Mikelan,Otsuka,Japan,1981
Antiadrenergic
(β-receptor).
ChEBI: Carteolol is a quinolone and a secondary alcohol. It has a role as a beta-adrenergic antagonist, an antihypertensive agent, an antiglaucoma drug, an anti-arrhythmia drug and a sympatholytic agent. It is a conjugate base of a carteolol(1+).
A mixture of 1.63 g of 5-hydroxy-3,4-dihydrocarbostyril, 2.5 g of
epibromohydrin and 2 drops of piperidine was heated at a temperature of
95°C to 100°C for a period of 4 hours with stirring. The reaction mixture was
then concentrated to dryness under reduced pressure and the residue was
recrystallized from acetone to obtain 1.2 g of 5-(2,3-epoxy)propoxy-3,4-
dihydrocarbostyril as a colorless powder having a melting point of 172°C to
173°C.
A mixture of 0.75 g of 5-(2,3-epoxy)propoxy-3,4-dihydrocarbostyril, 1.0 g of
tert-butylamine and 25 ml of ethanol was stirred at a temperature of from
50°C to 55°C for a period of 4 hours. Ethanol and unreacted tert-butylamine
were distilled off under reduced pressure and the resulting residue was
dissolved in acetone.
Cartrol (Abbott); Ocupress (Novartis).
Carteolol was implicated in allergic contact dermatitis
due to beta-blockers agents in eye-drops. It seems
that this molecule can be safely used in some patients
with hypersensitivity to other topical beta-blockers
agents.
Veterinary Drugs and Treatments
Carteolol HCl is a nonspecific beta adrenergic blocking agent and
it reduces aqueous humor production by decreasing cyclic-AMP
synthesis in the ciliary body. Carteolol is a suitable substitute for
timolol maleate or any of the other beta blocking agents although
it is rarely used in veterinary medicine. In humans, similar IOP
reducing effects have been shown for all members of this class.
Substitutes are necessary when one particular product induces
topical irritation upon application. As noted above, beta blocking
agents seem to be particularly useful in the management of primary
glaucoma in cats.
Carteolol (Cartrol) is a long-acting -blocker that is
suitable for dosing once per day. It is almost completely
absorbed and exhibits about 30% binding to plasma
proteins. Unlike many -blockers, carteolol is not extensively
metabolized. Up to
