LUMERA

Bimatoprost, also known as Latisse or Lumigan, belongs to a group of drugs called prostamides, which are synthetic structural analogs of prostaglandin.

Bimatoprost, marketed by Allergan, is administered in both the ophthalmic solution and implant form.

It has the ability to reduce ocular hypotension, proving effective in conditions such as ocular hypertension and glaucoma. 13, 14, 15, 20 Bimatoprost is also used to treat eyelash hypotrichosis, or sparse eyelash growth.

It was initially approved by the

FDA in for ocular hypertension and later approved for hypothrichosis in 2008, as eyelash growth became a desirable adverse effect for patients using this drug.

Bimatoprost is used for the reduction of elevated intraocular pressure in patients with open-angle glaucoma or ocular hypertension.

These patients must be intolerant to other intraocular pressure lowering medications or inadequately responsive to other treatments.

Bimatoprost is also indicated to treat eyelash hypotrichosis.

High intraocular pressure is a major risk factor for glaucoma-related visual field loss.

A linear relationship exists between intraocular pressure and the risk of damaging the optic nerve, which can lead to considerable visual impairment.

Therefore, conditions such as ocular hypertension and glaucoma can cause dangerous elevations of intraocular pressure.

Bimatoprost rapidly decreases intraocular pressure and reduces the risk for visual field loss from ocular hypertension due to various causes.

Other effects of this drug may include gradual changes in eyelid pigmentation, changes in iris pigmentation, changes in eyelash pigmentation, growth and thickness.

Patients should be informed of these possible effects, especially if this drug is only administered to one eye, which may noticeably change in appearance with bimatoprost treatment.

F2-alpha receptor Agonist Prostaglandin E2 receptor EP1 subtype Agonist Prostaglandin E2 receptor EP3 subtype Agonist.

This drug is absorbed systemically when administered to the eye.

A study was performed on 15 healthy volunteers and bimatoprost ophthalmic solution 0.03% was administered once daily for 14 days.

The mean

Cmax was approximately 0.08 ng/mL and AUC0-24hr was approximately 0.09 on days and 14 of the study.

By 10 minutes, peak blood concentration was achieved.

Bimatoprost was not detectable at 1.5 hours after administration in most subjects.

The maximum blood concentration in a study of 6 healthy volunteers was determined to be 12.2 ng/mL.

Steady state was reached in the first week of dosing.

One drug label mentions that onset of decreased intraocular pressure occurs approximately 4 hours after the first administration and the peak effect occurs in the range of 8-12 hours.

Bimatoprost effects may last up to 24 hours.

The volume of distribution at steady state is 0.67 L/kg. 13, 15.

Bimatoprost is hydrolyzed to its active form, bimatoprost acid, in the eye.

Bimatoprost undergoes oxidation, N-deethylation, and glucuronidation after it is systemically absorbed, and this leads to the production of various metabolites.

In vitro studies show that

CYP3A4 is an enzyme that participates in the metabolism of bimatoprost.

Despite this, many enzymes and pathways metabolize bimatoprost, therefore, no significant drug-drug interactions are likely to occur.

Glucuronidated metabolites comprise most of the excreted drug product in the blood, urine, and feces in rats.

Hover over products below to view reaction partners Bimatoprost 17-Phenyl-Trinor-PGF2alpha.

One pharmacokinetic study of bimatoprost in 6 healthy volunteers determined that 67% of the administered dose was found to be excreted in the urine while 25% of the dose was recovered in the feces.

The elimination half-life of bimatoprost is approximately 45 minutes. 13, 14.

The clearance was measured to be 1.5 L/hr/kg in healthy subjects receiving Intravenous administration of bimatoprost dosed at 3.12 ug/kg. 13, 14.

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No information is available at this time regarding bimatoprost overdose in humans.

Provide supportive symptomatic treatment if an overdose occurs.

Bimatoprost ophthalmic solution 0.03% is contraindicated in patients with hypersensitivity to bimatoprost or to any of the ingredients.

The recommended dosage is one drop in the affected eye(s) once daily in the evening.

Bimatoprost ophthalmic solution 0.03% should not be administered more than once daily since it has been shown that more frequent administration of prostaglandin analogs may decrease the intraocular pressure lowering effect.

Reduction of the intraocular pressure starts approximately 4 hours after the first administration with maximum effect reached within approximately to 12 hours.

Bimatoprost ophthalmic solution 0.03% may be used concomitantly with other topical ophthalmic drug products to lower intraocular pressure.

If more than one topical ophthalmic drug is being used, the drugs should be administered at least five minutes apart.

One drop in the affected eye(s) once daily in the evening.

Bimatoprost ophthalmic solution 0.03% is a clear, colorless sterile solution.

Practically free from visible particles packed in opaque white LDPE container with LDPE nozzle and turquoise color HDPE cap. 0.03% 2.5 mL fill in 5 mL bottle NDC 65862-802-44 5 mL fill in 10 mL bottle NDC 65862-802-05 7.5 mL fill in 10 mL bottle NDC 65862-802-10 Storage: Store at 2°C to 25°C (36°F to 77°F).

After opening, bimatoprost ophthalmic solution, 0.03% can be used until the expiration date stamped on the bottle.

There are no adequate and well-controlled studies of bimatoprost ophthalmic solution 0.03% administration in pregnant women.

There is no increase in the risk of major birth defects or miscarriages based on bimatoprost postmarketing experience.

In embryofetal developmental studies, administration of bimatoprost in pregnant mice and rats during organogensis, resulted in abortion and early delivery at oral doses at least 33 times (mice) or 94 times (rats) the human exposure at the recommended clinical dose (based on blood area under the curve [AUC] levels).

These adverse effects were not observed at 2.6 times (mice) and 47 times (rats) the human exposure at the recommended clinical dose.

In pre/postnatal development studies, administration of bimatoprost to pregnant rats from organogenesis to the end of lactation resulted in reduced gestation length and fetal body weight, and increased fetal and pup mortality at oral doses at least 41 times the human systemic exposure at the recommended clinical dose (based on blood AUC levels).

No adverse effects were observed in rat offspring at exposures estimated at 14 times the human exposure at the recommended clinical dose (based on blood AUC levels).

Because animal reproductive studies are not always predictive of human response bimatoprost ophthalmic solution 0.03% should be administered during pregnancy only if the potential benefit justifies the potential risk to the fetus.

In an embryofetal development rat study, abortion was observed in pregnant rats administered bimatoprost orally during organogenesis at 0.6 mg/kg/day (94 times the human systemic exposure at the recommended human ophthalmic dose [RHOD], based on AUC).

Level (NOAEL) for abortion was 0.3 mg/kg/day (estimated at 47 times the human systemic exposure at the RHOD, based on AUC).

No abnormalities were observed in rat fetuses at doses up to 0.6 mg/kg/day. In an embryofetal development mouse study, abortion and early delivery were observed in pregnant mice administered bimatoprost orally during organogenesis at doses greater than or equal to 0.3 mg/kg/day (33 times the human systemic exposure at the RHOD, based on AUC).

NOAEL for abortion and early delivery was 0.1 mg/kg/day (2.6 times the human systemic exposure at the RHOD, based on AUC).

No abnormalities were observed in mouse fetuses at doses up to 0.6 mg/kg/day (72 times the human systemic exposure at the RHOD, based on AUC).

In a pre/postnatal development study, treatment of pregnant rats with bimatoprost orally from gestation day to lactation day 20 resulted in reduced gestation length, increased late resorptions, fetal deaths, and postnatal pup mortality, and reduced pup body weight at doses greater than or equal to 0.3 mg/kg/day. These effects were observed at exposures at least 41 times the human systemic exposure at the RHOD, based on AUC.

NOAEL for postnatal development and mating performance of the offspring was 0.1 mg/kg/day (estimated at 14 times the human systemic exposure at the RHOD, based on AUC).

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.

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