn with cracked ice over a five to ten minute period. Dosage is dependent on the patients weight.
Osmoglyn should ideally not be used with diabetics because it has a high caloric load. Ismotic (Isosorbide 1.5% solution) is not contraindicated in diabetics but this medication is not currently available.
Hyperosmotics can cause nausea and vomiting.
TREATMENT OF AGE-RELATED MACULAR DEGENERATION
The National Eye Institutes Age Related Eye Disease Study (AREDS) demonstrated that oral supplements containing antioxidants with zinc and copper (specifically, Ocuvite Preservision) caused a 25% reduction in the rate of age-related macular degeneration over a 6-year period. Specifically, this reduction was only noted in intermediate to advanced ARMD. Dosage in this study was two tablets in the morning and two tablets in the evening. Preservision formulation is 15 mg vitamin A (as beta-carotene), 500 mg vitamin C, 400 IU vitamin E, 80 mg zinc oxide, and 2 mg cupric oxide.

Figure 19. Ocuvite Preservision (Beta-carotene, C, E, zinc, copper)
Vitamin supplements containing beta-carotene (such as Ocuvite Preservision) should not be prescribed to smokers, as it may enhance the lung cancer rate in this population. Ocuvite Lutein (which does not contain beta-carotene) is a better choice here. Combining high dosages of antioxidants with other vitamin supplements is also not advised because excessive zinc levels can cause toxicity in the body.

Figure 20. Ocuvite Extra with Lutein
The effects of lutein (such as that in Ocuvite Lutein) and xeathanthin (present in chamomile teas) on macular degeneration have not been definitively qualified as yet but the results of ongoing work look promising. Many practitioners recommend these substances to their ARMD patients even though definitive proof of efficacy has yet to be developed. (For more information on the treatment of ARMD, see the On-Line CE course titled "Age-Related Macular Degeneration: Treatment Advances" by Jay M. Haynie, O.D. in this series.
CONCLUSION
Treatment of specific ocular conditions with oral medications has become more and more commonplace in optometric practice. Optometrists must continue to maintain comfort and expertise in utilizing oral medications as part of their ocular treatment regimen.
Careful evaluation and judicious management, as well as weighing the benefits versus risks of prescribing oral medications, will only serve to benefit the patient.
REFERENCES
1. Bartlett JD, Jaanus SD, eds. Clinical Ocular Pharmacology (3rd Ed). Butterworth-Heinemann, Boston, 1996.
2. Rhee J, Pyfer MF (Eds.). The Wills Eye Manual (3rd Ed). Lippincott, Williams and Wilkins, 1999.
3. Hardman JG, Limbird LE, Gilman AG, eds. Goodman & Gilman's The Pharmacological Basis of Therapeutics (10th Ed.). McGraw-Hill Publishing, New York, 2001.
4. Spalton DJ, Hitchings RA, Hunter PA. Atlas of Clinical Ophthalmology (2nd Ed.). Gower Medical, 1994.
5. Kanski JJ. Clinical Ophthalmology (3rd Ed.). Butterworth-Heinemann, Oxford, 1994.
6. Glanze WD, Anderson KN, Anderson LE (Eds.). The Mosby Medical Encyclopedia (Revised Ed.). C.V. Mosby Company, New York, 1992.
7. Williams KC. A Closer Look at Oral Meds for the O.D. Review of Optometry, October 15, 2003.
8. Melton, R and Thomas, R. 2003 Clinical Guide to Ophthalmic Drugs (Review of Optometry supplement). Bausch & Lomb, May 2003.
9. Advanced Ocular Therapeutics Didactic Course. Oregon Optometric Physicians Association. 2003.
10. ePocrates Rx version 6.11 pharmacological index. Fang E., ed. www.epocrates.com
11. Herpetic Eye Disease Study Group. Acyclovir for the prevention of recurrent herpes simplex virus eye disease. New England Journal of Medicine. July 30; 339(5), pp. 300-306, 1998.
12. Age-Related Eye Disease Study Research Group. A randomized, placebo- controlled, clinical trial of high-dose supplementation with vitamins C and E, beta-carotene, and zinc for age-related macular degeneration and vision loss. AREDS report no. 8. Archives of Ophthalmology Oct; 119(10) 2001.
Contact this author:
Lorne B. Yudcovitch, O.D., M.S., F.A.A.O. Pacific University College of Optometry 2043 College Way Forest Grove OR 97116The author has no financial interest in any of the products mentioned in this course.
Pacific University College of Optometry provides On-Line CE as a service to optometrists. The college does not endorse or recommend any products, equipment, or services that might be discussed in the courses. Courses are prepared by individuals believed to be experts in their areas of specialization who are compensated for their efforts. The College relies on their expertise to produce accurate and timely courses. Questions or concerns about courses should be directed to the individual authors and/or the Continuing Education Department at the College of Optometry at kundart@pacificu.edu .
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