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Ординатура / Офтальмология / Английские материалы / Practical Ophthalmology A Manual for the Beginning Ophthalmology Residents 4th edition_Wilson_1996

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386 Appendix: Common Ocular Medications

Suggested Resources

Mauger TF, Craig EL, eds. Havener's Ocular Pharmacology. 6th ed. St Louis: Mosby-Year Book; 1994.

O'Connor Davies PH, Hopkins GA, Pearson RM. The Actions and Uses of Ophthalmic Drugs. 3rd ed. Boston: Butterworths; 1989.

Pavan-Langston D, ed. Manual of Ocular Diagnosis and Therapy. 3rd ed. Boston: Little, Brown & Co; 1991.

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Table A1 Topical Ophthalmic Antibacterial Agents

Antibiotic

Commercial Name Preparation

Aminoglycosides

Gentamicin

Tobramycin

Bacitracin

Bacitracin/polymyxin»|^

Chloramphenicol

Ciprofloxacin

Erythromycin

Neomycin/bacitracin/

polymyxin B

Neomycin/gramicidin/

polymyxin B

Ofloxacin

 

Sulfacetamide

ClJ

Tetracycline

 

Trimethoprim/

v

polymyxin B

*«*

Genoptic, Garamycin

Ointment or solution

Tobrex

Ointment or solution

AK-Tracin

Ointment

Polysporin

Ointment

Chloromycetin,

Ointment or solution

Ocu-Chlor, Chloroptic

 

Ciloxan

Solution

AK-Mycin, liotycin

Ointment

Neosporin

Ointment

.Neosporin

Drops

f

 

Ocuflox

Solution

Bleph-lO.Vasosulf,

Solution, ointment

Sulfamyd

(Sulfamyd)

Achromycin

Solution or ointment

 

Polytrim

Solution

 

Spectrum of Coverage

Enterobacteriaceae, P aeruginosa, 5 aureus.

Fortified drops may be formulated from intravenous preparations for topical use. Widely used in serious ocular infections (eg, corneal ulcers where G- organisms are implicated). Covers many G+ staphylococci but not streptococci.

More effective against streptococci and Pseudomonas than gentamicin.

G+ cocci (Staphylococcus, Streptococcus).

See action of each drug separately.

Broad-spectrum:G- bacilli (H influenza, N meningitidis), Spneumoniae, Salmonella, and anaerobes (B fragilis). Rare cases of aplastic anemia have been reported

Broad-spectrum; anaerobes usually resistant, may not be effective against some G+ cocci (streptococci).

G+ organisms, chlamydiae, mycoplasmas, some atypical mycobacteria, Hducreyi, Cjejuni, Ngonorrhoeae, Actinomyces. Particularly good in staphylococcal conjunctivitis. Bacteriostatic.

Neomycin can cause contact allergies in up to 10% of users. Neomycin has broad-spectrum activity in G+ and G- organisms.

Polymyxin: G- enteric bacteria, Paeruginosa. Inactive against G+ organisms. See above regarding neomycin.

Same as Ciloxan, but also covers Chlamydia and Bacteroides.

Sulfonamides: G+ and G- organisms but not P aeruginosa or enterococci. Bacteriostatic.

G+ organisms, enterobacteriaceae, vibrios, rickettsias. Inactive for P aeruginosa, Bacteroides, and group B streptococci.

Trimethoprim: G+ and G- organisms but not P aeruginosa or enterococci.

/

Table A2 ^t,v Mi Medications

Name of Drug Other Names

Chemical Composition How Administered

Mode of Action

Main Clinical Uses

 

 

 

 

Acyciovn

/.OVifdX

Purine analog

On itment, oral, parenteral

 

 

 

(ophthalmic ointment

 

 

 

not available in US)

^Famciclovir

Famvir

"Purine awtos

m#.

Oral

• Foscarnet

Foscavir

Pyrophosphate analog

Parenteral (IV)

.'Ganciclovir

Cytovene

Purine analog

 

Oral, parenteral (iV)

Idoxuridine

IDU, Stoxil, Herplex

Thymidine analog

 

0.1% ophthalmic drops qlh,

 

 

 

 

0.5% ointment q4h

Trifiundine

Viroptic

Thymidine analog

 

1 % solution, usually given

 

 

 

 

q2h to a maximum total

 

 

 

 

of 9 drops daily

Vidarabine

Vira-A

Purine analog

 

3% ophthalmic ointment,

 

 

 

»v.

applied q3h or 5x daily

 

 

 

for 6-10 days

 

 

 

 

Zidovudine

Retrovir

Thymidine analog

 

Oral, parenteral

Blocks viral UNA polymerase, thus selectively attacks viral replication in infected cells. Oral form (600-800 mg 5 times daily) reduces severity of skin and eye involvement. Particularly helpful in herpetic uveitis.

Same as ganciclovir.

Interferes with viral DNA polymerase and reverse transcriptase.

Interferes with viral DNA synthesis.

Inhibits thymidine incorporation into DNA.

Inhibits viral DNA synthesis.

Inhibits viral DNA synthesis.

Interferes with RNA-directed DNA polymerase.

Herpes simplex, varicellazoster, Epstein-Barr virus, cytomegalovnus (CMV)

Herpes simplex, vario zoster

CMV, HSV, EBV

CMV retinitis

Herpes simplex keratitis

Herpes simplex keratitis, some activity against varicella-zoster virus

Herpes simplex keratitis

HIV

 

 

 

 

M f

Table A3

Antifungal Agents

 

 

 

Name

 

Preparation

 

Comments

Amphotericin 13 (fungizone)

0 075 0 }% solution

 

Solution may be made in hospital pharmacy. May be extremely uncom-

 

 

 

 

fortable to the patient but is more effective than Nystatin. May be

 

 

 

 

given intravitreally for fungal endophthalmitis, although toxic to the

 

 

 

 

retina.

Clotrimazole

 

1% solution or cream

 

Ophthalmic preparation not available.

 

 

'.(i* ili

 

 

Fluconazole

(Diflucan)

Oral

 

Effective against Candida.

Ketoconazole (Nizoialj

Oral

_;

Effective against Candida, Cryptococcus, Histoplasma.

Mkonazote (MomstaU

1% intiavenous solution

Intravenous solution may be used topically.

Mil "nvcin (Natacym

5% suspension

 

Used with yeast and filamentary forms.

N\ t Hi! i (Mycostatin!

Ophthalmic ointment

not available

The dermatologic preparation (100,000 units per gram) may be used in

 

 

 

 

fungal keratitis.

Table A4 Mydriatics and Cycloplegics

Agent

How Available

Maximum Effect

Duration of

Comments

Side Effects

 

 

(Minutes)

Action

 

 

Phenylephrine

Solution

20

3 hours

Produces mydriasis but

May cause angina, increased blood

(Neo-synephrine)

 

 

 

no cycloplegia; avoid

pressure, myocardial infarction, stroke

2.5%, 10%

 

 

 

10% solution.

(mainly with 10%).

Tropicamide

Solution •

25

4-6 hours

Inadequate for cyclo-

 

(Mydriacy!) 0.5%, 1%

 

 

 

plegic refraction of

 

 

 

 

 

children.

 

Cyclopentolate

Solution

30

12-24 hours

Adequate for most cyclo-

Neurotoxicity can occur, particularly in

(Cyclogyl) 0.5%, 1%,

 

 

 

plegic refractions.

children: incoherence, visual hallucina-

2%

 

 

 

 

tion, ataxia, slurred speech, and seizures.

Homatropine 1%, 2%,

Solution

40

2-3 days

 

Side effects are rare.

5%

 

 

 

 

 

Scopolamine (Isopto

Solution

30

4-7

days

Hyoscine) 0.25%

 

 

 

 

Atropine 0.25%, 0.5%,

Ointment or.

30

1-2

weeks

1%

solution

 

 

 

CNS side effects: dizziness, disorientation.

Systemic absorption can result in flushing, fever, tachycardia, restlessness, and excited behavior.

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Table A5

Glaucoma Medications

Name of Agent

 

Concentration and Dosage

Cholinergic

agonists

 

 

Pilocaipine

 

 

0.5%-6% solution, 4% gel, also as sustained-release wafer

 

 

 

(Ocusert)

Carbachot

 

 

0.75%-3% solution, usually given qid

Echothiophate iodide

 

0.03%-0.25% solution, given once or twice daily or less

(Phoiphqfatf Iodide)

 

often

Adrenergic

Agonists

 

 

Epinephrine

(tpifrin, Glaucon)

 

0.25%, 0.5%, 1 %, and 2% solution, given bid

, Dipivefrin (Propine)

'• •

0 . 1 % solution given bid

 

. * 5 r i t . .ir

 

Apraclunidine (lopidine) '

' '

0.5% solution

Beta-Adrenergic Antagonists

 

 

Timolol maleate (Timoptic)

 

0.25% and 0.5% solution given bid

Hciaxulul (lieloptit)

 

0.5% solution given bid

Lesobuiiuiol (Beluga:

 

0.5% solution given bid

i

mm

Comments

1%-4% strengths are in widest use,instilled qid, >•. ••:•>-'-.-•••'; •'•-••. >.-••:

Used when pilocarpine is ineffective.

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Infrequently used because of its intense cholinergic effect and side effects, including salivation, nausea, vomiting, and diarrhea. Acts by indirect action as an irreversible cholinesterase inhibitor.

Nonselective adrenergic agonist.

Precursor to (pro-drug for) epinephrine. When it enters the eye, it is cleaved to the active form of the drug, theoretically giving fewer local and systemic side effects.

Relatively selective alpha-2 adrenergic agonist; indicated for shortterm adjunctive therapy in patients with inadequate control of intraocular pressure despite maximally tolerated medical therapy.

A nonselective beta blocker should be prescribed with care in patients with asthma, heart failure, and heart block. Has some corneal toxicity; also available in a once-daily-dose form (Timoptic XE).

A selective beta blocker, should reduce the risk of pulmonary side effects, particularly in patients with reactive or restrictive airway disease.

Comparable effects to timolol.

.

.

.

continued

Table A5 Glaucoma Medications (continued)

Name of Agent

Concentration and Dosage

Carbonic Anhydrase Inhibitors

 

(CAI)

 

Acetazolamicle (Diamox)

125 and 250 mg tablets, sustained-release 500 mg cap-

 

sule (sequel): tablets given bid to qid; capsules given

 

once or twice daily

Methazolamide (Neptazane)

50-100 mg given bid or tid

Dorzolainide (Trusopt)

A topical ophthalmic CAI (2% solution), given tid

HypeiOjmotiL Auents

 

iViunnilol

20% intravenous solution given 1.5-2 mg/kg intra-

 

venously

G^tenn (Gl\ IOI, Usmoglyity

50% solution usually given orally with water, orange

 

juice, or flavored normal saline solution over ice,

 

1-1.5 g/kg

Comments

May also be given intravenously in 500 mg ampules.

10% incidence of allergy.

Maximum ocular hypotensive effect occurs at 1 hour and lasts 5-6 hours.

Maximum ocular hypotensive effect occurs in 1 hour and lasts 4-5 hours. Can occasionally produce nausea, vomiting, and headache.

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