anti ulcer drugs

1. ANTI-ULCER DRUGS
• Slide presentation by-
ANURAG CHANDA
B.PHARM , 5th SEMESTER
GURUNANAK INSTITUTE OF PHARMACEUTICAL SCIENCE AND TECHNOLOGY

2. What is Peptic Ulcer?
• Peptic /stomach ulcer is
the condition in which
imbalance of aggressive
factor and defensive
factors.
• Aggressive factor :
Gastric acid, gastrin,
pepsin
• Defensive factor :
Prostaglandin, mucosa,
bicarbonate

3. •Abdominal pain,
classically epigastric
with severity relating to
mealtimes, after around 3
hours of taking a meal.
•Loss of appetite and
weight loss.
•Waterbrash (rush of
saliva after an episode of
regurgitation to dilute the
acid in esophagus)
•Nausea, and copious
vomiting

5. Classification Of Antiulcer Agent
1) Reduction of gastric acid secretion
H2 antihistamines: Cimetidine, ranitidine, famotidine
PPI’s : Omeprazole, lansoprazole, pantoprazole
Anticholinergics: Pirenzepine
Prostaglandin analogues:- Misoprostol
2) Neutralization of gastric acid by antacids-
Systemic : Sodium bicarbonate, sod. Citrate
Nonsystemic : Mg hydroxide, Mg trisilicate, Al hydroxide gel, calcium
carbonate
3) Ulcer protectives: Sucralfate, CBS ( Colloidal Bismuth Subcitrate)
4) Anti-H. pyloric drugs: Amoxicillin, clarithromycin, metronidazole, tinidazole,
tetracycline

6. Ranitidine- a nonimidazole H2, has several desirable features as compared to
cimetidine.
 5 times more potent than cimetidine
 no androgenic action, does not increase prolactin secretion
 Lesser permeability into brain
 Overall evidence of side effects is lower: headache, diarrhoea/constipation,
dizziness have an incidence similar to placebo.
Famotidine – a thiazole ring containing H2 blocker which binds tightly to H2
and exhibits longer duration of action despite elimination t1/2 of 2.5-3 hours.
Oral bio-availability of famotidine is 40-50% and is excreted by kidney, 70% in
the unchanged form
Incidece of adverse effects is low: headache, dizziness, bowel upset rarely
disorientation and rash have been reported
Because of higher potency it is considered more suitable for ZE syndrome and
for preparation pneumonia.

7. Antacid :-
These are the basic substances which neutralize gastric acidity..
 Systemic antacid :
 Sodium bicarbonate, water soluble, acts i.v. duration of action is short.
 Potent neutralizer, pH may rises above 7.
 Produces CO2 in stomach which leads to distention, discomfort.
 Non-systemic antacid:
 These are insoluble and poorly absorbed basic compound.
 React in stomach with acid to form respective chloride salts.
 Aluminium hydroxide gel:
 The Al+³ ions relaxes smooth muscle leads to delay in gastric emptying.
 This causes constipation.
Proton pump inhibitors-
OMEPRAZOLE-Most
active drug of this group
Powerful inhibitor of gastric acid secretion, when sufficient dosage
of about 20mg per day given the acid production can be
diminished by more than 95%
It is bio-available upto 50%.

8. Ulcer Protective's – Sucralfate:
It a basic aluminium salt of sulphated sucrose, a drug of its own
kind.
It has no acid neutralising action, but delay’s gastric emptying,
it’s own stay in stomach is prolonged.
It is minimally absorbed after oral administration, action is
entirely local
It promotes healing of both duodenal and peptic ulcer, efficacy
has been found similar to cimetidine at four weeks.
It is considered to be superior in patients who continue to smoke.
These are infrequently used now of need for large well timed
daily doses and the availability of simpler H2 blockers/PPI.

9. Anti Helicobacter pylori drugs
 H pylori: Spiral- shaped, pH-sensitive, gram-negative
bacteria.
 It attaches to the surface epithelium beneath the
mucus, has high urease activity
 Produces ammonia which maintains a neutral
microenvironment around the bacteria. Promotes
back diffusion of H+
 Antimicrobials found clinically effective against
H.pylori : Amoxicillin, clarithromycin,
metronidazole.
 Single drugs rapidly develops resistance
(metronidazole).
 CBS is active against H.pylori and resistance
does not develop to it.

10. Proglumide
PGE2
ACh
Histamine
Gastrin
Adenyl
cyclase
_
+
ATP cAMP
Protein Kinase
(Activated)
Ca++
+
Ca++
K+ H+
Proton pump
Gastric acid
Parietal cell
Lumen of stomach
Antacid
Omeprazole
Ranitidine
M3
Misoprostol
_
_
_
_
+
PGE
recepto
r
+
+
Gastrin
recepto
r
+
+
+

11. Reference-
1)Essentials of pharmacology byK.D. Tripathi
2)Introduction to pharmacology by S.K kulkarni
3) Foye’s principles of medicinal chemistry by
thomas m. lemke
4)Wikipedia.com
5)Google.com