Drug Information

Drug Interaction:

Allow at least 5 minutes between application of other topical opthalmic agents

Indication:

LUMIGAN® 0.01% and 0.03% (bimatoprost ophthalmic solution)

Initial U.S. Approval: 2001

LIST OF DRUGS DURING 2006

Sr.No- 73

Name of the Drug- Bimatoprost 300mg +

Timolol (as maleate) 5mg/ml eye drops Pharmacological Classification- For reduction of IOP

Date of Approval- 05-07-2006

Approved by U.S.FDA on 30-12-2006 (Ref- FDA approved List

Glaucoma or ocular hypertension

Approved by (DCI) Drug Controller GENERAL - India For Marketing

(Ref- IDMA Publication)

Name of Drug Indication Date of Approval

1. Bimatoprost Anti-Glaucoma 08-01-2002

2.Binatoprost 300mg + Timolol maleate 05-07-2006

5mg/ml eye drops

For reduction of IOP

3. Binatoprost eye drops 0.1mg.ml 05-08-2010

For the treatment of hypotrichosis of the eye lashes by

increasing their growth including length, thickness and

darkness

4. Binatoprost ophthalmic solution 09-10-2010

0.1% w/v - Addl. stgth

same as approved

5. Binatoprost ophthalmic solution 0.03% 30-03-2009

For the treatment of hypotrichosis of the eye lashes by

increasing their growth including length, thickness and

darkness

FIXED DOSE COMBINATIONS APPROVED BY DCG(I)

FROM JANUARY 1961 TILL NOVEMBER 2014

Name of Drug Indication Date of Approval

1.Bimaprost 0.3mg+ 28-02-2006

Timolol maleate IP eq.to Ttimlol 5.0mg

eye drops

For the reduction of IOP patients with open angle glaucoma, who are

insufficiently responsive to topical beta blockers or prptaglandin

analouges

2.Bimsprost 300mg+ 07-05-2006

Timolol maleate 5mg/ml eye drops

For reduction of IOP

Adverse Reaction:

Conjuntival hyperaemia Pain, irritation Growth and darkening of ey lashes , eye lids, iris discoloration (may be permanent )

Foreign body sensation, keratitis

Headache, visual disturbances

Ocular pruritus, itching or dryness,

Blepharitis, cataract Photophobia, infection

Asthenia, hirutism Hypertension

Conjunctival headache, raised liver enzymes

Contra-Indications:

Lactation

Special precautions

Hepatic , renal or respiratory impairment

History of significant ocular viral infection

Uveitis, or iritis

Risk factors of bradycardia, hypotension or macular oedema

Warn patients of possible eye lash growth, darkenening of eye lids, and change in color which may not be noticeble until several months

Monitor keratopathy in patients with dry eyes Contact lens ( leave interval of 15 minutes before reinserting )

Ocular inflammation

Pregnancy

Dosages/ Overdosage Etc:

Indication-

Glaucoma or ocular hypertension

Dosage-

1 drop in affected eye( s) once daily in the evening

Apply pressure to tear duct immediately following application

Wait for 5 minutes beforeapplying to the other eye medication

Do not exceed the recommended dose

Not recommended for children below 18 years

Patient Information:

PATIENT COUNSELING INFORMATION

1 Potential for Pigmentation

Patients should be advised about the potential for increased brown pigmentation

of the iris, which may be permanent.

Patients should also be informed about the possibility of eyelid skin darkening,

which may be reversible after discontinuation of LUMIGAN® 0.01% and 0.03%

(bimatoprost ophthalmic solution).

2. Potential for Eyelash Changes

Patients should also be informed of the possibility of eyelash and vellus hair changes

in the treated eye during treatment with LUMIGAN® 0.01% and 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.

3. Handling the Container

Patients should be instructed 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.

4. When to Seek Physician Advice

Patients should also be advised 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 LUMIGAN® 0.01% and 0.03%.

5. Use with Contact Lenses

Patients should be advised that LUMIGAN® 0.01% and 0.03% contains benzalkonium

chloride,which may be absorbed by soft contact lenses. Contact lenses should be

removed prior to instillation of LUMIGAN® and may be reinserted 15 minutes

following its administration.

6. Use with Other Ophthalmic Drugs

Patients should be advised that if more than one topical ophthalmic drug is being used,

the drugs should be administered at least five (5) minutes between applications.

U.S. Patents 5,688,819 and 6,403,649

Pharmacology/ Pharmacokinetics:

CLINICAL PHARMACOLOGY

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.

2. Pharmacokinetics

Absorption: 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.

Distribution: Bimatoprost is moderately

Pregnancy and lactation:

USE IN SPECIFIC POPULATIONS

1. Pregnancy

Pregnancy Category C

There are no adequate and well-controlled studies of LUMIGAN® 0.01% and 0.03%

(bimatoprost ophthalmic solution) administration in pregnant women.

Because animal reproductive studies are not always predictive of human response

LUMIGAN® should be administered during pregnancy only if the potential benefit

justifies the potential risk to the fetus.

2. Nursing Mothers

It is not known whether LUMIGAN® 0.01% and 0.03% 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 LUMIGAN® is administered to a nursing woman.

3. 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.

4. Geriatric Use

No overall clinical differences in safety or effectiveness have been observed

between elderly and other adult patients.

Bimatoprost - @-Agents for glaucoma-(FDC-List) (July 2006)

Drug Interaction

Indication

Adverse Reaction

Contra-Indications

Dosages/ Overdosage Etc

Patient Information

Pharmacology/ Pharmacokinetics

Pregnancy and lactation