GASTROINTESTINAL AGENTS  

 
Inorganic agents used to treat gastrointestinal disorders 
1. Products for altering gastric pH 
2. Protectives for intestinal inflammation 
3. Adsorbents for intestinal toxins 
4. Cathartics or laxatives for constipation 
 
- Do not require a prescription 
- Pharmacist is directly responsible --- should inform himself of the uses and limitations of the products and be 
ready to advise customers 
- Symptoms of a more serious condition 
 
ANTACIDS  
- Alkaline bases used to neutralize HCl (which may cause pain and ulceration) 
- Inactivate pepsin, a proteolytic enzyme 
 
Excess gastric juices can cause gastritis and peptic ulcer  
 
Stomach pH 
- pH 1 (empty) - pH 7 (food is present) 
 
Low acid pH - due to the presence of endogenous HCl (always present under physiological conditions) 
 
When hyperacidity develops, the results can range from gastritis to peptic ulcer. 
 
Gastritis - general inflammation of the gastric mucosa 
Peptic Ulcer - specified circumscribed erosion 
- Tense individual who contains emotions tends to have greater incidence of peptic ulcer 
- can be located in: 
● esophageal ulcer - lower end of esophagus 
- occurs when esophageal sphincter is defective  
- Heartburn (during belch or upon lying in bed) 
- Relief: sleeping on a bed elevated at the head (reduces flow of gastric fluid from 
the stomach to esophagus) 
● peptic ulcer - stomach 
● duodenal ulcer - duodenum 
 
TREATMENT: 
- Diet  
- Antacid and/or anti-cholinergic therapy to complete bed test and possible surgery 
- Removal of emotional stress  
 
CRITERIA OF AN ANTACID 
1. Should NOT be absorbable or cause systemic alkalosis 
2. Should NOT be a laxative or constipation 
3. Should exert the effect rapidly and over a long period of time 
4. Reaction of the antacid with gastric HCl should NOT cause a large evolution of gas 
5. Should buffer in the pH 4-6 range 
6. Should probably inhibit pepsin 
 
 
 
 
 
 
 
 
 
 
 
 
 
ANTACIDS  

  SYNONYMS  PROPERTIES  USES 

Sodium Bicarbonate     - Highly water soluble  - Effervescent antacid 

  - Rapid onset of actions but  preparations 
relatively short duration   - Reacts with acid (citric, 
- Can cause a sharp increase  tartaric, etc) with the 
in gastric pH up to pH 7  evolution of CO​2​. 
- Can case belching and  - “Sparkling 
flatulence ( because of the  flavor” - flat 
evolution of CO​2​)   saline taste 

Aluminum Hydroxide USP    - both are assayed in terms of   

    their aluminum oxide (Al​2​O​3​)   
    content and their   
    acid-consuming capacity   
       
       
1. Aluminum Hydroxide    - white viscous suspension,  - gastric antacid 
Gel USP 26 - white    permitted to contain  - Widely employed in the 
viscous suspension     aromatics like peppermint oil  treatment of 
    and sweetening substances  hyperchlorhydria and 
    (sucrose, glucose, glycerin,  peptic ulcer  
    saccharin or other similar  - Intestinal toxemia 
    subtances). Not more than 5%  - has the capacity to 
    of a preservative is also  adsorb HCl, toxins, gases 
    allowed (sodium benzoate,  and bacteria 
    benzoic acid, methyl paraben,  - interfere with the 
    etc.). pH between 5.5-8.0  adsorption of other drugs 
       
    - white, colorless, tasteless 
    amorphous powder insoluble 
2. Dried Aluminum  Dried Aluminum  in water and alcohol. Soluble 
Hydroxide Gel USP 26  Hydroxide Gel and  in dilute mineral acids and 
Tablets USP 26   solutions of fixed alkali 
hydroxide 

CALCIUM-CONTAINING ANTACIDS 
- Dependent upon their basic properties and not on an amphoteric effect  
- Those used in medicines are poorly soluble salts  
- Raise the stomach pH to nearly 7 
- Tend to be constipating and are usually found in combination with magnesium antacids 

Calcium Carbonate USP 26  Precipitated Chalk  - Fine, white, odorless, tasteless,  - one of the most popular 
microcrystalline powder  antacids 
- stable in air   - action is limited by 
- Insoluble in water and  amount of salt that will go 
alcohol  into solution 
- solubility increases by the  - as gastric HCl consumes 
presence of ammonium salt or  CaCO​3​, more goes into 
carbon dioxide  solution. This continues until 
- solubility decreases by the  one of the two is 
presence of any alkali  consumed. 
- dissolves with effervescence  - consipative effect 
in dil. CH​3​COOH, dil. HCl and  (reason why it is mostly 
dil HNO​3,  combined with 
  magnesium antacids) 
- Lozanges and Oral 
suspension 

Tribasic Calcium Phosphate  Precipitated  - white, odorless, tasteless  - antacid in treatment of 
- Found in nature as  Calcium Phosphate  powder  hyperacidity  
phosphorite or    - insoluble in water and  - poduct of primary and 
 phosphate rock and  Tertiary Calcium  alcohol  secondary phosphate 
apatite  Phosphate  - readily dissolves in dil. HCl  diminishes the hydrogen 
  and HNO​3  ion concentration in gastric 
Calcium Phosphate  HCl 
- ADVANTAGE: no gas 
produced that may cause 
flatulence 
- ADVANTAGE: does not 
alkalize the system  
- source of calcium, but 
only very little is absorbed 
-- not valuable in acute 
calcium deficiency 

MAGNESIUM CONTAINING ANTACIDS 

- All magnesium antacids function the same except for magnesium trisilicate 
- Poorly soluble salts which only go to solution as acid consumes the small amount of anion already in solution 
- As the pH of the stomach approaches neutrality, rate of magnesium salt dissolution slows down and stops at 
netrality ----it is the ANION raether than the magnesium cations that confers the antacid properties 
- Magnesium cations causes this group of antacid to be laxatives 
- Usually combined with aluminum and calcium antacids in an attempt to equalize the constipative and 
laxative actions 

Magnesium Carbonate USP  Carbonate of  - white, bulky, odorless powder  - its actacid properties are 
Magnesia  - slightly earthly taste  due to the hydroxide and 
  - often occurs in friable masses  carbonate anions reacting 
Magnesium  - nearly insoluble in water to  with the gastric HCl 
Carbonate  which imparts slightly alkaline  - due to its limited solubility, 
  reaction --- due to  it only dissolves as 
Heavy Magnesium  disassociation of Mg(OH)​2  carbonate and hydroxides 
Carbonate  - insoluble in alcohol  are being consumed 
Dissolves with effervescence in 
dilute acids 
 

Magnesium Hydroxide USP    - white, bulky powder  - efficient antacid 

  - insoluble in water and  - In high doses, it is used as 
  alcohol  laxative --- due to the 
  - dissolves in acids  formation of magnesium 
    chloride in the stomach  
     
     
    - minimize interaction of 
Milk of Magnesia  - Suspension of Magnesium  glass containers and 
Hydroxide  Mg(OH)​2​, small amounts of 
citric acid maybe added 
- suitable flavoring agents 
may be added  
- popular as an antacid 
and laxative 

Magnesium Oxide  Magnesia    - laxative, diuretic, antacid 

    - arsenic antidote 
    - in order to prevent the 
1. Light Magnesium  - the two forms are identical in  formation of a gelatinous 
Oxide  chemical composition and in  mass, it should be 
  purity  administered in about 29 
  - white, odorless, powders   times its weight of water 
2. Heavy Magnesium  - nearly insoluble in water and  - magnesia should be 
Oxide  in alcohol  added to water and not 
  - dissolve in dilute acids   reversed (to avoid 
- absorb carbon dioxide and  formation of hard lump_ 
moisture, when exposed to air 
- light magnesium oxide 
 hydrolyzes to Mg(OH)​2​ more 
easily 

Magnesium Trisilicate USP    - compound of magnesium  - gastric antacid --- 

oxide and silicon dioxide (+  valuable in peptic ulcer 
water)  - colloidal silicic acid or 
- fine, white, odorless, tasteless  hydrous silica has 
powder, free from grittiness  adsorptive powers and 
- insoluble in water and  could protect the ulcer 
alcohol  from acid and peptic 
- readily decomposed by  attack 
mineral acids    
- as amount of silicon dioxide 
increases with respect to 
magnesium oxide, there is loss 
in antacid capability 

Magnesium Phosphate USP  Tertiary Magnesium  - white, odorless, tasteless  - antacid 

Phosphate  powder  
- readily soluble in diluted 
mineral acids 
- almost insoluble in water 

COMBINATION ANTACID PREPARATIONS 

- Because no single antacid meets all the criteria of an ideal antacid, several products are on the market 
containing mixtures of antacids 
- Attempts to balance the constipative effect of calcium and aluminum with laxative effect of magnesium 
- One with rapid onset of action + one with supposedly longer duration of action 
 
a. Aluminum Hydroxide Gel - Magnesium Hydroxide Combination: Aludrox, WinGel, Maalox, Cremalin  
b. Aluminum Hydroxide Gel - Magnesium Trisilicate Combination: Gelusil, Tricareamaleate and Trisogel  
c. Magaldrate - chemical combination of Aluminum Hydroxide and Magnesium Hydroxide (Riopan) 
d. Simethicone-containing Antacids: Di-Gel, Mylanta, because many people with gastric hyperacidity complain 
of being “gassy”, the defoaming agent, simethicone, has been added to some antacids  
e. Alginic Acid - Sodium Bicarbonate containing Antacids: Gaviscon and Foamtab. This type of preparation was 
formulated in an attempt to provide symptomatic relief of reflux esophagitis.  
 
PROTECTIVES AND ABSORBENTS 
- commonly used for the treatment of mild diarrhea  
- Diarrhea: SYMPTOM not a DISEASE  
- Results when some factors impair digestion and/or absorption = increasing bulk of intestinal tract  
- Increased bulk: stimulates ​peristalsis​ (propelling intestinal contents in the anus)  
- Serious Condition: for young and elderly patients  
- Can lead to dehydration and electrolyte imbalances 
- Chronic Diarrhea resulted from:  
- GI surgery 
- Carcinomas 
- Chronic Inflammatory Conditions  
- Absorptive Effects  
 
For the treatment of diarrhea consists of:  
- absorptive-protective agent  
- antidiarrheal agent  
- antibacterial agent  
 
Antidiarrheal:  
- act directly on the smooth muscle of the gut = spasm-like effect  
- DECREASE peristalsis, INCREASE segmentation  
 
Antibacterial 
- only effective if there is an actual infection caused by microorganisms 
 
Absorbent- Protective  
- absorb toxins, bacteria, and viruses  
- provides protective coating of intestinal mucosa  
 
BISMUTH-CONTAINING PRODUCTS 
Bismuth Salts as Antidiarrheal Agent  
- water insoluble  
- small amount goes into solution  
- Soluble bismuth cation: exerts mild astringent and & antiseptic action  
- Intestinal Hydrogen Sulfide: acts upon bismuth salts to form BISMUTH SULFIDE = Black stool resulting from the 
administration of bismuth-containing preparationS 
 
 

  SYNONYMS   PROPERTIES   USES 

Bismuth Subnitrate USP  Basic Bismuth Nitrate  - White, slightly  - Effective 

White Bismuth   hygroscopic powder  non-irritant 
- Gives acid reaction =  intestinal 
blue litmus paper   antiseptic 
- incompatible with  - Bismuth lessens 
tragacanth   gastric secretion  
- Reduce acidity  
- Treats ulcers and 
inflammation  

Bismuth Carbonate USp  Basic Bismuth Carbonate   - White or pale yellowish  - Protective and 
white   Antacid effects: 
- odorless  inflammations 
and stomach 
bowels  
- Astringent  
- absorbent : 
diarrhea and 
dysentery  

Milk of Bismuth   Bismuth Magma   COMPOSITION:  - Astringent  

Bismuth Cream   - contains bismuth  - Antacid  
hydroxide and   
bismuth subcarbonate 
in suspension water  
 

Kaolin USP  Porcelain Clay   Soft, yellow or whitish  - Protective and 

China Clay   brown in lumps   absorbent in 
Bolus Alba   Earthly and clay-like  diarrheal disorder 
taste  

ACTIVATED CHARCOAL USP 31  

- ADSORBENT IN THE TREATMENT OF DIARRHEA  
- ANTIDOTE IN CERTAIN TYPES OF POISONING  
 
SALINE CATHARTICS 
- Saline Cathartics (Purgatives) are agents that quicken and increase evacuation from the vowels  
- Laxatives: Mild Cathartics  
- Can be purchased without prescription  
- Widely used and abused  
 
The 1972 AMA Drug Evaluation states the criteria when cathartics are properly used:  
1.) To ease defecation in patients with painful hemorrhoids or rectal disorders.  
2.) To avoid potentially hazardous rises in the blood pressure during defecation in patients with hypertension, 
cerebral arterial diseases.  
3.) To relieve acute constipation 
4.) To remove solid material from the intestinal tract prior to certain roentgenographic studies 
 
Laxatives 
- should only be used for short term therapy  
- prolonged use may lead to loss of spontaneous bowel rhythm 
- causes patient to become dependent on laxative = “LAXATIVE HABITS”  
 
Four Types of Laxatives:  
a. Stimulant Laxatives  
- act by local irritation on the intestinal tract = Increases PERISTALTIC ACTIVITY 
b. Bulk-forming Laxatives  
- ​made from cellulose and other non-digestible polysaccharides  
- swell = when wet  
- Increased bulk = stimulates PERISTALSIS 
c. Emollient Laxatives  
- act neither as LUBRICANTS = facilitating the passage of compacted fecal material nor as stool 
softeners  
- Ex: mineral oil 
d. Saline Cathartics  
- Increases the osmotic load of GI tract  
- Salts of poorly absorbable anions and cations  
- Body relieves the HYPERTONICITY OF THE GUT by secreting additional fluids into the intestinal tract 
- Increased bulk = stimulates PERISTALSIS 
 
 
 

  SYNONYMS   PROPERTIES  USES 

Monosodium Phosphate  - Sodium Dihydrogen  - Colorless crystals or  - Urinary Acidifier  

USP  Phosphate  white crystalline  - Cathartic  
- Sodium Acid  powder  - Salt = used to 
Phosphate   - Odorless and  render the urine 
- Primary Phosphate  deliquescent  acidic in case of 
- Sodium Biphosphate   - Solution= acid   CYSTITIS with 
- Effervesces with  HEXAMETHYLENETE
sodium carbonate  TRAMINE 
(Methanamine) 
 

Dibasic Sodium  - Dibasic Sodium  - Colorless or wite  - Saline cathartic 

Phosphate USP  Phosphate   granular salt  
- Disodium Hydrogen  - Effervesces in warm 
Phosphate  dry air  
- Secondary Sodium   
Phosphate  
 

Potassium Sodium  - Rochelle Salt  - Odorless crystals or  - Cathartic  

Tartrate USP  - Seignette Salt   white crystalline  - Ingredient of 
powder   Seidlitz Powder  
- Cooling saline test 
- Effervesces in warm 
dry air  
 Magnesium Sulfate USP   - Epsom Salt   - small , colorless  - Active cathartic  
- Bitter Salt   crystals  - Anticonvulsant 
- Needle like with  parenterally  
cooling saline bitter  - Anesthetic effect in 
taste   sprains and bruises  
- Efflorescent in air  
- Solution = neutral to 
litmus  

Magnesium Citrate USP   - Citrate of Magnesia   PREPARATION:   NONE 

- Purgative  - Made by reacting 
lemonade   magnesium 
carbonate with 
citric acid  
- Must be sterilized or 
pasteurized  
 
 
 
NON-SULFATE SALINE CATHARTICS 
a. Sodium Sulfate - ​Glauber’s Salt  
b. Potassium Sulfate - ​Dibasic Potassium Phosphate, Dipotassium Hydrogen Phosphate, DKP  
c. Potassium Bitartrate -​ Cream of Tartar, Potassium Acid Tartrate; Potassium Hydrogen Tartrate  
d. Calomel - ​Mercurous Chloride, Mild Mercury Chloride