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Flashcards in Pharmacology Deck (73):
1

Pirenzipine is obsolete for PUD but is a ___

M1+3 muscarinic receptor antagonist

2

PPIs block ___ on ___ NOT in ____
eg.s =

H+K+ATPase on apical membrane NOT in tuberovesicles
omeprazole

3

PGE1 analogue co-admined with NSAIDS to prevent PUD
Its effects =

misoprostol
decreases basal and stimulated secretion of acid
maintains/increases mucus and HCO3- secretion

4

Effect of COX-1 inhibitors on stomach

decrease PGE2 which increases acid secretion and causes PUD

5

eg. of H2 receptor antagonist

ranitidine

6

Drugs that inhibit gastric acid secretion are used to treat __(3)

GORD/dyspepsia
PUD
acid hypersecretion - by Zollinger-Ellison(gastrinoma)/Cushings (causes increased vagal tone)

7

mucosal strengtheners eg.s
Mechanism:

sucralfate
bismuth chealate
= bind to ulcer base and form gel with mucus, increase mucosal blood flow (^H+ removal), mucus, HCO3- and PG production

8

5-HT3 receptor antagonist eg.s

ondansetron, palonosetron

9

5-HT3 receptor antagonists are for ___
not ___
side effects:

For: chemo and radio acutely (long term add corticosteroid and (neurokinin) NK receptor ant.), Post op N+V
NOT motion sickness/dopaminergic v
constipation + headaches

10

5-HT3 receptor antagonists block receptors in __+_

peripheral (gut) and central (AP) receptors

11

muscarinic ACh receptor antagonist anti emetic eg.s

hyoscine, scopolamine

12

hyoscine and scopolamine (M antagonists) are used for

prophlaxis/treatment of motion sickness
can be given as a trans-dermal patch

13

side effects of M antagonist anti-emetics

para ANS = blurred vision, urinary retention, xerostomia
sedation

14

H1 receptor antagonist anti-emetic egs

cyclizine, cinnarizine

15

H1 rec. ant. antiemetics are used for ___

prophylaxis/treatment of motion sickness
acute labyrinthitis
stomach irritants

16

H1 rec ant.s block receptors in _+_ and so may cause sedation. Not for emesis causes that directly affect ___

vestibular nuclei and NTS
not CTZ

17

anti-emetics: dopamine receptor antagonist eg.s

domperidone
metoclopramide

18

dopamine rec ant anti-emetics are for __
and not ___

drug induced and GI disorder causes of N+V
NOT motion sickness

19

mechanism of action of dopamine rec ant anti-emetics

block D2+3 in CTZ and have prokinetic effects on oeso, stomach and intestines

20

dopamine rec. ant.s are restricted in ___
metoclopramide/domperidone crosses the BBB and causes ___ side effects

children
metoclopramide
extra-pyramidal effects - eg. disorders of movement

21

Anti emetic used for severe vomiting with partial D2 blockade

Phenothiazines

22

NK1 receptor antagonist anti emetic eg. =
assumed to antagonise ____

aprepitant
substance P

23

aprepitant (NK1 r. ant) is used in combination with _+_ in acute phase of chemo for anti-emesis
and with ___ in delayed phase

dexamethasone and 5-HT3 r. ant - eg. ondansetron
dexamethasone

24

CB1 (cannabinoid) r. ant anti-emetic eg.

nabilone

25

nabilone(CB1 r. ant) is used for ____ emesis
decreases emesis that is due to ___ stimulation
side effects =

cytotoxic chemo when others dont work
CTZ
drowsy, dizzy, xerostomia, mood changes

26

Anti-emetics used for motion sickness

Muscarinic r. ant.s - hyoscine/scopolamine
H1 r. ant.s - cyclizine/cinnarizine

27

Anti-emetics for chemo. emesis

5-HT3 r. ant (ondansetron) with NK1 r. ant (aprepitant) and dexamethasone
nabilone (CB1 r. ant.) if others don't work

28

Slow acting laxatives =

bulk laxatives
methylcellulose, Ispaghula husk = indigestible polysaccharides

29

Fast acting laxatives =

osmotic laxatives
Mg sulfate/hydroxide, lactulose PO
Na citrate PR

30

Stimulant purgatives eg.s

biasacodyl PO/suppository, senna, Na picosulfate

31

Faecal softener purgatives eg.s

docusate Na PO
arachis oil enema

32

To reverse warfarin give __ then ___

vitamin K
Prothrombin Complex Concentrate (contains 2, 7, 9 and 10)

33

In liver disease coagulopathy(prone to bleeding) give ___
however if is significant biliary obstruction the give ___ because it has ___

vitamin K first line
fresh frozen plasma - contains all clotting factors

34

Don't give ___ to bleeding ascitic patient as makes it worse

saline

35

Gentamicin can't be given___ (route)

PO

36

antibiotic for pseudomonas =

quinolones eg. ciprofloxacin PO

37

omeprazole and lansoprazole are __
indicated for

PPIs
PUD
GORD/dyspepsia
H. pylori eradication
Zollinger-Ellison

38

Reduces pepsinogen to pepsin
irreversibly blocks H+K+ATPase on canalicular membrane =

PPI
omeprazole

39

PPIs interact with ___ and ___ action of clopidogrel and ___ action of phenytoin and warfarin

cytochrome P450 isoenzymes
decrease clopidogrel
increase phenytoin and warfarin

40

Administration of PPIs =

PO od morning 30-60mins before food
IV for reccurent ulcer bleeds in high risk pt.s

41

PPIs may increase risk of ___ infection and disguise symptoms of

risk of C. diff
disguise gastric ca

42

Ranitidine is a

H2 receptor antagonist

43

H2 receptor antagonists are bettter than PPIs in this case

reducing acid pre-op as have a faster onset of action

44

loperamide and codeine phosphate are ___

anti-motility drugs

45

loperamide is indicated in

acute diarrhoea and IBS diarrhoea (symptom control only)

46

Mechanism of action of loperamide and codeine phosphate

agonise μ opiod receptors on enteric neurones > increase tone and rhythmic contraction of intestine, contrict SM sphincters and decrease peristalsis
also antisecretory

47

Contraindications for anti-motility drugs -

acute UC (megacolon and perf risk)
dysentry
C.diff colitis (therefore not for any hosp acquired diarr)
not if under 4yo

48

loperamide is administered ___

PO as capsule/tablet

49

Ispaghula husk is a

bulk laxative

50

Contraindications to bulk laxatives =

at risk/have intestinal obstruction/ileus
post-op constipation (may have ileus)

51

Administer bulk laxatives __ at __ with ___

PO
mealtimes
lots of water

52

lactulose and phosphate enemas are ___

osmotic laxatives

53

used in hepatic encephalopathy
because reduces ammonia reabsorption in gut by decreasing transit time
acidifies stool
inhibits proliferation of NH3 producing bacteria

lactulose

54

If faecal impaction try ___ before ___enema

stimulant eg. glycerol suppository
phosphate enema

55

Senna, bisocodyl, docusate Na and glycerol suppository are

stimulant laxatives

56

increase H2O and electrolyte secretion from colonic mucosa and stimulate peristalsis =

stimulant laxatives eg. senna

57

doperamide and metoclopramide are

D2 (dopamine) receptor anatagonist anti-emetics

58

cyclizine and cinnarizine are

H1 receptor antagonist anti-emetics

59

Mechanism of action of H1 receptor antagonist eg. cyyclizine

block H1 rec in VC and elsewhere in CNS (sedation)
block M1 rec in vestibular apparatus

60

side effects of H1 rec ants eg. cyclizine

xerostomia
sedation
transient tachy (if IV)

61

H1 rec ant.s treat nausea and vom in

vertigo, motion sickness and post-op

62

D2 rec ants treat nausea and vomiting in

esp if reduced gut motility as are pro-motility
in drug and chemo induced
vomiting in emergency hormonal contraception.

63

procloperazine =

phenothiazine anti-emetic

64

mechanism of action of procloperazine =

comp ant of D2, H1 and M1 receptors in VC, vestibular system and ENS

65

indications for procloperazine

nausea and vom (others preferred though) vertigo and chemo related
psychiatric disorders eg. schizophrenia

66

Contraindications for H1 rec ant anti emetics

at risk of hepatic encephalopathy
prostatic hyperplasia

67

contraindications for procloperazine

severe liver disease
prostatic hyperplasia
reduce dose in elderly as may lead to confusion

68

ondansetron is a

5-HT3 receptor antagonist anti-emetic

69

alosetron indication =

diarrhoea predominant IBS in females

70

indications for 5-HT3 rec ants =

nausea and vom chemo/radio induced/post op after general anaesthesia

71

high dose ondansetron can cause what side effect?

long QT syndrome

72

Contraindications for ondansetron

severe/prolonged constipation
intestinal obstruction/stricture
toxic megacolon
ischaemic colitis
Crohn's
UC
diverticulitis

73

Mechanism of action of ondansetron

comp ant 5-HT3 rec in CTZ, NTS and vagal afferent terminals in GI tract
Stop CTZ sensing emetogenics, stop visceral afferents from GI tract stimulating NTS in infection/chemo