Propine

1. Name Of The Medicinal Product

PROPINE®

2. Qualitative And Quantitative Composition

Dipivefrin hydrochloride 0.1% w/v.

3. Pharmaceutical Form

Eye drops.

4. Clinical Particulars

4.1 Therapeutic Indications

To control intraocular pressure in patients with chronic open angle glaucoma or ocular hypertensive patients with anterior chamber open angles.

4.2 Posology And Method Of Administration

The usual dosage is one drop in the affected eye(s) every 12 hours.

4.3 Contraindications

a) Patients suffering from closed angle glaucoma

b) Hypersensitivity to any component of the formulation

4.4 Special Warnings And Precautions For Use

Dipivefrin should be used with caution in patients with narrow angles since dilation of the pupil may trigger an attack of angle closure glaucoma.

Macular oedema is a rare occurrence with adrenaline use in aphakic patients. Prompt reversal generally follows discontinuance of the drug. Macular oedema with dipivefrin does present as a possibility in the aphakic patient.

PROPINE® should be used in caution with patients who have hypertension, heart disease or hyperthyroidism.

This product contains benzalkonium chloride and should not be used by patients continuing to wear soft (hydrophilic) contact lenses.

4.5 Interaction With Other Medicinal Products And Other Forms Of Interaction

Systemic absorption is a possibility for PROPINE® and consequently there is potential for the following interactions to occur:

Mono-amine oxidase inhibitors: There is an elevated risk of adrenergic reactions with concomitant use of MAOIs. These interactions may occur up to 14 days after ceasing the concomitant MAOI therapy.

Tricyclic antidepressants: The pressor response to adrenergic agents and the risk of cardiac arrhythmia may be exacerbated in those patients receiving concomitant tricyclic antidepressants. Upon their cessation the pressor response may persist for up to several days.

Halogenated anaesthetics: PROPINE® should not be administered during general anaesthesia with those anaesthetic agents which sensitise the myocardium to sympathomimetics since under these circumstances there is an elevated risk of ventricular fibrillation.

4.6 Pregnancy And Lactation

The safety of intensive or protracted use of dipivefrin during pregnancy has not been substantiated. Caution should be exercised when PROPINE® is administered to a nursing mother.

4.7 Effects On Ability To Drive And Use Machines

Mydriasis may occur in some patients. Do not drive or operate machinery if affected.

4.8 Undesirable Effects

a) Cardiovascular: tachycardia, arrhythmias and hypertension have been reported with ocular administration of adrenaline, and may occur rarely with dipivefrin therapy.

b) Ocular: the most frequently reported side effects are conjunctival hyperaemia, and burning and stinging on instillation.

Rebound vasodilation, mydriasis and allergic reactions, including blepharoconjunctivitis have been reported occasionally.

Adrenochrome deposits in the conjunctiva and cornea have been associated rarely with the use of dipivefrin.

Follicular conjunctivitis has been reported during long term therapy with dipivefrin. The condition is reversible upon discontinuance of the drug.

c) Body as a Whole: headache may occur rarely with dipivefrin (and is occasionally associated with hypertension and tachycardia).

4.9 Overdose

There are no data available on overdosage with PROPINE®, which is unlikely to occur via the ocular route.

5. Pharmacological Properties

5.1 Pharmacodynamic Properties

Dipivefrin is a prodrug that is converted inside the eye to adrenaline. Conversion takes place by enzyme hydrolysis.

Adrenaline, an adrenergic agonist, appears to exert its action by decreasing aqueous production and enhancing aqueous outflow facility.

5.2 Pharmacokinetic Properties

Onset of action after instillation is about 30 minutes. Time to peak effect is about 1 hour.

5.3 Preclinical Safety Data

-

6. Pharmaceutical Particulars

6.1 List Of Excipients

Benzalkonium chloride

Disodium edetate

Sodium chloride

Hydrochloric acid (to adjust pH)

Purified water

6.2 Incompatibilities

None known

6.3 Shelf Life

The shelf life of the unopened bottle is 18 months. Once opened, the shelf life is 28 days.

6.4 Special Precautions For Storage

Store at 25°C or less.

6.5 Nature And Contents Of Container

White, low density polyethylene 5 ml and 10 ml fill dropper bottle and tip in single or triple packs; white, medium impact polystyrene (MIPS) screw cap or compliance screw cap (C-cap®).

6.6 Special Precautions For Disposal And Other Handling

No special instructions required.

7. Marketing Authorisation Holder

Allergan Ltd

Marlow International

The Parkway

Marlow

Bucks

SL7 1YL

UK

8. Marketing Authorisation Number(S)

PL 00426/0040

9. Date Of First Authorisation/Renewal Of The Authorisation

27th May 2002

10. Date Of Revision Of The Text

20^th December 2007