Pilocarpine Hydrochloride Eye Drops 2% w / v

1. Name Of The Medicinal Product

Pilocarpine Hydrochloride Eye Drops 2%

2. Qualitative And Quantitative Composition

Pilocarpine Hydrochloride 2.0% w/v

For excipients, see 6.1.

3. Pharmaceutical Form

Eye drops, Solution.

A slightly viscous, almost clear and colourless solution.

4. Clinical Particulars

4.1 Therapeutic Indications

A directly acting miotic used for the treatment of Glaucoma.

Chronic Simple Glaucoma:

Patients may be maintained on pilocarpine as long as intraocular pressure is controlled and there is no deterioration in the visual fields.

Acute (Closed-Angle) Glaucoma):

Pilocarpine may be used alone or in conjunction with other agents to decrease intraocular pressure prior to surgical treatment.

Miosis:

To counter the effects of cycloplegic and mydriatic eye drops.

4.2 Posology And Method Of Administration

Adults and the Elderly

One or two drops up to four times daily or as prescribed. The frequency of installation and concentration of drops used are determined by the severity of the glaucoma and the response to treatment.

Children

At the discretion of the physician. Safety and efficacy of use in children has not been established.

4.3 Contraindications

Conditions where pupillary constriction is undesirable, eg: acute iritis, anterior uveitis and some forms of secondary glaucoma. Hypersensitivity to any component of the preparation. Patients with soft contact lenses should not use this preparation.

4.4 Special Warnings And Precautions For Use

Although systemic reactions rarely occur in the treatment of chronic simple glaucoma with the usual doses used, in the treatment of acute closed-angle glaucoma the possibility of systemic reactions must be considered because of the higher doses given. Caution is particularly advised with patients with acute heart failure, bronchial asthma, peptic ulceration, hypertension, urinary tract obstruction and Parkinson's disease. As with all miotics rare cases of retinal detachment have been reported when used in certain susceptible individuals and those with pre-existing retinal disease, therefore, fundus examination is advised in all patients prior to the initiation of therapy.

4.5 Interaction With Other Medicinal Products And Other Forms Of Interaction

None known

4.6 Pregnancy And Lactation

There is insufficient evidence as to drug safety in pregnancy and lactation. This product should not be used during pregnancy unless it is considered essential by a physician.

4.7 Effects On Ability To Drive And Use Machines

Causes difficulty with dark adaptation, therefore, caution is necessary with night driving and when hazardous tasks are undertaken in poor illumination. May cause accommodation spasm. Patients should be advised not to drive or use machinery if vision is not clear.

4.8 Undesirable Effects

Local: Burning, itching, smarting, blurring, ciliary spasm, conjunctival vascular congestion, induced myopia, sensitisation of the lids and conjunctiva, reduced visual acuity in poor illumination, lens changes with chronic use, increased pupillary block, retinal detachments and vitreous haemorrhages.

CNS: Browache and headache (especially in younger patients who have recently started therapy).

Systemic: Systemic reactions following ocular use are rare but they may include hypertension, tachycardia, bronchial spasm, pulmonary oedema, salivation, sweating, nausea, vomiting, diarrhoea and lacrimation.

4.9 Overdose

If accidentally ingested, induce emesis or perform gastric lavage. Observe for signs of toxicity (salivation, lacrimation, sweating, nausea, vomiting and diarrhoea). If these occur, therapy with anti-cholinergic agents, such as atropine, may be necessary.

5. Pharmacological Properties

5.1 Pharmacodynamic Properties

Pharmacotherapeutic Group: Antigluacoma Preparations & Miotics

ATC Code: S01E B01

Pilocarpine is a direct acting cholinergic parasympathomimetic agent which acts through direct stimulation of muscarinic neuro receptors and smooth muscle such as the iris and secretory glands. Pilocarpine produces miosis through contraction of the iris sphincter, causing increased tension on the scleral spur and opening of the trabecular mesh-work spaces to facilitate outflow of aqueous humour. Outflow resistance is thereby reduced, lowering intraocular pressure.

5.2 Pharmacokinetic Properties

Pilocarpine is able to cross the fat-water-fat corneal barrier thus good ocular penetration is actioned after topical instillation into the eye. In man, after administration of two drops of a 2% solution, concentrations in aqueous humour of 0.2% were found after 20 minutes.

Pilocarpine is hydrolysed by cholinesterase and excreted in the urine in combination with other substances.

5.3 Preclinical Safety Data

There are no preclinical data of relevance to the prescriber which are additional to that already included in other sections of the SPC.

6. Pharmaceutical Particulars

6.1 List Of Excipients

Boric acid

Sodium Citrate Dihydrate

Benzalkonium chloride

Hypromellose

Sodium hydroxide and / or Hydrochloric acid

Purified water

6.2 Incompatibilities

None known

6.3 Shelf Life

4 years (unopened), 1 month (after first opening).

6.4 Special Precautions For Storage

Do not store above 25^oC.

Keep away from direct sunlight.

Do not refrigerate.

Keep container tightly closed.

Discard 1 month after opening.

6.5 Nature And Contents Of Container

10ml Drop-Tainer - Natural Low Density Polyethylene bottle and plug.

Polystyrene or Polypropylene cap.

6.6 Special Precautions For Disposal And Other Handling

Do not touch dropper tip to any surface as this may contaminate the contents.

If the drop of medication is not retained in the eye upon dosing for any reason, instill another drop.

ADMINISTRATIVE DATA

7. Marketing Authorisation Holder

Cusi (UK) Limited

Pentagon Park

Boundary Way

Hemel Hempstead

Herts

HP2 7UD

8. Marketing Authorisation Number(S)

PL 16020/0013

9. Date Of First Authorisation/Renewal Of The Authorisation

10^th November 2000

10. Date Of Revision Of The Text

July 2003