Sucrafil O Gel

Indications

• Gastroesophageal reflux disease (GERD)
• Peptic ulcers
• Dyspepsia
• Hyperacidity

Dosage

Children: Refer to the BNF for Children for paediatric dosing recommendations.

Adults: Refer to the BNF for specific adult dosing recommendations.

Mechanism of action

Oxetacaine inhibits gastric acid secretion by suppressing gastrin secretion, while also exerting a local anesthetic effect on the gastric mucosa. It diminishes the conduction of sensory nerve impulses near the application site, reducing cell membrane permeability to sodium ions, which contributes to its anesthetic effects.

Pharmacodynamics

Oxetacaine improves common gastrointestinal symptoms, acting as an anesthetic antacid that raises gastric pH and provides prolonged pain relief at lower doses. It has been shown to produce a reversible loss of sensation and has antispasmodic effects on smooth muscle, blocking the action of serotonin. Its local anesthetic potency is significantly higher than that of other common agents, such as lignocaine and cocaine.

Pharmacokinetics

Information on the pharmacokinetics of oxetacaine, including absorption, distribution, metabolism, and excretion, is not provided in the sources. Further studies may be required to establish detailed pharmacokinetic profiles.

Adverse effects

• Nausea
• Vomiting
• Dizziness
• Allergic reactions
• Local irritation at the site of application

Precautions

• Use with caution in patients with a history of hypersensitivity to local anesthetics
• Caution is advised in patients with severe liver or kidney impairment
• Monitor for signs of systemic absorption, particularly if used in large quantities or over extensive areas

Pregnancy

There is limited data on the use of oxetacaine during pregnancy. Use only if clearly needed and after assessing the potential benefits and risks.

Breast-feeding

Limited data is available on the excretion of oxetacaine in breast milk. Caution is advised, and the benefits should be weighed against potential risks.

Storage

Store at room temperature, away from moisture and heat. Keep out of reach of children.

Formulations

• Topical gel
• Oral suspension

Indications

• Gastric ulcers
• Duodenal ulcers
• Prophylaxis of stress ulceration
• NSAID-associated ulcers

Dosage

Children: Refer to the BNF for Children for specific dosing information as it varies based on age and weight.

Adults: Adult: 1 g four times daily, taken on an empty stomach, or 2 g twice daily, depending on the clinical scenario. Maximum dosage is 8 g per day.

Mechanism of action

Sucralfate acts locally in the gastrointestinal tract. When it comes into contact with gastric acid, it undergoes a process of polymerization, forming a viscous gel that adheres to the ulcer site. This gel creates a physical barrier against further irritation and promotes healing by providing a conducive environment for repair. Additionally, sucralfate may stimulate mucosal defense mechanisms, including increased secretion of mucus and bicarbonate.

Pharmacodynamics

Sucralfate does not have systemic absorption; its effects are primarily localized within the gastrointestinal tract. The protective barrier it forms is effective against both acid and pepsin, reducing the damage to the mucosa and promoting ulcer healing. Its action is dose-dependent and requires administration on an empty stomach for optimal efficacy.

Pharmacokinetics

Sucralfate is minimally absorbed in the gastrointestinal tract, with over 90% of the administered dose remaining locally at the site of action. It has a half-life of approximately 6 to 12 hours, depending on the formulation and the individual patient's gastrointestinal transit time. It is excreted mainly in the feces and does not undergo significant hepatic metabolism.

Contra-indications

• Hypersensitivity to sucralfate or any of its components
• Patients with renal impairment (risk of aluminium accumulation)
• Children under 16 years (risk of Reye's syndrome)

Adverse effects

• Constipation
• Dry mouth
• Nausea
• Headache
• Vertigo
• Gastrointestinal disturbances
• Skin reactions
• Discoloration of mucous membranes

Interactions

• Sodium citrate: Severe interaction increasing risk of adverse effects
• Bictegravir: Unknown interaction decreasing exposure
• Warfarin: Unknown interaction decreasing effects
• Digoxin: Unknown interaction decreasing absorption
• Dolutegravir: Unknown interaction decreasing absorption
• Enteral feeds: Unknown interaction increasing risk of blocked enteral or nasogastric tubes
• Quinolones: Unknown interaction decreasing exposure
• Coumarins: Unknown interaction decreasing effects
• Sulpiride: Unknown interaction decreasing absorption
• Theophylline: Unknown interaction decreasing absorption

Precautions

• Caution in patients with renal impairment due to risk of aluminium accumulation
• Caution in patients receiving enteral feeds due to risk of bezoar formation
• Caution with concurrent use of other medications that may affect gastric pH

Pregnancy

Manufacturer advises to avoid unless essential; no information available regarding safety.

Breast-feeding

Amount probably too small to be harmful; limited information available.

Storage

Store in a cool, dry place away from direct sunlight. Keep out of reach of children.

Formulations

• Tablets
• Oral suspension

Mechanism of action

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.

Pharmacodynamics

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.