Ocupress®
Carteolol 1% · ophthalmic solution
Antiglaucoma
Approved uses
Elevated IOP in chronic open-angle glaucoma or intraocular hypertension
1 drop of 1% in the affected eye(s) BID
Twice-daily dosing gives a median IOP reduction of 22% to 25%.
Elevated IOP inadequately controlled on the twice-daily regimen alone
1 drop of 1% BID plus pilocarpine or another miotic, and/or epinephrine or dipivefrin, and/or a systemic carbonic anhydrase inhibitor such as acetazolamide
Combined with pilocarpine, mean IOP falls 6 to 10 mmHg, a 24% to 40% reduction.
Contraindications
- Bronchial asthma or a history of bronchial asthma.
- Severe chronic obstructive pulmonary disease.
- Sinus bradycardia.
- Second and third degree atrioventricular block.
- Overt cardiac failure.
- Cardiogenic shock.
- Hypersensitivity to any component.
Available Forms1% solution, 5 mL, 10 mL, 15 mL
Mechanism of ActionNonselective beta-adrenoceptor blocker with intrinsic sympathomimetic activity and without significant membrane-stabilizing activity; reduces normal and elevated IOP whether or not glaucoma is present. The label states the exact mechanism of the ocular hypotensive effect of beta-blockers has not been definitely demonstrated, and reports no significant effect on corneal sensitivity, tear secretion, or pupil size in the controlled trials.
Warnings & Precautions
- Systemic absorption: Not detected in plasma after ocular instillation, but systemic absorption can still occur and the same adverse reactions seen with systemic beta-blockade may follow topical use, including death due to bronchospasm in patients with asthma and, rarely, death in association with cardiac failure.
- Cardiac failure: Beta-blockade may precipitate more severe failure where sympathetic stimulation supports the circulation, and continued myocardial depression can lead to failure in patients with no history of it; discontinue at the first sign or symptom.
- Non-allergic bronchospasm: Caution in chronic bronchitis or emphysema, since bronchodilation produced by endogenous and exogenous catecholamine stimulation of beta-2 receptors may be blocked.
- Pulmonary function impairment: Caution in any patient with known diminished pulmonary function.
- Major surgery: Beta-blockade impairs the heart's response to reflex stimuli and has been followed by protracted severe hypotension during anesthesia; gradual withdrawal before elective surgery may be appropriate.
- Diabetes mellitus: Masks the signs and symptoms of acute hypoglycemia; caution in spontaneous hypoglycemia and in labile diabetics on insulin or oral hypoglycemics.
- Thyrotoxicosis: Masks certain clinical signs of hyperthyroidism such as tachycardia; avoid abrupt withdrawal, which might precipitate thyroid storm.
- Beta-blocker cross-hypersensitivity: Caution in patients with known hypersensitivity to other beta-adrenoceptor blocking agents.
- Angle-closure glaucoma: Little or no effect on the pupil, so in a closed angle it must be used with a miotic and not alone; the immediate objective remains reopening the angle.
- Anaphylaxis risk: Patients with a history of atopy or severe anaphylaxis may be more reactive on repeat allergen challenge and may be unresponsive to the usual epinephrine doses.
- Muscle weakness: Beta-blockade may potentiate myasthenic symptoms including diplopia, ptosis, and generalized weakness.
- Concomitant oral beta-blockers: Additive systemic beta-blockade; use with caution.
- Catecholamine-depleting drugs: Additive effects with reserpine may produce hypotension or marked bradycardia, with vertigo, syncope, or postural hypotension.
Common Side Effects
- Ocular: Transient eye irritation, burning, tearing, conjunctival hyperemia, and edema, in about 1 of 4 patients.
- Occasional ocular effects: Blurred and cloudy vision, photophobia, decreased night vision, ptosis, blepharoconjunctivitis, abnormal corneal staining, and changes in corneal sensitivity.
- Systemic: Bradycardia and decreased blood pressure, as characteristic of nonselective adrenergic blocking agents.
- Occasional systemic events: Cardiac arrhythmia, heart palpitation, dyspnea, asthenia, headache, dizziness, insomnia, sinusitis, and taste perversion.
- Beta-blocker class reactions: Reported with ophthalmic use of nonselective beta-adrenergic blockers, comprising arrhythmia, syncope, heart block, cerebrovascular accident, cerebral ischemia, congestive heart failure, palpitation, nausea, depression, hypersensitivity rash, bronchospasm predominantly in pre-existing bronchospastic disease, respiratory failure, masked hypoglycemia symptoms in insulin-dependent diabetics, keratitis, blepharoptosis, refractive changes, diplopia, and ptosis.
Pregnancy & LactationPregnancy: No adequate and well-controlled studies in pregnant women; use only if the potential benefit justifies the potential risk to the fetus. In animals, increased resorptions and decreased fetal weights occurred in rabbits and rats at maternally toxic doses approximately 1052 and 5264 times the maximum recommended human oral dose, and a dose-related increase in wavy ribs appeared in rat fetuses at approximately 212 times that dose.
Lactation: Excretion in human milk is unknown, although carteolol is excreted in breast milk in animal studies; exercise caution in nursing mothers.
Pediatric UseSafety and effectiveness in pediatric patients have not been established.