(LATANOPROST 50mg/ml)
DESCRIPTION
Drulatan® contains Latanoprost which is a prostaglandin F2a analogue.
Latanoprost is chemically identified as isopropyl-(2)-7[1R, 2R, 3R 5S) 3,5 – dihydoxy-2-[{3R) -3 – hydroxy -5 – phenyl pentyl] cyclo- pentyl] -5- heptenoate. The molecular formula is C26H40O5 and its molecular weight is 432.58.
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- WT. = 432.58
LATANOPROST
PHARMACOLOGY
Mechanism of Action:
Latanoprost is a prostanoid selective FP receptor agonist that is believed to reduce the intraocular pressure (IOP) by increasing the outflow of aqueous humor.
The main mechanism of action is increased uveoscleral outflow. Elevated IOP represents a major risk factor for glaucomatous field loss.
PHARMACOKINETICS/PHARMACODYNAMICS
Absorption: Latanoprost is absorbed through the cornea where the isopropyl ester prodrug is hydrolysed to the acid form to become biologically active. Peak concentration in the aqueous humor is reached about two hours after topical administration.
Metabolism: Latanoprost, an isopropyl ester prodrug is hydrolysed by esterases in the cornea to the biologically active acid. The active acid of Latanoprost reaching the systemic circulation, is primarily metabolized by the liver to the 1,2-dinor and 1,2,3,4-tetranor metabolites via fatty acid
b-oxidation.
Excretion: Elimination of the acid of Latanoprost from human plasma is rapid (t1/2 = 17 min) after both intravenous and topical administration. Systemic clearance is approximately 7ml/min/kg. After hepatic b-oxidation, the metabolites are mainly eliminated via the kidneys. About 88% and 98% of the administered dose is recovered in the urine after topical and intravenous dose respectively.
INDICATIONS
Drulatan® sterile ophthalmic solution is indicated for the reduction of elevated intraocular pressure in patients with open-angle glaucoma or ocular hypertension.
CONTRAINDICATIONS
Drulatan® is contraindicated in patients with known hypersensitivity to Latanoprost, Benzalkonium Chloride or any other ingredient in the product.
WARNINGS
Latanoprost ophthalmic solution has been reported to cause changes to pigmented tissues. Reported changes include increased pigmentation of the iris, periorbital tissue (eyelid) and eyelashes as well as growth of eyelashes.
After discontinuation, pigmentation of the iris is likely to be permanent while that of periorbital tissue and eyelash changes have been reported to be reversible in some patients.
PRECAUTIONS
Latanoprost sterile ophthalmic solution may gradually increase the pigmentation of the iris due to increased melanin content in the stromal melanocyte of the iris rather than to an increase in the number of melanocyte. Eyelid skin darkening which may be reversible has been reported in association with the use of Latanoprost
Drulatan® must be used with caution in patients with a history of intraocular inflammation (iritis/uveitis) and should generally not be used in patients with active intraocular inflammation.
Also during treatment with Latanoprost macular oedema, including cystoid macular oedema has been reported.
Contact lenses should also be removed before administration of Drulatan® and may be reinserted 15 minutes after administration.
If more than one topical ophthalmic drug is being used, the drugs should be administered at least five (5) minutes apart.
Pregnancy: Drulatan® should be used during pregnancy only if the potential benefit justifies the potential risks to the foetus.
Nursing Mothers: Drulatan® should be administered with caution to nursing mothers. This is because it is not known whether Latanoprost or its metabolites are excreted in human milk.
Paediatric patients: safety effectiveness in paediatric have not been established.
Geriatric patients: no difference in safety and effectiveness have been observed between elderly and young patients.
KEEP OUT OF THE REACH OF CHILDREN!
ADVERSE REACTIONS
These include eyelash changes (increased length, thickness, pigmentation, and number of lashes), eyelid skin darkening, intraocular inflammation (iritis/uvetis), macular oedema including cystoid macular oedema.
OVERDOSAGE
The ocular effects of Latanoprost administration at high doses are not known apart from ocular irritation, conjunctival or episcleral hyperemia.
However, if over dosage with Drulatan® sterile ophthalmic solution occurs, treatment should be symptomatic.
DOSAGE AND ADMINISTRATION
Recommended dosage is one drop (1.5mg) in the affected eye(s) once daily in the evening.
Administration of Drulatan® should not exceed once daily since it has been shown that more frequent administration may decrease the intraocular pressure lowering effect.
Intraocular pressure reduction starts approximately 3 to 4 hours after administration and the maximum effect is reached after 8 to 12 hours.
STORAGE
Store unopened bottle(s) in a refrigerator (20 – 80C). Once you have opened, bottle may be stored at a temperature below 30oC, away from moisture, heat and light. Discard after 28days of opening the bottle.
PRESENTATION
Drulatan® sterile ophthalmic solution is a clear, isotonic, buffered, preserved solution of Latanoprost 0.005% (50mg/ml).
It is supplied as a 2.5ml solution in a sterile lupolen bottle.