Subject: Pharm Chem -1 LEC (Chemistry & Pharmacy of Inorganic Medicinals)

Year& Section: Pre-Final Lecture for BS PH- 3A, 3B, 3C, 3D & 3E Revised: 082015
Schedule: 3A = 7-8 am, MWF; 3C = 8-9 Am, TThS ; 3E = 11:00-12:00 Noon MWF
3B = 7-8am, TThS; 3D = 9-10 Am TThS

PREFINAL Unit VI. Gastrointestinal Agents 4 Hours

1. Acidifying agents 3. Protectives and Adsorbents
2. Antacids 4. Saline Cathartics

Unit VII. Topical Agents 3 Hours

1. Protective Agents 2. Antimicrobials 3. Astringents

Unit VI. GASTROINTESTINAL AGENTS

I. ACIDIFYING AGENTS aka. D_ _ _ _ _ _ _ _ s (2x);

aka A _ _ _ _ _ _ _ _ s.
These are substances that promotes acidic environment.
aka. A _ _ _ _ _ _ _ _ s In Vitro used (Test Tube Expts.)
These are Agents that AID or facilitate Digestive Process.
aka D_ _ _ _ _ _ _ _ s (2x) In Vivo Used (Internal)
Representative Examples include : Dilute HCl & Citammic Acid HCl
Agents intended to relieve Stomach Trouble.

DILUTE HCl Utilized to relieve the GI Symptoms caused by ACHLORHYDRIA.

Usual dose is 5 mL diluted to 200 mL.

II. ANTACIDS Aka: A _ _ _ _ _ _ _ _ s

These are products used for Altering Gastric pH.

INDICATIONS: 1. To neutralize excess HCl n the Stomach which may causing PAIN &
Possible Ulceration: (PUD: G, D E or GERD)
2. To Inactivate proteolytic Enzyme PEPSIN.

PARADIGM: PEPSIN Pepsinogen HCl Formation

ANTACID THERAPY ANTACIDS are alkaline bases used to neutralize the excess
gastric HCl associated with Gastritis and Peptic Ulcer.
Requirement for ALL: Must raise the pH of the Stomach to 3.5 or more in 10 minutes

CRITERIA for an IDEAL ANTACID:

1. Should NOT be absorbable or cause Systemic Alkalosis.

2. Should NOT be a LAXATIVE or Cause Constipation.
3. Should exert the effect rapidly and over a long period of time.
4. The 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.
ANTACID DRUG LISTINGS:

I. Sodium Containing Antacids:

Sodium bicarbonate (BAKING SODA):
Highly Water Soluble with rapid Onset of Action but relatively Short Duration.
Causes Sharp Increase In gastric pH.
Causes BELCHING & FLATULENCE due to evolution of CO to produce Sparkling
Flavor in Preparations that will have saline taste.

II. Aluminum Containing Antacids:

A. ALUMINUM HYDROXIDE Types: Al (OH)3 Gel and Dried Al(OH)3

1. Alumiunum hydroxide GEL BN: CREAMALIN Gel; ALU-CAP; ALUDROX;

PEPSAMAR; ALHYDROGEL used to treat Hyperchlorhydria and Peptic Ulcer,
Intestinal Toxemia. It Absorbs HCl, Toxins, gases and Bacteria. It does NOT produce
Systemic Alkalosis.
This compound is also used to control phosphate (phosphorus) levels in the
blood of people suffering from kidney failure.

ALHYDROGEL An aluminium hydroxide adjuvant, since it absorbs protein well, it

also functions to stabilize vaccines by preventing the proteins in the vaccine from
Precipitating or sticking to the walls of the container during storage.

2. DRIED Aluminum Hydroxide Syn.: Aluminium hydroxide Powder; Activated Alumina

a dehydrated Aluminium hydroxide gel, using water-miscible non-aqueous solvents
like ethanol) to form an amorphous aluminium hydroxide powder, which is readily soluble
in acids. Aluminium hydroxide powder which has been heated to an elevated temperature
under carefully controlled conditions is known as Activated Alumina and is used as a
desiccant, an adsorbent, in gas purification, as a Claus catalyst support, water
purification, and an adsorbent for the catalyst during the manufacture of polyethylene by
the Sclairtech process.

B. ALUMINUM PHOSPHATE Its ACID-Conserving Ability is based on the

release of Phosphate anion. In medicine an aluminium phosphate sol is used as
adsorbent for toxoid and in the dried form, which contains hydrated AlPO.

III. Calcium Containing Antacids are dependent upon their basic properties;
unlike Aluminum Antacids, which depends on Amphoteric Properties. Calcium Antacids
tend to be constipating and are usually found in combination with magnesium.

1. Precipitated Calcium Carbonate (Syn: Precipitated Chalk) this is a Popular

Antacid because of its Fast Action. Its Action is limited by the amount of salt that will
go into solution.

2. Calcium carbonate Chewable 500 mg Tablet (BN: TUMS)

 3. TRIBASIC Calcium phosphate
Synonyms: Precipitated Calcium Phosphate; Tertiary Calcium Phosphate;
Calcium Phosphate
It is used as an antacid in the treatment of Hyperacidity.
MOA: The Production of 1 and 2 Phosphate, diminished the H concentration of
the gastric HCl.
Its advantage is it does NOT Produce gas that may cause flatulence and does
NOT alkalinize the system.

IV. Magnesium Containing Antacids: Mg++ causes laxative action. They

are found in combination with Aluminum and calcium Antacids to equalize the
Constipative and Laxative Action.

A. Magnesium carbonate
Synonyms: Carbonate of Magnesia; Heavy Magnesium Carbonate;
Kinds: Light Magnesium carbonate; and Dense/Heavy Magnesium carbonate
Used: ANTACIDS
MOA: OH and CO3 reacting with the gastric pH.

B. Magnesium hydroxide
Synonym: Milk of Magnesia
Use: as an ANTACID; LAXATIVE (In High Doses)
MOA: Formation of magnesium chloride in the Stomach which exerts a Salt Action
in the Intestinal Tract causing a Mild Laxative Action.

C. Magnesium oxide:
Synonym: MAGNESIA
Kinds: Light Magnesium Oxide and Heavy Magnesium Oxide
Use/s: It is used as a Laxative, Diuretic, Antacid and Antidote in Arsenic Poisoning.
NOTE: To prevent the formation of a gelatinous mass, it should be administered in
about 20 times its weight of water. The Magnesia should be added to water and NOT
reversed in order to avoid the formation of Hard LUMP.

D. Magnesium trisilicate:
Use: As a Gastric Antacid for Peptic Ulcer.
MOA: The colloidal silicic acid or hydrous silica, which is formed in the reaction, have
adsorptive powers and could protect the ulcer from acid and peptic attack.

E. Magnesium phosphate
Synonym: Tertiary Magnesium Phosphate

V. COMBINATION PRODUCTS MIXED Antacid Preparations

RATIONALE:
1. To balance the Constipative effect of Calcium and aluminum with the Laxative Effect
of Magnesium,
2. A mixture of an antacid with rapid onset of action and one with a supposedly longer
duration of action.
 Representative Examples:

A. Aluminum hydroxide Gel Magnesium hydroxide Combinations (MAALOX,

MELMAG)
B. Aluminum hydroxide Gel Magnesium trisilicate Combinations (GELUSIL)
C. MAGALDRATE (Hydrated Magnesium Aluminate)
D.
E. HYDROTALCITE (Aluminum-Magnesium Hydroxides Complex)
F. Simethicone Containing Antacids (KREMIL-S)
G. Dimethicone Containing Antacids (MAALOX Plus; SIMECO)

III. PROTECTIVES & ADSORBENTS:

These group of GI Agents are commonly used for the treatment of Mild Diarrhea.
MOA: Adsorbed Toxins, Bacteria & Viruses, while providing a Protective Coating on the
Intestinal Mucosa.
Examples: Insoluble Bismuth Salts (subgallate & subnitrate), Kaolin, Pectin, Attapulgite.

DIARRHEA is a Symptom and NOT a Disease. It results when some factor impair
digestion and/or absorption, thereby increasing the bulk of the Intestinal Tract, which then
stimulates peristalsis, propelling the Intestinal contents to the Anus.
DIARRHEA is a serious condition, particularly for the very young or elderly patients,
because the Loss of Fluids and electrolytes can quickly lead to dehydration and
Electrolyte Imbalance.

Most products for the treatment of Diarrhea will consist of:

a. ADSORPTIVE-PROTECTIVE Agents supposedly adsorb Toxins, Bacteria, and
Viruses along with providing a Protective Coating of the Intestinal Mucosa. Ex.
KAOLIN, ATTAPULGITE, etc.
b. ANTIBACTERIAL Agents these are only Effective if there is an actual infection
caused by Microorganisms. Ex. ANTIBIOTICS.
c. ANTIDIARRHEAL Agents Should act directly on the smooth Muscles of the GUT
to produce a spasm like effect, which decreases Peristalsis and Increases
Segmentation. Aka: Antiperistaltic Agent, that include Loperamide.

ANTIDIARRHEALS are considered as PROBLEM DRUGS: if you are chronic user, it

could stop the Peristalsis in the Intestines.

REPRESENTATIVE EXAMPLES: (Ph 3D)

I. BISMUTH-Containing Products:
MOA: The Soluble Bismuth Cation supposedly exerts a Mild Astringent and Antiseptic
Action. Intestinal Hydrogen sulfide gas acts upon the bismuth salts to form Bismuth
sulfate; hence, the black stools resulting from the oral administration of Bismuth-
containing Preparations.

A. BISMUTH subnitrate
Syn: Basic Bismuth nitrate; White Bismuth, Spanish White
Use/s: Effective Non-Irritant Intestinal Antiseptic for Gastric Ulcers, Inflammations and
common remedy for Diarrhea.

B. BISMUTH subcarbonate
Syn: Basic Bismuth carbonate
 Use/s: Protective and Antacid Effect in Inflammations of the Stomach and Bowels,
Radiopaque Contrast Medium, Astringent, and Adsorbent in Diarrhea.

C. MILK of BISMUTH also as an ANTACID

Syn: Bismuth Magma, Bismuth Cream
Use/s: Milk of Bismuth Contains Bismuth hydroxide and Bismuth subcarbonate in
suspension in water.
It is made by converting Bismuth subnitrate to Bismuth nitrate by the addition
of Nitric acid. Then by the Treatment with ammonium carbonate and Ammonia
solution, Bismuth subnitrate is converted to bismuth hydroxide and subcarbonate.
It is used as an Astringent and Antacid.

II. KAOLIN
Syn: Porcelain Clay, China Clay, Bolus Alba
Use/s: It is found together with the vegetables carbohydrate PECTIN (Kaopectate) and
employed as a protective and adsorbent in Diarrheal Disorders.

III. ACTIVATED CHARCOAL

Use/s: It is classified as a Universal Antidote in Poisoning. It is employed in the Treatment
of Diarrhea.
(Ph 3E )

IV. SALINE CATHARTICS aka: P_ _ _ _ _ _ _ _S

Agents that quicken and increase Evacuation of the BOWEL.
LAXATIVES Are MILD CATHARTICS.

USE/S: 1. To ease defecation in patients with Painful Hemorrhoids or Other

Rectal Disorders.
2. To avoid potentially hazardous rises in Blood Pressure during Defecation in
patients with Hypertension, cerebral or Arterial Diseases.
3. To relieve Acute Constipation.
4. To remove solid Material from the Intestinal tract prior to certain
Roentgenographic Studies.