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ANTI ULCER AGENTS
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The Digestive System
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PEPTIC ULCERS
Is erosion in the lining of the
stomach or duodenum.
The word peptic refers to pepsin,
stomach enzyme that breaks downproteins.
Occur when there is a hyper
secretion of hydrochloric acid andpepsin which erode the GI mucosal
lining
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Predisposing Factors:
Mechanical disturbancesGenetic influences
Bacterial organisms
Environmental factorsCertain drugs
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Duodenal & Gastric Ulcer
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CLASSIC SYMPTOM OF PEPTIC
ULCER
Gastric ulcer:Pain occurs 30 mins to 1.5 hrs
after eating
Duodenal ulcer:
Pain occurs 2-3 hours after
eating.
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Stress Ulcer:Usually follows a critical situation such
as extensive trauma or major surgery
HELICOBACTER PYROLI (H. Pylori)
Gram negative bacillusKnown to cause:
Gastritis
Gastric ulcerDuodenal ulcer
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TREATMENT
The use of only one antibacterialagent is not effective for eradicatingH.pylori
A. Bismuth 2 tabs QID+Amoxicillin 500mg cap TIDTetracycline 500mg 1 cap QID
+Metronidazole500mg tab PO X 2weeks
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B. Amoxicillin 500mg cap TID+
Omeprazole 20mg cap BID PO X 2weeks
C. Omeprazole 20mg cap BID
+Clarithromycin 500mg tab BID X 1week s
+Metronidazole 500mg tab PO X 2weeks
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D.
Ranitidine/Bismuth(pylorid)400mg 1 tab BID
+
Clarithromycin 500mg tab BID X
1-2 weeks
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7 GROUPS OF ANTI ULCER DRUGS:
1. Tranquilizers
2. Anticholinergic
3. Antacids
4. H2 blockers
5. PPIs
6. Pepsin Inhibitor Sucralfate
7. Prostaglandin E analogueMisoprostol
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TRANQUILIZER
Have minimal effect in preventing &
treating ulcersDecrease vagal stimulation &
anxiety
Example: LIBRAX
Combination of anxiolytic
chlordiazepoxide and theAnticholinergic clidirium bromide
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Side effects & Adverse Reactions
Dry mouth
Tachycardia
Urinary retentionConstipation
milk-alkali syndrome
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Milk-alkali syndrome
Is intensified if milk products areingested with calcium carbonate.
Confirmed by:
Presence of alkalosis,hypercalcemia, crystalluria &
renal failure
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Non Systemic Effect:
Composed of alkaline salts:
A. Aluminum(Aluminum hydroxide, aluminum
carbonate)
B. Magnesium
(Magnesium hydroxide, magnesium
carbonate)
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Magnesium compounds:Can cause diarrhea
Aluminum compounds:
Can cause constipation
A combination of magnesium &aluminum salts neutralizes gastricacid without causing severe diarrhea
& constipation.
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Pharmacokinetics
Aluminum Hydroxide:Small amount is absorbed in theGIT
Primarily bound to PO4 &excreted in the feces
Small portion excreted in theurine
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HISTAMINE 2 BLOCKERS (H2
Blockers)
Most popular drugs used in the
treatment of gastric & duodenal
ulcers.
Prevent acid reflux in the
esophagus (reflux esophagitis)
Blocks the H2 receptors of theparietal cells in the stomach
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3 H2 Blockers
RANITIDINE (Zantac 1983)
FAMOTIDINE (Pepcid 1986)NIZATIDINE (Axid 1988)
More potent than cimetidineDuration of Action: long
Fewer side effects & drug
interactions
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Pharmacokinetics
Ranitidine:
Is 5-12X more potent than
cimetidine but less potent than
famotidine.
Rapidly absorbed & reach the
peak concentration after a
single dose.Has a low protein-binding
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Pharmacokinetics
50% excreted unchanged in theurine
Ulcer healing for 8 weeks is 90%
Large doses are effective forcontrolling Zollinger-Ellison
Syndrome
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Pharmacodynamics
Ranitidine
Inhibits histamine at H2
receptor site
Effective in the treatmentx ofgastric & duodenal ulcer.
Relieves symptom of reflux
esophagitis
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Famotidine
is 50-80% more potent thancimetidine
is 5-8x more potent than ranitidine
indicated for short term use (4-8wks)(duodenal ulcer)
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Nizatidine
Latest H2 blocker Relieve nocturnal gastric acid
secretion for 12hours.Similar to famotidine in protein
binding & half-life
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PROTON PUMP INHIBITORS (PPIs)
Suppresses gastric acid secretion
by inhibiting the H/K ATPase
enzyme
Inhibit acid secretion by 90%greater than H2 blockers
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PROTON PUMP INHIBITORS (PPIs)
EXAMPLES:prazolelanzoprazole
rabeprazolepantoprazoleesomeprazole
Duration of treatment: 4-8 weeks
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PEPSIN INHIBITOR (Mucosal
Protective Drug
Ex:Sucralfate (Carafate)A complex of sulfated sucrose &
Aluminum hydroxide
Non absorbable & combines with
protein to form a viscous substance that
covers the ulcer & protect it from acid &pepsin.
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Does not neutralize acid nor decrease
acid secretions
Side effects: Constipation
Dosage: 1 gram QID AC & HS
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PROSTAGLANDIN ANALOGUE
Ex: Misoprostol (Cytotec)Appears to suppress gastric acid
secretions & increase cytoprotective
mucus in the GI tract.
Causes moderate decrease in PEPSIN
secretionsAs effective as Cimetidine
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PROSTAGLANDIN ANALOGUE
WHEN CLIENT IS TAKING HIGHDOSES OF NSAIDS, they frequently
recommended for the duration of the
NSAID therapy
Contraindication:Pregnancy
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