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Y4 Gastrointestinal > GI related drugs & side effects > Flashcards

GI related drugs & side effects Flashcards

1
Q

What is the mechanism of action of ‘setrons’ e.g. ondansetron, palonosetron?

A

They block peripheral and central 5-HT3 receptors

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2
Q

When are 5-HT3 receptor antagonists – ‘setrons’ used ?

A

To suppress chemotherapy- and radiation-induced emesis and post-operative nausea and vomiting

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3
Q

What are the potential side effects of 5-HT3 receptor antagonists – ‘setrons’ ?

A

Generally well tolerated – most common unwanted effects are constipation and headaches

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4
Q

What are the main contraindications of of 5-HT3 receptor antagonists – ‘setrons’ ?

A

Severe, or prolonged, constipation, intestinal obstruction, stricture, toxic megacolon, ischaemic colitis, Crohn’s disease, ulcerative colitis, diverticulitis

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5
Q

What is the mechanism of action of Muscarinic acetylcholine receptor antagonists (hyoscine)?

A

Block muscarinic acetylcholine receptors at multiple sites

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6
Q

What are Muscarinic acetylcholine receptor antagonists (hyoscine) used for ?

A
  1. Used for prophylaxis and treatment of motion sickness
  2. To relieve smooth muscle spasm in IBS
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7
Q

What are the main side effects of Muscarinic acetylcholine receptor antagonists (hyoscine)?

A

Have numerous unwanted effects:

  • blurred vision
  • urinary retention
  • dry mouth
  • centrally-mediated sedation
  • tachycardia
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8
Q

What is the mechanism of action of Histamine H1 receptor antagonists (e.g. cyclizine, cinnarizine + many others)

A

Blockade of H1 receptors in vestibular nuclei and NTS

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9
Q

What are Histamine H1 receptor antagonists (e.g. cyclizine, cinnarizine + many others) used for ?

A

Used for prophylaxis and treatment of motion sickness and acute labyrinthitis and nausea and vomiting caused by irritants in the stomach.

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10
Q

What are the main side effects of Histamine H1 receptor antagonists (e.g. cyclizine, cinnarizine + many others)?

A
  • Generally cause CNS depression and sedation – drowsiness
  • Dry mouth
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11
Q

When is the use of H1 receptor antagnosits avoided ?

A

Should be avoided in patients at risk of hepatic encephalopathy, or those with prostatic hyperplasia (anti-muscarinic action increases the likelihood of urinary obstruction)

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12
Q

What is the mechanism of action of Dopamine receptor antagonists (e.g. domperidone and metoclopramide)?

A
  • Centrally block dopamine D2 (and D3) receptors in the CTZ
  • Peripherally exert a prokinetic action on the oesophagus, stomach and intestine
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13
Q

What are Dopamine receptor antagonists (e.g. domperidone and metoclopramide) used for ?

A

Used for drug-induced vomiting (e.g. cancer chemotherapy, treatment of Parkinson’s disease with agents stimulating dopaminergic transmission) and vomiting in GI disorders.

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14
Q

What are the main side effects of Dopamine receptor antagonists (e.g. domperidone and metoclopramide)?

A

Diarrhoea

Domperidone does not cross the blood brain barrier and is less likely to result in the many unwanted effects of metoclopramide [e.g. disorders of movement (extrapyramidal effects) - can result in parkinsonism]

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15
Q

When is use of dopamine receptor antagnosits contraindicated ?

A

Both should be avoided in gastrointestinal obstruction and perforation

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16
Q

What are the 2 main PPI’s used ?

A

Omeprazole, lansoprazole

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17
Q

What is the mechanism of action of PPI’s ?

A

Cause irreversible blockade of H+/K+ ATPase of the gastric parietal cell.

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18
Q

What are the 3 major indications for the use of PPI’s?

A
  1. Prevention and treatment of peptide ulcer disease (DU, or GU)
  2. Symptomatic relief of dyspepsia and GORD
  3. Eradication of H. pylori infection (omeprazole in conjunction with Abx)
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19
Q

What are the main side effects of PPI’s?

A
  • Diarrhoea (particularly lansoprazole),
  • headache
  • abdominal pain
  • nausea
  • fatigue
  • dizziness
  • Increase risk of C.diff infection & osteoporosis
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20
Q

What is the mechanism of action of Ranitidine?

A

H2 receptor antagonist

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21
Q

What are the 2 main indications for the use of Ranitidine ?

A
  1. Prevention and treatment of peptic ulcer disease (DU, or GU, although PPIs are preferred)
  2. Symptomatic relief of dyspepsia (may be sufficient) and GORD (GORD; although PPIs are preferred in severe cases)
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22
Q

What are the main side effects of ranitidine ?

A
  • Side effects less commmon but similar to PPI’s
  • Diarrhoea
  • Headache
  • Abdo pain
  • Dizziness
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23
Q

What are the 3 main Alginates and Antacids used ?

A

Gaviscon, Peptac & Mucogel

24
Q

What is the mechanism of action of alginates & antacids ?

A

They act as buffers that increase the pH of gastric juice and additionally inactivate pepsin

25
Q

What are the main indications for the use of alginates & antacids ?

A

GORD & dyspepsia

26
Q

What are the main side effects of alginates & antacids ?

A

Diarrhoea, or constipation

27
Q

What are the 2 main antimotility drugs ?

A

Loperamide, codeine phosphate

28
Q

What is the mechanism of action of antimotility drugs?

A

synthetic opioid with agonist activity at μ opioid receptors (inhibiting peristalsis & causing a constipating effect)

29
Q

What are the main indications for the use of antimotlity drugs ?

A
  1. Treatment of acute diarrhoea for symptomatic relief (usually in the context of gastritis caused by viral, or bacterial, infection)
  2. Symptomatic relief of diarrhoea associated with IBS
  3. Analgesia for acute, or moderate, pain (codeine)
30
Q

What are the main side effects of antimotility drugs ?

A
  1. Constipation, abdominal cramping and flatulence
  2. Inappropriate inhibition of peristalsis may trigger serious conditions (==> contraindications to their use)
31
Q

What are the contraindications to the use of antimotility drugs ?

A
  1. Acute ulcerative colitis (risk of megacolon and perforation)
  2. Acute bloody diarrhoea (dysentery)
  3. Clostridium difficile colitis
32
Q

What are the 2 main Aminosalicylates (5-ASA) drugs?

A

Mesalazine & sulfasalazine

33
Q

What is the mechanism of action of aminosalicylates ?

A

Mechanism of action is not fully understood but 5-ASA may inhibit prostaglandin synthesis

34
Q

What are the main indications for the use of aminosalicylates ?

A
  1. Mesalazine and Sulfasalazine are first line treatment of mild/moderate ulcerative colitis
  2. Sulfasalazine is can be used in combination therapy as a disease modifying anti-rheumatic drug (DMARD) in RA. Mesalazine has no role in this context
35
Q

What are the side effects of aminosalicylates ?

A
  • Mesalazine = GI upset, headache, agranulocytosis, pancreatitis, interstitial nephritis
  • Sulphasalazine = same as mesalazine + ashes, oligospermia, headache, Heinz body anaemia, megaloblastic anaemia, lung fibrosis
36
Q

What is the main contraindication to the use of aminosalicylates ?

A

Avoid use in patients with aspirin (salicylate) hypersensitivity

37
Q

What is the main bulk forming laxative ?

A

Ispagula husk

38
Q

How do bulk forming laxatives work?

A

By osmosis, water is attracted to the stool, increasing bulk and stimulating peristalsis.

39
Q

What are the 2 main indications for the use of bulk forming laxatives ?

A
  1. Constipation and faecal impaction
  2. Mild chronic diarrhoea associated with diverticular disease, or IBS
40
Q

What are the main possible side effects of bulk forming laxatives ?

A

Abdominal distension and flatulence

41
Q

When are bulk forming laxatives contraindicated ?

A

Should not used in patients at risk of, or suffering from, intestinal obstruction. Avoid in ileus

42
Q

What are the 3 main osmotic laxatives ?

A

Lactulose, macrogols, and phosphate (or citrate) enemas

43
Q

What is the mechanism of action of osmotic laxatives ?

A

By osmosis, water is attracted to the stool, increasing bulk and stimulating peristalsis

44
Q

What are the 3 main indications for use of osmotic laxatives ?

A
  1. Constipation and faecal impaction
  2. Bowel preparation before endoscopy, or surgery
  3. Hepatic encephalopathy
45
Q

What are the main adverse effects of osmotic laxatives ?

A
  • Abdominal cramps
  • Nausea
  • Flatulence
  • Predictably diarrhoea
46
Q

What is the main contraindication to the use of osmotic laxatives ?

A

Intestinal obstruction (risk of perforation)

47
Q

What are the main stimulant laxatives ?

A

Senna, bisocodyl, glycerol suppository, docusate sodium, sodium picosulfate

48
Q

What is the mechanism of action of stimulant laxatives ?

A
  1. Increase electrolyte and thus water secretion from the colonic mucosa.
  2. Colonic content is increased stimulating peristalsis
49
Q

What are the 2 main indications for the use of stimulant laxatives ?

A
  1. Constipation
  2. Faecal impaction (as suppository)
50
Q

Whata are the main side effects of stimulant laxatives ?

A
  • Abdominal pain and cramping.
  • Diarrhoea
51
Q

What is the main contraindication to the use of stimulant laxatives ?

A

Intestinal obstruction (risk of perforation)

52
Q

What is the main Antiemetics, phenothiazines?

A

Procloperazine

53
Q

What is the mechanism of action of Antiemetics, phenothiazines?

A

Complex involving competitive antagonism of dopamine D2, histamine H1 and muscarinic M1) receptors in the vomiting centre, vestibular system and peripherally in the gut

54
Q

What are the 2 main indications for the use of Antiemetics, phenothiazines?

A
  1. Psychiatric disorders (e.g. schizophrenia)
  2. Treatment of nausea and vomiting in a wide range of conditions, particularly vertigo and sometimes in chemotherapy-induced nausea and vomiting (CINV). However, due to their adverse effect profile, other classes of antiemetic are generally preferred
55
Q

What are the main side effects of Antiemetics, phenothiazines?

A
  • Most commonly drowsiness and postural hypotension.
  • extrapyramidal symptoms (due to D2 block) are troublesome - . Long term treatment may result in tardive dyskinesia, or Parkinsonism
  • QT interval prolongation
56
Q

What is the main contraindication of Antiemetics, phenothiazines?

A

Avoid in severe liver disease (potential for hepatotoxicity)

Y4 Gastrointestinal (28 decks)

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