化合物信息

Drug Groups

approved; investigational

Description

Bimatoprost ophthalmic solution is a topical medication used for controlling the progression of glaucoma or ocular hypertension, by reducing intraocular pressure. It is a prostaglandin analogue that works by increasing the outflow of aqueous fluid from the eyes. It binds to the prostanoid FP receptor.

Indication

For the reduction of elevated intraocular pressure in patients with open angle glaucoma or ocular hypertension who are intolerant of other intraocular pressure lowering medications or insufficiently responsive (failed to achieve target IOP determined after multiple measurements over time) to another intraocular pressure lowering medication.

Pharmacology

Bimatoprost is a prostamide, a synthetic structural analog of prostaglandin with ocular hypotensive activity, that is chemically related to prostamide F. It selectively mimics the effects of naturally occurring substances, prostamides. Bimatoprost lowers intraocular pressure (IOP) in humans. Elevated IOP presents a major risk factor for glaucomatous field loss. The higher the level of IOP, the greater the likelihood of optic nerve damage and visual field loss.

Toxicity

In oral (by gavage) mouse and rat studies, doses up to 100 mg/kg/day did not produce any toxicity. This dose expressed as mg/m² is at least 70 times higher than the accidental dose of one bottle of bimatoprost for a 10 kg child.

Affected Organisms

Biotransformation

Bimatoprost undergoes oxidation, N-deethylation and glucuronidation to form a variety of metabolites.

Absorption

Systemically absorbed when administered to the eye.

Half Life

Elimination half-life is approximately 45 minutes.

Protein Binding

Approximately 88% of bimatoprost is bound in human plasma.

Elimination

Up to 67% of the administered dose was excreted in the urine while 25% of the dose was recovered in the feces.

Distribution

* 0.67 L/kg

Clearance

* 1.5 L/hr/kg [Healthy subjects receiving IV administration of 3.12 ug/kg]

References

External Links