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Pharmacology > Opiates > Flashcards

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

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2
Q

what are the 4 stages of nociception pathways??

A

1- transduction/nociception

2- transmission

3- perception

4- modulation

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3
Q

what are peripheral nerve endings called?

A

nociceptors

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4
Q

where are nociceptors found?

A

within the skin, muscle, joints, bones and viscera

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5
Q

what do nociceptors respond to?

A

tissue injury

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6
Q

injury leads to?

A

localized biochemical change

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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

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8
Q

what neurotransmitters are used to relay the transmission signal?

A

glutamate and substance P

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9
Q

what are some excitatory transmitters?

A

substance P
calcitonin gene related peptide
aspartate, glutamate

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10
Q

what are some inhibitory transmitters?

A

GABA
glycine
somatostatin
A2 agonists

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11
Q

what are primary nociceptor fibers?

A

alpha delta fibers

C fibers

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12
Q

what is the brain responsible for?

A

perception of pain

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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

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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

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15
Q

what do endogenous opioids do?

A

reduce the nociceptive transmissions and thus pain

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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

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17
Q

what neurotransmitters are responsible for mediating anti-nociceptive effects?

A

norepinephrine and serotonin

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18
Q

how is pain modulation achieved?

A

through dynorphins and change in opioid receptor number/activity

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19
Q

nociceptive pain can either be:

A

acute or chronic

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20
Q

nociceptive pain can only occur when:

A

all neural equipment is working properly

is the patient experiencing nociceptive pain?

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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

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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!

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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
Q

what is the first choice for treating pain related to post-surgical, dental, trauma, visceral pain and cancer?

A

opioids

all opioids relieve, to some degree, moderate to severe acute and chronic pain

26
Q

what are the 3 opioid receptors that are clinically important??

A

opioids act by stimulating _____ receptors mu, delta and/or kappa receptors

27
Q

stimulation of the opiate receptors inhibits…

A

the transmission of pain signals and the stimulation of pain control circuits in the SC

28
Q

what is released when an opioid receptor is stimulated?

A

endorphins (peptides)

29
Q

how are endorphins produced?

A

produced by the pituitary and hypothalamus

selective for mu receptors

30
Q

what are enkephalins?

A

produced throughout the CNS and peripheral nerve endings;

selective for delta

31
Q

what are dynorphins?

A

found in some nerve endings;

selective for kappa

32
Q

how do opioids “block” pain?

A

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
Q

what is the order of greatest to least analgesia produced by receptor activation?

A

mu>delta>kappa

34
Q

what is the MOA of opioid agonists in the SC and the brain??

A

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
Q

what are the clinical effects of mu opiate receptors?

A

euphoria
physical dependence
respiratory depression
supraspinal analgesia

36
Q

what are the clinical effects of kappa opiate receptors?

A

miosis (close eyes, constrict pupil)
sedation
spinal analgesia
respiratory depression

37
Q

what are the clinical effects of sigma opiate receptors?

A

dysphoria- unhappy, emotional state
hallucinations
respiratory stimulation
vasomotor stimulation

38
Q

what are additional (9) pharmacologic effects of opiates?

A

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
Q

how are opioids classified?

A

1- SOURCE: natural, semisynthetic, synthetic

2- POTENCY: strong, intermediate, weak

3- SPECIAL FEATURES

40
Q

what is the potency and effectiveness of morphine?

A

strong potency

poor oral effectiveness

releases histamine (bc it’s a base

41
Q

what is the potency and effectiveness of codeine?

A

intermediate potency as an analgesic

high potency as antitussive

good oral effectiveness

often combined with non-narcotics

excellent variety of dosage forms

42
Q

what are 3 semisynthetic narcotics?

A

heroine

dihydromorphine (Dilaudid)

oxycodone (OxyCotin, Percocet)

43
Q

what is the potency and effectiveness of heroin?

A

high potency

acetyl groups facilitate passage across BBB

better C/P ratio

more prevalent street narcotic

heroin= diacetyl morphine

44
Q

what is the potency and effectiveness of dihydromorphone?

A

high potency

excellent C/P ratio

45
Q

what is the potency and effectiveness of oxycodine?

A

used in well over 40 products

can be combined with non-narcotics

short-acting

widely abused

46
Q

what is a synthetic narcotic?

A

methadone (Dolophine)

47
Q

what is the potency and effectiveness of methadone?

A

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
Q

what opiate has the highest potency?

codeine
morphine
fentanyl
methadone

A

FENTANYL

49
Q

what is tolerance?

A

a given drug loses its effectiveness over time and an increase dose is required to produce desired therapeutic effect

50
Q

what is physical dependence?

A

dependence on a given drug to maintain normal homeostasis of the body

example: chronic opioid use/administration

51
Q

what is drug withdrawal?

A

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
Q

how do opioid antagonists work?

A

antagonists attach to the opioid receptor and displace the agonist

53
Q

what are examples of opioid antagonists?

A

naloxone (Narcan)

naltrexone (Trexan, Vivitrol) or nalmefene

54
Q

what is the MOA of naloxone?

A

competitive blocking of mu and kappa receptors

parenteral use only; very quick action

55
Q

when and how is naltrexone used?

A

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
Q

what are questions on a standard questionnaire: pain assessment?

A

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
Q

what are 2 natural opiates?

A

morphine and codeine

Pharmacology (8 decks)

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