INFORMATION FOR HEALTH PROFESSIONALS
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The sponsor (pharmaceutical company) of this product has
advised Medsafe that this product has either been discontinued or is no longer
marketed in New Zealand.
Therefore this Data Sheet may not be up to date.
Medsafe has elected to leave it on this web site because supplies of this
product may still be available, and health professionals should continue to
have access to this product information in the interim.
You may be able to find a more current Data Sheet containing the same medicine
by returning to the main Data Sheet page and searching by ingredient name.
Dipivefrine hydrochloride 1 mg/mL (0.1%), benzalkonium chloride 0.005%, disodium edetate, sodium chloride, hydrochloric acid to adjust pH, and purified water.
PROPINE® contains the active substance dipivefrine hydrochloride, as a prodrug which is biotransformed to liberate adrenaline, an adrenergic agonist, into the anterior chamber of the eye. This appears to exert its action by decreasing aqueous production and by enhancing outflow facility.
PROPINE® is effective alone in reducing intraocular pressure but is also most useful in conjunction with other β-blocker drops for difficult to control patients.
The onset of action with one drop of PROPINE® occurs about 30 minutes after treatment with maximum effect at approximately one hour.
The use of dipivefrine hydrochloride as a prodrug enhances absorption into the anterior chamber. Consequently less active compound is required topically for therapeutic effect.
Absorption, distribution, metabolism, and elimination of dipivefrine hydrochloride and adrenaline were compared after both parenteral and topical treatment. The rate of elimination of radioactive material following intravenous administration of 14C-dipivefrine labelled in the adrenaline moiety is similar to that following 14C- adrenaline treatment. Distribution of radioactive material in urine is also similar, with very little of the radioactivity appearing as dipivefrine in dipivefrine-treated animals.
Data indicate that dipivefrine is hydrolysed to adrenaline and mainly eliminated as adrenaline and its metabolites. After ocular administration of dipivefrine, ten times as much dipivefrine as adrenaline is absorbed into the eye (molar basis). This absorbed dipivefrine is rapidly hydrolysed in the cornea to adrenaline and the adrenaline portion of the molecule is slowly eliminated from the eye with some sequestering in iris and ciliary body tissues. The pivalate moiety is rapidly eliminated and does not appear to be sequestered in any ocular tissues.
Chronic open angle glaucoma and ocular hypertensive patients. In many cases, reduction of intraocular pressure can be obtained when miotics have failed.
Initial Glaucoma Therapy: The usual dosage of PROPINE® is one drop in the eye(s) every 12 hours.
Replacement with PROPINE®: When patients are being transferred to PROPINE® from antiglaucoma agents other than adrenaline, on the first day continue the previous medication and add one drop of PROPINE® in the eye(s) every 12 hours. On the following day, discontinue the previously used antiglaucoma agent and continue with PROPINE®.
When transferring patients from conventional adrenaline therapy to PROPINE®, simply discontinue the adrenaline medication and institute PROPINE® therapy.
Addition of PROPINE®: When patients on other antiglaucoma agents require additional therapy, add one drop of PROPINE® in the eye(s) every 12 hours.
Concomitant Therapy: For difficult to control patients, other antiglaucoma agents may be added to PROPINE® therapy.
PROPINE® should not be used in patients with narrow angle glaucoma since any dilation of the pupil may predispose the patient to an attack of angle-closure glaucoma.
This product is contraindicated in patients who are hypersensitive to dipivefrine hydrochloride, benzalkonium chloride or any of the other components.
Reproduction studies have been performed in rats and rabbits at daily oral doses up to 10 mg/kg body weight (5 mg/kg in teratogenicity studies) and have revealed no evidence of impaired fertility or harm to the foetus due to dipivefrine hydrochloride. There are, however, no adequate and well-controlled studies in pregnant women. Because animal reproduction studies are not always predictive of human response, this drug should be used during pregnancy only if clearly needed.
It is not known whether this drug is excreted in human milk, therefore caution should be exercised when PROPINE® is administered to nursing women.
Safety and efficacy in children has not been studied.
Macular oedema has been shown to occur in up to 30% of aphakic patients treated with adrenaline. Discontinuation of adrenaline generally results in reversal of the maculopathy.
As PROPINE® contains benzalkonium chloride, it should not be used in patients who continue to wear hydrophyllic (soft) contact lenses.
The most common side effects reported during clinical trials were hyperaemia, burning and stinging (irritation) upon instillation. Other side effects occasionally reported include conjunctivitis and follicular conjunctivitis, hypersensitivity, mydriasis, blurred vision, browache and photophobia.
On rare occasions, systemic adverse effects such as occipital headache, arrhythmia, palpitation, acceleration of the heart beat, hypertension, paleness, trembling and perspiration have been observed following adrenaline therapy so the possibility of their occurrence following PROPINE® therapy must be considered.
Symptoms of overdosage may include irritation, erythema, burning or stinging or swelling of the eyelids. The affected eye(s) should be flushed with water or sterile saline.
Shelf life 16 months
Storage Store below 25°C. Protect from light and excessive heat.
Discard unused contents 4 weeks after opening. Contents are sterile if seal is intact.
Prescription Medicine
7.5 mL eye drops, dropper bottle. 1 mg/mL (0.1%).
PROPINE® contains dipivefrine hydrochloride as a prodrug which is biotransformed to adrenaline. Chemical name:
(±)-3,4-Dihydroxy-α(methylamino)methyl]benzylalcohol 3,4-dipivalate hydrochloride
Allergan New Zealand Limited
Cnr Manu Tapu Drive & Joseph Hammond Place,
Auckland International Airport, Mangere,
Auckland, New Zealand
Toll free telephone: 0800 659 912
1 December 2004