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Clinical Pharmacology > 9.1.2 Opioids > Flashcards

9.1.2 Opioids Flashcards

1
Q

What are the different types of opioids?

A

Endogenous ligands
B-endorphins
Endonorphins
Dynorphins
Enkephalins

Opiates
Codeine
Morphine
Diacetyl morphine

Semi-synthetic
Hydrocodone

Synthetic
Methadone
Fentanyl

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2
Q

What is codeine metabolised to?

A

5% is metabolised to morphine by CYP2D6

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3
Q

How do opioids work?

A

Many endogenous opioid peptides but only 4 receptors

All Gai

µ opioid receptor responsible for most analgesic effects

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4
Q

What is effect of opioid binding at different neurones?

A

Pre-synaptic
Opioid binds causing a reduction in calcium entering the neurone
Reduction of glutamate released

Post-synaptic
Opioid binds causing K+ to move out causing hyperpolarisation, decrease, now further away from threshold potential

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5
Q

What are some examples of opioids?

A

Codeine &
Buprenorphine
Diamorphine
Fentanyl
Morphine
Tramadol &

&-considered to be a weaker opioid

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6
Q

What are opioids used for?

A

Analgesia
Antitussive (cough suppression)
Dyspnoea- pulmonary oedema
Anaesthetic
Anti-diarrhoeal
Palliation

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7
Q

What are the features of morphine?

A

Less lipid soluble
Slower onset
Long duration

PO,IV,IM,SC,PR

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8
Q

What are the features of fentanyl?

A

Highly lipid soluble
Fast onset
Short duration

100x potency of morphine
Less itching

Transdermal,IV,epidural,intrathecal

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9
Q

What are the features of codeine?

A

Prodrug
Primary metabolite less potent than morphine 10% of potency
Morphine as second metabolite~5%
Mediated by CYP2D6

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10
Q

What is the pain ladder?

A

Tool used to determine what pain relief should be given

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11
Q

What are the adverse drug reactions of opioids?

A

MORPHINE

Miosis
Overly sweaty (hyperhidrosis)
Respiratory depression
Pee retention and constipation
Itching
Nausea
Euphoria and dysphoria

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12
Q

When should you be careful in giving opioids?

A

HEROIN because heroin is bad

Head injury/ raised ICP
Exacerbates asthma
Respiratory depression
cOmatose patients
paralytic Ileus
Neonatal abstinence syndrome caused if pregnant

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13
Q

What are some important drug to drug interactions with opioids?

A
  • CNS depressants- including anti-epileptics and benzodiazepines
  • Other opioids
  • Drugs that reduce gut motility
  • Clarithromycin (buprenorphine)
  • Opioid receptor antagonists
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14
Q

What opioids are used in disorder or overdose?

A

Buprenorphine
Methadone
Naloxone (overdose)

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15
Q

What is buprenorphine?

A

Partial agonist
50x potency of morphine
Long action

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16
Q

Why is methadone so useful for opioid abuse?

A

Methadone is much more lipophilic than morphine and has a longer duration of action

Has some NMDA receptor antagonism

17
Q

What is naloxone?

A

Competitive opioid receptor antagonist used in overdose

Rapid distribution

Duration is 30-60 minutes

18
Q

Why may naloxone need to be administered many times in respiratory depression?

A

Short duration only 30-60 minutes

Opioids may still be in the system and act on their receptors again

19
Q

What are the signs of opioid overdose?

A

Airways- blue lips and nails
Breathing- slow, irregular or stopped
Cardiac- slow heart rate, weak pulse, low BP
Doesn’t respond to voice or touch
Eyes- pinpoint pupils

20
Q

How can naloxone be given?

A

Nasal sprays
Pre-filled injections

21
Q

Why are opioids addictive?

A

Reduction in GABA from GABA interneurones

Increased in dopamine as GABA is blocked

Dopamine is associated with please

22
Q

What is tolerance?

A

More of the drug needed to elicit same response

Can need 100x the amount to reduce pain significantly increase risk of death

23
Q

Why does tolerance happen?

A

cAMP compensation
Receptor phosphorylation
Internalisation and uncoupling

24
Q

What happens in cAMP compensation?

A

Increased cAMP without opioid inhibition

Excess of normal function particularly mediated in ventral tegmental area, locus coerules and gut

25
Q

How does withdrawal present?

A

Excess of normal neuronal activity

GABA break is no longer blocked which may lead to overdrive, increased firing and reduced dopamine release

Leads to insomnia, anxiety, excessive sweating, enlarged pupils, tachycardia, tachypnoea and diarrhoea

26
Q

How do people avoid cAMP compensation?

A

Keep taking opioids at higher and higher doses to feel normal

Breathing stops

Anyone can become addicted

27
Q

What are controlled drugs?

A

Classified from A-C based on how harmful it is

These drugs are prohibited in manufacture, supply and possession

28
Q

What are schedules?

A

Controlled drugs are further divided into schedules 1-5 which dictates how they are made, stored, sourced, prescribed etc.

Schedule 1 is not used medicinally
Schedule 2-5 decreasing controls and requirements

29
Q

Where are opioids placed as controlled drugs?

A

Opioids sit in class A-C
Schedule 2,3 and 5

Depending on the drug, preparation and route of admission

Clinical Pharmacology (45 decks)

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