Carteolol

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title: "Carteolol" type: doc version: 1 created: 2026-02-28 author: "Wikipedia contributors" status: active scope: public tags: ["2-quinolone-ethers", "5-ht1a-antagonists", "5-ht1b-antagonists", "beta-blockers", "n-tert-butyl-phenoxypropanolamines", "ophthalmology-drugs", "peripherally-selective-drugs"] description: "Chemical compound" topic_path: "general/2-quinolone-ethers" source: "https://en.wikipedia.org/wiki/Carteolol" license: "CC BY-SA 4.0" wikipedia_page_id: 0 wikipedia_revision_id: 0

::summary Chemical compound ::

| verifiedrevid = 443507665 | IUPAC_name = (RS)-5-[3-(tert-butylamino)-2-hydroxypropoxy]-3,4-dihydroquinolin-2(1H)-one | image = Carteolol skeletal.svg | image_class = skin-invert-image | width = | chirality = Racemic mixture

| tradename = Ocupress | Drugs.com = | MedlinePlus = a601078 | DailyMedID = Carteolol | pregnancy_AU = | pregnancy_US = C | pregnancy_category = | legal_AU = | legal_UK = | legal_US = Rx-only | legal_status = Rx-only | routes_of_administration = Eye drops

| bioavailability = 85% | protein_bound = | metabolism = Liver, active with 8-hydrocarteolol | elimination_half-life = 6–8 hours | excretion = Kidney (50–70%)

| IUPHAR_ligand = 7142 | CAS_number = 51781-06-7 | ATC_prefix = C07 | ATC_suffix = AA15 | ATC_supplemental = | PubChem = 2583 | DrugBank_Ref = | DrugBank = DB00521 | ChemSpiderID_Ref = | ChemSpiderID = 2485 | UNII_Ref = | UNII = 8NF31401XG | KEGG_Ref = | KEGG = D07624 | ChEBI_Ref = | ChEBI = 3437 | ChEMBL_Ref = | ChEMBL = 839

| C=16 | H=24 | N=2 | O=3 | SMILES = O=C2Nc1cccc(OCC(O)CNC(C)(C)C)c1CC2 | StdInChI_Ref = | StdInChI = 1S/C16H24N2O3/c1-16(2,3)17-9-11(19)10-21-14-6-4-5-13-12(14)7-8-15(20)18-13/h4-6,11,17,19H,7-10H2,1-3H3,(H,18,20) | StdInChIKey_Ref = | StdInChIKey = LWAFSWPYPHEXKX-UHFFFAOYSA-N 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.

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-HT1A and 5-HT1B receptor antagonist in addition to being a beta blocker.

Pharmacokinetics

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

Chemistry

The experimental log P of carteolol is 1.1 and its predicted log P ranges from 0.99 to 2.39. It is a hydrophilic or low-lipophilicity beta blocker.

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

References

1. (2006). "Analogue-based Drug Discovery". John Wiley & Sons.
2. (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.
3. (February 2021). "Neuropsychiatric Consequences of Lipophilic Beta-Blockers". Medicina (Kaunas).
4. "Carteolol".
5. (10 June 2024). "C16H24N2O3".
6. (19 September 2006). "Carteolol: Uses, Interactions, Mechanism of Action".
7. (February 2005). "The impact of lipophilicity in drug research: a case report on beta-blockers". Mini Rev Med Chem.

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