Products
Carteolol is available in the form of extended-release eye drops (Arteoptic LA). Carteolol has been approved in many countries since 1984. Arteopilo, the combination with pilocarpine, is no longer marketed in many countries.
Structure and properties
Carteolol (C16H24N2O3, Mr = 292.4 g/mol) is a dihydroquinolinone and a racemate. It is present in drugs as carteolol hydrochloride, white crystals or a white crystalline powder soluble in water.
Effects
Carteolol (ATC S01ED05) lowers intraocular pressure presumably by reducing the secretion of aqueous humor. However, the exact mechanism of action is unknown. Carteolol is a hydrophilic and nonselective beta-blocker with intrinsic sympathomimetic activity. As such, it has the potential to, among other things, constrict the bronchi and lower pulse rate and blood pressure. Carteolol is hardly locally anesthetic like other agents.
Indications
Carteolol is approved for the treatment of elevated intraocular pressure and for the treatment of glaucoma.
Dosage
According to the drug label. LA long-acting eye drops need only be administered once daily in the morning. See also under Administering eye drops.
Contraindications
- Hypersensitivity
- Certain respiratory diseases (eg asthma).
- Cardiovascular diseases
- Untreated pheochromocytoma
For complete precautions, see the drug label.
Interactions
Interactions that are possible with orally administered beta-blockers cannot be completely ruled out even when administered to the eye because the drug can be absorbed into the bloodstream. Carteolol can potentially potentiate the effects of oral beta-blockers. It is metabolized by CYP2D6.
Adverse effects
Possible adverse effects include local reactions to the eye such as irritation, dry eyes, and transient visual disturbances. Systemic beta-blocker adverse reactions may also occur. These include headache, dizziness, fatigue, low pulse, low blood pressure, cardiac rhythm disturbances, difficulty breathing, and bronchospasm.