PHARMACEUTICALL INORGANIC CHEMISTRY • It is used mainly to react with an acid with the

evolution of CO2 to produce a “sparkling” flavor

INSTRUCTOR: MRS. ANGELICA LOPEZ in preparations that will have saline taste.

TRANSCRIBED BY: MARK HAROLD C.

GONZALES
2. Aluminum hydroxide
CHAPTER 7: GASTROINTESTINAL AGENTS
7.1 ANTACIDS a. Aluminum hydroxide Gel
7.2 PROTECTIVES AND ADSORBENTS
• This is used to treat hyperchlorhydria and peptic
7.3 SALINE CATHARTICS
ulcer, intestinal toxemia.

• It absorbs HCl, toxins, gases, and bacteria.

7.1 ANTACIDS
• It does not produce systemic alkalosis.
Antacids – products for altering gastric pH;
alkaline basis used to neutralize the excess of b. Dried Aluminum hydroxide Gel
gastric

HCl associated with gastritis and peptic ulcers

3. Calcium-containing antacids
Indications: 1. to neutralize excess HCl which
may be causing pain and possible ulceration. ▪ These antacids are dependent not upon their basic
properties unlike aluminum antacids, which
2. To inactivate proteolytic enzyme, pepsin. depends on amphoteric properties.

Criteria for an ideal antacid ▪ Calcium antacids tend to be constipating and are
usually found in combination with magnesium.
1. Should not be absorbable or cause systemic
alkalosis.

2. Should not be a laxative or cause constipation. a. Precipitated Calcium carbonate

3. Should exert the effect rapidly and over a long Synonym: precipitated chalk
period of time.
▪ This is a popular antacid because of its fast
4. The reaction of the antacid with gastric HCl action.
should not cause a large evolution of gas.
▪ Its action is limited by the amount of salt that
5. Should buffer in the pH 4-6 range. will go into solution.

6. Should properly inhibit pepsin.

b. Tribasic Calcium phosphate

1. Sodium bicarbonate

• Highly water soluble with rapid onset of action Synonym: precipitated calcium phosphate; tertiary
but relatively short duration. calcium phosphate; calcium phosphate

• Causes sharp increase in gastric pH. ▪ It is used as an antacid in the treatment of

hyperacidity.
• Causes belching and flatulence due to evolution
of CO2 in the presence of acid.

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▪ MOA: The production of 1° and 2° phosphate  To prevent the formation of a gelatinous mass, it
diminished the II concentration of the gastric HCl. should be administered in about 20 times its
weight of water. The magnesia should be added to
 Its advantage is it does not produce gas that may water and not reversed in order to avoid the
cause flatulence and does not alkalinize the formation of hard lump.
system.

d. Magnesium trisilicate
4. Magnesium-containing antacids
 It is used as gastric antacid for peptic ulcer.
❖ Magnesium cation causes laxative action. They
are found in combination with aluminum and  MOA: The colloidal silicic acid or hydrous
calcium antacids to equalize the constipative and silica, which is formed in the reaction, have
laxative action. adsorptive powers and could protect the ulcer from
acid and peptic attack.
a. Magnesium carbonate

➢ Synonym: carbonate of magnesia, heavy

magnesium carbonate e. Magnesium phosphate

Synonym: Tertiary Magnesium phosphate

➢ Kinds: Light Magnesium Carbonate and Dense
or heavy Magnesium carbonate Combination Antacid Preparations

➢ Use: Antacid Rationale:

➢ MOA: OH- and CO3- reacting with the gastric 1. To balance the constipative effect of calcium
HCl and aluminum with the laxative effect of
magnesium.

2. A mixture of an antacid with rapid onset of

b. Magnesium hydroxide action and one with a supposedly longer duration
of action.
Synonym: Milk of magnesia
a. Al(OH)3 Gel-Mg(OH)2 Combinations
✓ It is used as an antacid, laxative (in high dose)
b. Al(OH)3 Gel-Magnesium Trisilicate
✓ MOA: Formation of magnesium chloride in the Combinations
stomach which exerts a “salt action” in the
intestinal tract causing a mild laxative action c. Magaldrate

d. Simethicone-containing antacids

c. Magnesium oxide e. Alginic acid-Sodium bicarbonate

Synonym: magnesia 7.2 PROTECTIVES AND ADSORBENTS

Kinds: Light Magnesium Oxide and Heavy  This group of GI agents is commonly used for
Magnesium Oxide the treatment of mild diarrhea.

 It is used as a laxative, diuretic, antacid, and  Diarrhea is a symptom and not a disease. It
antidote in arsenic poisoning. results when some factor impairs digestion and/or

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absorption, thereby increasing the bulk of the Use(s): Protective and antacid effect in
intestinal tract. inflammations of the stomach and bowels,
radiopaque contrast medium, astringent, absorbent
 This increased bulk stimulates peristalsis, in diarrhea.
propelling the intestinal contents to the anus.
c. Milk of Bismuth
 Diarrhea is a serious condition, particularly for
the very young or elderly patients. Synonyms: Bismuth Magma, Bismuth cream

 The loss of fluids and electrolytes can quickly • Milk of Bismuth contains bismuth hydroxide and
lead to dehydration and electrolyte imbalance. bismuth subcarbonate in suspension in water.

 Most products for the treatment of diarrhea will • It is made by concerting bismuth subnitrate to
consist of an adsorptive-protective, an bismuth nitrate by the addition of nitric acid. Then
antidiarrheal agent, and possibly an antibacterial by the treatment with ammonium carbonate and
agent. ammonia solution, bismuth nitrate is converted to
bismuth hydroxide and subcarbonate.
 The antidiarrheal agent should act directly on
the smooth muscles of the gut to produce a spasm- • It is used as astringent and antacid.
like effect, which decreases peristalsis and
increases segmentation. 2. Kaolin

 The antibacterials are only effective if there is Synonyms: Porcelain clay, China clay, Bolus Alba
an actual infection caused by microorganisms. Use(s): It is found together with the vegetables
 The adsorbent-protective supposedly adsorb carbohydrate, pectin (Kaopectate) and employed
toxins, bacteria, and viruses along with providing a as a protective and adsorbent in diarrheal
protective coating of the intestinal mucosa. disorders.

1. Bismuth-containing Products 3. Activated Charcoal

MOA: The soluble bismuth cation supposedly Use(s): It is classified as a universal antidote in
exerts a mild astringent and antiseptic action. poisoning. It is employed in the treatment of
Intestinal hydrogen sulfide gas acts upon the diarrhea.
bismuth salts to form bismuth sulfate; hence, the 7.3 SALINE CATHARTICS
black stools resulting from the oral administration
of bismuth-containing preparations. • This is also known as purgatives and is an agent
that quickens and increases evacuation from the
a. Bismuth subnitrate bowel.
Synonyms: Basic Bismuth nitrate; White Bismuth; • Laxatives are mild cathartics.
Spanish White
• Uses: a.) to ease defecation in patients with
Use(s): Effective non-irritant antiseptic, for gastric painful hemorrhoids or other rectal disorders.
ulcers, inflammation, and common remedy for
diarrhea. b.) to avoid potentially hazardous rises in blood
pressure during defecation in patients with
b. Bismuth subcarbonate hypertension, cerebral or arterial diseases.
Synonym: Basic Bismuth carbonate c.) to relieve acute constipation.

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d.) to remove solid material from the intestinal Synonym(s): sodium dihydrogen phosphate;
tract prior to certain roentgenographic studies. sodium acid phosphate; primary sodium phosphate

Use(s): it is used as urinary acidifier and a

cathartic.

2. Sodium phosphate

Four Types of Laxatives

Synonyms: Dibasic sodium phosphate; disodium
1. Stimulant Laxatives, hydrogen phosphate; secondary sodium phosphate
which act by local irritation on the intestinal tract, *This should never be confused with the
which increases peristaltic activity. commercial tribasic sodium phosphate, which is
very alkaline and caustic and should never be used
2. Bulk-forming Laxatives
for intestinal purposes.
are made from cellulose and other non-digestible
3. Potassium Sodium Tartrate
polysaccharides, which swell when, wet with the
increased bulk stimulating peristalsis.

3. Emollient Laxatives Synonyms: Rochelle’s salt; Seignette Salt

act wither as lubricants facilitating the passage of Use(s): It is used as a cathartic, hydragogue,
compacted fecal material or as stool softeners. ingredient in Scidlitz powder.
4. Saline Cathartics 4. Magnesium sulfate
act by increasing the osmotic load of the GI tract.
They are salts of poorly absorbable anions and
sometimes cations. The body relieves the Synonyms: Epsom salt; Bitter salt
hypertonicity of the gut by secreting additional
fluids into the intestinal tract. The resulting Use(s): It is an active cathartic, anticonvulsant,
increased bulk stimulates peristalsis. anesthetic, and reduces inflammation

• Poorly absorbed anions that are used as saline 5. Magnesium citrate

cathartics are biphosphate, phosphate, sulfate, and
tartrate.
Synonyms: Citrate of magnesia; purgative
• Soluble magnesium salts are cathartic due to the lemonade
poorly absorbed magnesium ion.
Non-Official Saline Cathartics
• The saline cathartics are water-soluble and are
taken with large amounts of water. This prevents
excessive loss of body fluids and reduces nausea
and vomiting if a too hypertonic solution should 1. Sodium sulfate or Glauber’s salt
reach the stomach
2. Potassium phosphate or dibasic potassium
Official Saline Cathartics phosphate, dipotassium hydrogen phosphate

1. Sodium biphosphate

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3. Potassium bitartrate or cream of tartar,
potassium acid tartrate, potassium hydrogen
tartrate

4. Calomel or mercurous chloride, mild mercury

chloride