Carteolol Hydrochloride

Pronunciation: (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%

Pharmacology

Blocks 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.

Pharmacokinetics

Absorption

Oral

Well absorbed. T max is 1 to 3 h. Bioavailability is about 85%.

Distribution

Oral

23% to 30% protein bound.

Metabolism

Oral

Metabolized to 8-hydroxycarteolol (active) and glucuronide conjugates.

Elimination

Oral

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 Populations

Renal Function ImpairmentOral

The t ½ may be prolonged and elimination decreased. Dosage adjustment may be needed.

Indications and Usage

Management of hypertension. Ophthalmic preparation for control of intraocular hypertension and lowering of IOP in chronic open-angle glaucoma.

Unlabeled Uses

Treatment of angina.

Contraindications

Hypersensitivity 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 Administration

Adults

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 Advice

For 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/Stability

Store at room temperature.

Drug Interactions

Clonidine

May enhance or reverse antihypertensive effect; may cause potentially life-threatening increases in BP, especially on simultaneous discontinuation of both drugs.

Epinephrine

May cause initial hypertensive episode followed by bradycardia.

Ergot derivatives

May cause peripheral ischemia with cold extremities. Peripheral gangrene possible.

NSAIDs

May impair antihypertensive effect.

Prazosin

May increase orthostatic hypotension.

Systemic beta-blocker

When coadministered with ophthalmic carteolol hydrochloride solution, may cause additive effects and toxicity.

Theophyllines

May reduce elimination of theophylline. May cause pharmacologic antagonism, reducing effects of one or both drugs.

Verapamil

May increase effects of both drugs.

Laboratory Test Interactions

None well documented.

Adverse Reactions

Cardiovascular

Hypotension; bradycardia; CHF; cold extremities; first-, second-, or third-degree atrioventricular block; arrhythmias; syncope.

CNS

Insomnia; fatigue; dizziness; depression; lethargy; drowsiness; forgetfulness; headache.

Dermatologic

Rash; hives; alopecia.

EENT

Dry eyes; blurred vision; tinnitus; slurred speech; dry mouth; sore throat. Eye discomfort or stinging; tearing; keratitis; drooping eyelids; visual disturbances; diplopia; ptosis (ophthalmic use).

GI

Nausea; vomiting; diarrhea; constipation.

Genitourinary

Impotence; painful, difficult, or frequent urination.

Hematologic

Agranulocytosis; thrombocytopenic purpura.

Metabolic

Hyperglycemia; hypoglycemia; unstable diabetes mellitus; hypercholesterolemia; hyperlipidemia; increased LDH.

Respiratory

Bronchospasm; shortness of breath; wheezing.

Miscellaneous

Weight changes; fever; facial swelling; cramps; muscle weakness. Antinuclear antibodies may develop.

Precautions

Monitor BP Monitor BP and pulse frequently when starting oral medication or when dosage is changed. IOP Perform measurements of IOP on regular basis to assess therapeutic effect of ophthalmic medication.

Pregnancy

Category C .

Lactation

Excreted in breast milk.

Children

Safety and efficacy not established.

Renal Function

Requires dosage adjustment.

Hepatic Function

Requires dosage adjustment.

Cessation of therapy

Discontinue therapy gradually, over about 2 wk, with careful observation of patient and limited physical activity.

CHF

Administer cautiously in patients with CHF treated with digitalis and diuretics.

Diabetes mellitus

Drug may mask signs and symptoms of hypoglycemia (eg, tachycardia, BP changes). May potentiate insulin-induced hypoglycemia.

Peripheral vascular disease

Drug may precipitate or aggravate symptoms of arterial insufficiency.

Thyrotoxicosis

May mask clinical signs of developing or continuing hyperthyroidism (eg, tachycardia). Abrupt withdrawal may exacerbate symptoms of hyperthyroidism, including thyroid storm.

Overdosage

Symptoms

Bradycardia, cardiac failure, hypotension, bronchospasm, hypoglycemia.

Patient Information

• Instruct patient in proper method of instilling eye drops.
• Teach patient how to monitor pulse before taking oral medication and to notify health care provider if pulse remains less than 50 bpm after taking drug and if fatigue and dizziness occur.
• Instruct patient to inform health care provider of any scheduled surgery or dental work; dosage may need to be gradually tapered (and ophthalmic solution discontinued) before surgery or treatment.
• Caution patient not to discontinue medication without consulting health care provider.
• Instruct diabetic patient to monitor blood glucose closely because carteolol hydrochloride may mask signs of hypoglycemia.
• Inform patient that ophthalmic solution may cause burning or stinging when first instilled in eye.
• Instruct patient to report these symptoms to health care provider: CHF, dizziness, decreased pulse, confusion, shortness of breath, rash, any unusual bleeding.
• Advise patient that drug may cause drowsiness and to use caution while driving or performing other tasks requiring mental alertness.

Copyright © 2009 Wolters Kluwer Health.

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