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Medical Disclaimer: This information is for educational purposes only and is not a substitute for professional medical advice.
Brimonidine Tartrate And Timolol Maleate
Brand Name
Brimonidine Tartrate/timolol Maleate
Generic Name
Brimonidine Tartrate And Timolol Maleate
Active Ingredient
BrimonidineCategory
Carbonic Anhydrase Inhibitor [EPC]
Salt Form
Tartrate
Variants
2
References used for this content
This page is for informational purposes only and does not replace medical advice. Before using any prescription or over-the-counter medication for Brimonidine Tartrate/timolol Maleate, you must consult a qualified healthcare professional.
Detailed information about Brimonidine Tartrate/timolol Maleate
Brimonidine is a selective alpha-2 adrenergic agonist used primarily to lower intraocular pressure in patients with open-angle glaucoma or ocular hypertension, and topically to reduce facial erythema associated with rosacea.
Dosage for Brimonidine varies significantly based on the condition being treated and the specific formulation prescribed.
Brimonidine is generally not approved for use in children under the age of 2 years. In fact, it is strictly contraindicated in neonates and infants due to the risk of severe central nervous system (CNS) depression, including lethargy, hypotonia (low muscle tone), hypothermia, and respiratory distress. For children aged 2 to 7 years, use is generally discouraged and must be monitored with extreme caution by a specialist, as systemic absorption can lead to significant somnolence (extreme sleepiness).
Brimonidine has not been extensively studied in patients with impaired kidney function. Because the drug is primarily excreted through the urine, healthcare providers typically exercise caution when prescribing it to patients with moderate to severe renal impairment. No specific dose adjustment formulas are currently standardized, but close monitoring for systemic side effects is required.
As the liver is the primary site of Brimonidine metabolism, patients with hepatic impairment (liver disease) may process the drug more slowly. This could lead to higher systemic levels. Healthcare providers will evaluate the risk-benefit ratio and may monitor these patients more frequently for signs of hypotension or sedation.
Clinical trials have shown no overall differences in safety or effectiveness between elderly and younger patients. However, older adults may be more sensitive to the systemic effects of alpha-2 agonists, such as orthostatic hypotension (a drop in blood pressure when standing up). Dosage remains standard, but monitoring is advised.
If you miss a dose of Brimonidine, take it as soon as you remember. However, if it is nearly time for your next scheduled dose, skip the missed dose and return to your regular routine. Do not double the dose to make up for a missed one. Consistency is key, especially in managing glaucoma, where maintaining stable intraocular pressure is vital for preventing vision loss.
Systemic overdose of Brimonidine is rare with ocular use but can occur if the medication is accidentally swallowed, particularly by children. Symptoms of overdose include:
In case of suspected overdose, contact your local poison control center or seek emergency medical attention immediately. Treatment is generally supportive and may require hospitalization to monitor cardiac and respiratory function.
> Important: Follow your healthcare provider's dosing instructions. Do not adjust your dose without medical guidance.
Side effects of Brimonidine can vary based on whether the drug is applied to the eye or the skin. For ophthalmic use, the most frequently reported side effects include:
Brimonidine is a powerful medication that affects both the autonomic nervous system and localized tissue. It is essential to understand that while it is applied topically (to the eye or skin), systemic absorption can occur, leading to effects throughout the body. Patients with pre-existing cardiovascular conditions, depression, or vascular insufficiency must use this medication with heightened awareness.
No FDA black box warnings for Brimonidine. However, the manufacturer and the FDA provide strong warnings regarding its use in the pediatric population. It is strictly contraindicated in children under 2 years of age due to the high risk of systemic toxicity.
There are certain conditions and scenarios where Brimonidine must never be used due to the risk of life-threatening complications:
Brimonidine is classified as Pregnancy Category B by the FDA. This means that animal reproduction studies have failed to demonstrate a risk to the fetus, but there are no adequate and well-controlled studies in pregnant women.
Brimonidine is a highly selective alpha-2 adrenergic receptor agonist. Its molecular mechanism involves the activation of Gi-protein coupled receptors. When Brimonidine binds to these receptors on the ciliary body of the eye, it inhibits the activity of adenylate cyclase. This leads to a decrease in intracellular cyclic AMP (cAMP), which in turn reduces the production of aqueous humor by the ciliary processes. Additionally, Brimonidine increases uveoscleral outflow by inducing the release of prostaglandins and changing the permeability of the uveoscleral tissues. In the skin, its action on alpha-2 receptors in vascular smooth muscle causes direct vasoconstriction of small arteries.
Common questions about Brimonidine Tartrate/timolol Maleate
Brimonidine is primarily used for two distinct medical purposes depending on its formulation. In the form of eye drops, it is prescribed to lower high pressure inside the eye in patients with open-angle glaucoma or ocular hypertension. When used as a topical gel, it is indicated for the treatment of persistent facial redness (erythema) caused by rosacea in adults. Additionally, a very low-dose over-the-counter version is used to relieve general eye redness. It works by reducing fluid production in the eye and constricting blood vessels in the skin. Your doctor will determine which formulation is appropriate for your specific diagnosis.
The most common side effects associated with Brimonidine eye drops include dry mouth, eye redness, and a temporary burning or stinging sensation upon application. Some patients also report feeling fatigued, having a headache, or experiencing blurred vision. For those using the topical gel for rosacea, the most frequent side effects are skin flushing, burning sensations, and a potential 'rebound' worsening of facial redness. Most of these effects are mild, but if they persist or become severe, you should contact your healthcare provider. It is important to note that many of the ocular side effects, like dry mouth, are due to small amounts of the drug entering the bloodstream.
It is generally advised to limit or avoid alcohol consumption while using Brimonidine. Brimonidine is an alpha-2 adrenergic agonist that can have sedative effects on the central nervous system, and alcohol is a known CNS depressant. When used together, they can have an additive effect, leading to increased drowsiness, dizziness, and impaired mental alertness. This can be particularly dangerous if you are driving or operating machinery. Furthermore, alcohol can sometimes affect blood pressure, which may complicate the management of conditions for which Brimonidine is prescribed. Always discuss your alcohol intake with your doctor when starting a new medication.
Brimonidine is classified as FDA Pregnancy Category B, meaning that while animal studies have not shown harm to the fetus, there is a lack of comprehensive data from human clinical trials. Because of this, it should only be used during pregnancy if the potential benefit to the mother justifies the potential risk to the developing baby. If you are pregnant or planning to become pregnant, you must discuss alternative treatments or the necessity of Brimonidine with your obstetrician and ophthalmologist. They may recommend specific techniques, such as punctal occlusion, to minimize systemic absorption of the eye drops. Safety during the first trimester is a particular point of clinical caution.
The time it takes for Brimonidine to work depends on the condition being treated. For reducing eye pressure in glaucoma, the effect typically begins within 1 to 2 hours, with the maximum pressure-lowering effect occurring about 2 hours after the drop is administered. For treating facial redness in rosacea, the topical gel usually begins to show visible results within 30 minutes to an hour, with the peak effect seen around 3 to 6 hours after application. The effects are not permanent; eye drops usually need to be used three times daily, and the skin gel is typically applied once every 24 hours to maintain the therapeutic benefit.
You should never stop taking Brimonidine eye drops suddenly without consulting your ophthalmologist first. For patients with glaucoma, stopping the medication abruptly can cause a rapid and significant increase in intraocular pressure, which can lead to irreversible damage to the optic nerve and permanent vision loss. If you are experiencing side effects that make it difficult to continue the medication, your doctor will likely transition you to a different class of drug to ensure your eye pressure remains controlled. For the topical gel used for rosacea, stopping the medication will generally result in the return of facial redness, but it does not carry the same risk of permanent damage as stopping glaucoma drops.
If you miss a dose of Brimonidine, you should apply it as soon as you remember. However, if it is almost time for your next scheduled dose, you should skip the missed dose and simply continue with your regular dosing schedule. You should never apply a double dose of the eye drops or the gel to make up for a missed application, as this increases the risk of systemic side effects like low blood pressure or extreme drowsiness. Setting a daily alarm or using a medication tracking app can be very helpful in maintaining the consistent schedule required for effective glaucoma management. If you miss multiple doses, contact your doctor for further instructions.
Weight gain is not a recognized or common side effect of Brimonidine based on clinical trial data and post-marketing surveillance. The medication primarily affects the adrenergic system to control eye pressure or blood vessel diameter and does not typically interfere with metabolic processes or appetite in a way that would lead to weight changes. If you experience unexpected weight gain while taking Brimonidine, it is likely due to other factors, such as lifestyle changes, other medications, or an underlying medical condition. You should discuss any significant changes in your weight with your healthcare provider to determine the actual cause and ensure proper management.
Brimonidine can interact with several other types of medications, so it is vital to provide your doctor with a full list of everything you take. It is particularly important to mention if you are taking blood pressure medications, heart medications (like digoxin), antidepressants (especially MAO inhibitors or tricyclic antidepressants), or any drugs that cause sleepiness. When using other eye drops, you should wait at least 5 to 10 minutes between applying Brimonidine and the other medication to prevent the first drop from being washed out. Your doctor will coordinate your treatment plan to avoid harmful interactions and ensure that all your medications work effectively together.
Yes, Brimonidine Tartrate is widely available as a generic medication in several concentrations, including the 0.15% and 0.2% ophthalmic solutions. Generic versions are typically much more cost-effective than brand-name versions like Alphagan P or Mirvaso. To be FDA-approved, a generic version must be 'bioequivalent' to the brand-name drug, meaning it has the same active ingredient and works in the same way. However, some patients may find that the inactive ingredients or preservatives in the generic version differ slightly from the brand name, which can occasionally affect how the eye feels. You should discuss with your pharmacist and doctor whether the generic version is suitable for your needs.
Other drugs with the same active ingredient (Brimonidine)
These effects may occur in a significant minority of patients and should be discussed with a doctor if they become bothersome:
Rarely, patients may experience more unusual reactions:
> Warning: Stop taking Brimonidine and call your doctor immediately if you experience any of these serious reactions.
With prolonged use, particularly for glaucoma, patients may develop allergic conjunctivitis or blepharoconjunctivitis. This is a delayed hypersensitivity reaction that can occur anywhere from 3 to 9 months after starting the medication. Symptoms include red, itchy, and swollen eyelids. If this occurs, the medication usually must be discontinued, as the reaction will likely recur if the drug is restarted.
Another long-term consideration is the potential for tachyphylaxis, where the drug's effectiveness in lowering eye pressure may diminish over time in some patients, necessitating a change in treatment regimen.
There are currently no FDA black box warnings for Brimonidine. However, the contraindication in children under 2 years of age is considered a critical safety warning that carries similar weight in clinical practice. The risk of life-threatening respiratory depression in infants is the most significant safety concern associated with this active ingredient.
Report any unusual symptoms to your healthcare provider.
Regular follow-up appointments are mandatory when using Brimonidine for glaucoma. Your ophthalmologist will perform the following:
Brimonidine may cause fatigue, drowsiness, or blurred vision in some individuals. These effects can impair your ability to drive or operate heavy machinery safely. It is recommended to wait and see how the medication affects you before engaging in these activities. If you experience significant somnolence, avoid driving entirely and consult your doctor.
Alcohol is a central nervous system (CNS) depressant. Since Brimonidine can also have sedative effects, consuming alcohol while taking this medication may lead to an additive effect, significantly increasing drowsiness and impairing coordination. It is advised to limit or avoid alcohol consumption during treatment.
For glaucoma treatment, Brimonidine must not be stopped abruptly unless directed by a doctor, as this can lead to a 'rebound' spike in eye pressure, which can permanently damage the optic nerve. If you need to stop the medication due to an allergic reaction, your doctor will provide an alternative treatment immediately. For rosacea treatment, stopping the gel may result in the return of facial redness to its baseline level.
> Important: Discuss all your medical conditions with your healthcare provider before starting Brimonidine.
There are no known significant interactions between Brimonidine and specific foods. However, general health factors apply:
Brimonidine is not known to significantly interfere with common laboratory tests, such as blood chemistry panels or urinalysis. However, always inform your laboratory technician and physician of all medications you are taking.
> Important: Tell your doctor about ALL medications, supplements, and herbal products you are taking.
These conditions require a careful risk-benefit analysis by a healthcare professional:
There is a potential for cross-sensitivity between Brimonidine and other alpha-2 adrenergic agonists, such as apraclonidine (Iopidine) or clonidine. If you have had a severe reaction to one of these medications, you should inform your doctor before starting Brimonidine, as you may be at a higher risk for a similar reaction.
> Important: Your healthcare provider will evaluate your complete medical history before prescribing Brimonidine.
As emphasized throughout this guide, pediatric use is the most critical safety area for Brimonidine.
Patients over the age of 65 represent the largest group using Brimonidine for glaucoma.
Brimonidine has not been studied in patients with renal impairment. Since the kidneys are responsible for 75% of the drug's excretion, patients with a GFR (Glomerular Filtration Rate) below 30 mL/min should be monitored closely for signs of systemic toxicity, such as extreme lethargy or low blood pressure.
Patients with liver cirrhosis or other forms of hepatic impairment may have reduced ability to metabolize Brimonidine. This can lead to a longer half-life and higher peak plasma concentrations. Use with caution in patients with Child-Pugh Class B or C impairment.
> Important: Special populations require individualized medical assessment.
| Parameter | Value |
|---|---|
| Bioavailability | Low (Systemic) / High (Local) |
| Protein Binding | ~29% |
| Half-life | 2 - 3 hours (Systemic) |
| Tmax | 1 - 4 hours (Ocular) |
| Metabolism | Hepatic (Aldehyde Oxidase / CYP) |
| Excretion | Renal (75%) |
Brimonidine is classified therapeutically as an Antiglaucoma Agent and a Selective Alpha-2 Adrenergic Agonist. Within the context of the EPC (Established Pharmacologic Class) system, it is often grouped with other glaucoma medications, though it is distinct from Carbonic Anhydrase Inhibitors and Beta-Blockers. Related medications include Apraclonidine and Clonidine.