opioids MT1

Question 1

this is an unpleasant sensory and emotional experience with actual or potential tissue damage or described in terms of such damage

Answer 1

pain

Question 2

the absence of pain

Answer 2

analgesia

Question 3

this type of pain is caused by tissue damage

Answer 3

nociceptive pain

Question 4

this type of pain is caused by nerve damage

Answer 4

neuropathic pain

Question 5

these are nerve endings that detect damaging mechanical, thermal and chemical stimuli. they are found on the skin, on internal surfaces such as the periosteum, joint surfaces and in some internal organs

Answer 5

nociceptors

Question 6

this is a physiological process by which stimuli that are associated with tissue damage activate neural pathways. the nervous systems processing information received by nociceptors

Answer 6

nociception

Question 7

what are the four stages of the nociceptive circuit

Answer 7

• transduction
• transmission
• modulation
• perception

Question 8

following an injury, a variety of chemicals are released and act on nociceptors. these chemicals include

Answer 8

• bradykinin
• serotonin
• histamine
• prostaglandins
• leukotrienes

Question 9

noxious stimuli is received via a nociceptor and transducer into electrical signals that are transmitted to the spinal cord. ____________ and _____________ are excitatory neurotransmitters found at these synapses and are released. from there the stimuli travels up the spinal cord to the thalamus and other various cortical structures (somatosensory cortex, insula, anterior cingulate cortex, or the prefrontal cortex)

Answer 9

glutamate and aspartate

Question 10

from the cortical structures, descending modulatory signals project downward and modulate the signal at the level of the dorsal root ganglion and spinal cord. _________ and _______ are key inhibitory neurotransmitters found at the supra-spinal and spinal level. the net effect of this pathway produces an individuals perception of pain and their overall pain experience

Answer 10

GABA and glycine

Question 11

this is when innocuous stimuli are detected as painful; pain due to a stimulus that does not normally provoke pain (e.g. a light feather touch causing pain)

Answer 11

allodynia

Question 12

this is an exaggerated response to noxious stimuli (e.g. feeling intense, excruciating pain when touching a recently burned area of skin or a hangnail)

Answer 12

hyperalgesia

Question 13

the site of action of these medications is (peripheral, supraspinal or spinal)
- lidocaine
-oxcarbazepine
-capsaicin
-anti-ngf
-anti-cgrp
-nsaids
-BoNT-A

Answer 13

peripheral

Question 14

the site of action of these medications is (peripheral, supraspinal or spinal)
- gabapentin/pregabalin
- opioids
- NMDA blockers
- TCAs
- SNRI
- clonidine

Answer 14

spinal

Question 15

the site of action of these medications is (peripheral, supraspinal, or spinal)
- gabapentin/pregabalin
- opioids
-TCA
-SNRI

Answer 15

supraspinal

Question 16

this is an analgesic that affects the GABA receptor

Answer 16

pregabalin/gabapentin

Question 17

what is the MOA of pregabalin/gabapentin

Answer 17

modulates hyper excited neurons
- drug binds to presynaptic neuron at the alpha2-delta subunit of the voltage gated calcium channels
- when the drug binds = reduced calcium influx
- less calcium PREVENTS DEPOLARIZATION = less release of excitatory neurotransmitters (e.g. glutamate, substance P, noradrenaline)

Question 18

What are some side effects of pregabalin/gabapentin

Answer 18

drowsiness, dizziness, dry mouth, headache, constipation, nausea, difficulty concentrating, weight gain

Question 19

what is the MOA of both TCA’s and SNRI’s

Answer 19

block the reuptake of serotonin and NE in the synaptic cleft (mechanism of pain relief is unknown)

Question 20

the brainstem centers that provide noradrenic input are thought to be pain inhibitory. the ____________ contains the greatest amount of noradrenergic neurons in the brain and is described as a pain suppressor. the noradrenic neurons of this project to the spinal dorsal horn, release NE to inhibit pain transmission

Answer 20

locus ceoruleus (LC)

Question 21

the two functions of increasing levels of this neurotransmitter are
- inhibits neuropathic pain through the alpha-adrenergic receptors
- acts on the LC and improves the function of an impaired descending noradrenergic inhibitory system

Answer 21

norepinephrine

Question 22

what are some adverse effects of TCAs

Answer 22

blurred vision, drowsiness, dry mouth, nausea, orthostatic hypotension, weight gain, cognitive impairment, constipation, urinary retention, arrythmias (antihsitamine and anticholinergic effects)

Question 23

what are some adverse effects of SNRI

Answer 23

drowsiness, insomnia, nausea, dry mouth, dizziness, constipation, excessive sweating

Question 24

this is a hormone like chemical in the body that contributes to inflammation, pain and fever by raising temperature and dilating blood vessels, which causes redness, swelling in the place where they are released

Answer 24

prostaglandins

Question 25

NSAIDs block _______ which plays a key role in makings prostaglandins thus NSAIDs help relieve pain

Answer 25

COX-1 and/or 2

Question 26

what are some adverse effects of NSAIDs

Answer 26

GI (ulceration, bleeding, dyspepsia) - more common in nonselective NSAIDs hypertension kidney damage increased risk of MI/stroke (celecoxib)

Question 27

when NSAIDs inhibit _____, platelet aggregation is decreases and increases risk of bleeding

Answer 27

COX 1

Question 28

this NSAID has less GI bleeding risk than non selective NSAIDs

Answer 28

celecoxib (COX2 selective)

Question 29

this is any compound that binds to opiate receptors

Answer 29

opioid

Question 30

opioids attach to ________ on nerve cells in the brain, spinal cord, gut and other parts of the body: this blocks pain messages sent from the body through the spinal cord to the brain

Answer 30

G-protein coupled opioid receptor

Question 31

G-protein-coupled opioid receptors also bind endogenous opioid peptides known as ________ which ar einvolved in pain modulation

Answer 31

endorphines

Question 32

this type of opioid receptor is responsible for analgesia

Answer 32

mu receptor

Question 33

what is the MOA for analgesia for opioids

Answer 33

- opioids inhibit adenylyl cyclase (decreases cAMP) - activate potassium efflux (increased post synaptic potassium) - suppresses calcium conductance (decreased presynaptic calcium) - inhibits neurotransmitter release (substance P0 overall it causes hyper polarization of the neuron making it LESS sensitive to excitatory neurons

Question 34

this class of opioid fully activates the opioid receptor, higher doses produce greater activation in a dose-dependant matter (e.g. morphine, oxycodone, methadone)

Answer 34

full agonist

Question 35

this class of opioid has low intrinsic activity with a ceiling on agonist activity. increasing the dose will only increase the effects to a certain level and further doses do not increase the effect (e.g. buprenorphine)

Answer 35

partial agonist

Question 36

this class of opioid occupies the receptor but does not activate, can reverse the effect of mu opioid agonists (naloxone, naltrexone)

Answer 36

antagonist

Question 37

what opioids have relatively long half lives

Answer 37

methadone and buprenorphine

Question 38

true or false: opioid receptors are widely distributed in both CNS and PNS

Answer 38

true

Question 39

what are some side effects of opioids

Answer 39

- constipation - drowsiness/dizziness - headache - N/V - flushing/sweating

Question 40

this occurs when an opioid is used on a regular basis, and the brain adjusts so the effects of the same amount of drug become less over time

Answer 40

tolerance

Question 41

what are the two theories that explain tolerance

Answer 41

1. opioid receptors may become less sensitive to the drug 2. neurons may remove opioid receptors from the cell wall thus less receptors available for binding

Question 42

this is a neurobehavioral disorder characterized by a repeated compulsive seeking or use of an opioid medication. it is accompanied by well-described physical dependance with a withdrawal syndrome and tolerance

Answer 42

dependance

Question 43

why does someone become dependant with opioids

Answer 43

opioids increase dopamine in the reward pathways of the brain by inhibiting the release of GABA (inhibitory neurotransmitter)

Question 44

what are some symptoms of withdrawal

Answer 44

- N/V/D - sweating - tremor - shivering - anxiety