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Gastro intestinal system
&
Analgesics
Compiled by C Settley
Drugs and the
gastrointestinal system
• Drugs can be used to influence the GIT
to:
– Increase gastric emptying & gastric motility
– Balance the ratio of acid-to-mucus secretion
in the stomach and neutralising gastric acid
– Relieving diarrhoea & intestinal colic
– Relieving constipation
Compiled by C Settley
Dyspepsia, pg 152
• Dyspepsia : heartburn
• Heartburn, also called acid indigestion, is
a symptom of gastro esophageal reflux
(GERD). It can occur when acid or other
contents from your stomach "back up" into
the esophagus. That's the tube food
passes through going from your mouth to
your stomach.
Compiled by C Settley
Dyspepsia, pg 152
Compiled by C Settley
Dyspepsia, pg 152
• Dyspepsia : heartburn
– Simple antacids neutralise stomach acid &
relieve pain
– E.g. Magnesium containing antacids (causes
diarrhoea) and aluminium containing antacids
(causes constipation).
– Combination of these is indicated
– NB drug interactions
Compiled by C Settley
Dyspepsia, pg 152
• Calcium carbonate and sodium
bicarbonate may be used as simple
antacids.
• However care should be taken as
Calcium carbonate may interfere with
normal acid base balance while sodium
bicarbonate should be used with caution in
patients who require a restricted sodium
intake (eg ?)
Compiled by C Settley
Peptic ulcer, pg 153
• Peptic ulcers are sores that develop in the
lining of the stomach, lower esophagus, or
small intestine (the duodenum), usually as
a result of inflammation caused by the
bacteria H. pylori, as well as from erosion
from stomach acids.
Compiled by C Settley
Peptic ulcer
Compiled by C Settley
Peptic ulcer
• Aim of treatment is to lower gastric acidity
to allow ulcer to heal.
• Simple antacids may be used.
• Antibiotics for ulcers? Recurrent ulcers
may be due to Helicobacter pylori
infection. Treated with a combination of
antibiotics.
Compiled by C Settley
Peptic ulcers: Causes
• Helicobacter pylori (H. pylori): a bacteria that can cause a
stomach infection and inflammation
• Frequent use of aspirin, ibuprofen, and other anti-inflammatory
drugs (risk associated with this behavior increases in women and
people over the age of 60)
• Smoking
• Drinking too much alcohol
• Radiation therapy
• Stomach cancer
Compiled by C Settley
Peptic ulcers: Symptoms
• The most common symptom of a peptic ulcer is burning abdominal
pain that extends from the navel to the chest, which can range from
mild to severe. In some cases, the pain may wake you up at night.
Small peptic ulcers may not produce any symptoms in the early
phases.
• Other common signs of a peptic ulcer include:
• changes in appetite
• nausea
• bloody or dark stools (melena)
• unexplained weight loss
• indigestion
• vomiting
• chest pain
Compiled by C Settley
Peptic ulcer: treatment-
Pro-kinetic drugs
• Used to treat and prevent nausea &
vomiting.
• Metoclopramide increases the rate of
gastric emptying and peristalsis.
Compiled by C Settley
Peptic ulcer: treatment-
Drugs that increase gastric pH
• Proton pump inhibitors
– Effect: prevents secretion of HCl (gastric acid)
– Increasing pH in stomach
– E.g. Omeprazole
Compiled by C Settley
Peptic ulcer: treatment-
Drugs that reduce gastric pH
• H2 receptor antagonists
– Blocks gastric H2 receptors
– Reduces gastric acid secretion
– Not as effective as proton pump inhibitors
– More possible drug interactions
– E.g. cimetidine
Compiled by C Settley
Peptic ulcer: treatment-
Cytoprotective drugs
• Protect sells of stomach lining against
corrosive effects of gastric acid
• By forming a protective layer
• Very good success rate in healing of
ulcers
• E.g. sucralfate
• Take one hour before meals
Compiled by C Settley
Treatment for diarrhoea
anti-motility agents
• First find cause of diarrhoea, not all
diarrhoea must be stopped
• E.g. loperamide
• Non-analgesic opioid
• Stimulate opioid receptors in enteric
nervous system
• To inhibit release of acetylcholine
• Decreases peristalsis
Compiled by C Settley
• A COMBINATION OF THESE DRUGS
ARE PRESCRIBED IN THE TREATMENT
OF PEPTIC ULCERS!!!
Compiled by C Settley
Intestinal colic (cramps)
• E.g. Hyoscine butylbromide (Buscopan)
• Has an anti-spasmodic action
Compiled by C Settley
Relieving constipation
• Laxatives should only be used to:
• Treat acute episodes of constipation
• To clean out the bowel
• To assist in elimination of drugs (overdose
or poisoning) e.g. kexelate,
organophosphates
Compiled by C Settley
Bulk-forming laxatives
• Only bulk-forming agents for chronic use
• Indigestible substances
• Help to retain water in bowel
• Stimulates peristalsis
• Take with large glass of water
• E.g. bran
Compiled by C Settley
Osmotic laxatives
• Action:
– Increase osmotic pressure in bowel 
– Water retained
• Mainly indicated for short term use or rapid
evacuation of bowel e.g. magnesium sulphate
• Lactulose can be used for longer periods
• Preparation for bowel surgery? Eg …
Compiled by C Settley
Irritants / contact laxatives
• Action:
• These agents stimulate / irritate the colon
directly
• Increases peristalsis
• E.g. bisacodyl, senna
• Not for chronic use, easily abused
Compiled by C Settley
Other
• Stool softeners: moisten the stool by
drawing water from the intestines
• Liquid paraffin: acts as intestinal lubricant
Compiled by C Settley
Drug action within the central
nervous system
• Opioid analgesics
• Action of OA’s:
– Suppress neurotransmission of pain sensations
– Main action in brain & spinal cord (opioid receptors)
• Analgesics of choice for severe pain (examples). Please go
through drug action, indication, side effects etc
• Morphine
• Pethidine
• Tramadol
Compiled by C Settley
Pethidine
• Has a rapid onset
• Its analgesic effects are limited to a few
hours in duration
• It has a toxic metabolite that accumulates
with repeated administration iow not suited
for the treatment of chronic pain
• Suited for post operative setting
• Obstetrics, ureter colic and biliary
obstruction
Compiled by C Settley
The difference between
Analgesics and NSAID’S
• An anti-inflammatory drug is one that
reduces inflammation or swelling.
• A pain killer, more properly called an
analgesic, is a drug that stops you from
feeling pain.
• Some drugs do both, such as ibuprofen.
But most drugs only do one or the other.
Compiled by C Settley
NSAID’S
• Anti inflammatory effects
• Antipyretic effects
• Constriction of blood vessels
• Examples: aspirin, diclofenac, paracetamol
• Read through clinical application- pg 144-145
Compiled by C Settley

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Gastro intestinal system & analgesics

  • 2. Drugs and the gastrointestinal system • Drugs can be used to influence the GIT to: – Increase gastric emptying & gastric motility – Balance the ratio of acid-to-mucus secretion in the stomach and neutralising gastric acid – Relieving diarrhoea & intestinal colic – Relieving constipation Compiled by C Settley
  • 3. Dyspepsia, pg 152 • Dyspepsia : heartburn • Heartburn, also called acid indigestion, is a symptom of gastro esophageal reflux (GERD). It can occur when acid or other contents from your stomach "back up" into the esophagus. That's the tube food passes through going from your mouth to your stomach. Compiled by C Settley
  • 5. Dyspepsia, pg 152 • Dyspepsia : heartburn – Simple antacids neutralise stomach acid & relieve pain – E.g. Magnesium containing antacids (causes diarrhoea) and aluminium containing antacids (causes constipation). – Combination of these is indicated – NB drug interactions Compiled by C Settley
  • 6. Dyspepsia, pg 152 • Calcium carbonate and sodium bicarbonate may be used as simple antacids. • However care should be taken as Calcium carbonate may interfere with normal acid base balance while sodium bicarbonate should be used with caution in patients who require a restricted sodium intake (eg ?) Compiled by C Settley
  • 7. Peptic ulcer, pg 153 • Peptic ulcers are sores that develop in the lining of the stomach, lower esophagus, or small intestine (the duodenum), usually as a result of inflammation caused by the bacteria H. pylori, as well as from erosion from stomach acids. Compiled by C Settley
  • 9. Peptic ulcer • Aim of treatment is to lower gastric acidity to allow ulcer to heal. • Simple antacids may be used. • Antibiotics for ulcers? Recurrent ulcers may be due to Helicobacter pylori infection. Treated with a combination of antibiotics. Compiled by C Settley
  • 10. Peptic ulcers: Causes • Helicobacter pylori (H. pylori): a bacteria that can cause a stomach infection and inflammation • Frequent use of aspirin, ibuprofen, and other anti-inflammatory drugs (risk associated with this behavior increases in women and people over the age of 60) • Smoking • Drinking too much alcohol • Radiation therapy • Stomach cancer Compiled by C Settley
  • 11. Peptic ulcers: Symptoms • The most common symptom of a peptic ulcer is burning abdominal pain that extends from the navel to the chest, which can range from mild to severe. In some cases, the pain may wake you up at night. Small peptic ulcers may not produce any symptoms in the early phases. • Other common signs of a peptic ulcer include: • changes in appetite • nausea • bloody or dark stools (melena) • unexplained weight loss • indigestion • vomiting • chest pain Compiled by C Settley
  • 12. Peptic ulcer: treatment- Pro-kinetic drugs • Used to treat and prevent nausea & vomiting. • Metoclopramide increases the rate of gastric emptying and peristalsis. Compiled by C Settley
  • 13. Peptic ulcer: treatment- Drugs that increase gastric pH • Proton pump inhibitors – Effect: prevents secretion of HCl (gastric acid) – Increasing pH in stomach – E.g. Omeprazole Compiled by C Settley
  • 14. Peptic ulcer: treatment- Drugs that reduce gastric pH • H2 receptor antagonists – Blocks gastric H2 receptors – Reduces gastric acid secretion – Not as effective as proton pump inhibitors – More possible drug interactions – E.g. cimetidine Compiled by C Settley
  • 15. Peptic ulcer: treatment- Cytoprotective drugs • Protect sells of stomach lining against corrosive effects of gastric acid • By forming a protective layer • Very good success rate in healing of ulcers • E.g. sucralfate • Take one hour before meals Compiled by C Settley
  • 16. Treatment for diarrhoea anti-motility agents • First find cause of diarrhoea, not all diarrhoea must be stopped • E.g. loperamide • Non-analgesic opioid • Stimulate opioid receptors in enteric nervous system • To inhibit release of acetylcholine • Decreases peristalsis Compiled by C Settley
  • 17. • A COMBINATION OF THESE DRUGS ARE PRESCRIBED IN THE TREATMENT OF PEPTIC ULCERS!!! Compiled by C Settley
  • 18. Intestinal colic (cramps) • E.g. Hyoscine butylbromide (Buscopan) • Has an anti-spasmodic action Compiled by C Settley
  • 19. Relieving constipation • Laxatives should only be used to: • Treat acute episodes of constipation • To clean out the bowel • To assist in elimination of drugs (overdose or poisoning) e.g. kexelate, organophosphates Compiled by C Settley
  • 20. Bulk-forming laxatives • Only bulk-forming agents for chronic use • Indigestible substances • Help to retain water in bowel • Stimulates peristalsis • Take with large glass of water • E.g. bran Compiled by C Settley
  • 21. Osmotic laxatives • Action: – Increase osmotic pressure in bowel  – Water retained • Mainly indicated for short term use or rapid evacuation of bowel e.g. magnesium sulphate • Lactulose can be used for longer periods • Preparation for bowel surgery? Eg … Compiled by C Settley
  • 22. Irritants / contact laxatives • Action: • These agents stimulate / irritate the colon directly • Increases peristalsis • E.g. bisacodyl, senna • Not for chronic use, easily abused Compiled by C Settley
  • 23. Other • Stool softeners: moisten the stool by drawing water from the intestines • Liquid paraffin: acts as intestinal lubricant Compiled by C Settley
  • 24. Drug action within the central nervous system • Opioid analgesics • Action of OA’s: – Suppress neurotransmission of pain sensations – Main action in brain & spinal cord (opioid receptors) • Analgesics of choice for severe pain (examples). Please go through drug action, indication, side effects etc • Morphine • Pethidine • Tramadol Compiled by C Settley
  • 25. Pethidine • Has a rapid onset • Its analgesic effects are limited to a few hours in duration • It has a toxic metabolite that accumulates with repeated administration iow not suited for the treatment of chronic pain • Suited for post operative setting • Obstetrics, ureter colic and biliary obstruction Compiled by C Settley
  • 26. The difference between Analgesics and NSAID’S • An anti-inflammatory drug is one that reduces inflammation or swelling. • A pain killer, more properly called an analgesic, is a drug that stops you from feeling pain. • Some drugs do both, such as ibuprofen. But most drugs only do one or the other. Compiled by C Settley
  • 27. NSAID’S • Anti inflammatory effects • Antipyretic effects • Constriction of blood vessels • Examples: aspirin, diclofenac, paracetamol • Read through clinical application- pg 144-145 Compiled by C Settley