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Spring '20/ L. PHARM TEST 2 - opioids, anticholinergics, cholinesterase > Opoids > Flashcards

Opoids Flashcards

1
Q

nociception define

A

the detection of painful stimuli

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2
Q

where are pain receptors found?

A

The receptor for pain are free (naked) nerve endings in the skin, muscle and viscera

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3
Q

substance P

A

Neurotransmitters for nociceptors include substance P. Inhibition of the release of substance P is the basis of pain relief by opioids

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4
Q

A-delta fibers

A

Fast sharp pain is carried by A-delta fibers. It has a rapid onset and offset and is well localized
A-delta fibers are thicker and myelinated
Myelinated
Transmit fast/sharp pain
Well localize , can point to pain

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5
Q

C fibers

A

Slow chronic pain is carried by C fibers. It is characterized as aching, burning or throbbing that is poorly localized.
C fibers are thinner and unmyelinated
Unmyelinated
Transmit slow/chronic pain
Diffuse , burning ,aching , throbbing sensation

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6
Q

Lamina II (and III)?

A

Lamina II (and III) is Substantia Gelatinosa

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7
Q

Entry of A- delta and C fibers into the posterior horn. where do the cell bodies lie? where do the fibers ascend or descend?

A

Cell bodies lies in dorsal root ganglia (DRG)

Fibers ascend or descend in track of Lissauer

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8
Q

Pathway for slow chronic pain

A

C fibers terminates in Lamina II and Lamina III (Substantia Gelatinosa ).
Interneuron transmit C fibers impulses to Lamina V from Lamina II and III.
Neurons leaving Lamina V cross immediately to the contralateral, lateral spinothalamic tract and ascend to brain

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9
Q

name the A- delta fiber neurotransmitter

A

A-  fiber; the neurotransmitter is glutamate

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10
Q

name the C fiber neurotransmitter.

what does it bind to?

A

C fibers; the neurotransmitter is substance P which binds to NK-1(neurokinin-1) receptor on the postsynaptic membrane

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11
Q

Pathway for fast sharp pain:

A

A-delta fibers terminates in Lamina I , cross to the contralateral, lateral spinothalamic tract and ascend to the brain

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12
Q

Neuraxial (intrathecal or Epidural ) placement of Hydrophilic Opioids: what drug is this?

A

Morphine, a hydorphilic opioid, crosses lipid membrane slowly

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13
Q

tell me about intrathecal (spinal) placement.morphine

onset?
ventilation?

A

Slow onset and long duration of analgesia
No early depression of ventilation
Late depression of ventilation occur due to rostral (towards head) spread of CSF

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14
Q

Epidural Placement: morphine

tell me about onset
ventilation

A

Slow onset and long duration of analgesia
Early depression of ventilation (within 2 hrs) due to increase systemic uptake
Late depression of ventilation occur due to rostral spread

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15
Q

Neuraxial (intrathecal or Epidural ) placement of Lipophilic Opioids : what drug is this?

A

fentanyl, alfentanil, sufentanil –rapidly diffuse through lipid membrane

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16
Q

Intrathecal (Spinal) Placement of fentanyl..

A

Rapid onset and short duration of analgesia
Early depression of ventilation due to systemic uptake
Late depression of ventilation does not occur

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17
Q

Epidural Placement of fentanyl…

A

Similar as intrathecal (spinal) placement

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18
Q

if you add one of the fentanyl to a spinal- what will the patient experience as a side effect

A

they will get an itchy nose

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19
Q

3mg epidural=?spinal

A

0.3 spinal

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20
Q

Spinal Analgesia

which receptor??

A

Occurs when transmission of pain through substantia gelatinosa (L II) is suppressed
mu-2 is the dominant receptor
After IV administration, opioid acts on periventricular and periaquaductal gray — spinal analgesia

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21
Q

Supraspinal Analgesia

which receptor??

A

Opioids act on limbic system, hypothalamus and thalamus.
mu-1 is the dominant receptor
After IV administration of opioids
“ I feel pain but I don’t care”

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22
Q

Acupuncture releases what?

A

endorphins

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23
Q

descending neurons form?

The interneuron release

enkephalin inhibit release of what??

Dorsolateral tract modulates pain by??

A

periventricular and periaqueductal gray terminates on interneuron in substantia geletinosa (Enkephalin neurons)

enkephalin

Enkephalin inhibit release of substance P-spinal analgesia

by hyperpolarizing second order neurons

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24
Q

Three types of opioids receptors, located in CNS, nerve terminals, GIT and ANS

A

mu
kappa
delta

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25
Opioids interact with opioid receptors and mimic the action of endogenous opioids which are?
(enkephalins, endorphins and dynorphins) and activate brain analgesia system
26
mu 2 responsible for?
mu-2 are responsible for respiratory depression and addiction
27
Supraspinal and spinal analgesia is primarily by
mu-receptors
28
k (Kappa) all of it
Analgesia (Spinal & Supraspinal) Dysphoria Low abuse Potential Miosis Diuresis
29
delta all of it
Analgesia (Spinal & Supraspinal) Respiratory depression Physical dependence Constipation (mild)
30
mu 2 all of it
Analgesia (Spinal) Respiratory depression(decrease sensitivity of resp. center to CO2) Addiction Constipation (marked) decrease motility and tone of GI muscles increase CSF pressure (cerebral edema) C/I in head injury
31
mu 1
Analgesia (Supraspinal and spinal) Euphoria Low abuse potential Miosis (PPP) Bradycardia Hypothermia Urinary retention-C/I in BPH
32
Opioid Agonist
``` Morphine, fentanyl (sublimaze), codeine, heroin, methadone, meperidine (demerol), dextromehtophan, hydormorphone (Dilaudid) Sufentanil (sufenta), Remifnetanil ( Ultiva) ```
33
clinical use: cough suppression
(dexomethorphan),
34
diarrhea
loperamide, diphenoxylate
35
acute pulmonary edema | maintenance program for addicts
methadone
36
toxicity of opioid agonist
addition respiratory depression constipation pinpoint pupil
37
if they have pinpoint pupils??
they need to be reversed
38
opioid mechanism of action
Modulate (decrease intensity) synaptic transmission by opening K+ channels and closing Ca++ channels lead to decrease synaptic transmission and decrease release of neurotransmitters (Ach, NE, glutamate, substance P)
39
Opioid Antagonist
Naloxone (Narcan), Naltrexone ( Trexate), Nalmefene | They are competitive antagonist of opioid receptor
40
opioid antagonist | side effects
``` increase sympathetic activity Reversal of Analgesia Excitement / Dysphoria Tachycardia Hypertension Dysrhythmias – V fib Pulmonary edema ```
41
Mixed Agonist/Antagonist will they experience respiratory depression
Nalorphine (Nalline) ,Dezocine(Dalgan), Buprenorphine ( Buprenex), Nulbuphine (nubain) , Butorphanol (Stadol), Pentazocine (Talwin) They have mixed agonist and antagonist activity – stimulate one receptor but block another Sever respiratory depression is unlikely
42
if you meant to give a epidural but gave a spinal where do you stick now?
stick above the spot
43
When do we give stadol
give it in OB
44
Side Effects of opioids | 9
``` Pruritus Due to histamine release Urinary retention Inhibit sacral (parasympathetic) nerve Bladder relaxation leads to retention Respiratory depression Monitor pulse ox Give Supplemental O2 Prophylactic naloxone Sedation CNS excitation Viral reactivation herpes- fentanyl- shows back up on their lips a few days lateral ``` Sustained erection Constipation Addiction
45
Kids and versed, grandma and Ativan
– cns excitation
46
If someon has treatment for addiction
- possibly no nartocs- will come with a letter from their treatment center
47
Morphine: moa
Derived from poppy Acts on opioid receptors Hyperpolarizes the nerve cells Inhibition of nerve firing Inhibits release of NT that carry pain sensation Acts on k receptors in Lamina I and II (spinal analgesia) Acts on mu-1 receptors (supraspinal analgesia) Decreases release of substance P
48
Morphine: actions
Analgesia – pain relief without loss of consciousness increase pain threshold Alters brain’s pain perception “ I feel the pain but I don’t care”
49
morphine actions to respirations?
Causes respiratory depression by decreasing sensitivity to CO2 MCC of death due to opioid overdose Euphoria
50
morphine cough action
Depression of cough reflex
51
morphine action of pupils
Pin point pupil (PPP) increase parasympathetic stimulation by III nerve Show no tolerance to the effect
52
morphine action gut
``` Emesis Stimulating CTZ GIT decrease motility , relieves diarrhea Constipation ```
53
morphine Actions | CVS
No major effect except for large doses | increase CO2 retention; increase CSF pressure ,therefore C/I in head injury
54
morphine action with histamine
Histamine release Itching and vasodilatation Bronchoconstriction, therefore C/I in asthma
55
morphine and hormones
Hormonal actions
56
morphine and labor
Labor: increase 2nd stage | Cross placenta increase resp depression and physical dependence in neonates
57
morphine uses?
Analgesia Diarrhea Cough relief Acute pulmonary edema associated with LVH
58
morpine Pharmacokinetics
Significant first-pass metabolism, therefore use parenterally Rapid distribution , cross placental barrier Conjugated in liver to active metabolite Excreted in urine Prolong duration when given in epidural space (less lipid soluble)
59
morphine Adverse effects
``` Severe respiratory depression Vomiting Dysphoria Hypotension increase ICP Urinary retention ```
60
morphine Tolerance and physical dependence
Tolerance to analgesic, euphoric and sedative effect
61
metabolite of morphine
Morphine-6-Glucuronide Greater duration of action 650 x analgesia then morphine Low permeability to BBB
62
Meperidine MOA
Through mu and kappa receptor
63
meperidine side effects
Respiratory depression decrease total peripheral resistance increase CO increase CSF pressure
64
meperidine uses
post op shivering | employed in obstetrics
65
meperidine what id the duration? is it well absorbed?
Well absorbed orally | Shorter duration of action
66
meperidine Adverse effect
Tremors, twitching or convulsion with large dose Hyperactive reflexes Hypotension with large dose Dry mouth and blur vision
67
Methadone receptor
Through mu receptor
68
methadone actions
respiratory depression< morphine
69
methadone Uses
Control heroin withdrawal symptoms
70
methadone Pharmacokinetics
Well absorbed orally | Shorter duration of action
71
methadone Adverse effect
Physical dependence like morphine
72
Cabg drug of choice?
sufentanil
73
Fentanyl
``` 100 x analgesic potency than morphine Highly lipophilic Rapid onset and short duration of action I/V , epidural , spinal Epidural in post operative analgesia and during labor Transdermal patch for cancer pain A/E: hypotension Use during cardiac surgery Metabolized by P450 Urinary excretion Adverse effect Hypotension ```
74
sufentanil is more potent than
fentanyl
75
Codeine (Moderate Agonist)
``` Converts to morphine leads to analgesia Much less analgesia than morphine Cough suppression Less euphoria Low potential of abuse Rarely produce dependence ```
76
Drugs that stimulate one receptor but block another are termed
agonist-antagonists
77
Pentazocine
``` Agonist on k receptor and weak antagonist on mu and delta receptors Moderate analgesia Less euphoria Respiratory depression in high doses decrease GIT activity High dose causes Hypertension increase work of heart Tolerance and dependence ```
78
Buprenorphine
Used in opioid detoxification Act on mu receptor Less severe side effects in high dose
79
Nalbuphine and butorphanol
Limited role as analgesic | Causes psychotic symptoms
80
Tramadol
Act on mu receptor Moderate to severe pain relief Less respiratory depression
81
Naloxone
Use to reverse respiratory depression of opioid over dose Competitive antagonist of mu, delta, kappa receptors Produces opioid withdrawal syndrome in abusers
82
mixed agonist/antagonist which receptors do they work on?
Mediate their effect by kappa and delta receptors
83
spinal analgesia act where?
After IV administration, opioid acts on periventricular and periaquaductal gray --- spinal analgesia
84
what is suppressed in spinal analgesia?
Occurs when transmission of pain through substantia gelatinosa (L II) is suppressed
85
supra spinal acts where?
Opioids act on limbic system, hypothalamus and thalamus.

Spring '20/ L. PHARM TEST 2 - opioids, anticholinergics, cholinesterase (8 decks)

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