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Z YEAR 2 Pharm > GORD Core Drugs > Flashcards

GORD Core Drugs Flashcards

1
Q

What are examples of NSAIDs?

A
  • ibuprofen
  • naproxen
  • diclofenac
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2
Q

What do NSAIDs inhibit?

A

enzyme cyclo-oxygenase (COX)

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3
Q

What does COX do?

A

rate-limiting step for the production of all prostanoids (prostaglandins & thromboxanes) from the parent arachidonic acid

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4
Q

What do prostanoids do?

A

act through a large number of prostanoid receptors to produce a highly complex array of actions

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5
Q

What are the anti-inflammatory actions, and probably most of the analgesic & antipyretic actions, of the NSAIDs related to?

A

Inhibition of COX-2

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6
Q

What are the unwanted effects of NSAIDs due to?

A

Inhibition of COX-1

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7
Q

What is the drug target of NSAIDs?

A

cyclo-oxygenase (COX) enzyme

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8
Q

What are the main side effects of NSAIDs?

A
  1. gastric irritation
  2. ulceration
  3. bleeding
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9
Q

What can NSAIDs cause in extreme cases?

A
  • perforation
  • reduced creatinine clearance and possible nephritis
  • bronchoconstriction in susceptible individuals (contraindicated in asthma)
  • Skin rashes and other allergies
  • dizziness
  • tinnitus
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10
Q

What may occur with prolonged use or in patients with existing CV risk with NSAIDs?

A

adverse cardiovascular effects (hypertension, stroke, MI)

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11
Q

What happens with prolonged analgesic abuse over a period of years?

A

chronic renal failure

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12
Q

What has been aspirin been linked to?

A

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

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13
Q

When are NSAIDs used as analgesic?

A

relief of mild to moderate pain (e.g. musculoskeletal pain, headache, dysmenorrhoea)

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14
Q

When are NSAIDs used as an antipyretic?

A

reduce fever

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15
Q

When are NSAIDs used for their anti-inflammatory properties?

A

chronic control of inflammatory diseases (e.g. rheumatoid arthritis, osteoarthritis)

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16
Q

When is aspirin used?

A

anti-aggregatory agent to inhibit platelet aggregation in patients who are at risk of stroke or myocardial infarction

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17
Q

How commonly were these drugs prescribed in the West London area in 2020?

A
  1. ibuprofen (48th), naproxen (45th), diclofenac (92nd)
  2. omeprazole (5th) and lansoprazole (10th)
  3. Ranitidine (37th)
  4. Paracetamol (14th)
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18
Q

What are examples of proton pump inhibitors (PPIs)?

A

omeprazole, lansoprazole

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19
Q

What do PPIs inhibit?

A

irreversible inhibitors of H+/K+ ATPase in gastric parietal cells

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20
Q

What are PPIs? Why do they last long?

A
  1. weak bases and accumulate in the acid environment of the canaliculi of the parietal cells
  2. concentrates their actions there and prolongs their duration of action
21
Q

How effective are PPIs?

A
  1. omeprazole plasma half-life approx. 1 h
  2. single daily dose affects acid secretion for 2-3 days)
  3. PPIs inhibit basal and stimulated gastric acid secretion by >90%.
22
Q

What is the drug target of PPIs?

A

H+/K+ ATPase (‘proton pump’)

23
Q

What are the uncommon unwanted side effects of PPIs?

A
  • headache
  • diarrhoea
  • bloating
  • abdominal pain
  • rashes
24
Q

What can the use of PPIs mask?

A

symptoms of gastric cancer

25
Q

What can omezrapole reduce the activity of?

A
  1. Omeprazole is an inhibitor of cytochrome P2C19

2. has been reported to reduce the activity of e.g. clopidogrel, when platelet function is monitored

26
Q

What happens to PPIs at low pH?

A
  • PPIs are pro-drugs
  • At low pH converted into 2 reactive species which react with sulphydryl groups in the H+/K+ ATPase responsible for transporting H+ ions out of the parietal cells
27
Q

How are PPIs given?

A

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

28
Q

What are examples of Histamine (H2) receptors antagonist?

A

ranitidine

29
Q

How do H2 receptor antagonists work?

A
  1. competitive antagonists of H2 histamine receptors (structural analogues of histamine)
  2. inhibit the stimulatory action of histamine released from enterochromaffin-like (ECL) cells on the gastric parietal cells
30
Q

How effective are H2 receptor antagonists?

A

nhibit gastric acid secretion by approximately 60%

31
Q

What are the targets of H2 receptor antagonists?

A

Histamine H2 receptors

32
Q

Are side effects of histamine H2 receptor antagonists?

A

no

33
Q

What are the main side effects of H2 receptor antagonists?

A
  1. Diarrhoea
  2. dizziness
  3. muscle pains
  4. transient rashes
34
Q

What does cimetidine affect?

A

(but not other H2 antagonists)

  1. inhibits cytochrome P450
  2. may retard the metabolism
  3. potentiate the effects of a range of drugs incl. oral anticoagulants and TCAs
35
Q

What is the dosage of ranitidine like?

A
  1. plasma half-life approx. 2-3 h – well tolerated so twice daily dosing effective
  2. 1st pass metabolism (50% bioavailability)
  3. low dose over-the-counter formulations available from pharmacies for short term use without prescription
36
Q

What is paracetamol also known as?

A

acetaminophen

37
Q

What is the mechanism of paracetamol?

A
  • largely restricted to nervous tissue but its mechanism of action is unclear
    1. both a central and peripheral action possibly involving interaction with a COX-3 isoform (inhibition of PG synthesis), cannabinoid receptors or the endogenous opioids
    2. Interactions at 5HT & adenosine receptors have also been proposed.
38
Q

What is the drug target of paracetamol?

A

Not yet well defined. COX-3 isoform?

39
Q

What are the side effects of paracetamol?

A
  1. very safe drug with few side-effects at therapeutic dose.
  2. does not cause gastric irritation
  3. occasional allergic skin reactions
40
Q

What does an overdose of paracetamol cause?

A

hepatotoxicity

41
Q

Is paracetamol anti-inflammatory?

A

not an NSAID as it has little anti-inflammatory activity

42
Q

What can paracetamol help with?

A

good analgesic for mild-to-moderate pain and also has antipyretic activity

43
Q

Are there restrictions on paracetamol sale?

A

Legal restrictions on sales of paracetamol have significantly reduced the number of fatalities from overdose in the UK although, regrettably, ingestion of large amounts of paracetamol remains a common method of suicide

44
Q

Do PGs cause pain?

A

NO

45
Q

How come COX causes pain?

A

-COX produces prostaglandins (PG)
-PGs do
not directly cause pain themselves, but they
sensitise peripheral nociceptors mediators (bradykinin
and histamine) which causes pain
-NSAIDs inhibit COX

46
Q

How do PGs in gastric mucosal cell protect the acid?

A
  • increase bicarbonate release
  • increase mucus production
  • increase blood flow
47
Q

Can topical drugs cause systemic side effects?

A

YES

48
Q

Why does ratinidine and H2 not cause fractures but PPIs do?

A

Not sure

49
Q

How does H2 histmaine receptors work?

A
  1. ↓ acid production from parietal cell
  2. Histamine receptors ↑ acid production via cAMP
    dependent activation of H+/K+ ATPase
  3. The
    damaged mucosal barrier leaves stomach wall exposed to acid  symptoms pain
  4. ↓ acid
    production, ↓ corrosive nature of environmen

Z YEAR 2 Pharm (9 decks)

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