Opioids Flashcards

1
Q

Name an analgesic for each stage in the WHO ladder:

Simple analgesia
Weak opioid
Strong opioid

A

Paracetamol, NSAID

Codeine

Morphine, fentanyl, oxycodone, alfentanil, methadone

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2
Q

Why are NSAIDs preferred over opioids in arthritis?

A

NSAIDs work better,

Tackle inflammation

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3
Q

To which two drug classes does neuropathic pain (e.g. diabetic neuropathy) respond well?

A

Antidepressants

Anticonvulsants

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4
Q

Describe the administration options of morphine

A

Basically all:
IM, IV, SC, PR, PO (syrup)
H/e gut absorption is unpredictable and morphine has high first pass metabolism

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5
Q

Decribe the distribution of morphine in relation to tissues, placenta and BBB

A

All tissues

Crosses the placenta and acts on the foetus (bab may be born with resp depression and withdrawl sx)

Struggles to cross the BBB therefore pts don’t get much of a high

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6
Q

How is morphine metabolised, and what effect do the metabolites have?

A

Glucuronidation in the liver

M3G - can cross the BBB and irritate the brain (morphine 3rd gen - pretty shit)

M6G - analgesic effect (morphine 6th gen - good shit)

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7
Q

How is morphine eliminated?

A

Renal elimination

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8
Q

What is the MoA of morphine?

A

Complete activation of u receptors

Minimal effect on K and delta

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9
Q

When is fentanyl used?

A
  • Surgery setting

- Patient-controlled analgesia machines

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10
Q

Name three ways fentanyl can be administered

A

IV
Epidural
PO

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11
Q

What is the metabolism and elimination of fentanyl?

A

Metabolised in the liver by CYP3A4

Eliminated by the kidneys, but less so than morphine so can be used in ore renally impaired pts

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12
Q

How do the affinity and intrinsic activity of fentanyl compare to morphine?

A

Higher therefore fentanyl is more potent

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13
Q

State three side effects of morphine and fentanyl

A
  • Resp depression (reduces responsiveness of the medullary resp centre to CO2)
  • Emesis (stimulates CTZ)
  • Constipation and nausea
  • Asthma attacks in asthmatics (mast cell degranulation, more so in morphine)
  • Miosis
  • Drowsiness and dizziness
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14
Q

What are the two methods of administration of codeine?

A

PO

SC

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15
Q

How is codeine metabolised, and how does this vary between individuals?

A

Liver
Codeine -> morphine by CY2D6

Some people express this more, so get lots of morphine and side effects

Some people express this less therefore codeine doesn’t work

Inhibited by fluoxetine

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16
Q

How does the potency of codeine compare to morphine?

A

Not as potent, therefore used more for mild to moderate pain and as a cough depressant

17
Q

State two side effects of codeine

A

Constipation (give laxative if using long term)

Resp depression (worse in children bc of larger adenoids and tonsils which can obstruct airways)

18
Q

State three uses for buprenorphine

A

Chronic pain

Palliative care (admin options, and less likely to have falls)

Opioid addiction treatment

19
Q

State tw administration options of buprenorphine

A
  • Transdermal (patch on the skin, lasts for a week)
  • Buccal
  • Sublingual
20
Q

Describe the metabolism of buprenorphine

A

Half life of 37hrs

Liver
By CYP3A4, then glucuronidation

21
Q

How is buprenorphine eliminated?

A

Billiary excretion

Therefore safe in renally impaired

22
Q

Compare the affinity and action of buprenorphine

A
Very high affinity for the u receptor
partial agonist (low intrinsic activity) therefore fewer side effects and less activation of receptors
23
Q

State three administration options of naloxone

A

IV, IM, intranasal

PO has a 2% bioavailability so not rly used

24
Q

What is naloxone used for?

A

Competitive antagonist of u receptors, so used to treat opioid overdose

Can give people close to known addics nasal naloxone, so if the pt overdoses, friend can give naloxone before ambulance arrives

Has a short half-life (30-60mins) so give as slow infusion so you don’t crash from the overdose again

25
Q

State three cases which give cause for special consideration as to whether or not to give opioids

A
Manual labourers
Drivers
Elderly
Renal impairment
Billiary tract obstruction
Asthmatics
Pregnant women
26
Q

State three cases where opioids are contraindicated

A
Hepatic failure
Acute resp distress
Comatose
Head injury (M3G irritate brain)
Raised ICP
27
Q

What would a typical presribing regime be for someone on palliative care concerning opioids?

A

Long acting opioid e.g. zomorph

Short acting opioid for breakthrough pain relief e.g. oramorph

Drugs to manage side effects of nausea and constipation