Action And Clinical Pharmacology: Dipivefrin is a member of a class of drugs known as prodrugs. Prodrugs are chemical modifications of valuable therapeutic agents which make the parent compound a more useful drug. These modifications are undertaken to enhance absorption, decrease side effects and enhance stability and comfort. Enhanced absorption makes the prodrug a more efficient delivery system for the parent drug because less drug will be needed to produce the desired therapeutic response.
Dipivefrin is a prodrug of epinephrine formed by the diesterification of epinephrine and pivalic acid. The addition of pivaloyl groups to the epinephrine molecule enhances its lipophilic character and as a consequence, its penetration into the anterior chamber.
Indications And Clinical Uses: As initial or adjunctive therapy for the control of elevated intraocular pressure in chronic open angle glaucoma and in ocular hypertensive patients.
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. Not recommended for use in children.
Manufacturers’ Warnings In Clinical States: Because the diagnosis of narrow-angle glaucoma is 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 tension follow the instillation of dipivefrin solution, appropriate hypotensive therapy by the treating physician is recommended.
Precautions: Avoid contamination of the dropper tip which may result from contact with the eye or skin or any other surface.
Pregnancy: Pregnancy Category B: 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 for safety and efficacy in children have not been done.
Adverse Reactions: Dipivefrin is well tolerated and possesses few side effects. The most common side effects reported during clinical trials were burning/stinging/irritation upon instillation. Other side effects occasionally reported include conjunctivitis, blurred vision, browache and photophobia.
Adverse effects of epinephrine although not usually seen with dipivefrin therapy include reactive hyperemia, hypersensitivity or orbital pain, mydriasis and follicular conjunctivitis.
On rare occasions, systematic adverse effects such as occipital headache, palpitation, paleness, acceleration of the heart beat, trembling and perspiration have been observed following epinephrine therapy; the slight possibility of their occurrence following dipivefrin therapy should be borne in mind.
Aphakic Patients: Macular edema in aphakic patients have been known to occur with epinephrine therapy. Discontinuation of epinephrine generally results in prompt reversal. Very rarely have cases of macular edema in aphakic patients been reported with dipivefrin. Reversal occurred upon discontinuation of therapy.
Adrenochrome Deposits: Although epinephrine therapy has led to adrenochrome deposits in the conjunctiva and cornea, these have been reported rarely following the use of dipivefrin.
Symptoms And Treatment Of Overdose: Symptoms and Treatment: Overdosage has not been reported to date. In the event of such an occurrence, symptomatic treatment, as for epinephrine, should be initiated.
Dosage: Adults: 1 drop in each affected eye every 12 hours. Keep out of reach of children.
Availability And Storage: Each mL contains: dipivefrin hydrochloride 1 mg in a sterile, isotonic aqueous ophthalmic solution. Also contains benzalkonium chloride 0.005% as preservative, and edetate disodium, sodium chloride, and hydrochloric acid to adjust the pH. Plastic dropper bottles of 10 and 15 mL.
Store at room temperature; keep tightly closed. Protect from light and excessive heat. Do not use if solution is discolored. Not for injection.
PROPINE® Allergan Dipivefrin HCl Glaucoma Therapy