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Pharmacology Term 6 > 8.1- Opioids > Flashcards

8.1- Opioids Flashcards

(43 cards)

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1
Q

Define nociception

A

non-conscious neural traffic in response to potential trauma

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2
Q

Define pain

A

An unpleasant sensory and emotional experience associated with actual or potential tissue damage

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3
Q

Define nociceptive pain

A

pain caused by an inflammatory or non-inflammatory response to an overt or potentially tissue- damaging physical stimulus

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4
Q

Define neuropathic pain

A

pain caused by a lesion or disease of the somatosensory nervous system ( ie to the actual neurone itself )

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5
Q

Name 5 types of analgesia

A
  • Paracetamol
  • NSAIDs
  • Opioids
  • Adjuvants
  • Placebo
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6
Q

What would you give as step 1 on the WHO analgesia ladder? ie MILD PAIN

A

give a NON-OPIOID +/- adjuvant

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7
Q

What would you give on step 2 on the WHO analgesia ladder? ie MODERATE PAIN

A

-give a WEAK OPIOID
+/- non opioid
+/- adjuvant

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8
Q

What would you give on step 3 on the WHO analgesia ladder? ie SEVERE PAIN

A

give a STRONG OPIOID
+/- non opined
+/- adjuvant

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9
Q

Give 3 examples of a non-opioid

A

ibuprofen
other NSAID
Paracetamol
aspirin

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10
Q

Give 3 examples of WEAK OPIOIDS

A

codeine
tramadol
low-dose morphine

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11
Q

Give 4 examples of STRONG OPIOIDS

A 
morphine 
fentanyl
oxycodone 
hydromorphone 
buprenorphine
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12
Q

What are some adjuvants for pain?

A 
antidepressants 
anticonvulsants 
antispasmodic 
muscle relaxant 
bisphosphonate
corticosteroid
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13
Q

What are the primary sensory afferent neurones of pain?

A

Adelta or C fibres

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14
Q

Between which 2 neurones does pain transmission occur?

A

between primary afferent sensory neurone and secondary relay neurone ie synapse of substance P

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15
Q

Where do the primary and secondary neurones synapse?

A

SUBSTANTIA GELATINOSA in the dorsal horn of the spinal cord

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16
Q

Where does inhibition of this pain transmission come from?

A

1) Inhibitory interneurones linked to Adelta and Abeta fibres, inhibiting synapse between primary and secondary neurones
2) inhibitory descending pathways from higher centres of the brain

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17
Q

Where are descending analgesia producing pathways located in the brain?

A

Periaqueductal Grey Matter ( PAG) in the midbrain

projects to Dorsal horn of spinal cord

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18
Q

Describe the central modulation of pain

Study These Flashcards
A
  • PAG sends signals to RVM and carried down medial pathways to serotonergic and Noradrenergic neurones
  • Serotoneric and noradrenergic neurones are stimulated and release Serotonin and NA into spinal cord
  • –> activate inhibitory interneurones which
  • -> release ENDOGENOUS OPIOIDS binding to opioid receptors–> inhibit substance P release to secondary neurones going up ascending pathways
19
Q

DEFINE:
A) Opiate
B) Opioid

Study These Flashcards
A

a) Opiate: any agent derived from opium. ( alkaloid mixture from poppy seeds)
b) OPIOID: substances ( exogenous or endogenous ) with morphine-like properties
- act primarily in the SPINAL CORD and brain to inhibit transmission of pain

20
Q

How do opioid work?

Study These Flashcards
A

bind to specific opioid receptors in the CNS to mimic the endogenous peptide neurotransmitters

21
Q

what are the endogenous opioids released by the inhibitory interneurone?

Study These Flashcards
A

Enkephalins
B-endorphins
Dynorphins

22
Q

Name:
2 natural opioids
3 semisynthetic opioids
3 synthetic opioids

Study These Flashcards
A

NATURAL: morphine, codeine
SEMIsynthetic: hydrocodone, hydromorphone, oxycodone, oxymorphone, Buprenorphine
SYNTHETIC: fentanyl, tramadol, methadone

23
Q

Describe the opioid receptors

Study These Flashcards
A
  • G protein coupled receptors
  • Coupled to Gi; inhibitory G-protein subtype
  • located pre AND post synaptically
24
Q

Name the 4 types of opioid receptors

Study These Flashcards
A

μ mu opioid receptor- most important
δ delta opioid receptor
K kappa opioid receptor
ORL1 ( Opioid receptor like 1 (NOP)

25
Describe opioid action PRE-SYNAPTIC
Gαβγi → Gαi + Gβγi • Gβγi inhibits voltage operated Ca2+ channels (VOCC) • Reduced Ca2+ → less neurotransmitter release of substance P going to ascending pathways
26
Describe opioid action POST-SYNAPTIC
Gαβγi → Gαi + Gβγi • Gβγi opens K+ channels • K+ efflux→ hyperpolarises the cells and makes them less excitable
27
Give an example of: a) An opioid agonist b) A partial opioid agonist c) An opioid antagonist
a) MORPHINE b) BUPRENORPHINE c) NALOXONE
28
Give 3 uses of an opioid antagonist
- treats opioid toxicity - reverses respiratory depression - treatment for opioid dependence
29
Which opioid antagonist is commonly used?
NALOXONE always prescribe with morphine to save time in an emergency half life of 1-1.5 hrs
30
Give some routes of morphine admin
``` IV PO IM SC nebulized rectal epidural ```
31
Which route is the most preferred
IV - gives the most rapid response - AVOIDS hepatic first pass metabolism - often used for severe pain w intrathecal route - patient controls the level of analgesia directly (PCA)
32
Describe the oral pharmacokinetics of morphine
-well absorbed from gut -undergoes EXTENSIVE first pass metabolism w a 25% oral bioavailability normally its half life is 2 hours
33
What are the two metabolites of morphine (orally)?
morphine-6-glucoronide | morphine-3-glucoronide
34
What is the danger of morphine given orally and what condition is it avoided in?
morphine normally has a half life of 2 hrs, BUT one of its metabolites, Morphine-6-glucoronide is pharmacologically equivalent to morphine and has a half life of 4-5 hours this EXTENDS the period of effective analgesia Avoided in hepatic and renal failure as they can impair morphine excretion and increase half lives up to 50 hrs--> can cause morphine toxicity and terminal organ failure
35
What would you give methadone for and why?
suitable for treating chronic pain rather than post-op pain -has a half life of 24 hours
36
What is the special case of codeine pharmacokinetics?
Codeine has to be metabolised to morphine by CYP2D6 in order to become pharmacologically active BUT CYP2D6 polymorphisms (genetic) are present in some Caucasian populations therefore they cannot effectively convert codeine to morphine therefore no analgesia achieved in these populations
37
Name 4 desirable pharmacological effects of morphine?
* Effective analgesia: At spinal and supraspinal level * Sedation & Euphoria: By effect on midbrain dopaminergic, serotoninergic and noradrenergic nuclei * Effect on bowel movements: Decrease in motility, increase smooth muscle tone * Depression of cough reflex: Codeine and morphine have antitussive properties
38
Give a clinical use for each drug: a) Morphine b) Diamorphine c) Methadone d) Tramadol e) Tapendatol
a) analgesic in terminal illness ( ADR is diarrhoea) b) analgesic in terminal illness ( unlicensed epidural analgesic) c) maintenance in dependence d) analgesic ( 5-HT and NA effects) e) Analgesic ( specific mu agonist, NA reuptake inhibitor
39
What opioid is given in labour as analgesia?
PETHIDINE given IM for convulsions as a norpethidine metabolite
40
Name some undesirable side effects of opioids? (10)
``` Respiratory depression Nausea, vomiting Smooth muscle spasm Hallucinations Pruritis Bradycardia Hypotension Miosis Drowsiness Dysphoria ( if no pain, morphine can cause restlessness, unhappiness and agitation ```
41
Why would you get dependence and tolerance on opioid drugs?
down regulation of opioid receptors or decreased production of endogenous opioids body becomes more tolerant to drug therefore increased dose needed for desired effect
42
How should prescriptions for controlled drugs be written?
- INDELIBLE - signed by PRESCRIBER - DATED - contain PRESCRIBER'S ADDRESS
43
What points should a prescription of a controlled drug ALWAYS state?
• the name and address of the patient • the form (and where appropriate the strength) of the preparation; • for liquids, the total volume in millilitres (in both words and figures) to be supplied; • for dosage units, the number (in both words and figures) to be supplied; • in any other case, the total quantity (in both words and figures) to be supplied; • the dose

Pharmacology Term 6 (10 decks)

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