Dipivefrin

Table of contents

  • Brand Names
  • Drug Combinations
  • Chemistry
  • Pharmacologic Category
  • Mechanism of Action
  • Therapeutic Use
  • Unlabeled Use
  • Pregnancy and Lactation Implications
  • Contraindications
  • Warnings and Precautions
  • Adverse Reactions
  • Genes that may be involved
  • Drug Interactions
  • Dosage
  • Pharmacokinetics and Pharmacodynamics
  • Special Considerations

Brand Names

Europe

Austria: Oftanex; Belgium: Propine; Germany: D Epifrin; Greece: Diopine, Glaucodose; Italy: Propine; Netherlands: Diopine; Poland: Oftalar, Pivepol; UK: Propine.

North America

Canada: Dipivefrin, Propine; USA: Akpro, Dipivefrin, Propine.

Latin America

Brazil: Propine.

Asia

Japan: Pivalephrine, Progate.

Drug combinations

Dipivefrin and Guanethidine

Dipivefrin and Pilocarpine

Chemistry

Dipivefrin Hydrochloride: C~19~H~29~NO~5~ HCl. Mw: 387.90. (1) Propanoic acid, 2,2-dimethyl-, 4-[1-hydroxy-2-(methylamino)ethyl]-1,2-phenylene ester, hydrochloride, (±)-; (2)(±)-3,4-Dihydroxy-α-[(methylamino)methyl]benzyl alcohol 3,4-dipivalate hydrochloride. CAS-64019-93-8.

Pharmacologic Category

EENT Preparations; Mydriatics; α/β Agonist. Antiglaucoma Ophthalmic Agent. Ophthalmic Vasoconstrictor Agent. (ATC-Code: S01EA02).

Mechanism of action

Synthetic sympathomimetic amine prodrug of epinephrine, which is the active agent that stimulates α- and/or β-adrenergic receptors increasing aqueous humor outflow. Dipivefrin is a mydriatic.

Therapeutic use

Reduces elevated intraocular pressure (IOP) in chronic open-angle glaucoma.

Pregnancy and lactiation implications

There are no adequate, controlled studies to date using dipivefrin in pregnant women, and the drug should be used during pregnancy only when clearly needed. Should be used with caution in nursing women.

Unlabeled use

Dipivefrin has been used to reduce IOP in the treatment of other ocular conditions, including ocular hypertension and pseudoexfoliative, low-tension, and secondary (e.g. post-angle closure, pigmentary, traumatic, herpes zoster) glaucomas.

Contraindications

Hypersensitivity to dipivefrin, any component of the formulation, or epinephrine. Angle-closure glaucoma, or patients predisposed to angle-closure.

Warnings and precautions

Use with caution in vascular hypertension or cardiac disorders (including arrhythmias and cardiovascular disease). Product contains benzalkonium chloride. May cause transient burning or stinging. Blepharoconjunctivitis, requiring discontinuance of dipivefrin, reported. Karyomegaly of conjunctival epithelial cells, chemosis of the conjunctiva, dry eczematoid dermatitis of the eyelids, pruritus, and blepharitis also reported. Allergic reactions may be caused by excipients in the preparation. Cross-sensitivity reported in patients who have previously exhibited a sensitivity reaction to epinephrine. Reversible macular edema reported in aphakic patients with glaucoma treated with epinephrine (use caution). Systemic sympathomimetic effects occur rarely with topical administration of dipivefrin. Common adverse effects are ocular congestion or hyperemia, burning, or stinging.

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