Opiates Flashcards

1
Q

what are the 2 elements that comprise pain??

A

1- LOCAL IRRITATION- stimulation of peripheral nerves

2- RECOGNITION- of the pain within the CNS

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

what are the 4 stages of nociception pathways??

A

1- transduction/nociception

2- transmission

3- perception

4- modulation

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

what are peripheral nerve endings called?

A

nociceptors

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

where are nociceptors found?

A

within the skin, muscle, joints, bones and viscera

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

what do nociceptors respond to?

A

tissue injury

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

injury leads to?

A

localized biochemical change

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

describe the transmission stage:

A

signals are relayed to a second set of neurons in the dorsal horn of the spinal cord

neurotransmitters are used to relay the signal

they are excitatory because they activate or “excite” new signals in the second set of relay neurons

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

what neurotransmitters are used to relay the transmission signal?

A

glutamate and substance P

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

what are some excitatory transmitters?

A

substance P
calcitonin gene related peptide
aspartate, glutamate

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

what are some inhibitory transmitters?

A

GABA
glycine
somatostatin
A2 agonists

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

what are primary nociceptor fibers?

A

alpha delta fibers

C fibers

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

what is the brain responsible for?

A

perception of pain

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

describe the perception stage:

A

pain is perceived by an individual once all the incoming nervous messages are interpreted by the brain

this involves the integration of all the nociceptive impulses and the interpretation of what these mean

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

describe the modulation stage:

A

DESCENDING INHIBITION

areas in the midbrain can be stimulated to trigger nervous impulses that travel down the SC and release neurotransmitters (serotonin & NE) and the endogenous opioids

clamps down on pain response when appropriate

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

what do endogenous opioids do?

A

reduce the nociceptive transmissions and thus pain

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

what are descending connections that modulate incoming pain impulses?

A

fibers that descend from the BS to SC modulating incoming signals

neurotransmitters
opioid receptors

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
17
Q

what neurotransmitters are responsible for mediating anti-nociceptive effects?

A

norepinephrine and serotonin

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
18
Q

how is pain modulation achieved?

A

through dynorphins and change in opioid receptor number/activity

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
19
Q

nociceptive pain can either be:

A

acute or chronic

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
20
Q

nociceptive pain can only occur when:

A

all neural equipment is working properly

is the patient experiencing nociceptive pain?

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
21
Q

how is nociceptive pain managed?

A

analgesic selection and overall treatment approach will depend on the type, duration and intensity of the pain

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
22
Q

what is neuropathic pain?

A

pain that is the result of injury to the NS (CNS and/or PNS)

may occur after trauma as well as acute and chronic

while it may be intermittent, it is chronic

affects more than 2 million people in the US alone

notoriously difficult to treat!

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
23
Q

what is allodynia?

A

the interpretation of non-painful stimuli as painful

24
Q

what is hyperpathia?

A

an exaggerated and prolonged response to painful stimuli

25
what is the first choice for treating pain related to post-surgical, dental, trauma, visceral pain and cancer?
opioids all opioids relieve, to some degree, moderate to severe acute and chronic pain
26
what are the 3 opioid receptors that are clinically important??
opioids act by stimulating _____ receptors mu, delta and/or kappa receptors
27
stimulation of the opiate receptors inhibits...
the transmission of pain signals and the stimulation of pain control circuits in the SC
28
what is released when an opioid receptor is stimulated?
endorphins (peptides)
29
how are endorphins produced?
produced by the pituitary and hypothalamus selective for mu receptors
30
what are enkephalins?
produced throughout the CNS and peripheral nerve endings; selective for delta
31
what are dynorphins?
found in some nerve endings; selective for kappa
32
how do opioids "block" pain?
naturally derived or synthetic molecules that mimic the actions of the body's endogenous opioid peptides these substances bind to OPIOID RECEPTORS in the pain transmission and perception circuits to block both pain transmission and pain perception
33
what is the order of greatest to least analgesia produced by receptor activation?
mu>delta>kappa
34
what is the MOA of opioid agonists in the SC and the brain??
decreases Ca2+ influx in response to incoming AP. This decreases release of excitatory neurotransmitters such as glutamate activation of the opioid receptor increases K+ efflux and decreases the response of the post-synatpic neuron to excitatory neurotransmitters
35
what are the clinical effects of mu opiate receptors?
euphoria physical dependence respiratory depression supraspinal analgesia
36
what are the clinical effects of kappa opiate receptors?
miosis (close eyes, constrict pupil) sedation spinal analgesia respiratory depression
37
what are the clinical effects of sigma opiate receptors?
dysphoria- unhappy, emotional state hallucinations respiratory stimulation vasomotor stimulation
38
what are additional (9) pharmacologic effects of opiates?
anti-tussive (exception= meperidine)- used to prevent/relieve cough alterations in smooth muscle tone: increase smooth muscle tone while inhibiting peristalsis in the gut inhibit parasympathetic stimulation: affects the intestines (mechanism: blocks ACh release) decrease urine formation: opiates stimulate the secretion of anti-diuretic hormone (ADH) miosis: pinpoint pupil mood alteration: euphoria/dysphoria respiratory depression: via direct effect on respiratory centers (primarily associated with mu receptors) nausea/emetic effect: via direct stimulation of chemoreceptor trigger zone (CTZ) direct release of histamine: hives, itching, flushing
39
how are opioids classified?
1- SOURCE: natural, semisynthetic, synthetic 2- POTENCY: strong, intermediate, weak 3- SPECIAL FEATURES
40
what is the potency and effectiveness of morphine?
strong potency poor oral effectiveness releases histamine (bc it's a base
41
what is the potency and effectiveness of codeine?
intermediate potency as an analgesic high potency as antitussive good oral effectiveness often combined with non-narcotics excellent variety of dosage forms
42
what are 3 semisynthetic narcotics?
heroine dihydromorphine (Dilaudid) oxycodone (OxyCotin, Percocet)
43
what is the potency and effectiveness of heroin?
high potency acetyl groups facilitate passage across BBB better C/P ratio more prevalent street narcotic heroin= diacetyl morphine
44
what is the potency and effectiveness of dihydromorphone?
high potency excellent C/P ratio
45
what is the potency and effectiveness of oxycodine?
used in well over 40 products can be combined with non-narcotics short-acting widely abused
46
what is a synthetic narcotic?
methadone (Dolophine)
47
what is the potency and effectiveness of methadone?
potency equal to morphine (strong) very long half life accumulates if taken once daily can produce steady-state plasma concentration that is both analgesic and will prevent withdrawal used for both chronic pain management & maintenance programs/weaning
48
what opiate has the highest potency? codeine morphine fentanyl methadone
FENTANYL
49
what is tolerance?
a given drug loses its effectiveness over time and an increase dose is required to produce desired therapeutic effect
50
what is physical dependence?
dependence on a given drug to maintain normal homeostasis of the body example: chronic opioid use/administration
51
what is drug withdrawal?
a set of symptoms that are consistent with the stoppage of a drug which produces physical dependence ``` physical symptoms of opiate withdrawal include: excessive yawning lacrimation rhinorrhea restlessness increased pain sensitivity nausea vomiting diarrhea cramps muscle aches sweating dysphoric mood ```
52
how do opioid antagonists work?
antagonists attach to the opioid receptor and displace the agonist
53
what are examples of opioid antagonists?
naloxone (Narcan) naltrexone (Trexan, Vivitrol) or nalmefene
54
what is the MOA of naloxone?
competitive blocking of mu and kappa receptors parenteral use only; very quick action
55
when and how is naltrexone used?
orally effective; long acting used in treatment programs to prevent addicts from getting high on street narcotics can be used to reduce craving, relapse and drinking in alcohol-troubles persons
56
what are questions on a standard questionnaire: pain assessment?
onset when and how did the pain start? location/site where is pain located? what has happened since onset? characteristics/quality of pain: describe the pain severity? unpleasantness/distress: how unpleasant is the pain? are there any other symptoms? (numbness, weakness, bowel/bladder dysfunction, insomnia, etc? does the pt suffer from depression? anxiety? what makes the pain worse? better? impact of function and activities. how are work and ADLs affected? response to past treatments? does the pt smoke? drink? drugs? how much/often? how is the pt coping with the pain?
57
what are 2 natural opiates?
morphine and codeine