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PCM Exam 4 > GI Drugs 1 > Flashcards

GI Drugs 1 Flashcards

1
Q

what are the second generation H2 receptor antagonists?

A

ranitidine, famotidine and nizatidine; better than the first generation H2 receptor antagonist which is cimetidine because 2nd generation has no anti-adrenergic or CNS adverse effects

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2
Q

motilin in GI peristalsis ↑ GI motility by binding to ______ or _______

A
  • binds directly to the motilin receptor on the muscularis layer
    OR
  • binds to the enteric neuron which then releases acetylcholine that binds to the M1 receptor on the muscularis layer
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3
Q

triple therapy for H. Pylori eradication lasts for ______ days. what are the drugs used in triple therapy

A

10-14 days

clarithromycin + amoxicillin + PPI
OR
clarithromycin + metronidazole + PPI

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4
Q

what receptors does metoclopramide work on?

A
  • D2 (dopamine) receptor ANTAGONIST
  • vagal and central 5HT3 ANTAGONIST
  • 5 HT4 agonist

effects confined to the upper digestive tract

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5
Q

why can’t you give misoprostol to pregnant patient?

A

it has abortifacient effects (cause uterine contractions)

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6
Q

what receptors are involved in the motion sickness cause of vomiting

A

H1 and muscarinic receptors in cerebellum

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7
Q

describe the mechanism by which prostaglandin ____ is protective

A

E2; it is coupled to a Gi receptor which DOWNREGULATES the adenylate cyclase activity → ↓ cAMP release → ↓ proton pump

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8
Q

when would you use quadruple therapy for H. pylori eradication?
what are the drugs and how long does this last?

A
  • give quadruple therapy for patients with H. pylori infection in endemic regions where there is macrolide resistant H. pylori
  • bismuth subsalicylate (antacid) + metronidazole + tetracycline + PPI
  • lasts 14 days
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9
Q

_______ is an analog of PGE1

A

misoprostol

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10
Q

clopidogrel is converted to the active form via ________

A

CYP2C19

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11
Q

what are the complications of peptic ulcer disease

A
  • upper GI bleeding
  • gastric/duodenal perforation
  • gastric outlet obstruction
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12
Q

what drugs are H1 antagonists? what can they be used for?

A
  • lizine: meclisine and cycling
  • diphenhydramine

can be used for motion sickness and postoperative emesis

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13
Q

blackening of the stool and tongue is seen with use of what drug?

A

bismuth subsalicylate (harmless)

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14
Q

are msucarinic (m1) receptor agonists good agents for ↑ GI motility?

A

no because they dont create a coordinated contraction; for a coordinated contraction want to use a drug that works at the level of the enteric neurons or higher

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15
Q

aprepitant can affect the metabolism of many drugs such as warfarin and oral contraceptives because _________

A

aprepitant undergoes extensive CYP3A4 metabolism

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16
Q

M___ receptor is repsobiblry for GI motility

A

M1

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17
Q

why do you give PPI’s as part of the triple therapy for H. pylori infection

A
  1. direct antimicrobial properties of PPI’s
  2. raises gastric pH thus lowers the minimal inhibitory concentrations of antibiotics needed to clear the organism because the ↑ in pH causes the organism to divide and that is when it is most susceptible to destruction
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18
Q

explain the triple therapy for H. Pylori eradication

A

2 antibiotics + 1 PPI

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19
Q

PPI’s ______ bind to the H/K ATPase pump

A

irreversibly

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20
Q

how do benzodiazepines help treat nausea? q

A
  • reduce the anticipatory component of nausea and vomiting and thus works on the cerebrum
    NO INTRINSIC ANTIEMETIC EFFECTS
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21
Q

misoprostol is an analog of _____

A

PGE1

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22
Q

all three compounds ultimately activates ______ which then increases the acid secretion into the gastric lumen by ______

A

protein kinase which then ↑ the activity of the K/H protein pump in the parietal cells: H+ is pumped into the gastric lumen when K is pumped into the parietal cell

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23
Q

how do corticosteroids help treat nausea in patients with metastatic cancer?

A
  • suppression of peritumoral inflammation and prostaglandin production
    drugs: dexamethasone and methylprednisolone
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24
Q

extrapyramidal effects are an AE of what drugs

A

promethazine and droperidol

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25
Q

antacids are a _______ antagonist

A

chemical; does NOT act on any receptor but rather converts the acid into a salt and water

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26
Q

what is the MOA of benzodiazepines

A

facilitate GABA action in the CNS by ↑ frequency of chloride channel opening

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27
Q

______ ulcers are alleviated by eating

A

duodenal

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28
Q

misoprostol binds to the ______ receptor and situates the ______ pathway

A

EP3 receptor → stimulates Gi pathway to DECREASE gastric acid secretion

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29
Q

antacids should NOT be co-admistered with what 4 types of drugs

A

tetracyclines, fluoroquinolones, itraconazole and iron therapy

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30
Q

______ antagonists are the DOC for prophylaxis against immediate CINV (chemotherapy induced nausea and vomitin)

A

5HT3 antagonists

CANNOT BE USED FOR DELAYED CINV OR MOTION SICKNESS

31
Q

what would you give for triple therapy for H. pylori infection in patients with allergy to penicillin?

A
  • carlithromycin + metronidazole + PPI

usually would give amoxicillin instead of metronidazole in non penicillin allergic patients

32
Q

what three compounds lead to the release of acid in the stomach?

A
  • histamine : activate adenylate cyclase and ↑ cAMP due to Gs
  • Acetylcholine (M3 which is Gq protein) : release Calcium
  • Gastrin (CCKb) : release calcium
33
Q

cimetidine is a potent ______ of the CYP450 system. this can affect the concentration on which 3 drugs

A

INHIBITOR; can cause ↑ serum concentration of: warfarin, diazepam and phenytoin

34
Q

how can blood borne emetics cause vomiting?

blood borne emetics include

A

the blood born emetics act on the area prostrema chemoreceptor trigger zone
receptors: 5HT3, D2, M1, CB1
and also causes irritation of the stomach and SI (receptors: 5HT3)
chemotherapy agents

35
Q

can erythromycin be used for longer term therapy

A

NO because rapid down regulation of motilin receptor lets to early tolerance

36
Q

______ is an antacid that can cause osmotic diarrhea

A

magnum hydroxide

37
Q

what are some adverse effects of PPI’s?

A
  • B12 deficiency
  • CAP and C. difficile infection
  • HYPOmagnesemia → ↓ absorption of calcium → osteopenia
38
Q

________ are the most potent inhibitors of gastric acid secretion

A

PPI; effectively suppress basal and meal release of astray acid

39
Q

-setron drugs are _______ drugs

A

5HT3 antagonists; ondansetron and granisetron

40
Q

what are the 4 main inputs into the medulla emetic center?

A
  • cerebrum (anticipation/fear)
  • cerebellum (motion sickness, H1 receptor and Muscarinic receptor)
  • area prostrema (5Ht3, D2, M1, CB1)
  • solitary tract nucleus (5HT3, D2, M, H1, NK1, CB1)
41
Q

of the two methods of gastric acid secretion: ______ and ______, H2RA’s strongly suppress the ________ gastric acid secretion

A

basal and meal stimulated;

H2RA’s strongly suppress the BASAL gastric acid secretion with moderate effect on meal stimulated release

42
Q

what are the receptors on the solitary tract nucleus

A

5HT3, D2, M, H1, NK1, CB1

43
Q

_____, _____ and ______ are PPI’s that inhibit CYP2C19 which is required for the activation of what drug?

A

omeprazole, esomeprazole and lansoprazole

CYP2C19 is required for the activation of the prodrug Clopidrogrel

44
Q

gastrin binds to _______ receptor

A

CCKb

45
Q

histamine works on the ____ receptors

A

H2; the effects of H2 antagonists are mainly upstream

46
Q

what are some AE of metoclopramamide?

A
  • extrapyramidal effects (due to the D2 receptor antagonist effect) commonly sen in kids and young adults
  • galactorrhea (↑ release of prolactin due to D2 receptor antagonism)
47
Q

sucralfate binds via charge interaction; it is ______ charged and the ulcers are _______ charged

A

negative; positive

48
Q

gastric ulcers are alleviated/worsened by eating

A

worsened

49
Q

what is the effect of metoclopramide on the LES tone?

A

↑ the LES tone (can be used for GERD) and stimulates antral and SI contractions

50
Q

which PPI is associated with CYP450 metabolism?

A

omeprazole (CYP450 INHIBITOR)

drugs that will have ↑ concentration: warfarin, diazepam and phenytoin

51
Q

drugs that end in _______ are PPI’s

A

-prazole

omeprazole, esomeprazole, lansoprazole, rabeprazole, pantoprazole

52
Q

______ is a macrolide that has the highest incidence of diarrhea as a side effect. why?

A

erythromycin because it has agonist effects at the motilin receptor

53
Q

what vitamin deficiency is an adverse effect of cimetidine use?

A

B12 deficiency (and myelosuppression). because cimetidine can ↑ gastric pH making it harder for pepsin to cleave off the B12 from animal products

54
Q

_______ is a pro kinetic drug that is no longer prescribed due to potential to induce serious and fatal cardiac ventricular arrhythmias

A

cispapride; (5HT-4 receptor agonist)

55
Q

promethazine and droperidol can be used in what area that causes emesis?

A

these are D2 receptor antagonists and this receptor can be found on the CTZ (chemoreceptor trigger zone) in the area prostrema

56
Q

________ is a mucosal protective agent that binds selectively to ulcers

A

sucralfate; binds by charge interaction because it is negatively charged and the proteins of the ulcer are positively charged

57
Q

PPI’s put people at risk for what kind of infections?

A

CAP and C. difficile colitis

58
Q

if your patient had a recent MI and is taking clopidogrel, and now needs PPI’s because he has GERD, what are some PPI’s you can prescribe him and why?

A
  • give pantoprazole or rabeprazole because omeprazole, esomeprazole and lansoprazole are CYP2C19 inhibitors and CYP2C19 is required to convert clopidogrel to the active form
59
Q

can H2 receptor antagonists be used for long term therapy? how long does it take to work and how long do the effects last?

A

no cannot be used for long term therapy because build resistance and tachyphylaxis develops within 2-6 weeks

onset: 2.5 hrs
duration: 4-10 hours

60
Q

what are 3 mechanisms by which misoprostol is protective

A
  • ↓ gastric acid secretion by simulation Gi
  • stimulates mucus and bicarbonate secretion
  • enhances mucosal blood flow
61
Q

promethazine and droperidol are use to effectively treat what symptom?

A

motion sickness;

NOT effective in CINV

62
Q

_______ receptors are found in critical sites involved in chemotherapy induced vomiting

A

5HT3

63
Q

______ and ______ are D2 antagonists

A

promethazine and droperidol

64
Q

_______ is useful for treated delayed CINV

A

aprepitant / fosaprepitant

65
Q

bismuth salicylate is contraindicated in patients with renal failure due to accumulation of ______

A

salcyclate

66
Q

what are some adverse effects of calcium carbonate antacids?

A
  • belching caused by carbon dioxide and can lead to alkalosis
67
Q

solitary tract nucleus causes emesis by receiving input from: ___________

A

area prostrema and the stomach/SI irritations (vagal and sympathetic afferents)

68
Q

______ is an antacid the can cause constipation

A

Aluminum hydroxide

69
Q

NK1 antagonists (_________) are usually given in combination with ______ and ________

A

aprepitant/fosaprepitant

given with dexamethasone and a 5HT3 receptor antagonist

70
Q

erythromycin is the DOC for what GI condition

A

diabetic gastroparesis

71
Q

how does serotonin ↑ GI motility?

A

binds to 5HT-4 receptors on the enteric neuron which then releases Ach onto the M1 receptor

72
Q

the most common side effect of sucralfate is _____

A

constipation

73
Q

sucralfate should not be given with ______ antacids

A

aluminium containing antacids or in patients with renal failure and are at high risk for aluminum overload

PCM Exam 4 (44 decks)

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