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Ocupress (Carteolol Hydrochloride Ophthalmic) - Description and Clinical Pharmacology

 
 



Ocupress

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(1 H)–quinolinone monohydrochloride. The structural formula is as follows:

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.

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