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BCN EXAM 4 > Intro to Narcotics > Flashcards

Intro to Narcotics Flashcards

1
Q

Non opiate drug examples

A 
local anesthetics, 
GABA agonists 
non N-methylD asparate (NMDA) antagnists, 
COX inhibitors 
corticosteroids
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2
Q

Antidepressants are useful in treating chronic pain because

A

they increase the availability of serotonin or norepi in pain modulating descending pathways

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3
Q

NSAIDs

A

ibuprofen
aspirin
acetominophen

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4
Q

NSAID action

A

non specific COX inhibitors, peripheral and spinal

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5
Q

COX 2 inhibitor example and action

A

celecoxib
COX 2 selective inhibitor
Peripheral and spinal

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6
Q

Opioids example and action

A

morphine
mu receptor agonist
supraspinal and spinal

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7
Q

Anticonvulsants example and action

A

Gabapentin
Na+ channel block
alpha2delta subunit of Ca+ channel
supraspinal and spinal

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8
Q

Tricyclic antidepressants example and action

A

amitryptiline

inhibits uptake of serotonin and Norepi (therefor prolongs the effect of these)

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9
Q

Opium contains

A

Morphine (10-15%)
Codeine (1-3%)
Thebaine (1-2%)

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10
Q

Opioid receptors in the brain

A

expressed in many parts of the brain, cerebellum, nucleus accumbens and hypothalamus
many of the regions are involved in pain perception, emotion, reward and addiction

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11
Q

Opioid activity in the brainstem

A

can affect breathing by quieting neurons that control respiration
respiratory depression is serious side fx and commonly sited in case of opioid overdose

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12
Q

opioid receptors in the spinal cord

A

Pain transmission in the dorsal horn is dampened by opioids.
This a useful and intended target for pain treatment

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13
Q

Opioid receptors in the periphery neurons

A

opioid drugs can bind pain sensing neurons and curb nociceptive messages

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14
Q

Opioid receptors in the intestines

A

expressed in neurons regulating peristalsis

inhibition of these cells can lead to constipation

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15
Q

Examples of pain pathways

A

afferent neuron - AS (alpha delta neurons) (fast and myelinated) and C fiber (slow, visceral, unmyelinated)
Dorsal root & ganglia
Substantia gelatinosa
Contralateral Spinothalamic tract - Neospinal (sharp) and Paleospinal (dull)
Supraspinal thalamic nuclei that project to the cortex

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16
Q

Gate theory

A

cutaneous sensory input activate inhibitory interneurons or descending projections release various NTs: GABA, NE or endogenous opioids
These NTs bind to presynapse of afferent pain fibers and inhibit Ca+ channels leading to reduced vesicle release
They bind post synaptically and signal via G proteins to cause K+ efflux or Cl- influx (both of which hyperpolarize)

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17
Q

Descending control of pain

A

PAG –> Nucleus Raphe Magnus and Lateral tegmental nucleus —> excitatory to Enkephalin neurons in Lamina 2 (sub gelatinosa) —> inhibit Spinothalamic tract

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18
Q

4 step model of Pain

A

Transduction, transmission, perception, modulation
acute stimulation in form of noxious input, impulses to thalamus and cortex. Cortical and limbic structures in brain are involved in awareness and interpretation of pain. Pain is inhibited or facilitated by mechanisms in the ascending and descending pathways

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19
Q

Physiology of Endogenous Opioids

A

released by pituitary gland and hypothalamic neurons in response to pain, stress, exercise and labour

  • act to relieve pain and anxiety
  • asso. with feelings of euphoria, increased appetite and enhancement of immune response
  • “runner’s” high = increased release during long, strenuous exercise and results in euphoria and increased pain threshold
  • play a role in social bonding
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20
Q

Examples of endogenous opioids

A

proorphanin
prodynorphin
proenkephalin
POMC - beta endorphins

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21
Q

What produces POMC? what is it a precursor for?

A

…

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22
Q

Beta endorphin

A

31 AA
tyr-gly-gly-phe-met (Met Enkephalin) , replace met with Leu for Leu enkephalin
the Leu sequence is seen in number of endogenous opioids

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23
Q

Analgesia

A

stimulation of AS (alpha delta) and C afferents can stimulate release of endogenous opioid beta endorphin from hypothalamus
Dynorphin released from PAG

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24
Q

Analgesia pathway

A

Transmission cell sends spinoreticular tract to RF which sends to hypothalamus. Hypothalamus (B endorphin) –> PAG —-> Raphe nucleus (serotonin) —-> via Dorsolateral tract acts on Enkephalin interneuron which releases enkephalin on the transmission cell
From transmission cell receives from (As and C fibers)
enkephalin interneuron from transmission cell

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25
Q

Endorphin is selective for

A

mu opioid receptors

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26
Q

How do opioid receptors work?

A

decrease synaptic transmission
binding activates G proteins that, in turn, activate potassium channels (neuronal membrane hyperpolariztion) inhibit voltage operated calcium conductance and neurotransmitter release

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27
Q

Dynorphin is co released with

A

Orexin

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28
Q

neuropeptides that modulate neurotransmitter action

A

Endorphins

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29
Q

Mechanism of Action of Endorphins

A 
directly stimulate opioid receptors on the pre and post synaptic membranes 
rapidly degraded peptidases 
each binds a different opioid receptor 
-B endorphin and endomorphin (mu) 
-enkephalin (delta) 
-dynophin (kappa)
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30
Q

Nociceptin receptor

A

ORL-1

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31
Q

synthetic agonists for mu receptors

A

Morphine
codeine
heroin

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32
Q

synthetic agonists for kappa opioid receptor

A

pentazocine

oxycodone?

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33
Q

What receptor Naloxone not an antagonist for?

A

ORL-1

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34
Q

What type of receptors are opioid receptors?

A

G protein receptors

35
Q

B-FNA is an antagonist for?

A

Mu receptor

36
Q

Natrindole is an antagonist for?

A

Delta receptor

37
Q

In general, stimulation of opioid receptors result in

A

hyperpolarization of neurons

inhibition of NT release

38
Q

Effects of mu receptors

A 
analgesia 
relief of anxiety 
euphoria 
nausea 
constipation 
cough suppression 
dependence
39
Q

Effects of delta receptor

A

like mu but less marked

40
Q

Effects of Kappa receptor

A

Analgesia
aversion
Diuresis

41
Q

Leu and Met enkephalin

A

short interneurons associated with pain pathways emotional behavior and motor control

42
Q

what are endorphins co released with?

A

from pituitary with ACTH (Stress hormone)

43
Q

Dynorphins are co localized with ….

A

vasopression, suggesting role in fluid homeostasis

in the spinal cord lowers pain threshold

44
Q

Name opioid therapeutic for diarrhea

A

diphenoxylate

loperamide

45
Q

Opioid for relief of cough

A

dextromethorphan

46
Q

Treatment for opioid withdrawal

A

methadone

47
Q

Treatment for opioid overdose

A

naltrexone

48
Q

Treatment for constipation

A

methylnaltrexone

49
Q

Treatment for postoperative ileus

A

alvimonpan

50
Q

Narcotic analgesics

A 
morphine 
codeine 
hydrocodiene 
oxycodone 
fentany
51
Q

Mu opioid receptor

A 
Main pharma site 
mu1 = analgesia 
mu2 = analgesia, respiratory depression 
Euphoria (m1), miosis, dependence (m2) 
sedation
52
Q

Kappa opioid receptor

A

predominantly endogenous opiates
spinal analgesia
miosis
sedation dysphoria

53
Q

Delta opioid receptor

A

analgesia

respiratory depression

54
Q

dysphoria

A

state of unease or general dissatisfaction with life

55
Q

Non opiate approaches: Transduction

A

nonsteriodal anti inflam. drug (NSAIDs) and cyclooxygenase (COX) 2 inhibitors - target the inflam. processes

56
Q

Strong opioid agonists

A 
Fentanyl 
Heroin - rapid brain entry increases abuse 
Meperidine - physician's drug of choice 
Methadone - withdrawal less severe 
Morphine - the original
57
Q

Moderate opioids agonists

A

Codeine

Propoxyphene

58
Q

Opioid antagonists

A

Naloxone-short acting must provide adequate breathing

Naltrexone

59
Q

What limits narcotic analgesic clinical use?

A

induction of tolerance and dependence

which are influenced by their efficacy

60
Q

Morphine is a _____ agonist

A

Full

  • very potent analgesic
  • High degree of dependence
61
Q

Codeine/ Dextropropoxyphene

A

milder analgesia and dependence

lower first pass metabolism

62
Q

Tramadol

A

weaker full agonist

less respiratory suppression

63
Q

Methadone

A

full agonist for treating addicts

64
Q

Mu opioid receptor (m1)

A 
central analgesia 
miosis*
bradycardia 
euphoria 
physcial dependence 
increased prolactin release 
inhibits Ach release*
65
Q

Mu opioid receptors (m2)

A 
Respiratory depression **
GI motility 
spinal analgesia 
GH release 
miosis*
bradycardia
66
Q

Kappa opioid receptor effects

A 
central analgesia with k1 
sedation ** 
disorientation, hallucinations 
depersonalization 
less miosis 
dysphoria 
ADH release - (diuresis) k1 
Central analgesia
67
Q

Delta opioid receptor

A

positive reinforcement of central analgesia
suppresses noxious thermal stimuli at spinal cord
enhances m agonists

68
Q

Pharma action of Morphine

A 
analgesia 
euphoria/sedation 
decreased respiration 
suppression of the cough reflex 
miosis
emesis 
GI effects 
cardiovascular effects 
Hormones - CRH and ACTH, Gonadotropin releasing hormone
69
Q

Tolerance develops to most of morphine’s effects, with the exception of

A

miosis
constipation
pruritis

70
Q

What is different about codeine’s structure that reduces its first pass metabolism in comparison to Morphine?

A

The H on OH in Morphine is replaced by CH3 for codeine which makes it more resistant to glucuronidation

71
Q

Morphine chemical structure

A

about four rings with O between two
Has two OH groups vulnerable to glucuronidation
N-CH3 group open to demethylation (minor)
Glucuronidation of the OH not subbed in codeine will increase potency of analgesia

72
Q

Morphine mechanism of action

A

via activation of mu receptors and to lesser extent kappa
Analgesia: inhibition of ascending nociceptive info
activate descending pain control circuits
25% effective for oral vs. parenteral admin

73
Q

Does morphine cross the BBB?

A

Yes but to a lesser extent that many opioids

74
Q

Therapeutic uses for Morphine

A 
acute pain (do NOT use in chronic malignant pain) 
dyspnea and pulmonary edema 
pre anesthetic medication 
open heart surgery 
to decrease fear in dying
75
Q

Opioid analogs are designed after

A

morphine, thebaine, codeine

  • simplification of morphine structure
  • mod by addition to thebaine
76
Q

Effects of Morphine on respiration

A

primary and continuous depression of respiration related to dose

  • decrease in rate
  • decrease volume
  • decrease tidal exchange
77
Q

Effects of morphine on N&V

A

stimulation of CTZ (?) in area postrema of medulla
sitmualtion by stretch receptors causes nausea and vomiting
has afferents from gut and ear
involved in motion sickness

78
Q

Constipation as side effect from Morphine results from

A

increase in tone in stomach, small intestine and large intestine
decrease in mobility
decrease concentration of HCl secretion
altogether delays passage of food so more reabsorption of water
Tolerance to this effect does NOT occur

79
Q

CV effects of Morphine

A

vasodilation which leads to decrease in BP
cause release of histamine
suppression of central adrenergic tone
suppression of reflex vasoconstriction

80
Q

Morphine effects on the biliary tract

A

marked increase in pressure
10 fold over normal
due to contraction of sphincter of Oddi

81
Q

Urinary bladder effects of Morphine

A

tone of detrusor muscle increased
feel urinary urgency
urinary retention due to increased muscle tone where sphincter closed off

82
Q

Bronchial muscle effects of Morphine

A

bronchoconstriction

**is contraindicated in asthmatics, particularly before surgery

83
Q

Uterine effects of Morphine

A

contraction uterus can prolong labour

84
Q

Neuroendocrine effects of opioids

A

inhibit release of GnRH and CRF thus decreasing LH, FSH, ACTH and b-endorphin
as a result, decreased concentration circulating which leads to less testosterone and cortisol in plasma
-Thyrotropin is unaffected

BCN EXAM 4 (8 decks)

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