The pharmacology of bimatoprost (Lumigan (TM))

Bimatoprost (Lumigan (TM)) is a pharmalogically unique and highly efficacio us ocular hypotensive agent. It appeal's to mimic the activity of a newly d iscovered family of fatty acid amides, termed prostamides. Our biosynthetic route to the prostamides involves anandamide as the precursor. Bimatoprost pharmacology has been extensively characterised by binding and functional studies at more than 100 drug targets, which comprise a diverse variety of receptors, ion channels, and transporters. Bimatoprost exhibited no meaning ful activity at receptors known to include antiglaucoma drug targets as fol lows: adenosine (A(1-3)), adrenergic (alpha (1), alpha (2), beta (1), beta (2)), cannabinoid (CB1, CB2), dopamine (D1-5). muscarinic (M1-5), prostanoi d (DP, EP1-4, FP, IF, TP), and serotonin (5HT(1-7)). Bimatoprost does, here ever, exhibit potent inherent pharmacological activity in the feline iris sphincter preparation, which is prostamide-sensitive. Bimatoprost also rese mbles the prostamides ill that it is a potent and highly efficacious ocular hypotensive agent. A single dose of bimatoprost markedly reduces intraocul ar pressure in dogs and laser-induced ocular hypertensive monkeys. Decrease s in intraocular pressure are well maintained for at least 24 h post-dose. Human studies have demonstrated that systemic exposure to bimatoprost is lo w and that accumulation does not occur. Tile sclera is the preferred route of accession to the eye. The high scleral permeability coefficient Papp is a likely contributing factor to tile rapid onset and long-acting ocular hyp otensive profile of bimatoprost.