Gaspel
Gaspel Uses, Dosage, Side Effects, Food Interaction and all others data.
Alumunium hydroxide acts on the HCI in the stomach by neutralization, forming aluminium chloride salt and water.
Magnesium hydroxide increases peristaltic activity causing osmotic retention of fluids, thus resulting in bowel evacuation. It also reduces stomach acid by reacting with hydrochloric acid to form Mg chloride.
As an antacid, magnesium hydroxide suspension neutralizes gastric acid by reacting with hydrochloric acid in the stomach to form magnesium chloride and water. It is practically insoluble in water and does not have any effect until it reacts with the hydrochloric acid in the stomach. There, it decreases the direct acid irritant effect and increases the pH in the stomach leading to inactivation of pepsin. Magnesium hydroxide enhances the integrity of the mucosal barrier of the stomach as well as improving the tone of both the gastric and esophageal sphincters.
As a laxative, the magnesium hydroxide works by increasing the osmotic effect in the intestinal tract and drawing water in. This creates distension of the colon which results in an increase in peristaltic movement and bowel evacuation.
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 | Gaspel |
| Generic | Aluminium Hydroxide + Magnesium Hydroxide + Oxetacaine |
| Type | Suspension |
| Therapeutic Class | |
| Manufacturer | |
| Available Country | India |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Aluminium Hydroxide is used for Duodenal ulcer, Dyspepsia, Flatulence, Gastric Hyperacidity, Gastric ulcer, Gastritis, Gastroesophageal reflux disease (GERD), Gastrointestinal hyperacidity, Heartburn, Heartburn & gastritis, Hyperacidity, Indigestion, Oesophagitis, Peptic ulcer disease, Stomach distension, Upper Gl bloating.
Acid regurgitation, Constipation, Gastric ulcer, Gastrointestinal hyperacidity, Heartburn, Indigestion, Non ulcer dyspepsia, Osmotic laxative
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.
Gaspel is also used to associated treatment for these conditions: Acid indigestion, Colic, Constipation, Dyspepsia, Flatulence, Gastric Ulcer, Heartburn, Upset stomach, Antacid therapy, Gastric Acid SuppressionAcid Reflux, Anal Fissures, Hemorrhoids, Proctitis, Pruritus Ani, Anal eczema
How Gaspel works
The suspension of magnesium hydroxide is ingested and enters the stomach. According to the amount ingested, the magnesium hydroxide will either act as an antacid or a laxative.
Through the ingestion of 0.5-1.5 grams (in adults) the magnesium hydroxide will act by simple acid neutralization in the stomach. The hydroxide ions from the magnesium hydroxide suspension will combine with the acidic H+ ions of the hydrochloric acid made by the stomachs parietal cells. This neutralization reaction will result in the formation of magnesium chloride and water.
Through the ingestion of 2-5 grams (in adults) the magnesium hydroxide acts as a laxative in the colon. The majority of the suspension is not absorbed in the intestinal tract and will create an osmotic effect to draw water into the gut from surrounding tissues. With this increase of water in the intestines, the feces will soften and the intraluminal volume of the feces will increase. These effects still stimulate intestinal motility and induce the urge to defecate. Magnesium hydroxide will also release cholecystokinin (CKK) in the intestines which will accumulate water and electrolytes in the lumen and furthermore increase intestinal motility.
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.
Dosage
Gaspel dosage
Usual Adult Dose: Up to 1 g daily.
Dyspepsia: 500 to 600 mg orally 4 to 6 times a day as needed, between meals and at bedtime.
Duodenal Ulcer: 500 to 1500 mg orally 4 to 6 times a day as needed, between meals and at bedtime.
Erosive Esophagitis: 500 to 1500 mg orally 4 to 6 times a day as needed, between meals and at bedtime.
Gastric Ulcer: 500 to 1500 mg orally 4 to 6 times a day as needed, between meals and at bedtime.
Gastroesophageal Reflux Disease: 500 to 1500 mg orally 4 to 6 times a day as needed, between meals and at bedtime.
Zollinger-Ellison Syndrome: 500 to 3600 mg orally 4 to 6 times a day as needed, between meals and at bedtime.
Hyperphosphatemia: 500 to 1000 mg orally 4 times a day, with meals and at bedtime. The dosage should be titrated to the serum phosphate level. Max Dosage: 10 g daily in divided doses may be taken with or without food.
Gastrointestinal hyperacidity:
- Adult: Up to 1 g daily, usually given in conjunction with an aluminium-containing antacid eg, aluminium hydroxide.
Osmotic laxative:
- Adult: 2.4-4.8 g daily as a single dose or in divided doses.
- Child: 6-11 yr: 1.2-2.4 g daily; 2-5 yr: 0.4-1.2 g daily. Doses may be given as a single dose or in divided doses.
Side Effects
Constipation; intestinal obstruction (with large doses); phosphate depletion may occur with prolonged admin or large doses.
GI irritation, diarrhoea, abdominal cramps; hypermagnesaemia (in patients with renal impairment). Paralytic ileus.
Toxicity
LD50=8500 mg/kg (rat, oral)
Common side effects include drowsiness or flushing (warmth, redness or tingly feeling).
Daily use of magnesium hydroxide can result in fluid and electrolyte disturbances.
Excessive use of the laxative effects of magnesium hydroxide may result in abdominal cramping, nausea and/or diarrhea.
In overdose, symptoms of gastrointestinal irritation and/or watery diarrhea may occur.
Magnesium hydroxide poisoning can result in hypermagnesemia which includes symptoms of: nausea, vomiting, flushing, thirst, hypotension, drowsiness, confusion, loss of tendon reflexes, muscle weakness, respiratory depression, cardiac arrhythmias, coma and cardiac arrest.
Not to be used in individuals with any form of kidney disease or renal failure, a magnesium restricted diet or with any sudden changes in bowel movement lasting over two weeks. Also not to be used in those individuals with abdominal pain, nausea, vomiting, symptoms of appendicitis or myocardial damage, heart block, fecal impaction, rectal fissures, intestinal obstruction or perforation or renal disease. Not to be used in women who are about to deliver as magnesium crosses the placenta and is excreted in small amounts in breast milk.
Using magnesium hydroxide with aluminum hydroxide can decrease the absorption rate of these drugs.
Magnesium hydroxide can react with digoxin, dicoumerol and cimetidine.
Use of ibuprofen with magnesium hydroxide can increase the absorption of the ibuprofen.
Use of magnesium hydroxide with penicallamine, bisphosphates, ketoconazole, quinolones or tetracycline can decrease the absorption of these drugs.
Enteric-coated tablets can be prematurely released when taken with magnesium hydroxide.
It is important to routinely monitor levels of serum magnesium and potassium in patients using magnesium hydroxide. Serum magnesium levels are necessary to determine how much magnesium is being absorbed and how much is being excreted by the kidneys. Excessive diarrhea can occur from use of magnesium hydroxide and thus it is important to also monitor serum potassium levels to ensure hypokalemia does not occur.
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.
Precaution
Chronic renal impairment; CHF; oedema; cirrhosis and low Na diets; patients with recent Gl haemorrhage. Administer 2-3 hrs before/after another medication to minimise drug interactions. Pregnancy and lactation
Colostomy, ileostomy; electrolyte imbalance. Monitor for toxicity in patients with impaired renal function. Pregnancy.
Interaction
Enhanced absorption with citrates or ascorbic acid. Decreases absorption of allopurinol, tetracyclines, quinolones, cephalosporins, biphosphonate derivatives, corticosteroids, cyclosporin, delavirdine, Fe salts, imidazole antifungals, isoniazid, mycophenolate, penicillamine, phosphate supplements, phenytoin, phenothiazines, trientine.
Decreases absorption of tetracyclines and biphosphonates. Separate administration of these and other drugs by around 2 hr.
Volume of Distribution
The peak action and distribution of magnesium hydroxide are variable.
This pharmacokinetic property has not been studied.
Elimination Route
About 15%-50% of magnesium hydroxide is absorbed very slowly through the small intestine.
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
N/A
Oxetacaine presents a very short half-life of approximately one hour.
Clearance
Magnesium hydroxide is mainly excreted in the urine by the kidneys. Since the kidneys play a major role in its clearance, individuals with renal failure are at risk of hypermagnesemia with long term consumption as the appropriate amounts of magnesium may not be excreted.
This pharmacokinetic property has not been studied.
Elimination Route
After oral administration, up to 50% of the magnesium hydroxide suspension may be absorbed as magnesium ions through the small intestines and then rapidly excreted in the urine through the kidneys. The unabsorbed drug is mainly excreted in the feces and saliva.
Less than 0.1% of the amdinistered dose is recovered in urine within 24 hours in the form of unchanged oxetacaine or its metabolites.
Pregnancy & Breastfeeding use
Pregnancy Category C. Animal reproduction studies have shown an adverse effect on the fetus and there are no adequate and well-controlled studies in humans, but potential benefits may warrant use of the drug in pregnant women despite potential risks
Pregnancy category- A.
Contraindication
Hypersensitivity to aluminium salts.
Intestinal obstruction, faecal impaction; renal failure; appendicitis.
Innovators Monograph
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