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Carteolol (ophthalmic): Drug information

Carteolol (ophthalmic): Drug information
(For additional information see "Carteolol (ophthalmic): Patient drug information")

For abbreviations, symbols, and age group definitions used in Lexicomp (show table)
Pharmacologic Category
  • Ophthalmic Agent, Antiglaucoma
Dosing: Adult
Elevated intraocular pressure

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

Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.

Dosing: Kidney Impairment: Adult

There are no dosage adjustments provided in the manufacturer’s labeling.

Dosing: Hepatic Impairment: Adult

There are no dosage adjustments provided in the manufacturer’s labeling.

Dosing: Older Adult

Refer to adult dosing.

Adverse Reactions

The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified.

>10%: Ophthalmic: Burning sensation of eyes, conjunctival edema, conjunctival hyperemia, eye irritation, lacrimation

Frequency not defined: Ophthalmic: Blepharoconjunctivitis, blepharoptosis, blurred vision, cloudy vision, corneal sensitivity, corneal staining, night blindness, photophobia

Postmarketing:

Cardiovascular: Cardiac arrhythmia, chest tightness (Wu 2019), palpitations, second-degree atrioventricular block (Ruiz-Ruiz 2002)

Gastrointestinal: Dysgeusia

Nervous system: Asthenia, dizziness, headache, insomnia

Respiratory: Dyspnea (Wu 2019), sinusitis

Contraindications

Hypersensitivity to carteolol or any component of the formulation; sinus bradycardia; second- or third-degree atrioventricular block; cardiogenic shock; bronchial asthma or history of bronchial asthma; severe chronic obstructive pulmonary disease; overt cardiac failure.

Warnings/Precautions

Concerns related to adverse events:

• Anaphylactic reactions: Use caution with history of atopy or a history of severe anaphylaxis to a variety of allergens; patients taking beta-blockers may become more sensitive to repeated challenges. Treatment of anaphylaxis (eg, epinephrine) in patients taking beta-blockers may be ineffective or promote undesirable effects.

• Choroidal detachment: Beta-blockade and/or other aqueous suppressive therapy have been associated with choroidal detachment following filtration procedures.

Disease-related concerns:

• Diabetes: Use with caution in patients with diabetes mellitus (especially labile diabetes); may potentiate hypoglycemia and/or mask signs and symptoms.

• Heart failure (HF): Use with caution in patients with compensated heart failure and monitor for a worsening of the condition; may lead to heart failure in patients without a history of heart failure. Use is contraindicated in overt heart failure. In a scientific statement from the American Heart Association, carteolol has been determined to be an agent that may exacerbate underlying myocardial dysfunction (magnitude: major) (AHA [Page 2016]).

• Myasthenia gravis: Use with caution in patients with myasthenia gravis; may worsen disease or other myasthenic symptoms (diplopia, ptosis, and generalized weakness).

• Peripheral vascular disease and Raynaud disease: Can precipitate or aggravate symptoms of arterial insufficiency in patients with peripheral vascular disease (PVD) and Raynaud disease. Use with caution and monitor for progression of arterial obstruction.

• Respiratory disease: In general, patients with bronchospastic disease should not receive beta-blockers; if used at all, should be used cautiously with close monitoring. Severe respiratory reactions, including fatalities due to bronchospasm in patients with asthma, have been reported with ophthalmic use. Use is contraindicated in bronchial asthma or history of bronchial asthma and severe COPD.

• Thyroid disease: May mask signs of hyperthyroidism (eg, tachycardia). If thyrotoxicosis is suspected, carefully manage and monitor; abrupt withdrawal may exacerbate symptoms of hyperthyroidism or precipitate thyroid storm.

Special populations:

• Contact lens wearers: Some products may contain benzalkonium chloride, which may be absorbed by soft contact lenses; remove lens prior to administration and wait 15 minutes before reinserting.

Dosage form specific issues:

• Absorption: Systemic absorption of carteolol and adverse effects may occur with ophthalmic use, including respiratory and cardiovascular effects (eg, bradycardia and/or hypotension).

• Appropriate use: Should not be used alone in angle-closure glaucoma (has no effect on pupillary constriction). Multidose vials have been associated with development of bacterial keratitis; avoid contamination.

• Surgery: May block systemic effects of beta agonists (eg, epinephrine, norepinephrine); notify anesthesiologist if patient is receiving ophthalmic beta blocker therapy. Patients undergoing planned major surgery should be gradually tapered off therapy (if possible) prior to procedure. If necessary during surgery, effects of beta blocker therapy may be reversed by adrenergic agonists.

Dosage Forms: US

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Solution, Ophthalmic, as hydrochloride:

Generic: 1% (5 mL, 10 mL, 15 mL)

Generic Equivalent Available: US

Yes

Pricing: US

Solution (Carteolol HCl Ophthalmic)

1% (per mL): $4.01

Disclaimer: A representative AWP (Average Wholesale Price) price or price range is provided as reference price only. A range is provided when more than one manufacturer's AWP price is available and uses the low and high price reported by the manufacturers to determine the range. The pricing data should be used for benchmarking purposes only, and as such should not be used alone to set or adjudicate any prices for reimbursement or purchasing functions or considered to be an exact price for a single product and/or manufacturer. Medi-Span expressly disclaims all warranties of any kind or nature, whether express or implied, and assumes no liability with respect to accuracy of price or price range data published in its solutions. In no event shall Medi-Span be liable for special, indirect, incidental, or consequential damages arising from use of price or price range data. Pricing data is updated monthly.

Administration: Adult

For topical ophthalmic use only. Wash hands before use. To avoid contamination, do not touch dropper tip to eyelids or other surfaces when placing drops in eyes. Remove contact lenses prior to administration; wait 15 minutes before reinserting if using products containing benzalkonium chloride.

Use: Labeled Indications

Elevated intraocular pressure: Treatment of elevated intraocular pressure (IOP) in patients with chronic open-angle glaucoma and intraocular hypertension.

Medication Safety Issues
Sound-alike/look-alike issues:

Carteolol may be confused with carvedilol

Metabolism/Transport Effects

Substrate of CYP2D6 (minor); Note: Assignment of Major/Minor substrate status based on clinically relevant drug interaction potential

Drug Interactions

Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the Lexicomp drug interactions program by clicking on the “Launch drug interactions program” link above.

Acetylcholinesterase Inhibitors: May enhance the bradycardic effect of Beta-Blockers. Risk C: Monitor therapy

Alpha2-Agonists: May enhance the AV-blocking effect of Beta-Blockers. Sinus node dysfunction may also be enhanced. Beta-Blockers may enhance the rebound hypertensive effect of Alpha2-Agonists. This effect can occur when the Alpha2-Agonist is abruptly withdrawn. Management: Closely monitor heart rate during treatment with a beta blocker and clonidine. Withdraw beta blockers several days before clonidine withdrawal when possible, and monitor blood pressure closely. Recommendations for other alpha2-agonists are unavailable. Risk D: Consider therapy modification

Amiodarone: May enhance the bradycardic effect of Beta-Blockers. Possibly to the point of cardiac arrest. Amiodarone may increase the serum concentration of Beta-Blockers. Risk C: Monitor therapy

Antidiabetic Agents: Beta-Blockers (Nonselective) may enhance the hypoglycemic effect of Antidiabetic Agents. Beta-Blockers (Nonselective) may diminish the therapeutic effect of Antidiabetic Agents. Risk C: Monitor therapy

Antipsychotic Agents (Phenothiazines): May enhance the hypotensive effect of Beta-Blockers. Beta-Blockers may decrease the metabolism of Antipsychotic Agents (Phenothiazines). Antipsychotic Agents (Phenothiazines) may decrease the metabolism of Beta-Blockers. Risk C: Monitor therapy

Beta2-Agonists: Beta-Blockers (Nonselective) may diminish the bronchodilatory effect of Beta2-Agonists. Risk X: Avoid combination

Bradycardia-Causing Agents: May enhance the bradycardic effect of other Bradycardia-Causing Agents. Risk C: Monitor therapy

Cannabis: Beta-Blockers may enhance the adverse/toxic effect of Cannabis. Specifically, the risk of hypoglycemia may be increased. Risk C: Monitor therapy

Ceritinib: Bradycardia-Causing Agents may enhance the bradycardic effect of Ceritinib. Management: If this combination cannot be avoided, monitor patients for evidence of symptomatic bradycardia, and closely monitor blood pressure and heart rate during therapy. Risk D: Consider therapy modification

Cholinergic Agonists: Beta-Blockers may enhance the adverse/toxic effect of Cholinergic Agonists. Of particular concern are the potential for cardiac conduction abnormalities and bronchoconstriction. Risk C: Monitor therapy

Dipyridamole: May enhance the bradycardic effect of Beta-Blockers. Risk C: Monitor therapy

Disopyramide: May enhance the bradycardic effect of Beta-Blockers. Beta-Blockers may enhance the negative inotropic effect of Disopyramide. Risk C: Monitor therapy

DOBUTamine: Beta-Blockers may diminish the therapeutic effect of DOBUTamine. Risk C: Monitor therapy

Dronedarone: May enhance the bradycardic effect of Beta-Blockers. Dronedarone may increase the serum concentration of Beta-Blockers. This likely applies only to those agents that are metabolized by CYP2D6. Management: Use lower initial beta-blocker doses; adequate tolerance of the combination, based on ECG findings, should be confirmed prior to any increase in beta-blocker dose. Increase monitoring for clinical response and adverse effects. Risk D: Consider therapy modification

EPHEDrine (Systemic): Beta-Blockers may diminish the therapeutic effect of EPHEDrine (Systemic). Risk C: Monitor therapy

EPINEPHrine (Nasal): Beta-Blockers (Nonselective) may enhance the hypertensive effect of EPINEPHrine (Nasal). Risk C: Monitor therapy

EPINEPHrine (Oral Inhalation): Beta-Blockers (Nonselective) may enhance the hypertensive effect of EPINEPHrine (Oral Inhalation). Risk C: Monitor therapy

Epinephrine (Racemic): Beta-Blockers (Nonselective) may enhance the hypertensive effect of Epinephrine (Racemic). Risk C: Monitor therapy

EPINEPHrine (Systemic): Beta-Blockers (Nonselective) may enhance the hypertensive effect of EPINEPHrine (Systemic). Risk C: Monitor therapy

Ergot Derivatives (Vasoconstrictive CYP3A4 Substrates): Beta-Blockers may enhance the vasoconstricting effect of Ergot Derivatives (Vasoconstrictive CYP3A4 Substrates). Risk C: Monitor therapy

Etilefrine: May enhance the bradycardic effect of Beta-Blockers. Beta-Blockers may diminish the therapeutic effect of Etilefrine. Risk C: Monitor therapy

Etofylline: Beta-Blockers may diminish the therapeutic effect of Etofylline. Risk X: Avoid combination

Etrasimod: May enhance the bradycardic effect of Bradycardia-Causing Agents. Risk C: Monitor therapy

Fexinidazole: Bradycardia-Causing Agents may enhance the arrhythmogenic effect of Fexinidazole. Risk X: Avoid combination

Fingolimod: Bradycardia-Causing Agents may enhance the bradycardic effect of Fingolimod. Management: Consult with the prescriber of any bradycardia-causing agent to see if the agent could be switched to an agent that does not cause bradycardia prior to initiating fingolimod. If combined, perform continuous ECG monitoring after the first fingolimod dose. Risk D: Consider therapy modification

Grass Pollen Allergen Extract (5 Grass Extract): Beta-Blockers may enhance the adverse/toxic effect of Grass Pollen Allergen Extract (5 Grass Extract). More specifically, Beta-Blockers may inhibit the ability to effectively treat severe allergic reactions to Grass Pollen Allergen Extract (5 Grass Extract) with epinephrine. Some other effects of epinephrine may be unaffected or even enhanced (e.g., vasoconstriction) during treatment with Beta-Blockers. Management: Consider alternatives to either grass pollen allergen extract (5 grass extract) or beta-blockers in patients with indications for both agents. Canadian product labeling specifically lists this combination as contraindicated. Risk D: Consider therapy modification

Insulins: Beta-Blockers (Nonselective) may enhance the hypoglycemic effect of Insulins. Beta-Blockers (Nonselective) may diminish the therapeutic effect of Insulins. Risk C: Monitor therapy

Isoproterenol: Beta-Blockers may diminish the therapeutic effect of Isoproterenol. Risk C: Monitor therapy

Ivabradine: Bradycardia-Causing Agents may enhance the bradycardic effect of Ivabradine. Risk C: Monitor therapy

Lacosamide: Bradycardia-Causing Agents may enhance the AV-blocking effect of Lacosamide. Risk C: Monitor therapy

Mavacamten: Beta-Blockers may enhance the adverse/toxic effect of Mavacamten. Specifically, negative inotropic effects may be increased. Risk C: Monitor therapy

Methacholine: Beta-Blockers may enhance the adverse/toxic effect of Methacholine. Risk C: Monitor therapy

Methoxyflurane: May enhance the hypotensive effect of Beta-Blockers. Risk C: Monitor therapy

Midodrine: May enhance the bradycardic effect of Bradycardia-Causing Agents. Risk C: Monitor therapy

Mivacurium: Beta-Blockers may enhance the therapeutic effect of Mivacurium. Risk C: Monitor therapy

NIFEdipine: May enhance the hypotensive effect of Beta-Blockers. NIFEdipine may enhance the negative inotropic effect of Beta-Blockers. Risk C: Monitor therapy

Nitrendipine: May enhance the therapeutic effect of Beta-Blockers. Risk C: Monitor therapy

Nonsteroidal Anti-Inflammatory Agents: May diminish the antihypertensive effect of Beta-Blockers. Risk C: Monitor therapy

Nonsteroidal Anti-Inflammatory Agents (Topical): May diminish the therapeutic effect of Beta-Blockers. Risk C: Monitor therapy

Ozanimod: May enhance the bradycardic effect of Bradycardia-Causing Agents. Risk C: Monitor therapy

Ponesimod: Bradycardia-Causing Agents may enhance the bradycardic effect of Ponesimod. Management: Avoid coadministration of ponesimod with drugs that may cause bradycardia when possible. If combined, monitor heart rate closely and consider obtaining a cardiology consult. Do not initiate ponesimod in patients on beta-blockers if HR is less than 55 bpm. Risk D: Consider therapy modification

Reserpine: May enhance the bradycardic effect of Beta-Blockers. Reserpine may enhance the hypotensive effect of Beta-Blockers. Risk C: Monitor therapy

Rivastigmine: May enhance the bradycardic effect of Beta-Blockers. Risk X: Avoid combination

Siponimod: Bradycardia-Causing Agents may enhance the bradycardic effect of Siponimod. Management: Avoid coadministration of siponimod with drugs that may cause bradycardia. If combined, consider obtaining a cardiology consult regarding patient monitoring. Risk D: Consider therapy modification

Succinylcholine: Beta-Blockers may enhance the neuromuscular-blocking effect of Succinylcholine. Risk C: Monitor therapy

Sulfonylureas: Beta-Blockers (Nonselective) may enhance the hypoglycemic effect of Sulfonylureas. Beta-Blockers (Nonselective) may diminish the therapeutic effect of Sulfonylureas. Risk C: Monitor therapy

Tasimelteon: Beta-Blockers may diminish the therapeutic effect of Tasimelteon. Management: Consider avoiding nighttime administration of beta-blockers during tasimelteon therapy due to the potential for reduced tasimelteon efficacy. Risk D: Consider therapy modification

Theophylline Derivatives: Beta-Blockers (Nonselective) may diminish the bronchodilatory effect of Theophylline Derivatives. Risk C: Monitor therapy

Tofacitinib: May enhance the bradycardic effect of Bradycardia-Causing Agents. Risk C: Monitor therapy

White Birch Allergen Extract: Beta-Blockers may enhance the adverse/toxic effect of White Birch Allergen Extract. Specifically, beta-blockers may reduce the effectiveness of beta-agonists that may be required to treat systemic reactions to white birch allergen extract. Risk X: Avoid combination

Pregnancy Considerations

Adverse events were observed in some animal reproduction studies. The same adverse effects observed with systemic administration of beta-blockers may occur following ophthalmic use of carteolol. If ophthalmic agents are needed for the treatment of glaucoma during pregnancy, the minimum effective dose should be used in combination with punctal occlusion to decrease potential exposure to the fetus (Johnson 2001; Salim 2014; Samples 1988).

Breastfeeding Considerations

It is not known if carteolol is excreted in breast milk following ophthalmic administration. The minimum effective dose should be used in combination with punctual occlusion to decrease potential exposure to the nursing infant (Johnson 2001; Samples 1988). The manufacturer recommends that caution be exercised when administering carteolol (ophthalmic) to nursing women.

Monitoring Parameters

Intraocular pressure; monitor for systemic effect of beta-blockade with ophthalmic administration; blood pressure

Mechanism of Action

Blocks both beta1- and beta2-adrenergic receptors and reduces intraocular pressure by reducing aqueous humor production or possibly increases the outflow of aqueous humor

Pharmacokinetics (Adult Data Unless Noted)

Absorption: ~25% of ophthalmic dose is absorbed systemically (Chrisp 1992)

Metabolism: Hepatic via CYP2D6 (Henness 2007)

Half-life elimination: ~5 hours (urinary elimination); 13.8 hours (terminal) (Henness 2007)

Time to peak: Plasma 0.25 hours (Henness 2007)

Excretion: Urine (Henness 2007)

Brand Names: International
International Brand Names by Country
For country code abbreviations (show table)

  • (AR) Argentina: Cartens | Carteolol skin | Elebloc | Glauteolol | Poenglaucol | Singlauc;
  • (BE) Belgium: Arteoptic la | Carteabak | Carteol;
  • (BF) Burkina Faso: Carteol;
  • (CH) Switzerland: Arteoptic;
  • (CN) China: Mei kai lang | Mikelan;
  • (CZ) Czech Republic: Arteoptic | Carteol lp;
  • (DE) Germany: Arteoptic | Carteol LA;
  • (EG) Egypt: Arteoptic;
  • (ES) Spain: Arteoptic | Elebloc | Mikelan oftalmico;
  • (FI) Finland: Arteoptic;
  • (FR) France: Carteabak | Carteol | Carteol lp;
  • (GB) United Kingdom: Carteabak | Teoptic;
  • (GR) Greece: Cardelol | Fortinol;
  • (HK) Hong Kong: Arteoptic;
  • (HU) Hungary: Arteoptic | Fortinol;
  • (ID) Indonesia: Arteoptic;
  • (IE) Ireland: Teoptic;
  • (IT) Italy: Carteabak | Carteol | Fortidose | Fortinol;
  • (JO) Jordan: Carteol | Carteol lp | Opti tens;
  • (JP) Japan: Blokyleate | Carteolol hydrochloride pf nitten | Carteolol hydrochloride wakamoto | Carteolol t | Mercatoa | Mikelan | Rienton | Rienton mita | Rienton nidek;
  • (KR) Korea, Republic of: Caltamol | Calte | Carol | Carteolol | Catelol | Catelon | Mikelan | Mikelan la;
  • (LU) Luxembourg: Carteabak | Carteol;
  • (MA) Morocco: Carteol;
  • (NL) Netherlands: Carteabak | Teoptic;
  • (PE) Peru: Carteof;
  • (PK) Pakistan: Carteol;
  • (PL) Poland: Arteoptic | Carteol | Carteol lp;
  • (PR) Puerto Rico: Carteolol HCL;
  • (PT) Portugal: Arteoptic | Carteabak | Physioglau;
  • (RO) Romania: Carteol | Fortinol ep;
  • (SA) Saudi Arabia: Carteol lp | Teoptic;
  • (SE) Sweden: Arteoptic;
  • (SK) Slovakia: Arteoptic | Carteol lp;
  • (TH) Thailand: Arteoptic;
  • (TN) Tunisia: Carteol lp;
  • (TR) Turkey: Carteol;
  • (TW) Taiwan: Arteoptic | Carleo | Catol | Elebloc | Karteol | Mikelan;
  • (ZA) South Africa: Teoptic
  1. Carteolol [prescribing information]. Bridgewater, NJ: Bausch & Lomb, Inc; June 2016.
  2. Chrisp P, Sorkin EM. Ocular carteolol. A review of its pharmacological properties, and therapeutic use in glaucoma and ocular hypertension. Drugs Aging. 1992;2(1):58-77. [PubMed 1554974]
  3. Henness S, Swainston Harrison T, Keating GM. Ocular carteolol: a review of its use in the management of glaucoma and ocular hypertension. Drugs Aging. 2007;24(6):509-528. [PubMed 17571916]
  4. Johnson SM, Martinez M, Freedman S. Management of glaucoma in pregnancy and lactation. Surv Ophthalmol. 2001;45(5):449-454. [PubMed 11274697]
  5. Page RL 2nd, O'Bryant CL, Cheng D, et al; American Heart Association Clinical Pharmacology and Heart Failure and Transplantation Committees of the Council on Clinical Cardiology; Council on Cardiovascular Surgery and Anesthesia; Council on Cardiovascular and Stroke Nursing; and Council on Quality of Care and Outcomes Research. Drugs That May Cause or Exacerbate Heart Failure: A Scientific Statement From the American Heart Association [published correction appears in Circulation. 2016;134(12):e261]. Circulation. 2016;134(6):e32-e69. doi: 10.1161/CIR.0000000000000426. [PubMed 27400984]
  6. Ruiz-Ruiz FJ, Perez-Calvo JI, Sanjuan-Cuartero R. Topical beta blockers and atrioventricular block in the elderly. J Postgrad Med. 2002;48(4):327-328. [PubMed 12571398]
  7. Salim S. Glaucoma in pregnancy. Curr Opin Ophthalmol. 2014;25(2):93-97. [PubMed 24469077]
  8. Samples JR, Meyer SM. Use of ophthalmic medications in pregnant and nursing women. Am J Ophthalmol. 1988;106(5):616-623. [PubMed 2903673]
  9. Wu JH, Jerng JS, Su CC. Insidious-onset, non-wheezing carteolol-induced asthma in an atopic patient without asthma history. BMJ Case Rep. 2019;12(4):e229343. doi:10.1136/bcr-2019-229343 [PubMed 2903673]
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