Dipivefrine
Dipivefrine
Dipivefrine, also known as dipivefrin, is a prodrug of epinephrine (adrenaline) used in the treatment of glaucoma. It is an adrenergic agonist that reduces intraocular pressure by decreasing the production of aqueous humor and increasing its outflow.
Mechanism of Action
Dipivefrine is converted into epinephrine in the eye. Epinephrine acts on both alpha and beta adrenergic receptors. The activation of these receptors leads to a reduction in aqueous humor production by the ciliary body and an increase in the outflow of aqueous humor through the trabecular meshwork and the uveoscleral pathway.
Clinical Use
Dipivefrine is primarily used in the management of open-angle glaucoma and ocular hypertension. It is administered as an ophthalmic solution and is typically used when other medications, such as beta blockers or prostaglandin analogs, are not sufficient or suitable.
Side Effects
Common side effects of dipivefrine include:
- Eye irritation
- Conjunctival hyperemia
- Mydriasis (pupil dilation)
Less common but more serious side effects can include:
Pharmacokinetics
Dipivefrine is a prodrug that is rapidly converted to epinephrine by esterase enzymes in the eye. This conversion allows for better penetration into the anterior chamber of the eye compared to epinephrine itself, which is why dipivefrine is preferred for ocular use.
History
Dipivefrine was developed to improve the ocular bioavailability of epinephrine and to reduce its systemic side effects. It was first approved for medical use in the 1970s and has since been a valuable option in the treatment of glaucoma.
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