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Psychopharmacology > Opiates > Flashcards

Opiates Flashcards

(61 cards)

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1
Q

General info about opiates?

A

POTENT analgesics (primary medicinal use)

Very reinforcing

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2
Q

When did opiates start getting used?

A

May predate history of man

7000 years +

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3
Q

What are the main effects of opiates?

A

Analgesic

Antitussive (cough-supressant)

Sedative

Gastro-intestinal muscle relaxant (you poop)

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4
Q

Where were opiates derived from historically?

A

Poppy plant

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5
Q

What (ecologically) is opium?

A

The resin that oozes out of poppy plants

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6
Q

Where do you get morphine / codeine from?

A

Extracted from opium

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7
Q

What are the endogenous opioids?

A

Enkephalins
Endorphins
Dynorphins

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8
Q

What are synthetic opiates like compared to naturally-occuring?

A

e.g. fentanyl

100x as powerful as morphine

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9
Q

What pharmacological factor varies administration of opiates?

A

Fat solubility

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10
Q

How is morphine generally administered?

A

Orally, by inhalation, or by injection (injection fastest, it’s slow-absorbing)

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11
Q

How is heroin generally administered?

What is its fat solubility compared to morphine?

A

Smoked or injected.

Increased lipid solubility

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12
Q

What happens to heroin once it’s in the CNS?

A

Converted to morphine

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13
Q

What do naloxone/naltrexone do?

A

Direct opiate antagonists
Synthetically developed

Used in EMT cocktail

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14
Q

What happens to codeine in the CNS?

Where are its effects?

A

Converted to morphine (like heroin)

Little effect on its own, only cough centers in brainstem

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15
Q

Where are all the opiates metabolized?

A

Liver; excreted by kidney in urine

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16
Q

What do the half-lives of morphine / heroin look like?

A

~4 hr

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17
Q

What do the half lives of opiates in general look like?

A

Widely variable

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18
Q

What is the basic pharmacodynamic effect of opiates?

A

Direct agonists

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19
Q

Which receptors do opiates work on?

A

Opiate receptors (three main kinds)

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20
Q

Are opiate receptors metabotropic or ionitropic?

A

Metabotropic

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21
Q

What happens to changes in ion conductances with opiates?

A

Inhibition

Decrease excitability (K+)

Synaptic transmission (Ca2+)

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22
Q

How do opiates affect K+ channels?

A

Increase opening for leak channels

As an EPSP comes along, driving force for K+ gets changed

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23
Q

What happens with opiates and postsynaptic inhibition?

A

Open K+ channels

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24
Q

What happens with opiates and axoaxonic inhibition?

A

Close Ca2+ channels

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25
What happens with opiates and presynaptic autoreceptors?
Reduce neutrotransmitter release Colocalization with neurotransmitter / opioid
26
Who first discovered opiate receptors?
Snyder and Pert, 1972
27
What is the Mu receptor?
Opiate receptor Most sensitive to morphine / heroin / codeine. It's the one that binds these.
28
How / where do opiates alter pain sensitivity? What is the first place possible?
Dorsal horns are the first place, chock full of opiate receptors
29
(And where is the first place touch can get modulated?)
Medulla, somatosensory axons just project directly there (pain axons stop at dorsal horns)
30
Why does rubbing help with pain?
Somatosensory neurons have inputs to pain-modulating inhibitory interneurons These interneurons get excited by the somatosensory neurons Interneurons project to pain neurons, inhibiting them
31
What physiological responses to Mu receptors modulate?
Euphoric, brain and spinal analgesic, sedative, GI motility effects
32
What do opiates do to peristaltic contraction in the GI tract?
Inhibit it (lots of opiate receptors in GI tract!)
33
What are Delta opiate receptors? What is the difference between them and Mu?
More sensitive to endogenous opiates (e..g enkephalins) Involved in spinal mechanisms of analgesia
34
What are Kappa opiate receptors?
Most sensitive to dynorphin Not involved in rewarding properties of opiates Mostly in spinal cord, brainstem
35
What is nociceptin/orphanin (NOP-R)?
No clue, but it's new learning, motor function, neuroendocrine? regulates hormonal pathways / stress response...
36
Who discovered the endogenous opiates?
Both Kosterlitz and Hughes, 1975. Discovered them independently
37
What did both kosterlitz and Hughes isolate?
Enkephalins - changes to endorphins ('naturally occurring substance that acts like DA')
38
How do the endogenous opiates begin prior to synthesis?
Begin as large molecules made by neurons | proopiomelanocortin, etc
39
How are the endogenous opiates synthesized?
Large molecules cleaved into different types of chemical messengers
40
What is the potency of large molecule opiate precursors?
Much more potent than most endogenous opiates
41
When are endogenous opiates released?
Stress response, times of pain, strenuous exercise (childbirth, fight, long-distance running)
42
What (generally) are the behavioral effects of the opiates?
Sedative-hypnotic like | But not considered sedative hypnotics b/c they have other effects
43
What opiate receptor subtype is most involved in analgesic effects?
Mu
44
What opiate receptor subtype is most involved in euphoric effects?
Mu
45
Which opiate receptor subtype is most involved generally?
'Mu leads the way'
46
What brain areas are involved in pain sensation?
NAcc Amygdala Thalamus
47
What brain areas are affective during pain?
NAcc ACC Thal
48
What is the first place pain is modulated at?
Dorsal horn, right when it enters spinal cord
49
Where does pain sensation go after?
Medulla > through pons > reticular formation/periaquaductal grey in midbrain > up to somatosensory cortex
50
Where does supraspinal control of pain begin?
Frontal lobes / hypothalamus
51
Where is the periaquaductal grey?
Encircles cerebral aquaduct FULL of receptors involved in control of pain Activates during anxiety / stress, mutes perception of pain
52
What is the locus coereleus and when does it activate?
It's the brain's equivalent of adrenal gland - release EP, NE (adrenaline) when you're stressed
53
Where is the LC?
Junction of mesencephalon and pons
54
How do opiates reduce pain in the spinal cord?
A) Inhibit projection neurons B) Inhibit interneurons that activate projection neurons C) Exciting interneurons that inhibit projection neurons
55
How quickly does opiate tolerance develop?
Incredibly fast, and LOTS of tolerance - way more than anything else
56
What protein kinase do opiate second messengers modulate? Why is this important?
PKC Modulates NMDA receptors; opiate tolerance can be reduced by concurrent administration of NDMA antagonists
57
What is the difference between conditioned and contingent tolerance?
Conditioned = pavlovian - environmental. Environment becomes stimulus for the response. "Where am I taking drug" Contingent = tolerance dependent on the activity of a specific neural circuit when an analgesic is present. "What am I doing while taking drug"
58
How do you reduce opiate tolerance with a drug?
Apply an NMDA antagonist | Because opiate receptors activate PKC, which agonizes NMDA receptors
59
How bad is opiate withdrawal?
Real bad, but not as bad as the press makes out Bad case of the flu in worst case scenario
60
What are the physical effects of opiate withdrawal?
Anxiety, runny nose, nausea, fever, etc
61
What are the psychological effects of opiate withdrawal?
Fueled by negative reinforcement (avoidance of withdrawal) and positive (seeking rewarding effects)

Psychopharmacology (12 decks)

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