Drugs COPY Flashcards

1
Q

Give examples of proton pump inhibitors

A

Omeprazole, lansoprazole and pantoprazole

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2
Q

Explain the MoA of PPIs

A

Irreversibly binding to and inhibition of the ATPase of gastric parietal cells. (Final common pathway)
This reduces acid secretion.

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3
Q

State the major indications for PPIs

A

Prevention and treatment of peptide ulcer disease
Symptomatic relief of dyspepsia
Treatment of gastro-oesophageal reflux disease
Part of triple therapy for eradication of H.pyolri

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4
Q

What are the adverse effects associated with PPIs

A
Diarrhoea (Lansoprazole in particular)
Headache
Abdominal pain
Nausea
Fatigue
Dizziness
All relativly uncommon
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5
Q

What are the associated risks of PPIs

A

Increased risk of C.diff infection
Rebound hypersecretion upon discontinuation
Can mask the sign of gastric cancer

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6
Q

Give examples of histamine type 2 receptor agonists

A

Ranitidine

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7
Q

Explain the MoA of histamine type 2 receptor agonists

A

Competitive antagonism of the H2 receptors located on the basolateral membrane of parietal cells. (This is from enterochromaffin-like cells)
This reduces stimulation to the proton pumps, in turn reducing the acid secretion

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8
Q

State the major indications for histamine type 2 receptor agonist

A

Prophylaxis and treatment of peptic ulcer disease

Symptomatic relief of dyspepsia and GORD (PPIs prefered)

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9
Q

What are the adverse effects associated with histamine type 2 receptor agonist

A
Less than those of PPIs
Diarrhoea and less commonly constipation
Headache
Abdominal pain
Dizziness
All uncommon
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10
Q

What risks are associated with histamine type 2 receptor agonist

A

Can mask signs of gastric cancer

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11
Q

Give examples of Alginates & Antacids

A

Gaviscon, Peptac, Mucogel

Prescribed as brand names

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12
Q

Explain the MoA of Alginates & Antacids

A

Act as a buffer to the gastric contents

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13
Q

State the major indications for Alginates & Antacids

A

Gastro-oesophageal reflux disease for symptomatic relief

Dyspepsia for a short term relief

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14
Q

What are the adverse effects associated with Alginates and Antacids

A

Non recorded

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15
Q

What are the risks associated with Alginates and Antacids

A

High sodium and potassium so should be avoided in the salt restricted diet

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16
Q

Give examples of antimuscarinic drugs

A

Hyoscine butyl-bromide

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17
Q

Explain the MoA of antimuscarinic drugs

A

A competitive antagonist of muscarinic ACh receptors (M3) and thus oppose the action of the parasympathetic innervation to the gut.
This reduces spasm of the smooth muscle peristalsis.

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18
Q

State the major indication for antimuscarinic drugs

A

To relieve smooth muscle spasm in IBS. (symptomatic relief)

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19
Q

What are the adverse effects associated with antimuscarinic drugs

A
Suppression of the parasympathetic division of the ANS.
Tachycardia
Dry mouth
Constipation
Urinary retention
Blurred vision
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20
Q

What are the risks associated with antimuscarinic drugs

A

Used in caution with cardiac arrhythmias

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21
Q

Give examples of antimotility drugs

A
Loperamide (prefered due to not crossing the BBB, no narcotic effect)
Codeine phosphate (prefered if analgesia is also needed, mostly in palliation)
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22
Q

Explain the MoA of antimotility drugs

A

Action to reduce the peristaltic action whilst increasing the tone and rhythmic contractions of the intestine.

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23
Q

State the major indications for antimotility drugs

A

Treatment of acute diarrhoea for symptomatic relief (infective gastroenteritis normally)
Symptomatic relief of diarrhoea associated with IBS

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24
Q

What are the adverse effects associated with antimotility drugs

A

Constipation
Abdominal cramping
Flatulence

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25
Q

What are the contradictions to the use of antimotility drugs

A

Acute ulcerative colitis
Acute bloody diarrhoea
C.diff colitis

Hospital setting with an unknown aetiology

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26
Q

Give examples of aminosalicylates

A

Mesalazine

Balsalazide

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27
Q

Explain the MoA of aminosalicylates

A

These drugs break down to form 5-ASA

5-ASA acts locally as an anti-inflammatory and immunosuppressant.

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28
Q

State the major indications for aminosalicylates

A

First line treatment of mild to moderate ulcerative colitis

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29
Q

What are the adverse effects associated with aminosalicylates

A

Commonly causes GI upset and headaches

Possible blood abnormalities, leading to renal complications

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30
Q

What are the contraindications for aminosalicylates

A

Avoid in use for those with aspirin hypersensitivity

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31
Q

Give examples of bulk-forming laxatives

A

Ispagula husk

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32
Q

Explain the MoA of bulk-forming laxatives

A

Hydrophilic agents so osmotically draw water to the stool increasing its bulk which in turn stimulates peristalsis
Faecal consistency is improved
(Note that an important fluid ingestion is important for this group as they take 2-3 days to impose action)

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33
Q

State the major indications for bulk-forming laxatives

A

Constipation adn faecal impaction

Mild chronic diarrhoea assocaites with diverticular disease or IBS

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34
Q

What are the adverse effects of bulk-forming laxatives

A

Abdominal distention
Flatulence
Rarely cause faecal impaction and GI obstruction

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35
Q

What are the contraindications of bulk-forming laxatives

A

Intestinal obsution

Avoid in ileus

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36
Q

Give examples of osmotic laxatives

A

Lactulose
Macrogols
Phosphate/citrate enemas

37
Q

Explain the MoA of osmotic laxatives

A

Osmotically active agents which attract water into the stool increasing the bulk which in turn stimulates peristalsis.
Lactulose reduces ammonia absorption by decreasing the transit time which acidifies the stool and inhibits prolifiration of ammonia produces bacteria which is helpful in patients with liver failure

38
Q

State the major indications for osmotic laxatives

A

Constipation and faecal impaction
Bowel preparation before endoscopy/surgery
Hepatic encephalopathy

39
Q

What are the adverse effects associated with osmotic laxative

A

Abdominal cramping
Nausea
Flatulence
Diarrhoea

Phosphate enemas cause local irritation

40
Q

What are the contraindications for osmotic laxative use

A

Intestinal obstruction (risk of perforation)

Phosphate enemas are cautioned in heart failure, ascites and electrolyte abnormalities

41
Q

Give examples of stimulant laxatives

A
Senna
Bisocodyl
Glycerol suppository
Docusate sodium
Sodium picosulfate
42
Q

Explain the MoA of stimulant laxatives

A

Increasing the electrolyte (thus water) secretion from the colonic mucosa.
Colonic content increases which in turn stimulates peristalsis, for some agents (E.g senna) this is a direct action of the enteric nervous system.

43
Q

State the major indications for stimulant laxatives

A
Constipation
Faecal impaction (when given as a suppository)
44
Q

What are the adverse effects associated with stimulant laxatives

A

Abdominal pain
Abdominal cramps
Diarrhoea

Prolonged use may lead to an irreversible atonic colon and reversible melanosis coli

45
Q

What are the contradications for stimulant laxatives

A

Intestinal obstuction (risk of perforation)

Avoided in patients with anal fissures and haemorrhoids

46
Q

Give examples of dopamine (D2) receptor antagonists

A

Domperidone

Metoclopramide

47
Q

Explain the MoA of dopamine (D2) receptor antagonists

A

Act as an antagonist to the dopamine D2 receptors which in the gut relaxes the stomach and LOS and disrupts gastroduodenal coordination

48
Q

What are the major indications for dopamine (D2) receptor antagonists

A

Treatment of nausea and vomiting
- Particularly when reduced gut motility is evident
Treatment of gastro-oesophageal reflux disease, as add on for those don’t respond to PPIs/H2 receptor antagonists

49
Q

What are the adverse effects associated with dopamine (D2) receptor antagonists

A

Diarrhoea most commonly

50
Q

What are the contraindications of dopamine (D2) receptor antagonists

A

Avoided in GI obstruction and perforation

Metoclopramide is best avoided in younger people (children and teens)

51
Q

Give examples of histamine (H1) receptor antagonists

A

Cyclizine

Cinnarazine

52
Q

Explain the MoA of histamine (H1) receptor antagonsits

A

Competitive antagonism of the H1 receptors in the vomiting centre
An additional block of M1 receptors of the vestibular apparatus also contributes

53
Q

State the major indications for histamine (H1) receptor antagonists

A

Treatment of nausea and vomiting, in particular, motion sickeness
Used for post-operative nausea and vomiting [PONV]

54
Q

What are the adverse effects associated with histamine (H1) receptor antagonists

A

Drowsiness and sedation
Dry mouth
Transient tachycardia if given IV

55
Q

What are the contraindications for histamine (H1) receptor antagonists

A

Patients at risk of hepatic encephalopathy

Prostatic hyperplasia

56
Q

Give examples of phenothiazines

A

Procloperazine

57
Q

Explain the MoA of phenothiazines

A

Competitive inhibition fo D2, H1 and M1 receptors of the vomiting centre to reduce nausea

58
Q

State the major indications for phenothiazines

A

Treatment of nausea and vomiting in particular vertigo and chemotherapy-induced nausea and vomiting (other classes are prefered)
Psychiatric disorders

59
Q

What are the adverse effects associated with phenothiazines

A

Drowsiness
Postural hypotension

Long term treatment may lead to tardive dyskinesia or parkinsonism
QT prolongation may occur

60
Q

What are the contraindications of phenothiazines

A

Avoid in severe liver disease (risk of hepatotoxicity)

Avoid in cases of prostatic hyperplasia

61
Q

Give examples of 5-HT3 receptor antagonists

A

Ondansetron

62
Q

Explain the MoA of 5-HT3 receptor antagonists

A

Competitive antagonism of 5-HT3 at the CTZ and NTS to reduce the stimulation of the vomiting centre.

63
Q

State the major indications for 5-HT3 receptor antagonists

A

Treatment of nausea and vomiting, namely that associated with chemo and radiotherapy along with following surgery involving general anaesthetic

64
Q

What are the adverse effects associated with 5-HT3 receptor antagonists

A

Consitpation most commonly

Diarrhoea and headaches less commonly

65
Q

What are the contraindications to 5-HT3 receptor antagonists

A
Severe or prolonged constipation
Intestinal obstruction
Strictures
Toxic megacolon
Ischaemic colitis
Crohn's disease
Ulcerative colitis
Diverticulitis

Ondansetron prolongs the QT interval so is best avoided in those with a prolonged QT interval

66
Q

Omeprazole

A

PPI

67
Q

Lansoprazole

A

PPI

68
Q

Ranitidine

A

Histamine type 2 (H2) receptor antagonist

Anti-acid

69
Q

Gaviscon

A

Compound alginate (alginate and antacid)

70
Q

Peptac

A

Compound alginate (alginate and antacid)

71
Q

Hyoscine butyl-bromide

A

Antimuscarinic, antispasmodic

72
Q

Loperamide

A

Antimotility drugs

73
Q

Codeine phosphate

A

Antimotility drugs

74
Q

Mesalazine

A

Aminosalicylate (5-ASA)

75
Q

Balsalazide

A

Aminosalicylate (5-ASA)

76
Q

Ispagula husk

A

Bulk-forming laxative

77
Q

Lactulose

A

Osmotic laxative

78
Q

Macrogols

A

Osmotic laxative

79
Q

Phosphate/citrate enemas

A

Osmotic laxative

80
Q

Senna

A

Stimulant laxative

81
Q

Glycerol suppository

A

Stimulant laxative

82
Q

Docusate sodium

A

Stimulant laxative

83
Q

Sodium picosulfate

A

Stimulant laxative

84
Q

Domperidone

A

Dopamine (D2) receptor antagonist, anti emetic

85
Q

Metoclopramide

A

Dopamine (D2) receptor antagonist, anti emetic

86
Q

Cyclizine

A

Histamine (H1) receptor antagonist, antiemetic

87
Q

Cinnarizine

A

Histamine (H1) receptor antagonist, antiemetic

88
Q

Prochlorperazine

A

Phenothiazines, antiemetic

89
Q

Ondansetron

A

5-HT3 receptor antagonists, antiemetic