Ординатура / Офтальмология / Английские материалы / Drugs in Ophthalmlogy_Fong, Law, Schmidt-Erfurth_2006

Fluorescein Sodium

97

debilitated patients, hepatic dysfunction, jaundice, ulcerative

colitis, bilirubin elevation. Genitourinary: azotemia, creatini-

ne and BUN elevation, crystalluria, renal failure. Hematolo-

gic: anemia, agranulocytosis, aplastic anemia, eosinophilia,

leukopenia, pancytopenia, thrombocytopenia. Neurologic:

ataxia, hearing loss, headache, paresthesia, Parkinsonism, pe-

ripheral neuropathy, pyrexia, vertigo, sedation, convulsions.

Psychiatric: confusion, hallucinations, psychosis. Miscellane-

ous: fatigue, hypoglycemia, hypokalemia, weakness, allergic

Pregnancy Category

reactions, Lyell‘s syndrome.

C.

Drug Interactions

Cytosine arabinoside, a cytostatic agent, has been reported

to inactivate antifungal activity by competitive inhibition.

Drugs that impair glomerular filtration may prolong the bio-

logical half-life of flucytosine. Antifungal synergism between

Ancobon and polyene antibiotics, particularly amphotericin

B, has been reported.Drug/laboratory test interactions: measu-

rement of serum creatinine levels should be determined by

the Jaffe method since Ancobon does not interfere with the

determination of creatinine values by this method, as it does

when the dry-slide enzymatic method with the Kodak Ekta-

chem analyzer is used.

Brand Name

Fluorescite Injection.

Class of Drug

Diagnostic aid.

Indications

Diagnostic fluorescein angiography or angioscopy of the fun-

Dosage Form

dus and iris vasculature.

Ampule: 10% in 5-ml ampule, 25% in 2-ml ampule.

Dose

Parenteral drug products should be inspected visually for

particulate matter and discoloration prior to administration

whenever solution and container permit. Do not mix or dilute

with other solutions or drugs. A syringe filled with fluorescein

is attached to transparent tubing and a 25-gauge scalp-vein

needle for injection. Insert the needle and draw the patient‘s

blood to the hub of the syringe so that a small air bubble se-

parates the patient‘s blood in the tubing from the fluorescein.

With the room lights on, slowly inject the blood back into the

vein while watching the skin over the needle tip. If the needle

has extravasated, the patient‘s blood will be seen to bulge

the skin, and the injection should be stopped before any

fluorescein is injected. When assured that extravasation has

not occurred, the room light may be turned off and the flu-

orescein injection completed. Luminescence appears in the

Fluorescein Sodium and Benoxinate HCl

99

Indications

For staining the anterior segment of the eye when: (a) deline-

ating a corneal injury, herpetic lesion, or foreign body; (b) de-

termining the site of an intraocular injury; (c) fitting contact

lenses; (d) testing to ascertain postoperative closure of the

sclerocorneal wound in delayed anterior chamber reformati-

Dosage Form

on; (e) testing lacrimal drainage.

Fluorescein sodium 1 mg, 9 mg per strip.

Dose

Gently touch the strip to the inferior fornix.

Warnings

Never use while the patient is wearing soft contact lenses be-

cause the lenses may become stained. Whenever fluorescein

is used, flush the eyes with sterile, normal saline solution, and

wait at least 1 h before replacing the lenses.

Brand Name

Fluress; Flurox; Flurate.

Class of Drug

Diagnostic aid, topical anesthetic.

Indications

For procedures in which a topical ophthalmic anesthetic

agent in conjunction with a disclosing agent are indicated:

corneal anesthesia of short duration, e.g., tonometry, goni-

oscopy, removal of corneal foreign bodies, and short corneal

Dosage Form

and conjunctival procedures.

Fluorescein sodium 0.25% and benoxinate HCl 0.4%.

Dose

Usual dosage (removal of foreign bodies and sutures, and for

tonometry): 1–2 drops (in single installations) in each eye be-

fore operating. Deep ophthalmic anesthesia: 2 drops in eye(s)

Contraindications

at 90-s intervals for three instillations.

In patients with known hypersensitivity to the product or any

Warnings

of its components.

Prolonged use of a topical ocular anesthetic is not recom-

mended. It may produce permanent corneal opacification

Adverse Reactions

with accompanying visual loss.

Occasional: temporary stinging, burning, conjunctival red-

ness. Rare: severe, immediate-type, apparently hyperallergic

corneal reaction with acute, intense, and diffuse epithelial

keratitis, a gray, ground-glass appearance, sloughing or large

areas of necrotic epithelium, corneal filaments, and someti-

Pregnancy Category

mes, iritis with descemetitis.

C.

Fluorometholone

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Keratitis, conjunctivitis, corneal ulcers, mydriasis, conjunctival

hyperemia, loss of accommodation, and ptosis have occasi-

onally been reported following local use of corticosteroids.

Development of secondary ocular infection (bacterial, fungal,

viral) has occurred. Fungal and viral infections of the cornea

are particularly prone to develop coincidentally with long-

term applications of steroids. The possibility of fungal invasi-

on should be considered in any persistent corneal ulceration

where steroid treatment has been used. Use of ocular stero-

ids may prolong the course and may exacerbate the severity

of many viral infections of the eye (including herpes simplex).

Employment of corticosteroid medication in the treatment of

patients with a history of herpes simplex requires great cauti-

on; frequent slit lamp microscopy is recommended. Corticos-

teroids are not effective in mustard gas keratitis and Sjögren‘s

Pregnancy Category

keratoconjunctivitis.

C.

Brand Name

FML-S.

Class of Drug

Topical steroid antibiotic.

Indications

For steroid-responsive inflammatory ocular conditions for

which a corticosteroid is indicated and where superficial

bacterial ocular infection or a risk of bacterial ocular infection

exists. The use of a combination drug with an anti-infective

component is indicated where the risk of superficial ocular

infection is high or where there is an expectation that potenti-

ally dangerous numbers of bacteria will be present in the eye.

The anti-infective drug in this product, sulfacetamide, is acti-

ve against the following common bacterial eye pathogens:E.

coli, S. aureus, S. pneumoniae, Streptococcus (viridans group), H.

influenzae, Klebsiella spp., and Enterobacter spp. The product

does not provide adequate coverage against Neisseria spp.

and S. marcescens. A significant percentage of staphylococcal

Dosage Form

isolates are completely resistant to sulfa drugs.

Ophthalmic suspension: fluorometholone 0.1% and sulfacet-

Dose

amide sodium 10%.

1 drop into the conjunctival sac four times per day. If signs

and symptoms fail to improve after 2 days, the patient should

be re-evaluated. Dosing may be reduced, but care should

be taken not to discontinue therapy prematurely. In chronic

conditions, withdrawal of treatment should be carried out by

Contraindications

gradually decreasing the frequency of applications.

In most viral diseases of the cornea and conjunctiva, inclu-

ding epithelial herpes simplex keratitis (dendritic keratitis),

vaccinia, and varicella; mycobacterial infection of the eye;

fungal diseases of ocular structures; in patients with a known

or suspected hypersensitivity to the product or any of its

Warnings

components, sulfonamides, or other corticosteroids.

See »FML; Fluor-Op; Eflone; Flarex; FML Forte; FML S.O.P.« Fa-

talities have occurred, although rarely, due to severe reactions

5-Fluorouracil (5-FU)

103

Contraindications

As cancer chemotherapy: Injection therapy for patients in

poor nutritional state, those with depressed bone marrow

function, those with potentially serious infections, or in pa-

tients with a known hypersensitivity to the product or any of

Warnings

its components.

As cancer chemotherapy: daily dose of injection not to ex-

ceed 80 mg. It is recommended that patients be hospitalized

during their first course of treatment. Should be used with

extreme caution in poor-risk patients with a history of high-

dose pelvic irradiation or previous use of alkylating agents,

those who have a widespread involvement of bone marrow

by metastatic tumors, or those with impaired hepatic or renal

function. Rarely, unexpected, severe toxicity (e.g., stomatitis,

diarrhea, neutropenia, neurotoxicity) associated has been at-

tributed to deficiency of dipyrimidine dehydrogenase activi-

Adverse Reactions

ty.

As cancer chemotherapy: Patients should be informed of ex-

pected toxic effects, particularly oral manifestations; alerted

to the possibility of alopecia as a result of therapy; and infor-

med that it is usually a transient effect. A highly toxic drug

with a narrow margin of safety. Sever hematological toxicity,

gastrointestinal hemorrhage, and even death may result, de-

spite meticulous selection of patients and careful adjustment

of dosage. Therapy is to be discontinued promptly whenever

one of the following signs of toxicity appears: stomatitis or

esophagopharyngitis, leukopenia, or rapid falling WBC, in-

tractable vomiting, diarrhea, gastrointestinal ulceration and

bleeding, thrombocytopenia, and hemorrhage from any site.

Off-label: as an adjuvant in glaucoma surgery: bleb leakage,

hypotony, flat anterior chamber, blebitis, endophthalmitis,

ocular inflammation, uveitis, epithelial defect, ocular discom-

fort, decrease of vision; late bleb leak or endophthalmitis may

Pregnancy Category

be associated with use for glaucoma surgery.

D.

Drug Interactions

May cause fetal harm when administered to a pregnant wo-

man. Women of childbearing potential should be advised to

avoid becoming pregnant while taking the drug and should

be told of potential hazard to the fetus. Should be used du-

ring pregnancy only if the potential benefit justifies the po-

tential risk to the fetus. Leucovorin calcium may enhance

toxicity.

Fomivirsen Sodium

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Dosage Form

Single-use vials contain 0.25 ml, 6.6 mg/ml.

Dose

Treatment involves an induction and a maintenance phase.

Recommended dose is 330 µg (0.05 ml).Induction dose: one

injection every other week for two doses. Subsequent main-

tenance doses: once every 4 weeks after induction. For unac-

ceptable inflammation in the face of controlled CMVR, it is

worthwhile interrupting therapy until the level of inflammati-

on decreases and therapy can resume. For patients whose di-

sease progresses during maintenance, an attempt at reinduc-

tion at the same dose may result in resumed disease control.

Instructions for intravitreal injection: administer 0.05 ml/eye

to affected eye(s) following application of standard topical

and/or local anesthetics and antimicrobials using a 30-gauge

Contraindications

needle on a low-volume (e.g., tuberculin) syringe.

In patients who have known hypersensitivity to the product

Warnings

or any of its components.

For intravitreal injection use only. CMVR may be associated

with CMV disease elsewhere in the body. Provides localized

therapy limited to the treated eye; does not provide treat-

ment for systemic CMV disease. Patients should be monito-

red for extraocular CMV disease or disease in the contralateral

eye. Not recommended for use in patients who have recently

(2–4 weeks) been treated with either i.v. or intravitreal cidofo-

Adverse Reactions

vir because of risk of exaggerated ocular inflammation.

Most frequent: Ocular inflammation (uveitis), including iritis

and vitreitis, has been reported to occur in approximately

one in four patients. Inflammatory reactions are more com-

mon during induction dosing. Delaying additional treatment

and the use of topical corticosteroids have been useful in

the medical management of inflammatory changes, and

with both medical management and time, patients may be

able to continue to receive intravitreal injections after the

inflammation has resolved. Increased IOP has been common-

ly reported; the increase is usually a transient event and in

most cases, pressure returns to the normal range without

any treatment or with temporary use of topical medications.

IOP should be monitored at each visit, and elevations of IOP,

if sustained, should be managed with medications to lower

IOP. Reported by 5–20% of patients: Ocular—abnormal vision,

anterior chamber inflammation, blurred vision, cataract, con-

junctival hemorrhage, decreased visual acuity, desaturation

of color vision, eye pain, floaters, increased IOP, photophobia,

retinal detachment, retinal edema, retinal hemorrhage, reti-

nal pigment changes, uveitis, vitreitis. Systemic—abdominal

pain, anemia, asthenia, diarrhea, fever, headache, infection,

nausea, pneumonia, rash, sepsis, sinusitis, systemic CMV,

vomiting. Reported by 2–5% of patients: Ocular—application-

site reaction, conjunctival hyperemia, conjunctivitis, corneal

edema, decreased peripheral vision, eye irritation, hypotony,

keratic precipitates, optic neuritis, photopsia, retinal vascu-