Monograph: |
Carteolol Hydrochloride
Adverse Effects, Treatment, and Precautions
As for Beta Blockers See Betaxolol.
Interactions
The interactions associated with beta blockers are discussed on Betaxolol.
Pharmacokinetics
Carteolol is well absorbed from the gastrointestinal tract with a peak plasma concentration being reached within 1 to 3 hours of oral doses. The bioavailability is about 85%. It has low lipid solubility. About 20 to 30% is protein bound. The plasma half-life is reported to be 5 to 6 hours. The major route of elimination is renal with 50 to 70% of a dose being excreted unchanged in the urine; carteolol therefore accumulates in patients with renal disease. Major metabolites are 8-hydroxycarteolol and glucuronic acid conjugates of carteolol and 8-hydroxycarteolol. The 8-hydroxycarteolol metabolite is active; its half-life is reported to be 8 to 12 hours.
Uses and Administration
Carteolol is a non-cardioselective beta blocker .It is reported to possess intrinsic sympathomimetic activity but lacks significant membrane-stabilising activity.
Carteolol is used as the hydrochloride in the management of glaucoma , hypertension, and some cardiac disorders such as angina pectoris and cardiac arrhythmias.
Eye drops containing carteolol hydrochloride 1% or 2% are instilled twice daily to reduce raised intra-ocular pressure in open-angle glaucoma and ocular hypertension.
In hypertension carteolol hydrochloride is given in initial doses of 2.5 mg once daily by mouth, increased, if necessary according to response, to 10 mg once daily; higher doses have also been used. In cardiac disorders such as angina pectoris and arrhythmias carteolol hydrochloride has been used in doses of up to 30 mg daily.
The oral dose of carteolol hydrochloride should be reduced in patients with renal impairment .
Administration in renal impairment.
The oral dose of carteolol should be reduced in patients with renal impairment. A suggested regimen for patients with hypertension is to increase the dosage interval from 24 to 48 hours in patients with a creatinine clearance of 20 to 60 mL/minute and to 72 hours in patients with a creatinine clearance of less than 20 mL/minute.
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