DRUGS AFFECTING GASTROINTESTINAL SECRETIONS

KEY TERMS:
Acid rebound – reflex response of the stomach to lower-than-normal acid levels
Antacids – neutralize stomach acid
Digestive enzymes - break down foods into usable nutrients
Gastrointestinal protectant – drug that coats any injured area in the stomach to prevent further injury from acid or pepsin
Histamine-2 (H2) Antagonist – drug that blocks the H2 receptor sites, used to decrease acid production in the stomach
Peptic ulcer – erosion of the lining of the stomach or duodenum
Prostaglandin – any one of the numerous tissue hormones that have local effects on various systems and organs of the body
Proton pump inhibitor – drug that blocks the H+, K+-ATPase enzyme system on the secretory surface of the gastric parietal cells
*DRUG LISTS ARE ON THE BOOK PAGE 2463.

DRUGS USED TO TREAT GASTROESOPHAGEAL REFLEX DISEASE (GERD) AND ULCER DISEASE
Histamine-2 (H2) Antagonists
Block the release of hydrochloric acid in
response to gastrin
DRUGS:
1. Cimetidine (Tagamet HB)
2. Ranitidine (Zantac)
3. Famotidine (Pepcid)
4. Nizatidine (Axid)
(Other drugs and their user indications
are in the book page 2473)
THERAPEUTIC ACTION &
INDICATIONS
- Block H2 receptors located on the parietal
cells.
- Blocking these receptors prevents about
70% of the hydrochloric acid release from
the parietal cells
- Also decrease pepsin production by the
chief cells
USED IN THE FOLLOWING:
1. Short-term treatment of active duodenal
ulcer or benign gastric ulcer.
2. Treatment of pathological hypersecretory
conditions such as Zollinger Ellison
Syndrome
3. Prophylaxis of stress-induced ulcers and
acute upper GI bleeding in critical patients
4. Treatment of erosive gastroesophageal
reflux
5. Relief of symptoms of heartburn, acid
indigestion, and sour stomach
Antacids Proton pump inhibitors Gastrointestinal protectants Prostaglandins
Interact with acids at the chemical level Suppress the secretion of Coat any injured area in the Inhibit the secretion of gastrin and
to neutralize them hydrochloric acid into the lumen of stomach to prevent further injury increase the secretion of mucous
the stomach from acid lining of the stomach providing a
buffer.
DRUGS:
1. Sodium Bicarbonate (Bell-ans)
2. Calcium carbonate (Oystercal, Tums,
and others)
3. Magnesium Salts (Milk of Magnesia
and others)
4. Aluminum salts (
Amphojel & others)
THERAPEUTIC ACTIONS &
INDICATIONS
- neutralize stomach acid by direct
chemical reaction
- recommended for the symptomatic
relief of upset stomach and associated
with hyperacidity, as well as
hyperacidity associated with peptic
ulcer, gastritis, peptic esophagitis,
gastric hyperacidity, and hiatal hernia.

PHARMACOKINETICS: PHARMACOKINETICS:
1. Cimetidine – oral and parenteral, 1st drug 1. Sodium Bicarbonate – oldest drug,
in the class to be developed, associated with ready in the form of baking soda,
antiandrogenic effects inc. gynecomastia and
galactorrhea
Peak: 1 – 1.5 hours
Metabolized : liver, slow the metabolism of
other drugs that use the same metabolizing
enzyme system
excreted: urine
Half-life: 2 hours
2. Ranitidine – oral and parenteral, more
potent, not associated with antiandrogenic
effects
Peak:5 – 15 mins (parenteral), 1-3 hours
(oral)
Duration: 8 – 12 hours
Half-life: 2 – 3 hours
3. Famotidine – oral and parenteral, similar
to ranitidine but much more potent than the
two.
Peak: 1 – 3 hours
Duration: 6 – 15 hours
Half-life: 2.5 to 3.5 hours
Approved in children for 1 – 16 years old
4. Nizatidine – oral, newest drug, similar to
ranitidine in effectiveness and adverse
Difference: eliminated by kidneys with no
1st pass metabolism in the liver.
- Drugs for patients with liver dysfunction
and for those who are taking metabolism an
is slowed hepatic activity of other 3 H2
Antagonists.
Peak: 0.5 – 3 hours
Half-life: 1 – 2 hours
powder, tablets, solutions, and
injectable for treating systemic acidosis
- widely distributed, orally
- Peak: 1-3 hours
- Excreted: urine, can cause
serious electrolyte imbalance in people
with renal impairment
2. Calcium Carbonate – precipitated
chalk, tablet and powder forms
- DRAWBACKS: constipation
and acid rebound
- ONSET: 3-5 mins, cause
calcium imbalance (systematically
absorbed)
- Metabolized: liver
- Excreted: urine & feces
- Half-life: 1-3 hours
3. Magnesium Salts – buffer acid in
the stomach but cause diarrhea
(sometimes laxatives)
- in the form of tablets,
chewable tablets, capsules, and liquid
forms
- EXCRETED: feces
- Lead to nerve damage and
even coma is absorbed, it is excreted in
urine
4. Aluminum salts – do not cause acid
rebound, but are effective in
neutralizing acid
- in the form of tablets,
capsules, suspensions, and liquid form
- related to severe
constipation
*Many of these drugs are combined to
take advantage of the acid-neutralizing
effect and block adverse effects.

CONTRAINDICATIONS AND CONTRAINDICATIONS AND

CAUTIONS CAUTIONS
1. Allergy to this class 1. Allergy to antacid
2. Caution in pregnancy and lactation 2. Caution in any condition exacerbated
3. Care taken in prolonged use by electrolyte or acid-base imbalance
3. electrolyte imbalance
4. GI obstruction
5. Renal dysfunction
6. Pregnancy and lactation
ADVERSE EFFECTS ADVERSE EFFECTS
1. GI Effects of diarrhea or constipation 1. Acid rebound, which can cause to
2. CNS effects of dizziness increase in symptoms, which results in
3. Headache increase intake of the antacid
4. Somnolence 2.
5. Confusion
6. Hallucinations
7. Cardiac arrythmias and hypotension
8. Gynecomastia
9. Impotence
DRUG-DRUG INTERACTIONS DRUG-DRUG INTERACTIONS
Effects of cimetidine, famotidine, &
ranitidine:
- They slow the metabolism of other drugs
leading to increased serum levels and
possible toxic reactions
THESE ARE THE DRUGS:
1. Warfarin anticoagulants
2. Phenytoin
3. Beta-adrenergic blockers
4. Alcohol
5. Quinidine
6. Lidocaine
7. Theophylline
8. Chloroquine
9. Benzodiazepines
9. Nifedipine
10. Pentoxifylline
11. Tricyclic antidepressants (TCAs)
12. Procainamide
13. Carbamazepine