Carteolol

Pronunciation

(KAR tee oh lole)

U.S. Brand Names

Cartrol®; Ocupress® [DSC]

Synonyms

Carteolol Hydrochloride

Generic Available

Yes: Ophthalmic solution

Canadian Brand Names

Cartrol® Oral; Ocupress® Ophthalmic

Use

Management of hypertension; treatment of chronic open-angle glaucoma and intraocular hypertension

Pregnancy Risk Factor

C (manufacturer); D (2nd and 3rd trimesters - expert analysis)

Lactation

Excretion in breast milk unknown/use caution

Contraindications

Hypersensitivity to carteolol or any component of the formulation; sinus bradycardia; heart block greater than first-degree (except in patients with a functioning artificial pacemaker); cardiogenic shock; bronchial asthma, bronchospasm, or COPD; uncompensated cardiac failure; pulmonary edema; pregnancy (2nd and 3rd trimesters)

Warnings/Precautions

Avoid abrupt discontinuation in patients with a history of CAD; slowly wean while monitoring for signs and symptoms of ischemia. Use caution in patients with PVD (can aggravate arterial insufficiency). Use caution with concurrent use of beta-blockers and either verapamil or diltiazem; bradycardia or heart block can occur. Patients with bronchospastic disease should not receive beta-blockers. Use cautiously in diabetics because it can mask prominent hypoglycemic symptoms. Can mask signs of thyrotoxicosis. Can cause fetal harm when administered in pregnancy. Dosage adjustment is required in patients with renal dysfunction. Use care with anesthetic agents that decrease myocardial function. Beta-blockers with intrinsic sympathomimetic activity have not been demonstrated to be of value in CHF.

Adverse Reactions

Ophthalmic:

>10%: Ocular: Conjunctival hyperemia

1% to 10%: Ocular: Anisocoria, corneal punctate keratitis, corneal staining, decreased corneal sensitivity, eye pain, vision disturbances

Systemic:

>10%:

Central nervous system: Drowsiness, insomnia

Endocrine & metabolic: Decreased sexual ability

1% to 10%:

Cardiovascular: Bradycardia, palpitation, edema, CHF, reduced peripheral circulation

Central nervous system: Mental depression

Gastrointestinal: Diarrhea or constipation, nausea, vomiting, stomach discomfort

Respiratory: Bronchospasm

Miscellaneous: Cold extremities

<1% (Limited to important or life-threatening): Chest pain, arrhythmia, orthostatic hypotension, nervousness, headache, depression, hallucinations, confusion (especially in the elderly), psoriasiform eruption, itching, polyuria, thrombocytopenia, leukopenia, dyspnea

Overdosage/Toxicology

Symptoms of intoxication include cardiac disturbances, CNS toxicity, bronchospasm, hypoglycemia, and hyperkalemia. The most common cardiac symptoms include hypotension and bradycardia. Atrioventricular block, intraventricular conduction disturbances, cardiogenic shock, and asystole may occur with severe overdose, especially with membrane-depressant drugs (eg, propranolol). CNS effects include convulsions, coma, and respiratory arrest (commonly seen with propranolol and other membrane-depressant and lipid-soluble drugs). Treatment is symptomatic and supportive.

Drug Interactions

Substrate of CYP2D6 (minor)

Albuterol (and other beta2 agonists): Effects may be blunted by nonspecific beta-blockers.

Alpha-blockers (prazosin, terazosin): Concurrent use of beta-blockers may increase risk of orthostasis.

Carteolol causes hypertension when used with local anesthetics (tetracaine, lidocaine, or bupivacaine) containing epinephrine.

Clonidine: Hypertensive crisis after or during withdrawal of either agent.

Drugs which slow AV conduction (digoxin): Effects may be additive with beta-blockers.

Glucagon: Carteolol may blunt the hyperglycemic action of glucagon.

Insulin: Carteolol may mask tachycardia from hypoglycemia.

NSAIDs (ibuprofen, indomethacin, naproxen, piroxicam) may reduce the antihypertensive effects of beta-blockers.

Salicylates may reduce the antihypertensive effects of beta-blockers.

Sulfonylureas: Beta-blockers may alter response to hypoglycemic agents.

Verapamil or diltiazem may have synergistic or additive pharmacological effects when taken concurrently with beta-blockers.

Ethanol/Nutrition/Herb Interactions

Herb/Nutraceutical: Avoid dong quai if using for hypertension (has estrogenic activity). Avoid ephedra, yohimbe, ginseng (may worsen hypertension). Avoid garlic (may have increased antihypertensive effect).

Mechanism of Action

Blocks both beta1- and beta2-receptors and has mild intrinsic sympathomimetic activity; has negative inotropic and chronotropic effects and can significantly slow AV nodal conduction

Pharmacodynamics/Kinetics

Onset of action: Oral: 1-1.5 hours

Peak effect: 2 hours

Duration: 12 hours

Absorption: Oral: 80%

Protein binding: 23% to 30%

Metabolism: 30% to 50%

Half-life elimination: 6 hours

Excretion: Urine (as metabolites)

Dosage

Adults:

Oral: 2.5 mg as a single daily dose, with a maintenance dose normally 2.5-5 mg once daily; doses >10 mg do not increase response and may in fact decrease effect.

Ophthalmic: Instill 1 drop in affected eye(s) twice daily.

Dosing interval in renal impairment: Oral:

Clcr >60 mL/minute/1.73 m² : Administer every 24 hours.

Clcr 20-60 mL/minute/1.73 m² : Administer every 48 hours.

Clcr<20 mL/minute/1.73 m² : Administer every 72 hours.

Administration

Oral: Administer with meals.

Ophthalmic: Intended for twice daily dosing. Keep eye open and do not blink for 30 seconds after instillation. Wear sunglasses to avoid photophobic discomfort. Apply gentle pressure to lacrimal sac during and immediately following instillation (1 minute).

Monitoring Parameters

Ophthalmic: Intraocular pressure; Systemic: Blood pressure, pulse, CNS status

Patient Education

Inform prescriber of all prescriptions, OTC medications, or herbal products you are taking, and any allergies you have. Do not take with antacids and avoid taking OTC medications (eg, cold remedies) without consulting prescriber. Do not take any new medication during therapy unless approved by prescriber. Oral: Take with meals. Do not increase, decrease, or adjust dosage without consulting prescriber. Take pulse daily, prior to medication; follow prescriber's instruction about holding medication. If you have diabetes, monitor serum blood glucose closely (drug may alter glucose tolerance or mask signs of hypoglycemia). May cause fatigue, dizziness, or postural hypotension (use caution when changing position from lying or sitting to standing, when driving, or climbing stairs until response to medication is known); alteration in sexual performance (reversible). Report unresolved swelling of extremities, respiratory difficulty or new cough, unresolved fatigue, unusual weight gain, unresolved constipation, or unusual muscle weakness. Pregnancy/breast-feeding precautions: Inform prescriber if you are or intend to become pregnant. Consult prescriber if breast-feeding.

Ophthalmic: Wash hands before instilling. Sit or lie down to instill. Open eye, look at ceiling, and instill prescribed amount of medication. Keep eye open and do not blink for 30 seconds after instillation. Apply gentle pressure to inner corner of eye during and immediately following installation (1 minute). Do not touch tip of applicator or let tip of applicator touch eye. Temporary stinging or burning may occur. Wear sunglasses to avoid sun sensitivity or eye discomfort. Report persistent pain, burning, vision changes, swelling, itching, or worsening of condition.

Anesthesia and Critical Care Concerns/Other Considerations

Due to alterations in the autonomic nervous system, beta-blockade may result in less hemodynamic response in the elderly. Despite decreased sensitivity to the chronotropic effects of beta blockade with age, there appears to be an increased myocardial sensitivity to the negative inotropic effect.

Carteolol has mild intrinsic sympathomimetic activity and is a nonspecific beta-blocker. Thus, the cardiovascular benefits of carteolol are less clear compared to other beta-blockers. Furthermore, the beta-2 blocking activity may be accompanied by an increased level of side effects with respect to bronchospasm and peripheral vasoconstriction.

Surgery: Atenolol has also been shown to improve cardiovascular outcomes when used in the perioperative period in patients with underlying cardiovascular disease who are undergoing noncardiac surgery. Bisoprolol in high-risk patients undergoing vascular surgery reduced the perioperative incidence of death from cardiac causes and nonfatal myocardial infarction.

Withdrawal: Beta-blocker therapy should not be withdrawn abruptly, but gradually tapered to avoid acute tachycardia and hypertension.

Cardiovascular Considerations

Hypertension: Beta-blocker therapy in the treatment of hypertension has been associated with improved cardiovascular outcomes. This class of drug is beneficial for elderly patients with hypertension. A recent UKPDS study showed that beta-blocker therapy (atenolol) was as effective as an ACE inhibitor in reducing cardiovascular events and that the benefits of therapy were related more to the degree of antihypertensive efficacy rather than the class of drug used.

Myocardial infarction: Beta-blockers, in general without intrinsic sympathomimetic activity (ISA), have been shown to decrease morbidity and mortality when initiated in the acute treatment of myocardial infarction and continued long-term. In this setting, therapy should be avoided in patients with hypotension, cardiogenic shock, or heart block.

Surgery: Atenolol has also been shown to improve cardiovascular outcomes when used in the perioperative period in patients with underlying cardiovascular disease who are undergoing noncardiac surgery. Bisoprolol in high-risk patients undergoing vascular surgery reduced the perioperative incidence of death from cardiac causes and nonfatal myocardial infarction.

Atrial fibrillation: Beta-blocker therapy provides effective rate control in patients with atrial fibrillation.

Angina: Beta-blockers are effective in the treatment of angina as monotherapy or when combined with nitrates and/or calcium channel blockers. In patients with severe intractable angina requiring negative cardiac chronotropic medications, pacemaker placement has been carried out to maintain heart rate in the setting of large doses of beta-blockers and/or calcium channel blockers. Beta-blockers are ineffective in the treatment of pure vasospastic (Prinzmetal) angina.

Unstable angina/non-ST-segment elevation MI: In the treatment of unstable angina/non-ST-segment elevation MI, a beta-blocker, with the first dose administered intravenously if there is ongoing chest pain, followed by oral administration, is recommended (in the absence of contraindications).

Withdrawal: Beta-blocker therapy should not be withdrawn abruptly, but gradually tapered to avoid acute tachycardia and hypertension.

Heart failure: There is emerging evidence that beta-blocker therapy, without intrinsic sympathomimetic activity (ISA), should be initiated in select patients with stable congestive heart failure (NYHA Class II-III). To date, carvedilol, sustained release metoprolol, and bisoprolol have demonstrated a beneficial effect on morbidity and mortality. It is important that beta-blocker therapy be instituted initially at very low doses with gradual and very careful titration.

Dental Health: Effects on Dental Treatment

Carteolol is a nonselective beta-blocker and may enhance the pressor response to epinephrine, resulting in hypertension and bradycardia. Many nonsteroidal anti-inflammatory drugs, such as ibuprofen and indomethacin, can reduce the hypotensive effect of beta-blockers after 3 or more weeks of therapy with the NSAID. Short-term NSAID use (ie, 3 days) requires no special precautions in patients taking beta-blockers.

Dental Health: Vasoconstrictor/Local Anesthetic Precautions

No information available to require special precautions

Mental Health: Effects on Mental Status

May cause fatigue, insomnia, confusion, and nightmares and clinically look like a major depression

Mental Health: Effects on Psychiatric Treatment

Antipsychotics and MAO inhibitors may increase the effects of beta-blockers; conversely beta-blockers may increase the effects of antipsychotics and benzodiazepines

Dosage Forms

[DSC] = Discontinued product

Solution, ophthalmic, as hydrochloride: 1% (5 mL, 10 mL, 15 mL) [contains benzalkonium chloride]

Ocupress® [DSC]: 1% (5 mL, 10 mL, 15 mL) {contains benzalkonium chloride]

Tablet, as hydrochloride (Cartrol®): 2.5 mg, 5 mg

References

Braunwald E, Antman EM, Beasley JW, et al, "ACC/AHA 2002 Guideline Update for the Management of Patients With Unstable Angina and Non-ST-Segment Elevation Myocardial Infarction - Summary Article: A Report of the American College of Cardiology/American Heart Association Task Force on Practice Guidelines (Committee on the Management of Patients With Unstable Angina)," J Am Coll Cardiol , 2002, 40(7):1366-74. Available at: http://www.acc.org/clinical/guidelines/unstable/incorporated/index.htm. Accessed May 20, 2003.

"Consensus Recommendations for the Management of Chronic Heart Failure. On Behalf of the Membership of the Advisory Council to Improve Outcomes Nationwide in Heart Failure," Am J Cardiol , 1999, 83(2A):1A-38A.

Gibbons RJ, Abrams J, Chatterjee K, et al, "ACC/AHA 2002 Guideline Update for the Management of Patients With Chronic Stable Angina - Summary Article: A Report of the American College of Cardiology/American Heart Association Task Force on Practice Guidelines (Committee on the Management of Patients With Chronic Stable Angina)," J Am Coll Cardiol , 2003, 41(1):159-68.

Mokhlesi B, Leikin JB, Murray P, et al, "Adult Toxicology in Critical Care: Part II: Specific Poisonings," Chest , 2003, 123(3):897-922.

International Brand Names

Arteolol® (ES); Arteoptic® (CH, CZ, DE, DK, HK, PL, PT, SE, TH); Cartéabak® (FR); Carteol® (BE); Cartéol® (FR); Carteol® (LU, RO, TR); Cartrol® Oral (CA); Elebloc® (AR, ES); Endak® (DE); Glauteolol® (AR); Mikelan® (ES, FR, HK, ID, JP, ZA); Ocupress® Ophthalmic (CA); Poenglaucol® (AR); Singlauc® (AR); Teoptic® (GB, IE, NL, ZA)

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