Ocupress

OCUPRESS- carteolol hydrochloride solution
Novartis Ophthalmics

OCUPRESS ®

(carteolol HCl ophthalmic solution)

1% STERILE

DESCRIPTION

Ocupress® (carteolol hydrochloride ophthalmic solution), 1%, is a nonselective beta-adrenoceptor blocking agent for ophthalmic use.

The chemical name for carteolol hydrochloride is (±)–5–[3–[(1,1–dimethylethyl) amino]–2 hydroxypropoxy]–3, 4–dihydro–2(1H)–quinolinone monohydrochloride. The structural formula is as follows:

Image from Drug Label Content

Each mL contains 10 mg carteolol HCl and the inactive ingredients – Benzalkonium chloride 0.05 mg (0.005%) as a preservative; sodium chloride; sodium phosphate, dibasic; sodium phosphate, monobasic; and water for injection, USP. The product has a pH of 6.2 to 7.2

CLINICAL PHARMACOLOGY

Carteolol HCl is a nonselective beta-adrenergic blocking agent with associated intrinsic sympathomimetic activity and without significant membrane-stabilizing activity.

Ocupress (carteolol HCl) reduces normal and elevated intraocular pressure (IOP) whether or not accompanied by glaucoma. The exact mechanism of the ocular hypotensive effect of beta-blockers has not been definitely demonstrated.

In general, beta-adrenergic blockers reduce cardiac output in patients in good and poor cardiovascular health. In patients with severe impairment of myocardial function, beta-blockers may inhibit the sympathetic stimulation necessary to maintain adequate cardiac function. Beta-adrenergic blockers may also increase airway resistance in the bronchi and bronchioles due to unopposed parasympathetic activity.

Given topically twice daily in controlled domestic clinical trials ranging from 1.5 to 3 months, Ocupress produced a median percent reduction of IOP 22% to 25%. No significant effects were noted on corneal sensitivity, tear secretion, or pupil size.

Ocupress Indications and Usage

Ocupress Ophthalmic Solution, 1%, has been shown to be effective in lowering intraocular pressure and may be used in patients with chronic open-angle glaucoma and intraocular hypertension. It may be used alone or in combination with other intraocular pressure lowering medications.

CONTRAINDICATIONS

Ocupress Ophthalmic Solution is contraindicated in those individuals with bronchial asthma or with a history of bronchial asthma, or severe chronic obstructive pulmonary disease (see WARNINGS); sinus bradycardia; second- and third-degree atrioventricular block; overt cardiac failure (see WARNINGS); cardiogenic shock; or hypersensitivity to any component of this product.

WARNINGS

Ocupress Ophthalmic Solution has not been detected in plasma following ocular instillation. However, as with other topically applied ophthalmic preparations, Ocupress may be absorbed 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 (see CONTRAINDICATIONS).

Cardiac Failure

Sympathetic stimulation may be essential for support of the circulation in individuals with diminished myocardial contractility, and its inhibition by beta-adrenergic receptor blockade may precipitate more severe failure.

In Patients Without a 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, Ocupress should be discontinued.

Non-allergic Bronchospasm

In patients with non-allergic bronchospasm or with a history of non-allergic bronchospasm (e.g., chronic bronchitis, emphysema), Ocupress should be administered with caution since it may block bronchodilation produced by endogenous and exogenous catecholamine stimulation of beta2 receptors.

Major Surgery

The necessity or desirability of withdrawal of beta-adrenergic blocking agents prior to major surgery is controversial. Beta-adrenergic receptor blockade impairs the ability of the heart to respond to beta-adrenergically mediated reflex stimuli. This may augment the risk of general anesthesia in surgical procedures. Some patients receiving beta-adrenergic receptor blocking agents have been subject to protracted severe hypotension during anesthesia. For these reasons, in patients undergoing elective surgery, gradual withdrawal of beta-adrenergic receptor blocking agents may be appropriate.

If necessary during surgery, the effects of beta-adrenergic blocking agents may be reversed by sufficient doses of such agonists as isoproterenol, dopamine, dobutamine or levarterenol (see OVERDOSAGE).

Diabetes Mellitus

Beta-adrenergic blocking agents should be administered with caution in patients subject to spontaneous hypoglycemia or to diabetic patients (especially those with labile diabetes) who are receiving insulin or oral hypoglycemic agents. Beta-adrenergic receptor blocking agents may mask the signs and symptoms of acute hypoglycemia.

Thyrotoxicosis

Beta-adrenergic blocking agents may mask certain clinical signs (e.g., tachycardia) of hyperthyroidism. Patients suspected of developing thyrotoxicosis should be managed carefully to avoid abrupt withdrawal of beta-adrenergic blocking agents which might precipitate a thyroid storm.

PRECAUTIONS

General

Ocupress Ophthalmic Solution should be used with caution in patients with known hypersensitivity to other beta-adrenoceptor blocking agents.

Use with caution in patients with known diminished pulmonary function.

In patients with angle-closure glaucoma, the immediate objective of treatment is to reopen the angle. This requires constricting the pupil with a miotic. Ocupress has little or no effect on the pupil. When Ocupress is used to reduce elevated intraocular pressure in angle-closure glaucoma, it should be used with a miotic and not alone.

Information to the Patient

For topical use only. To prevent contaminating the dropper tip and solution, care should be taken not to touch the eyelids or surrounding areas with the dropper tip of the bottle. Keep bottle tightly closed when not in use. Protect from light.

Risk from Anaphylactic Reaction

While taking beta-blockers, patients with a history of atopy or a history of severe anaphylactic reaction to a variety of allergens may be more reactive to repeated accidental, diagnostic, or therapeutic challenge with such allergens. Such patients may be unresponsive to the usual doses of epinephrine used to treat anaphylactic reactions.

Muscle Weakness

Beta-adrenergic blockade has been reported to potentiate muscle weakness consistent with certain myasthenic symptoms (e.g., diplopia, ptosis and generalized weakness).

Drug Interactions

Ocupress should be used with caution in patients who are receiving a beta-adrenergic blocking agent orally, because of the potential for additive effects on systemic beta-blockade.

Close observation of the patient is recommended when a beta-blocker is administered to patients receiving catecholamine-depleting drugs such as reserpine, because of possible additive effects and the production of hypotension and/or marked bradycardia, which may produce vertigo, syncope, or postural hypotension.

Carcinogenesis, Mutagenesis, Impairment of Fertility

Carteolol hydrochloride did not produce carcinogenic effects at doses up to 40 mg/kg/day in two-year oral rat and mouse studies. Tests of mutagenicity, including the Ames Test, recombinant (rec)-assay, in vivo cytogenetics and dominant lethal assay demonstrated no evidence for mutagenic potential. Fertility of male and female rats and male and female mice was unaffected by administration of carteolol hydrochloride dosages up to 150 mg/kg/day.

Pregnancy

Teratogenic Effects

Pregnancy Category C

Carteolol hydrochloride increased resorptions and decreased fetal weights in rabbits and rats at maternally toxic doses approximately 1052 and 5264 times the maximum recommended human oral dose (10 mg/70 kg/day), respectively. A dose-related increase in wavy ribs was noted in the developing rat fetus when pregnant females received daily doses of approximately 212 times the maximum recommended human oral dose. No such effects were noted in pregnant mice subjected to up to 1052 times the maximum recommended human oral dose. There are no adequate and well-controlled studies in pregnant women. Ocupress (carteolol hydrochloride) should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.

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