Brainscape's Knowledge GenomeTM

Browse over 1 million classes created by top students, professors, publishers, and experts.


See full index

Block 3 Up To Quiz 1 > Analgesics and Opiods > Flashcards

Analgesics and Opiods Flashcards

1
Q

Stimulation of periaqueductal grey and nociception

A

stimulates analgesia in which animal can respond to touch, pressure, and temperature still

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

Neurons in PAG path

A
  1. Excitatory connections neurons of rostroventral medulla

2. Seratonergic neuron axons project though D region spinal cord where form inhibitory connections w/ SC neurons

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

noradernergic system originating locus coerulues and other nuclei of the medulla and pons and analgesia

A
  • this noradernergic descending system has projections that inhibit neurons in DH through direct and indirect synaptic actions -> suppression nociceptive neurons in DH
  • this endogenous pain suppression pathway triggered by emotions or expectation (brain) can override nociceptive input
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

How do drugs reduce pain

A

analgesics can inhibit nociceptive:

  • transduction
  • transmission
  • projection
  • perception
  • promote intrinsic analgesia
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

reduce pain inhibiting transduction

A
  • directly or indierectly (via GPCRs) inhibit nociceptive sensors (TRP/ P2X) diminishing generator potentials
  • promote K+ channel activity hyper polarizing nociceptor -> harder to get action potential
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

reduce pain inhibit transmission

A
  • inhibit Na+ channels b/c voltage-gated Na+ channels transmit pain
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

pain projection through CNS how

A
  • nociceptive signals propagated in CNS via glutamatergic synapses
  • voltage gated Ca2+ channels -> glutamate released
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

reduce pain projection and propigation through CNS

A
  • antagonize NMDA receptors

- promote K+ channel activity

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

reduce pain promoting intrinsic analgesic pathways

A
  • block seratonin/ noradrenerin reuptake

- these drugs affect other brain activities

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

Molecular mechanism and neural circuit opiate action

A
  1. morphine and other opiates interact w/ specific receptors on neurons in SC and brain
  2. isolation endogenous neuropeptides w/ opiate-like activities at these receptors
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

opiates

A
  • naturally occurring alkaloids found in opium poppy plant

- morphine

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

opioids

A
  • any substance that binds body’s opiod receptor sites

- natural and synthetic alkaloids and endogenous peptides

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

opioids vs opiates

A

all opiates are opioids BUT not all opioids are opiates

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

morphine opioid or opiate?

A

both

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

Opioid receptor classes and what type receptor are they

A
  • u (mu MOP)
  • s (delta: DOP)
  • k (kappa: KOP)
  • orphanin FQ (N/OFQ)
  • these are all GPCRs
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

Opioid Mechanism of action

A
  • activate opioid receptor ->
  • inhibition voltage-sensitive Ca2+ channels in presynaptic neuron -> less NT released
  • activation inwardly rectifying K+ channels (GIRKs) in post synaptic neuron -> membrane hyperpolarization
  • modulation cAMP-gated K+ channels

These activities -> attenuation neuronal excitability and reduction in neurotransmitter release

17
Q

endogenous opioid peptides

A
  • processed from large polypeptide precursors by enzymatic cleaveage
  • distributed widely in CNS; individual peptides at sites processing or modulation nociceptive information
18
Q

side effects opiods

A
  • constipation
  • sedation
  • dizziness
  • nausea
  • V+
  • physical dependence
  • tolerance
  • respiratory depression
  • confine administration to SC or periphery to minimize side effects
19
Q

capsaicin

A
  • approved for topical treatment neuropathic pain

Additional info learn if time
- selectively activates TRPV1 channel -> indirect inhibition mechxnosensitive Piezo channel -> analgesia

20
Q

NMDA receptor antagonist

A
  • inhibits post-synaptically localized NDMA receptors which play central role in pain sensitization -> analgesia
  • some of these drugs enhance effects NDAIDs, Gabapentin, and opiods
21
Q

Cannabinoids

A
  • endogenous analgesics
  • activate CB1 GPCRs (couple with Gi) -> suppress voltage-gated Ca2+ channels and promote K+ channels (making membrane harder to depolarize)
22
Q
  • opioid overdose can ->
A

respiratory depression, V+ constipation

23
Q

reversal agents opiods

A
  • naloxone antagonizes u opioid receptors
  • altipamezole reversal agent demedetomidine (kicks off agonists from alpha-2 adrenergic receptor)
  • flumazenil reverses benzodiazepines (kicks off agonists from GABAA receptor)
24
Q

reasons for failures of targeted analgesic research

A
  • complex neurobio
  • inadequate animal models
  • difficulty reaching optimal therapeutic dose
  • inability cross blood brain barrier
  • lack specificity and off target effects
  • high placebo response rate
  • lack of reliable biomarker
25
Q

progress in new generation of analgesics

A
  • developing novel small molecules to target important plays in pain pathway
  • developing structure-based drug designs with hopes biased opiods that inhibit G-protein pathways (pain) but not B-arrestin cascade (respiratory depression and addiction)
26
Q

G-Protein Coupled receptor summary

A
  • 7 transmembrane helical proteins
  • alphasubunit is GDP bound in resting state when activated by ligand binding to receptor -> conformational change or alpha subunit-> alpha subunit release GDP-> GTP binds alpha subunit -> conformation change -> alpha subunit dissociates from receptor and beta and gamma subunits -> free GTP bound alpha subunit which can effect other proteins in cell
27
Q

GAs can activate

A

-AC -> cAMP -> PKA (pathway activated) (PKA= protein kinase A)

28
Q

GAi subcalss

A
  • inhibit cAMP and in turn inhibit pKA
29
Q

Gq

A
  • PIP2-> DAG and IP3 -> PKC (protein kinase C)

Block 3 Up To Quiz 1 (24 decks)

Brainscape helps you reach your goals faster, through stronger study habits.
© 2024 Bold Learning Solutions. Terms and Conditions