for introductory purposes

1. DRUGS USED IN
PEPTIC ULCER

2. Peptic Ulcer
A localized loss of gastric as well
as duodenal mucosa leads to the
formation of peptic ulcer
Symptoms –
heartburn, abdominal pain, bloating,
loss of appetite and weight loss

3. C
Clla
as
ssii
if
fi
i
ic
catiio
on
I. Reduction of gastric acid secretion -
a) H2 receptor antagonists : Cimetidine,
Ranitidine, Famotidine
b) Proton pump inhibitors : Omeprazole,
Lansoprazole, Pantoprazole
c) Anticholinergics : Pirenzepine, Telenzepine
d) Prostaglandin analogue : Misoprostol

4. II. Neutralization of gastric acid (Antacids) –
a) Systemic : Sodium bicarbonate
Sodium citrate
b) Nonsystemic : Magnesium hydroxide
Magnesium trisilicate
Aluminum hydroxide
Calcium carbonate

5. III. Ulcer protectives – Sucralfate,
Colloidal bismuth subcitrate (CBS)
IV. Anti-H.pylori drugs - Amoxicillin,
Clarithromycin, Metronidazole,
Tinidazole, Tetracycline

6. HISTAMINE
GR ST M?
M3
H2
GR
ATP
ase C
H+ K+
Cl-
Food
A
Gastrin
G cells
Somatostatin
D cells
Acetylcholine
+
-
ECL cell
Parietal celH
lH
2 blo
l
o
lo
c
c
kers

7. H
H2
2 R
Rec
ecep
eptor
tor An
Anta
tagon
gonis
ists
ts -
C
i
m
C
i
m
e
t
i
d
e
t
i
d
i
i
n
n
e
,
e
,R
Ra
an
nit
iti
id
din
ine,
e,
Fa
Fam
motid
otidin
ine
e
H2 Receptor Antagonists - Cimetidine,
Ranitidine, Famotidine
Mechanism of action
• Competitive inhibition of H2 receptors -
Inhibits gastric acid secretion (60-70%)
• Suppresses all phases of acid secretion,
mainly nocturnal acid secretion; pH↑to 4-5

8. Therapeutic uses
✓ Peptic ulcer : Gastric and Duodenal ulcer
✓ Gastroesophageal reflux disease (GERD)
✓ Stress ulcers and Gastritis
✓ Zollinger-Ellison syndrome

9. Adverse effects
Cimetidine - antiandrogenic effect
• Gynaecomastia, impotence – men
• Menstrual irregularities, galactorrhoea –
women
Enzyme inhibitor - inhibits metabolism
of many co-administered drugs –
toxicity

10. HISTAMINE
GR ST M?
M3
H2
GR
ATP
C
H+ K+
Cl-
Food
A
Gastrin
G cells
Somatostatin
D cells
Acetylcholine
+
-
ECL cell
Parietal celH
lH
2 blo
l
o
lo
c
c
kers
PP
as
I
e s

11. P
PP
PI
Is:
s:
O
Om
mep
epra
raz
zol
ole
e,
, P
Pa
an
nt
top
opra
raz
zo
ol
le
e
La
Lan
nso
sop
pra
raz
zol
ole,
e,
R
Ra
abe
bep
pra
raz
zo
ol
le
e
PPIs: Omeprazole, Pantoprazole
Lansoprazole, Rabeprazole
Mechanism of action
PPIs (prodrugs)
sulfenamide cation
(activated form)
binds with sulfhydryl groups of the H+K+-
ATPase - inactivate it irreversibly

12. Therap
pe
eu
ut
tic uses
✓ Peptic ulcer
✓ H.pylori associated ulcers
✓ NSAID induced ulcers
✓ GERD
✓ Zollinger-Ellison syndrome
✓ Stress ulcers

13. Advers
se
e effects
▪Muscle & joint pain
▪Rashes, leucopenia, headache
▪Atrophic gastritis

14. P
Prostagl
rostaglan
and
din
ina
a
n
n
a
a
l
l
o
g
u
o
g
u
e
s
e
sM
Mi
iso
sop
pro
rost
sto
ol
l
(P
(PG
GE
E1
1)
)
Prostaglandin analogues
Misoprostol (PGE1)
❖ “Cytoprotective action” -
increases mucus & bicarbonate
secretion, increases mucosal
blood flow
Therapeutic use
✓ NSAID induced ulcers

15. Adverse effects
Diarrhea, abdominal cramps, uterine
contractions & bleeding
Multiple daily dosing – poor patient
compliance

16. Telenzepine
A
An
nt
tic
ich
hol
olin
ine
er
rg
gi
ic
cs
s -
Pir
ire
en
nz
ze
epin
pine,
e,
elenzepine
Anticholinergics - Pirenzepine,
Telenzepine
▪Selective M1 receptor blockers
▪Inhibits acid secretion - heals peptic
ulcer

17. A
An
nt
tacids
Basic substances which neutralize
gastric acid and raise pH of
gastric contents.

18. Sodium bicarbonate
Reacts rapidly with HCl – produces CO2and
NaCl
Demerits
➢ Distension and belching
➢ Metabolic alkalosis
➢ Fluid retention
➢ Acid rebound

19. Magn
ne
es
sium hydro
ox
xi
i
ide and
Alu
um
mii
in
nu
um h
hy
yd
droxide
➢ Reacts slowly with HCl
➢ No belching
➢ No metabolic alkalosis
➢ Mg salts diarrhea , Al salts
constipation so both are administered
together

20. Antacid co
om
mb
binations
▪ Magnesium hydroxide – fast acting
Aluminum hydroxide – slow acting
▪ Mg salts – diarrhea
Al salts – constipation
▪Dose reduction – reduced toxicity

21. Ul
Ulcer
cer p
pr
ro
ot
tect
ectives
ives–
S
u
S
u
c
r
a
c
r
a
l
l
f
f
a
a
t
t
e
e,
, C
Col
oll
lo
oid
ida
al
l
Bism
Bismu
ut
th
h Su
Subc
bcitr
itra
at
te
e
Ulcer protectives –Sucralfate ,
Colloidal Bismuth Subcitrate
Sucralfate
MOA –
• At acidic pH < 4, it undergoes
extensive polymerization – forms a
sticky gel over the ulcer base –
protects it

22. Use – duodenal and gastric ulcers
Adverse effects – constipation, dry
mouth & hypophosphatemia

23. Colloidal B
Bii
i
s
smuth Subcitrate
(CBS)
• Detaches H.pylori from surface of mucosa
Use – Eradication of H.pylori infection
Adverse effects – blackening of stool &
tongue

24. Helicobacter pylori
• Gram –ve bacilli
• Attaches beneath the
mucus
• Cause back diffusion of
H+ ions
• Present in 90% of cases
with peptic ulcers

25. A
An
nt
tii H
H
.
.
p
p
y
y
ll
o
o
r
r
ii d
dr
ru
ug
gs
s
• Amoxicillin
• Clarithromycin
• Tetracycline
• Metronidazole/Tinidazole
• PPIs, H2 blockers, CBS

26. D
D
r
r
u
u
g
g r
r
e
e
g
g
ii
m
m
e
e
n
n
s
s -
- t
t
r
r
ii
p
p
ll
e
e t
t
h
h
e
e
r
r
a
a
p
p
y
y
Lansoprazole 30 mg
+
Amoxicillin 1000 mg
+
Clarithromycin 500 mg
(All twice daily for 2 weeks)

27. THANK YOU