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Pharmacology > HNNS L16 - Opioid Analgesics > Flashcards

HNNS L16 - Opioid Analgesics Flashcards

1
Q

Examples of strong opioid analgesics

A

Morphine & related compounds, e.g. codeine, heroin

Phenylpeperidines, e.g. pethidine, fentanyl and derivatives

Methadone

*For intense pain

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2
Q

Examples of mild opioid analgesics

A

Propoxyphene, e.g. dextropropoxyphene, Doloxene, Dologesic (banned???)

Partial agonists, e.g. Pentazocine, Buprenorphine (Temgesic), Butorphanol, Tramadol[?]

*For mild pain

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3
Q

Fentanyl

A

Strong opioid

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4
Q

Sufentanil

A

Strong opioid (fentanyl family)

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5
Q

Alfentanil

A

Strong opioid (fentanyl family)

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6
Q

Remifentail

A

Strong opioid (fentanyl family)

  • ultra-short-acting
  • low lipid solubility
  • -> does not show much increase in the time required for a certain % drop in effector site concentration in prolonged infusion
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7
Q

Codeine

A

Morphine related opioid analgesic

Strong opioid

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8
Q

Heroin

A

Morphine related opioid analgesic

Strong opioid

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9
Q

Methadone

A 
(Physeptone)
Strong opioid
Longest acting
Used for getting over opioid addiction
'Complex' analgesic (activity not solely based on opioid receptor)
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10
Q

Effect when you use strong and mild opioids together

A

Weaker than using strong opioid alone.
(Mild opioids displacing the strong opioids)
*NO synergistic effect!!!

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11
Q

Dextroprophoxyphene

A

Under prophoxyphene

Mild opioid

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12
Q

Doloxene

A

Under prophoxyphene

Mild opioid

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13
Q

Pentazocine

A

Partial opioid receptor agonist (mixed agonist / antagonist)

Mild opioid analgesic

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14
Q

Buprenorphine (Temgesic)

A

Partial opioid receptor agonist (mixed agonist / antagonist)

Mild opioid analgesic

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15
Q

Butorphanol

A

Partial opioid receptor agonist (mixed agonist / antagonist)

Mild opioid analgesic

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16
Q

Tramadol

A

Partial opioid receptor agonist (mixed agonist / antagonist)[?]
Mild opioid analgesic

No major side effects except

  • nausea / vomiting
  • miosis
  • constipation
  • drug interaction with anti-depressants

Not a controlled drug

17
Q

Which opioid analgesic is NOT a controlled drug?

A

Tramadol
(No major side effects e.g. respiratory depression;
No euphoria –> not likely to abuse)

18
Q

Drug interaction of tramadol

A

(Mild opioid analgesic)
Drug interaction with anti-depressants
- decrease serotonin, NA uptake in CNS

19
Q

Side effects of Tramadol

A

(Mild opioid analgesic)

  • nausea / vomiting
  • miosis
  • constipation
  • drug interaction with anti-depressants
20
Q

What features of opioid analgesics cause higher addictive potential?

A

Euphoria

Higher lipid solubility + higher non-ionized fraction –> favour crossing of BBB

21
Q

What parameter to look at when you want an opioid analgesic with faster onset? Is it preferrable to have a faster onset?

A 
Lipid solubility (favour crossing of BBB)
Non-ionized fraction????

Faster onset –> easier to correct the dosage (prevent respiratory depression)

22
Q

Opioid analgesic: peak effect site concentration determined by… (explain in terms of plasma concentration and effect site concentration)

A

Peak effect site level = isoconcentration level (level at which plasma concentration = effect site concentration)

Before:

  • plasma concentration dropping
  • effect site concentration increasing

After isoconcentration, both drop.

23
Q

What to take note of if you want to repeat administration of opioid analgesics?

A

Reduce subsequent doses if repeated administration of opioid analgesics is required.

Longer infusion time of opioid –> longer time required to show a certain % decrease in effector site concentration

  • Drugs would accumulate in peripheral tissues, e.g. muscles and fat
  • Slowly diffuse out –> redistribute to CNS

*Over therapeutic window: respiratory depression

24
Q

Metabolism of morphine

A

Formation of normorphine, morphine-3-glucuronide and morphine-6-glucuronide in liver

Morphine-6-glucuronide is an ACTIVE metabolite (30% morphine activity)
- Do NOT miss it when considering the dose.

Excretion by kidneys
- dysfunction –> accumulation of active metabolites

25
Q

Giving morphine to patients with

  1. Liver failure
  2. Renal failure
A
  1. Liver responsible for metabolising morphine into normorphine, morphine-3-glucuronide and morphine-6-glucuronide (active metabolite)
    - -> accumulation of morphine
  2. Kidney for excretion of metabolites of morphine
    - -> accumulation of ACTIVE metabolites
26
Q

Giving pethidine to patients with renal failure?

A

Pethidine: renal excretion of metabolite *norpethidine (from minor pathway)
*major pathway: esterification, conjugation

  • -> Norpethidine may accumulate in kidney dysfunction
  • -> convulsion
27
Q

Route of administration for opioid analgesics

A
  1. IV
  2. Indwelling subcutaneous patch
  3. Transmucosal (lollipop-like)
  4. Epidural / Subarachnoid
  5. Transdermal

*Patient-controlled Analgesia

Oral administration not preferred

  • Many side effects (vomit the drugs out!)
  • Decreased absorption with first pass effect
28
Q

Advantage of epidural / subarachnoid administration of opioid analgesic

A

Bypass BBB –> more effective

29
Q

Acute side effects of opioid analgesics

A
  1. Sedation
  2. Nausea / vomiting
  3. Respiratory depression
  4. Euphoria
  5. Miosis
30
Q

Side effects of prolonged use of opioid analgesics

A
  1. Constipation
  2. Tolerance / dependence
  3. Acute side effects:
    - Sedation
    - Nausea / vomiting
    - Respiratory depression
    - Euphoria
    - Miosis
31
Q

For opioid analgesics, instead of reading ED50 and LD50 for the therapeutic window, what should we read?

A

ED95 and LD05

- LD05 already very dangerous!

32
Q

Which of the following causes the most severe euphoria?

Morphine, Methadone, pethidine

A

Pethidine > morphine > methadone

33
Q

What defines physical dependence of morphine?

A

It is the physiological adaptation of the body to the presence of an opioid, an is defined by the development of withdrawal symptoms when

  • opioids are discontinued,
  • dose is reduced abruptly, or
  • an antagonist (e.g. naloxone) or a partial agonist (e.g. pentazocine) is administered
34
Q

What to take note of when administering opioid analgesics?

A

According to the Dangerous Drugs Regulations, medical practitioners are required to maintain proper records of ALL dangerous drugs, whether supplied, dispensed or administered.

*Lock it up as well

35
Q

Antagonist of opioid analgesic

A

Naloxone (Narcan)

  • For PCA overdose for exmaple
  • IV
  • Half-life shorter than most opioid analgesics –> keep the patient for observation after one dose
36
Q

Naloxone (Narcan)

A

Antagonist of opioid analgesics

  • e.g. for PCA overdose
  • IV
  • Half-life shorter than most opioid analgesics –> keep the patient for observation after one dose
37
Q

Which opioid analgesic would interact with anti-depressants?

A

Tramadol

- increase serotonin and NA uptake in CNS

38
Q

Can you release a patient with opioid overdose after giving one dose of naloxone (opioid antagonist)?

A

No.
Half life of naloxone is shorter than most opioid analgesics.
Keep the patient under observation after one dose of naloxone.

39
Q

What to take note of when choosing an opioid analgesic?

A
  1. Efficacy
  2. Side effects
  3. Onset and duration
  4. Route of administration and availability
  5. Safety
  6. Addictive potential

Pharmacology (10 decks)

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