Antiglaucoma preparations and miotics, beta blocking agents - ATC code: S0lED05

carteolol hydrochloride

Carteolol hydrochloride 1% w/v Excipients: Benzalkonium chloride 0.005%. Carteolol hydrochloride 2% w/v Excipients: Benzalkonium chloride 0.005%.

Eye drops solution. A clear, colourless solution.

For the reduction of intraocular pressure e.g. in ocular hypertension, chronic open angle glaucoma, some secondary glaucomas.

Adults: Initially one drop of 1% eye drops instilled twice daily in each affected eye. If the clinical response is not adequate the dosage may be altered to one drop of 2% eye drops twice daily in each affected eye.

Nasolacrimal occlusion or closing the eyelids after drug instillation can reduce the systemic absorption. This may result in a decrease in systemic adverse events and an increase in local activity. It is recommended that the period of occlusion is five minutes in duration.

The dispenser remains sterile until the original closure is broken. Patients must be instructed to avoid allowing the tip of the dispensing container to contact the eye or surrounding structures as this may contaminate the solution.

If the patients IOP is not at a satisfactory level with this regimen, concomitant treatment with other IOP lowering drugs may be considered.

If more than one medication needs to be instilled in the eye, an interval of at least 5 minutes between application of the different medicinal products must be allowed.

Safety and effectiveness of carteolol has not been established.

There is no indication that dosage needs to be modified for the elderly.

The carteolol eye drops are contraindicated in patients:

- with unsatisfactorily controlled cardiac insufficiency, sinus bradycardia, second- or third-degree atrioventricular block, and or cardiogenic shock (these diseases or symptoms may be exacerbated).

- with symptoms or a history of bronchospasm including bronchial asthma or severe chronic obstructive pulmonary disease (these diseases or symptoms may be exacerbated).

- known hypersensitivity to carteolol hydrochloride or to any of the excipients

Like other topically applied ophthalmic drugs, carteolol hydrochloride may enter the systemic circulation and systemic effects or systemic adverse effects seen with oral beta-blockers may occur.

Carteolol eye drops must be administered with caution in the following patients:

- Patients with right heart failure due to pulmonary hypertension

- Patients with congestive heart failure. Cardiac failure should be adequately controlled before beginning therapy with carteolol. Patients with a history of severe cardiac disease should be watched for signs of cardiac failure.

- Patients with sick sinus syndrome, Prinzmetal's angina, untreated phaeochromocytoma, severe peripheral circulatory disturbances (Raynaud disease), and hypotension

- Patients with unsatisfactorily controlled diabetes mellitus. Careful monitoring of blood glucose levels is required during therapy.

- Patients with diabetic ketoacetosis or metabolic acidosis.

- Patients with hyperthyroidism

- Patients with myasthenia gravis. Beta-adrenergic blockade may potentiate muscle weakness related to certain myasthenic symptoms, such as diplopia, ptosis and generalised weakness.

Severe prolonged hypotension has been observed in some patients after administration of systemic beta-blockers during anaesthesia.

In patients with angle-closure glaucoma, the immediate objective of treatment is to reopen the angle. This requires constricting the pupil with a miotic.

Carteolol has little or no effect on the pupil. When carteolol is used to reduce intraocular pressure in angle-closure glaucoma it must be used with a miotic and not alone.

Risk from anaphylactic reactions: While taking beta-blockers, patients with a history of atropy or a history of severe anaphylactic reaction to a variety of allergens may be more reactive to repeated challenge with such allergens, either accidental, diagnostic or therapeutic [55]. Such patients may be unresponsive to the usual dose of adrenaline used to treat anaphylactic reactions.

As with any glaucoma treatment, regular examination of the intraocular pressure and cornea is recommended.

Eye drops are not for injection. They should never be injected subconjunctivally, nor should they be directly introduced into the anterior chamber of the eye.

The carteolol eye drops contain benzalkonium chloride as a preservative.

Therefore, the medicament should not be used while wearing soft contact lenses. The lenses must be removed before application of the drops and not reinserted earlier than 15 minutes after use.

The effect on intraocular pressure or the known effects of systemic betablockade may be exaggerated when carteolol is given to patients already receiving an oral beta-blocking agent. The response of these patients should be closely observed.

A drug in the same pharmacological class as carteolol, ophthalmic timolol maleate has been shown to potentiate the mydriatic effect of adrenaline when combined.

As carteolol may be absorbed systemically the following interactions as those seen with oral betablockers may occur:

- Carteolol may potentially add to the effects of oral calcium antagonists such as verapamil, and diltiazem, to induce congestive heart failure or cardiac conduction disturbances such as bradycardia and AV block.

- Digitalis glycosides, parasympathomimetics: association with betablockers may increase auriculoventricular conduction time.

- Class I anti-arrhythmic drugs (e.g. disopyramide, quinidine) and amiodarone: may have potentiating effect on atrial-conduction time and induce negative inotropic effect.

If a supplementary ophthalmic medication is used, there must be an interval of at least five minutes between the administration of the two products.

Ocular: Signs and symptoms of eye irritation including eye pain, eye pruritus, ocular hyperaemia, sensation of foreign body, dry eyes, burning and stinging.

Sensitivity to light (photophobia), conjunctival discharge, conjunctivitis, blepharitis, keratitis, vision blurred, conjunctival hyperaemia, oedema and decreased corneal sensitivity. Ptosis has been observed in other topical beta blockers.

Cardiovascular: Bradycardia, chest pain, atrioventricular block, syncope and palpitations. Cerebrovascular accident has been observed in other topical beta blockers.

Respiratory: Dyspnoea and asthma attacks. Respiratory and cardiac reactions, including death due to bronchospasm in patients with asthma have been reported.

Skin: Hypersensitivity reactions, including localised and generalised rash.

Isolated cases of urticaria, alopecia, psoriasiform-like lesions or exacerbation of psoriasis have been reported. There have been reports of skin rashes and/or dry eyes associated with the use of beta-adrenergic receptor blocking drugs.

Other: Headache, discomfort, malaise, dizziness, nausea and bitter taste. weakness, sinusitis and depression.

Spectrum Thea Pharmaceuticals Limited

(POM)

16 February 2012