Brimonidine Tartrate Ophthalmic Solution

Overview:

Brimonidine tartrate ophthalmic solution is a medication that reduces intraocular pressure in patients with glaucoma or ocular hypertension. It decreases the production of aqueous humor, a clear fluid that fills the front portion of the eye. It is available in two strengths: 0.1 and 0.15 percent. The active component, Brimonidine tartrate, is an alpha agonist. It functions as a blood vessel constrictor in the eye. This helps decrease fluid production in the eye and lower intraocular pressure. The solution is administered as eye drops, and the recommended dosage depends on the respective patient and the severity of their condition. Common side effects of Brimonidine tartrate ophthalmic solution include a burning sensation in the eye, dry eyes, and eye irritation. It is important to follow the doctor’s instructions and use the drug exactly as prescribed.

How Does Brimonidine Tartrate Work?

Brimonidine tartrate belongs to a class of medications called alpha-2 agonists. They work by reducing the production of fluid in the eye. Brimonidine tartrate activates alpha-2 receptors in the cells that produce aqueous humor, the clear fluid, and helps maintain its shape. In an activated state, these receptors reduce the production of aqueous humor, which in turn decreases the pressure inside the eye. These receptors in the activated state also relax the eye muscles, which leads the eye to relax and the blood vessels in the eye to constrict. Thus, this mechanism decreases fluid production in the eye, which helps lower intraocular pressure.

In addition to reducing intraocular pressure, Brimonidine tartrate has more effects on the eye, such as reducing inflammation and decreasing oxidative stress. These additional results may also contribute to its ability to protect the optic nerve and restrict the progression of glaucoma.

Uses:

• Brimonidine eye drops are used alone or in combination with other drugs to lower pressure inside the eye caused by open-angle glaucoma or ocular (eye) hypertension.

• Brimonidine eye drops are also used to reduce the redness of the eye induced by minor eye irritations.

• Additional uses of Brimonidine tartrate ophthalmic solution may include reducing swelling in the eye and preventing or improving symptoms of ocular hypertension. However, better research is required to confirm the effectiveness of these potential uses.

Dosage:

The recommended dosage of Brimonidine tartrate solution eye drop is one drop of the solution in the affected eye three times a day, approximately eight hours separated. The ophthalmic solution can be used concomitantly with other topical eye drops used to lower intraocular pressure. If more than one topical ophthalmic eye drop solution is to be used, the other medications should be administered at least five minutes apart. The 0.1 percent strength is used once or twice a day, whereas the 0.15 percent strength eye drop is used once a day. Brimonidine tartrate is provided sterile in teal opaque plastic bottles. The medication is available in two strengths as follows-

1. 0.1 Percent -

• 5 mL in a 10 mL bottle.

• 10 mL in a 10 mL bottle.

• 15 mL in a 15 mL bottle.

1. 0.15 Percent -

• 5 mL in a 10 mL bottle.

• 10 mL in a 10 mL bottle.

• 15 mL in a 15 mL bottle.

The eye drops should be stored at 15 to 25 degreesCelsius (59 to 77 degrees Fahrenheit).

Warning:

Possibility of Vascular Insufficiency-

Brimonidine tartrate may potentiate syndromes associated with vascular insufficiency. It should be used with warning in patients with cerebral or coronary insufficiency, depression, and Raynaud’s phenomenon.

Severe Cardiovascular Diseases-

Even though Brimonidine tartrate ophthalmic solution has minimal impact on blood pressure, carefulness should be exercised in treating patients with severe cardiovascular disease.

Contamination of Topical Ophthalmic Products After Use-

Reports of bacterial keratitis related to using multiple-dose containers of topical ophthalmic products have been received. The containers get contaminated by patients who, in most cases, have a simultaneous corneal disease or a disruption of the ocular epithelial surface.

For Patients:

Learn About Glaucoma:

Glaucoma is a class of eye diseases that can cause vision loss or blindness if not treated properly. It damages a nerve in the back of the eye called the optic nerve. The symptoms can begin so slowly that they may be left unnoticed. The only way to diagnose glaucoma is to get a comprehensive dilated eye examination. Early diagnosis and treatment can often prevent damage and protect the vision. However, there is no more for glaucoma. There are various types of glaucoma, but the most common are open-angle glaucoma, angle-closure glaucoma, and congenital glaucoma.

Initially, glaucoma may not present with any symptoms. This is why half of the people with glaucoma do not even know they have it. Over the duration, the patient with glaucoma can slowly lose vision, generally starting with the peripheral vision — particularly the part of the vision that is closest to the nose. As it occurs so slowly, many people can not suggest that their vision is changing at first. However, as the disease worsens, the patient starts to notice that they can not see things off to the side anymore. If not treated, glaucoma can ultimately cause blindness.

Before Starting Brimonidine Tartrate:

A few things need to be considered before starting treatment with Brimonidine tartrate:

1. Tell the physician if there is an allergy, especially to medications or foods.

2. Tell the physician about all the ongoing medications, including prescription and non-prescription medications, and any vitamins or supplements.

3. Inform the physician if there are any medical conditions, mainly cardiovascular disease or a history of low blood pressure.

4. If pregnant, nursing, or planning to become pregnant, tell the physician before starting treatment with Brimonidine tartrate.

5. Follow the administration and dosage instructions provided by the physician. Do not take extra or less of the medication than directed.

6. If the dose of Brimonidine tartrate is missed, it should be taken as soon as remembered. If it is nearly time for the next dose, then skip that dose and take the next dose at the regular time. Avoid taking two doses of the drug at the same time.

7. Store Brimonidine tartrate at room temperature. Keep it away from moisture and heat. Keep the drug out of reach of children.

Why and When to Switch to Brimonidine Tartrate?

Several reasons a healthcare provider may recommend switching to Brimonidine tartrate:

• Inadequate IOP Control: If a patient's intraocular pressure is not well regulated with their current glaucoma drug, the healthcare provider may advise switching to Brimonidine tartrate or putting it into their ongoing treatment regimen.

• Adverse Effects: If a patient is undergoing adverse effects with their existing glaucoma medication, the healthcare provider may recommend switching to Brimonidine tartrate or putting it into their present treatment regimen.

• Interactions: If a glaucoma patient has a drug that interacts with their existing glaucoma medication, the healthcare provider may advise switching to Brimonidine tartrate or adding it to their existing treatment regimen.

• Convenience: If a patient has a problem remembering to take their medication or is experiencing difficulty administering their current medication, the healthcare provider may recommend changing to Brimonidine tartrate, which is available as an eye drop.

For Doctors

Indication:

Brimonidine tartrate ophthalmic solution is an alpha-adrenergic receptor agonist. It is indicated to reduce elevated intraocular pressure (IOP) in cases with open-angle glaucoma or ocular hypertension.

Pharmacology:

Brimonidine tartrate ophthalmic solution is a selective alpha-2 adrenergic receptor agonist, a topical intraocular pressure lowering agent. The solution is clear, greenish-yellow in color. Brimonidine tartrate appears as a pale yellow to off-white powder. It is soluble in both water and in the product vehicle.

Brimonidine tartrate ophthalmic solution 0.1 or 0.15 percent contains the active ingredient Brimonidine tartrate 0.1 or 0.15 percent. The inactive ingredients include sodium borate, sodium carboxymethylcellulose, boric acid, potassium chloride, calcium chloride, magnesium chloride, and sodium chloride.

Mechanism of Action:

Absorption:

Ocular administration of Brimonidine tartrate of either a 0.1 or 0.15 percent solution causes the plasma concentrations to peak within half to two and a half hours and decline with a systemic half-life of about two hours.

Metabolism:

Brimonidine tartrate is considerably metabolized by the liver.

Excretion:

The primary route of excretion of Brimonidine tartrate is through urine.

Warnings and Precautions:

Little information exists on the accidental ingestion of Brimonidine tartrate in adults. The only adverse reaction notified has been hypotension. Symptoms of Brimonidine tartrate overdose have been noted in neonates, infants, and children receiving the drug by accidental oral ingestion or as a part of medical treatment of congenital glaucoma.

Dosage Strength and Forms:

The Brimonidine tartrate ophthalmic solution contains 1 mg/mL or 1.5 mg/mL Brimonidine tartrate. It is available in two strengths 0.1 and 0.15 percent.

Dosage and Administration:

Brimonidine tartrate ophthalmic solution that is used to reduce pressure in the eye in people with glaucoma and ocular hypertension. The recommended dose is one drop of the solution in the affected eye three times daily, approximately eight hours apart. It can be used in combination with other eye drops to lower intraocular pressure, but it is important to maintain at least five minutes between the eye drops to permit proper absorption. It is important to follow the doctor’s advice and instructions before starting the medication.

Considerations for Administration:

Patients must be instructed that eye drops, if not handled properly or if the tip of the dispensing container reaches the eye or surrounding structures, can become contaminated by common bacteria that can cause ocular infections. Severe damage to the eye and succeeding blindness may result from using contaminated solutions. Replace the cap after using it. Do not use the solution if its color has changed or it has become cloudy. Do not use the product if it has expired. Patients should also be instructed that if they have developed an intercurrent ocular condition such as trauma or infection, they should directly seek their physician's advice regarding the constant use of the present multidose container. More than one topical ophthalmic drug when used, they should be administered at least five minutes apart.

Brimonidine tartrate may cause fatigue or drowsiness in some patients, as with other equivalent medications. Patients who are doing unsafe activities should be warned of the potential for a decrease in mental alertness.

Contraindications:

Brimonidine tartrate ophthalmic solution 0.1 or 0.15 percent is contraindicated in infants (below the age of two years). This is because the safety and effectiveness of the medication in this age group have not been established.

Hypersensitivity:

Symptoms of hypersensitivity can vary from mild such as hives or itching to severe such as anaphylaxis. If a patient has had a hypersensitivity reaction to any component of Brimonidine tartrate in the past, they should not use the medication again as it is likely that they will have a similar reaction.

Drug Interactions:

Antihypertensive or Cardiac Glycosides- As Brimonidine tartrate may reduce blood pressure, care while using drugs such as antihypertensives and/or cardiac glycosides is recommended.

• CNS Depressants- Since distinct drug interaction studies have not been conducted with Brimonidine tartrate, the causality of an additive effect with CNS depressants such as barbiturates, alcohol, opiates, anesthetics, or sedatives should be considered.

• Tricyclic Antidepressants- Tricyclic antidepressants are known to reduce the hypotensive effect of systemic clonidine. It is unknown whether the concurrent use of these agents with Brimonidine tartrate in humans can lead to resulting interference with the intraocular pressure lowering effect.

• Monoamine Oxidase Inhibitors- Monoamine oxidase (MAO) inhibitors can interfere with the metabolism of Brimonidine tartrate. It can cause an increased systemic side effect such as hypotension. A warning is advised in patients taking MAO inhibitors as they can affect the metabolism and uptake of circulating amines.

Brimonidine Tartrate During Pregnancy:

There are no sufficient and well-controlled studies in pregnant women; however, in animal studies, Brimonidine tartrate crossed the placenta and entered into fetal circulation to a limited extent. As animal reproduction studies are not always certain of human response, Brimonidine tartrate should be used during pregnancy only if the potential advantage to the mother explains the potential risk to the fetus.

Breastfeeding and Brimonidine Tartrate:

It is unknown whether the Brimonidine tartrate ophthalmic solution is safe for breastfeeding. The active ingredient, Brimonidine tartrate, can pass into human milk and may cause side effects in a nursing infant. Additionally, it is not known whether the medication could affect the quality or quantity of breast milk. If one is breastfeeding and considering using Brimonidine tartrate ophthalmic solution, it is important to discuss the potential risks and benefits with the healthcare provider. They may recommend alternative treatments or suggest ways to minimize the risk to the nursing infant.

Brimonidine Tartrate in Geriatric Patients:

Brimonidine tartrate ophthalmic result is generally considered safe and effective for senior individuals. As with any drug, there is a threat of side effects, and it is important for senior individuals to nearly follow the instructions of their healthcare provider when using this drug. Elderly individuals may be more sensitive to the side effects of Brimonidine tartrate ophthalmic solution. They may be more likely to witness dry mouth, greenishness or itching of the eye, and dizziness. It is important to report any side effects to the healthcare provider.