Clinical medicine profile
Brimonidine/ Timolol
Therapeutic agent (verify pharmacological class)
- Route
- OPHTHALMIC
- Schedule
- POM
- ATC
- Not assigned
- PPB status
- registered
This profile needs source confirmation
Some sections contain general class guidance rather than medicine-specific evidence. Confirm prescribing decisions against the current SmPC and Kenya STG/EML.
Safety essentials
The information most likely to change a prescribing or dispensing decision.
Contraindications
- [From component Timolol maleate] 4 CONTRAINDICATIONS Dorzolamide hydrochloride and timolol maleate ophthalmic solution is contraindicated in patients with: Bronchial asthma or a history of bronchial asthma, severe chronic obstructive pulmonary disease.
- ( 4.1 ) Sinus bradycardia, second or third degree atrioventricular block, overt cardiac failure, cardiogenic shock.
- ( 4.2 ) Hypersensitivity to any component of this product.
- ( 4.3 , 5.3 ) 4.1 Asthma, COPD Dorzolamide hydrochloride and timolol maleate ophthalmic solution is contraindicated in patients with bronchial asthma, a history of bronchial asthma, or severe chronic obstructive pulmonary disease [see Warnings and Precautions ( 5.1 )] . 4.2 Sinus Bradycardia, AV Block, Cardiac Failure, Cardiogenic Shock Dorzolamide hydrochloride and timolol maleate ophthalmic solution is contraindicated in patients with sinus bradycardia, second or third degree atrioventricular block, overt cardiac failure, and cardiogenic shock [see Warnings and Precautions ( 5.2 )] . 4.3 Hypersensitivity Dorzolamide hydrochloride and timolol maleate ophthalmic solution is contraindicated in patients who are hypersensitive to any component of this product [see Warnings and Precautions ( 5.3 )] .
Precautions
- Warnings For external use only Do not use if solution changes color or becomes cloudy Stop use and ask a doctor if you experience eye pain, changes in vision, continued redness or irritation of the eye condition worsens or persists for more than 3 days If pregnant or breast-feeding, ask a health professional before use.
- Keep out of reach of children.
- If swallowed, get medical help or contact a Poison Control Center right away.
Dosing matrix
Population and organ-function guidance, shown together for faster comparison.
Directions adults and children 5 years of age and over: instill 1 drop in the affected eye(s) every 6-8 hours do not use more than 4 times daily remove contact lenses before use wait at least 10 minutes before re-inserting contact lenses after use if using other ophthalmic products while using this product, wait at least 5 minutes between each product to avoid contamination, do not touch tip of container to any surface replace cap after each use children under 5 years of age: consult a doctor
See label paediatric section if present; otherwise use paediatric formulary — do not extrapolate adult doses.
Review renal impairment dosing; many agents need CrCl/eGFR adjustment.
- CrCl 0–120: Confirm renal dosing in product SmPC / primary label.
Review hepatic impairment dosing; monitor LFTs if agent is hepatically cleared or hepatotoxic.
Use, effects & interactions
Indications
- Use relieves redness of the eye due to minor eye irritations Clinical selection for Brimonidine/ Timolol should follow culture results where relevant, Kenya STG/EML recommendations, and the current product SmPC.
- Class context: Therapeutic agent (verify pharmacological class).
- Confirm site-specific dose, duration and monitoring before prescribing.
Adverse effects
- [From component Timolol maleate] 6 ADVERSE REACTIONS The most frequently reported adverse reactions were taste perversion (bitter, sour, or unusual taste) or ocular burning and/or stinging in up to 30% of patients.
- Conjunctival hyperemia, blurred vision, superficial punctate keratitis or eye itching were reported between 5 to 15% of patients.
- ( 6 ) To report SUSPECTED ADVERSE REACTIONS, contact at 1-833-856-0880 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch . 6.1 Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice.
- Dorzolamide hydrochloride and timolol maleate ophthalmic solution was evaluated in 1,035 patients with elevated intraocular pressure treated for open-angle glaucoma or ocular hypertension for up to 15 months.
- Approximately 5% of all patients discontinued therapy because of adverse reactions.
- The most frequently reported adverse reactions occurring in up to 30% of patients were taste perversion (bitter, sour, or unusual taste) or ocular burning and/or stinging.
- The following adverse reactions were reported in 5 to15% of patients: conjunctival hyperemia, blurred vision, superficial punctate keratitis or eye itching.
- The following adverse reactions were reported in 1 to 5% of patients: abdominal pain, back pain, blepharitis, bronchitis, cloudy vision, conjunctival discharge, conjunctival edema, conjunctival follicles, conjunctival injection, conjunctivitis, corneal erosion, corneal staining, cortical lens opacity, cough, dizziness, dryness of eyes, dyspepsia, eye debris, eye discharge, eye pain, eye tearing, eyelid edema, eyelid erythema, eyelid exudate/scales, eyelid pain or discomfort, foreign body sensation, glaucomatous cupping, headache, hypertension, influenza, lens nucleus coloration, lens opacity, nausea, nuclear lens opacity, pharyngitis, post-subcapsular cataract, sinusitis, upper respiratory infection, urinary tract infection, visual field defect, vitreous detachment.
- Other adverse reactions that have been reported with the individual components are listed below: Dorzolamide 2% Angioedema, asthenia/fatigue, bronchospasm, contact dermatitis, epistaxis, eyelid crusting, ocular discomfort, photophobia, signs and symptoms of ocular allergic reaction, transient myopia.
- Timolol (ocular administration) Body as a Whole: Asthenia/fatigue
- Cardiovascular: Arrhythmia, syncope, cerebral ischemia, worsening of angina pectoris, palpitation, cardiac arrest, pulmonary edema, edema, claudication, Raynaud’s phenomenon, and cold hands and feet
- Digestive: Anorexia, abdominal pain
- Immunologic: Systemic lupus erythematosus
- Nervous System/Psychiatric: Increase in signs and symptoms of myasthenia gravis, somnolence, insomnia, nightmares, behavioral changes and psychic disturbances including confusion, hallucinations, anxiety, disorientation, nervousness, and memory loss
Drug interactions
Open multi-drug checker ↗- Fixed-dose/multi-ingredient product.
- Clinical details partially inherited from component monographs: Timolol maleate.
- Confirm combination SmPC for exact dosing.
Mechanism & disposition
Combination product.
Read complete mechanism
Combination product. Component mechanism (Timolol maleate): 12.1 Mechanism of Action Dorzolamide hydrochloride and timolol maleate ophthalmic solution is comprised of two components: Dorzolamide hydrochloride and timolol maleate. Each of these two components decreases elevated intraocular pressure, whether or not associated with glaucoma, by reducing aqueous humor secretion. Elevated intraocular pressure is a major risk factor in the pathogenesis of optic nerve damage and glaucomatous visual field loss. The higher the level of intraocular pressure, the greater the likelihood of glaucomatous field loss and optic nerve damage. Dorzolamide hydrochloride is an inhibitor of human carbonic anhydrase II. Inhibition of carbonic anhydrase in the ciliary processes of the eye decreases aqueous humor secretion, presumably by slowing the formation of bicarbonate ions with subsequent reduction in sodium and fluid transport. Timolol maleate is a beta1 and beta2 (non-selective) adrenergic receptor blocking agent that does not have significant intrinsic sympathomimetic, direct myocardial depressant, or local anesthetic (membrane-stabilizing) activity. The combined effect of these two agents administered as dorzolamide hydrochloride and timolol maleate ophthalmic solution twice daily results in additional intraocular pressure reduction compared to either component administered alone, but the reduction is not as much as when dorzolamide administered three times daily and timolol twice daily are administered concomitantly. [See Clinical Studies ( 14 )].
Product-specific
Product-specific
OPHTHALMIC
are product-specific. Consider food effects, protein binding, hepatic CYP/UGT
when adjusting for organ impairment, age and drug interactions. Verify parameters in the current SmPC.
Pregnancy, lactation & diet
[From component Timolol maleate] 8.1 Pregnancy Teratogenic Effects . Developmental toxicity studies with dorzolamide hydrochloride in rabbits at oral doses of ≥ 2.5 mg/kg/day (37 times the recommended human ophthalmic dose) revealed malformations of the vertebral bodies. These malformations occurred at doses that caused metabolic acidosis with decreased body weight gain in dams and decreased fetal weights. No treatment-related malformations were seen at 1 mg/kg/day (15 times the recommended human ophthalmic dose). Teratogenicity studies with timolol in mice, rats, and rabbits at oral doses up to 50 mg/kg/day (7,000 times the systemic exposure following the maximum recommended human ophthalmic dose) demonstrated no evidence of fetal malformations. Although delayed fetal ossification was observed at this dose in rats, there were no adverse effects on postnatal development of offspring. Doses of 1,000 mg/kg/day (142,000 times the systemic exposure following the maximum recommended human ophthalmic dose) were maternotoxic in mice and resulted in an increased number of fetal resorptions. Increased fetal resorptions were also seen in rabbits at doses of 14,000 times the systemic exposure following the maximum recommended human ophthalmic dose, in this case without apparent maternotoxicity. There are no adequate and well-controlled studies in pregnant women. Dorzolamide hydrochloride and timolol maleate ophthalmic solution should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.
[From component Timolol maleate] 8.3 Nursing Mothers It is not known whether dorzolamide is excreted in human milk. Timolol maleate has been detected in human milk following oral and ophthalmic drug administration. Because of the potential for serious adverse reactions from dorzolamide hydrochloride and timolol maleate ophthalmic solution in nursing infants, a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother.
Brands & loaded prices
| Brand | Manufacturer | Pack | Observed price |
|---|---|---|---|
| COMBIGAN EYE | Not recorded | DROPS 5ML | KES 1,812.45Daima Chemist price-list reference ↗ Source date not recorded · verify current price |
Sources & review state
Decision support only. Confirm patient-specific decisions against the current product SmPC, Kenya STG/EML, and professional judgement.