Source: Medicines & Healthcare Products Regulatory Agency (GB) Revision Year: 2015 Publisher: Laboratories Thea, 12 Rue Louis Blériot, 63017, Clermont-Ferrand Cedex 2, France
Pharmacotherapeutic group: Antiglaucoma preparations and miotics, beta blocking agents
ATC code: S0lED05
Carteolol is a non-selective beta-adrenergic blocking agent with associated intrinsic sympathomimetic activity (ISA) and without significant membrane stabilizing activity. It has been shown that beta blocking agents with ISA affect cardiac output, heart rate at rest, peripheral vascular resistance and consequently peripheral circulation less than beta blocking agents without ISA.
Carteolol reduces normal and elevated intraocular pressure whether or not accompanied by glaucoma. The exact mechanism of the ocular hypotensive effect of beta-blockers has not been definitely demonstrated. However, it appears that ophthalmic beta-adrenergic blocking agents mainly act by reducing aqueous humor production.
Given topically twice daily in controlled clinical trials, carteolol eye drops effectively reduced IOP in patients with glaucoma or ocular hypertension. No significant effects were noted on corneal sensitivity in healthy subjects or tear secretion or pupil size.
Administration of carteolol to the eyes of animals and healthy individuals has shown that carteolol increases the iris tissue blood velocity in the treated eye of rabbits and may increase tissue blood flow in the human optic nerve head.
Whereas topical nonselective beta-adrenergic blockers decrease serum HDL and worsen the total cholesterol/HDL ratio, beta-blockers with intrinsic sympathomimetic activity appear to have a lesser effect.
A single ocular instillation of 14C-labelled carteolol hydrochloride 2% solution into rabbit eyes demonstrated that carteolol penetrates the cornea quickly. The highest concentration levels were found in the cornea, iris, anterior sclera, ciliary body and conjunctiva 30 to 60 minutes after dosing but declined rapidly to 5 to 10% of the maximum level after 8 hours.
CYP2D6 mediated 8-hydroxylation is the only cytochrome P450 catalyzed metabolic reaction of carteolol. Carteolol has neither stimulatory nor inhibitory effects on CYP1A2, 2C9, 2C19, 2E1, and 3A4 activities. 8- Hydroxycarteolol was estimated to be more potent than carteolol in lowering IOP both in rabbits and in monkey. No data is available on metabolism after ocular application of carteolol in humans.
One drop of a 2% carteolol hydrochloride solution was instilled in each eye of healthy volunteers. Approximately 16% of the dose was excreted in the urine as unchanged compound during the first 24 hours after instillation. The urinary elimination half-life was about 5 hours. The plasma level of carteolol hydrochloride after topical administration in the eye was below the detection limit (5ng/mL).
Preclinical data reveal no special hazard for humans based on conventional studies of acute and repeated dose toxicity, genotoxicity, carcinogenic potential, and toxicity to reproduction.
© All content on this website, including data entry, data processing, decision support tools, "RxReasoner" logo and graphics, is the intellectual property of RxReasoner and is protected by copyright laws. Unauthorized reproduction or distribution of any part of this content without explicit written permission from RxReasoner is strictly prohibited. Any third-party content used on this site is acknowledged and utilized under fair use principles.
