Carteolol is a medication primarily used to treat high eye pressure in conditions like glaucoma. It belongs to a class of drugs known as beta blockers. By reducing the production of aqueous humor in the eye, carteolol helps in lowering intraocular pressure, which can prevent optic nerve damage and vision loss associated with conditions like glaucoma. It's typically administered in the form of eye drops.

Carteolol is a non-selective beta-blocker that blocks both beta 1 and beta 2 receptors. It is available as a topical formulation for ophthalmic use in patients with raised intraocular pressure or intraocular hypertension and chronic open-angle Glaucoma.

Carteolol Adult dose:

Carteolol Use of Carteolol in the treatment of raised intraocular pressure (as in Glaucoma)

• For high eye pressure, you usually put one drop of carteolol in the affected eye or eyes two times a day.

Carteolol Dose in children:

 It has not been studied in pediatric patients.

Pregnancy Risk Factor C

• Carteolol is categorized as Pregnancy Risk Factor C, meaning adverse events were noted in animal studies.
• Similarly, adverse effects associated with systemic use of beta-blockers might also occur with ophthalmic use of carteolol.
• If using eye medications like carteolol for glaucoma during pregnancy is necessary, doctors recommend using the lowest effective dose along with punctal occlusion to minimize potential exposure to the fetus.
• This recommendation is based on findings from various studies conducted by researchers such as Johnson in 2001, Salim in 2014, and Samples in 1988.

Carteolol use during breastfeeding

• It's uncertain whether carteolol passes into breast milk after being applied to the eyes.
• To minimize any potential risk to the nursing infant, it's advised to use the lowest effective dose along with punctal occlusion, according to studies conducted by Johnson in 2001 and Samples in 1988.
• The manufacturer suggests caution when administering carteolol eye drops to nursing women.

Carteolol dose in renal disease:

• According to the manufacturer's labeling, there are no specific dosage adjustments recommended for carteolol in individuals with renal impairment.

Carteolol Dose in liver disease:

• According to the manufacturer's labeling, no specific dosage adjustments are outlined for carteolol in individuals with hepatic impairment.

Common Side Effects of Carteolol Include:

• Ocular:
  • Conjunctival hyperemia

Less Common Side Effects of Carteolol Include:

• Ocular:
  • Corneal staining
  • Corneal sensitivity decreased
  • Anisocoria
  • Corneal punctate keratitis
  • Eye pain
  • Vision disturbances

Contraindications to Carteolol include:

• If you're allergic to carteolol or any ingredient in it, have certain heart conditions like slow heart rate or severe heart failure, or have a history of asthma or serious COPD, you shouldn't use carteolol.
• There's limited evidence on whether allergic reactions to one beta blocker mean you'll react to another, but because they're similar in structure and how they work, there's a chance of a reaction.

Warnings and Precautions

Anaphylactic reactions

• If you have a history of allergies or severe reactions to different allergens or if you've had serious allergic reactions before, be careful when using carteolol because it can cause severe allergic reactions.
• People on beta-blockers might become more sensitive to allergens over time.
• If you have an allergic reaction while on beta-blockers, using treatments like epinephrine might not work well or could have unwanted effects.

Choroidal detachment:

• After certain eye surgeries to reduce pressure, like filtration procedures, using beta-blockers or other treatments to lower eye fluid might lead to choroidal detachment, a serious condition where the layer under the retina separates.

Diabetes:

• If you have diabetes, be cautious when using carteolol because it can affect your blood sugar levels.
• It might make hypoglycemia (low blood sugar) worse or hide its signs and symptoms, making it harder for you to notice when your blood sugar is too low.

Heart failure:

• If you have heart failure, be careful when using carteolol.
• It's especially important to watch for any signs that your condition might be getting worse.
• Carteolol can potentially worsen heart failure, especially in those without a history of it.
• If your heart failure is already severe, don't use carteolol at all.
• According to a statement from the American Heart Association, carteolol is considered a medication that could make existing heart muscle problems worse.

Respiratory disease

• For individuals with respiratory conditions like asthma or chronic obstructive pulmonary disease (COPD), beta-blockers like carteolol should generally be avoided.
• If they are used, it should be done cautiously with close monitoring.
• Serious respiratory reactions, including cases of severe bronchospasm leading to fatalities, have been reported with the use of carteolol eye drops.
• Therefore, carteolol is contraindicated in individuals with a history of bronchial asthma or severe COPD.

Myasthenia gravis:

• If you have myasthenia gravis, be cautious when using carteolol because it might make your condition worse or worsen symptoms like double vision, drooping eyelids, and overall weakness.

Raynaud and peripheral vascular disease:

• For individuals with peripheral vascular disease (PVD) or Raynaud disease, it's important to be cautious when using carteolol because it could make symptoms of reduced blood flow worse or worsen conditions like Raynaud's phenomenon.
• Carteolol may potentially precipitate or exacerbate symptoms of arterial insufficiency in these patients.
• It's essential to use it carefully and to monitor for any progression of arterial obstruction.

Thyroid disease:

• If you have thyroid disease, be aware that carteolol may hide signs of an overactive thyroid, like fast heart rate.
• If you suspect you have an overactive thyroid, it's important to manage and monitor it carefully.
• Suddenly stopping carteolol could make symptoms of an overactive thyroid worse or even trigger a thyroid storm, a severe complication.

Carteolol (ophthalmic): Drug Interaction

Note: Drug Interaction Categories:

• Risk Factor C: Monitor When Using Combination
• Risk Factor D: Consider Treatment Modification
• Risk Factor X: Avoid Concomitant Use

Monitoring parameters:

Intraocular Pressure:

• Keep an eye on your eye pressure, especially with ophthalmic (eye) use of beta-blockers like carteolol.
• Beta-blockers can sometimes affect other parts of your body, so it's essential to monitor for any changes.

Systemic Effects:

• With eye drops containing beta-blockers like carteolol, there's a chance it could affect your whole body.
• Keep track of your blood pressure and watch for any changes, as beta-blockers can sometimes lower it.

How to administer Carteolol:

Topical Ophthalmic Use Only:

• Carteolol eye drops are meant for use on the eyes only, so don't use them for anything else.

Clean Hands:

• Wash your hands before using the eye drops to keep them free from germs.

Avoid Contamination:

• When putting drops in your eyes, don't let the dropper tip touch your eyelids or anything else. This helps prevent contamination.

Remove Contact Lenses:

• Take out your contact lenses before using carteolol eye drops.
• If the eye drops contain benzalkonium chloride, wait 15 minutes before putting your contacts back in.

Mechanism of action of Carteolol:

• Carteolol blocks both beta- and beta-adrenergic receptors in the eye.
• This action helps to decrease the pressure inside the eye by either reducing the production of aqueous humor (the fluid inside the eye) or possibly by increasing its outflow.
• By doing this, it helps to manage conditions like glaucoma by lowering the pressure in the eye, which can help prevent damage to the optic nerve and preserve vision.

Absorption:

• Approximately 25% of the dose applied to the eyes is absorbed into the bloodstream.

Metabolism:

• Carteolol is broken down in the liver primarily by an enzyme called CYP2D6.

Half-life Elimination:

• The half-life of elimination for carteolol is about 5 hours when it's removed from the body through urine. The terminal half-life, which is the time it takes for the drug concentration to decrease by half in the body, is approximately 13.8 hours.

Time to Peak:

• It takes around 0.25 hours (15 minutes) for the concentration of carteolol in the bloodstream to reach its highest level after administration.

Excretion:

• Carteolol and its metabolites are primarily eliminated from the body through urine.

International brands of Carteolol:

• Arteoptic
• Arteoptic LA
• Calte
• Carteabak
• Carteof
• Carteol
• Carteol LP
• Catelol
• Catol
• Elebloc
• Endak
• Fortinol
• Fortinol EP
• Glauteolol
• Karol
• Mikelan
• Mikelan LA
• Singlauc
• Teoptic

Carteolol Brands in pakistan: