Hosta

Carteolol is a non-selective beta blocker used to treat glaucoma. It is administered in the form of eye drops.^{[citation needed]}

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.^[2] It is selective for the β₁-adrenergic receptor and has intrinsic sympathomimetic activity.^[2] 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.^[3]

Pharmacokinetics

Carteolol is classified as a beta blocker with low lipophilicity and hence lower potential for crossing the blood–brain barrier.^[2] This in turn may result in fewer effects in the central nervous system as well as a lower risk of neuropsychiatric side effects.^[2]

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.

References

^ Fischer J, Ganellin CR (2006). Analogue-based Drug Discovery. John Wiley & Sons. p. 460. ISBN 978-3-527-60749-5.
^ ^a ^b ^c ^d Cojocariu SA, Maștaleru A, Sascău RA, Stătescu C, Mitu F, Leon-Constantin MM (February 2021). "Neuropsychiatric Consequences of Lipophilic Beta-Blockers". Medicina (Kaunas). 57 (2): 155. doi:10.3390/medicina57020155. PMC 7914867. PMID 33572109.
^ Langlois M, Brémont B, Rousselle D, Gaudy F (January 1993). "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. doi:10.1016/0922-4106(93)90061-d. PMID 8093601.

El-Kamel A, Al-Dosari H, Al-Jenoobi F (2006). "Environmentally responsive ophthalmic gel formulation of carteolol hydrochloride". Drug Delivery. 13 (1): 55–59. doi:10.1080/10717540500309073. PMID 16401594. S2CID 30222292.
Kuwahara K, Oizumi N, Fujisawa S, Tanito M, Ohira A (March 2005). "Carteolol hydrochloride protects human corneal epithelial cells from UVB-induced damage in vitro". Cornea. 24 (2): 213–220. doi:10.1097/01.ico.0000141232.41343.9d. PMID 15725891. S2CID 20523541.
Trinquand C, Romanet JP, Nordmann JP, Allaire C (February 2003). "[Efficacy and safety of long-acting carteolol 1% once daily. A double-masked, randomized study]". Journal Français d'Ophtalmologie. 26 (2): 131–136. PMID 12660585.

[1] Fischer J, Ganellin CR (2006). Analogue-based Drug Discovery. John Wiley & Sons. p. 460. ISBN 978-3-527-60749-5.

[pmid33572109-2] Cojocariu SA, Maștaleru A, Sascău RA, Stătescu C, Mitu F, Leon-Constantin MM (February 2021). "Neuropsychiatric Consequences of Lipophilic Beta-Blockers". Medicina (Kaunas). 57 (2): 155. doi:10.3390/medicina57020155. PMC 7914867. PMID 33572109.

[pmid8093601-3] Langlois M, Brémont B, Rousselle D, Gaudy F (January 1993). "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. doi:10.1016/0922-4106(93)90061-d. PMID 8093601.

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