Bimatoprost Ophthalmic Solution

Bimatoprost Ophthalmic Solution, 0.03% is indicated to treat hypotrichosis of the eyelashes by increasing their growth including length, thickness and darkness.

Pregnancy

Teratogenic effects: In embryo/fetal developmental studies in pregnant mice and rats, abortion was observed at oral doses of bimatoprost which achieved at least 33 or 97 times, respectively, the maximum intended human exposure (based on blood AUC levels after topical ophthalmic administration to the cornea or conjunctival sac).

At doses at least 41 times the maximum intended human exposure, the gestation length was reduced in the dams, the incidence of dead fetuses, late resorptions, peri- and postnatal pup mortality was increased, and pup body weights were reduced.

There are no adequate and well-controlled studies of Bimatoprost Ophthalmic Solution 0.03% administration in pregnant women. Because animal reproductive studies are not always predictive of human response, Bimatoprost Ophthalmic Solution should be administered during pregnancy only if the potential benefit justifies the potential risk to the fetus.

Nursing Mothers

It is not known whether Bimatoprost Ophthalmic Solution is excreted in human milk, although in animal studies, bimatoprost has been shown to be excreted in breast milk. Because many drugs are excreted in human milk, caution should be exercised when Bimatoprost Ophthalmic Solution is administered to a nursing woman.

Pediatric Use

Pediatric use information for patients ages 5 to 17 years is approved for Allergan Inc.'s Bimatoprost Ophthalmic Solution, 0.03% product. However, due to Allergan Inc.’s marketing exclusivity rights, this drug product is not labeled with that pediatric information.

Geriatric Use

No overall clinical differences in safety or effectiveness have been observed between elderly and other adult patients.

Mechanism of Action

Bimatoprost is a structural prostaglandin analog. Although the precise mechanism of action is unknown the growth of eyelashes is believed to occur by increasing the percent of hairs in, and the duration of the anagen or growth phase.

Pharmacokinetics

After one drop of Bimatoprost Ophthalmic Solution 0.03% was administered once daily into both eyes (cornea and/or conjunctival sac) of 15 healthy subjects for two weeks, blood concentrations peaked within 10 minutes after dosing and were below the lower limit of detection (0.025 ng/mL) in most subjects within 1.5 hours after dosing. Mean Cmax and AUC0-24hr values were similar on days 7 and 14 at approximately 0.08 ng/mL and 0.09 ng•hr/mL, respectively, indicating that steady state was reached during the first week of ocular dosing. There was no significant systemic drug accumulation over time.

Bimatoprost is moderately distributed into body tissues with a steady-state volume of distribution of 0.67 L/kg. In human blood, bimatoprost resides mainly in the plasma. Approximately 12% of bimatoprost remains unbound in human plasma.

Bimatoprost is the major circulating species in the blood once it reaches the systemic circulation. Bimatoprost then undergoes oxidation, N-deethylation, and glucuronidation to form a diverse variety of metabolites.

Following an intravenous dose of radiolabeled bimatoprost (3.12 mcg/kg) to six healthy subjects, the maximum blood concentration of unchanged drug was 12.2 ng/mL and decreased rapidly with an elimination half-life of approximately 45 minutes. The total blood clearance of bimatoprost was 1.5 L/hr/kg. Up to 67% of the administered dose was excreted in the urine while 25% of the dose was recovered in the feces.

Bimatoprost Ophthalmic Solution, 0.03% is supplied sterile in opaque white low density polyethylene dispenser bottles and tips with turquoise polystyrene caps accompanied by sterile, disposable applicators:

3 mL in a 4 mL bottle with 70 applicators - NDC 0781-6206-93

5 mL in a 8 mL bottle with 140 applicators - NDC 0781-6206-75

Storage: Store at 2° to 25°C (36° to 77°F).

This medicine is only for use in the eye. Do not take by mouth. Follow the directions on the prescription label. Wash hands before and after use. Tilt the head back slightly and pull down the lower lid with the index finger to form a pouch. Try not to touch the tip of the dropper to your eye or into the pouch. Squeeze the prescribed number of drops into the pouch and gently close the eyes for 1 to 2 minutes. Do not blink. Use your doses at regular intervals. Do not use your medicine more often than directed. If you are using another eye product, wait at least 5 minutes between use of this medicine and the other eye product.

Talk to your pediatrician regarding the use of this medicine in children. Special care may be needed.

They need to know if you have any of these conditions:

• closed angle glaucoma
• eye abrasion, infection, or swelling
• wear contact lenses
• an unusual or allergic reaction to bimatoprost or other medicines, foods, dyes, or preservatives
• pregnant or trying to get pregnant
• breast-feeding

If you miss a dose, use it as soon as you can. If it is almost time for your next dose, use only that dose. Do not use double or extra doses.

Visit your doctor or health care professional for regular checks on your progress. Report any serious side effects right away. Stop using this medicine if your eyes get swollen, painful, or have a discharge, and see your doctor or health care professional as soon as you can.

This medicine may cause your eye, eyelashes, and eyelids to change color. Tell your doctor or health care professional if this happens. If only one eye is being treated with this medicine, a difference may develop between the treated and untreated eye in eyelash length, darkness or thickness, and/or color changes of the eyelid skin or iris. These changes may be permanent.

If you wear contact lenses, take them out before putting drops in the eye. Contact lenses may be put back in 15 minutes after putting the drops in your eyes.

Wear dark glasses if this medicine makes your eyes more sensitive to light.

Keep out of the reach of children.

Store this medicine between 2 and 25 degrees C (36 and 77 degrees F). Throw away any unused medicine after the expiration date.