Action And Clinical Pharmacology: Dipivefrin is converted to epinephrine inside the human eye by enzyme hydrolysis. The liberated epinephrine, an adrenergic agonist, appears to exert its action by decreasing aqueous production and by enhancing outflow facility. The dipivefrin hydrochloride prodrug delivery system is a more efficient way of delivering the therapeutic effects of epinephrine, with fewer side effects than are associated with conventional epinephrine therapy.
Indications And Clinical Uses: As initial therapy for the control of intraocular pressure in chronic open-angle glaucoma. Patients responding inadequately to other antiglaucoma therapy may respond to the addition of dipivefrin.
Contra-Indications: Should not be used in patients with narrow angles 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 any of its components.
Manufacturers’ Warnings In Clinical States: Not for injection. For topical ophthalmic use only.
Because the diagnosis of narrow-angle glaucoma is frequently missed during normotensive intervals (between attacks), it is very important that careful slit lamp and gonioscopic study be done before initiating therapy with this drug. Should an elevation of intraocular pressure follow the instillation of dipivefrin, appropriate hypotensive therapy is recommended.
Precautions: General: Aphakic Patients: Macular edema has been shown to occur in up to 30% of aphakic patients treated with epinephrine. Discontinuation of epinephrine generally results in reversal of the maculopathy. Macular edema has been reported rarely with dipivefrin; reversal occurred upon discontinuation of therapy.
Pregnancy: 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 fetus due to dipivefrin. 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.
Lactation: It is not known whether this drug is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when dipivefrin is administered to a nursing woman.
Children: Clinical studies to determine safety and efficacy in children have not been done.
Adverse Reactions: Cardiovascular: Tachycardia, arrhythmias and hypertension have been reported with ocular administration of epinephrine.
Local Effects: The most frequent side effects reported with dipivefrin alone were injection in 6.5% of patients and burning and stinging in 6%. Follicular conjunctivitis, conjunctivitis, blurred vision, browache, photophobia, mydriasis, hyperemia and hypersensitivity or orbital pain have been reported infrequently.
On rare occasions, systemic adverse effects such as occipital headache, palpitation, paleness, acceleration of the heartbeat, trembling and perspiration have been observed following epinephrine therapy; the slight possibility of their occurrence following therapy with dipivefrin 0.1% should be borne in mind.
Macular edema in aphakic patients has been known to occur with epinephrine therapy. Discontinuation of epinephrine generally results in prompt reversal. Rarely have cases of macular edema in aphakic patients been reported with dipivefrin. Reversal occurred upon discontinuation of therapy.
Epinephrine therapy can lead to adrenochrome deposits in the conjunctiva and cornea. However, these have been reported rarely following the use of dipivefrin.
Symptoms And Treatment Of Overdose: Symptoms and Treatment: Overdosage in the use of topical preparations is a remote possibility. Discontinue medication when heavy or protracted use is suspected and initiate symptomatic treatment if deemed necessary.
Dosage And Administration: Initial Glaucoma Therapy: The usual dosage is 1 drop in the eye(s) every 12 hours.
Replacement Therapy: When patients are being transferred to dipivefrin from antiglaucoma agents other than epinephrine, on the first day continue the previous medication and add 1 drop of the dipivefrin ophthalmic solution to each eye(s) every 12 hours. On the following day, discontinue the previously used antiglaucoma agent and continue with dipivefrin.
In transferring patients from conventional epinephrine therapy to dipivefrin, simply discontinue the epinephrine medication and institute the dipivefrin regimen.
Additional Therapy: When patients on other antiglaucoma agents require additional therapy, add 1 drop of dipivefrin every 12 hours.
Concomitant Therapy: For difficult to control patients, the addition of dipivefrin to other agents such as pilocarpine, carbachol, echothiophate iodide or acetazolamide has been shown to be effective.
Availability And Storage: Each mL of sterile, isotonic, ophthalmic solution contains: dipivefrin hydrochloride 0.1% and benzalkonium chloride 0.005% as preservative. Nonmedicinal ingredients: edetate disodium, purified water, sodium chloride, and hydrochloric acid and/or sodium hydroxide (to adjust pH). Opaque plastic Drop-Tainer dispensers of 5, 10 and 15 mL. Store at controlled room temperature (15 to 25°C). Protect from light and excessive heat.
DPE Alcon Dipivefrin HCl Glaucoma Therapy
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