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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
Q

Effect of opioids on vascular use

A

Histamine release > vasodilation> risk of hypotension

26
Q

Effect of opioids on heart

A

SNS suppression > PNS enhancement (via CNS) :
Miosis
bradycardia
Cardioprotection after MI

27
Q

Effect of opioids on respiratory system

A

Reduced sensitivity to hypoxia (via CNS medulla) > respiratory depression

28
Q

Benefits of opioids on respiratory system

A

Treats breathlessness, cough, acute pulmonary oedema

29
Q

Clinical use of opioids

A

Analgesia
Antidiarrhoeals
Antitussives

30
Q

Opioids side effects

A 
Drowsiness
Constipation 
Dizziness & confusion 
Pruritus (some)
Nausea & vomiting 
Euphoria 
Dependance & withdrawal
Overdose  (unconsciousness,
Opioid drugs
death by respiratory depression)
31
Q

What is tolerance?

A

decreased sensitivity to drug with chronic use: increased dose required for similar effect

32
Q

What cause drug tolerance in opioids

A

desensitisation and endocytosis of opioid receptors

33
Q

Opioids withdrawal symptoms

A

Restlessness, anxiety, insomnia (early)
Diarrhoea, nausea, abdominal cramps, tachycardia,
high blood pressure (late, often intense)

34
Q

Codeine is converted into morphine via

A

Hepatic metabolism

35
Q

Morphine

A

Strong analgesic used in moderate-severe pain.

Also used in myocardial infarction, acute pulmonary oedema and dyspnoea

36
Q

How is morphine administered?

A

Oral or injection

Infusion pumps

37
Q

Analgesics often measured by “equianalgesic” comparison to which opioid?

A

Morphine

38
Q

Codeine

A

Weak opioid analgesic & cough suppressant

39
Q

____ of codeine is converted to morphine in first pass metabolism.

A

20%

40
Q

In approximately 10% of population codeine is not effective, why?

A

Limited CYP2D6

41
Q

Co-codamol

A

Codeine + paracetamol

42
Q

Most common opioid taken

A

Codeine

43
Q

Diamorphine (heroin)

A

Strong opioid analgesic severe pain Also used after myocardial infarction

44
Q

Properties of diamorphine

A

Highly lipophilic – rapidly crosses BBB Vastly increases euphoric experience Major drug of abuse

45
Q

Diamorphine as administered only via

A

Injection - due to first pass metabolism to morphine with oral administration

46
Q

Pethidine

A

Weak opioid

Synthetic, minimal histamine release, ~30% effective as morphine. Fast acting & short half-life. Anticholinergic metabolite (norpethidine).

47
Q

Fentanyl

A

Strong opioid

Synthetic, does not cause pruritis. Lipophilic (transdermal, intrathecal injection). Very strong opioid,
~50-100x morphine.

48
Q

Loperamide

A
  • 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
Q

Naloxone

A

Short acting Opioid antagonist
Respiratory recovery in newborn infants
Precipitates withdrawal in addicts
Normally by injection; oral relief of opioid constipation

50
Q

Naltrexone

A

Long-acting opioid antagonist
Opioid addiction recovery (subcutaneous implant) Alcohol addiction recovery
Pruritus in chronic liver disease

51
Q

Methylnatrexone

A

Opioid antagonistic

Peripheral only – relieve opioid-induced constipation and nausea

52
Q

Neuropathic Pain

A

Pain due to nerve disorder - diabetes, damage

53
Q

How is neuropathic pain treated

A

With antidepressants (e.g. amitryptiline) or anticonvulsants (e.g. pregabalin, carbamazepine)

54
Q

Tramadol

A

serotonin-noradrenaline reuptake inhibitor ~25% morphine equianalgesia
Used for mod-severe pain

55
Q

Tramadol is more effective to treat

A

Neuropathic pain

56
Q

Side effects of Tramadol

A

Less respiratory depression, but convulsion risk Hallucination risk

57
Q

Tapentadol

A

Similar to tramadol but only inhibits NA reuptake. ~40% morphine equianalgesia.

UM2010 Pharmacology (7 decks)

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