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pharmacology 3 > non-opioid and opioidanalgesia > Flashcards

non-opioid and opioidanalgesia Flashcards

1
Q

analgesia

A

absense of pain in response to stimulation which would normally be painful

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2
Q

anagesic

A

pain killers

drugs that result in analgesia

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3
Q

maajor calsses of analgesics

A

opiod

non-opiod - NSAIDS, paracetomol, other

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4
Q

nociceptive pain

A

adaptive, high threshold pain

early warning system

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5
Q

inflammatory pain

A

adaptive, low threshold pain

tenderness and promotes repair

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6
Q

proostaglandin synthesis pathway

A 
essential fatty acids 
membrane phospholipids 
arachidonic acid 
prostaglandin H2
prostacyclin, prostaglandins, thromboxane
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7
Q

what do NSAIDS do

A

block cyclo-oxygenase (COX) which is normally responsible for converting arachidonic acid into Prostaglandin H2

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8
Q

GI adverse effects of NSAIDS

A

GI irritability, inflammation, bleeding

gastric/duodenal ulceration (bleeds/peforations)

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9
Q

renal adverse effects of NSAIDS

A

no effect if normal renal function
fl;uid retention, oedema, hypertenson (significant in patients wth heart failure
renal dysfunction/failure (acute/chronic)

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10
Q

platelet adverse effects of NSAIDs

A

increase risk of bleeding (non-selectve NSAIDs)

selective COX-2 inhibition leads to increased risk of thrombotic events

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11
Q

respiratory adverse effects of NSAIDs

A

15% asthmatics get NSAID-induced asthma

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12
Q

3 effects of NSAIDs

A
  • anti inflammatory
  • analgesics
  • anti-pyretic effects (prevent or reduce fever)
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13
Q

choice of NSAID depends on

A
  • route of administration
  • duration of treatment
  • patient factors
  • relative contraindications in renal failure, asthma, uncontrolled hypertension, previous GI ulceration/gastritis, inflammatory bowel disease, past stroke or TIA (except aspirin), upcoming surgery or other bleeding risk
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14
Q

non selective NSAIDs

A
  • salicylates - aspirin
  • propionic acids - ibuprofen, naproxen
  • phenylacetic acids - diclofenac, ketorolac (intramuscular)
  • oxicam’s - meloxicam, piroxicam
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15
Q

cox-2 selective

A

coxibs - celecoxib, parecoxib (IV), rofecoxib (withdrawn)

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16
Q

advantages of COX-2 selective inhibitors

A 
coxibs 
lower GI adverse events 
reduced risk of intraoperative bleeding 
do not cause bronchospasm in NSAID sensitive asthmatics 
reduced risk of renal adverse effects
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17
Q

issues with selective cox-2 inhibitors

A
  • rofecoxib was withdrawn from market in 2004 due to increased thromboembolic events
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18
Q

when are NSAIDS and coxibs useful

A
  • useful as non opiod analgesics

- useful in inflammatory condtions

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19
Q

when are NSAIDs and coxibs less useful

A
  • elderly
  • risk of GI ulcers
  • patients with CV risk factors
  • patients with renal risk factors
  • for prolonged use
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20
Q

aspirin is used for

A

analgesc effects

anti-inflammatory effects

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21
Q

analgesic aspirin dose

A

analgesic dose 300-900mg up to three times per day

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22
Q

anti platelet effects of aspirin

A

prevention of acute myocardial infarction and stroke

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23
Q

mechanism of acton of aspirin

A

at low dose it selectively inhibts cyclooxegenase
stops platelet activation - irreversible inhibition of platelt dependant thromboxane A2 formation - inhibits vasoconstricton and platelet aggregation

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24
Q

commonest toxicity of aspirin

A

G side effects simlar to NSAIDs
bleeding - rsk of subdural haemorrhage
long term hgh dose can cause hepatic or renal impairment

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25
Q

reyes syndrome

A

occurs at therapeutic dose of asirin
uncommon, affects mainly children
hepatic failure, encephalopathy, cerebral oedema
mortality is up to 40%
aspirin not recommended for children <12 years

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26
Q

aspirin in overdose

A

1-2% mortality
affects metabolic state - uncouples oxidative phosphorylation
respiratory alkalosis - direct stimulation of respiratory centre
metabolic acidosis - premorbid state
renal papillary necrosis

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27
Q

paracetamol

A

acetaminophen
analgesic effect
antipyretic effect
no antiinflammatory effects

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28
Q

paracetamol method of action

A

only theories

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29
Q

paracetamol is a recommended first line anagesic for

A

osteoarthritis
musculoskeletal pain in elderly
patients with renal disease
treatment of cancer pain

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30
Q

paracetamol is inactive at

A

kidney - no renal impairment
GI tract - no peptic ulcer risk
inflammation - not an anti inflammatory

31
Q

oral bioavailability of paracetamol

A

80%

32
Q

metabolism of paracetamol

A

hepatic metabolism via glucuronidaton to 2 inactive compounds (excreted in urine)
normally a small amount of a highly toxic compound NAPQI (N-acetyl-p-benzoquinolone imine) is produces and rapidly inactivated by the liver

33
Q

paracetamol metabolism in overdose or in abnormal liver function

A

NAPQI levels can increase and cause hepatocellular necrosis - fulminant liver failure

34
Q

risks for paracetamol toxicity

A
  • accidental overdose
  • starvation, malnutrition, low body weight
  • HIV
  • alcoholism
  • deliberate overdose - often unaware of danger
35
Q

opiate

A

all naturally occuring substances with morphone-like proporties

36
Q

opiod

A

general term that also includes synthetic substances with an affinity for opiod receptors

37
Q

opiod receptors

A

abour 400 amino acids
7 transmembrane domains
inhibitory G-protein coupled receptors
3 major classes of receptors

38
Q

opiod agonists

A

opiod agonists binds to receptor and cause inhibition of neurotransmitter release
- leads to hyperpolarization of nuerones (peripheral psinal cord, brain)

39
Q

3 classes of opiod receptors

A

Mu, Kappa, Delta

40
Q

Mu opiod receptor

A 
analgesia
miosis - pupillary constriction 
euphoria 
respiratory depression 
bradycardia 
reduced gut motility 
physical dependance
41
Q

kappa opiod receptor

A

analgesia
sedation
depression
miosis

42
Q

delta opiod receptor

A

analgesia
physical dependance
respiratory depression

43
Q

opiod receptors in the brain

A

brainstem - mu
limbic system - kappa > mu
cortex - kappa > delta > mu

44
Q

opiod receptors in the dorsal horn of the spinal cord

A

presynaptic (analgesia) - mu and delta

postsynaptic - mu and kappa

45
Q

opiod receptors in the PNS

A

on nociceptive fibres expressed after injury - analgesia - mu

46
Q

morphine

A

naturally occuring mu receptor agonist

oral, IV, IM, SC

47
Q

morphine dosing

A

titrate to effects - minimise life threatening adverse effects eg. sedation, respiratory depression
5-10 minute onset of action
peak effect 30-60 minutes following intramuscular administration
duration of action 3-4 hours

48
Q

morphine metabolism

A

metabolised in the liver to
morphine-3-gluconuride
morphine-6-gluconuride
nomorphine

metabolites are renally excreted

49
Q

morphine-6-glucuronide

A

analgesic effect

accumulates in renal failure

50
Q

indications fro morphine use

A

moderate to severe acute pain
palliative care
used perioperatively - during anaesthesia and post operative analgesia

51
Q

considerations for morphine

A

variable sensitivity to opiods
hepatic and renal failure
patients at risk of airway and breathing problems

52
Q

side effects of the mu receptor

A
  • miosis
  • euphoria
  • sedation
  • respiratory depression
  • reduced airway reflexes
  • hypotension
  • pruritis
  • nausea and vomiting
  • constipation
  • urinary retention
  • physical dependance
53
Q

codeine

A

prodrug
inactive until metabolised in the body
often used in combination with paracetamol/ibuprofen
analgesic effect due to demethylaton to morphine
10x less potent than morphine

54
Q

genetic variability for codeine

A

10% of patients lack the enzyme to convert codeine
genetic variability with CYP-2D6 enzyme
small proportion of people are rapid metabolisers there therefore have risk of adverse effects on normal doses

55
Q

codiene bioavailability

A

good oral bioavalability - usualy taken orally (IM route available)

56
Q

uses of codiene

A

mild to moderate acute pain

anttussive (cough supressant)

57
Q

side effects of codeine

A

nausea, vomiting, constipation

58
Q

oxycodone

A
  • synthetic opiod

predominantly Mu-opiod receptor agonist

59
Q

clinicala uses of oxycodone

A

moderate to severe pain relief

60
Q

different preparations of oxycodone

A

immidiate release - endone, oxynorm
controlled release - OxyContin
controlled release with naloxone - Targin

61
Q

naloxone

A

is an oopiod antagonist

reduces opdiod induced constipation and is a deterant from abuse

62
Q

adverse effects with oxycodone

A

similar to morphine
tolerance and dependance can occur with all preparations
increasing rates of addiction, abuse and overdose

63
Q

tramadol

A

atypical central acting analgesic with relatively weak opiod effects
has effects on non-opioid pathways as well

64
Q

mechanism of action of tramadol

A
  • metabolised in the liver to active metabolite
    opioid receptor agonist mu > kappa, delta
    serotonin reuptake inhibitor
    noradrenaline reuptake inhibitor
65
Q

tramadol compared to morphine

A

at equi-analgesic doses, has less respiratory depression and less constipation

66
Q

serotonergic effects of tramadol

A

nausea, vomting and confusion

interaction with other serotonergic drugs - lowers seizure threshold, avoid in epilepsy

67
Q

uses of tramadol

A

useful in situations to avoid opioid adverse effects
- respiratory depression, constipation, abuse, sedation, confusion
neuropathic pain

68
Q

fentanyl

A

synthetic opioid
good parenteral, mucosal and transdermal option (good GI absorption but high first pass metabolism so not effective by oral route)

69
Q

methadone

A

NMDA antagonist effect
good in neuropathic pain
major use is for opioid replacement in addiction (long half life over 24 hours, less sedating, less euphoria, still addictive)

70
Q

pethidine

A

effective pain relief but side effects
short half life, increased risk of seizures especially in renal failure
avoid

71
Q

opioid tolerance

A 
developmetn of the need to increase the dose to achieve the same analgesic effects 
all opioid agonists 
usually takes 2 weeks with morphine 
limits clinial use 
does not imply addiction or abuse
72
Q

physical dependance occurs with

A

abrupt discontinuation, substantial dose reduction or administration of antagonist
occurs with opiod use of longer than a week

73
Q

opioid withdrawal symptoms

A

nausea, vomiting, anorexia, diarrhea, sweating, shivering, anxiety, depresion

74
Q

analgesic ladder

A

mild pain - non opioid
mild to moderate pain - opioid for mild to moderate pain plus non-opioid
moderate to severe pain - opioid for moderate to severe pain plus non-opioid with/without adjuvant analgesic

pharmacology 3 (8 decks)

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