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Indications and Dosage
Ophthalmic
Ocular hypertension, Open-angle glaucoma Adult: As 1% solution: Instill 1 drop in the affected eye(s) bid. Oral Hypertension Adult: 2.5-30 mg/day, adjusted according to response. Oral Angina pectoris, Cardiac arrhythmias Adult: 2.5-30 mg/day, adjusted according to response.
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Renal Impairment
Oral:
Hypertension:
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Administration
Should be taken with food.
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Contraindications
AV block (2nd and 3rd degree), sinus bradycardia, sino-atrial block, sick sinus syndrome, overt cardiac failure, cardiogenic shock. Bronchospasm, bronchial asthma, severe COPD, pulmonary oedema.
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Special Precautions
Patients w/ 1st degree AV block, Raynaud's disease, untreated phaeochromocytoma, COPD, DM, myasthenia gravis. May mask symptoms of hyperthyroidism and hypoglycaemia. Abrupt withdrawal may precipitate a thyroid storm. Renal impairment. Pregnancy and lactation.
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Adverse Reactions
Bradycardia, hypotension, heart failure. GI and taste disturbances, headache, dizziness, insomnia and sinusitis, localized and generalized rash, pruritus. Ocular irritation (e.g. itching, tearing, redness), photophobia, blurred vision.
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Ophth: C
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Overdosage
Symptoms: Dizziness, headache, shortness of breath, symptomatic bradycardia, hypotension, bronchospasm, and acute cardiac failure. Management: Symptomatic and supportive treatment. In case of ocular overdose, the eyes should be flushed w/ water or saline soln.
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Drug Interactions
Coadministration w/ catecholamine-depleting drugs (e.g. reserpine), Ca channel blockers, antiarrhythmics (including amiodarone), digitalis glycosides, parasympathomimetics may cause additive effects e.g. hypotension and/or marked bradycardia. Mydriasis may occur w/ concomitant epinephrine.
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Action
Description:
Mechanism of Action: Carteolol is a non-cardioselective β-blocker w/ intrinsic sympathomimetic activity. It decreases aqueous humour production which causes intraocular pressure reduction. Pharmacokinetics: Absorption: Well absorbed from the GI tract. Bioavailability: Approx 84%. Time to peak plasma concentration: 1-4 hr. Distribution: Plasma protein binding: Approx 20-30%. Metabolism: Undergoes CYP2D6-mediated 8-hydroxylation to its active metabolite (8-hydroxycarteolol), and glucuronic acid conjugates of carteolol and 8-hydroxycarteolol. Excretion: Via urine: Approx 50-70% (as unchanged drug). Plasma half-life: 3-6 hr. |
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Storage
Store between 15-25°C. Protect from light.
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MIMS Class
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References
Anon. Carteolol (Ophthalmic): Drug information. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 25/11/2013. Buckingham R (ed). Carteolol Hydrochloride. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 25/11/2013. Carteolol Hydrochloride Solution (Alcon Laboratories, Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 25/11/2013. Wickersham RM. Carteolol Hydrochloride. Facts and Comparisons [online]. St. Louis, MO. Wolters Kluwer Clinical Drug Information, Inc. https://www.wolterskluwercdi.com/facts-comparisons-online/. Accessed 25/11/2013.
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