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Inflammatory and GI diseases > NSAIDs Therapeutics > Flashcards

NSAIDs Therapeutics Flashcards

1
Q

What is paracetamol?

A
  • Paracetamol is mainly used as an analgesic (pain) and as an antipyretic (prevent or reduce fever)
  • Paracetamol is not described as an NSAID as it does NOT have significant anti-inflammatory effect which is on the peripheral COX inhibition
  • Paracetamol is generally well tolerated when taken in standard doses and when patient considerations are taken into account

Special patient groups:
1. Children (correct strength should be supplied and appropriate dosing schedule is used)

  1. Low body weight (<50kg)
  2. Liver impairment (or those with risk factors for hepatotoxicity)
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2
Q

In what patients is analgesic (i.e. paracetamol) preferred over NSAIDs?

A
  1. Elderly patients (older people are more at risk of the side effects associated with NSAIDs)
  2. Patients with; Hypertension, CVD, renal impairment and GI issues (can be worsened by the potential adverse effects of NSAIDs)
  3. Patients on medication that interacts with NSAIDs, e.g. Warfarin
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3
Q

What preparations are available for paracetamol?

A
  1. Tablet, caplet, capsule, orodispersible tablets
  2. Suspensions
  3. Suppositories
  4. Infusion
  5. Compound preparations - Co-codamol (paracetamol and codeine), co-dryamol, OTC preparations - Lemsip etc.
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4
Q

For what 2 purposes is Aspirin used for?

A

An analgesic and anti platelet

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5
Q

What are aspirins anti platelet effects?

A

As an anti platelet, aspirin is used to inhibit thrombus formation in the arterial system.

In these fast flowing vessels, thrombi are composed mainly of platelets with little fibrin.

Therefore the use of anti platelets aspirin is used for primary and secondary prevention of CVD and events.

Standard dose: 75mg daily
- But can be increased to 300mg daily
- At these doses it has no anti-inflammatory or analgesic effect.

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6
Q

How is asprin used as an analgesic?

A

Standard oral dose: 300-900mg every 4-6 hours when required for pain (max 4g per day)

  • Aspirin rarely used now in inflammatory conditions due to the risk of side effects

Special patient groups:
1. Contraindicated in children under 16- due to a risk of Reyes disease (swelling in the brain), exception Kawasaki

  1. Contraindicated in patients with:
    - Previous of active peptic ulcerations
    - Bleeding disorders
    - Severe cardiac failure
    - Previous hypersensitivity to aspirin or NSAIDs

As aspirin can increase the risk of bleeding (due to anti platelet effect) and GI irritation and exacerbate cardiac failure.

  1. Elderly (older patients more at risk of side effects)

4 Caution in patients with Asthma due to the risk of bronchospasm hence an increase in their symptoms

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7
Q

What are the interactions for aspirin?

A
  • Drugs that increase the risk of GI irritation and bleeding- steroids, NSAIDs, SSRIs, anticoagulants
  • Drugs that increase the risk of renal side effects - e.g. Bisphosphonates
  • Drugs where aspirin can increase the toxicity of other drugs - e.g. Methotrexate
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8
Q

What preparations are available for Aspirin?

A
  • Tablets, enteric coated (EC), dispersible
  • Suppositories
  • Compound preparation - Beechams powders (aspirin/caffeine), codes 500, Alka-seltzer
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9
Q

How do NSAIDs work therapeutically?

A

In regular full dosage, NSAIDs have lasting analgesic and anti-inflammatory effects

  • Analgesic effect starts soon after first administration and full effect obtained within a week
  • Anti-inflammatory effect may not be achieved for up to 3 weeks

The difference in anti-inflammatory effect of the different NSAIDs is small
- Considerable variation in individual response and tolerance

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10
Q

What should the selection of the NSAID be based on?

A

Should be based on the characteristics of the drug and individual patient risk factors for adverse effects

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11
Q

What are the key side effects of NSAIDs?

A
  • GI mucosa
  • Kidney
  • Cardiovascular system
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12
Q

What should be done if an NSAID is indicated for treatment?

A

The LOWEST effective dose should be used for the SHORTEST duration to reduce risk of adverse effects

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13
Q

What are the GI side effects caused by NSAIDs and why?

A

Examples: Epithelial damage, ulceration and bleeding

These are caused by:

  1. Suppression of the COX-1 enzyme inhibiton which causes:
    - Reduced mucus production
    - Reduced bicarbonate production
    - Reduced mucosal blood flow
    Resulting in damage, ulceration and bleeding
  2. Topical irritation and direct epithelial damage

All NSAIDs are associated with GI issues
- Highest incidence in the elderly
- Consider cautions and contraindications
- Monitor patients

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14
Q

Which NSAIDs are considered to have the HIGHEST risk of GI side effects?

A

Piroxicam
Ketoprofen
Ketorolac

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15
Q

Which NSAIDs are considered to have the INTERMEDIATE risk of GI side effects?

A

Indometacin
Diclofenac
Naproxen

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16
Q

Which NSAIDs are considered to have the LOWEST risk of GI side effects?

A

Ibuprofen (low dose, up to 1.2g)
Coxibs (COX 2 selective)

17
Q

What are the key points to consider when giving NSAIDs in terms of GI side effects?

A
  1. Lowest risk agent preferred
  2. Start at lowest dose
  3. Use for the shortest duration (review)
  4. Do not use more than one NSAID at a time
  5. Advise medication to be taken with food to reduce contact irritation
  6. Co-prescrible with gastroprotection in those patients at risk of GI ulceration, i.e. PPI (omeprazole)
  7. Monitor for adverse events
  8. Review patient for risk factors
18
Q

Interactions of what other drugs can increase the risk of GI effects with NSAIDs?

A
  • Aspirin
  • Other NSAIDs
  • Other drugs increasing the risk of GI ulceration and bleeding - steroids, bisphosphonates
  • Other drugs increasing the risk of bleeding: SSRIs, anticoagulants
19
Q

What monitoring can be done when on NSAIDs for GI side effects?

A
  • Patient is able to recognise and report symptoms of dyspepsia/GI irritation/burning sensation/pain
  • Hb - haemoglobin (bleeding)
  • Signs of GI bleeding- haemoptysis / dark stools
20
Q

What is the reason for CV events when taking NSAIDs?

A

Due to increased COX 2 inhibition over COX 1 inhibition of the vasculature, platelets and potential effects from the kidney

21
Q

Which NSAIDs are considered to have the HIGHEST risk of CV events?

A

COX-2 inhibtors
Diclofenac (150mg daily)
Ibuprofen (2.4g or more daily)

22
Q

Which NSAIDs are considered to have LOWER THROMBOTIC risk of CV events?

A

Naproxen (1g daily)

23
Q

Which NSAIDs are considered to have NO EVIDENCE FOR INCREASED risk of CV events?

A

Ibuprofen (low dose, 1.2g or less)

24
Q

What are the key points to consider when giving NSAIDs in terms of CV events?

A
  1. Selection of NSAID is important
  2. Use the lowest effective dose
  3. Use for the shortest duration (review and see if there is a need of long term therapy)
  4. Monitor for adverse events
  5. Review patient for risk factors
  • COX 2 inhibitors, diclofenac and high dose ibuprofen are contraindicated in ischaemic heart disease, cerebrovascular disease and some stages of heart failure.
  • Other non-selective NSAIDs have been cautioned in patients with:
  • heart failure
  • cerebrovascular disease
  • ischaemic heart disease
  • risk factors for CVD
25
Q

Interactions of what other drugs can increase the risk of CV events with NSAIDs?

A
  • Antihypertensives (NSAIDs are known to increase a patient’s blood pressure - opposite effects)
  • Antiplatelet dose aspirin (75mg)
26
Q

What monitoring can be done when on NSAIDs for CV events?

A
  • Increase occurrence or first occurrence of CV event
  • Risk factors for increased CV risk: increased BP, medical history or diabetes/hypercholesterolaemia
27
Q

In what patients is renal side effects mostly seen when taking NSAIDs?

A

Mainly seen in individuals where compensatory prostaglandins are playing a role to maintain renal function, i.e:
- advanced age (renal function will be decreased)
- renal impairment
- heart failure
- volume depletion
- liver cirrhosis
Prostaglandins will be playing an important role in maintaining a patients renal function.

  • If we use NSAIDs in these patient groups, we could potentially be reducing their renal function and could lead to renal failure.

NSAIDs can cause:
- A decrease in renal blood flow and increase the risk of acute kidney injury
- Sodium and water retention- oedema and hypertension

Therefore NSAIDs should be avoided in patients with:
1. The above risk factors
2. Avoid in severe impairment/avoid or use with caution in other renal impairment:
- Use the LOWEST effective dose for the SHORTEST duration
- Close monitoring of renal function

28
Q

Interactions of what other drugs can increase the risk of renal side effects with NSAIDs?

A
  • Other co-prescribed nephrotoxic medicines - E.g. Diuretics, ACE inhibitors
  • Anti-hypertensive - (opposite effect)
  • Lithium and methotrexate - decreased renal elimination causing toxicity
29
Q

What monitoring can be done when on NSAIDs for renal side effects?

A
  • Renal function- GFR, urine output, urea
  • Blood pressure
  • Electrolytes - sodium and potassium
  • Oedema (weight, visual signs)
30
Q

What other considerations need to be taken when giving NSAIDs?

A
  1. Bronchospasms; asthmatic patients
  2. Topical therapies
    - Available OTC
    - Systemic absorption is much lower than any other form
    - Systemic absorption can occur
  3. General interactions:
    - Anticoagulants; Patients should no self medicate and close monitoring required if given
31
Q

What counselling points should be provided when taking NSAIDs?

A
  • Take the lowest effect dose for the shortest period
  • Take with or after food
  • Self monitor for signs of GI disturbance - report
  • Do not self medicate with other NSAIDs or aspirin

Inflammatory and GI diseases (22 decks)

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