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Gwen - Anaesthetics > Opiods - Strong > Flashcards

Opiods - Strong Flashcards

1
Q

What are indications for strong opioids?

A
  • Acute severe pain
  • Relief of chronic pain
  • Relief of breathlessness in the context of end of life care
  • Relieve anxiety and breathlessness in acute pulmonary oedema
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2
Q

What is the mechanism of action of strong opiods?

A

Act against mu receptors in the CNS. Activation of these G protein-coupled receptors has several effects that, overall, reduce neuronal excitability and pain transmission.

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3
Q

How do opioids cause respiratory depression?

A

In the medulla, they blunt the response to hypoxia and hypercapnoea, reducing respiratory drive and breathlessness.

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4
Q

How do opioids reduce sympathetic activity?

A

By relieving pain, breathlessness and associated anxiety, opioids reduce sympathetic nervous system (fight or flight) activity

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5
Q

What are the main opioid receptors?

A
  • Mu receptors
  • Delta Receptors
  • Kappa receptors
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6
Q

What type of membrane protein are opioid receptors?

A

G-protein coupled transmembrane receptors

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7
Q

How does binding of opioids to opioid receptors dull pain?

A

Causes reduction of synaptic transmission

  • Closing of presynaptic Ca2+ channels → hyperpolarization → reduced release of acetylcholine, noradrenaline, serotonin, glutamate, nitric oxide, and substance P (presynaptic inhibition)
  • Opening of postsynaptic K+ channels → hyperpolarization (postsynaptic inhibition)
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8
Q

What are the two main mechanisms by which opioids relieve pain?

A
  • Raise pain threshold
  • Change in pain perception
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9
Q

What is the mechanism of action of tramadol?

A

A synthetic analogue of codeine - best classified as a ‘moderate’ strength opioid. Once made active, acts against:

  • µ-receptor agonists
  • Serotonergic pathways
  • Adrenergic pathways

Due to Sertonergic and Adrenergic activity, acts as serotonin and norad reuptake inhibitors - contributes to effect

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10
Q

What are the therapeutic effects of opioids which act against mu receptors?

A
  • Analgesia
  • Slowed GI transit
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11
Q

What are side effects of mu receptor agonism?

A
  • Respiratory depression with subsequent rise in CO2 (and possibly ICP)
  • Constipation
  • Miosis
  • Bradycardia
  • Strong addiction
  • Euphoria
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12
Q

What are therapeutic effects of delta receptor agonism?

A

Analgesia

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13
Q

What are the side effects of delta receptor agonism?

A
  • Respiratory depression
  • Tolerance
  • Addiction
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14
Q

What are therapeutic effects of kappa receptor agonism?

A
  • Analgesia
  • Sedation
  • Slowed gastrointestinal transit
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15
Q

What are side effects of kappa receptor agonism?

A
  • Dysphoria
  • Sedation
  • Constipation
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16
Q

What is meant by receptor affinity in terms of opioids?

A

Certain opioids have a stronger receptor affinity than comparatively stronger opioids - the weaker opioid inhibits the stronger opioid competitively, which has no effect

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17
Q

What is meant by intrinsic activity of opioids?

A

Substances that bind to a receptor but have no intrinsic activity can antagonise the effect of the agonists, if the receptor affinity of the antagonist is higher

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18
Q

What does the strongly lipophilic nature of fentanyal mean in terms of onset and penetration in the CNS?

A

Rapid onset of action and penetration into the CNS

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19
Q

What are examples of strong opioids?

A
  • Morphine
  • Morphine sulphate modified release tablets (MST)
  • Morphine PCA
  • Fentanyl PCA
  • Oxycodone
  • Tramadol
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20
Q

What are side effects of strong opioids?

A
  • Respiratory depression
  • Neurological depression
  • Nausea and vomiting
  • Pupillary constriction
  • Constipation
  • Tolerance
  • Dependence
  • Withdrawal reaction
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21
Q

How would you treat acute severe pain in a high dependency area?

A

IV morphine for rapid effect - 2-10mg

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22
Q

How might you treatacute severe pain in a ward setting?

A

Morphine IM/SC

23
Q

What is the brand name given to short acting morphine tablets?

A

Sevredol

24
Q

What is oromorph?

A

Morphine Oral solution - short acting morphine

25
Q

What is MST?

A

Long acting (modified release) morphine

26
Q

What is shortec?

A

Short-acting oxycodone capsules

27
Q

How is fentanyl administered?

A
  • Sublingual tablets
  • Nasal spray
  • Transdermal patches
28
Q

What is the most appropriate route of administration of strong opiates in chronic pain?

A

Oral

29
Q

If prescribing morphine for chornic pain, what would you initially start with?

A

Oromorph 5mg every 4 hours - immediate release

30
Q

When prescribing opioids for chronic pain, what would you you prescribe following initially titrating oromorph dose?

A

MST

31
Q

How would you calculate dosing for breakthrough analgesia?

A

Prescribe immediate release morphine at 1/10th to 1/6th of the regular 24 hour dose, as required.

32
Q

Why can partial opioid agonists cause withdrawal symptoms in patients with strong opioid/full potency opiates?

A

Receptor affinity: certain opioids have a stronger receptor affinity than comparatively stronger opioids → the weaker opioid inhibits the stronger opioid competitively, which then has no effect → opioids of different potencies must not be combined

33
Q

When converting opioids from one opioid to another, what is used as the reference potency?

A

Morphine (relative potency: 1) → a higher relative potency allows a lower dose for the same analgesic effect

34
Q

How much stronger is oxycodone than morphine?

A

2x stronger

35
Q

How much more potent is fentanyl than oral morphine?

A

Approximately 100-150 times more potent than oral morphine

36
Q

How much more potent is alfentanil than oral morphine?

A

Approximately thirty times more potent than oral morphine

37
Q

What are indications for prescribing alfentanil?

A
  • Third line for moderate to severe opioid responsive pain in patients unable to tolerate morphine, diamorphine or oxycodone due to persistent side effects
  • Injectable analgesic for moderate to severe, opioid responsive pain in patients with Stage 4-5 CKD, or severe acute renal impairment.
  • Episodic/ incident pain.
38
Q

What are indications for prescribing fentanyl?

A
  • Second line opioid for moderate/severe opioid responsive pain.
  • Pain that is stable.
  • Oral and subcutaneous routes are not suitable.
  • Patient unable to tolerate morphine/ diamorphine due to persistent side effects.
  • Compliance is poor, but supervised patch application is possible.
39
Q

What would you consider giving to someone on strong opiates?

A

Antiemetics and Laxatives

40
Q

How would you titrate dose of oral morphine to control pain?

A
  • Increase regular oromorph dose each day in steps of about 30% (or according to breakthrough doses used) until pain is controlled or side effects develop.
  • Increase laxative dose as needed.
  • Convert to MST when stable.
  • Divide 24 hour dose of immediate release morphine by 2.
  • Prescribe as MST - 12 hourly.
  • Prescribe breakthrough analgesia at correct dose (1/10th to 1/6th of 24 hour morphine dose).
41
Q

What are features of opioid toxicity?

A
  • Altered mental status (euphoria to apathy)
  • Bilateral miosis (pinpoint pupils)
  • Respiratory depression (decreased RR and tidal volume)
  • Seizures
  • Decreased bowel sounds
  • Decreased heart rate and blood pressure, hypothermia
  • Rhabdomyolysis
42
Q

How would you manage opioid toxicity?

A
  • Airway management
  • IV naloxone
  • Manage complications - e.g. seizures
43
Q

What is the classic triad of opioid toxicity?

A
  • Altered metnal status
  • Respiratory Depression
  • Miosis
44
Q

What is important to remember about the administration of naloxone?

A

Quickly metabolised - effect can wear off

45
Q

What is the mechanism of action of naloxone?

A

Binds to opioid receptors (particularly mu receptors), where it acts as a competitive antagonist. It has little to no effect in the abscence of an exogenous opioid. It is used to restore an adequate level of consciousness and RR

46
Q

What are side effects to naloxone use?

A

Opioid withdrawal reaction

47
Q

What are features of opioid withdrawal?

A
  • Flu-like symptoms: rhinorrhea, chills, piloerection, myalgia, arthralgia, leg cramps
  • Gastrointestinal complaints: nausea, vomiting, abdominal pain, diarrhea, hyperactive bowel sounds
  • Features of sympathetic hyperactivity: mydriasis, tachycardia, hypertension, hyperreflexia
  • Features of CNS stimulation: insomnia, yawning, irritability, anxiety, agitation, aggression
48
Q

What are the flu like syptoms of opioid withdrawal?

A
  • Rhinorrhoea
  • Chills
  • Piloerection
  • Myalgia
  • Arthralgia
  • Leg cramps
49
Q

What are GI symptoms of opioid withdrawal?

A
  • Nausea
  • Vomiting
  • Abdominal pain
  • Diarrhoea
  • Hyperactive bowel sounds
50
Q

What are sympathetic features of opioid withdrawal?

A
  • Mydriasis
  • Tachycardia
  • Hypertension
  • Hyperreflexia
51
Q

How would you treat opioid withdrawal?

A

Buprenorphine/methadone

52
Q

What side effects of opioids diminish with chronic use?

A

Sedative, orthostatic and emetic effects

53
Q

What side effects of opioid use persist with chornic use?

A

Miosis and constipation

Gwen - Anaesthetics (16 decks)

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