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Pharmacology 3001 > Pain I: Opioids - McDougall 1 > Flashcards

Pain I: Opioids - McDougall 1 Flashcards

1
Q

What is pain?

A

An unpleasant sensory and emotional experience associated with actual or potential tissue damage, or described in terms of such damage

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2
Q

Nociception

A

Physiological processes in response to noxious stimuli

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3
Q

Allodynia

A

Pain in response to a normally innocuous stimuli

Enhanced pain repsonse

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4
Q

Hyperalgesia

A

Enhanced pain to a normally painful stimuli

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5
Q

Nociceptive pain

A

Direct activation of nociceptors by noxious stimuli

Ie. Touching something hot

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6
Q

Inflammatory pain

A

Activation by inflammatory mediators

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7
Q

Neuropathic pain

A

Pain arising from nerve damage

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8
Q

Pain pathway

A

Ascending processes
Nociceptor - Primary afferent - Dorsal root ganglion (cell body) - Second order neuron in SC - Brain

Pain sensation, cognitive interpretation, affective behaviour

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9
Q

Normal movement pathway

A

Ascending processes

Mechanosensors - Primary afferent - Dorsal root ganglion (cell body) - Second order neuron in SC - Brain

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10
Q

Peripheral sensitization pathway

A

Ascending processes

Nociceptor - Primary afferent - Dorsal root ganglion (cell body) - Second order neuron in SC - Brain

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11
Q

Central sensitization pathway

A

Ascending processes

Nociceptor - Primary afferent - Dorsal root ganglion (cell body) - Second order neuron - brain

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12
Q

Referred pain

A

Pain at a point in the body
Nerves in areas surrounding synapse onto the same projection neutron, giving feeling of pain in those areas too
Because of development of fetus and different derm layers

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13
Q

Glyco-heroin

A

To be used as cough suppressant

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14
Q

Mrs. Winslows Soothing Syrup

A

Opium and alcohol for soothing teething children

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15
Q

Opium

A

c. 3400 BC, lower Mesopotamia

1806: isolated morphine

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16
Q

Morphine

A

10% of opium

High analgesia, addictive

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17
Q

Codeine

A

0.3-2% opium

Less powerful analgesia, less addictive

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18
Q

Heroin

A

Bayer and Co synthetically modified morphine to reduce negative side-effects
Replaced 2H with 2CH3CO to make diacetylmorphine
Made heroin: highly potent analgesic but extremely addictive
Passes BBB better than morphine

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19
Q

Opiate

A

Drugs derived from opium

20
Q

Opioid

A

Agents with opiate-like actions
Synthetic
Proteins that mimic opiate actions
Endorphins

21
Q

Narcotic

A 
Sleep inducing (pharmacological)
Producing dependence (legal)
22
Q

Opioid receptor subtypes

A

mu, delta, kappa, NOP

23
Q

Mu opioid receptor

A

Endogenous ligand: endomorphin
Exogenous ligand: morphine, codeine, heroin
Antagonist: CTOP, DAMGO

24
Q

Delta opioid receptor

A

Endogenous ligand: enkephalin
Exogenous ligand: diprenorphine
Antagonist: Naltrindole

25
Kappa opioid receptor
Endogenous ligand: dynorphin Exogenous ligand: etorphine Antaongist: nor-BNI
26
NOP opioid receptor
Endogenous ligand: nociception Exogenous ligand: orphanin FQ(1-11) Antagonist: nocistatin
27
Naloxone
Not-specific antagonist for opioid receptors
28
Site of action of opioids: Periphery
Receptors in periphery Reduction in production of pain causing chemicals Reduction in release of algogenic agents Desensitize peripheral nerve
29
Site of action of opioids: SC
Mu opioid receptors on presynaptic terminal Binding causes reduction of release of excitatory NT, resulting in reduction of CIP, Glu and SP, and reducing Ca influx Postsynaptically, increasing K to cause hyperpolarization
30
Site of action of opioids: Supraspinal
Periaqueductal grey, insular cortex, dorsal raphe nucleus, nucleus raphe magnus Opioids bind to receptors activating descending inhibitory pathways Spinal release of 5-HT and NA Inhibitory nerves activated Receptors close to respiratory centres can cause respiratory depression
31
Site of action of opioids: Mesolimbic system
Ventral tegmental area, nucleus accumbens, amygdala Stimulate dopaminergic circuits involved in reward, euphoria Alters emotional response to pain
32
Acute inflammation
Upregulation of mu-opioid receptors in DRG Increase axonal transportation of MOR Increase in MOR in periphery and dorsal horn Increase opioid analgesia
33
Chronic pain
Most painful conditions, >3mo Opioids have reduced efficacy in chronic pain Down regulations in areas of chronic inflammation Opioid analgesia less effective
34
Negative side effects of opioids
Severe constipation, somnolescence, cardiorespiratory depression Tolerance
35
Tolerance
Increasing doses required to achieve therapeutic level Minimized by "start low, go slow" Occurs 2-3 weeks after frequent opioid use
36
Mechanism of tolerance
Desensitization and trafficking via GPCR kinases After arrestin binding, receptor is desensitized at surface, and then internalized Receptors either recycled to cell surface of degraded in lysosome
37
Treatment of tolerance
Rotation to another opioid | Recouple to a non-opioid adjunct
38
Dependence
Addiction State of physical and psychological dependence Preoccupation with acquiring and using drugs despite knowledge of adverse health effects Risk factors: serious history of substance abuse, mental illness, addictive personality
39
Physical dependence
Drug withdrawal produced physical abstinence syndrome Mild: lacrimation, sweating, yawning Severe: anorexia, cramps, nausea, vomiting, restlessness, irritability, tremor, HR/BP changes, chills, spasms, PAIN
40
Psychological dependence
Compulsive drug seeking behaviour Occurs with drugs with mood enhancing properties Activated dopaminergic circuits (endogenous reward system)
41
Treatment of dependence
Cessation of drug intake Naltrexone (mu-antagonist) Methalone (mu-agonist)
42
Methalone
Mu-agonist Good oral bioavailability, selective Long-lasting and slow withdrawal
43
Paradoxical opioid-induced hyperalgesia
Prolonged opioid use increases pain Sensitization of peripheral nociceptors Sensitization of dorsal horn neurons Altered descending control mechanisms: Glu receptor involvement therefore, co-adminsiter Glu antagonist
44
Polypharmacy
Opioid + cannabinoid: synergistic effect (mu-opioid receptors dimerize with CB1) Opioid + low dose amphetamine: offset sedation Opioid + antidepressant: useful for neuropathic pain
45
Peripherally restricted opioids
Can target pain at the source Reduce sensitization of nociceptors Do not pass BBB Less likely to cause addiction issues, centrally-mediated site effects like respiratory depression
46
Improve opioid receptor levels
Inhibit beta-arrestin activity to reduce receptor internalization Inhibit receptor degradation (proteinase inhibitors) Promote receptor recycling

Pharmacology 3001 (19 decks)

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