Chapter V Gastrointestinal Agents Inorganic agents used to treat gastrointestinal disorders 1. Altering gastric pH 2.

. Protectives for intestinal inflammation 3. Adsorbents for intestinal toxins 4. Cathartics/Laxatives for constipation Dont require prescription Pharmacists responsibility

Antacids
Alkaline bases used to neutralize excess HCl which may cause pain and ulceration Inactivate the proteolytic enzyme, pepsin Stomach pH pH: 1 (empty) pH: 7 (food present) Hyperacidity Gastritis or peptic ulcer (circumscribed erosion) Criteria for ideal antacid 1. Should not be absorbable or cause systemic alkalosis 2. Not Laxative or should not cause constipation 3. Rapid effect over long period of time 4. Should not cause large evolution of gas 5. Buffer pH: 4 6 6. Inhibit pepsin Peptic Ulcer Lower end of esophagus Esophageal ulcer (Esophageal sphincter is defective) May experience Heartburn (HCl reflux) Prevention: Headrest is elevated to prevent reflux Stomach Gastric ulcer (malignancy, hemorrhage are common) Duodenum Duodenal ulcer (perforation of stomach is common) Correlation with emotional stress Treatment depends on severity of ulcer (Diet, Antacid, Anticholinergic, Bed rest) Sodium Bicarbonate ( NaHCO3 ) H2O Soluble Rapid onset but short duration Sharp increase pH to 7 or higher Evolution of CO2 Flatulence and Belching Effervescent antacid preparations o React with acid with evolution of CO2 Sparkling flavor to oral solutions Aluminum Hydroxide ( Al(OH)3 ) 2 Physical forms: 1. Al(OH)3 Gel USP 26 White viscous suspension that may contain aromatics (Peppermint oil, sweetening) Sodium benzoate, benzoic acid, etc > 0.5% preservative is not allowed 2. Dried Al(OH)3 Gel USP 26 White colorless, tasteless, amorphous powder
Insoluble in H2O and alcohol but soluble in dilute mineral acids & sol. Fixed Alkali OH

Gel form Very fine particle: Greater surface area coverage: Adsorption Ideal buffers pH: 3 5 Amphoteric characters Loss of antacid properties upon aging May cause constipation, nausea and vomiting Treatment: Hyperchlorhydia, intestinal toximea and Peptic ulcer Theory: Capability of adsorbing HCl, toxins, gases & bacteria Adsorbs pepsin and may interfere adsorption of other drugs

Calcium containing Antacid Dependent upon their basic properties and not on amphoteric effect Raise stomach pH to nearly 7 Constipating Counteract: Combination with Magnesium antacids Calcium Carbonate ( CaCO3 ) Precipitated Chalk Fine, white odorless, tasteless, microcrystalline powder Stable in air Insoluble in H2O and Alcohol ( Solubility by adding nay ammonium or CO2) Effervescence if diluted CH3COOH, HCl, HNO3 present One of the most popular antacid Fast action Action is limited with the amount of salt in the solution May cause Constipation Counteract: Combination with Mg2+ antacids Dosage forms : Lozenges or Oral suspension Tribasic Calcium Phosphate Pppted. Calcium Phosphate, Tertiary Calcium Phosphate, Calcium phosphate White, odorless, tasteless powder Insoluble in H2O and Alcohol (Dissolves: Presence of diluted HCl and HNO3) Abundant in nature as Phosphorite or Phosphate rock and Apatite Advantage over NaHCO3: No gas is produced (Flatulence) & Doesnt Alkanize system Magnesium containing Antacids Poorly soluble salts As pH of stomach approaches neutrality, Mg salt slows down and stops at neutrality Laxative properties Counteract: Combination with Al+3 and Ca+2 antacids Magnesium Carbonate Carbonate of Magnesia, Heavy Magnesium Carbonate White, bulky, odorless powder with earthly taste in friable masses Insoluble in H2O and Alchol Antacid properties Due to OH- and CO32- anions Magnesium Hydroxide ( Mg(OH)2 ) White, bulky powder Insoluble in H2O and Alcohol but dissolves in Acids High doses: Laxative Milk of Magnesia Suspension of Mg(OH)2 Popular Antacid and Laxative Magnesium Oxide ( MgO ) - Magnesia 2 Varieties: 1. Light Magnesium Oxide 5 g occupy 40 50 mL Hydrolyzes Mg(OH)2 easily 2. Heavy Magnesium Oxide 5 g occupy 10 20 mL White, odorless powder that are identical in chemical composition and purity Differ in Density Dissolves in dilute acids but insoluble in H2O and Alcohol Absorbs CO2 and moisture Laxative, diuretic and antacid Add MgO to H2O 29 times its weight of water to prevent gelatinous mass

Magnesium Trisilicate Compound of MgO + SiO2 (Silicone dioxide) Fine, white, odorless, tasteless powder that is free from grittiness Insoluble in H2O and Alcohol but decomposed by mineral acids As SiO2 , the antacid capability Introduced as gastric antacid for peptic ulcer Colloidal silicic acid adsorptive powers that can protect from ulcer Magnesium Phosphate ( Mg3(PO4)2 ) Tertiary Magnesium Phosphate White odorless and tasteless powder Insoluble in H2O but soluble in diluted mineral acid Combination Antacid Preparation To balance constipative effect (Ca2+ , Al3+) and laxative effect (Mg2+) Mixture may give rapid onset and longer duration of action Examples: 1. Aluminum Hydroxide Gel Magnesium Hydroxide Combination: Aludrox, Wingel, Maalox & Cremalin 2. Aluminum Hydroxide Gel Magnesium Trisilicate Combination: Gelusil, Tricreamalate, Triosgel 3. Magaldrate Al(OH)3 + Mg(OH)2 (Riopan) 4. Simethicone Defoaming agent to get rid of gassy feeling; Absorbs gas Containing antacids: Di-gel, Mylanta 5. Alginic Acid Provide relief from Reflux esophagitis NaHCO3 antacid containing antacid: Gaviscon, Foamtab

Protectives and Adosrbents Treatment for mild diarrhea (Symptom not a disease) Diarrhea Impair digestion or absorption which increase bulk of intestinal tract that
stimulates peristalsis o Loss of fluid and electrolyte Dehydration and electrolyte imbalance o Acute Diarrhea Tissue damage or irritation; electrolytes from body fluids to intestinal tract Caused by bacteria, poisons, drugs, allergy, disease o Chronic Diarrhea Gastrointestinal surgery, carcinomas, inflammatory and adsorptive defects Usually consist of Adsorptive-protective agents Absorbs toxins, bacteria, viruses that provides protective coating of intestinal mucosa Ideal antidiarrheal Act directly on smooth muscle to produce spasm-like effect that decreases peristalsis and increase segmentation Antibacterials are effective if infection is cause by microorganisms