Formulary
Timolol maleate: Indications, Dosing, Side Effects and Interactions
Timolol maleate clinical drug profile including indications, dosing, side effects, cautions and interactions.
MedNext Academy | 5 min read
Timolol maleate: Indications, Dosing, Side Effects and Interactions
Timolol maleate clinical drug profile including indications, dosing, side effects, cautions and interactions.
Indications and dose
**Hypertension**
- **Adult** (By Mouth): Initially 10 mg daily in 1-2 divided doses, then increased if necessary up to 60 mg daily, doses to be increased gradually. Doses above 30 mg daily given in divided doses, usual maintenance 10-30 mg daily; maximum 60 mg per day.
**Angina**
- **Adult** (By Mouth): Initially 5 mg twice daily, then increased in steps of 10 mg daily (max. per dose 30 mg twice daily), to be increased every 3-4 days.
**Prophylaxis after myocardial infarction**
- **Adult** (By Mouth): Initially 5 mg twice daily for 2 days, then increased if tolerated to 10 mg twice daily.
**Migraine prophylaxis**
- **Adult** (By Mouth): 10-20 mg daily in 1-2 divided doses.
**Chronic open-angle glaucoma,Ocular hypertension**
- **Adult** (To The Eye): Apply twice daily.
**Reduction of intra-ocular pressure in primary open-angle glaucoma**
- **Adult** (To The Eye): Apply once daily, to be applied in the morning.
**Primary congenital and primary juvenile glaucoma [for a transitional period, before surgery or following failed surgery] for timolol maleate**
- **Child** (To the eye): Apply once daily; increased if necessary up to 2 drops daily, max. two drops daily into each affected eye. If applied twice daily, to be applied 12 hours apart. The lowest concentration solution that controls symptoms should be used.
**Reduction of intra-ocular pressure in primary and secondary glaucoma for Timoptol-LA**
- **Child** (To the eye): Apply once daily.
**Reduction of intra-ocular pressure primary and secondary glaucomas for Tiopex**
- **Child** (To the eye): Apply once daily, to be applied in the morning.
Cautions
For all beta-adrenoceptor blockers (systemic) Diabetes; first-degree AV block; history of obstructive airways disease (introduce cautiously); myasthenia gravis; portal hypertension (risk of deterioration in liver function); psoriasis; symptoms of hypoglycaemia may be masked; symptoms of thyrotoxicosis may be masked Cautions, further information Elderly Screening Tool of Older Persons' potentially inappropriate Prescriptions (STOPP) criteria to aid medication reviews (see Prescribing in the elderly for information). Potentially inappropriate: in combination with verapamil or diltiazem (risk of heart block) with bradycardia (heart rate less than 50 beats per minute), or second- or third-degree AV block (contra-indicated; risk of complete heart block, asystole) in diabetes mellitus patients with frequent hypoglycaemic episodes (risk of suppressing hypoglycaemic symptoms) if prescribed a non-selective beta-blocker (including topical beta-blockers) in a history of asthma requiring treatment (contra-indicated in asthma; risk of increased bronchospasm) Cautions For timolol maleate When used by eye Consider also cautions listed for systemically administered beta blockers; patients with corneal disease
Contraindications
For all beta-adrenoceptor blockers (systemic) Asthma; cardiogenic shock; hypotension; marked bradycardia; metabolic acidosis; phaeochromocytoma (apart from specific use with alpha-blockers); Prinzmetal's angina; second-degree AV block; severe peripheral arterial disease; sick sinus syndrome; third-degree AV block; uncontrolled heart failure Contra-indications, further information Bronchospasm Beta-blockers, including those considered to be cardioselective, should usually be avoided in patients with a history of asthma, bronchospasm or a history of obstructive airways disease. However, when there is no alternative, a cardioselective beta-blocker can be given to these patients with caution and under specialist supervision. In such cases the risk of inducing bronchospasm should be appreciated and appropriate precautions taken. Contra-indications For timolol maleate When used by eye Also consider contra-indications listed for systemically administered beta blockers; bradycardia; heart block
Side effects
For all beta-adrenoceptor blockers (systemic) Common or very common Abdominal discomfort; bradycardia; confusion; depression; diarrhoea; dizziness; dry eye (reversible on discontinuation); dyspnoea; erectile dysfunction; fatigue; headache; heart failure; nausea; paraesthesia; peripheral coldness; rash (reversible on discontinuation); Raynaud's phenomenon; sleep disorders; syncope; visual impairment; vomiting Uncommon Alopecia; atrioventricular block; bronchospasm Rare or very rare Hallucination; psoriasis exacerbated Side-effects, further information With administration by intravenous injection, excessive bradycardia can occur and may be countered with intravenous injection of atropine sulfate. Overdose Therapeutic overdosages with beta-blockers may cause lightheadedness, dizziness, and possibly syncope as a result of bradycardia and hypotension; heart failure may be precipitated or exacerbated. With administration by intravenous injection, excessive bradycardia can occur and may be countered with intravenous injection of atropine sulfate. For details on the management of poisoning, see Beta-blockers, under Emergency treatment of poisoning . Side-effects For timolol maleate General side-effects: Common or very common Eye disorders; eye inflammation; vision disorders Specific side-effects: Common or very common When used by eye (topical) Eye discomfort Rare or very rare With oral use Arthralgia; retroperitoneal fibrosis; skin reactions Frequency not known With oral use Angioedema; arrhythmia; asthenia; cardiac arrest; cerebrovascular insufficiency; chest pain; cough; cyanosis; drowsiness; dry mouth; eye irritation; gastrointestinal discomfort; hypoglycaemia; intermittent claudication exacerbated; memory loss; myalgia; myasthenia gravis; oedema; palpitations; psychotic disorder; sexual dysfunction; systemic lupus erythematosus (SLE); taste altered; vertigo Side-effects, further information Systemic absorption can follow topical application to the eyes; consider side-effects listed for systemically administered beta blockers.
Interactions
**Other interactions (12):**
- AZARGA contains brinzolamide, a carbonic anhydrase inhibitor and, although administered topically, is absorbed systemically.
- There is a potential for an additive effect on the known systemic effects of carbonic anhydrase inhibition in patients receiving an oral carbonic anhydrase inhibitor and brinzolamide eye drops.
- The concomitant administration of eye drops containing brinzolamide and oral carbonic anhydrase inhibitors is not recommended.
- The cytochrome P-450 isozymes responsible for metabolism of brinzolamide include CYP3A4 (main), CYP2A6, CYP2B6, CYP2C8 and CYP2C9.
- It is expected that inhibitors of CYP3A4 such as ketoconazole, itraconazole, clotrimazole, ritonavir and troleandomycin will inhibit the metabolism of brinzolamide by CYP3A4.
- Brinzolamide is not an inhibitor of cytochrome P-450 isozymes.
Pregnancy
For all beta-adrenoceptor blockers (systemic) Beta-blockers may cause intra-uterine growth restriction, neonatal hypoglycaemia, and bradycardia; the risk is greater in severe hypertension.
Breast feeding
For all beta-adrenoceptor blockers (systemic) With systemic use in the mother, infants should be monitored as there is a risk of possible toxicity due to beta-blockade. However, the amount of most beta-blockers present in milk is too small to affect infants. Breast feeding For timolol maleate Manufacturer advises avoidance.
Hepatic impairment
With oral use: Manufacturer advises caution. Dose adjustments With oral use: Manufacturer advises consider dose reduction.
Renal impairment
With oral use: Use with caution. M Dose adjustments With oral use: Consider dose reduction. M
Medicinal forms
Tablet,Drops,Gel
Clinical governance
**Author:** MedNext Clinical Team. **Clinical reviewer:** Dr Shameer Deen, MBBS, MS, MRCS. **Sources:** BNF, Indian Pharmacopoeia, CIMS India. **Correction:** Report errors at support@mednext.academy.
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