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MD4001 Pharmacology > Opoids > Flashcards

Opoids Flashcards

1
Q

What are included in the WHO’s step 1 in the analgesic ladder?

A
  • Nonopoid
  • Analgesics
  • NSAIDs
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2
Q

What are included in the WHO’s step 2 in the analgesic ladder?

A

Weak opioids

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3
Q

What are included in the WHO’s step 3 in the analgesic ladder?

A
  • Strong opioids
  • Methadone
  • Oral administration
  • Transdermal patch
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4
Q

What are included in the WHO’s step 4 in the analgesic ladder?

A
  • Nerve block
  • Epidurals
  • PCA pump
  • Neurolytic block therapy
  • Spinal stimulators
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5
Q

What is opium?

A

Natural extract of the poppy Papaver somniferum. It contains morphine and other related compounds

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6
Q

What is an opioid?

A

Any substance (natural or synthetic) that produces morphine like effects which are blocked by a morphine antagonist

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7
Q

What is an opiate?

A

A naturally occuring opioid (e.g. morphine)

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8
Q

What is the “ceiling effect”?

A
  • Seen in opioids

- Escalation of dose typically causes side effects without improving analgesia

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9
Q

What are examples of strong opioids?

A
  • Morphine
  • Oxycodone
  • Diamorphine (heroin) (highly lipid soluble)
  • Fentanyl (most commonly used IV opioid)
  • Pethidine (also anticholinergic, tachycardic, will not give pinpoint pupils)
  • Remifentanil (short acting, used in intensive care and anesthesia)
  • Methadone
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10
Q

Conversion factors

A

Learn

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11
Q

What are examples of weak opioids?

A
  • Codeine
  • Dihydrocodeine
  • Loperamide (immodium) (not analgesic, opioid receptors in myenteric plexus, used for diarrhoea)
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12
Q

What is significant property of weak opioids?

A
  • Partial agonsits

- Have a ceiling effect

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13
Q

What opioid is used to treat diahhroea?

A

Loperamide

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14
Q

What is tramadol?

A
  • First developed as anti-depressant
  • Found to have analgesic actions
  • Serotonin and opioid receptors
  • Pro-convulsant drug
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15
Q

What opioid should be avoided in epilepsy?

A

Tramadol

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16
Q

By what route are opioids given post-operatively?

A
  • IV

- IM (through buttock)

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17
Q

What nerve must be avoided during IM injection through the buttocks?

A

Sciatic

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18
Q

By what route are opioids given in palitive care usually?

A
  • Oral (most common)

- Trans-dermal patches (fentanyl)

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19
Q

When in labour, how can opioids be delivered?

A

The extra-dural route

- Catheter is placed in extra dural space, either by bolus or infusion, usually with mixture of local anesthetic

20
Q

What drug can be given via lozenges often in military settings?

A

Fentanyl (oral transmucosal route)

21
Q

What is oral bioavailibility?

A

Percentage of total dose that reaches systemic circulation

22
Q

Give an example of a prodrug?

A

Codeine (has to be metabolised in liver)

23
Q

Where does the vast majority of opioid action take place?

A

Mu opioid receptor (MOP)

24
Q

What are 4 different types of opioid receptors?

A
  • Mu opioid peptide receptor (MOP)
  • Kappa (KOP)
  • Delta (DOP)
  • Nociception
25
Q

Where are mu opioid receptors found?

A

All over the NS

- Specifically pain, peripheral afferent nerve terminals, dorsal horn, PAG, thalamus, cerebral cortex

26
Q

On the primary afferents where are the opioid receptors?

A

Pre-synaptic

- Inhibit the release of glutamate on dorsal horn (diminish the transmission of nociceptor stimulus)

27
Q

What are examples of endogenous opioids?

A
  • Endorphins (produced in pituitary)
  • Dinorphins
  • Enkephalins
28
Q

Describe the structure of the opioid receptor?

A
  • Proteins with a serpentine formation with 7 transmembrane spanning proteins
  • Couples to G proteins
29
Q

Following activation by an opioid what happens to the receptor at a cellular level?

A
  • Closure of voltage sensitive Ca2+ channels
  • Opening of K+ channels, K+ efflux causes hyperpolarisation of the cell, less likely to depolarise
  • Ca2+ influx reduces Neurotransmitter release
  • Inhibition of adenylate cyclase (ATP not converted to cAMP)
  • Reduction in neurotransmitter release (principally glutamate)
30
Q

What is the effect of opioids on the respiratory rate?

A
  • Brain becomes less sensitive to rising CO2 levels and Respiratory Rate depressed, tidal volume depressed also
  • Anti tussive (codeine linctus)
  • Morphine can cause bronchoconstriction in patients with asthma - histamine release
31
Q

What is the effect of opioids on the cardiovascular system?

A
  • Bradycardia (pethidine exception)
  • Direct action on SA node
  • Decreased sympathetic drive
  • Peripheral vasodilation (morphine due to histamine release)
32
Q

What is the effect of opioids on the GI system?

A
  • Delayed motility - nausea and constipation
  • Direct action on CTZ and vestibular sensitisation increased
  • Constipation (usually prescribed with laxatives)
33
Q

What are other side-effects of opioids?

A
  • Urticaria, due to Ach release, causes itch
  • Urinary retention
  • Abcesses, immune supression
  • Decreased ACTH, Prolactin, increased ADH
34
Q

What percentage of people metabolise codeine at a slow rate?

A
  • Western europeans (8-10%)
  • Africans (0-20%)
  • East Asian (0-1%)
35
Q

A mutation in what causes a defect in codeine metabolism?

A

CYP2D6

36
Q

What percentage of people are ultra fast codeine metabolisers?

A
  • Western europeans: 1-4%
  • Southern europeans: 7-10%
  • Africans: 5-30%
  • Arabians: Up to 20%
37
Q

Death in children due to codeine was though to be due to what?

A

Ultra-fast metabolism

38
Q

Where are active opioid metabolites excreted?

A

Kidneys (renal imapairment may lead to toxicity)

39
Q

What is usually the opioid of choice for people with renal impairment?

A

Fentanyl (not metabolised to active metabolites)

40
Q

What can pinpoint pupils indicate?

A

Opioid toxicity

41
Q

What is the starting dose for morphine in adults?

A

Parenteral dose:
- 10mg (0.1mg/kg)
Oral dose:
- 30mg (0.3mg/kg)

42
Q

What is the starting dose for fentanyl in adults?

A

Parenteral dose:

- 100 micrograms (1 - 2 micrograms / kg)

43
Q

What is an opioid antagonist that is used to treat opioid overdose and what are some of its properties?

A

Naloxone

  • High affinity for the receptor but no intrinsic activity
  • Titrated in
44
Q

What is an opioid antagonist that can be used to treat addiction?

A

Naltrexone

45
Q

How can methadone affect a patient’s dental hygiene?

A
  • Sugary
  • Dries mouth and stops secretions in mouth
  • Can give patients “munchies”
46
Q

What is methadone’s biovailibility?

A

High oral

- Low first pass metabolism

MD4001 Pharmacology (8 decks)

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