Carteolol
Anton C. de Groot in 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).
Medical Therapy for Glaucoma
Neil T. Choplin, Carlo E. Traverso in Atlas of Glaucoma, 2014
Carteolol (Ocupress; no longer available as a branded product) 1.0% solution is comparable in efficacy to 0.5% timolol maleate. Carteolol possesses a quality known as intrinsic sympathomimetic activity (ISA). Carteolol, while acting as a β-adrenergic competitive antagonist, also causes mild stimulation of the β-receptors. Thus, it may have less of an effect on the cardiovascular and respiratory systems. Although studies have shown that carteolol causes a smaller reduction of serum high-density lipoprotein-cholesterol (HDL-C) compared to timolol, topical β-adrenoreceptor antagonist therapy has not been associated with an increased risk of myocardial infarction despite the association of reduced serum HDL-C with an increased risk of myocardial infarction.
Application of Bioresponsive Polymers in Drug Delivery
Deepa H. Patel in Bioresponsive Polymers, 2020
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].
Formulation of carteolol chitosomes for ocular delivery: formulation optimization, ex-vivo permeation, and ocular toxicity examination
Published in Cutaneous and Ocular Toxicology, 2021
Ameeduzzafar Zafar, Nabil K. Alruwaili, Syed Sarim Imam, Omar Awad Alsaidan, Khalid Saad Alharbi, Mohd Yasir, Mohammed Elmowafy, Mohammad Javed Ansari, Mohammed Salahuddin, Sultan Alshehri
Carteolol (CT) is the second most commonly used non-selective β-blocker for the treatment of open-angle glaucoma13. It exhibits intrinsic sympathomimetic activity and effectively reduces intraocular pressure, ocular hypertension, and decreases the production of aqueous humour from the ciliary body. It is well tolerated and offers no cardiovascular and respiratory side effects in healthy volunteers8. After topical administration, it reaches the systemic circulation from the precorneal area through the nasolacrimal duct. Due to this reason, the ocular bioavailability of the CTL solution is very low (1% or less)1. So, the study was aimed to formulate, optimise and evaluate the CT-loaded noisome coated with CH. The formulations were characterised for various in-vitro parameters including drug release, bioadhesion, ex-vivo permeation study, histopathological evaluation, toxicity, and stability study.
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].
Related Knowledge Centers
- Beta Blocker
- Glaucoma
- Receptor Antagonist
- Serotonin
- Eye Drop
- Adrenergic Receptor
- Binding Selectivity
- 5-Ht1A Receptor
- 5-Ht1B Receptor
- Blood–Brain Barrier