Bimatoprost (Page 2 of 3)

8.2 Lactation

Risk Summary

It is not known whether topical ocular treatment with bimatoprost ophthalmic solution 0.03% could result in sufficient systemic absorption to produce detectable quantities in human milk. In animal studies, bimatoprost has been shown to be present in breast milk of lactating rats at an intravenous dose (i.e., 1 mg/kg) 324 times the RHOD (on a m2g/m basis), however no animal data is available at clinically relevant doses.

The developmental and health benefits of breastfeeding should be considered along with the mother’s clinical need for bimatoprost ophthalmic solution 0.03% and any potential adverse effects on the breastfed child from bimatoprost ophthalmic solution 0.03%.

8.4 Pediatric Use

Use in pediatric patients below the age of 16 years is not recommended because of potential safety concerns related to increased pigmentation following long-term chronic use.

8.5 Geriatric Use

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


No information is available on overdosage in humans. If overdose with bimatoprost ophthalmic solution 0.03% occurs, treatment should be symptomatic.

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 ophthalmic solution 0.03% for a 10 kg child.


Bimatoprost ophthalmic solution 0.03% is a synthetic prostamide analog with ocular hypotensive activity. Its chemical name is (Z)-7-[(1R ,2R ,3R ,5S)-3,5-Dihydroxy-2 [(1E ,3S) 3-hydroxy-5-phenyl-1-pentenyl]cyclopentyl]-5-N -ethylheptenamide, and its molecular weight is 415.58. Its molecular formula is C25 H37 NO4 . Its chemical structure is:

Molecuar Structure
(click image for full-size original)

Bimatoprost is a powder, which is very soluble in ethyl alcohol and methyl alcohol and slightly soluble in water. Bimatoprost ophthalmic solution 0.03% is a clear, isotonic, colorless, sterile ophthalmic solution with an osmolality of approximately between 260 and 320 mOsmol/kg.

Bimatoprost ophthalmic solution 0.03% contains Active: bimatoprost 0.3 mg/mL; Inactives: benzalkonium chloride 0.05 mg/mL; sodium chloride; sodium phosphate, dibasic (Heptahydrate); citric acid monohydrate; and water for injection. Sodium hydroxide and/or hydrochloric acid may be added to adjust pH. The pH during its shelf life ranges from 6.8-7.8.


12.1 Mechanism of Action

Bimatoprost, a prostaglandin analog, is a synthetic structural analog of prostaglandin with ocular hypotensive activity. It selectively mimics the effects of naturally occurring substances, prostamides. Bimatoprost is believed to lower intraocular pressure (IOP) in humans by increasing outflow of aqueous humor through both the trabecular meshwork and uveoscleral routes. 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.

12.3 Pharmacokinetics


After one drop of bimatoprost ophthalmic solution 0.03% was administered once daily to both eyes 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 following ocular dosing. 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.


13.1 Carcinogenesis, Mutagenesis, Impairment of Fertility


Bimatoprost was not carcinogenic in either mice or rats when administered by oral gavage for 104 weeks at doses of up to 2 mg/kg/day and 1 mg/kg/day respectively (at least 192 and 291 times the human systemic exposure at the RHOD, respectively, based on blood AUC levels).


Bimatoprost was not mutagenic or clastogenic in the Ames test, in the mouse lymphoma test, or in the in vivo mouse micronucleus tests.

Impairment of Fertility

Bimatoprost did not impair fertility in male or female rats at doses up to 0.6 mg/kg/day (at least 103 times the human system exposure at the RHOD, based on blood AUC levels).


In clinical studies of patients with open angle glaucoma or ocular hypertension with a mean baseline IOP of 26 mmHg, the IOP-lowering effect bimatoprost ophthalmic solution 0.03 once daily (in the evening) was 7-8 mmHg.


Bimatoprost ophthalmic solution 0.03% is supplied sterile in opaque white low density polyethylene ophthalmic dispenser bottles and tips with turquoise polystyrene caps in the following sizes:

2.5 mL fill in 5 mL container -NDC 70069-401 -01

5 mL fill in 5 mL container -NDC 70069-402 -01

7.5 mL fill in 10 mL container -NDC 70069-403 -01

Storage: Store at 2°-25°C (36°-77°F). After opening, bimatoprost ophthalmic solution 0.03% can be used until the expiration date stamped on the bottle.


Potential for Pigmentation

Advise patients about the potential for increased brown pigmentation of the iris, which may be permanent. Also inform patients about the possibility of eyelid skin darkening, which may be reversible after discontinuation of bimatoprost ophthalmic solution 0.03%.

Potential for Eyelash Changes

Inform patients of the possibility of eyelash and vellus hair changes in the treated eye during treatment with bimatoprost ophthalmic solution 0.03%. These changes may result in a disparity between eyes in length, thickness, pigmentation, number of eyelashes or vellus hairs, and/or direction of eyelash growth. Eyelash changes are usually reversible upon discontinuation of treatment.

Handling the Container

Instruct patients to avoid allowing the tip of the dispensing container to contact the eye, surrounding structures, fingers, or any other surface in order to avoid contamination of the solution by common bacteria known to cause ocular infections. Serious damage to the eye and subsequent loss of vision may result from using contaminated solutions.

When to Seek Physician Advice

Advise patients that if they develop an intercurrent ocular condition (e.g., trauma or infection), have ocular surgery, or develop any ocular reactions, particularly conjunctivitis and eyelid reactions, they should immediately seek their physician’s advice concerning the continued use of bimatoprost ophthalmic solution 0.03%.

Contact Lens Use

Advise patients that bimatoprost ophthalmic solution 0.03% contains benzalkonium chloride, which may be absorbed by soft contact lenses. Contact lenses should be removed prior to instillation of bimatoprost ophthalmic solution 0.03% and may be reinserted 15 minutes following its administration.

Use with Other Ophthalmic Drugs

Advise patients that if more than one topical ophthalmic drug is being used, the drugs should be administered at least five (5) minutes between applications.

Manufactured for:

Somerset Therapeutics, LLC

Hollywood, FL 33024

Made in India

Code No.:KR/DRUGS/KTK/28/289/97



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