opiates and receptors Flashcards
(132 cards)
1
Q
what do endogenous opiates have similarities in?
A
AA sequence
2
Q
(T/F) some endogenous opiates are derived from the same precursor molecule?
A
T
3
Q
what receptor does morphine act on?
A
mu
4
Q
what receptor does ketocyclazocine act on?
A
kappa
5
Q
is the sigma receptor an opioid receptor?
A
no
6
Q
which three receptors have some identical AA sequences?
A
mu, delta, kappa
7
Q
what three drugs make up the phenanthrene class?
A
codeine, morphine, dihydromorphone
8
Q
what 2 drugs make up the levorphanol class?
A
levorphanol and dextrorphan
9
Q
what 3 drugs make up the fentanyl class?
A
fentanyl, alfentanyl, sufentanyl
10
Q
what three drugs make up the methadone class?
A
methadone, LAAM, propoxyphene
11
Q
what type of opiate agonists are the agents?
A
direct acting agonists
12
Q
what drug is the gold standard opioid agonist?
A
morphine
13
Q
(T/F) opioid agonists have reuptake blockers and degredation inhibitors
A
F
14
Q
(T/F) opioid agonists have synthesis inhibitors and precursors
A
F
15
Q
(T/F) opioid agonists do not have neuron activators or releasors
A
T
16
Q
where are the main effects of mu opioid agonists?
A
CNS
17
Q
what is the main effect of opioid mu receptor agonists on the CNS?
A
analgesia without anesthesia
18
Q
(T/F) mu receptor agonists cause anethesia
A
F
19
Q
what are the 6 minor effects on the CNS by mu receptor agonists?
A
sedation, respiratory depression, nausea, anti-tussive, miosis, neuroendocrine effects
20
Q
what is the difference between NSAIDs and morphine?
A
NSAIDS relieve the pain and morphine the pain is still there but not bothersome
21
Q
what type of pain is morphine affective towards: dull/throbbing or sharp/cutaneous?
A
dull/throbbing
22
Q
do opiates work at the source of pain?
A
no
23
Q
where is the primary source of pain relief from opiates?
A
reduced appreciation of pain by CNS
24
Q
(T/F) opiates are anti-inflammatory
A
F
25
A patient with inflammation would benefit from ____
NSAIDs
26
a patient who had surgery and has bone pain would benefit from ____
opiates
27
where is supraspinal analgisa?
PAG (brain)
28
where is spinal analgisa?
spinal cord dorsal horn and spinothalamic tract
29
morphine produces CNS _____
depression
30
the most common cause of death in opioid OD is ___
respiratory depression
31
where are the mu receptors?
medulla
32
what does respiratory depression do to PCO2 levels?
inc
33
what does respiratory depression do to RR, minute volume, and tidal exchange?
dec
34
what is a consequence with nausea side effect from opioids?
choking on the nausea
35
what is miosis?
constricted pupil
36
is miosis from excitation on the parasympthetic or sympathetic nervous system?
miosis is excitation on the parasympathetic nervous system innervating pupil
37
what happens upon anoxia?
mydriasis
38
what two hormones are inc with morpine?
GH and PRL
39
other than the CNS, where at the 3 places morphine can act?
cardiovascular, GI, smooth muscle
40
what happens to SNS tone and reflexes from morphine?
dec
41
what happens to vascular resistance from morphine?
dec, vasodilation
42
what happens to baroreceptor reflex from morphine?
blunted
43
what happens to gastric emptying and motility of the GI with morphine?
dec
44
what impact does morphine have on the bowel movement?
constipation
45
do nonpropulsive contractions increase or decrease with morphine?
inc, lead to spasms
46
do propulsive contractions increase or decrease with morphine?
dec, lead to stasis
47
what happens to anal sphincter tone with morphine?
inc
48
what happens to bladder external sphincter tone with morphine?
inc
49
what happens to bladder volume and voiding with morphine?
bladder volume inc
voiding dec
50
what happens to biliary pressure with morphine?
10x fold increase in pressure
51
there is _____ worsening of gall stone/kidney stone pain
paradoxical
52
what causes the worsening of the gall/kidney stone pain?
increases smooth muscle contraction by morphine acting on mu receptor squeezing on stone
53
are young or old more sensitive to morphine?
both
54
what is responsible for skin flushing?
morphine histamine response
55
acute overdose problem includes?
opiate triad
56
what are the 3 parts of the opiate triad?
respiratory depression, comatose, miosis
57
how do you treat the opioid triad?
naloxone iv
58
what are the three chronic treatment issues?
dependence, addiction, tolerance
59
what has a higher effect morphine or codeiene?
morphine
60
what CYP does codeiene get metabolized by?
2D6
61
what is morphine's prodrug?
codeiene
62
heroin is _____ morphine
diacetyl
63
heroine has _____ CNS entry
fast
64
heroine is a _____ of morphine
prodrug
65
in OD, what is the marker for heroin use?
6MAM
66
what three phenanthrenes are alagesics?
hydrocodone, oxycodone, hydromorphine
67
is immediate release or XR preferred?
immediate release
68
you should avoid opioids in combo with _____
benzos
69
with acute pain, you start with a ___ dose
low
70
what is levorphanol's efficacy in relation to morphines?
same efficacy
71
what is dextrorphan's use?
anti-tussive
72
is dextrorphan an opioid?
non-opiate
73
what receptor does dextrorphan interact with?
NMDA
74
what is meperidine's efficacy in relation to morphine's?
lower efficacy
75
what happens with convulsions on merperidine?
inc
76
which version of merperidine is responsible for convulsions?
normerperidine
77
is merperidine used?
no
78
what is normerperidine's efficacy compared to merperidine?
1/2 as effective as merperidine
79
what is normerperidine's toxicity in comparison to merperidine?
2x as toxic as merperidine
80
when combined with _____ normerperidine's toxicity increases
SSRI
81
what is common with serotonin syndrome
normerperidine toxicity symptoms + fever
82
what are the 4 common normerperidine toxicity manifestations?
seizure, irritability, tremor, myoclonus
83
diphyloxylate and loperamide are used for?
diarrhea
84
merperidine begins as....
MPTP
85
MPTP becomes____ when enters the brain
MPP+
86
MPP+ finally converts to...
DA
87
neuron death leads to _____ syndrome
parkinsons
88
what is fentanyls potency and efficacy compared to morphine?
higher
89
fentanyl is a ____ opioid
synthetic
90
fentanyl is used for 2 purposes _____ and ______
anesthesia + analgesia
91
three fentanyl analogs are...
alentanil, sulfentanil, remifentanil
92
(T/F) fentanyl is often used as an additive to make something more potent
T
93
"designer drug" lead to passing of which act?
controlled substance analog act
94
what is methadone's efficacy compared to morphine?
same
95
what happens to methadone's t1/2 with repeat doses?
inc
96
LAAM's efficacy is similiar to ___
methadone
97
propoxyphene's efficacy is lower than ______
codeiene
98
fentanyl has a ____ efficacy
superior
99
morphine and methadone have a ____ efficacy
high
100
codeiene has ____ efficacy
good
101
propoxyphene has ____ efficacy
low
102
efficacy as an analgesic correlates with efficacy to produce ____
euphoria
103
you should use the ____ efficacy possible for the pain
lowest
104
two liabilities with mu agonists are...
OD and abuse liability
105
a mu selective agonist is...
methadone
106
the ligand selectivity is based on...
receptor binding
107
analgesia, euphoria, and respiratory depression are common to which receptor subtypes?
mu
108
analgesia, dysphoria, and NO respiratory depression are common to which receptor subtypes?
kappa
109
opiate mixed agonist/antagonist combine actions at which two receptors?
mu and kappa
110
nalorphine MOA
mu antagonist/ kappa agonist
111
nalorphine had ____ abuse liability
no (mu antagonizing)
112
nalorphine had ____ analgesic action
good (kappa agonist)
113
pentazocine MOA?
mu partial agonist/kappa weak agonist
114
is pentazocine abuse -free?
no
115
Nalbuphine MOA?
weak mu antagonist/weak kappa agonist
116
butorphanol MOA?
partial mu agonist/weak kappa agonist
117
buprenorphine MOA?
partial mu agonist/weak kappa antagonist
118
how fast does buprenorphine leave the mu receptor?
slow offset from mu receptor
119
the maximum number of drug-receptor transduction effects is greater if drugs leave receptors ____ after producing effect
fast
120
narcan has a ___t1/2
short
121
naltrexone has a ____t1/2
long
122
naltrexone can be given ___ form
oral
123
narcan (naloxone) is given ___ form
iv
124
what does it mean if a small dose of iv naloxone is given and some reversal?
opioid involvement
125
(T/F) naloxone can cause withdrawal
T
126
narcan has two forms... they are ___ and ___
nasal and iv
127
the two full antagonists are...
vivitrol + narcan
128
what happens to the endogenous opiates as a result of vivitrol?
they are blocked too so no "normal good feelings"
129
vivitrol is active in the ____ form
po
130
(T/F)spinal intrathecal administration is addictive
F
131
rate the following opioid agonist/antagonist mixed compounds from most to least efficient? nalorphine, pentazocine, buprenorphine
buprenorphine >
pentazocine >
nalorphine
132
which opiate is available as sustained release?
oxycontin
