Oxetacaine
Oxetacaine Uses, Dosage, Side Effects, Food Interaction and all others data.
Oxetacaine, also called oxethazaince, is a potent surface analgesic with the molecular formula N, N-bis-(N-methyl-N-phenyl-t-butyl-acetamide)-beta-hydroxyethylamine that conserves its unionized form at low pH levels. Its actions have shown to relieve dysphagia, relieve pain due to reflux, chronic gastritis, and duodenal ulcer. Oxetacaine is approved by Health Canada since 1995 for its use as an antacid combination in over-the-counter preparations. It is also in the list of approved derivatives of herbal products by the EMA.
Oxetacaine improves common gastrointestinal symptoms. Oxetacaine is part of the anesthetic antacids which increase the gastric pH while providing relief from pain for a longer period of duration at a lower dosage. This property has been reported to relieve the symptoms of hyperacidity. Oxetacaine is reported to produce a reversible loss of sensation and to provide a prompt and prolonged relief of pain. In vitro, oxetacaine was showed to produce an antispasmodic action on the smooth muscle and block the action of serotonin.
The local efficacy of oxetacaine has been proven to be 2000 times more potent than lignocaine and 500 times more potent than cocaine. Its anesthetic action produces the loss of sensation which can be explained by its inhibitory activity against the nerve impulses and de decrease in permeability of the cell membrane.
| Trade Name | Oxetacaine |
| Generic | Oxetacaine |
| Oxetacaine Other Names | Oxetacaine |
| Type | |
| Formula | C28H41N3O3 |
| Weight | Average: 467.654 Monoisotopic: 467.314792192 |
| Protein binding | Due to the low half-life, it is thought that oxetacaine, when absorbed, presents a very low protein plasma binding. |
| Groups | Approved, Investigational |
| Therapeutic Class | |
| Manufacturer | |
| Available Country | |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Oxetacaine is an antacid used to treat gastritis, peptic ulcer disease, heartburn, esophagitis, hiatus hernia, and anorexia.
Oxetacaine is available as an over-the-counter antacid and it is used to alleviate pain associated with gastritis, peptic ulcer disease, heartburn, esophagitis, hiatus hernia, and anorexia.
Oxetacaine is also used to associated treatment for these conditions: Acid Reflux, Anal Fissures, Hemorrhoids, Proctitis, Pruritus Ani, Anal eczema
How Oxetacaine works
Oxetacaine inhibits gastric acid secretion by suppressing gastrin secretion.
Moreover, oxetacaine exerts a local anesthetic effect on the gastric mucosa. This potent local anesthetic effect of oxetacaine may be explained by its unique chemical characteristics in which, as a weak base, it is relatively non-ionized in acidic solutions whereas its hydrochloride salt is soluble in organic solvents and it can penetrate cell membranes. Oxetacaine diminishes the conduction of sensory nerve impulses near the application site which in order reduces the permeability of the cell membrane to sodium ions. This activity is performed by the incorporation of the unionized form into the cell membrane.
Toxicity
When orally administered, oxetacaine presents a good tolerance. However, following intravenous injection, oxetacaine toxicity is high and it is presented as a depression in myocardial contractility and impaired conduction.
Food Interaction
No interactions found.Volume of Distribution
This pharmacokinetic property has not been studied.
Elimination Route
A peak plasma concentration of oxetacaine of approximately 20 ng/ml is attained about one hour after oral administration. LEss than 1/3 of the administered dose is absorbed as it undergoes extensive metabolism.
Half Life
Oxetacaine presents a very short half-life of approximately one hour.
Clearance
This pharmacokinetic property has not been studied.
Elimination Route
Less than 0.1% of the amdinistered dose is recovered in urine within 24 hours in the form of unchanged oxetacaine or its metabolites.
Innovators Monograph
You find simplified version here Oxetacaine
