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BRIMONIDINE TARTRATE

Brimonidine Tartrate is a synthetic, highly selective third generation α2-adrenergic agonist that was first developed in the ‘70s (by Pfizer)1. In 1996 it was introduced as first-line therapeutic in the US and since then has been approved in more than 50 countries for the lowering of intraocular pressure in patients with ocular hypertension and glaucoma.2

C2 PHARMA is the exclusive distributor of Brimonidine Tartrate manufactured by Laurus Labs Limited, one of the world’s leading API manufacturers.

USES

As 0.2% ophthalmic solution Brimonidine is used to reduce interocular pressure through a dual mechanism of action; the reduction of aqueous humour production by the ciliary body, and increased uveoscleral outflow.3,4 Topically applied as 0.33% gel, it provides a treatment for persistent (nontransient) erythema associated with rosacea.

MECHANISM OF ACTION

α2-Adrenergic agonists are responsible for intraocular pressure reduction through the inhibition of adenylate cyclase via the activation of a G protein-coupled receptor (GPSRs). This signaling cascade pathway is induced by Brimonidine which results in the reduction of second messenger cyclic adenosine monophosphate (cAMP) levels and aqueous humour production by ciliary body. In addition, strong evidence supports the hypothesis that prostaglandins can be released by α2-adrenergic agonists which are the cause for the increased uveoscleral outflow4.
When applied topically on skin, Brimonidine reduces erythema through direct vasoconstriction of small arteries and veins.6

REFERENCES

  1. Patent US4029792A, 1975.
  2. Cantor, B.L., Exp. Opin. Pharmacother. 2000, 4, 815-834.
  3. Toris, C.B., Camras, C.B., Yablonski, M.E.,  Arch. Ophthalmol1995, 113, 1514-1517.
  4. Toris, C.B., Camras, C.B., Yablonski, M.E.,  Am. J. Ophthalmol1999, 128, 8-14.
  5. Toris, C.B., Camras, C.B., Yablonski, M.E., Ophthalmology.  1993, 100, 1297-1304.
  6. Jackson J.M., Knuckles M., Minni J.P., Johnson S.M, Belasco K.T. Clin. Cosmet. Investig. Dermatol. 2015, 8, 529-38.