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Brimonidine

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Brimonidine Basic information
Brimonidine Chemical Properties
  • Melting point:207.5 °C
  • Boiling point:432.6±55.0 °C(Predicted)
  • Density 1.82±0.1 g/cm3(Predicted)
  • storage temp. Store at RT
  • solubility 45% (w/v) aq 2-hydroxypropyl-β-cyclodextrin: <0.8 mg/mL
  • pka7.69±0.10(Predicted)
  • Merck 14,1375
  • CAS DataBase Reference59803-98-4(CAS DataBase Reference)
Safety Information
  • Hazard Codes T
  • Risk Statements 25-36/37/38
  • Safety Statements 26-36-45
  • RIDADR UN 2811 6.1/PG 3
  • WGK Germany -
  • RTECS VD1200000
  • HazardClass 6.1
  • PackingGroup 
  • HS Code 29332900
MSDS
Brimonidine Usage And Synthesis
  • DescriptionLaunched in the US for open-angle glaucoma and ocular hypertension, brimonidine is a relatively selective and potent α2a,-adrenergic agonist with low affinity for the imidazoline l1 receptor. Topical application reduces intraocular pressure. This bypasses any central hypotensive effects at the l1 receptor (which can also give rise to a decrease in blood pressure and heart rate) if given systemically, since topical application results in low plasma levels concomitant with rapid systemic elimination. Brimonidine can be prepared in a four-step sequence from 4-nitrophenylenediamine.
  • Chemical PropertiesYellow Solid
  • OriginatorAllergan (USA)
  • Usesα2-Adrenoceptor agonist. Antiglaucoma.
  • Usescoronary vasodilator calcium ion influx inhibitor
  • Usesa2-Adrenoceptor agonist. Antiglaucoma
  • brand nameAlphagan (Allergan).
  • HazardA poison by ingestion.
  • Biological ActivityFull α 2 adrenergic agonist. Centrally active following systemic administration in vivo . Also available as part of the α 2 -Adrenoceptor Tocriset™ and Mixed Adrenergic Tocriset™ .
  • Veterinary Drugs and TreatmentsBrimonidine is an alpha-adrenergic receptor agonist. It has a peak ocular hypotensive effect occurring at two hours post-dosing. Fluorophotometric studies in animals and humans suggest that brimonidine tartrate has a dual mechanism of action by reducing aqueous humor production and by and increasing uveoscleral outflow. After ocular administration of either a 0.1% or 0.2% solution, plasma concentrations peaked within 0.5 to 2.5 hours and declined with a systemic half-life of approximately 2 hours. In humans, systemic metabolism of brimonidine is extensive. It is metabolized primarily by the liver. Urinary excretion is the major route of elimination of the drug and its metabolites. Approximately 87% of an orally-administered radioactive dose was eliminated within 120 hours, with 74% found in the urine.
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