Bimatoprost

Molecular formula C2SH37NO4 Molecular weight 415.57 CAS Registry No 155206-00-1 

Mobile phase Gradient. A B 100 0 for 1 min, to 40 60 over 16 min (-h curved), maintain at 40 60 for 4 min, return to initial conditions over 1 min, re-equilibrate at initial conditions for 8 min. A was MeCN 20 mM pH 2.8 potassium phosphate buffer 20 80. B was MeCN 20 mM pH 2.8 potassium phosphate buffer 50 50. 

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Bimatoprost Prostamide Lumigan Solution 0.03 1 drop every night ... 

The ocular hypotensive lipids in typical ophthalmology practice are considered first-line alternatives to topical P-blockers because of their superior efficacy and safety profiles. Many clinicians may choose to use the ocular hypotensive lipids as first-line agents, especially in patients that have an initial requirement to lower IOP by more than 25%, or in patients that have relative or absolute contraindications to topical P-blockers. However, latanoprost is currently the only ocular hypotensive lipid drug that has a Food and Drug Administration (FDA) indication for first-line therapy. Bimatoprost and travoprost are indicated by the FDA for patients who are intolerant of other IOP-lowering therapy or insufficiently responsive to another IOP-lowering medication.10,38... 

BIMATOPROST, LATANOPROST, TRAVOPROST The recommended dosage is 1 drop in the affected eye(s) once daily in the evening. Do not exceed once-daily dosage because it has been shown that more frequent administration may decrease the lOP-lowering effect. 

Bimatoprost, latanoprost, and travoprost may be used concomitantly with other topical ophthalmic drug products to lower lOP. If more than 1 topical ophthalmic drug is being used, administer the drugs at least 5 minutes apart. 

Active intraocular inflammation Use bimatoprost and latanoprost with caution in patients with active intraocular inflammation (eg, uveitis). 

Ophthalmic - Bimatoprost-associated ocular adverse events that occurred in 3% to 10% of patients, in descending order of incidence, included the following Ocular dryness, visual disturbances, ocular burning, foreign body sensation, eye pain, pigmentation of the periocular skin, blepharitis, cataract, superficial punctate keratitis, eyelid erythema, ocular irritation, eyelash darkening. 

Contraindications Hypersensitivity to bimatoprost or any other component of the formulation... 

Latanoprost, bimatoprost, travoprost, unoprostone Increased outflow Topical... 

Penile injection (Caverject, Edex) 5, 10, 20, 40 meg sterile powder for reconstitution Parenteral (Prostin VR Pediatric) 500 mcg/mL ampules Bimatoprost (Lumigan)... 

Topical PGE2 and PGF2qi significantly reduce intraocular pressure for at least 24 hours and are used in the treatment of glaucoma. Derivatives of the isopropyl ester of PGF2qi appear to be the most effective. Transient ocular adverse effects include conjunctival hyperemia, local irritation, intermittent photophobia, and pain in the eye (66-68). Newer derivatives, such as latanoprost, travoprost, and bimatoprost, appear to be better tolerated, with less severe and less frequent adverse effects (69). They reduce intraocular pressure by increasing uveoscleral outflow. 

Bimatoprost is an analogue of PGF, used to treat glaucoma. It is believed to lower intraocular pressure by increasing the outflow of aqueous humor through both the trabecular meshwork and uveoscleral routes. 

Bimatoprost can cause gradual darkening of the color of the eyes and the eyelid skin, increased thickness, numbers and darkness of eyelashes, conjunctival hyperemia, and ocular pruritus (1). Darkening of the iris occurs in 1.1% of patients (2). 

Eyelash growth was reported in 36 18% of patients after 6 months of using bimatoprost (2). 

Cantor LB. Bimatoprost a member of a new class of agents, the prostamides, for glaucoma management. Expert Opin Investig Drugs 2001 10(4) 721-31. 

Sherwood M, Brandt J. Bimatoprost Study Groups 1 and 2. Six-month comparison of bimatoprost once-daily and twice-daily with timolol twice-daily in patients with elevated intraocular pressure. Surv Ophthalmol 2001 45(Suppl 4) S361-8. 

Seven patients using different topical prostaglandin F2a analogues developed bilateral poliosis, which appeared at 1.5-6 months after the start of therapy (17). Four used latanoprost, two used bimatoprost, and one used travaprost... 

The success of latanoprost has stimulated development of similar prostanoids with ocular hypotensive effects, and bimatoprost, travaprost, and unoprostone are now available. These drugs act at the FP receptor and are administered as drops into the conjunctival sac once or twice daily. Adverse effects include irreversible brown pigmentation of the iris and eyelashes, drying of the eyes, and conjunctivitis. 

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