Carteolol

Carteolol is a prescription medication used to treat glaucoma and high eye pressure.  Carteolol belongs to a group of drugs called beta-blockers. These work by decreasing the pressure in the eye. 

This medication comes as an eye drop solution. It is usually used as one drop twice a day in the affected eye. 

Common side effects of carteolol include temporary eye irritation, eye burning, and eye tearing.

Carteolol can also cause dizziness and blurred vision.  Do not drive or operate heavy machinery until you know how carteolol affects you.

Carteolol may be found in some form under the following brand names:

• Cartrol

• Ocupress

Carteolol is part of the drug class:

• Beta blocking agents, non selective

Carteolol Hydrochloride Ophthalmic Solution, USP 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:

                                                      C16H24N2O3•HCl                                       Mol. Wt. 328.84

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 range of 6.2 – 7.2.

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

Carteolol Hydrochloride Ophthalmic Solution, USP 1% reduces normal and elevated intraocular pressure (lOP) 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, Carteolol Hydrochloride Ophthalmic Solution, USP 1% produced a median percent reduction of IOP 22% to 25%. No significant effects were noted on corneal sensitivity, tear secretion, or pupil size.

Carteolol Hydrochloride Ophthalmic Solution, USP 1% has not been detected in plasma following ocular instillation. However, as with other topically applied ophthalmic preparations, Carteolol Hydrochloride Ophthalmic Solution, USP 1% 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, Carteolol Hydrochloride Ophthalmic Solution, USP 1% 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), Carteolol Hydrochloride Ophthalmic Solution, USP 1% 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.

The following adverse reactions have been reported in clinical trials with Carteolol Hydrochloride Ophthalmic Solution, USP 1%:

Ocular

Transient eye irritation, burning, tearing, conjunctival hyperemia and edema occurred in about 1 of 4 patients. Ocular symptoms including blurred and cloudy vision, photophobia, decreased night vision, and ptosis and ocular signs including blepharoconjunctivitis, abnormal corneal staining, and corneal sensitivity occurred occasionally.

Systemic

As is characteristic of nonselective adrenergic blocking agents, Carteolol Hydrochloride Ophthalmic Solution, USP 1% may cause bradycardia and decreased blood pressure (see WARNINGS). The following systemic events have occasionally been reported with the use of Carteolol Hydrochloride Ophthalmic Solution, USP 1%: cardiac arrhythmia, heart palpitation, dyspnea, asthenia, headache, dizziness, insomnia, sinusitis, and taste perversion.

The following additional adverse reactions have been reported with ophthalmic use of beta1 and beta2 (nonselective) adrenergic receptor blocking agents:

Body As a Whole:

Headache

Cardiovascular:

Arrhythmia, syncope, heart block, cerebral vascular accident, cerebral ischemia, congestive heart failure, palpitation (see WARNINGS).

Digestive:

Nausea

Psychiatric:

Depression

Skin:

Hypersensitivity, including localized and generalized rash

Respiratory:

Bronchospasm (predominantly in patients with pre-existing bronchospastic disease), respiratory failure (see WARNINGS)

Endocrine:

Masked symptoms of hypoglycemia in insulin-dependent diabetics (see WARNINGS)

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 ophthalmic use of these agents.

To report SUSPECTED ADVERSE REACTIONS, contact Bausch + Lomb, a division of Valeant Pharmaceuticals North America LLC, at 1-800-321-4576 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch.

The usual dose is one drop of Carteolol Hydrochloride Ophthalmic Solution, USP 1%, in the affected eye(s) twice a day.

If the patient’s IOP is not at a satisfactory level on this regimen, concomitant therapy with pilocarpine and other miotics, and/or epinephrine or dipivefrin, and/or systemically administered carbonic anhydrase inhibitors, such as acetazolamide, can be instituted.

Store between 15°-25°C (59°-77°F). Protect from light.

DO NOT USE IF IMPRINTED NECKBAND IS NOT INTACT.

KEEP OUT OF REACH OF CHILDREN

Revised: June 2016
Bausch + Lomb, a division of Valeant Pharmaceuticals North America LLC
Bridgewater, NJ 08807 USA

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