Brimonidine + Timolol

Thông tin thuốc gốc
Chỉ định và Liều dùng
Ocular hypertension, Open-angle glaucoma
Adult: Available preparation:
Brimonidine 2 mg and timolol 5 mg per mL of eye drop solution

For the reduction of elevated IOP in patients who are inadequately responsive to topical β-blockers: Instil 1 drop into the affected eye(s) bid, approx 12 hours apart.
Chống chỉ định
Reactive airway disease including bronchial asthma or history of bronchial asthma, severe COPD; sick sinus syndrome, sinus bradycardia, sinoatrial block, 2nd- or 3rd-degree AV block not controlled with a pacemaker, overt cardiac failure, cardiogenic shock. Children <2 years. Concomitant use with antidepressants which affect noradrenergic transmission (e.g. TCAs, mianserin); concomitant use with or within 14 days of discontinuing MAOI therapy.
Thận trọng
Patient with CV disease (e.g. CHD, Prinzmetal's angina, compensated cardiac failure, 1st-degree heart block), severe peripheral circulatory disorder (e.g. severe forms of Raynaud's syndrome); mild or moderate COPD, history of bronchospastic disease (other than bronchial asthma); spontaneous hypoglycaemia, diabetes mellitus (particularly labile diabetes), metabolic acidosis, untreated phaeochromocytoma; myasthenia gravis, corneal disease, history of atopy or severe anaphylactic reaction to variety of allergens; dry eye, depression, cerebrovascular insufficiency, orthostatic hypotension, thromboangiitis obliterans. Patients undergoing surgery. Avoid abrupt withdrawal (particularly in patients with suspected thyrotoxicosis). Timolol may mask the signs and symptoms of hypoglycaemia and hyperthyroidism (particularly tachycardia). Renal and hepatic impairment. Pregnancy and lactation.
Tác dụng không mong muốn
Significant: Allergic conjunctivitis, allergic blepharitis, delayed ocular hypersensitivity reactions, dry eye; choroidal detachment (post-filtration procedures); may precipitate or potentiate symptoms of vascular insufficiency, may aggravate symptoms of myasthenia gravis.
Cardiac disorders: Palpitations, bradycardia, tachycardia, arrhythmia.
Eye disorders: Conjunctival hyperaemia, burning or stinging sensation in the eye, corneal erosion, superficial punctate keratitis, conjunctival folliculosis, visual disturbance, epiphora, foreign body sensation, eye discharge, pain, pruritus, or irritation; eyelid oedema, pruritus, or erythema; blurred vision.
Gastrointestinal disorders: Oral dryness.
General disorders and administration site conditions: Asthenia.
Nervous system disorders: Headache, somnolence.
Psychiatric disorders: Depression.
Vascular disorders: Hypertension, hypotension.
Potentially Fatal: Severe respiratory reactions including bronchospasm in patients with asthma. Rarely, cardiac failure.
Thông tin tư vấn bệnh nhân
Remove contact lenses before administration and reinsert them after at least 15 minutes. This drug may cause transient blurring of vision, visual disturbance, fatigue, and/or drowsiness, if affected, do not drive or operate machinery.
Chỉ số theo dõi
Monitor IOP and blood pressure. Assess for signs of systemic effects of β-blockade.
Tương tác
Brimonidine: May diminish therapeutic effect with mianserin and TCAs. MAOIs may interfere with the metabolism of brimonidine, which may result in increased systemic side effects (e.g. hypotension). Concomitant use with CNS depressants (e.g. barbiturates, sedatives, opiates, anaesthetics) may produce additive or potentiated CNS depressant effects.
Timolol: Effect on IOP or the known effects of systemic β-blockade may be potentiated when given with systemic (e.g. oral or IV) β-adrenergic blockers. Potential additive effects leading to hypotension and/or marked bradycardia with oral or IV Ca channel blockers, antiarrhythmics (including amiodarone), digitalis glycosides, parasympathomimetics, reserpine, or guanethidine. May block the systemic β-agonist effect of epinephrine; concomitant use of ophthalmic timolol and epinephrine may result in mydriasis. May enhance the hypertensive reaction to the sudden withdrawal of clonidine. Enhanced systemic β-blockade (e.g. decreased heart rate) with CYP2D6 inhibitors (e.g. fluoxetine, paroxetine, quinidine). May attenuate compensatory tachycardia and may increase the risk of hypotension with anaesthetics. May enhance the hypoglycaemic effects of antidiabetic agents.
Tương tác với thức ăn
Brimonidine: May have additive or potentiated CNS depressant effect with alcohol.
Tác dụng
Mechanism of Action: Brimonidine is a selective α2-adrenergic agonist. It is suspected to reduce IOP by decreasing aqueous humour production and enhancing uveoscleral outflow.
Timolol is a non-selective β-adrenergic receptor blocker and has no significant intrinsic sympathomimetic, direct myocardial depressant, or membrane-stabilising activity. It reduces IOP by decreasing aqueous humour production or by possibly increasing the outflow of aqueous humour.
Onset: Timolol: IOP reduction: 30 minutes.
Duration: Timolol: 24 hours.
Absorption: Brimonidine: Time to peak plasma concentration: 1-4 hours.
Timolol: Time to peak plasma concentration: 1-3 hours.
Distribution: Brimonidine: Plasma protein binding: Approx 29%.
Timolol: Enters breast milk. Plasma protein binding: Approx 60%.
Metabolism: Brimonidine: Extensively metabolised in the liver.
Timolol: Partially metabolised in the liver.
Excretion: Brimonidine: Via urine. Elimination half-life: Approx 3 hours.
Timolol: Elimination half-life: 4 hours.
Đặc tính

Chemical Structure Image

Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 2435, Brimonidine. Accessed Nov. 28, 2022.

Chemical Structure Image

Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 33624, Timolol. Accessed Nov. 22, 2023.

Bảo quản
Store between 15-25°C. Protect from light.
Phân loại MIMS
Thuốc trị tăng nhãn áp
Phân loại ATC
S01ED51 - timolol, combinations ; Belongs to the class of beta blocking agents. Used in the treatment of glaucoma.
Tài liệu tham khảo
Allergan New Zealand Limited. Brimonidine Tartrate 0.2% and Timolol (as Maleate) 0.5% Eye Drops data sheet April 2019. Medsafe. Accessed 17/11/2022.

Anon. Brimonidine (Ophthalmic). Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. Accessed 17/11/2022.

Anon. Brimonidine and Timolol. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. Accessed 17/11/2022.

Anon. Timolol (Ophthalmic). Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. Accessed 17/11/2022.

Brimonidine Tartrate and Timolol Maleate Solution/Drops (Pacific Pharma, Inc.). DailyMed. Source: U.S. National Library of Medicine. Accessed 17/11/2022.

Buckingham R (ed). Brimonidine Tartrate. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. Accessed 22/11/2022.

Buckingham R (ed). Timolol Maleate. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. Accessed 17/11/2022.

Combigan 2 mg/mL + 5 mg/mL Eye Drops, Solution (AbbVie Ltd). MHRA. Accessed 17/11/2022.

Combigan Eye Drops (Allergan Malaysia Sdn Bhd). National Pharmaceutical Regulatory Agency - Ministry of Health Malaysia. Accessed 17/11/2022.

Joint Formulary Committee. Brimonidine with Timolol. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. Accessed 17/11/2022.

Preston CL (ed). Alpha-2 Agonists; Ophthalmic + Miscellaneous. Stockley’s Drug Interactions [online]. London. Pharmaceutical Press. Accessed 23/11/2022.

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