Sucralfate and Oxethazaine Suspension

Sucralfate is a medication that is widely used to prevent and treat a number of diseases in the gastrointestinal tract such as duodenal ulcers  gastro-esophageal reflux disease (GERD), gastritis, peptic ulcer disease, stress ulcer, in addition to dyspepsia .It is considered a cytoprotective agent, protecting cells in the gastrointestinal tract from damage caused by agents such as gastric acid, bile salts, alcohol, and acetylsalicylic acid (aspirin), among other substances.
Sucralfate has been shown to be a well-tolerated and safe drug. It is sold under many brands and is available in both tablet and suspension forms. It was approved by the FDA 1982 in tablet form, and in 1994 for the suspension form.

oxethazaince also called Oxetacaine, 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. It 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.

Sucralfate and Oxethazaine is used in the treatment of acidity, heartburn and stomach ulcers.

Mechanism of action

This is a combination of two medicines: Sucralfate and Oxetacaine / Oxethazaine. Sucralfate is a medication to treat ulcers. It covers the damaged ulcer tissue in the stomach and protects it from acid or injury to facilitate healing. Oxetacaine / Oxethazaine is a local anesthetic whose numbing effect provides fast relief from pain caused due to ulcers or acidic injury in the stomach.

pharmacodynamics:

Sucralfate: This drug aids in the healing of duodenal ulcers, relieving painful inflammation by creating a protective mechanical barrier between the lining or skin of the gastrointestinal tract and damaging substances . In addition, sucralfate acts to increase levels of growth factors locally, and also causes an increase in prostaglandins which are important in the healing of the mucosa (lining) of the gastrointestinal tract.
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. 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.

pharmacokinetics:

Sucralfate:
Absorption: This drug is absorbed from the gastrointestinal tract in very minimal quantities . The adsorbed sulfated disaccharide is excreted in the urine .This drug contains aluminum and after the administration of 1 g of sucralfate 4 times per day, about 0.001% to 0.017% of this aluminum content is absorbed in patients with normal renal function .
Metabolism: This drug is absorbed in very small quantities and is not significantly metabolized
Elimination: The negligible amount of this drug that is absorbed is excreted mainly in the urine within 48 hours.

Oxetacaine:
Absorption: 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.
Metabolism: 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.
Elimination: Less than 0.1% of the amdinistered dose is recovered in urine within 24 hours in the form of unchanged oxetacaine or its metabolites.

Common side effects include

• Constipation
• Allergic reaction
• dry mouth,
• upset stomach, gas
• nausea