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

140

Latanoprost

inflammation (iritis/uveitis); iris pigmentation changes; and

macular edema, including cystoid macular edema, which

have mainly occurred in aphakic patients, in pseudophakic

patients with a torn posterior lens capsule, or in patients with

known risk factors for macular edema. Should be used with

caution in patients who do not have an intact posterior cap-

sule or who have known risk factors for macular edema and

in patients with a history of intraocular inflammation (iritis/

uveitis); should generally not be used in patients with active

intraocular inflammation. There is limited experience in the

treatment of angle closure, inflammatory, or neovascular

glaucoma.

Controlled clinical trials: Symptoms reported in 5–15% of pati-

ents—blurred vision, burning and stinging, conjunctival hy-

peremia, foreign-body sensation, itching, increased pigmen-

tation of the iris, and punctate epithelial keratopathy. Local

conjunctival hyperemia was observed; however, less than 1%

of the patients required discontinuation of therapy because

of intolerance to conjunctival hyperemia. Symptoms repor-

ted in 1–4% of patients—dry eye, excessive tearing, eye pain,

lid crusting, lid discomfort/pain, lid edema, lid erythema,

photophobia. Symptoms reported in less than 1% of pati-

ents—conjunctivitis, diplopia, and discharge. Extremely rare

reports—retinal artery embolus, retinal detachment, vitreous

hemorrhage from diabetic retinopathy. Most common syste-

mic adverse events—URTI/cold/flu, which occurred at a rate

of approximately 4%. Chest pain/angina pectoris, muscle/

joint/back pain, and rash/allergic skin reaction each occurred

at a rate of 1–2%. Postmarketing use in clinical practice: asthma

and exacerbation of asthma; corneal edema and erosions;

dyspnea; eyelash and vellus hair changes (increased length,

thickness, pigmentation, and number); eyelid skin darke-

ning; herpes keratitis; intraocular inflammation (iritis/uveitis);

keratitis; macular edema, including cystoid macular edema;

misdirected eyelashes, sometimes resulting in eye irritation;

Pregnancy Category

toxic epidermal necrolysis.

C.

Drug Interactions

In vitro studies have shown that precipitation occurs when

eye drops containing thimerosal are mixed with Xalatan. If

such drugs are used, they should be administered at least

5 min apart.

142

Levobunolol Hydrochloride

Dose

Typical dosing with 0.25% ophthalmic solution is 1–2 drops

two times per day. In patients with more severe or uncont-

rolled glaucoma, 0.5% solution can be administered two ti-

mes per day As with any new medication, careful monitoring

of patients is advised. Dosages above 1 drop 0.5% two times

per day are not generally more effective. Patients should not

typically use two or more topical ophthalmic beta-adrener-

Contraindications

gic-blocking agents simultaneously.

In patients with bronchial asthma or history of bronchial

asthma or severe chronic obstructive pulmonary disease;

sinus bradycardia; secondand third-degree AV block; overt

cardiac failure; cardiogenic shock; hypersensitivity to the pro-

duct or any of its components. Should be used with caution

in patients with a known hypersensitivity to other beta-adre-

Warnings

noceptor-blocking agents.

As with other topically applied ophthalmic drugs, may be ab-

sorbed systemically. The same adverse reactions found with

systemic administration of beta-adrenergic-blocking agents

may occur with topical administration. For example, severe

respiratory reactions and cardiac reactions, including death

due to bronchospasm in patients with asthma and, rarely,

death in association with cardiac failure, have been reported

with topical application of beta-adrenergic-blocking agents.

Patients with history cardiac failure: Beta-adrenergic blockade

may precipitate more severe failure. Patients without history

of cardiac failure: Continued depression of the myocardium

with beta-blocking agents over a period of time can, in some

cases, lead to cardiac failure. At the first sign or symptom of

cardiac failure, discontinue therapy. Obstructive pulmonary

disease: Patients with chronic obstructive pulmonary disease

(e.g., chronic bronchitis, emphysema) of mild or moderate se-

verity, bronchospastic disease, or a history of bronchospastic

disease (other than bronchial asthma or a history of bronchial

asthma, in which Betagan is contraindicated) should, in gene-

ral, not receive beta-blockers, including Betagan. However, if

Betagan is deemed necessary in such patients, then it should

be administered cautiously since it may block bronchodilati-

on produced by endogenous and exogenous catecholamine

stimulation of beta-2 receptors. Major surgery: The necessity

or desirability of withdrawal of beta-adrenergic-blocking

agents prior to major surgery is controversial. Beta-adrener-

gic blockade impairs the ability of the heart to respond to

beta-adrenergically mediated reflex stimuli. This may aug-

ment the risk of general anesthesia in surgical procedures.

Some patients receiving beta-adrenergic-blocking agents

have been subject to protracted severe hypotension during

anesthesia. Difficulty in restarting and maintaining the heart-

beat has also been reported. For these reasons, in patients

undergoing elective surgery, gradual withdrawal of beta-

adrenergic-blocking agents may be appropriate. If necessa-

144

Levocabastine Hydrochloride

sthenia gravis, paresthesia. Skin—hypersensitivity, including

localized and generalized rash, alopecia, Stevens–Johnson

syndrome. Respiratory—bronchospasm (predominantly in

patients with preexisting bronchospastic disease), respiratory

failure, dyspnea, nasal congestion. Urogenital—impotence.

Endocrine—masked symptoms of hypoglycemia in insulin-

dependent diabetics. Special senses—signs and symptoms

of keratitis; blepharoptosis; visual disturbances, including

refractive changes (due to withdrawal of miotic therapy in

some cases); diplopia; ptosis. Other reactions associated with

the oral use of nonselective adrenergic receptor blocking

agents should be considered potential effects with ophthal-

Pregnancy Category

mic use of these agents.

C.

Drug Interactions

Although Betagan used alone has little or no effect on pu-

pil size, mydriasis resulting from concomitant therapy with

epinephrine may occur. Close observation is recommended

when a beta-blocker is administered to patients receiving ca-

techolamine-depleting drugs, such as reserpine, because of

possible additive effects and the production of hypotension

and/or marked bradycardia, which may produce vertigo, syn-

cope, or postural hypotension. Patients receiving beta-adre-

nergic-blocking agents along with either oral or i.v. calcium

antagonists should be monitored for possible AV conduction

disturbances, left ventricular failure, and hypotension. In pati-

ents with impaired cardiac function, simultaneous use should

be avoided altogether. Concomitant use of beta-adrenergic-

blocking agents with digitalis and calcium antagonists may

have additive effects on prolonging AV conduction time.

Phenothiazine-related compounds and beta-adrenergic-blo-

cking agents may have additive hypotensive effects due to

each inhibiting metabolism of the other.Risk of anaphylactic

reaction: While taking beta-blockers, patients with a history

of severe anaphylactic reaction to a variety of allergens may

be more reactive to repeated challenge, either accidental, di-

agnostic, or therapeutic. Such patients may be unresponsive

to the usual doses of epinephrine used to treat allergic reac-

tion.

Brand Name

Xylocaine.

Class of Drug

Local anesthetic.

Indications

Local anesthesia.

Dosage Form

Parenteral for injection (0.5/½%)

Dose

maximum dose 200 mg.

Maximum2.9 mg/kg body weight. Rapid onset (<2 min), last

Contraindications

for 1–1.5 h; in combination with vasoconstrictor, up to 4 h.

Most significant: Adams–Stokes syndrome, lidocaine toxicity,

severe heart block. Significant: congestive heart failure, hypo-

volemia, incomplete AV heart block, reduced hepatic blood

flow, shock, sinus bradycardia, Wolff–Parkinson–White pat-

Adverse Reactions

tern. Possibly significant: renal disease.

Allergic reactions, anaphylaxis, CNS toxicity, erythema, me-

themoglobinemia, myocardial, dysfunction, nausea, pruritus,

skin rash, sneezing, urticaria, vasodilation of blood vessels,

Drug Interactions

vomiting.

Possibly safe in pregnancy. It is not known whether this drug

or its metabolites are excreted in human milk. Relative cont-

raindication:risk of systemic toxicity possible in pediatric pa-

Pregnancy Category

tients.

B.

148

Loteprednol Etabonate

suspected hypersensitivity to the product or any of its com-

Warnings

ponents or to other corticosteroids.

Prolonged use of corticosteroids may result in glaucoma with

damage to the optic nerve, defects in visual acuity and fields

of vision, and posterior subcapsular cataract formation. Ste-

roids should be used with caution in the presence of glauco-

ma. Prolonged use of corticosteroids may suppress the host

response and thus increase the hazard of secondary ocular

infections. In those diseases causing thinning of the cornea

or sclera, perforations have been known to occur with the

use of topical steroids. In acute purulent conditions of the

eye, steroids may mask infection or enhance existing infec-

tion. Use of ocular steroids 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 her-

pes simplex requires great caution. If signs and symptoms fail

to improve after 2 days, the patient should be re-evaluated.

If this product is used for 10 days or longer, IOP should be

monitored. Fungus invasion must be considered in any per-

sistent corneal ulceration where a steroid has been used or is

Adverse Reactions

in use. Fungal cultures should be taken when appropriate.

Reactions associated with ophthalmic steroids include eleva-

ted IOP, which may be associated with optic nerve damage;

visual acuity and field defects; posterior subcapsular cataract

formation; secondary ocular infection from pathogens, in-

cluding herpes simplex; and perforation of the globe where

there is thinning of the cornea or sclera.Ocular: in clinical stu-

dies, included abnormal vision/blurring, burning on instilla-

tion, chemosis, discharge, dry eyes, epiphora, foreign-body

sensation, itching, injection, and photophobia (in 5–15%

of patients); included conjunctivitis, corneal abnormalities,

eyelid erythema, keratoconjunctivitis, ocular irritation/pain/

discomfort, papillae, and uveitis (in less than 5% of patients);

some of these events were similar to the underlying ocular di-

sease being studied. Nonocular: included headache, rhinitis,

and pharyngitis (in less than 15% of patients).

In a summation of controlled, randomized studies of individu-

als treated for 28 days or longer with loteprednol etabonate,

the incidence of significant elevation of IOP (≥10 mmHg) was

2% (15/901) among patients receiving loteprednol etabonate,

7% (11/164) among patients receiving 1% prednisolone aceta-

te, and 0.5% (3/583) among patients receiving placebo. Among

a smaller study group of patients treated with Alrex, the inci-

dence of clinically significant increases in IOP (≥10 mmHg) was

Pregnancy Category

1% (1/133) with Alrex and 1% (1/135) with placebo.

C.

Brand Name

Lotemax.

Class of Drug

Corticosteroid.