Analgesics in MOS 2 Flashcards

1
Q

What is the most common cause of acute liver injury in Europe and North America?

A

Paracitamol poisoning

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2
Q

What are the main properties of paracetamol?

A
  • antipyretic
  • analgesic
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3
Q

What type of pain should paracetamol be used for following oral surgery ?

A

mild to moderate

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4
Q

What is the maximum therapeutic dose of paracetamol ?

A

4g/24h

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5
Q

What are PROMs ?

A

patient reported outcome measures

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6
Q

What does the oral surgery guidance for commissioners of service recommend following oral surgery?

A

it recommends that all patients be contacted by telephone 24 hours after their surgery to enquire about unmanaged pain, haemorrhage and nerve injury

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7
Q

What is the most commonly used opioid analgesic?

A

Paracetamol

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8
Q

The US approved name for paracetamol is …

A

acetaminophen

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9
Q

Paracetamol causes euphoria and alters the mood. True or false

A

False

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10
Q

Paracetamol is the _______ name

A

International non-properietary name

British Approved Name

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11
Q

Acetaminophen was sold under the name ____ in the USA (1955)

A

Tylenol

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12
Q

In 1956, 500 mg tablets of paracetamol went on sale in the UK under the brand name ______.

A

panadol

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13
Q

The childrens formulation of paracetamol was released in 1958 and called…

A

Panadol Elixer

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14
Q

What is the MOA of paracetamol?

A
  • inhibition of COX-3 isoenzyme
  • inhibition of COX-1 variant and subsequent reduced release of prostanoid release in the CNS

(is effective in COX-1 variant present in CNS; reduces prostaglandins that have a role in causing fevers)

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15
Q

What is the primary mechanism by which paracetamol is able to reduce fever

A

central inhibition

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16
Q

When are weak plasma concentrations of paracetamol present following ingestion ?

A

30-60 minutes

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17
Q

Briefly describe how paracetamol is inactivated

A

it is inactivated by conjugation to glucoronide and sulphate (to a lesser extent)

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18
Q

How is paracetamol excreted?

A

via the kidneys

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19
Q

What is the NNT for 1g of paracetamol in oral surgery ? What does this mean

A

1.87

This means that for every 2 (1.87 rounded up) patients who receive 1g of paracetamol, one will get greater than 50% pain relief and would not have done so if they received the placebo

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20
Q

Why has paracetamol been described as a weak analgesic?

A

this because it has affected by the ceiling effect meaning that increasing the dose will not confer any further analgesic benefit

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21
Q

What is the benefit of using paracetamol with other analgesics ?

A
  • superior pain relief
  • permits reduction in opioid drug doses
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22
Q

What are the indications for paracetamol use ?

A
  • headache
  • fever
  • period pain
  • toothache, other dental pain
  • back pain
  • muscular and joint pain
  • neuralgia
  • pain associated with colds/flus
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23
Q

Why is paracetamol the analgesic of choice for children?

A

this is because it is not associated with Reyes syndrome

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24
Q

Why is paracetamol sometimes preferred for use in the elderly?

A

because it lacks the gastric erosive properties

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25
Q

How can you guard patients from accidental overdoses?

A
  • advise them to follow dosing regime on the label
  • avoid prolonged and excessived doses
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26
Q

Patients and their escorts must always be informed if paracetamol has been used intra/post operatively. True or false

A

True

this will prevent further overdose as patient is made aware that they have received it during their treatment

-allows pt to monitor futher dose

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27
Q

Why should patients be warned about combination analgesics ?

A

this is because they may also contain paracetamol

Allows patient to monitor dose and prevent overdose

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28
Q

Recent evidence has shown that high dose levels of paracetamol may be associated with …

A

the same GI and cardiovascular adverse events as non-selective NSAIDs

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29
Q

What dose of paracetamol is recognised as toxic?

A
  • 150mg/kg
  • 12 g
    or less if they are a high risk patient then the dose required for hepatotoxicity may be less
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30
Q

State some patients that may be at increased risk of hepatotoxicity from paracetamol

A
  • adolescents with eating disorder
  • adolescents with gluthathione depletion
  • patients taking enzyme inducing drugs such as phenytoin or rifampicin (this has not been definitely shown)
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31
Q

What is reported to reduce the ceiling of toxicity of paracetamol?

(causing a lower dose to be hepatotoxic)

A

chronic alcohol ingestion

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32
Q

Many individuals have no symptoms 24h after a paracetamol overdose. True or false

A

True

33
Q

What are some symptoms that may be experienced in the first 24 hours of a paracetamol overdose?

A
  • vague abdominal pain
  • nausea
34
Q

What are the signs of a paracetamol overdose after the first 24 hours?

A
  • signs of liver failure
  • encephalopathy
  • hypoglcaemia
  • coagulopathy
35
Q

It is not important to establish the exact timing and amount of paracetamol injected in an overdose. True or false

A

False

an attempt should be made, it is prudent to do so

36
Q

What treatment can be provided for hepatotoxic overdose that has occurred within the last hour?

A

gastric decontamination with activated charcoal

37
Q

What is the mainstay treatment paracetamol poisoning?

A

N-acetylcysteine

38
Q

The decision to start N-acetylcysteine treatment depends on…

A
  • time of presentation after the overdose
  • serum levels of paracetamol
  • liver enzymes
39
Q

What is the effect of prolonged and short term use of paracetamol on coumarins?

A

Prolonged use:
* enhace anticoagulant effect of coumarins (e.g. warfarin)

short term use (i.e. post operative analgesic)
* unlikely to have an effect

40
Q

What is the effect of concomitant use of paracetamol and antiepileptic drugs?

A

(antiepileptic drugs like carbamazapine, phenobarbital and phenytoin)

metabolism of paracetamol is accelarated thus reducing its analgesic efficacy

41
Q

Briefly describe the drug interaction that occurs between paracetamol and busulfan

A
  • metabolism of cytotoxic drug busulfan is inhibited in the presence of paracetamol
  • thus caution is advised within 72 hours of paracetamol use
42
Q

1g dose of paracetamol provides analgesia for…

A

4 hours

43
Q

What is the maximum dose of safety for paracetamol?

A

4g

[[hence 1g dose of paracetamol cannot be taken every 4 hours despite the analgesic effect wearing off after 4 hours]]

44
Q

What formulation of paracetamol can improve patient compliance with regards to appropriate dosing?

A

controlled release formulation

45
Q

Why should control release formulations of paracetamol be taken regularly and not “as required”?

A

they may take as long as 4 hours to reach peak analgesic effect

46
Q

Outline the composition of the modified release paracetamol preparation Panadol Extend

A
  • bilayer tablet contaning paracetamol 665mg
  • one layer containng immediate release paracetamol (31% 0ff 665mg)
  • second layer containing sustained release paracetamol (69% of 665mg)
47
Q

What is the recommended dose of Panadol Extend?

A

2 665mg (1.33g) tablets 3x daily
maximum daily dose of 6 tablets (3.99g)

48
Q

Panadol extend can provide analgesic relief for up to __ hours

A

8

49
Q

What route of administration for paracetamol has a predictable onset and duration of action?

A

parenteral

50
Q

1g of IV paracetamol has a similar analgesic efficacy to …

A

2 g of the prodrug of paracetamol, proparacetamol

51
Q

What is second port of call (after paracetamol) for analgesia in children?

A

ibuprofen

52
Q

What is the first choice OTC for analgesia and antipyresis in children?

A

paracetamol

53
Q

Children seem to be less susceptible to acute toxicity with paracetamol compared to adults. True or false

A

True

54
Q

What is the global paediatric dose for paracetamol ?

A

varies between 10-15mg/kg

55
Q

What is the paediatric dose of paracetamol in the UK?

A

10mg/kg every 4-6 hours up to a maximum of 4 doses a day

56
Q

What is the recommended paediatric dose of paracetamol in the USA?

A

10-15mg/kg up to 5x daily
total dose of 50-75mg/kg

57
Q

What is the recommended paediatric dose of paracetamol in Australia?

A

15mg/kg every 4 hours
total dose of 60mg/kg/day

58
Q

Oral elixirs of paracetamol cannot be used to substitute purpose made suppositories. Why is this?

A

this is because they are not absorbed rectally

59
Q

What is the analgesic of choice in pregnancy?

A

paracetamol

60
Q

Why is the use of paracetamol not contraindicated in breastfeeding despite it being excreted in breast milk?

A

it is not excreted in clinically significant amounts

61
Q

Codeine alone is a poor analgesic for acute pain. What can improve its analgesic strength?

A

combination with paracetamol

62
Q

What is the NNT of paracetamol (600/650mg) with 60mg of codeine ?

A

3.6

63
Q

What is the NNT of 1g of paracetamol with 60mg of codeine?

A

2.2

(lower NNT- higher analgesic efficacy)

64
Q

What compound analgesic containing paracetamol was withdrawn from the UK market by the MHRA? Why?

A

Co-proximol
325mg paracetamol + 32.5 mg dextroproxyphene

due to fatal toxiciy with often as little as 15-20 tablets particularly when taken with alcohol

65
Q

What paracetamol /NSAID combination has shown signs of superiority compared to others according to cochrane systematic reviews?

A

paracetamol and ibuprofen

66
Q

What does the choice of analgesia depend on?

A
  • the anticipated severity of post operative pain
  • age
  • patient health
67
Q

Paracetamol has grown in its use for intravenous day case GA for oral surgery. True or false

A

True

68
Q

What is the oral dose of paracetamol for adults?

A

1g every 4-6 hours
Maximum 4g for 24 hours

69
Q

What is the oral dose of paracetamol for children aged 2-4 years old?

A

180mg

70
Q

What is the oral dose of paracetamol for children aged 4-6 years old?

A

240 mg

71
Q

What is the oral dose of paracetamol for children aged 6-8 years old ?

A

240-250mg

72
Q

What is the oral dose of paracetamol for children aged 8-10 years old?

A

360-375mg

73
Q

What is the oral dose of paracetamol for children aged 10-12 years old?

A

480-500mg

74
Q

What is the oral dose of paracetamol for children aged 12-16 years old?

A

480-750mg

75
Q

What is the IV infusion dose over 15 minutes for paracetamol for children 10-15kg in weight?

A

15mg/kg every 4-6h
maximum 60mg/kg/24h

76
Q

What is the IV infusion dose over 15 minutes for paracetamol for adults and children over 50kg?

A

1g every 4-6 hours
max 4g/24 hours

77
Q

What is the dose of paracetamol by rectum for adults and children over 12 years?

A

1g ever 4-6 hours
max 4g/24hours

78
Q

What is the dose of paracetamol by rectum for children 1-5 years old?

A

125-250mg

79
Q

What is the dose of paracetamol by rectum for children 5-12 years old ?

A

250-500mg
max 4g/24hours