Bimatoprost - IMCURE

What is Bimatoprost?

11 DESCRIPTION Bimatoprost ophthalmic solution 0.03% is a synthetic prostamide analog with ocular hypotensive activity. Its chemical name is ( Z )-7-[(1 R ,2 R ,3 R ,5 S )-3,5-Dihydroxy-2-[(1 E ,3 S )-3-hydroxy-5-phenyl-1-pentenyl]cyclopentyl]-5- N -ethylheptenamide, and its molecular weight is 415.58. Its molecular formula is C 25 H 37 NO 4 . Its chemical structure is: Bimatoprost is a white to off-white color powder, which is freely soluble in methanol and slightly soluble in water. Bimatoprost ophthalmic solution 0.03% is a clear, isotonic, colorless, sterile ophthalmic solution with an osmolality of approximately 290 mOsmol/kg. Bimatoprost ophthalmic solution 0.03% contains Active: bimatoprost 0.3 mg/mL; Inactives: benzalkonium chloride 0.05 mg/mL, citric acid monohydrate, disodium hydrogen phosphate heptahydrate, sodium chloride 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 to 7.8. Chemical Structure

Uses of Bimatoprost

Established uses

1 INDICATIONS AND USAGE Bimatoprost ophthalmic solution 0.03% is indicated for the reduction of elevated intraocular pressure in patients with open angle glaucoma or ocular hypertension.
Bimatoprost ophthalmic solution 0.03% is a prostaglandin analog indicated for the reduction of elevated intraocular pressure in patients with open angle glaucoma or ocular hypertension.
( 1 )

How Bimatoprost works

In more detail: 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.

How to take Bimatoprost

2 DOSAGE AND ADMINISTRATION 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 8 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 (5) minutes apart. One drop in the affected eye(s) once daily in the evening. ( 2 )

Dosage

Follow the dose prescribed by your doctor or pharmacist. The ranges below are general information, not a personal prescription.

Adults: 2 DOSAGE AND ADMINISTRATION 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 8 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 (5) minutes apart. One drop in the affected eye(s) once daily in the evening. ( 2 )

Side effects of Bimatoprost

Common

6 ADVERSE REACTIONS The following adverse reactions are described elsewhere in the labeling: • Pigmentation [see Warnings and Precautions (5.1) ] • Eyelash Changes [see Warnings and Precautions (5.2) ] • Intraocular Inflammation [see Warnings and Precautions (5.3) ] • Macular Edema [see Warnings and Precautions (5.4) ] • Hypersensitivity [see Contraindications (4) ] Most common adverse reaction (45%) is conjunctival hyperemia ( 6.1 ).
To report SUSPECTED ADVERSE REACTIONS, contact Aurobindo Pharma USA, Inc.
at 1-866-850-2876 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch .
6.1 Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice.
In clinical trials, the most frequent events associated with the use of bimatoprost ophthalmic solution 0.03% occurring in approximately 15% to 45% of patients, in descending order of incidence, included conjunctival hyperemia, growth of eyelashes, and ocular pruritus.
Approximately 3% of patients discontinued therapy due

Warnings and who should not take it

Who should NOT take Bimatoprost?

4 CONTRAINDICATIONS Bimatoprost ophthalmic solution 0.03% is contraindicated in patients with hypersensitivity to bimatoprost or to any of the ingredients [see Adverse Reactions (6.2) ].
Hypersensitivity.

Overdose

10 OVERDOSAGE 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 general toxicity studies, doses up to 100 mg/kg/day did not produce any toxicity. This dose expressed as mg/m 2 is at least 70 times higher than the accidental dose of one bottle of bimatoprost ophthalmic solution 0.03% for a 10 kg child.

Safety at a glance

PregnancyCaution

8.1 Pregnancy Risk Summary 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

Children and elderly

Children

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.

Elderly

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

Frequently asked questions

What is Bimatoprost used for?

1 INDICATIONS AND USAGE Bimatoprost ophthalmic solution 0.03% is indicated for the reduction of elevated intraocular pressure in patients with open angle glaucoma or ocular hypertension., Bimatoprost ophthalmic solution 0.03% is a prostaglandin analog indicated for the reduction of elevated intraocular pressure in patients with open angle glaucoma or ocular hypertension., ( 1 ).

How should I take Bimatoprost?

2 DOSAGE AND ADMINISTRATION 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 8 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 (5) minutes apart. One drop in the affected eye(s) once daily in the evening. ( 2 )

What are the common side effects?

6 ADVERSE REACTIONS The following adverse reactions are described elsewhere in the labeling: • Pigmentation [see Warnings and Precautions (5.1) ] • Eyelash Changes [see Warnings and Precautions (5.2) ] • Intraocular Inflammation [see Warnings and Precautions (5.3) ] • Macular Edema [see Warnings and Precautions (5.4) ] • Hypersensitivity [see Contraindications (4) ] Most common adverse reaction (45%) is conjunctival hyperemia ( 6.1 )., To report SUSPECTED ADVERSE REACTIONS, contact Aurobindo Pharma USA, Inc., at 1-866-850-2876 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch ., 6.1 Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice., In clinical trials, the most frequent events associated with the use of bimatoprost ophthalmic solution 0.03% occurring in approximately 15% to 45% of patients, in descending order of incidence, included conjunctival hyperemia, growth of eyelashes, and ocular pruritus., Approximately 3% of patients discontinued therapy due.

Who should not take Bimatoprost?

4 CONTRAINDICATIONS Bimatoprost ophthalmic solution 0.03% is contraindicated in patients with hypersensitivity to bimatoprost or to any of the ingredients [see Adverse Reactions (6.2) ].; Hypersensitivity..

Can I take Bimatoprost during pregnancy?

8.1 Pregnancy Risk Summary 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

Can children take Bimatoprost?

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.