High Purity 99% White Powder Bimatoprost CAS 155206-00-1

Bimatoprost More Info

Bimatoprost is a synthetic analog of prostaglandin F2α (PGF2α) used primarily in ophthalmology for the treatment of elevated intraocular pressure (IOP) in conditions such as open-angle glaucoma and ocular hypertension. It is also marketed for cosmetic purposes to enhance eyelash growth.

Mechanism of Action

Bimatoprost lowers intraocular pressure through several mechanisms:
Increased Aqueous Humor Outflow: Bimatoprost enhances the outflow of aqueous humor primarily via two pathways:
Trabecular Meshwork Pathway: By decreasing resistance to outflow through the trabecular meshwork.
Uveoscleral Pathway: It increases the pressure-insensitive outflow via the uveoscleral route, leading to improved drainage of aqueous humor from the eye.
Stimulation of Remodeling Enzymes: Bimatoprost may increase levels of tissue inhibitors of metalloproteinases (TIMP) and matrix metalloproteinases (MMP), which contribute to structural changes in the ciliary muscle and sclera, facilitating better aqueous outflow.
Mimicking Prostaglandin Effects: Although it is a prostaglandin analog, bimatoprost does not act on traditional prostaglandin receptors but instead mimics endogenous prostamides, which are similar in structure and function.

Applications

Bimatoprost is indicated for:
Open-Angle Glaucoma: Used alone or in combination with other medications to reduce elevated IOP.
Ocular Hypertension: Effective in managing increased pressure within the eye.
Hypotrichosis of Eyelashes: Approved for cosmetic use to promote eyelash growth, enhancing both length and thickness.

Routes of Administration

Bimatoprost is administered topically as an ophthalmic solution. The typical dosage involves instilling one drop into the affected eye(s) once daily.

Safety and Side Effects

Bimatoprost is generally well-tolerated, but potential side effects include:
Common Side Effects: Redness of the eyes (conjunctival hyperemia), dry eyes, blurred vision, and changes in eyelash pigmentation (darkening and increased growth).
Serious Reactions: Allergic reactions, such as rash or itching, may occur. Long-term use may lead to cataract formation.
Contraindications: Should be avoided in patients with hypersensitivity to bimatoprost or any components of the formulation.

Pharmacokinetics

Bimatoprost has distinct pharmacokinetic properties:
Absorption: Well absorbed through the cornea; systemic absorption occurs but is limited. Peak plasma concentrations are reached within approximately 10 minutes after administration.
Distribution: The volume of distribution is about 0.67 L/kg, with significant penetration into ocular tissues, particularly the ciliary body.
Metabolism: Primarily metabolized by oxidation and glucuronidation. The active form, bimatoprost acid, is produced in the eye.
Elimination: Approximately 67% is excreted via urine and 25% via feces. The elimination half-life is about 45 minutes.
Protein Binding: Bimatoprost has a high plasma protein binding rate (approximately 88%).