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Carteolol
Published in Anton C. de Groot, Monographs in Contact Allergy, 2021
Carteolol is a synthetic quinolinone derivative and nonselective β-adrenoceptor blocking agent with anti-glaucoma activity. Upon topical administration to the eye, carteolol decreases aqueous humor production, thereby reducing both elevated and normal intraocular pressure. It is indicated for the treatment of intraocular hypertension and chronic open-angle glaucoma. According to some sources, carteolol may also be used as an anti-arrhythmia, anti- angina and antihypertensive agent. In pharmaceutical products (mostly eye drops), carteolol is employed as carteolol hydrochloride (CAS number 51781-21-6, EC number 257-415-7, molecular formula C16H25ClN2O3) (1).
Application of Bioresponsive Polymers in Drug Delivery
Published in Deepa H. Patel, Bioresponsive Polymers, 2020
Manisha Lalan, Deepti Jani, Pratiksha Trivedi, Deepa H. Patel
Mourice and Srinivas reported use of gellan gum for permeation enhancement of the fluorescein in humans as compared to isotonic buffer solution. The ability of gelation at physiological Ca2+ levels was used. The selected polymer significantly increased the duration of pilocarpine action to 10-h and carteolol to 8-h, reducing frequency of drug administration in case of carteolol [111].
Adrenergic Antagonists
Published in Sahab Uddin, Rashid Mamunur, Advances in Neuropharmacology, 2020
Carteolol is a β receptor non-selective antagonist and has intrinsic sympathomimetic activity (Janczewski et al., 1988; Mayama et al., 2013; Veld et al., 1982). Carteolol produces a vasodilating effect, which is higher when compared to β-blockers without ISA such as timolol. The actual mechanism of ISA within the body is not much understood.
Beta-blocker carteolol and oxprenolol produce cutaneous analgesia in response to needle pinpricks in the rat
Published in Neurological Research, 2023
There are limitations to this study. Firstly, in an equipotent basis (ED25, ED50, and, ED75), the duration of blockade induced by carteolol was longer than that induced by oxprenolol or bupivacaine, but it does not appear to be a consistent relationship between the beta-blocker potency and total recovery time. Secondly, prolonged vasoconstriction can cause ischemic damage and this should be considered. Thirdly, Beta-adrenergic receptor antagonists rapidly reach the central nervous system and therefore some of the observed effects may also occur systemically (eg. acting centrally) rather than locally [35,36]. To prevent the central effect of drugs, the 6 stings were performed in the demarcated area immediately after the CTMPs were evoked outside the wheal. Lastly, we did not estimate whether beta-blockers induced neurotoxicity or systemic toxicity. Beta-blockers as FDA-approved drugs were used to treat congestive heart failure and tachycardia [1]. Over the past 10 years, there have been increasing reports of topical beta-blockers for various skin diseases [31]. However, the toxicities should be examined before the use of Beta-blockers as an infiltrative anesthetic.
Adrenergic agonists and antagonists as antiglaucoma agents: a literature and patent review (2013–2019)
Published in Expert Opinion on Therapeutic Patents, 2019
Alessio Nocentini, Claudiu T. Supuran
Carteolol is a nonselective β-blocker with some ISA and no local anesthetic activity [33] Aqueous humor formation was reduced by 20.4% with carteolol. Carteolol is available in 1 and 2% solutions (Ocupress®, Teoptic®) and has to be applied twice daily. In randomized comparative studies, carteolol 1 and 2% were as effective as timolol 0.5% in lowering IOP [33]. Ocular adverse effects, such as irritation and pain occurring shortly after application, were observed less often during carteolol treatment than with timolol. Carteolol reportedly possesses ISA but shows β-blocking effects on pulse rate, blood pressure, and exercise-induced dyspnea. Plasma high density lipoprotein (HDL) cholesterol levels are increased and plasma triglyceride levels are reduced after carteolol administration [34]. This effect has been ascribed to the ISA properties of carteolol.
Fixed-combination topical anti-hypertensive ophthalmic agents
Published in Expert Opinion on Pharmacotherapy, 2020
Lindsay Machen, Reza Razeghinejad, Jonathan S. Myers
Carteolol hydrochloride 2% is a nonselective beta-adrenergic receptor antagonist [88]. Unlike other beta-blockers, carteolol has intrinsic sympathomimetic activity, which is postulated to reduce systemic cardiovascular side effects while retaining effective IOP lowering [88]. Carteolol has been reported to have a less deleterious effect on lipid profiles than timolol [89]. Fixed-combination latanoprost 0.005%-carteolol 2% (FCLC, Mikeluna®, Otsuka Pharmaceutical Co, Ltd., Tokyo, Japan) is a solution with an approximate pH of 6.0–6.7 [88]. Unlike other fixed-combination agents, FCLC does not contain BAK and is instead preserved with boric acid and disodium edetate [90].