Pharmacology: Pharmacodynamics: The active substance latanoprost, a prostaglandin F2α analogue, is a selective prostanoid FP receptor agonist which reduces the intraocular pressure by increasing the outflow of aqueous humour. Reduction of the intraocular pressure in man starts about three to four hours after administration and maximum effect is reached after eight to twelve hours. Pressure reduction is maintained for at least 24 hours.
The main mechanism of action is increased uveoscleral outflow, although some increase in outflow facility (decrease in outflow resistance) has been reported in man.
Latanoprost is effective as monotherapy and in combination with beta-adrenergic antagonists (timolol). The effect of latanoprost is additive in combination with adrenergic agonists (dipivalyl epinephrine), oral carbonic anhydrase inhibitors (acetazolamide) and at least partly additive with cholinergic agonists (pilocarpine).
Latanoprost has not been found to have any effect on the blood-aqueous barrier.
Latanoprost has no or negligible effects on the intraocular blood circulation when used at the clinical dose and studied in monkeys. However, mild to moderate conjunctival or episcleral hyperaemia may occur during topical treatment.
Latanoprost has not induced fluorescein leakage in the posterior segment of pseudophakic human eyes during short-term treatment.
Pharmacokinetics: Latanoprost (mw 432.58) is an isopropyl ester prodrug which per se is inactive, but after hydrolysis to the acid of latanoprost becomes biologically active.
The prodrug is well absorbed through the cornea and all drug that enters the aqueous humour is hydrolysed during the passage through the cornea.
There is practically no metabolism of the acid of latanoprost in the eye. The main metabolism occurs in the liver. The half life in plasma is 17 minutes in man. The main metabolites, the 1,2-dinor and 1,2,3,4-tetranor metabolites, exert no or only weak biological activity in animal studies and are excreted primarily in the urine.
Reduction of elevated intraocular pressure (IOP) in patients with open-angle glaucoma, chronic angle closure glaucoma, and ocular hypertension.
Reduction of elevated intraocular pressure in paediatric patients with elevated intraocular pressure and paediatric glaucoma.
Ocular use; Use in adults (including the elderly): The recommended dosage is one drop in the affected eye(s) once daily. Optimal effect is obtained if the product is administered in the evening. If one does is missed, treatment should continue with the next dose as normal.
The dosage of the product should not exceed once daily since it has been shown that more frequent administration decreases the intraocular pressure lowering effect.
If more than one topical ophthalmic drug is being used, the drugs should be administered at least five minutes apart.
Contact lenses should be removed before instillation of the eye drops and may be reinserted after 15 minutes.
Pediatric Population: Latanoprost eye drops may be used in paediatric patients at the same posology as in adults. No data are available for preterm infants (less than 36 weeks gestational age). Data in the age group <1 year (4 patients) are limited.
Apart from ocular irritation and conjunctival hyperaemia, no other ocular side effects are known if the product is overdosed.
More than 90% is metabolized during the first pass through the liver. If overdosage with the product occurs, treatment should be symptomatic.
Avetaprost 0.005% Eye drop should not be used if patients are allergic (hypersensitive) to latanoprost, benzalkonium chloride or any of the other ingredients of Avetaprost 0.005% Eye drop.
Warnings: The product has been reported to cause changes to pigmented tissues. The most frequently reported changes have been increased pigmentation of the iris, periorbital tissue (eyelid) and eyelashes, and growth of eyelashes. Pigmentation of the iris is likely to be permanent.
The colour change is due to increased melanin content in the stromal melanocytes of the iris and not to an increase in number of melanocytes. The long-term effect on the melanocytes and the consequences of potential injury to the melanocytes and/or deposition of pigment granules to other areas of the eye are currently unknown. The iris colour change is slightly in the majority of cases and often not observed clinically. Patients who receive treatment should be informed of the possibility of increased pigmentation.
Eyelid skin darkening, which may be reversible, has been reported in association with the use of this medication.
The product may gradually change eyelashes, and vellus hair in the treated eye; these changes include increased length, thickness, pigmentation, the number of lashes or hairs, and misdirected growth of eyelashes. Eyelash changes are usually reversible upon discontinuation of treatment.
Patients should be informed of the possibility of a disparity between eyes in length, thickness, pigmentation, number of eyelashes or vellus hairs, and/or direction of eyelash growth.
Do not use the product if the patient is allergic (hypersensitive) to latanoprost, benzalkonium chloride or any of the other ingredients of the product.
Take special care with the product: There is no experience of the product in inflammatory and neovascular glaucoma, inflammatory ocular conditions, or congenital glaucoma. Therefore, it is recommended that the product should be used with caution in these conditions until more experience is obtained.
In patients with known predisposing risk factors for iritis/uveitis, the product can be used with caution.
This medication should be used with caution in aphakic patients, in pseudophakic patients with torn posterior lens capsule or anterior chamber lenses, or in patients with known risk factors for cystoid macular oedema.
This medication should be used with caution in patients with renal or hepatic impairment.
Pediatric Population: Efficacy and safety data in the age group <1 year are very limited. No data are available for preterm infants (less than 36 weeks gestational age).
Precautions during administration: Patients should be instructed to avoid allowing the tip of the dispensing container to contact the eye. Patients developed an intercurrent ocular condition (e.g., trauma, or infection) or had ocular surgery should take special care with this drug product.
If more than one topical ophthalmic drug is being used, the drugs should be administered at least five minutes apart
Latanoprost should be used with caution in patients with a history of herpetic keratitis, and should be avoided in cases of active herpes simplex keratitis and in patients with a history of recurrent herpetic keratitis specifically associated with prostaglandin analogues.
Latanoprost cannot be used when woman is pregnant or breast-feeding.
It is not known whether this drug or its metabolites are excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when this drug product is administered to a nursing woman.
Very common effects (likely to affect more than 1 in 10 people): A gradual change in the eye colour by increasing the amount of brown pigment in the coloured part of the eye known as the iris. If the patient has mixed-colour eyes (blue-brown, grey-brown, yellow-brown or green-brown) the patient is more likely to see this change than if the patient has eyes of one colour (blue, grey, green or brown eyes). Any changes in the eye colour may take years to develop although it is normally seen within 8 months of treatment. The colour change may be permanent and may be more noticeable if the patient use Avetaprost in only one eye. There appears to be no problems associated with the change in eye colour. The eye colour change does not continue after Avetaprost treatment is stopped.
Redness of the eye.
Eye irritation (a feeling of burning, grittiness, itching, stinging or the sensation of a foreign body in the eye).
A gradual change to eyelashes of the treated eye and the fine hairs around the treated eye, seen mostly in people of Japanese origin. These changes involve an increase of the colour (darkening), length, thickness and number of the eye lashes.
Common effects (likely to affect less than 1 in 10 people): Irritation or disruption to the surface of the eye, eyelid inflammation (blepharitis) and eye pain.
Uncommon effects (likely to affect less than 1 in every 100 people): Eyelid swelling, dryness of the eye, inflammation or irritation of the surface of the eye (keratitis), blurred vision and conjunctivitis.
Skin rash
Rare effects (likely to affect less than 1 in every 1000 people): Inflammation of the iris, the coloured part of the eye (iritis/uveitis); swelling of the retina (macular oedema), symptoms of swelling or scratching/damage to the surface of the eye, swelling around the eye (periorbital oedema) misdirected eyelashes or an extra row of eyelashes.
Skin reactions on the eyelids, darkening of the skin of the eyelids.
Asthma, worsening of asthma and shortness of breath (dyspnoea).
Very rare effects (likely to affect less than 1 in 10,000 people): Worsening of angina in patients who also have heart disease. Chest pain.
Patients have also reported the following side-effects: fluid filled area within the coloured-part of the eye (iris cyst), headache, dizziness, palpitations, muscle pain and joint pain.
Side effects seen more often in children compared to adults are: runny itchy nose and fever.
If any of the side effects become serious, or if patient notices any side effects not listed in this leaflet, contact a doctor or pharmacist.
If more than one topical ophthalmic drug is being used, the drugs should be administered at least five minutes apart.
The effect of latanoprost is additive in combination with beta-adrenergic antagonists (timolol), adrenergic agonists (dipivalyl epinephrine), oral carbonic anhydrase inhibitors (acetazolamide) and at least partly additive with cholinergic agonists (pilocarpine).
The use of two or more prostaglandins, prostaglandin analogues or prostaglandin derivatives is not recommended.
Store in a refrigerator (2°C - 8°C). Protect from light.
After first opening the bottle: do not store above 25°C and use within four weeks.
S01EE01 - latanoprost ; Belongs to the class of prostaglandin analogues. Used in the treatment of glaucoma.
Avetaprost eye drops 0.005% w/v
3 mL x 1's
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