Generic Name: bimatoprost

Bimatoprost ophthalmic (for the eyes) is used to treat certain types of glaucoma and other causes of high pressure inside the eye. Bimatoprost ophthalmic may also be used for purposes not listed in this medication guide. Important InformationFollow all directions on your medicine label and package. Tell each of your healthcare providers about all your medical conditions, allergies, and all medicines you use. Before taking this medicine you should not use bimatoprost if you are allergic to it. To make sure bimatoprost is safe for you, tell your doctor if you have ever had:

eye surgery or injury;

swelling or infection in your eye;

glaucoma, cataracts, or vision problems;

any type of infection; or

if you are pregnant or breastfeeding. It is not known whether bimatoprost passes into breast milk or if it could harm a nursing baby. You should not breastfeed while using this medicine.

Bimatoprost ophthalmic can slowly change the color of your eyes to brown. These changes may be permanent even after your treatment ends, and may occur only in the colored part of your eye (iris). This could result in the uneven coloring of the iris, with parts of the iris becoming browner than others. Call your doctor if you have eye discomfort or vision changes. Using bimatoprost may increase your risk of developing macular edema (swelling in the center of your retina). Stop using this medicine and call your doctor at once if you have sudden vision loss in one or both eyes. Avoid wearing contact lenses while you are using this medicine. Bimatoprost ophthalmic can make contact lenses uncomfortable to wear. If you use Latanoprost, take it at least 5 minutes before or after bimatoprost ophthalmic.

Drug Interactions

Your doctor should check your progress at regular visits. Tell each of your healthcare providers about all medicines you use, including prescription and over-the-counter medicines, vitamins, and herbal products. Some drugs can affect bimatoprost ophthalmic, and bimatoprost ophthalmic may affect other drugs you are taking. This includes prescription and over-the-counter medicines, vitamins, and herbal products. Not all possible interactions are listed in this medication guide.

Tell your doctor about all your other medicines, especially:

any other eye drops or medications;

cyclosporine (Gengraf, Neoral, Sandimmune); or

travoprost (Travatan). This list is not complete. Other drugs may affect bimatoprost ophthalmic, including prescription and over-the-counter medicines, vitamins, and herbal products. Not all possible drug interactions are listed here.

Bimatoprost ophthalmic (for the eyes) is used to treat certain types of glaucoma and other causes of high pressure inside the eye. Bimatoprost ophthalmic may also be used for purposes not listed in this medication guide.

Pharmacokinetics

The systemic exposure of bimatoprost following ocular administration is low. In a study that included 28 subjects with open-angle glaucoma or ocular hypertension, the mean peak concentration (Cmax) and area under the curve (AUC) of bimatoprost in plasma were both less than 0.1 ng/mL•h and occurred at approximately 5 minutes after dosing. The mean elimination half-life was 45 minutes.

Nonclinical Toxicology

Carcinogenesis, Mutagenesis, Impairment of Fertility

In two-year carcinogenicity studies in CD-1 mice, no evidence of tumorigenicity was observed with bimatoprost at oral doses up to 0.03 mg/kg/day (approximately 10 times the maximum recommended human ocular dose of 3.3 mcg/day, based on body surface area). Bimatoprost was not mutagenic or clastogenic in an Ames test or in a chromosome aberration assay in Chinese hamsters.

In rats, bimatoprost administration at subcutaneous doses up to 300 mcg/kg/day (approximately 100 times the maximum recommended human ocular dose) for 78 weeks prior to mating, and through gestation and lactation, produced no adverse effects on fertility or reproductive performance of the offspring.

Clinical Studies

Effectiveness was demonstrated in two 12-week multicenter, randomized, masked studies in patients with open-angle glaucoma or ocular hypertension. The two studies were similar in design and are combined here for the presentation. A total of 862 subjects were randomized, 431 to bimatoprost and 431 to timolol maleate. The mean baseline intraocular pressure (IOP) was similar between the treatment groups (bimatoprost 25.8 mmHg, timolol 26.5 mmHg). Patients had a mean age of approximately 64 years (range: 21-93), approximately 53% were female, and 97% were white.

Both studies demonstrated that bimatoprost was significantly more effective than timolol at reducing IOP when dosed once daily in the evening. The results for the primary efficacy measure are presented in Table 1.

Side Effects

The following adverse reactions have been identified during post-approval use of bimatoprost ophthalmic solution. Because these reactions are reported voluntarily from a population of uncertain size, it is not always possible to reliably estimate their frequency or establish a causal relationship to drug exposure.

The most common adverse reaction related to the use of bimatoprost ophthalmic solution 0.03% was conjunctival hyperemia, occurring in approximately 4% of patients in clinical trials. Other common adverse reactions (occurring in 1% to 3% of patients) include: iritis/uveitis, eye pain/discomfort, increased lacrimation, and a decrease in visual acuity. The following additional adverse reactions have been reported during post-marketing experience with bimatoprost ophthalmic solution 0.03%. These reactions are presented in order of decreasing frequency within each category.

Dosage and Administration

Bimatoprost Ophthalmic Solution 0.03% is supplied as a sterile, preservative-free aqueous solution of bimatoprost-free base 0.3 mg/mL in plastic bottles:

7.5 mL in a white low-density polyethylene (LDPE) bottle with a natural HDPE dispensing plug and white polypropylene cap bearing code TZC on the plug and 5AL on the cap (NDC 0023-0111-05).

15 mL in a white LDPE bottle with natural HDPE dispensing plug and white polypropylene cap bearing code TZC on the plug and 5AM on the cap (NDC 0023-0111-15).

Each mL of solution contains a 0.3 mg bimatoprost-free base (equivalent to 0.3386 mg of the active moiety, bimatoprost). It also contains disodium phosphate anhydrous, mannitol, and sodium chloride in Water for Injection. The pH is adjusted to 7.8 ± 0.2 with hydrochloric acid or sodium hydroxide before being placed into the bottle. Bimatoprost Ophthalmic Solution has an osmolality of approximately 290 mOsm/mL and tonicity of approximately 270 mOsm/kg. It does not contain any preservatives; therefore, once opened it should be used within 4 weeks.

Overdose

There have been no reports of overdosage with Lumigan in humans. If overdose occurs, general supportive care is indicated. Because bimatoprost is highly protein bound if dialysis is considered, it may not be an effective method of removing the drug from the body.

Storage

Bimatoprost Ophthalmic Solution 0.03% should be stored at room temperature, 15°C to 25°C (59°F to 77°F). Protect from light. Do not freeze. Once opened, use solution within 4 weeks. Discard any remaining solution after 4 weeks of opening the bottle.