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BCN EXAM 4 > Intro to Narcotics > Flashcards

Intro to Narcotics Flashcards

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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
Endorphin is selective for
mu opioid receptors
26
How do opioid receptors work?
decrease synaptic transmission binding activates G proteins that, in turn, activate potassium channels (neuronal membrane hyperpolariztion) inhibit voltage operated calcium conductance and neurotransmitter release
27
Dynorphin is co released with
Orexin
28
neuropeptides that modulate neurotransmitter action
Endorphins
29
Mechanism of Action of Endorphins
``` 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) ```
30
Nociceptin receptor
ORL-1
31
synthetic agonists for mu receptors
Morphine codeine heroin
32
synthetic agonists for kappa opioid receptor
pentazocine | oxycodone?
33
What receptor Naloxone not an antagonist for?
ORL-1
34
What type of receptors are opioid receptors?
G protein receptors
35
B-FNA is an antagonist for?
Mu receptor
36
Natrindole is an antagonist for?
Delta receptor
37
In general, stimulation of opioid receptors result in
hyperpolarization of neurons | inhibition of NT release
38
Effects of mu receptors
``` analgesia relief of anxiety euphoria nausea constipation cough suppression dependence ```
39
Effects of delta receptor
like mu but less marked
40
Effects of Kappa receptor
Analgesia aversion Diuresis
41
Leu and Met enkephalin
short interneurons associated with pain pathways emotional behavior and motor control
42
what are endorphins co released with?
from pituitary with ACTH (Stress hormone)
43
Dynorphins are co localized with ....
vasopression, suggesting role in fluid homeostasis | in the spinal cord lowers pain threshold
44
Name opioid therapeutic for diarrhea
diphenoxylate | loperamide
45
Opioid for relief of cough
dextromethorphan
46
Treatment for opioid withdrawal
methadone
47
Treatment for opioid overdose
naltrexone
48
Treatment for constipation
methylnaltrexone
49
Treatment for postoperative ileus
alvimonpan
50
Narcotic analgesics
``` morphine codeine hydrocodiene oxycodone fentany ```
51
Mu opioid receptor
``` Main pharma site mu1 = analgesia mu2 = analgesia, respiratory depression Euphoria (m1), miosis, dependence (m2) sedation ```
52
Kappa opioid receptor
predominantly endogenous opiates spinal analgesia miosis sedation dysphoria
53
Delta opioid receptor
analgesia | respiratory depression
54
dysphoria
state of unease or general dissatisfaction with life
55
Non opiate approaches: Transduction
nonsteriodal anti inflam. drug (NSAIDs) and cyclooxygenase (COX) 2 inhibitors - target the inflam. processes
56
Strong opioid agonists
``` Fentanyl Heroin - rapid brain entry increases abuse Meperidine - physician's drug of choice Methadone - withdrawal less severe Morphine - the original ```
57
Moderate opioids agonists
Codeine | Propoxyphene
58
Opioid antagonists
Naloxone-short acting must provide adequate breathing | Naltrexone
59
What limits narcotic analgesic clinical use?
induction of tolerance and dependence | which are influenced by their efficacy
60
Morphine is a _____ agonist
Full - very potent analgesic - High degree of dependence
61
Codeine/ Dextropropoxyphene
milder analgesia and dependence | lower first pass metabolism
62
Tramadol
weaker full agonist | less respiratory suppression
63
Methadone
full agonist for treating addicts
64
Mu opioid receptor (m1)
``` central analgesia miosis* bradycardia euphoria physcial dependence increased prolactin release inhibits Ach release* ```
65
Mu opioid receptors (m2)
``` Respiratory depression ** GI motility spinal analgesia GH release miosis* bradycardia ```
66
Kappa opioid receptor effects
``` central analgesia with k1 sedation ** disorientation, hallucinations depersonalization less miosis dysphoria ADH release - (diuresis) k1 Central analgesia ```
67
Delta opioid receptor
positive reinforcement of central analgesia suppresses noxious thermal stimuli at spinal cord enhances m agonists
68
Pharma action of Morphine
``` analgesia euphoria/sedation decreased respiration suppression of the cough reflex miosis emesis GI effects cardiovascular effects Hormones - CRH and ACTH, Gonadotropin releasing hormone ```
69
Tolerance develops to most of morphine's effects, with the exception of
miosis constipation pruritis
70
What is different about codeine's structure that reduces its first pass metabolism in comparison to Morphine?
The H on OH in Morphine is replaced by CH3 for codeine which makes it more resistant to glucuronidation
71
Morphine chemical structure
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
Morphine mechanism of action
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
Does morphine cross the BBB?
Yes but to a lesser extent that many opioids
74
Therapeutic uses for Morphine
``` 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
Opioid analogs are designed after
morphine, thebaine, codeine - simplification of morphine structure - mod by addition to thebaine
76
Effects of Morphine on respiration
primary and continuous depression of respiration related to dose - decrease in rate - decrease volume - decrease tidal exchange
77
Effects of morphine on N&V
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
Constipation as side effect from Morphine results from
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
CV effects of Morphine
vasodilation which leads to decrease in BP cause release of histamine suppression of central adrenergic tone suppression of reflex vasoconstriction
80
Morphine effects on the biliary tract
marked increase in pressure 10 fold over normal due to contraction of sphincter of Oddi
81
Urinary bladder effects of Morphine
tone of detrusor muscle increased feel urinary urgency urinary retention due to increased muscle tone where sphincter closed off
82
Bronchial muscle effects of Morphine
bronchoconstriction | **is contraindicated in asthmatics, particularly before surgery
83
Uterine effects of Morphine
contraction uterus can prolong labour
84
Neuroendocrine effects of opioids
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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