Drugs in Alimentation

Dr.Y.Illangasekera
Drugs acting on the Gastrointestinal tract

• Antiemetics
• Laxatives
• Antidiarrhoeal drugs
• Prokinetic drugs
 Antiemetics
Control of vomiting
 Neurotransmitters and receptors involved
in vomiting
• Acetylcholine (M)
• Dopamine (D2)
• 5HT (5HT3)
• Histamine (H1)
• Substance P (NK1 rec.)
• Endocannabinoids (CB1)
 H1 receptor antagonists
• Cinnarazine, promethazine, cyclizine,
dimenhydrinate
• Vestibular diseases i.e. acute labrynthitis
Meniers disease (Betahistine)
• Causes sedation
 Muscarinic receptor antagonists
• Hyoscine hydrobromide (Scopolamine)
• Useful in motion sickness
• Well absorbed from GIT, skin
• Metabolized in liver
• Oral, dermal patch
• Adverse effects
– Dry mouth, blurred vision, drowsiness

• Cinnarazine (Antihistamine) also effective in motion sickness

 Dopamine D2 receptor antagonists

• Metoclopramide, Domperidone, prochlorperazine

• Drug-induced vomiting, autonomic gastroparesis,
migraine
• Gastric prokinetic action – metochlorpramide,
domperidone
• Oral, rectal, i.m., i.v.
• Dystonic reactions possible i.e. metoclopramide,
prochlorperazine
 5HT3 receptor antagonists
• Granisetron, Ondansetron
• High efficacy in chemotherapy / radiation-induced vomiting, post-
operative vomiting
• Given i.v, p.o.

• Adverse effects : lack ADEs of dop. antagonists

– Headache
– Transient elevation of hepatic aminotransferases
– Constipation
 Neurokinin1 receptor antagonists

• Chemotherapy-induced vomiting
• Aprepitant
• Given p.o.
• Metabolised by CYP 3A4
 Cannabinoid receptor agonists

• Nabilone, Dronabinol
• Chemotherapy-induced vomiting
• Adverse effects
– Postural hypotension
– Mood changes
 Laxatives
• Bulk-forming laxatives
• Stimulant laxatives
• Osmotic laxatives
• Stool lubricants
 Bulk-forming laxatives
• Increased fibre intake
– Diet, indigestible polysaccharides
– Fibre supplements (Psyllium, Methylcellulose,
Polycarbophil)

• Increase volume of colonic contents

stimulating peristalsis
 Stimulant laxatives
• Bisacodyl, Senna
• Stimulates secretion & motility of small intestine &
colon
• Act on nerve plexus
• Tablets, suppositories
• Abdominal cramps
• Contraindicated in intestinal obstruction
 Osmotic laxatives
• Increase bowel bulk by water retention
• Lactulose
– Synthetic disaccharide (galactose & fructose)
linked by a bond resistant to disaccharidases
– Undergoes bacterial fermentation in colon

• Magnesium salts (i.e MgSO4)

 Stool softeners and lubricants
• Softener i.e docusate
• Lubricants i.e arachis oil, liquid paraffin

– Adverse effects
• Malabsorption of fat-soluble vitamins
• Anal seepage
• Lipoid pneumonia
 Antidiarrhoeal drugs
• Should not be used in infective diarrhoeas
• Used in motility disorders like irritable bowel
syndrome, autonomic neuropathy

• Opioids
– Loperamide: µ opioid receptor antagonist (decrease
activity in myenteric plexus)
• Muscarinic antagonists
– Atropine/diphenoxylate (co-phenotrope)
 Prokinetic drugs
• Accelerate gastric emptying, small bowel &
colonic transit

• D2 antagonists
• 5HT4 agonists
• Motilin agonists
 Metoclopramide
• D2 antagonist
• Also has 5HT3 antagonist, 5HT4 agonist effects
• No significant effect on colonic motility
 Metoclopramide
• Hepatic metabolism; half-life 4–6 h
• Given p.o., i.m., i.v.
• Crosses BBB; acute dystonic reactions esp. in children
• May cause hyperprolactinaemia
 Domperidone
• D2 antagonist
• Does not cross BBB
• Given p.o., rectally
 Motilin agonists
• Motilin secreted from duodenum, jejunum
• Controls inter-digestive contractions
• Erythromycin, clarithromycin, azithromycin
• Cause antral contraction
• Used in diabetic gastroparesis
• Adverse effects
– Abdominal pain, vomiting
– Cardiac arrhythmias