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aa BDS M6 - Therapeutics > 5. Analgesia - Aspirin/NSAIDs > Flashcards

5. Analgesia - Aspirin/NSAIDs Flashcards

1
Q

What is the ‘proper’ name for aspirin?

A

acetylsalicylic acid

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2
Q

What are the therapeutic activities of aspirin?

A
  • anti-pyrexic
  • anti-platelet/thrombotic
  • anti-inflammatory
  • analgesic - mild/moderate
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3
Q

What is the presentation and route of aspirin?

A
  • white tablet
  • dispersible form available
  • not dissolvable in the mouth
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4
Q

What might happen if a patient puts an aspirin directly on their mucosa in their mouth etc?

A

aspirin burn - sloughing/ulceration of tissues (aspirin is acidic)

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5
Q

In terms of mechanism of action, what do aspirin and NSAIDs affect?

A

COX (cyclo-oxygenase) isoenzyme
- inhibition of COX-1, COX-2, COX-3

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6
Q

What does COX inhibition result in?

A

reduction in Eicosanoid (Prostanoid) production
- reduces the production of prostaglandin (PGE2), prostacycline (PGI2), thromboxane (TXA)
- leads to irreversible inhibition, hence the permanent action of aspirin on platelet aggregation

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7
Q

What are some of the actions of PGE2 (prostaglandin) and TXA (thromboxane)?

A
  • Regulate BP
  • Renal Effects
  • Inflammatory response
  • Duration & intensity of pain
  • Fever
  • Gastric effects
  • Inhibits platelet aggregation and thrombosis
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8
Q

What mechanism does aspirin use to reduce the synthesis of COX products?

A

irreversible acetylation of COX enzymes

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9
Q

What does aspirin have more of an affect on, COX-1 or COX-2?

A

COX-1 > COX-2 (x100 greater effect on COX-1)

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10
Q

What kind of functions is COX-1 involved in?

A

physiological/homeostatic functions - COX-1 is constitutive

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11
Q

What kind of functions is COX-2 involved in?

A

inflammation - COX-2 is inducible

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12
Q

What stimulates COX-1 and COX-2?

A
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13
Q

What are the indications for aspirin?

A
  • Acute pain
  • Dental Pain
  • Rheumatic fever
  • Rheumatoid arthritis
  • Other inflammatory disease
  • Fever
  • Acute coronary syndrome /ischemic stroke
  • Anti-thrombotic
    (MI, CVA, AF, Angina, Revascularisation after CABG, IHD, peripheral artery disease…..)
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14
Q

How does aspirin work as an anti-pyretic (reduce fever)?

A

infection/inflammation results in the release of cytokines, which reuslts in prostaglandins release in the hypothalamus which leads to a raised body temperature

aspirin inhibits prostaglandins —> reduces fever

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15
Q

How is aspirin absorbed?

A

by the GI, mainly small intensive (and stomach) and then quickly hydrolysed to salicylate

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16
Q

What is the half life of aspirin?

A

20-30mins

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17
Q

What is a normal dose of aspirin?

A

300-600mg - dose related efficacy, generally has a plateau effect up to about 1000mg

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18
Q

What is the half life of salicylate at anti-inflammatory doses?

A

~12 hrs

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19
Q

What is the % plasma binding of salicylate to albumin?

A

80-90%

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20
Q

How is aspirin’s distribution in the body?

A

widely distributed, crosses placenta, evident in breast milk

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21
Q

Where does aspirin undergo biotransformation?

A

in the liver via conjugation

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22
Q

How is aspirin excreted from the body?

A

by glomerular filtration and active proximal tubular secretion in the kidney, 10% is excreted unchanged

23
Q

Why should aspirin be avoided in the 3rd trimester of pregnancy?

A

may cause premature closure of the ductus artereosis which could lead to pulmonary vascular abnormalities in the baby

24
Q

What are the contraindications and side effects of aspirin?

A
  • Gastrointestinal effects
  • Respiratory –AERD
  • Renal ( 3x increase Renal failure)
  • CVS K+, HBP, Oedema
  • Haematological
  • Gout (increases uric acid)
  • Tinnitus at higher doses.
  • Skin reactions
  • Glycaemic control
  • Pregnancy (avoid in 3rd trimester)
25
Q

What GI side effects can aspirin have?

A
  • epigastric pain, dyspepsia and nausea
  • occult stomach ulceration and bleeding (in potentially 70% of long-term users)
26
Q

What respiratory side effects can aspirin have?

A
  • bronchospasm (particularly asthma or those with hypersensitivity reactions to NSAIDs)
  • urticaria
  • angioedema
  • rhinitis
  • AERD - aspirin exacerbated respiratory disease
27
Q

Why is aspirin contraindicated in congestive heart failure/what is the potential renal side effect?

A

if pt has congestive heart failure they may have reduced flow to the kidneys which may precipitate acute renal failure

28
Q

In those with renal impairment how is the risk of renal failure impacted by NSAID used?

A

3x increased risk of renal failure compared to those not using NSAIDs

29
Q

What CVS side effects can aspirin have?

A
  • hyperkalaemia
  • peripheral oedema
  • elevated blood pressure
  • decompensation of heart failure
30
Q

What haematological contraindications does aspirin have?

A

effects platelets so avoided in congenital or acquired bleeding disorders e.g.
- haemophilia
- anticoagulant therapy
- liver disease

31
Q

Why is aspirin generally avoided in gout?

A

as it increases uric acid concentrations in the blood, worsening gout

32
Q

What doses of aspirin may cause hypoglycaemia?

A

higher doses, particularly over 5g/day

33
Q

Why should NSAIDs be avoided in some renal issues?

A

inhibits the prostaglandins which are modulating blood flow in the kidneys, which can therefore reduce kidney perfusion and cause acute renal failure

some renal issues to avoid NSAIDs in:
- congestive heart failure
- nephrotic syndrome
- liver cirrhosis
- salt depletion

34
Q

Why are GI issues common as a side effect of aspirin?

A

ulcerogenic properties related to the reduced prostaglandin production in the gastric mucosa

35
Q

Why can prostaglandin inhibition cause GI issues?

A

the effects of prostaglandin are protective, and are essential for mucous secretion

prostaglandin inhibition:
- decreases mucous production
- increases acid production
- mediates bicarbonate
- influence cell permeability H+
- mucous layer less hydrophobic

36
Q

Why should aspirin be avoided in children (under 16 in UK)?

A

Reye’s syndrome:
- generally presents with acute enphelophatic illness and fatty degeneration of the viscera especially the liver
- often occurs after infectious illness
- aetiology unknown
- mechanism likely due to damage to cellular mitochondria especially in the liver

37
Q

What doses on aspirin can cause overdose, and why can it be fatal?

A

10-30g

Complex acid-base disturbances:
- CO2 in skeletal muscle presents as hyperventilation, hyperthermia and dehydration, tinnitus, deafness, vasodilations, and sweating

38
Q

How are complex acid-base disturbances caused by aspirin overdose treated?

A

require hospitalisation to monitor pH, electrolytes and plasma salicylate, fluid replacement and bicarbonate tot balance, may require haemodialysis

39
Q

What are the principle interactions with aspirin?

A

4 ANTS like aspirin - AAAANTS
- Anticoagulants
- Antihypertensives
- Antidepressants
- Anti-epileptics
- NSAIDs
- Thrombocytes (drugs that affect)
- Steroids (corticosteroids)

40
Q

What can aspirin and anticoagulant interaction cause?

A

it may displace anticoagulants from their plasma bound state, increasing their effect

e.g. warfarin only has around 3% non-plasma bound exerting its action, increasing this can cause fatal bleeding

41
Q

What can aspirin and antihypertensive interaction cause?

A

may lead to risk of renal impairment and a blunting of the antihypertensive effect

42
Q

What can aspirin and antidepressant interaction cause?

A

can lead to increased risk of bleeding with the likes of SSRIs

43
Q

What can aspirin and anti-epileptic interaction cause?

A

enhances the effects of anti-epileptics

44
Q

What can aspirin and thrombocyte affecting drug interaction cause?

A

can get enhanced bleeding through a combination with any other drug that effets platelets and thrombocytes e.g. clopidogrel

45
Q

What can aspirin and corticosteroid interaction cause?

A

enhanced GI effects

46
Q

What is the difference between aspirin and ibuprofen’s effect on platelet COX?

A

most NSAIDs are reversible inhibitors of COX whereas aspirin is a permanent inhibitor

47
Q

What is the absorption and binding of most other NSAIDs (not aspirin)?

A

rapid absorption via oral administration - peak plasma conc. 1.5hrs, extensive binding 99%

48
Q

What percentage of people discontinue their use of NSAIDs due to the side effects?

A

15%

49
Q

What should NSAIDs be avoided in?

A
  • pregnancy, asthmatics, anti-coagulated, methotrexate, allergy
  • caution in elderly, renal or hepatic insufficiency, IHD, GI complications
50
Q

What is the standard adult dose of aspirin?

A

300-900mg 4-6 hourly, maximum of 4g daily (preferably with food)

51
Q

What is the standard adult dose of ibuprofen?

A

oral 400mg approx. 3 times per day (~8 hourly), maximum 1.8g-2.4g/day

52
Q

What is the standard adult dose of diclofenac?

A

oral 50mg 3 times/day, maximum 150mg/day

53
Q

What should be given to patients alongside NSAIDs if they are at risk of gastric upset?

A

proton pump inhibitor (PPI) omeprazole/lansoprazole

54
Q

Summary of aspirin

A

aa BDS M6 - Therapeutics (6 decks)

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