Carteolol HydrochloridePronouncation: (CAR-tee-oh-lahl HIGH-droe-KLOR-ide) Class: Beta-adrenergic blocking agent Trade Names: Cartrol - Tablets 2.5 mg - Tablets 5 mg Trade Names: Carteolol Hydrochloride - Solution, ophthalmic 1% PharmacologyBlocks beta-receptors, primarily affecting cardiovascular system (eg, decreases heart rate, cardiac contractility, BP) and lungs (promotes bronchospasm). Ophthalmic use reduces IOP, probably by decreasing aqueous production. PharmacokineticsAbsorptionOral Well absorbed. T max is 1 to 3 h. Bioavailability is about 85%. DistributionOral 23% to 30% protein bound. MetabolismOral Metabolized to 8-hydroxycarteolol (active) and glucuronide conjugates. EliminationOral The t ½ is about 6 h (carteolol) and about 8 to 12 h (8-hydroxycarteolol). About 50% to 70% is excreted unchanged by the kidneys. Special PopulationsRenal Function Impairment Oral The t ½ may be prolonged and elimination decreased. Dosage adjustment may be needed. Indications and UsageManagement of hypertension. Ophthalmic preparation for control of intraocular hypertension and lowering of IOP in chronic open-angle glaucoma. Unlabeled UsesTreatment of angina. ContraindicationsHypersensitivity to beta-blockers; persistently severe bradycardia; greater than first-degree AV block; CHF unless secondary to tachyarrhythmia treatable with beta-blockers; overt cardiac failure; sinus bradycardia; cardiogenic shock; bronchial asthma or bronchospasm, including severe chronic obstructive pulmonary disease (COPD). Dosage and AdministrationAdults PO 2.5 to 10 mg every day. Ophthalmic use 1 drop twice daily in affected eye(s). Consider concomitant therapy if IOP is not at satisfactory level. General AdviceFor ophthalmic solution, pull out lower lid to create pocket, administer drop without touching eye, release lower lid, close eye, and apply gentle pressure on inner canthus of eye to avoid systemic absorption. Storage/StabilityStore at room temperature.
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