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PROPINE

 * Generic Name: dipivefrin
 * Brand Name: Propine
 * Drug Class: Antiglaucoma, Miotics

Medical Editor: John P. Cunha, DO, FACOEP Last updated on RxList: 7/26/2022

home drugs a-z list propine (dipivefrin) drug


DRUG SUMMARY

WHAT IS PROPINE?

Propine (dipivefrin HCI ophthalmic solution) works by regulating the flow of
fluid within the eye to maintain a normal pressure and is used to treat
open-angle glaucoma or ocular hypertension (high pressure inside the eye).
Propine is available in generic form.

WHAT ARE SIDE EFFECTS OF PROPINE?

Common side effects of Propine include:


 * burning/stinging/irritation/itching of the eyes
 * redness of the eye or eyelid
 * eye pain
 * blurred vision
 * headache, and
 * increased sensitivity to light

WHAT ARE THE POSSIBLE SIDE EFFECTS OF PROPINE?

Propine may cause serious side effects including:

 * hives,
 * difficulty breathing,
 * swelling of your face, lips, tongue, or throat,
 * rash, and
 * severe dizziness

Get medical help right away, if you have any of the symptoms listed above.

Seek medical care or call 911 at once if you have the following serious side
effects:

 * Serious eye symptoms such as sudden vision loss, blurred vision, tunnel
   vision, eye pain or swelling, or seeing halos around lights;
 * Serious heart symptoms such as fast, irregular, or pounding heartbeats;
   fluttering in your chest; shortness of breath; and sudden dizziness,
   lightheartedness, or passing out;
 * Severe headache, confusion, slurred speech, arm or leg weakness, trouble
   walking, loss of coordination, feeling unsteady, very stiff muscles, high
   fever, profuse sweating, or tremors.

This document does not contain all possible side effects and others may occur.
Check with your physician for additional information about side effects.

DOSAGE FOR PROPINE

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

WHAT DRUGS, SUBSTANCES, OR SUPPLEMENTS INTERACT WITH PROPINE?

Other drugs may interact with Propine ophthalmic. Avoid using any eye
medications your doctor has not prescribed. Tell your doctor all medications and
supplements you use.

PROPINE DURING PREGNANCY OR BREASTFEEDING

Propine should be used only when prescribed during pregnancy. It is unknown if
this drug passes into breast milk. Consult your doctor before breastfeeding.

ADDITIONAL INFORMATION

Our Propine (dipivefrin HCI ophthalmic solution) Side Effects Drug Center
provides a comprehensive view of available drug information on the potential
side effects when taking this medication.


FDA DRUG INFORMATION

 * Drug Description
 * Indications
 * Dosage
 * Side Effects & Drug Interactions
 * Warnings & Precautions
 * Overdose & Contraindications
 * Clinical Pharmacology
 * Medication Guide


DESCRIPTION FOR PROPINE

PROPINE® contains dipivefrin hydrochloride in a sterile, isotonic solution.
Dipivefrin HCI is a white, crystalline powder, freely soluble in water.

Empirical Formula:

C19-H29O5N•HCI







Chemical Name: (±) -3,4-Dihydroxy-α-[(methyl-amino) methyl] benzyl-alcohol
3,4-dipivalate hydrochloride.

Contains: Active: dipivefrin HCI 0.1%

Preservative: benzalkonium chloride; Inactives: edetate disodium; sodium
chloride; hydrochloric acid to adjust pH; and purified water.




USES FOR PROPINE

PROPINE® (dipivefrin HCI ophthalmic solution, USP) is indicated as initial
therapy for the control of intraocular pressure in chronic open-angle glaucoma.
Patients responding inadequately to other antiglaucoma therapy may respond to
addition of PROPINE® (dipivefrin) .

In controlled and open-label studies of glaucoma, PROPINE® (dipivefrin)
ophthalmic solution demonstrated a statistically significant intraocular
pressure-lowering effect. Patients using PROPINE® (dipivefrin) twice daily in
studies with mean durations of 76-146 days experienced mean pressure reductions
ranging from 20-24%.

Therapeutic response to PROPINE® (dipivefrin) ophthalmic solution twice daily is
somewhat less than 2% epinephrine twice daily. Controlled studies showed
statistically significant differences in lowering of intraocular pressure
between PROPINE® (dipivefrin) and 2% epinephrine. In controlled studies in
patients with a history of epinephrine intolerance, only 3% of patients treated
with PROPINE® (dipivefrin) ophthalmic solution exhibited intolerance, while 55%
of those treated with epinephrine again developed intolerance.

Therapeutic response to PROPINE® (dipivefrin) twice daily therapy is comparable
to 2% pilocarpine 4 times daily. In controlled clinical studies comparing
PROPINE® (dipivefrin) ophthalmic solution and 2% pilocarpine, there were no
statistically significant differences in the maintenance of IOP levels for the
two medications. PROPINE® (dipivefrin) does not produce miosis or accommodative
spasm which cholinergic agents are known to produce. Night blindness often
associated with miotic agents is not present with PROPINE® (dipivefrin) therapy.
Patients with cataracts avoid the inability to see around lenticular opacities
caused by constricted pupil.


DOSAGE FOR PROPINE

INITIAL GLAUCOMA THERAPY

The usual dosage of PROPINE® (dipivefrin) is one drop in the eye(s) every 12
hours.

REPLACEMENT WITH PROPINE® (DIPIVEFRIN) OPHTHALMIC SOLUTION

When patients are being transferred to PROPINE® (dipivefrin) from antiglaucoma
agents other than epinephrine, on the first day continue the previous medication
and add one drop of PROPINE® (dipivefrin) ophthalmic solution in each eye every
12 hours. On the following day, discontinue the previously used antiglaucoma
agent and continue with PROPINE® (dipivefrin) .

In transferring patients from conventional epinephrine therapy to PROPINE®
(dipivefrin) ophthalmic solution, simply discontinue the epinephrine medication
and institute the PROPINE® (dipivefrin) regimen.

ADDITION OF PROPINE® (DIPIVEFRIN) OPHTHALMIC SOLUTION

When patients on other antiglaucoma agents require additional therapy, add one
drop of PROPINE® (dipivefrin) every 12 hours.

CONCOMITANT THERAPY

For difficult to control patients, the addition of PROPINE® (dipivefrin)
ophthalmic solution to other agents such as pilocarpine, carbachol,
echothiophate iodide or acetazolamide has been shown to be effective.

Note: Not for injection.


HOW SUPPLIED

PROPINE® (dipivefrin HCI ophthalmic solution, USP) 0.1%, is supplied sterile in
plastic dropper bottles as follows: 5 mL - 0023-9208-05; 10 mL - 0023-9208-10;
15 mL - 0023-9208-15.

Note: Store in tight, light-resistant containers.

Allergan, Inc. Irvine, CA 92612, U.S.A. Revised December 2000. FDA Rev date:
4/12/2002




SIDE EFFECTS FOR PROPINE

CARDIOVASCULAR EFFECTS

Tachycardia, arrhythmias and hypertension have been reported with ocular
administration of epinephrine.

LOCAL EFFECTS

The most frequent side effects reported with PROPINE® (dipivefrin) alone were
injection in 6.5% of patients and burning and stinging in 6%. Follicular
conjunctivitis, eye pain, mydriasis, blurry vision, eye pruritus, headache and
allergic reaction to PROPINE® (dipivefrin) ophthalmic solution have been
reported. Epinephrine therapy can lead to adrenochrome deposits in the
conjunctiva and cornea.


DRUG INTERACTIONS FOR PROPINE

No information provided.


WARNINGS FOR PROPINE

No information provided.


PRECAUTIONS FOR PROPINE

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.

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 HCI. 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.

NURSING MOTHERS

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 PROPINE®
(dipivefrin) ophthalmic solution is administered to a nursing woman.

PEDIATRIC USE

Safety and effectiveness in pediatric patients have not been established.

ANIMAL STUDIES

Rabbit studies indicated a dose-related incidence of meibomian gland retention
cysts following topical administration of both dipivefrin hydrochloride and
epinephrine.


OVERDOSE INFORMATION FOR PROPINE

No information provided.


CONTRAINDICATIONS FOR PROPINE

PROPINE® (dipivefrin) 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.


CLINICAL PHARMACOLOGY FOR PROPINE

PROPINE® (dipivefrin HCI ophthalmic solution, USP) is a member of a class of
drugs known as prodrugs. Prodrugs are usually not active in themselves and
require biotransformation to the parent compound before therapeutic activity is
seen. These modifications are undertaken to enhance absorption, decrease side
effects and enhance stability and comfort, thus making the parent compound a
more useful drug. 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.

PROPINE® (dipivefrin) ophthalmic solution 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.

PROPINE® (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 PROPINE® (dipivefrin) 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.

The onset of action with one drop of PROPINE® (dipivefrin) occurs about 30
minutes after treatment, with maximum effect seen at about one hour.

Using a prodrug means that less drug is needed for therapeutic effect since
absorption is enhanced with the prodrug. PROPINE® ophthalmic solution at 0.1%
dipivefrin was judged less irritating than a 1% solution of epinephrine
hydrochloride or bitartrate. In addition, only 8 of 455 patients (1.8%) treated
with PROPINE® (dipivefrin) reported discomfort due to photophobia, glare or
light sensitivity.


PATIENT INFORMATION FOR PROPINE

No information provided. Please refer to the PRECAUTIONS section.


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