Carteolol Explained

Carteolol is a non-selective beta blocker used to treat glaucoma. It is administered in the form of eye drops.

Carteolol was patented in 1972 and approved for medical use in 1980.^[1]

Pharmacology

Pharmacodynamics

Carteolol is a beta blocker, or an antagonist of the β-adrenergic receptors. It is selective for the β₁-adrenergic receptor and has intrinsic sympathomimetic activity. Carteolol has also been found to act as a serotonin 5-HT_1A and 5-HT_1B receptor antagonist in addition to being a beta blocker.^[2]

Pharmacokinetics

Carteolol is classified as a beta blocker with low lipophilicity and hence lower potential for crossing the blood–brain barrier.^[3] This in turn may result in fewer effects in the central nervous system as well as a lower risk of neuropsychiatric side effects.

Society and culture

Brand names

Brand names of carteolol include Arteolol, Arteoptic, Calte, Cartéabak, Carteol, Cartéol, Cartrol, Elebloc, Endak, Glauteolol, Mikelan, Ocupress, Poenglaucol, Singlauc, and Teoptic.

Further reading

• El-Kamel A, Al-Dosari H, Al-Jenoobi F . Environmentally responsive ophthalmic gel formulation of carteolol hydrochloride . Drug Delivery . 13 . 1 . 55–59 . 2006 . 16401594 . 10.1080/10717540500309073 . 30222292 . free .
• Kuwahara K, Oizumi N, Fujisawa S, Tanito M, Ohira A . Carteolol hydrochloride protects human corneal epithelial cells from UVB-induced damage in vitro . Cornea . 24 . 2 . 213–220 . March 2005 . 15725891 . 10.1097/01.ico.0000141232.41343.9d . 20523541 .
• Trinquand C, Romanet JP, Nordmann JP, Allaire C . [Efficacy and safety of long-acting carteolol 1% once daily. A double-masked, randomized study] . Journal Français d'Ophtalmologie . 26 . 2 . 131–136 . February 2003 . 12660585 .

Notes and References

1. Book: Fischer J, Ganellin CR . Analogue-based Drug Discovery . 2006 . John Wiley & Sons . 978-3-527-60749-5 . 460 . en.
2. Langlois M, Brémont B, Rousselle D, Gaudy F . Structural analysis by the comparative molecular field analysis method of the affinity of beta-adrenoreceptor blocking agents for 5-HT1A and 5-HT1B receptors . European Journal of Pharmacology . 244 . 1 . 77–87 . January 1993 . 8093601 . 10.1016/0922-4106(93)90061-d .
3. Cojocariu SA, Maștaleru A, Sascău RA, Stătescu C, Mitu F, Leon-Constantin MM . Neuropsychiatric Consequences of Lipophilic Beta-Blockers . Medicina (Kaunas) . 57 . 2 . February 2021 . 155 . 33572109 . 7914867 . 10.3390/medicina57020155 . free .