Antiulcer Drugs

ANTI ULCER DRUGS
Visit
www.bpharmstuf.com
For more ppt’s
INTRODUCTION
► Ulcers are sores or open wounds that occur on the
skin or along the lining of the digestive tract due
to loss of tissue.
► Peptic ulcers are the most common types of ulcers
.
► The lifetime risk for developing a peptic ulcer is
approximately 10%.
► In the United States about 4 million people have
active peptic ulcers and about 350,000 new cases
are diagnosed each year.
Visit :www.bpharmstuf.com
TYPES OF ULCERS
► Peptic Ulcers: Peptic ulcers is
a broad term which includes
ulcers of digestive tract in the
stomach or the duodenum.
► The causative agent is infection
caused by the bacteria H. pylori
or reaction to certain medicines
like non-steroidal anti-
inflammatory drugs (NSAIDs)
► Ulcers of the duodenum are
called duodenal ulcers, whereas
those in the stomach are called
stomach ulcers or gastric ulcers
MOUTH ULCERS
 Sores that develop in the inner lining of the
mouth are referred to as mouth ulcers.
 Anemia, measles, viral infection, oral
candidiasis, chronic infections, throat
cancer, mouth cancer and vitamin B
deficiency are some of the common causes
of ulcers or sores in the mouth.
 These mouth sores are round or oval in
shape and white, yellow or gray in colour.
 These are usually cured within 10-14 days.
However, in severe cases it may take
several weeks for these to heal completely.
ESOPHAGEAL ULCERS
► Esophageal ulcers are lesions that
occur in the esophagus (the food
pipe).
► These most commonly form in the end
of the food pipe and can be felt as a
pain right below the breastbone in the
same area where symptoms of
heartburn are felt.
► Esophageal ulcers are associated with
acid reflux or GERD, prolonged use of
drugs like NSAIDs, and smoking.
GENITAL ULCERS
► Genital ulcers are caused due to
sexually transmitted diseases like
syphilis, genital herpes, or thrush.
► Non-sexual causes of genital ulcers
are infections caused by yeast,
scabies, pyoderma genital trauma
and Behcet's disease.
► Genital ulcers manifest as single or
multiple ulcers which are mostly
painful.
PRESSURE SORES
► These lesions are caused in patients
who are confined to bed due to
some debilitating illness or are on
their way to recovery in hospital.
► In the initial stages a bedsore
manifests itself as a persistent area
of red skin that hurts and feels warm
► As the severity increases there is loss
of the upper layer of skin and
subsequent damage to the
underlying tissue.
Causes of ulcer
 Peptic ulcer disease was once thought of simply as
a problem of too much acid and stress.
 It results of an imbalance between digestive fluids
(hydrochloric acid and pepsin) in the stomach and
duodenum.
 Much of that imbalance is clearly related to
infection with the bacteria Helicobacter pylori ( H.
pylori ).
 The other major risk factor for the development of
ulcers is ingestion of nonsteroidal antiinflammatory
drugs (NSAIDs) such as aspirin.
PATHOPHYSIOLOGY
Peptic ulcer results
probably due to an Aggressive Defensive
imbalance between the factors factors
aggressive and defensive
factors. Increase in acid- Acid Mucous
pepsin secretion and Pepsin Bicarbonate
decrease in mucosal Helicobacter Prostaglandins
resistance appears to be Pylori
the basic cause for peptic NSAIDS Mucous blood
ulceration flow
PATHOPHYSIOLOGY
DIAGNOSIS
► Perform diagnostic tests to see if
there is an ulcer:
► ~ Upper endoscopy, which involves
inserting a small lighted tube into the
stomach to look for abnormalities. A
small sample of tissue (biopsy) is
removed and analyzed to confirm
diagnosis.
► ~ Testing for H. pylori infection by
either a stool sample or by obtaining
a breath sample. If the test is
positive, the patient is treated with
antibiotics. If negative, the focus of
the evaluation will be on the other
causes of peptic ulcer disease, such
as NSAID consumption.
TREATMENT
Approaches for the treatment of peptic ulcer
are
 Reduction of gastric acid secretion
 Neutralization of gastric acid
 Ulcer protectives
 Anti-H.pylori drugs
ANTI ULCER DRUGS
REDUCTION OF GASTRIC ACID
SECRETION
► Histamine antagonist: Cimetidine, ranitidine
► Proton pump inhibitors: omeprazole,
pantaprazole
► Acetyl choline antagonist: pirenzepine,
propantheline
► Prostaglandin analogue: misoprostol
ANTIULCER DRUGS
 Neutralization of gastric acid(antacids)
Systemic : Sodium bicarbonate,Sodium citrate
Nonsystemic : Magnesium hydroxide,Aluminium
hydroxides
 Ulcer potectives :
Sucralfate
 Anti hlicobacter pylori :
amoxicillin,clarithromycin,etc
Histamine antagonist
Cimetidine
Cimetidine belongs to a class of
medications called histamine
H2-antanists.
Histamine is a natural chemical
that stimulates stomach cells to
produce acid. Histamine H2-
antagonists inhibit the action of
histamine on the acid-producing
cells of the stomach and reduce
stomach acid
CIMETIDINE
SIDE EFFECTS; it include constipation, diarrhea,
fatigue, headache, insomnia, muscle pain, and
vomiting. Major side effects include confusion and
hallucinations, enlargement of the breasts;
impotence.
DRUG INTERACTIONS: Cimetidine may increase

the blood levels of several drugs by reducing their
elimination by the liver. This interaction may occur
between cimetidine and warfarin (Coumadin), a
commonly used blood thinning agent
CIMETIDINE
► DOSE: 400 mg at bed time
► USES: it is used in treatment of duodenal ulcer,

Gastric ulcer, stress ulcer, GERD, zollinger ellision
syndrome
PROTON PUMP INHIBITORS
OMEPRAZOLE
► Omeprazole is inactive at neutral pH, but at pH<5
rearranges to two charged cationic forms(a
sulphenic acid and a sulphenamide
configurations)that react covalently with SH groups
of the H+K+ATPase enzyme and inactivate it
irreversibly, especially when two molecules of
omeprazole react with one molecule of the enzyme.
OMEPRAZOLE
► SIDE EFFECTS Stomach
pain,Diarrhea,Constipation,Dizziness,CoughBack,
Pain,Rash,Hives,Itching,seizures
► DRUG INTERACTION
Omeprazole inhibits oxidation of certain drugs:
diazepam, phenytion and warfarin levels may be
increased. Clarithromycin inhibits omeprazole
metabolism and increases its plasma concentration.
It reduces bioavailability of ketoconazole
ACETYL CHOLINE ANTAGONIST
Atropinic drugs reduce the volume of gastric
juice without raising it’s pH unless there
is food in stomach to dilute the secreted acid.
stimulated gastric secretion is less completely
inhibited.
DRUGS:
Pirenzepine
Oxyphononium
ACETYL CHOLINE ANTAGONIST
PIRENZEPINE
 MECHANISM:
It selectively block M1 muscaranic recptors
and inhibits gastric secretion. The more likely
site of action of pirenzepine in stomach
intramural plexuses and ganglionic cells
rather than the parietal cells themselves
 DOSE
Pirenzepine 50mg orally twice or thrice daily
for 4-6 weeks Visit :www.bpharmstuf.com
Pirenzepine
► SIDE EFFECTS:
Dry mouth, blurred vision, drowsiness,

dizziness, nausea or loss of appetite may occur
the first few days as your body adjusts to the
medication.
► USES
The medication is used in the treatment of ulcers
PROSTAGLANDIN ANALOGUE
prostaglandins are produced in the gastric
mucosa and appear to serve a protective role by inhibiting
acid secretion and promoting mucus
and bicarbonate secretion. In addition, PGs inhibits
gastrin production, increase mucosal blood flow
and probably have an ill defined cytoprotective
action.
DRUGS: Misoprostol
Colloidal bismuth subcitrate
PROSTAGLANDIN ANALOGUE
MISOPROSTOL
MECHANISM:
Misoprostol is approved for use in the
prevention of NSAID-induced gastric ulcers. It acts
upon gastric parietal cells, inhibiting the secretion
of gastric acid via G-protein coupled receptor-
mediated inhibition of adenylate cyclase, which
leads to decreased intracellular cyclic AMP levels
and decreased proton pump activity at the apical
surface of the parietal cell
MISOPROSTOL
► Side effects
Diarrhea is one of the most common side effects
reported after using Misoprostol.
Other common side effects include: abdominal pain,
nausea, flatulence, headache, dyspepsia, vomiting,
and constipation.
► contraindication
Misoprostol should not be taken by pregnant
women to reduce the risk of NSAID-induced gastric
ulcers because it increases uterine tone and
contractions in pregnancy which may cause partial
or complete abortions, and because its use in
pregnancy has been associated with birth defects.
ANTACIDS
► Antiacids can raise gastric pH from 1 to 3.5.
Their duration of action is determined by their
acid-combining ability and the length of stay in
the stomach
► The potency of an antacid is generally

expressed in terms of its acid neutralizing
capacity, which is defined as number of mEq of
1N HCl that brought to pH 3.5 in 15 min by unit
dose of the acid preparation.
Sodium bicarbonate
It is water soluble, acts instantaneously,
but duration of action is short. It is a potent
neutralizer(1g-12mEq HCl), pH may raises above 7.
Adverse reactions
It causes systemic alkalosis, gastric distention,
rebound acidity and milk-alkali syndrome
Drug interactions
Sodium containing antacids reduce antihypertensive
drug effect
Uses
It is restricted to casual treatment of heartburn and
to treat acidosis Visit :www.bpharmstuf.com
ULCER PROTECTIVES
SUCRALFATE
MCHANISM:
► Sucralfate is a locally acting substance that in an
acidic environment (pH < 4), reacts with
hydrochloric acid in the stomach to form a cross-
linking, viscous, paste-like material capable of acting
as an acid buffer for as long as 6 to 8 hours after a
single dose. It also attaches to proteins on the
surface of ulcers, such as albumin and fibrinogen, to
form stable insoluble complexes. These complexes
serve as protective barriers at the ulcer surface,
preventing further damage from acid, pepsin, and
bile. Visit :www.bpharmstuf.com
SUCRALFATE
► Side effects
The most common side effects seen are
constipation. Less commonly reported include
flatulence, cephalalgia (headache), xerostomia
(dry mouth).
► Drug interactions
Sucralfate interferes with the absorption of
tetracyclines, flouroquinolones, cimetidine,
phenytion and digoxin. Antacids reduce the
efficacy of sucralfate
SUCRALFATE
► DOSE: 1 gm taken for 1 hr
► USES:
It is used in treatment of
Gastritis,
Stress ulcers.
ANTI H.PYLORI DRUGS
 Anti microbials that have been found clinically
effective against H.pylori are: amoxicillin,
clarithromycin, tetracycline and metronidazole.
 Bismuth active against H.pylori and resistance not
develop to it.
 A combination regimen is preferred, using gastric
acid inhibitors and antibiotics. Two examples are:
 A proton pump inhibitor or H2 blocker + amoxicillin +
clarithromycin or metronidazole
 A proton pump inhibitor + bismuth subsal +
tetracycline + metronidazole
REFERENCES
► Medicalpharmacology by tripathi
► Pharmacology by salil.k.bhattacharya
► Pharmacology by H.P rang, M.M dale & J.M
Ritter
QUERIES ?
THANk you

Antiulcer Drugs

Uploaded by

Document Information

Copyright

Available Formats

Share this document

Share or Embed Document

Sharing Options

Did you find this document useful?

Is this content inappropriate?

Copyright:

Available Formats

Antiulcer Drugs

Uploaded by

Copyright:

Available Formats

ANTI ULCER DRUGS

DRUG INTERACTIONS: Cimetidine may increase

► USES: it is used in treatment of duodenal ulcer,

Dry mouth, blurred vision, drowsiness,

► The potency of an antacid is generally

You might also like