GI drugs

Nicole Micallef, Sara Caruana, Sven Kilger,

William Gal, Elenia Xiberras
 The Gastrointestinal System

The GI tract consists of the:

• oral cavity
• pharynx
• esophagus
• stomach
• small & large intestine
• anal canal
The Gastrointestinal System
Accessory organs indirectly aid in ingestion or digestion.

Some examples are:

• teeth
• tongue
• glandular organs (e.g., salivary glands)
• liver
• gallbladder
• pancreas
Main functions of
the GI system

• ingestion and digestion of food

• nutrient absorption

• secretion of water and enzymes

• excretion of waste products

 Gastrointestinal (GI)
pharmacology
This is the study of properties and actions of drugs affecting the
gastrointestinal system.

Pathologies of the gastrointestinal tract are due to impairment of one

or more of these simple functions:
• secretion
• absorption
• motility
 1. Functional diseases:
measurable changes to tissues, organs, or
body systems.

Examples: irritable bowel syndrome (IBS),

Diseases dyspepsia.

affecting the GI
tract 2. Organic diseases:
abnormal symptoms or changes in function
but with no measurable changes in tissues.

Examples: inflammatory bowel disease

(IBD), peptic ulcer, gastroesophageal reflux
disease (GERD).
 Mechanisms of drugs working on
the gastrointestinal system
Drug type Mechanism of action Conditions requiring Common side-effects
this drug and examples

Proton  Inhibit proton pump Few adverse effects:

 GERD
pump (H+/K+) ATPase) in  Headache
inhibitors stomach lining’s parietal  Peptic ulcers  Rash
(PPIs) cells.  Dizziness
 Zollinger-Ellison
 H+ K+ ATPase pump – Syndrome (rare GI symptoms:
responsible for final step  nausea,
digestive disorder
in gastric acid  abdominal
production. that results in too  pain,
 flatulence,
 PPIs block this pump = much gastric acid)
 constipation,
reduction in gastric acid  Ex: Omeprazole,  diarrhoea
 Mechanisms of drugs working on
the gastrointestinal system
H2 Receptor  Histamine H2 receptors –
 diarrhoea,
Blockers responsible for stimulating  Peptic ulcers
production of gastric acid  constipation,
 GERD
 Inhibit histamine H2  fatigue,
 other hypersecretory
receptors in stomach lining  drowsiness,
 reduction in amount of conditions.
acid produced.  headache
 muscle aches

Antacids  Neutralize stomach acid.  GERD

 Diarrhoea or constipation
 Raise pH.
 Alleviate: heartburn,  Flatulence
indigestion
 Stomach cramps
 Side effects: constipation or
diarrhoea  Feeling sick or vomiting
 Mechanisms of drugs working on
the gastrointestinal system
Prokinetic  Enhance GI motility.  Gastroparesis
Agents (delayed gastric  Abdominal cramps
emptying)
 diarrhoea
 GERD
 Nausea
 Ex: Metoclopramide
– dopamine  Vomiting
receptor agonist,
stimulates  Depression
acetylcholine
release  increased  Blurred vision
peristalsis &
improved  Upset stomach
coordination of
 Mechanisms of drugs working on
the gastrointestinal system
Antiemetics  Act on many receptors in the central  Ex: Ondansetron –
nervous system to prevent/reduce serotonin receptor agonist  Headache
nausea blocking serotonin
signalling to brain   Dizziness
suppression of nausea and
vomiting  constipation

Laxatives  Promote bowel movements by Examples:

many mechanisms  Psyllium – bulk forming  Bloating
laxative, absorbs water in
intestine.  Flatulence

 Bisacodyl – stimulant  Tummy cramps

laxative – directly stimulates
intestinal muscles  Feeling sick

 Polyethylene glycol –  Dehydration leading to light-

osmotic laxative – increases
water content in stool headedness and concentrated urine
making it easier to pass.
 Mechanisms of drugs working on
the gastrointestinal system
Antidiarrheal  Reduce diarrhoea.  Bismuth subsalicylate
Agents – antimicrobial, anti-
inflammatory effects  Acid or sour stomach
to reduce irritation
& relieve diarrhoea
 Belching
 Ex: Loperamide –
opioid receptor
agonist acting on  Bloating
intestinal muscles 
slows down peristalsis
and increases time  Dry mouth
taken for stool to
move through
intestine (increased  heartburn
water uptake)
 Further examples
Histamine 2 blockers Antacids
• Zantac (ranitidine) • Milk of magnesia (magnesium
hydroxide)
• Pepcid (famotidine)
• Tums (calcium carbonate)
• Aid AR (nizatidine) • Gaviscon (aluminum hydroxide/
magnesium trisilicate)
• Tagamet HB (cimetidine)
• Gelusil (aluminum/magnesium
hydroxide/ simethicone)
 Further examples
Proton pump inhibitors Antiemetics

• Nexium (esomeprazole) • Ativan (Iorazepam)

• Dexilant (dexlansoprazole) • Reglan (metoclopramide)

• Protonix (pantoprazole) • Emetol (phosphorated carbohydrate

• Aciphex (rabeprazole) soluon)

• Lorazepam Intensol (lorazepam)

 Further examples

Laxatives
• Dulcolax (bisacodyl)
• Plenvu (polyethylene glycol 3350 with electrolytes)
• Colace (Docusate sodium)
References
• https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7887997/#:~:text=In%20general%2C%20PPIs%20are%20believed,flatulen
ce%2C%20constipation%2C%20and%20diarrhea
.
• https://www.drugs.com/sfx/anti-diarrheal-side-effects.html
• https://www.nhs.uk/conditions/laxatives/
• https://www.ncbi.nlm.nih.gov/books/NBK532303/#:~:text=Intravenous%20(IV)%20and%20oral%20(,patients%20with%20
known%20prolonged%20QTc
.
• https://www.webmd.com/heartburn-gerd/what-to-know-prokinetic-agents
• https://www.nhs.uk/conditions/antacids/
• https://www.ncbi.nlm.nih.gov/books/NBK547929/#:~:text=Side%20effects%20are%20uncommon%2C%20usually,by%20t
he%20cytochrome%20P450%20system
.
• https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7887997/#:~:text=In%20general%2C%20PPIs%20are%20believed,flatulen
ce%2C%20constipation%2C%20and%20diarrhea
.