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PharChemLec Chapter V | Reviewer | Shaira Ysabel Orqueta | 1A-Pharmacy

CHAPTER V- GASTROINTESTINAL AGENTS


Inorganic agents used to treat gastrointestinal disorders includes:
1. Products for altering gastric pH
2. Protectives for intestinal inflammation
3. Adbsorbents for intestinal toxins
4. Cathartics or laxatives for constipation
- do not require a prescription; places the responsibility directly on the pharmacist as to who should purchase these
items.

ANTACIDS - alkaline bases used to neutralize gastric HCl associated with gastritis (general inflammation of the
gastric mucosa) and peptic ulcers (specified circumscribed erosion); to inactivate the proteolytic enzyme, pepsin
Stomach pH (1 when empty; 7 when food is present)
Low acid pH is due to the presence of endogenous HCl which is always present
When hyperacidity develops, results can range from gastritis to peptic ulcer.
o Esophageal ulcer- in the lower end of the esophagus
-occurs when the esophageal sphincter is defective
-causes heartburn (gastric acid entering the esophagus either during a belch or
upon lying in bed); obtain relief by sleeping on a bed elevated at the head to reduce the
flow of gastric fluid from stomach to esophagus
o Gastric ulcer- in the stomach; causes malignancy and hemorrhage
o Duodenal ulcer- in the duodenum; causes perforation
A tense individual who contains his emotions tends to have a greater incidence of peptic ulcer than does a
person who can release his tension
Treatment depends on severity and location of an ulcer
o Diet
o Antacid and/or anti-cholinergic therapy
o Complete bed test
o Surgery
o Removal of an emotional stress situation
While no antacid is ideal, there have been certain criteria that have been developed
o The antacid should not be absorbable or cause systemic alkalosis
o The antacid should not be a laxative or cause constipation
o The antacid should exert the effect rapidly and over a long period of time
o The reaction of the antacid with gastric HCl should not cause a large evolution of gas.
o The antacid should buffer in the pH 4-6 range
o The antacid should probably inhibit pepsin

Sodium bicarbonate as an antacid
- highly water soluble
-rapid onset of action
-relatively short duration
-can cause a sharp increase in gastric pH up to or
above pH 7
-can cause belching and flatulence
-found in many effervescent antacid preparations
-main function is to react with an acid (citric, tartaric,
etc.) with the evolution of CO2 which results to a
sparkling flavor in preparations instead of a flat
saline taste

Aluminum hydroxide
- has two physical forms
Aluminum hydroxide Gel
- white viscous suspension
-small amounts of clear liquid may separate
on standing
-permitted to contain aromatic (peppermint
oil) and sweetening substances (sucrose,
glycerin, saccharin, etc.)
-nmt 0.5% of preservative is allowed (sodium
benzoate, benzoic acid, methyl paraben, etc.)
- pH between 5.5 and 8.0
Dried Aluminum hydroxide Gel
- White colorless, tasteless, odorless,
amorphous powder
- insoluble in water and alcohol
- soluble in dilute mineral acids and soln
of fixed alkali hydroxide
PharChemLec Chapter V | Reviewer | Shaira Ysabel Orqueta | 1A-Pharmacy
- also official as Dried Aluminum
hydroxide Gel and Tablets, a convenient
dosage form.
- both forms are assayed in terms of their aluminum
oxide (Al2O3) content and their acid-consuming
capacity
-has very fine colloidal particle that would exhibit a
large SA and thus great adsorptive powers upon w/c
its therapeutic value depends
- ideal buffers in the pH 3-5 region due to their
amphoteric characters
-a problem is that of a loss of antacid properties on
aging
- because of the water soluble astringent salt AlCl3,
the product of the reaction with HCl, Al(OH)2 gel can
cause constipation and occasionally nausea and
vomiting

Uses:
-gastric antacid
-treatment of hyperchlorhydria and peptic ulcer
-intestinal toxemia
-mechanism of action is attributed to its capability of
adsorbing HCl, toxin, gases and bacteria
-adsorbs pepsin
-interferes with the adsorption of other drugs

Calcium-containing Antacids
-dependent upon their basic properties and not on an amphoteric effect
-those used in medicine are poorly insoluble salts which can only go into the soln if there is acid present to consume
the small amt of solubilized salt already present in the soln
-raise the stomach pH to nearly 7
-tend to be constipating
-usually found in combination with magnesium antacids

Calcium carbonate (Precipitated Chalk)
-fine, white, odorless, tasteless, microcrystalline
powder
-stable in air
-practically insoluble in water
-solubility is increased by the presence of nay
ammonium salt or CO2
- presence of any alkali reduces solubility
-insoluble in alcohol
-dissolves with effervescence in diluted acetic acid,
diluted HCl and diluted nitric acid
-fast action
-action is limited by the amt of salt that will go into
soln
-as gastric HCl consumes the solubilized calcium
carbonate, more goes into soln. this continues until
the acid or the calcium carbonate is consumed
-found in combination with the magnesium antacids

Uses:
-one of the most popular antacids
-Calcium carbonate Lozenges and oral susp

Tribasic Calcium Phosphate (Precipitated Calcium
Phosphate, Tertiary Calcium Phosphate, Calcium
Phosphate)
-variable mixture of calcium phosphate having the
approx composition 10CaO.3P2O5.H2O
-after ignition at 800
o
for 30 mins, it contains an amt of
phosphate equivalent to nlt 90% of tribasic calcium
phosphate, Ca3(PO4)2
-found abundantly in nature as phosphorite and
phosphate rock and apatite Ca3(PO4)2.CaF2
-white, odorless, tasteless powder
-insoluble in water and alcohol
-dissolves readily in diluted HCl and nitric acid

Uses:
-antacid in treatment of hyperacidity
the production of primary and secondary
phosphate diminishes the hydrogen ion concentration
of the gastric HCl
-advantage over sodium bicarbonate or other
carbonates
No gas is produced that may cause
flatulence and does not alkalinize the system
-source of calcium for the system but because of its
insolubility, very little calcium is absorbed, making it
invaluable in acute calcium deficiency


Magnesium-containing Antacids
-except magnesium trisilicate, they all function in the same manner
-poorly soluble salts w/c only go into soln as acid consumes the small amt of anion already in the soln
-as the pH in the stomach approaches neutrality, the rate of dissolution of the Mg salt slows down and stops at
neutrality.
PharChemLec Chapter V | Reviewer | Shaira Ysabel Orqueta | 1A-Pharmacy
-it is the anion rather than the Mg cation that confers the antacid properties; the Mg cation causes this group to be
laxatives
-usually found in combination with aluminum and calcium antacids in an attempt to equalize the constipative and
laxative actions

Magnesium carbonate [Mg(CO3)4.Mg(OH)2.5H2O]
-Carbonate of Magnesia, Heavy Magnesium
Carbonate
-white, bulky, odorless powder
-slightly earthly taste
-often occurs in friable masses
-nearly insol in water to w/c it imparts a slightly
alkaline reactions (due to a slight dissociation of the
Mg(OH)2)
-insoluble in alcohol
-dissolves with effervescence in diluted acids
-antacid properties are due to the hydroxide and
carbonate ions reacting with the gastric HCl
-due to very limited solubility, it dissolves only as
hydroxide and carbonate are being consumed

Magnesium hydroxide
-white, bulky powder
-practically insol in water and alcohol
-dissolves in acids

Uses:
-efficient antacid due to basic character
- laxative in high doses
Due to the formation of magnesium chloride
in the stomach w/c exerts a salt action in the
intestinal tract, causing a mild laxative action

Milk of Magnesia
-susp of Mg(OH)2
- nlt 7% and mt 8.5% Mg(OH)2
-to minimize the interaction of glass containers and
Mg(OH)2, small amt of citric acid maybe added
-suitable flavoring maybe added
-very popular antacid and laxative

Magnesium Oxide (Magnesia)
-Light Magnesium Oxide and Heavy Magnesium
Oxide
Identical in chemical composition and in
purity; differs in density (Light 5g/40ml to 5g/50ml;
Heavy 5g/10ml to 5g/20ml)
-white, odorless powders
-nearly insol in water and alcohol
-dissolves in dilute acids
-absorb carbon dioxide and moisture upon exposure
to air
-Light variety hydrolyzes Mg(OH)2 more easily than
heavy variety
Uses:
-laxative, diuretic, antacid
In order to prevent formation of gelatinous
mass, it should be administered in about 29x its wt in
water. Magnesia should be added to water and not
the reversed order to avoid formation of hard lump
-arsenic antidote

Magnesium Trisilicate (2MgO.3SiO2.xH2O)
-nlt 20% of MgO and nmt 45% of silicon dioxide
-fine, white, odorless, tasteless powder, free from
grittiness
-insol in water and alcohol
-readily decomposed by mineral acids
-assayed in terms of SiO2 and MgOand must have
definite MgO/ SiO2 ratio
-As amt of increases SiO2 with respect to MgO, there
is loss in antacid capability

Uses:
-gastric antacid especially valuable in peptic ulcer
-colloidal silica acid and hydrous silica w/c is formed
in the reaction has adsorptive powers and could
protect the ulcer from further acid and peptic attack
and possible adsorbs the pepsin

Magnesium Phosphate [Mg3 (PO4)2.5H2O]
-Tertiary Magnesium Phosphate
-white odorless and tasteless powder
-readily soluble in diluted mineral acids
-almost insoluble in water
-antacid


Combination Acid Preparation
-an attempt to balance the constipative effect of calcium and aluminum with the laxative effect of magnesium
-a mixture of an antacid with rapid onset of action and one with a supposedly longer duration of action

a) Aluminum Hydroxide Gel- Magnesium Hydroxide
Conbination: Aludrox, WinGel, Maalox and Cremalin
PharChemLec Chapter V | Reviewer | Shaira Ysabel Orqueta | 1A-Pharmacy
b) Aluminum Hydroxide Gel- Magnesium Trisilicate
Combination: Gelusil, Tricreamalate, Triosgel
c) Magaldrate- combination of aluminum hydroxide and magnesium hydroxide (Riopan)
d) Simethicone- defoaming agent (for people with gastric hyperacidity who complain of being gassy)
- Di-Gel, Mylanta
e) Alginic acid- contains sodium carbonate
- To provide a symptomatic relief of reflux esophagitis
- Gavison, Foamtab

Protective and Adsorbents
-treatment of mild diarrhea (consist of an adsorptive-protective, an antidiarrheal agent and possibly an antibacterial
agent)
Diarrhea- results when some factors impair digestion and or adsorption, thereby increasing the bulk of the
intestinal tract which stimulates peristalsis, propelling the intestinal contents to the anus
- Loss of fluids and electrolytes that can lead to dehydration and electrolyte imbalance
Acute diarrhea- caused by bacterial toxins, chemical poisons, drugs, allergy and disease
- May cause tissue damage or irritation and causing electrolytes to flow from body fluids into the intestinal
tract
Chronic diarrhea- can result from GO surgery, carcinomas, chronic inflammatory conditions and various
adsorptive defects
-ideal antidiarrheal should act directly on the smooth muscles of the gut to produce a spasm-like effect w/c decreases
peristalsis and increase segmentation
- antibacterials are only effective if there is an actual infection caused by the microorganism
-adsorbent-protective supposedly adsorb toxins, bacteria and viruses along w/ providing a protective coating of the
intestinal mucosa

Bismuth-containing products
-antidiarrheal agent
-water insoluble but a small amt go into the soln
-soluble bismuth cations exerts a mild astringent and antiseptic action
-intestinal hydrogen sulfide acts upon the bismuth salts to form bismuth sulfide hence the black stool resulting from
oral administration of bismuth-containing preparations

Bismuth subnitrate [Bi(OH)2(NO3)4.BiO(OH)]
-Basic Bismuth Nitrate, White Bismuth
-white- slightly hygroscopic powder
-acid reaction using blue litmus paper
-practically insoluble in alcohol
-readily dissolved in HCl
-assayed in terms of bismuth trioxide
-incompatible with tragacanth because it precipitates
as a hard mass in the presence of the salt (maybe
overcome by adding sodium biphosphate or trisodium
phosphate)

Uses:
-effective non-irritant intestinal antiseptic
-lessens gastric secretion
-reduce acidity
-treatment of gastric ulcers and inflammation
-remedy against diarrhea



Bismuth subcarbonate [BiO2(CO3)2.H2O]
-Basic Bismuth Carbonate
-white or pale yellowish white odorless tasteless
powder
-stable in air but slowly affected by light
-practically in sol in water
-dissolves in HCl w/ effervescence
-assayed in terms of its bismuth trioxide content

Uses:
-protective and antacid effect in inflammations of the
stomach and bowels
-for rendering the alimentary canal opaque to x-ray in
large doses (60g)
-astringent and adsorbent
-treatment of diarrhea and dysentery





PharChemLec Chapter V | Reviewer | Shaira Ysabel Orqueta | 1A-Pharmacy
Milk of Bismuth (Bismuth Magma, Bismuth Cream)
- bismuth hydroxide and bismuth subcarbonate in
susp in water
-made by converting bismuth subnitrate to bismuth
nitrate by adding nitric acid
-then by the treatment of ammonium carbonate and
ammonia solution, bismuth nitrate is converted to
bismuth hydroxide and subcarbonate

Uses:
-astringent and antacid

Kaolin (Porcelain Clay, China Clay, Bolus Alba)
-native hydrated aluminum silicate, powdered and
freed from gritty particles by elutriation
-20.9% of aluminum with an approx formula
Al2O3.2SiO2.2H2O formed by weathering of feldspar
KalSi3O8
-soft yellowish white or whitish powder or in lumps
-insol in water and in cold dilute acids and in solns of
alkali hydroxides
-earthly and clay-like taste
-assumes a darker color and develops a marked clay-
like color when moistened
-found together w/ the vegetable carbohydrate
(Kaopectate, Kao-con)

Uses:
-protective and adsorbent in diarrheal disorders
-to interfere materially w/ the intestinal absorption of
lincomycin

Activated Charcoal
-adsorbent in the treatment of diarrhea
-antidote in certain types of poisoning


Saline Cathartics
-quicken and increase evacuation from the bowels (cathartics)
-water insoluble
-taken with large amts of water (prevents excessive loss of body fluids and reduces nausea and vomiting if a too
hypertonic soln should reach the stomach)
-laxatives are mild cathartics
-can be purchased w/o prescription
-widely abused and often overpromoted

(1972 AMA Drug Evaluation) criteria when cathartics are properly used:
1. To ease defecation in patients w/ painful hemorrhoids or other rectal disorders
2. To avoid potentially hazardous rises in BP during defecation in patients with HTN, 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 as prolonged use may lead to loss of spontaneous bowel
rhythm. May cause the patient to be laxative-dependent aka laxative habit

4 Types of Laxatives
1. Stimulant Laxatives- local irritation on the intestinal tract; increases peristaltic activity
2. Bulk-forming Laxatives- made from cellulose and other non-digestible polysaccharides w/c swell when wet
and with the increased bulk stimulates peristalsis
3. Emollient Laxatives- act either as lubricants facilitating the passage of compacted fecal material or as stool
softeners. (eg. Mineral Oil)
4. Saline Cathartics- act by increasing the osmotic load of the GIT
-salts of poorly absorbable anions and sometimes cations
-relieves the hypertonicity of the gut by secreting additional fluids into the intestinal tract
-the resolution increased bulk stimulates peristalsis
-Poorly absorbed anions that are used as saline cathartics
Biphosphate
Phosphate
Sulfate
Tartrate
-soluble magnesium salts are cathartic due to the poorly absorbed Mg ion



PharChemLec Chapter V | Reviewer | Shaira Ysabel Orqueta | 1A-Pharmacy
Monobasic Sodium Phosphate [NaH2PO4.H2O]
-Sodium Dihydrogen Phosphate, Sodium Acid
Phosphate, Primary Sodium Phosphate, Sodium
Biphosphate
-colorless crystals or white cryst. Powder
-odorless
-slightly deliquescent
-acid to litmus
-effervescence w/ sodium carbonate
-acidic properties due to the acid dihydrogen
phosphate anion
-anhydrous and with 1 or 2 moles water of hydration

Uses:
-urinary acidifier
-cathartic
-to render the urine acidic in the case of cystitis with
hexamethylenetetramine (methenamine)
Decomposes into formaldehyde only in the
presence of acids

Dibasic Sodium Phosphate [Na2HPO4.7H2O]
-Disodium Hydrogen Phosphate, Secondary Sodium
Phosphate
-colorless or white granular salt
-effervesces in warm dry air
-alkaline to litmus and phenolphthalein (w/ pH of 9.5)
-freely soluble in water and very soluble in alcohol
-one, two, seven or twelve moles water of hydration
-poor intestinal permeability of the monohydrogen
phosphate ion

Uses: saline cathartic

Potassium Sodium Tartrate [KNaC4H4O6.4H2O]
-Rochelle Salt, Seignette Salt
-colorless crystals or white cryst. Powder
-cooling saline taste
-effloresces in warm dry air
-crystals are often coated with a white powder
-freely soluble in water and practically insol in alcohol

Uses:
-cathartic (ranging from mild laxative to the more
potent hydragogue depending on the dose)
-pharmaceutical necessity
-ingredient of Seidlitz Powder (as cathartic)
-effervescent preparation
-palatable product
-reagent in Fehlings solution officially called Alkaline
Cupric Tartrate
Chelate complexation
The concentration of the cupric is very little
and is not precipitated by the sodium hydroxide in the
reagent

Magnesium Sulfate [MgSO4.7H2O]
-Epsom salt, Bitter salt
-can be prepared by:
1. Treating the mineral magnesite (MgCO3) w/
hot dilute H2SO4
2. Dissolving the mineral kiersersite
MgSO4.H2O in water, heating then
concentrating the soln to crystallization
3. Heating by calcinations dolomite
MgCO3 .CaCO3 then treating with HCl and
evaporating to dryness. Dried mass is
dissolved in H2SO4, boiled and filtered.
Filtrate containing magnesium sulfate is
evaporated to crystallization
-small colorless crystals, usually needle-like
-cooling saline bitter taste
-effloresces in air
-neutral to litmus
-freely sol in boiling water and sparingly in alcohol

Uses:
-active cathartic operating with but little pain or
nausea and producing watery stools
-disagreeable bitter taste w/c can be lessened by
administrating soln in an ice-cold condition
-anticonvulsant (parenterally)
-anesthetic effect in sprains and bruises (applied
locally in saturated soln)
-antiphlogistic action

Magnesium Citrate (Citrate of Magnesia, Purgative
Lemonade)
- Made by reacting magnesium carbonate with citric
acid
- soln + flavoring agents +sodium or potassium
bicarbonate to react with the remaining citric acid
palatable, carbonated, lemon-flavored soln
-sterilized or pasteurized


NON-OFFICIAL SALINE CATHARTICS
- Sodium Sulfate- Glaubers salt
- Potassium Phosphate- Dibasic Potassium Phosphate, Dipotassium Hydrogen Phosphate, DKP
- Potassium Bitartrate- Cream of Tartar, Potassium Acid Tartrate, Potassium Hydrogen Tartrate
- Calomel- Mercurous Chloride, Mild Mercury Chloride