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Brimonidine | CAS No: 59803-98-4 | GMP-certified suppliers
A medication that lowers intraocular pressure in open-angle glaucoma or ocular hypertension and reduces persistent facial erythema associated with rosacea in adults.
Therapeutic categories
Adrenergic AgentsAdrenergic AgonistsAdrenergic alpha-2 Receptor AgonistsAdrenergic alpha-AgonistsAntiglaucoma Preparations and MioticsCardiovascular Agents
Generic name
Brimonidine
Molecule type
small molecule
CAS number
59803-98-4
DrugBank ID
DB00484
Approval status
Approved drug
ATC code
D11AX21
Primary indications
- Opthalmic**
- Indicated for lowering intraocular pressure (IOP) in patients with open-angle glaucoma or ocular hypertension [label] as monotherapy or combination product with [brinzolamide]
- Topical**
- Indicated for the treatment of persistent (non-transient) facial erythema of rosacea in adults 18 years of age or older
Product Snapshot
- Brimonidine is an ophthalmic and topical small‑molecule formulation supplied mainly as solutions, suspensions, and gels for conjunctival or cutaneous administration
- It is used to lower intraocular pressure in open‑angle glaucoma or ocular hypertension and to reduce persistent facial erythema associated with rosacea
- It is approved in the US, EU, and Canada
Clinical Overview
Brimonidine (CAS 59803-98-4) is a selective alpha‑2 adrenergic receptor agonist used in ophthalmic and dermatologic applications. It is indicated for lowering intraocular pressure in open‑angle glaucoma and ocular hypertension, either as monotherapy or in fixed‑dose combination with brinzolamide. A separate topical gel formulation is approved for persistent facial erythema of rosacea in adults. Chemically, brimonidine is a quinoxaline derivative and a 2‑imidazoline compound.
Brimonidine displays approximately 1000‑fold selectivity for alpha‑2 over alpha‑1 receptors. This receptor preference limits alpha‑1–mediated ocular effects and reduces systemic adrenergic reactions seen with less selective agents. Pharmacodynamically, peak ocular hypotensive activity occurs around two hours after dosing, with sustained efficacy documented over long‑term treatment periods.
Mechanistically, activation of ocular alpha‑2 receptors inhibits adenylyl cyclase, decreases cyclic AMP, and reduces norepinephrine release. This suppresses beta‑2 receptor–mediated aqueous humor production. With chronic dosing, brimonidine also enhances uveoscleral outflow. It does not influence episcleral venous pressure. In topical dermatologic use, brimonidine induces direct vasoconstriction of small cutaneous vessels, leading to reduction of erythema.
Brimonidine is rapidly absorbed following ophthalmic administration. Systemic exposure can produce dose‑dependent cardiovascular effects such as reduced blood pressure and heart rate, and PR‑interval prolongation, although these are uncommon with ocular dosing. Ocular adverse effects may include conjunctival vasoconstriction and allergic reactions. In rosacea therapy, transient erythema fluctuation may occur. Experimental neuroprotective findings have been reported, but their clinical relevance has not been established.
Notable products include Alphagan ophthalmic solution, the brinzolamide combination Simbrinza, and the topical rosacea agent Mirvaso.
For API procurement, suppliers should provide consistent stereochemical integrity, impurity control aligned with ICH guidelines, and stability data suitable for both ophthalmic and dermal formulation development.
Brimonidine displays approximately 1000‑fold selectivity for alpha‑2 over alpha‑1 receptors. This receptor preference limits alpha‑1–mediated ocular effects and reduces systemic adrenergic reactions seen with less selective agents. Pharmacodynamically, peak ocular hypotensive activity occurs around two hours after dosing, with sustained efficacy documented over long‑term treatment periods.
Mechanistically, activation of ocular alpha‑2 receptors inhibits adenylyl cyclase, decreases cyclic AMP, and reduces norepinephrine release. This suppresses beta‑2 receptor–mediated aqueous humor production. With chronic dosing, brimonidine also enhances uveoscleral outflow. It does not influence episcleral venous pressure. In topical dermatologic use, brimonidine induces direct vasoconstriction of small cutaneous vessels, leading to reduction of erythema.
Brimonidine is rapidly absorbed following ophthalmic administration. Systemic exposure can produce dose‑dependent cardiovascular effects such as reduced blood pressure and heart rate, and PR‑interval prolongation, although these are uncommon with ocular dosing. Ocular adverse effects may include conjunctival vasoconstriction and allergic reactions. In rosacea therapy, transient erythema fluctuation may occur. Experimental neuroprotective findings have been reported, but their clinical relevance has not been established.
Notable products include Alphagan ophthalmic solution, the brinzolamide combination Simbrinza, and the topical rosacea agent Mirvaso.
For API procurement, suppliers should provide consistent stereochemical integrity, impurity control aligned with ICH guidelines, and stability data suitable for both ophthalmic and dermal formulation development.
Identification & chemistry
| Generic name | Brimonidine |
|---|---|
| Molecule type | Small molecule |
| CAS | 59803-98-4 |
| UNII | E6GNX3HHTE |
| DrugBank ID | DB00484 |
Pharmacology
| Summary | Brimonidine is a selective alpha‑2 adrenergic receptor agonist that reduces intraocular pressure by inhibiting aqueous humor production and, with continued use, enhancing uveoscleral outflow. Its action on alpha‑2 receptors also produces cutaneous vasoconstriction, which decreases facial erythema. Major pharmacodynamic effects reflect high alpha‑2 selectivity, including ocular hypotension and peripheral vasoconstriction. |
|---|---|
| Mechanism of action | In the eye, alpha-1 adrenoceptors play a role in vasoconstriction, mydriasis, eyelid retraction, and elevation of intraocular pressure (IOP) whereas alpha-2 adrenoceptors are responsible for IOP reduction via a complex Gi-coupled signaling cascade pathway. Activation of alpha-2 receptors leads to inhibition of adenylyl cyclase and reduction of cyclic AMP levels. As a result, there is a decrease in norpinephrine (NE) release at the synaptic junction, NE-induced stimulation of beta-2 adrenoceptors, and production of aqueous humor by the ciliary epithelium.An elevated IOP is the most significant risk factor for developing glaucomatous optic neuropathy, which is associated with progressive visual field loss and functional disability if left untreated.Regardless of the etiology of the disease, the aim of current therapies for glaucoma is to reduce IOP, as reduction of IOP significantly reduces the risk of progression of vision loss even when IOP is already within the normal range.When administered ophthalmically, brimonidine is rapidly absorbed into the eye, acts as an agonist at ocular alpha-2 adrenoceptors and lowers IOP via a dual mechanism of action.It is proposed that initial dosing of the drug causes a reduction in aqueous humour production and chronic dosing leads to an increase in uveoscleral outflow.Brimonidine does not affect episcleral venous pressure.By reducing IOP, brimonidine aims to reduce the likelihood of glaucomatous visual field loss in ocular hypertension, and slow the progression of visual field defect in established open-angle glaucoma.When applied topically on skin, brimonidine reduces erythema through direct vasocontriction of small arteries and veins.As brimonidine mediates a potent peripheral vasoconstrictive activity by selectively working on the alpha-2 adrenoceptors, the use of brimonidine is thought to be efficacious for the treatment of facial erythema of rosacea, which is thought to arise from vasomotor instability and abnormal vasodilation of the superficial cutaneous vasculature of the face. |
| Pharmacodynamics | Brimonidine is a highly selective alpha-2 adrenergic receptor agonist that is 1000-fold more selective for the alpha2-adrenergic receptor than the alpha1-adrenergic receptor.This characteristic gives the drug some therapeutic advantages, since it reduces the risk of systemic side effects, such as systemic hypotension, bradycardia, and sedation. In addition, there is a reduction in the risk for developing alpha-1 mediated ocular unwanted effects, such as conjunctival blanching, mydriasis, and eyelid retraction.However, despite high alpha-2 receptor specificity, brimonidine may still produce alpha-1 adrenoceptor-mediated ocular effects, such as conjunctival vasoconstriction.Brimonidine has a peak ocular hypotensive effect occurring at two hours post-dosing.[label] In a randomized, double-blind clinical study, ocular administration of 0.2% brimonidine in healthy volunteers resulted in a 23% reduction of mean intraocular pressure from baseline at 3 hours following administration.In comparative studies consisting of patients with open-angle glaucoma or ocular hypertension, the ocular hypotensive effect of brimonidine was maintained during treatment periods of up to 1 year. Brimonidine mediates vasoconstrictive effects and it was shown to exhibit anti-inflammatory properties in _ex vivo_ human skin model and _in vivo_ inflammation models.In a clinial trials consisting of adults with moderate to severe facial erythema of rosacea, brimonidine was shown to improve the extent of redness at 3 hours after application, compared to placebo.It was shown to be a potent vasoconstrictor of human subcutaneous vessels with a diameter of less than 200 µm. In _in vivo_ mouse inflammation models, brimonidine displayed anti-inflammatory properties by inhibiting edema.In a randomized, double-blind study, brimonidine reduced erythema for the 12 hours of the study in a dose-dependent manner. When adminsitered systemically, brimonidine was shown to cause cardiovascular effects by decreasing blood pressure, decreasing heart and respiratory rate, and prolonging the PR interval in the electrocardiogram. This is due to the targeting of adrenoceptors by the drug.Although the clinical significance has not been established, there is evidence that brimonidine exhibits neuroprotective activity in experimental models of cerebral ischemia and optic nerve injury._In vitro_ studies show that brimonidine mediated protective effects on neuronal cells from kainate acid insult and on cultured retinal ganglion cells from glutamate-induced cytotoxicity, which is a possible mediator of secondary neuronal degeneration in human glaucoma. Neuroprotective actions of brimonidine were also demonstrated in rat models of acute retinal ischemia and chronic IOP elevation. It has been proposed that brimonidine may exert neuroprotective effects on the retina and optic nerve by enhancing intrinsic retinal ganglion cell survival mechanisms and/or induction of neuronal survival factors, such as bFGF.However, further investigations are needed to conclude on these possible therapeutic benefits of the drug. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Alpha-2A adrenergic receptor | Humans | agonist |
| Alpha-2B adrenergic receptor | Humans | agonist |
| Alpha-2C adrenergic receptor | Humans | agonist |
ADME / PK
| Absorption | Brimonidine readily penetrates the cornea following ocular administration to reach pharmacologically active concentrations in the aqueous humor and ciliary body, the putative sites of its IOP-lowering activity.Following ocular administration of 0.2% brimonidine solution, the peak plasma concentrations were achieved within 1 to 4 hours.[label] In a clinical study of adult subjects with facial erythema of rosacea, brimonidine was cutaneously applied on facial skin in a repeated manner. While there was no drug accumulation in plasma, the highest peak plasma concentrations (Cmax) and AUC were 46 ± 62 pg/mL and 417 ± 264 pgxhr/mL, respectively. |
|---|---|
| Half-life | Following ocular administration of 0.2% brimonidine solution, the systemic half-life was approximately 3 hours.[label] |
| Protein binding | The protein binding of brimonidine has not been studied. |
| Metabolism | Brimonidine is reported to be metabolized in the cornea. Brominidine that reaches the systemic circulation upon topical administration undergoes extensive hepatic metabolism mediated by hepatic aldehyde oxidases.[label] |
| Route of elimination | Brimonidine and its metabolites are predominantly eliminated via urinary excretion, with 74% of the total dose being found in the urine.[label] |
| Volume of distribution | The volume of distribution of brimonidine has not been established. In animal studies, brimonidine was shown to cross the placenta and enter into the fetal circulation to a limited extent.[label] As its lipophilicity is relatively low, brimonidine is not reported to easily cross the blood-brain barrier. |
| Clearance | The apparent clearance has not been studied. However, the systemic clearance of brimonidine is reported to be rapid.Approximately 87% of the total radioactive dose of brimonidine was shown to be eliminated within 120 hours following oral administration.[label] |
Formulation & handling
- Formulated primarily as ophthalmic solutions, the small‑molecule API requires aqueous vehicles with solubilizers or pH adjustment due to low intrinsic water solubility.
- Chemical stability in solution benefits from controlled pH and protection from oxidation, with typical handling as a light‑sensitive solid during API storage.
- Topical gel formulations use suitable polymers to maintain uniformity and support dermal penetration without specialized cold‑chain requirements.
Regulatory status
| Lifecycle | The active ingredient is in a late‑stage lifecycle across Canada, the US, and the EU, with key US and Canadian patents expiring between 2012 and 2022. These expiries indicate a mature market with broad generic entry expected or already established in all major regions. |
|---|
| Markets | Canada, US, EU |
|---|
Supply Chain
| Supply chain summary | Brimonidine was originally developed and commercialized by a small group of originator companies, with subsequent manufacturing and packaging now carried out by numerous firms, indicating a well‑established and diversified supply base. Branded products such as Alphagan and Alphagan P have long-standing availability in the US, Canada, and EU. Multiple key patents have expired in major markets, with the most recent U.S. protections ending in 2022, supporting the presence of existing and broad generic competition. |
|---|
Safety
| Toxicity | **LD<sub>50</sub> and Overdose** Oral LD<sub>50</sub> is 50 mg/kg in mice and 100 mg/kg in rats.[MSDS] While there is limited clinial data on brimonidine overdose in adults, some common symptoms from oral overdoses of alpha-2 adrenergic agonists include hypotension, asthenia, vomiting, lethargy, sedation, bradycardia, arrhythmias, miosis, apnoea, hypotonia, hypothermia, respiratory depression and seizure. Treatment of an oral overdose includes supportive and symptomatic therapy. Cases of brimonidine overdose have been reported in neonates, infants, and pediatric patients receiving brimonidine tartrate as part of medical treatment of congenital glaucoma or by accidental oral ingestion. In these cases, children experienced symptoms consistent with previously reported oral overdoses of alpha-2 adrenergic agonists in young children. **Nonclinical Toxicology** At oral doses of up to 2.5 and 5 mg/kg/day in pregnant rats and rabbits, brimonidine was not shown to be teratogenic during gestation days 6 through 18. Findings from various _in vitro_ and _in vivo_ studies, including the Ames bacterial assay, CHO cell chromosomal aberration assay, and CD-1 mice studies, did not demonstrate any mutagenic or clastogenic potential of brimonidine.[label] There were no observable adverse effects on male or female fertility when tested at oral doses of up to 1 mg/kg, which is approximately 200 times the systemic exposure following the maximum recommended ophthalmic dose of 0.5% brimonidine.[label] **Use in special populations** Due to limited clinical data on the use of brimonidine pregnant or breastfeeding female patients, the use of brimonidine in these patients is generally not recommended and the use should be only considered after taking into account the benefit-to-risk ratio of continuing the drug therapy in these patients. In nursing mothers, the decision should be made whether to discontinue the drug or discontinue breastfeeding.[label] As the systemic absorption and elimination of brimonidine are not significantly affected by age, the use of brimonidine is considered safe in geriatric patients. In contrast, the use of brimonidine in infants under the age of 2 and pediatric patients under the age of 18 is strongly not recommended due to the reports of serious adverse events following ophthalmic administration of brimonidine in infants between the age of 28 days and 3 months. |
|---|
High Level Warnings:
- Acute toxicity is moderate, with reported oral LD50 values of 50 mg/kg (mice) and 100 mg/kg (rats)
- Oral exposure may elicit CNS and cardiovascular depression consistent with alpha‑2 agonist effects
- Overdose reports describe hypotension, bradyarrhythmias, respiratory depression, and marked sedation, with heightened sensitivity documented in neonates and young pediatric populations
Written Confirmation
When an API is imported into the European Union from elsewhere in the world, it should be accompanied by a “written confirmation” (WC). A written confirmation is a document set up by the health authorities of the country where the API was manufactured. After inspections were successfully performed under EU/GMP equivalent standards, the health authorities can provide a WC. These inspections will also have to regularly take place in the future.
Brimonidine is a type of Ocular preparations
Ocular preparations are a vital subcategory of pharmaceutical active pharmaceutical ingredients (APIs) used in the formulation of medications and treatments for various eye conditions. These specialized formulations are designed to deliver therapeutic agents directly to the eye, ensuring maximum effectiveness and minimal systemic absorption.
Ocular preparations encompass a wide range of products, including eye drops, ointments, gels, and inserts. These formulations may contain API components such as antibiotics, corticosteroids, antihistamines, lubricants, or mydriatics, depending on the intended therapeutic purpose.
Eye drops are the most common form of ocular preparations, delivering medications in liquid form directly onto the eye surface. They are often used to treat conditions like dry eyes, glaucoma, allergies, and infections. Ointments and gels provide a more viscous consistency, enabling longer contact time with the eye surface and prolonged drug release. Inserts, such as punctal plugs, are used to deliver sustained-release medications.
Ocular preparations are formulated to ensure compatibility with the delicate structures of the eye and to enhance drug penetration. Factors like pH, osmolality, and viscosity are carefully controlled to optimize drug delivery and patient comfort. Additionally, preservatives are often added to prevent microbial contamination and maintain product stability.
In summary, ocular preparations are crucial in treating various eye conditions effectively. They provide targeted drug delivery and ensure optimal therapeutic outcomes with minimal side effects. Whether in the form of eye drops, ointments, gels, or inserts, these pharmaceutical APIs play a vital role in promoting eye health and improving patient well-being.
Brimonidine (Ocular preparations), classified under Ophthalmic Agents
Ophthalmic agents belong to the pharmaceutical API (Active Pharmaceutical Ingredient) category specifically designed for ophthalmic applications. These agents are formulated to treat various eye conditions and disorders. Ophthalmic agents encompass a wide range of medications, including eye drops, ointments, gels, and intraocular implants.
These agents are developed to address specific therapeutic needs related to the eyes, such as reducing intraocular pressure in glaucoma, treating inflammation and infection, relieving dryness and itching, and managing allergies. They may also be used to dilate the pupils during diagnostic procedures or surgeries.
Ophthalmic agents are formulated with precise concentrations of active ingredients to ensure efficacy and safety. Common classes of ophthalmic agents include beta-blockers, prostaglandin analogs, carbonic anhydrase inhibitors, corticosteroids, and antihistamines.
When administering ophthalmic agents, it is crucial to follow proper application techniques to ensure optimal drug delivery and minimize side effects. Eye drops, for example, are typically applied as a gentle instillation into the conjunctival sac, while ointments are applied along the lower eyelid.
These pharmaceutical API ophthalmic agents undergo rigorous quality control and regulatory scrutiny to meet industry standards and ensure patient safety. Manufacturers must comply with Good Manufacturing Practices (GMP) and adhere to stringent quality assurance protocols.
Overall, ophthalmic agents play a vital role in the management and treatment of various eye conditions, providing patients with targeted relief and improving ocular health. It is important to consult with a healthcare professional to determine the appropriate ophthalmic agent for individual needs and to receive proper guidance on usage and potential side effects.
Brimonidine API manufacturers & distributors
Compare qualified Brimonidine API suppliers worldwide. We currently have 16 companies offering Brimonidine API, with manufacturing taking place in 5 different countries. Use the table below to review supplier type, countries of origin, certifications, product portfolio and GMP audit availability.
| Supplier | Type | Country | Product origin | Certifications | Portfolio |
|---|---|---|---|---|---|
| Cedarburg Pharma | Producer | United States | United States | CEP, CoA, FDA, USDMF | 12 products |
| Centaur Pharma | Producer | India | India | CoA, GMP, USDMF, WC | 40 products |
| Farmak | Producer | Czech Republic | Czech Republic | CEP, CoA, FDA, GMP, KDMF, USDMF | 19 products |
| Global Pharma Tek | Distributor | India | India | BSE/TSE, CoA, FDA, GMP, ISO9001, MSDS | 484 products |
| Indoco Remedies | Producer | India | India | CEP, CoA, FDA, GMP, KDMF, USDMF, WC | 19 products |
| Laurus Labs | Producer | India | India | CoA, GMP, USDMF, WC | 50 products |
| LGM Pharma | Distributor | United States | World | BSE/TSE, CEP, CoA, GMP, MSDS, USDMF | 441 products |
| Lupin | Producer | India | India | CoA, USDMF | 155 products |
| Medichem | Producer | Spain | Unknown | CEP, CoA, FDA, GMP, KDMF, USDMF | 39 products |
| Micro Labs | Producer | India | India | CoA, GMP, WC | 38 products |
| Piramal Healthcare | Producer | United Kingdom | India | CoA, GMP, WC | 31 products |
| Piramal Pharma Solutions | Producer | India | Unknown | CEP, CoA, FDA, GMP, JDMF, KDMF, USDMF, WC | 44 products |
| Symed Labs | Producer | India | India | CoA, GMP, USDMF, WC | 28 products |
| Tenatra Exports Private L... | Distributor | India | India | BSE/TSE, CoA, FDA, GMP, MSDS | 263 products |
| Unichem Labs. | Producer | India | India | CoA, GMP, USDMF, WC | 62 products |
| Veeprho Group | Producer | Czech Republic | Czech Republic | CoA | 144 products |
When sending a request, specify which Brimonidine API quality you need: for example EP (Ph. Eur.), USP, JP, BP, or another pharmacopoeial standard, as well as the required grade (base, salt, micronised, specific purity, etc.).
Use the list above to find high-quality Brimonidine API suppliers. For example, you can select GMP, FDA or ISO certified suppliers. Visit our help page to learn more about sourcing APIs via Pharmaoffer.
Frequently asked questions about Brimonidine API
Sourcing
What matters most when sourcing GMP-grade Brimonidine?
Key considerations include confirming compliance with GMP and the regulatory requirements of the US, Canada, and EU. Suppliers should demonstrate reliable manufacturing and packaging controls consistent with a mature and diversified global supply base. It is also important to verify that the material aligns with post‑patent generic standards given the broad competition in these markets.
Which documents are typically required when sourcing Brimonidine API?
Request the core API documentation set: CoA (16 companies), GMP (13 companies), USDMF (11 companies), WC (8 companies), FDA (7 companies). Confirm versions and validity dates match the destination market to avoid delays in qualification.
Which manufacturers are known to produce Brimonidine API?
Known or reported manufacturers for Brimonidine: Global Pharma Tek, Veeprho Group, LGM Pharma, Tenatra Exports Private Limited. Evaluate their GMP history, scale, and regional coverage before requesting dossiers or allocating demand.
How can I request quotes for Brimonidine API from GMP suppliers?
Submit quote requests through the supplier listings with your specs and required documents (specifications, target volume, delivery timeline, and destination). Providing consistent details upfront speeds comparable offers and clarifies technical feasibility.
Is a GMP audit report available for Brimonidine manufacturers?
Audit reports may be requested for Brimonidine: 8 GMP audit reports available. Confirm the scope and recency of any audit before relying on it for qualification decisions.
How many suppliers offer Brimonidine API on Pharmaoffer?
Reported supplier count for Brimonidine: 16 verified suppliers. Filter listings by certifications, regions, and delivery options to match your qualification plan.
Which countries are known to manufacture Brimonidine API?
Production countries reported for Brimonidine: India (10 producers), Czech Republic (2 producers), United States (1 producer). Knowing the manufacturing geography helps anticipate logistics lead times and import compliance needs.
Which certifications do suppliers of Brimonidine usually hold?
Common certifications for Brimonidine suppliers: CoA (16 companies), GMP (13 companies), USDMF (11 companies), WC (8 companies), FDA (7 companies). Always verify issuing authorities and expiry dates when reviewing audit packages.
Technical
What is Brimonidine (CAS 59803-98-4) used for?
Brimonidine is used to lower intraocular pressure in open‑angle glaucoma and ocular hypertension by reducing aqueous humor production and increasing uveoscleral outflow. It is also used topically to reduce persistent facial erythema in adults with rosacea through localized vasoconstriction of small cutaneous vessels.
Which therapeutic class does Brimonidine fall into?
Brimonidine belongs to the following therapeutic categories: Adrenergic Agents, Adrenergic Agonists, Adrenergic alpha-2 Receptor Agonists, Adrenergic alpha-Agonists, Antiglaucoma Preparations and Miotics. This positioning helps teams compare alternative APIs, anticipate pharmacology expectations, and align early research priorities.
What conditions is Brimonidine mainly prescribed for?
The primary indications for Brimonidine: Opthalmic**, Indicated for lowering intraocular pressure (IOP) in patients with open-angle glaucoma or ocular hypertension [label] as monotherapy or combination product with [brinzolamide], Topical**, Indicated for the treatment of persistent (non-transient) facial erythema of rosacea in adults 18 years of age or older. These use cases frame the target patient populations and help prioritize formulation and safety evaluations.
How does Brimonidine work?
In the eye, alpha-1 adrenoceptors play a role in vasoconstriction, mydriasis, eyelid retraction, and elevation of intraocular pressure (IOP) whereas alpha-2 adrenoceptors are responsible for IOP reduction via a complex Gi-coupled signaling cascade pathway. Activation of alpha-2 receptors leads to inhibition of adenylyl cyclase and reduction of cyclic AMP levels. As a result, there is a decrease in norpinephrine (NE) release at the synaptic junction, NE-induced stimulation of beta-2 adrenoceptors, and production of aqueous humor by the ciliary epithelium.An elevated IOP is the most significant risk factor for developing glaucomatous optic neuropathy, which is associated with progressive visual field loss and functional disability if left untreated.Regardless of the etiology of the disease, the aim of current therapies for glaucoma is to reduce IOP, as reduction of IOP significantly reduces the risk of progression of vision loss even when IOP is already within the normal range.When administered ophthalmically, Brimonidine is rapidly absorbed into the eye, acts as an agonist at ocular alpha-2 adrenoceptors and lowers IOP via a dual mechanism of action.It is proposed that initial dosing of the drug causes a reduction in aqueous humour production and chronic dosing leads to an increase in uveoscleral outflow.Brimonidine does not affect episcleral venous pressure.By reducing IOP, Brimonidine aims to reduce the likelihood of glaucomatous visual field loss in ocular hypertension, and slow the progression of visual field defect in established open-angle glaucoma.When applied topically on skin, Brimonidine reduces erythema through direct vasocontriction of small arteries and veins.As Brimonidine mediates a potent peripheral vasoconstrictive activity by selectively working on the alpha-2 adrenoceptors, the use of Brimonidine is thought to be efficacious for the treatment of facial erythema of rosacea, which is thought to arise from vasomotor instability and abnormal vasodilation of the superficial cutaneous vasculature of the face.
What should someone know about the safety or toxicity profile of Brimonidine?
Brimonidine has a moderate acute toxicity profile, with reported oral LD50 values of 50 mg/kg in mice and 100 mg/kg in rats. Systemic exposure can cause CNS and cardiovascular depression, including hypotension, bradyarrhythmias, respiratory depression, and marked sedation, with greater sensitivity observed in neonates and young children. Typical ophthalmic dosing rarely produces significant systemic effects, though dose‑dependent reductions in blood pressure and heart rate can occur. Local reactions may include conjunctival vasoconstriction, allergic responses, or transient erythema fluctuation with dermatologic use.
What are important formulation and handling considerations for Brimonidine as an API?
Important considerations include managing its low water solubility by using solubilizers or pH adjustment when preparing aqueous ophthalmic solutions. Solution stability is supported by maintaining a controlled pH and protecting the API from oxidation, and the solid form should be handled as light‑sensitive during storage. For topical gel formulations, appropriate polymers are needed to maintain uniformity and support dermal penetration. No special cold‑chain conditions are required.
Is Brimonidine a small molecule?
Brimonidine is classified as a small molecule. That classification shapes process design, impurity profiling, and analytical control strategies.
Are there special stability concerns for oral Brimonidine?
Brimonidine is primarily formulated as aqueous ophthalmic solutions, where stability depends on controlled pH, protection from oxidation, and mitigation of its low intrinsic water solubility. As an API, it is handled as a light‑sensitive solid. These fundamental stability characteristics would remain relevant for any oral formulation approach, requiring attention to solubility and oxidative degradation.
Regulatory
Where is Brimonidine approved or in use globally?
Brimonidine is reported as approved in the following major regions: Canada, US, EU. Understanding geographic coverage informs regulatory filings, supply planning, and risk assessments before escalating procurement.
What’s the regulatory and patent landscape for Brimonidine right now?
Brimonidine has established regulatory authorization in Canada, the United States, and the European Union for its approved ophthalmic uses. Patent considerations are jurisdiction‑specific and operate independently of these regulatory listings, with protection timelines determined by each region’s patent framework.
Pharmaoffer
How does Pharmaoffer’s Smart Sourcing Service help with Brimonidine procurement?
Pharmaoffer's Smart Sourcing Service coordinates compliant suppliers, documentation, and competitive quotes for Brimonidine. It centralizes outreach, follow-ups, and document validation to shorten procurement timelines.
Is Brimonidine included in the PRO Data Insights coverage?
PRO Data Insights coverage for Brimonidine: 1472 verified transactions across 394 suppliers and 182 buyers worldwide. Use the dataset to benchmark suppliers and monitor regulatory activity where available.
Where can I access the API market report for Brimonidine?
Market report availability for Brimonidine: Report Available. The report highlights demand trends, pricing drivers, and supplier landscape insights for procurement planning.
