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UM2010 Pharmacology > Opioids > Flashcards

Opioids Flashcards

1
Q

Classification of opioids

A

Natural
Semi-synthetic
Synthetic

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2
Q

Natural opioids

A

Alkaloids derived from the opium poppy (morphine, codeine)

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3
Q

Semi-synthetic opioids

A

Chemically derived from opiates (diamorphine, hydrocodone)

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4
Q

Synthetic opioids

A

not chemically derived from opiates (fentanyl, pethidine, tramadol)

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5
Q

Opioids receptors

A

μ receptors (MOPr)
κ receptors (KOPr)
δ receptors (DOPr)

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6
Q

Opioids receptors bind to what type of proteins ?

A

Gi or Go

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7
Q

Gi protein function

A

Inhibits adenylate cyclase > reduces activity of protein kinase A

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8
Q

Go protein function

A

Galpha subunit binds to Ca2+channels > less Calcium enters cell L
Gbetagamma subunit binds to K+ channels > more K+ leaves cell

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9
Q

Most important opioids receptors

A

MOPr (gamma)

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10
Q

Endogenous opioids

A

Peptide hormones/ neurotransmitters generally released in response to pain and stress; induce analgesia

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11
Q

β-endorphins

A

produced in and released from pituitary gland; also elevates mood. Mostly acts via μ receptors

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12
Q

Enkephalins

A

released throughout brain; involved in regulation of nociception and elevates mood. Acts via μ / δ receptors.

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13
Q

Dynorphins

A

induces analgesia and but also dysphoria (anxiety, depressive symptoms) via κ receptors

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14
Q

Key sites of action for opioids

A

Peripheral
Spinal
Supra-spinal

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15
Q

Main site of action for opioids

A

Spinal

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16
Q

MOA of opioids

A

Pre-synaptic and post-synaptic suppression

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17
Q

Opioids are most potent at

A

spinal level= inhibition of presynaptic vesicle release and postsynaptic excitability in dorsal horn

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18
Q

Side effects of opioids on CNS

A

Drowsiness
Unconsciousness (overdose)
Decreased cognitive function
No clinical e edit

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19
Q

Side effects of opioids on Chemoreceport Trigger zone (CTZ)

A

Nausea

Vomiting

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20
Q

Side effects of opioids on Limbic system

A

Euphoria
Anxiolytics
Potential for abuse

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21
Q

Opioids receptors in enteric nervous system effect in the GI tract

A

Decreases gastric motility Increased water reabsorption Decreased acid secretion

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22
Q

Why can opioids be sued as a treatment for diarrhoea?

A

Decreases gastric motility Increased water reabsorption Decreased acid secretion

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23
Q

Side effects of opioids of GI tract

A

Constipation for other therapeutic uses

24
Q

Effect of opioids on immune

A

Mast cell degranulation > Pruritis

25
Effect of opioids on vascular use
Histamine release > vasodilation> risk of hypotension
26
Effect of opioids on heart
SNS suppression > PNS enhancement (via CNS) : Miosis bradycardia Cardioprotection after MI
27
Effect of opioids on respiratory system
Reduced sensitivity to hypoxia (via CNS medulla) > respiratory depression
28
Benefits of opioids on respiratory system
Treats breathlessness, cough, acute pulmonary oedema
29
Clinical use of opioids
Analgesia Antidiarrhoeals Antitussives
30
Opioids side effects
``` Drowsiness Constipation Dizziness & confusion Pruritus (some) Nausea & vomiting Euphoria Dependance & withdrawal Overdose (unconsciousness, Opioid drugs death by respiratory depression) ```
31
What is tolerance?
decreased sensitivity to drug with chronic use: increased dose required for similar effect
32
What cause drug tolerance in opioids
desensitisation and endocytosis of opioid receptors
33
Opioids withdrawal symptoms
Restlessness, anxiety, insomnia (early) Diarrhoea, nausea, abdominal cramps, tachycardia, high blood pressure (late, often intense)
34
Codeine is converted into morphine via
Hepatic metabolism
35
Morphine
Strong analgesic used in moderate-severe pain. | Also used in myocardial infarction, acute pulmonary oedema and dyspnoea
36
How is morphine administered?
Oral or injection | Infusion pumps
37
Analgesics often measured by “equianalgesic” comparison to which opioid?
Morphine
38
Codeine
Weak opioid analgesic & cough suppressant
39
____ of codeine is converted to morphine in first pass metabolism.
20%
40
In approximately 10% of population codeine is not effective, why?
Limited CYP2D6
41
Co-codamol
Codeine + paracetamol
42
Most common opioid taken
Codeine
43
Diamorphine (heroin)
Strong opioid analgesic severe pain Also used after myocardial infarction
44
Properties of diamorphine
Highly lipophilic – rapidly crosses BBB Vastly increases euphoric experience Major drug of abuse
45
Diamorphine as administered only via
Injection - due to first pass metabolism to morphine with oral administration
46
Pethidine
Weak opioid Synthetic, minimal histamine release, ~30% effective as morphine. Fast acting & short half-life. Anticholinergic metabolite (norpethidine).
47
Fentanyl
Strong opioid Synthetic, does not cause pruritis. Lipophilic (transdermal, intrathecal injection). Very strong opioid, ~50-100x morphine.
48
Loperamide
* Pethidine analogue (discovered 1976) * Non-analgesic: high affinity substrate for P- glycoprotein transporter in BBB * Effective on myenteric plexus; decreased GI motility * Enterohepatic circulation – minimal metabolism * Treats diarrhoea, travel sickness, IBS
49
Naloxone
Short acting Opioid antagonist Respiratory recovery in newborn infants Precipitates withdrawal in addicts Normally by injection; oral relief of opioid constipation
50
Naltrexone
Long-acting opioid antagonist Opioid addiction recovery (subcutaneous implant) Alcohol addiction recovery Pruritus in chronic liver disease
51
Methylnatrexone
Opioid antagonistic | Peripheral only – relieve opioid-induced constipation and nausea
52
Neuropathic Pain
Pain due to nerve disorder - diabetes, damage
53
How is neuropathic pain treated
With antidepressants (e.g. amitryptiline) or anticonvulsants (e.g. pregabalin, carbamazepine)
54
Tramadol
serotonin-noradrenaline reuptake inhibitor ~25% morphine equianalgesia Used for mod-severe pain
55
Tramadol is more effective to treat
Neuropathic pain
56
Side effects of Tramadol
Less respiratory depression, but convulsion risk Hallucination risk
57
Tapentadol
Similar to tramadol but only inhibits NA reuptake. ~40% morphine equianalgesia.

UM2010 Pharmacology (7 decks)

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