Antacids and

Acid-Controlling Agents
Antacids
H2 Antagonists
Proton Pump Inhibitors
 Acid-Related Pathophysiology
The stomach secretes:
Hydrochloric acid (HCl)
Bicarbonate
Pepsinogen
Intrinsic factor
Mucus
Prostaglandins
 Glands of the Stomach
Cardiac
Pyloric
Gastric*

*The gastric glands are the largest in

number
 Cells of the Gastric Gland
Parietal
Chief
Mucoid
 Cells of the Gastric Gland
Parietal Cells
Produce and secrete HCl
Primary site of action for many acid-
controller drugs
 Cells of the Gastric Gland
Chief Cells
Secrete pepsinogen, a proenzyme
Pepsinogen becomes PEPSIN when
activated by exposure to acid
Pepsin breaks down proteins (proteolytic)
 Cells of the Gastric Gland
Mucoid Cells
Mucus-secreting cells (surface epithelial
cells)
Provide a protective mucous coat
Protects against self-digestion by HCl
 Hydrochloric Acid
Secreted by the parietal cells
Maintains stomach at a pH of 1 to 4
Secretion stimulated by:
– Large, fatty meals
– Excessive amounts of alcohol
– Emotional stress
 Acid-Related Diseases
Caused by imbalance of the three cells
of the gastric gland and their secretions
Most common: Hyperacidity
Most harmful: Peptic ulcer disease
(PUD)
Lay terms for overproduction of HCl by
the parietal cells: indigestion, sour
stomach, heartburn, acid stomach
Instructors may want to use
EIC Image #123:

Parietal Cell Stimulation and

Secretion
Antacids: Mechanism of Action
Promote the gastric mucosal defense
mechanisms
Secretion of:
– Mucus: Protective barrier against HCl
– Bicarbonate: Helps buffer acidic
properties of HCl
– Prostaglandins: Prevent activation of
proton pump
Antacids: Mechanism of Action
Antacids DO NOT prevent the
overproduction of acid.
Antacids DO neutralize the acid once
it’s in the stomach.
 Antacids: Drug Effects
Reduction of pain associated with
acid-related disorders
Raising gastric pH from 1.3 to 1.6
neutralizes 50% of the gastric acid.
Raising gastric pH 1 point (1.3 to 2.3)
neutralizes 90% of the gastric acid.
 Antacids
OTC formulations available as:
Capsules and tablets Powders
Chewable tablets Suspensions
Effervescent granules and tablets
 Antacids
Aluminum salts
Magnesium salts
Calcium salts
Sodium bicarbonate

Used alone or in combination

 Antacids
Aluminum Salts
Forms: carbonate, hydroxide, phosphate
Have constipating effects
Often used with magnesium to counteract
constipation
Example: aluminum carbonate (Basaljel)
 Antacids
Magnesium Salts
Forms: carbonate, hydroxide, oxide, trisilicate
Commonly cause a laxative effect
Usually used with other agents to counteract
this effect
Dangerous when used with renal failure—the
failing kidney cannot excrete extra
magnesium, resulting in accumulation
Examples: magnesium hydroxide (MOM);
combination products such as Maalox, Mylanta
(aluminum and magnesium)
 Antacids
Calcium Salts
Forms: many, but carbonate is most common
May cause constipation
Their use may result in kidney stones
Long duration of acid action may cause
increased gastric acid secretion (hyperacidity
rebound)
Often advertised as an extra source of dietary
calcium
Example: Tums (calcium carbonate)
 Antacids
Sodium Bicarbonate
Highly soluble
Quick onset, but short duration
May cause metabolic alkalosis
Sodium content may cause problems in
patients with CHF, hypertension, or renal
insufficiency
 Antacids and Antiflatulents
Antiflatulents: used to relieve the
painful symptoms associated with
gas
Several agents are used to bind or
alter intestinal gas, and are often
added to antacid combination
products.
 Antacids and Antiflatulents
OTC Antiflatulents
activated charcoal
simethicone
– Alters elasticity of mucus-coated
bubbles, causing them to break.
– Used often, but there are limited data to
support effectiveness.
 Antacids: Side Effects
Minimal, and depend on the compound
used
Aluminum and calcium
– Constipation
Magnesium
– Diarrhea
Calcium carbonate
– Produces gas and belching; often
combined with simethicone
 Antacids: Drug Interactions
Chelation
– Chemical binding, or inactivation, of
another drug
Chemical inactivation
– Produces insoluble complexes
Result: reduced drug absorption
 Antacids: Drug Interactions
Increased stomach pH
Increased absorption of basic drugs
Decreased absorption of acidic drugs
Increased urinary pH
Increased excretion of acidic drugs
Decreased excretion of basic drugs
Antacids: Nursing Implications
Assess for allergies and preexisting
conditions that may restrict the use
of antacids, such as:
Fluid imbalances Renal
disease CHF
Pregnancy GI obstruction
Patients with CHF or hypertension
should use low-sodium antacids such
as Riopan, Maalox, or Mylanta II.
Antacids: Nursing Implications
Use with caution with other
medications due to the many drug
interactions.
Most medications should be given 1 to
2 hours after giving an antacid.
Antacids may cause premature
dissolving of enteric-coated
medications, resulting in stomach
upset.
Antacids: Nursing Implications
Be sure that chewable tablets are
chewed thoroughly, and liquid forms
are shaken well before giving.
Administer with at least 8 ounces of
water to enhance absorption (except
for the “rapid dissolve” forms).
Caffeine, alcohol, harsh spices, and
black pepper may aggravate the
underlying GI condition.
Antacids: Nursing Implications
Monitor for side effects:
– Nausea, vomiting, abdominal pain,
diarrhea
– With calcium-containing products:
constipation, acid rebound
Monitor for therapeutic response:
– Notify heath care provider if symptoms
are not relieved.
Histamine Type 2 (H2)
Antagonists
 H2 Antagonists
Reduce acid secretion
All available OTC
Most popular drugs for treatment of
acid-related disorders
cimetidine (Tagamet)
famotidine (Pepcid)
nizatidine (Axid) ranitidine (Zantac)
 H2 Antagonists:
Mechanism of Action
Block histamine (H2) at the
receptors of acid-producing
parietal cells
Production of hydrogen ions is
reduced, resulting in decreased
production of HCl
 H2 Antagonists: Drug Effect
Suppressed acid secretion in the
stomach
H2 Antagonists: Therapeutic
Uses
Shown to be effective for:
Gastric ulcer Gastroesophageal reflux
disease (GERD)
Upper GI Duodenal ulcer (with or
bleeding without H. pylori)
May be effective for:
– Stress ulcers Peptic esophagitis
– Prevention and management of allergic
conditions, when used with H1 blockers
H2 Antagonists: Side Effects
Overall, less than 3% incidence of
side effects
Cimetidine may induce impotence
and gynecomastia
 H2 Antagonists: Drug
Interactions
Cimetidine
– Binds with P-450 microsomal oxidase
system in the liver, resulting in inhibited
oxidation of many drugs and increased
drug levels
– All H2 antagonists may inhibit the
absorption of drugs that require an
acidic GI environment for absorption.
 H2 Antagonists: Drug
Interactions
SMOKING has been shown to
decrease the
effectiveness of H2 blockers
 H2 Antagonists: Nursing
Implications
Assess for allergies and impaired
renal or liver function.
Use with caution in patients who are
confused, disoriented, or elderly.
Take 1 hour before or after antacids.
Ranitidine may be given
intravenously; follow administration
guidelines.
Proton Pump Inhibitors
 Proton Pump Inhibitors
The parietal cells release positive
hydrogen ions (protons) during HCl
production.
This process is called the “proton
pump.”
H2 blockers and antihistamines do
not stop the action of this pump.
 Proton Pump Inhibitors:
Mechanism of Action
Irreversibly bind to H+/K+ ATPase
enzyme.
This bond prevents the movement of hydrogen
ions from the parietal cell into the stomach.
Result: Achlorhydria—ALL gastric acid
secretion
is blocked.
– In order to return to normal acid secretion,
the parietal cell must synthesize new H+/K+
ATPase.
Proton Pump Inhibitors: Drug
Effect
Total inhibition of gastric acid
secretion
lansoprazole (Prevacid) omeprazole
(Prilosec)
rabeprazole (Aciphex) pantoprazole
(Protonix)
esomeprazole (Nexium)
 Proton Pump Inhibitors:
Therapeutic Uses
GERD maintenance therapy
Erosive esophagitis
Short-term treatment of active
duodenal and benign gastric ulcers
Zollinger-Ellison syndrome
Treatment of H. pylori-induced ulcers
Proton Pump Inhibitors: Side
Effects
Safe for short-term therapy
Incidence low and uncommon
 Proton Pump Inhibitors:
Nursing Implications
Assess for allergies and history of liver
disease
Pantoprazole is the only proton pump
inhibitor available for parenteral
administration, and can be used for
patients who are unable to take oral
medications
May increase serum levels of diazepam,
phenytoin, and cause increased chance
for bleeding with warfarin
 Proton Pump Inhibitors:
Nursing Implications
Instruct the patient taking
omeprazole:
It should be taken before meals.
The capsule should be swallowed whole,
not crushed, opened or chewed.
It may be given with antacids.
Emphasize that the treatment will be
short-term.
 Other Drugs
sucralfate (Carafate)
misoprostol (Cytotec)
 Sucralfate (Carafate)
Cytoprotective agent
Used for stress ulcers, erosions, PUD
Attracted to and binds to the base of
ulcers and erosions, forming a
protective barrier over these areas
Protects these areas from pepsin,
which normally breaks down proteins
(making ulcers worse)
 Sucralfate (Carafate)
Little absorption from the gut
May cause constipation, nausea, and dry
mouth
May impair absorption of other drugs,
especially tetracycline
Binds with phosphate; may be used in
chronic renal failure to reduce
phosphate levels
Do not administer with other medications
 misoprostol (Cytotec)
Synthetic prostaglandin analogue
Prostaglandins have cytoprotective
activity:
– Protect gastric mucosa from injury by
enhancing local production of mucus or
bicarbonate
– Promote local cell regeneration
– Help to maintain mucosal blood flow
 misoprostol (Cytotec)
Used for prevention of NSAID-
induced gastric ulcers
Doses that are therapeutic enough to
treat duodenal ulcers often produce
abdominal cramps, diarrhea
 THANK YOU

WITHOUT FAITH , IT IS
IMPOSSIBLE TO PLEASE GOD
ROMEL Y. FELARCA,MD,DFM.