Anti Ulcer Agents

7/28/2019 Anti Ulcer Agents

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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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Anti Ulcer Agents