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Oxetacaine API Manufacturers & Suppliers

General Description:

Oxetacaine, identified by CAS number 126-27-2, is a notable compound with significant therapeutic applications. 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.

Indications:

This drug is primarily indicated for: 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. Its use in specific medical scenarios underscores its importance in the therapeutic landscape.

Metabolism:

Oxetacaine undergoes metabolic processing primarily in: Oxetacaine is rapidly and extensively metabolized hepatically. After metabolism, there is a formation of primary metabolites such as beta-hydroxy-mephentermine and beta-hydroxy-phentermine. The major metabolites are found in the plasma in insignificant amounts. This metabolic pathway ensures efficient processing of the drug, helping to minimize potential toxicity and side effects.

Absorption:

The absorption characteristics of Oxetacaine are crucial for its therapeutic efficacy: 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. The drug's ability to rapidly penetrate into cells ensures quick onset of action.

Half-life:

The half-life of Oxetacaine is an important consideration for its dosing schedule: Oxetacaine presents a very short half-life of approximately one hour. This determines the duration of action and helps in formulating effective dosing regimens.

Protein Binding:

Oxetacaine exhibits a strong affinity for binding with plasma proteins: Due to the low half-life, it is thought that oxetacaine, when absorbed, presents a very low protein plasma binding. This property plays a key role in the drug's pharmacokinetics and distribution within the body.

Route of Elimination:

The elimination of Oxetacaine from the body primarily occurs through: Less than 0.1% of the amdinistered dose is recovered in urine within 24 hours in the form of unchanged oxetacaine or its metabolites. Understanding this pathway is essential for assessing potential drug accumulation and toxicity risks.

Volume of Distribution:

Oxetacaine is distributed throughout the body with a volume of distribution of: This pharmacokinetic property has not been studied. This metric indicates how extensively the drug permeates into body tissues.

Clearance:

The clearance rate of Oxetacaine is a critical factor in determining its safe and effective dosage: This pharmacokinetic property has not been studied. It reflects the efficiency with which the drug is removed from the systemic circulation.

Pharmacodynamics:

Oxetacaine exerts its therapeutic effects through: 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. The drug's ability to modulate various physiological processes underscores its efficacy in treating specific conditions.

Mechanism of Action:

Oxetacaine functions by: 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. This mechanism highlights the drug's role in inhibiting or promoting specific biological pathways, contributing to its therapeutic effects.

Toxicity:

Classification:

Oxetacaine belongs to the class of organic compounds known as amphetamines and derivatives. These are organic compounds containing or derived from 1-phenylpropan-2-amine, classified under the direct parent group Amphetamines and derivatives. This compound is a part of the Organic compounds, falling under the Benzenoids superclass, and categorized within the Benzene and substituted derivatives class, specifically within the Phenethylamines subclass.

Categories:

Oxetacaine is categorized under the following therapeutic classes: Agents for Treatment of Hemorrhoids and Anal Fissures for Topical Use, Anesthetics, Anesthetics, Local, Cytochrome P-450 CYP3A Inhibitors, Cytochrome P-450 CYP3A4 Inhibitors, Cytochrome P-450 CYP3A4 Inhibitors (strength unknown), Cytochrome P-450 Enzyme Inhibitors, Vasoprotectives. These classifications highlight the drug's diverse therapeutic applications and its importance in treating various conditions.

Experimental Properties:

Further physical and chemical characteristics of Oxetacaine include:

• Water Solubility:<0.1 g/100 ml at 23 ºC
• Melting Point: 100-101 ºC
• Boiling Point: 630 ºC at 760 mm Hg
• pKa: 6.25