DRUGS FOR PEPTIC ULCER

Gastric Ulcer – Acid secretion is normal or low

Duodenal Ulcer – Acid secretion is high in half the people and low in other

REGULATION OF GASTRIC SECRETION

1)Gasrtrin-------G receptors in parietal cells-------IP3/DAG---

2)Histamine-----H2 receptors in parietal cells-----cAMP------- Ca2+-------Acid Secr

3)Ach-----------M3 in parietal cells-------------IP3/DAG--------

Ganglion cell

N M1

Vagus

CLASSIFICATION
Reduction of gastric acid secretion
1. antihistaminics
2.Anticholinergics
3.Prostaglandin analogues
4.Proton pump inhibitors

Neutralisation of gastric acids

1.systemic antacids
2.nonsystemin antacids

Ulcer protectives

Anti H.pylori
 H2 Antagonist
Insert actions of H2 receptors

ACTIONS
• Block histamine induced acid sectetion
o All phases of gastric secretion
o Nocturnal basal- complete inhibition
• Volume, pepsin content, intrinsic factor decrease- 60-70%
• But no vit b12 def on chronic treatment
• Stress and drug induced

KINETICS
• Good oral abs
• Don’t interfere with food

ADR
• General anticholinergic side effects
o PB--- Histamine is cholinomimetic
• Cimetidine – Antiandrogenic

INTERACTIONS
• Antacids reduce absorption. So 2 hr gap should be given

DRUGS
RANITIDINE
• 5x cimetidine
• No antiandrogenic action
• Less permeable to BBB

FAMOTIDINE
• Bind tightly to H2 receptors
o Longer duration of action
• Most suitable for ZOLLINGER ELLISON SYNDROME
USES
Duodenal ulcer
• Gastric ulcer
• Stress ulcer
• ZE syndrome
o 2nd choice to PPIs
• Mild GERD
• Aspiration pneumonia prophylaxis

PPIs
MOA
• Rearranges to 2 charged cationic forms
• Sulphenic acid and sulphenamide
• Reacts covalently to SH group of H+ K+ ATPase and inactivates irreversibly
• Drug accumulate in canaliculi as charged ions formed in canaliculi are not able to
diffuse back

KINETICS
• Bioavailability reduced by food
• Taken empty stomach and 1 hr after food

ADR
• Compensatory hypergastrinemia

USES
• Peptic Ulcer
• Stress ulcer
• GERD
• ZE synd
• Asp pneumonia
DRUGS
RABIPRAZOLE

ESOMIPRAZOLE

LANSOPRAZOLE

PANTHOPRAZOLE

ANTICHOLINERGICS
• M1 selective- Pirenzipine
• Not commonly used due to side effects

PROSTAGLANDIN ANALOGUE
• Ill defined cytoprotective role
• Inhibit acid secretion
• Promote mucous and HCO3 secretion
• Inhibit gastrin production
• Increase mucosal blood flow

KINETICS
• Short t half
• Poor in releaving ulcer pain

ADR
• Need multiple doses
• Diarrhea, abd cramps, uterine bleeding

USES
• Prevention and treatment of NSAID induced ulcer

ANTACIDS

MOA
• Pepsin complexes with inhibitory terminal moiety. It dissociates below pH 5. So
pH must be maintained above 5
 • ANC- number of meq of 1N HCl that are brought to pH 3.5 in 15 min/60 min
• Action time- empty stomach – 30 min
• With meals - 2-3 hrs

SYSTEMIC
SODIUM BICARBONATE
• Disadvantages
• Short duration of action
• Systemic absorption – alkalosis
• Belching
• Acid rebound
• Edema, CHF due to increased Na load

NON SYSTEMIC
MAG HYDROXIDE
• Laxative action of MgCl2
• Cant be used in renal problems as 5% Mg is absorbed

Mg TRISILICATE

Al HYDROXIDE GEL
• Constipation due to SM relaxing action
• Mucosal astringent action
• Hypophosphatemia due to binding to intestinal phosphates
• Al toxicity, renal failiure

MAGALDRATE
• Hydrated complex of Hydroxy Mg Aluminate
• Both quick and delayed action
• Initially reacts with acid
• Then release AlOH3 which reacts slowly

Ca CARBONATE
• Marked acid rebound due to direct action of Ca2+
• Constipation
• Cause milk alkali syndrome
COMBINATIONS
• Fast + Slow acting- Mg+Al salts
• Costipating + Laxating- Mg+Al salts
• Hastening + delaying gastric emptying - Mg+Al salts

INTERACTIONS
• Decrease absorption of many drugs like teracyclin, Fe salts, H2 blockers

USES
• Pain relief in Acidity
• GERD

ULCER PROTECTIVE
SUCRALFATE
• Basic Al salt of sulfated sucrose

MOA
• Polymerise at pH<4 to form a sticky gel, adheres to ulcer base
• Ppts surface proteins, dietary proteins and form layers

EFFICACY
• Effective in smokers

ADR
• 4 large well timed doses required

COLLOIDAL BISMUTH SUBCITRATE (Tripottasium

dicitrato bismuthate)
MOA
• Stimulation of PGE2-----Secretion of mucus------Mucus+CBS-------Glycoprotein
Bi complex
• Detaches H.pylori from the surface and kills it
ADR
• Osteodystrophy, encephalopathy on prolonged use of Bi
• Blackening of tongue and dentition
• Strict dosing schedule

ANTI H.PYLORI DRUGS

MOA
• High urease activity
• Produce NH3- Neutral environment around Bacteria
• So promote back diffusion of H+ ions

DRUGS
• Amox, Clarithro, Tetracyclin, Metronidazole