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GI > PHARMACOLOGY > Flashcards

PHARMACOLOGY Flashcards

1
Q

mechanism of PPIs

A

irreversible inhibition by covalent modification of the gastric gland parietal cell H+/K+ ATPase present in the apical membrane

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2
Q

where are PPIs activated?

A

in the acidic environment of the canaliculus

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3
Q

indications for PPIs

A
  1. peptic ulcer disease (prevention and treatment)
  2. dyspepsia and GORD (symptomatic relief)
  3. eradication of H pylori
  4. Zollinger-Ellison syndrome
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4
Q

give examples of PPIs

A

omeprazole

lansoprazole

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5
Q

adverse effects of PPIs

A
  • diarrhoea
  • headache
  • abdominal pain
  • fatigue
  • dizziness
    ? increased risk of C diff
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6
Q

what might prolonged therapy with a PPI result in?

A

rebound acid hyper secretion upon discontinuation

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7
Q

risk associated with long term therapy using PPIs in the elderly

A

increased risk of bone fracture

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8
Q

what happens due to interaction of PPIs with cytochrome p450 isoenzymes?

A

decrease the anti platelet activity of clopidogrel

increase the effect of phenytoin and warfarin

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9
Q

administration of PPIs

A

once daily in the morning PO before food

IV to treat recurrent ulcer bleeding in high risk patients

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10
Q

example of histamine type 2 receptor antagonists

A

ranitidine

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11
Q

mechanism of action of H2 receptor antagonists

A

competitive antagonism of the H2 receptor located on the basolateral membrane of acid secreting parietal cells of the gastric glands

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12
Q

PPIs are more effective than H2 receptor antagonists

A

TRUE

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13
Q

indications for H2 receptor antagonists

A
  1. peptic ulcer disease (prevention and treatment)

2. dyspepsia and GORD (symptomatic relief)

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14
Q

adverse effects of H2 receptor antagonists

A
  • diarrhoea
  • less commonly constipation
  • headache
  • abdominal pain
  • dizziness
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15
Q

what may H2 receptor antagonists and PPIs disguise the symptoms of?

A

gastric cancer

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16
Q

administration of H2 receptor antagonists

A

PO twice daily

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17
Q

name anti motility drugs

A

loperamide

codeine phosphate

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18
Q

mechanism of action of loperamide

A

synthetic opioid with agonist activity at u opioid receptors expressed by enteric neurones of the GIT

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19
Q

effect of loperamide and codeine

A

increases the tone and rhythmic contractions of the intestine
constricts smooth muscle sphincters
inhibits peristalsis
= constipating

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20
Q

when is codeine preferred over loperamide?

A

when additional analgesia is required

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21
Q

indications for anti motility drugs

A
  1. acute diarrhoea (symptomatic relief)
  2. diarrhoea associated with IBS (symptomatic relief)
  3. analgesia for acuter moderate pain
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22
Q

adverse effects of anti motility drugs

A

constipation
abdominal cramping
flatulence

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23
Q

contraindications for anti motility drugs

A

acute UC (risk of megacolon and perforation)
acute bloody diarrhoea (dysentery
C diff colitis

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24
Q

when can anti motility drugs be prescribed in the hospital setting?

A

once the probable cause has been identified and c diff is excluded

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25
Q

who should anti motility drugs be prescribed to?

A

children under 4

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26
Q

administration of anti motility drugs

A

PO as capsule or tablet

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27
Q

name a bulk forming laxative

A

ispagula husk

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28
Q

what are bulk laxatives?

A

hydrophilic agents which are indigestible

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29
Q

mechanism of action of bulk laxatives

A

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

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30
Q

what is important for the action of bulk laxatives?

A

adequate fluid ingestion

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31
Q

indications for bulk laxatives

A
  1. constipation and faecal impaction

2. mild chronic diarrhoea associated with diverticular disease or IBS

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32
Q

adverse effect of bulk laxatives

A

rarely may cause faecal impaction and GI obstruction

33
Q

when should bulk laxatives be avoided?

A

patients at risk of or suffering from intestinal obstruction
ileus

34
Q

administration of bulk laxatives

A

PO (as powders, granules, tablets)

around meal times with plenty of water

35
Q

name osmotic laxatives

A

lactulose
macrogols
citrate and phosphate enemas

36
Q

what are osmotic laxatives?

A

osmotically active agents which are neither digested nor absorbed

37
Q

mechanism of action of osmotic laxatives

A

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

38
Q

why is lactulose helpful in patients with renal failure?

A

reduces ammonia absorption by decreasing transit time, acidifying the stool and inhibiting the proliferation of ammonia producing bacteria

39
Q

indications for osmotic laxatives

A
  1. constipation and faecal impaction
  2. bowel preparation before endoscopy or surgery
  3. hepatic encephalopathy
40
Q

adverse effects of phosphate enemas

A

local irritation and electrolyte disturbance

41
Q

contraindications for osmotic laxatives

A

intestinal obstruction (risk of perforation)

42
Q

when should phosphate enemas be used with caution?

A

patients with heart failure and where electrolyte disturbances are present

43
Q

administration of osmotic laxatives

A

PO as powders dissolved in water or liquids with or without food
as enema, once only or as required but no more than once daily

44
Q

name stimulant laxatives

A

Senna
bisocodyl
glycerol suppository
docusate sodium

45
Q

mechanism of action of stimulant laxatives

A

increase water and electrolyte secretion from the colonic mucosa
colonic content is increased by stimulating peristalsis

46
Q

what additional action does decussate sodium have?

A

faecal softening

47
Q

indications for stimulant laxatives

A
  1. constipation

2. faecal impaction (as suppository)

48
Q

adverse effects of stimulant laxatives

A

prolonged use may cause an irreversible atonic colon and reversible melanosis coli

49
Q

contraindications for stimulant laxatives

A

intestinal obstruction (risk of perforation)

50
Q

when should rectal preparations of stimulant laxatives be avoided?

A

in patients with anal fissures or haemorrhoids

51
Q

administration of stimulant laxatives

A

for constipation PO

for faecal impaction, as suppository, once only or as required but no more than once daily

52
Q

name dopamine D2 receptor antagonists

A

domperidone

metoclopramide

53
Q

mechanism of action of domperidone

A

antagonist of dopamine D2 receptors in the CTZ but does not cross the BBB

54
Q

additional action of metoclopramide

A

additional activity as an antagonist at 5-HT3 receptors and as an agonist at 5-HT4 receptors

55
Q

indications for D2 receptor antagonists

A
  1. treatment of nausea and vomiting particularly when reduced gut motility is evident eg drug or chemotherapy induced nausea and vomiting
  2. treatment of GORD (as an add-on to patients who do not respond to H2 antagonists or PPIs)
  3. vomiting associated with emergency hormonal contraception
56
Q

adverse effects of D2 receptor antagonists

A
  • diarrhoea

- metoclopramide may cause extra pyramidal symptoms

57
Q

contraindications to D2 receptor antagonists

A

GI obstruction and perforation

58
Q

when is metoclopramide best avoided?

A

in children and young adults in which extra pyramidal side effects are most common

59
Q

administration of D2 receptor antagonists

A

PO up to three times a day

metoclopramide is available IV, IM or injection

60
Q

name histamine H1 receptor antagonists

A

cyclizine

cinnarazine

61
Q

mechanism of action of H1 receptor antagonists

A

competitive antagonism of H1 receptors in the VC

additional block of muscarinic ACh receptors in the vestibular apparatus probably contributes to their effectiveness

62
Q

indications for H1 receptor antagonists

A
  1. motion sickness and vertigo

2. post operative nausea and vomiting

63
Q

adverse effects of H1 receptor antagonists

A
  • drowsiness and sedation
  • reduce saliva leading to dry mouth
  • IV may cause a transient tachycardia
64
Q

when should H1 receptor antagonists be avoided?

A

in patients at high risk of hepatic encephalopathy or those with prostatic hyperplasia

65
Q

administration of H1 receptor antagonists

A

PO regularly, or as required

cyclizine may be given IM or IV or injection

66
Q

name a phenothiazine

A

procloperazine

67
Q

mechanism of action of phenothiazine

A

involves competitive antagonism of D2, H and M1 receptors in the vomiting centre, vestibular system and peripherally in the gut

68
Q

indications for phenothiazines

A
  1. vertigo
  2. sometimes chemo induced nausea and vomiting
  3. schizophrenia
69
Q

adverse effects of phenothiazines

A
  • drowsiness
  • postural hypertension
  • long term treatment = tardive dyskinesia or Parkinsonism
  • QT interval prolongation
70
Q

when to avoid phenothiazines?

A

in severe liver disease (potential for hepatotoxicity)

in prostatic hyperplasia

71
Q

when to reduce the dose of phenothiazines?

A

in elderly patients as they may be liable to confusion

72
Q

administration of phenothiazines

A

orally or deep IM for acute episode with further oral doses as necessary

73
Q

name the 5-HT3 receptor antagonist

A

ondansetron

74
Q

mechanism of action of 5-HT3 receptor antagonists

A

competitive antagonism of inotropic 5-HT3 receptors which are located in the CTZ, NTS and also peripherally on the terminals of vagal afferent fibres innervating the GI tract

75
Q

indications for 5HT3 receptor antagonists

A
  1. chemo and radiotherapy nausea and vomiting
  2. post operative nausea and vomiting
  3. IBS
  4. hyperemesis gravidarum
76
Q

adverse effects of 5HT2 receptor antagonists

A
  • constipation
  • diarrhoea
  • headaches
77
Q

contraindications for 5HT3 receptor antagonists

A 
severe or prolonged 
constipation
intestinal obstruction 
stricture 
toxic megacolon 
ischaemic colitis 
Crohn's disease
UC 
diverticulitis
78
Q

when should ondansetron be avoided?

A

patients with a prolonged QT interval or who are taking drugs which prolong the QT interval

79
Q

administration of andansetron

A

PO
PR
IM
IV

GI (9 decks)

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