Pivalephrine

Pivalephrine Uses, Dosage, Side Effects, Food Interaction and all others data.

Pivalephrine is a prodrug of adrenaline, which is used to treat glaucoma. It is available as ophthalmic solution (eye drops).

Pivalephrine 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. Pivalephrine 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.

Trade Name Pivalephrine
Availability Discontinued
Generic Dipivefrin
Dipivefrin Other Names Dipivalyl epinephrine, Dipivefrin, Dipivefrina, Dipivéfrine, Dipivefrine, Dipivefrinum
Related Drugs epinephrine ophthalmic, latanoprost ophthalmic, timolol ophthalmic, brimonidine ophthalmic, pilocarpine ophthalmic, Xalatan, Lumigan
Type
Formula C19H29NO5
Weight Average: 351.4373
Monoisotopic: 351.204573043
Groups Approved
Therapeutic Class
Manufacturer
Available Country
Last Updated: September 19, 2023 at 7:00 am
Pivalephrine
Pivalephrine

Uses

Pivalephrine is a prodrug of epinephrine used in ophthalmic solutions to reduce intraocular pressure in chronic open-angle glaucoma.

Pivalephrine is a prodrug which is used as initial therapy for the control of intraocular pressure in chronic open-angle glaucoma.

Pivalephrine is also used to associated treatment for these conditions: Increased Intra Ocular Pressure (IOP), Intraocular Pressure (IOP), Normal Tension Glaucoma

How Pivalephrine works

Pivalephrine is a prodrug with little or no pharmacologically activity until it is hydrolyzed into epinephrine inside the human eye. The liberated epinephrine, an adrenergic agonist, appears to exert its action by stimulating α -and/or β2-adrenergic receptors, leading to a decrease in aqueous production and an enhancement of outflow facility. The 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.

Toxicity

Oral LD50 in rat is 183 mg/kg.

Food Interaction

No interactions found.

Pivalephrine Disease Interaction

Major: aphakia, narrow angles

Elimination Route

Well absorbed following occular administration.

Innovators Monograph

You find simplified version here Pivalephrine

*** Taking medicines without doctor's advice can cause long-term problems.
Share