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

Dipivefrin Hydrochloride

75

Postmarketing experience with topical NSAIDs also suggests

that use more than 24 h prior to surgery or beyond 14 days

post surgery may increase patient risk for occurrence and se-

verity of corneal adverse events. Results from clinical studies

indicate that Voltaren has no significant effect upon ocular

pressure. However, elevations in IOP may occur following ca-

Adverse Reactions

taract surgery.

Identified during postmarketing use of topical diclofenac

sodium ophthalmic solution 0.1% in clinical practice: corneal

erosion, corneal infiltrates, corneal perforation, corneal thin-

ning, corneal ulceration, epithelial breakdown, superficial

punctate keratitis.Ocular: 15% of patients across studies ex-

perienced transient burning and stinging; up to 28% of pa-

tients in cataract surgery studies reported keratitis although

in many of these cases keratitis was initially noted prior to the

initiation of treatment; ~15% of patients undergoing cataract

surgery reported elevated IOP; ~30% of case studies under-

going incisional refractive surgery complained of lacrimation;

~5% or less of patients experienced: abnormal vision, acute

elevated IOP, blurred vision, conjunctivitis, corneal deposits,

corneal edema, corneal opacity, corneal lesions, discharge,

eyelid swelling, injection, iritis, irritation, itching, lacrimation

disorder, ocular allergy. Systemic: 3% or less of patients repor-

ted abdominal pain, asthenia, chills, dizziness, facial edema,

fever, headache, insomnia, nausea, pain, rhinitis, viral infec-

Pregnancy Category

tion, vomiting.

C.

Drug Interactions

Carcinogenesis, mutagenesis, impairment of fertility: Long-term

carcinogenicity studies in rats given Voltaren in oral doses up

to 2 mg/kg per day (approximately the human oral dose) re-

vealed no significant increases in tumor incidence. There was

a slight increase in benign rat mammary fibroadenomas in

mid-dose females (high-dose females had excessive mor-

tality), but the increase was not significant for this common

rat tumor. A 2-year carcinogenicity study conducted in mice

employing oral Voltaren up to 2 mg/kg per day did not reveal

any oncogenic potential. Did not show mutagenic potenti-

al in various mutagenicity studies, including the Ames test.

Administered to male and female rats at 4 mg/kg per day

did not affect fertility. Nonteratogenic effects: because of the

known effects of prostaglandin biosynthesis-inhibiting drugs

on the fetal cardiovascular system (closure of ductus arterio-

sus), use during late pregnancy should be avoided.

Dorzolamide Hydrochloride

77

tant administration of 0.5% timolol two times per day and

Dosage Form

2.0% dorzolamide three times per day

Topical ophthalmic solution: each milliliter contains 20 mg

Dose

dorzolamide hydrochloride and 5 mg timolol maleate.

1 drop two times per day

Contraindications

In patients with bronchial asthma, history of bronchial asth-

ma, severe chronic obstructive pulmonary disease, sinus

bradycardia, secondor third-degree AV block, overt cardiac

failure, cardiogenic shock, or hypersensitivity to the product

Warnings

or any of its components.

Contains dorzolamide, a sulfonamide; and timolol maleate, a

beta-adrenergic-blocking agent. Although administered to-

pically, it is absorbed systemically (see »Timolol Maleate« and

Adverse Reactions

»Dorzolamide«).

Approximately 5% of all patients discontinued therapy be-

cause of adverse reactions.Most frequently reported: taste per-

version (bitter, sour, or unusual taste) or ocular burning and/

or stinging (up to 30% of patients); conjunctival hyperemia,

blurred vision, superficial punctate keratitis, or eye itching

(between 5–15% of patients); abdominal pain, back pain,

blepharitis, bronchitis, cloudy vision, conjunctival discharge,

conjunctival edema, conjunctival follicles, conjunctival injec-

tion, conjunctivitis, corneal erosion, corneal staining, cortical

lens opacity, cough, dizziness, dryness of eyes, dyspepsia,

eye debris, eye discharge, eye pain, eye tearing, eyelid ede-

ma, eyelid erythema, eyelid exudate/scales, eyelid pain or

discomfort, foreign-body sensation, glaucomatous cupping,

headache, hypertension, influenza, lens nucleus coloration,

lens opacity, nausea, nuclear lens opacity, pharyngitis, post-

subcapsular cataract, sinusitis, URTI, UTI, visual field defect,

vitreous detachment (1–5% of patients).

The following occurred in clinical practice: bradycardia, cardi-

ac failure, cerebral vascular accident, chest pain, depression,

diarrhea, dry mouth, dyspnea, hypotension, iridocyclitis, my-

ocardial infarction, nasal congestion, paresthesia, photopho-

bia, respiratory failure, skin rashes, urolithiasis, and vomiting.

Other adverse reactions that have been reported with the

individual components are listed separately under »Dorzola-

Pregnancy Category

mide« and »Timolol Maleate.«

C.

Drug Interactions

CAIs: Potential for additive effect on the known systemic ef-

fects of CAIs in patients receiving an oral carbonic anhydrase

inhibitor and Cosopt; concomitant administration with oral

CAIs is not recommended. Acid-base disturbances: although

acid-base and electrolyte disturbances were not reported in

clinical trials with dorzolamide hydrochloride ophthalmic so-

Dorzolamide Hydrochloride

79

patic impairment and should therefore be used with caution

in such patients. There is a potential for an additive effect on

the known systemic effects of carbonic anhydrase inhibition

in patients receiving an oral carbonic anhydrase inhibitor and

Trusopt. Concomitant administration with oral carbonic anhy-

drase inhibitors is not recommended. Choroidal detachment

has been reported with administration of aqueous suppres-

Adverse Reactions

sant therapy (e.g., dorzolamide) after filtration procedures.

Most frequent: ocular burning, stinging, or discomfort im-

mediately following ocular administration (approximately

one-third of patients). Bitter taste following administration

(approximately one-quarter of patients). Superficial puncta-

te keratitis (10–15% of patients), and signs and symptoms of

ocular allergic reaction (approximately 10% of patients). Less

frequent: conjunctivitis and lid reactions, blurred vision, eye

redness, tearing, dryness, and photophobia (approximately

1–5% of patients). Other ocular and systemic events: include

headache, nausea, asthenia/fatigue, and, rarely, skin rashes,

urolithiasis, and iridocyclitis (reported infrequently).

The following occurred either at low incidence (<1%) during

clinical trials or have been reported during use in clinical

practice: signs and symptoms of systemic allergic reactions,

including angioedema, bronchospasm, pruritus, and urti-

caria; dizziness; paresthesia; ocular pain; transient myopia;

choroidal detachment following filtration surgery; eyelid

crusting; dyspnea; contact dermatitis; epistaxis; dry mouth;

Pregnancy Category

throat irritation.

C.

Drug Interactions

Although acid-base and electrolyte disturbances were not

reported in clinical trials, these disturbances have been re-

ported with oral carbonic anhydrase inhibitors and have, in

some instances, resulted in drug interactions (e.g., toxicity

associated with high-dose salicylate therapy). Therefore, the

potential for such drug interactions should be considered.

Brand Name

Phospholine Iodide.

Class of Drug

Parasympathomimetic, miotic. Cholinesterase inhibitor.

Indications

Glaucoma: OAG or ACG after iridectomy or where surgery

is refused or contraindicated; certain nonuveitic secondary

glaucoma, especially glaucoma following cataract surgery.

Accommodative esotropia: concomitant esotropias with a si-

Dosage Form

gnificant accommodative component.

Topical ophthalmic solution: 0.03%, 0.06%, 0.125%, 0.25%.

Dose

Glaucoma: brief trial of 0.03% two times per day before hig-

her strengths are used. Accommodative esotropia diagnosis: 1

drop of 0.125% may be instilled once per day in both eyes on

retiring for a period of 2 or 3 weeks. If the esotropia is accom-

modative, a favorable response will usually be noted, which

may begin within a few hours. Accommodative esotropia treat-

ment: Echothiophate iodide is prescribed at the lowest con-

centration and frequency, which gives satisfactory results. Af-

ter the initial period of treatment for diagnostic purposes, the

schedule may be reduced to 0.125% every other day or 0.06%

every day. These dosages can often be gradually lowered as

treatment progresses. The 0.03% strength has proven to be

effective in some cases. The maximum usually recommended

dosage is 0.125% once per day although more intensive the-

Contraindications

rapy has been used for short periods.

Active uveal inflammation; most cases of ACG due to the

possibility of increasing angle block (gonioscopy is recom-

mended prior to initiation of therapy); hypersensitivity to the

Warnings

product or any of its components.

Succinylcholine should be administered only with great

caution, if at all, prior to or during general anesthesia to

patients receiving anticholinesterase medication because

of possible respiratory or cardiovascular collapse. Caution

should be observed in treating glaucoma with echothio-

phate iodide in patients who are at the same time undergo-

ing treatment with systemic anticholinesterase medications

for myasthenia gravis because of possible adverse additive

Adverse Reactions

effects.

Although the relationship, if any, of retinal detachment to the

administration of echothiophate iodide has not been estab-

lished, retinal detachment has been reported in a few cases

during the use of echothiophate iodide in adult patients wi-

thout a previous history of this disorder. Stinging, burning,

lacrimation, lid-muscle twitching, conjunctival and ciliary

redness, and brow ache-induced myopia with visual blurring

may occur. Activation of latent iritis or uveitis may occur. Iris

cysts may form, and if treatment is continued, may enlarge

and obscure vision. This occurrence is more frequent in child-

ren. The cysts usually shrink upon discontinuance of the me-

dication and reduction in strength of the drops or frequency

Epinephrine

83

Brand Name

Emadine.

Class of Drug

Selective histamine H1 antagonist.

Indications

Allergic conjunctivitis.

Dosage Form

Topical ophthalmic solution 0.05%.

Dose

1 drop up to four times per day.

Contraindications

In patients with a known hypersensitivity to the product or

Warnings

any of its components.

Somnolence and malaise have been reported following daily

oral administration. Oral ingestion of the contents of a 15 ml

drop-tainer would be equivalent to 7.5 mg. In case of overdo-

Adverse Reactions

se, treatment is symptomatic and supportive.

In controlled clinical studies lasting for 42 days, the most fre-

quent adverse reaction was headache (11%). Less than 5%

of patients experienced the following events, of which some

were similar to the underlying disease being studied: abnor-

mal dreams, asthenia, bad taste, blurred vision, burning or

stinging, corneal infiltrates, corneal staining, dermatitis, dis-

comfort, dry eye, foreign-body sensation, hyperemia, kerati-

Pregnancy Category

tis, pruritus, rhinitis, sinusitis, and tearing.

B.

Brand Name

Epifrin.

Class of Drug

Glaucoma. Adrenergic agonist.

Indications

Primary OAG (POAG).

Dosage Form

Topical ophthalmic solution 0.5%, 1%, 2%.

Dose

1 drop once or two times per day.

Contraindications

Should not be used in patients who have had an attack of

NAG since dilation of the pupil may trigger an acute attack.

Do not use in patients who are hypersensitive the product or

Warnings

any of its components .

Use with caution in patients with hypertensive cardiovascular

disease or coronary artery disease. Contains sodium metabi-

sulfite, a sulfite that may cause allergic-type reactions inclu-

ding anaphylactic symptoms and life-threatening or less-se-

vere asthmatic episodes in certain susceptible people. Overall

prevalence of sulfite sensitivity in the general population is

unknown and probably low; sulfite sensitivity is seen more

frequently in asthmatic than in nonasthmatic people.