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Pharmacology and Therapeutics > GORD/Peptic Ulcer Disease - Core Drugs > Flashcards

GORD/Peptic Ulcer Disease - Core Drugs Flashcards

1
Q

List drug classes used to treat GORD/PUD

A

NSAIDs
proton pump inhibitors
Histamine (H2) receptor antagonists
paracetamol

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2
Q

list examples of NSAIDs used to treat GORD/PUD

A

ibuprofen
naproxen
diclofenac

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3
Q

primary mechanism of action of NSAIDs

A

inhibits COX enzyme > slows production of prostaglandins & thromboxanes

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4
Q

It is thought that the anti-inflammatory actions, and probably most of the analgesic & antipyretic actions, of the NSAIDs are related to inhibition of?

A

COX-2

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5
Q

It is thought that the unwanted effects of NSAIDs are largely a result of?

A

inhibition of COX-1

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6
Q

drug target of NSAIDs

A

COX enzyme

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7
Q

side effects of NSAIDs

A

gastric irritation, ulceration and bleeding and, in extreme cases, perforation; reduced creatinine clearance and possible nephritis, Skin rashes & other allergies, dizziness, tinnitus.

adverse CVS effects (hypertension, stroke, MI) may occur following prolonged use or in patients with pre-existing CV risk.

Prolonged analgesic abuse over a period of years is associated with chronic renal failure.

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8
Q

Aspirin has been linked with what in children?

A

rare but serious post-viral encephalitis (Reye’s syndrome)

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9
Q

main uses of NSAIDs

A

analgesics for mild/moderate pain
antipyretics
antiinflammatory
(aspirin only) as an anti-aggregatory

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10
Q

NSAIDs are contraindicated for what population and why?

A

asthma

causes bronchoconstriction

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11
Q

list examples of proton pump inhibitors used to treat GORD/PUD

A

omeprazole

lansoprazole

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12
Q

drug target for proton pump inhibitors

A

H+/K+ ATPase (‘proton pump’)

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13
Q

mechanism of action of proton pump inhibitors

A

irreversible inhibitors of H+/K+ ATPase in gastric parietal cells > are weak bases + accumulate in acid environment of canaliculi > concentrates their actions there and prolongs their duration of action

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14
Q

omeprazole plasma half life

A

1 hour

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15
Q

single daily dose of omeprazole affects acid secretion for how long?

A

2-3 days

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16
Q

side effects of proton pump inhibitors

A

headache, diarrhoea, bloating, abdominal pain & rashes

17
Q

use of proton pump inhibitors can mask the symptoms of what disease?

A

gastric cancer

18
Q

omeprazole is also an inhibitor of _____ and has been reported to reduce the activity of _____

A

cytochrome P2C19

clopidogrel

19
Q

how are PPIs administered?

A

orally but degrade rapidly at low pH so administered as capsules containing enteric-coated granules.

20
Q

PPIs are pro drugs. how are they converted to their active forms?

A

at low pH, are converted into 2 reactive species which react with sulphydryl groups in the H+/K+ ATPase

21
Q

list an example of a histamine (H2) receptor antagonist

A

ranitidine

cimetidine

22
Q

drug target of histamine (H2) receptor antagonist

A

histamine H2 receptor

23
Q

mechanism of action of histamine receptors antagonist

A

competitive antagonists (structural analogues of histamine) > inhibit stimulatory action of histamine released from enterochromaffin-like (ECL) cells on the gastric parietal cells

24
Q

list side effects of histamine receptor antagonists

A

diarrhoea
dizziness
muscle pains
transient rashes

25
Q

cimetidine also inhibits?

A

cytochrome P450

26
Q

other actions of cimetidine include?

A

may retard the metabolism and potentiate the effects of a range of drugs incl. oral anticoagulants and TCAs

27
Q

ranitidine plasma half life?

A

2-3 hours

28
Q

bioavailability of ranitidine

A

undergoes first pass metabolism

50% bioavailability

29
Q

drug target of paracetamol

A

Not yet well defined. COX-3 isoform?

30
Q

mechanism of action of paracetamol is unclear. list examples of current hypotheses

A

interaction with a COX-3 isoform (inhibition of PG synthesis), cannabinoid receptors or the endogenous opioids. also Interactions at 5HT & adenosine receptors

31
Q

In serious overdose of paracetamol what can occur?

A

serious hepatotoxicity

occasional allergic skin reaction

32
Q

main uses of paracetamol

A

analgesic

anti-pyretic activity

Pharmacology and Therapeutics (16 decks)

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