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Daddy Pharm > Opioids (Exam 2) > Flashcards

Opioids (Exam 2) Flashcards

1
Q

T/F
anaphylaxis is possible from opioids

A

True

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2
Q

T/F
SEs can be beneficial.

A

True
depends on patient and situation. These effects could be good for some pts and bad for others

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3
Q

Respiratory depression d/t

A

decreased SNS outflow and direct effect in respiratory parts of the brain

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4
Q

effects on cerebral blood flow & ICP

A

Decreased CBF
increased ICP

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5
Q

occurrence of N/v

A

30-40% of pts esp on first dose

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6
Q

Effects on body temp

A

Hypothermia

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7
Q

T/F
tolerance cannot be built against opioid SEs

A

False

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8
Q

Constipation

A

direct effect of Mu receptors in GIT to decrease peristaltic activity

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9
Q

Histamine release MoA

A

innate allergy reaction to morphine causing histamine release
can be life threatening or minimal (pruritis)

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10
Q

Your pt states he got itchy when receiving morphine in the past. What should you do?

A

caution when giving an opioid

second exposure can enhance/worsen the allergic rxn on subsequent exposures

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11
Q

Muscular rigidity effects

A

due to inhibition of dopamine release in the striatum (Parkinson-like)

risk ventilation difficulty d/t laryngeal contraction & chest wall rigidity

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12
Q

Striatum

A

area in brain that controls motion

Parkinsons: decrease in dopamine in striatum

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13
Q

Bradycardia due to

A

increased vagal outflow

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14
Q

Orthostatic hypotension/syncope due to

A

decreased sympathetic outflow from the CNS

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15
Q

Are opioids absorbed well in the GIT?

A

most are

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16
Q

T/F
PO opioids are susceptible to first pass metab

A

True
undergo large first pass metab

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17
Q

Which type of agents reach higher CNS conc. faster?

A

more lipid soluble

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18
Q

T/F
most opioids distribute well in circulation

A

True

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19
Q

T/F
↑ lipid solubility agents are more likely to be abused

A

True
higher lipid solubility crosses into brain faster, which creates the euphoria

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20
Q

Which has greater euphoria?
heroin
morphine

A

heroin
more lipid soluble

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21
Q

Fetal effects

A

Most cross placenta well, but fetus can not metabolize much, so conc. is high.

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22
Q

T/F
all opioids are metabolized to some extent

A

True

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23
Q

Excretion mainly via

A

renal and biliary mechanisms of metabolized forms

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24
Q

Two chemical classes of Opium Alkaloids: (resin from poppy)

A

Phenanthrenes:
Morphine
Codeine
Thebain

Benzylisoquinolines:
Papaverine
Noscapine

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25
Q

Morphine structure

A

4 ring-system w/ an overring (“5” rings)
tertiary amine
pKa of >8.0 (bases), so mostly ionized at physiologic pH

very lipid soluble on its own bc of its rings despite OH group

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26
Q

T/F
The benzylisoquinolines family has a structural resemblance to morphine.

A

False
Phenanthrenes

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27
Q

1/10 of morphine’s potency

A

codeine
(Phenanthrenes)

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28
Q

(Phenanthrenes)
Thebain

A

paramorphine
CNS stimulant, can cause convulsions

“Thebain of my existence”

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29
Q

most Phenanthrenes have a pka of ___, so at body pH, what happens?

A

> 8.0 (base)

body pH is more acidic (more H+)
drug will pick up H’s
becomes ionized

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30
Q

Phenanthrenes
Which isomer is more active?

A

Levo

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31
Q

lack standard opioid activity

A

Benzylisoquinolines

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32
Q

(Benzylisoquinolines)
Papaverine

A

a smooth muscle relaxant
phosphodiesterase inhibitor (PEDI) = ↑ cAMP

“relax, papa”(verine)

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33
Q

(Benzylisoquinolines)
Noscapine

A

antitussive and anticancer(?)
Similar effect to codeine

“NOsCA= no cough/cancer”

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34
Q

possess similar effects to codeine

A

Noscapine

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35
Q

phosphodiesterase inhibitor (PDEI)

A

inhibit breakdown of cAMP

(cAMP usually metabolized by PDE)

With papaverine (PDEI):↑cAMP = smooth muscle relaxation (esp GIT)
Note: diff cells have diff rxn to cAMP

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36
Q

T/F
cAMP produces consistent effects regardless of cell type

A

False
cells differ in their response to cAMP and what type of PDE they contain

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37
Q

T/F
Papaverine is a highly specific PDEI

A

False
fairly non specific

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38
Q

Heroin is also known as

A

diacetylmorphine

acetylate morphine’s 2 OH (remove H) groups –> 2 new -COCH3

increases lipid solubility
enters CNS faster

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39
Q

dont memorize, but what are these?

A

opioid antagonists

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40
Q

naltrexone
MoA
Vs morphine

A

opioid antagonist

similar structure to morphine but binds stronger and does not have same agonist activity

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41
Q

Alkaloids (natural compounds) & semi-synthetics

A
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42
Q

Synthetics

A

Meperidine, the fentanyls, lomotil, imodium

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43
Q

base structure for synthetics

A

Space between 3, 6, 17 positions have same angles as morphine nucleus
fits in morphine receptors

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44
Q

First synthetic compound

A

Meperidine

“MEPeridine = ME Pirst”

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45
Q

compound in Lomotil

A

Diphenoxylate

(for GI spasms; drrha)

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46
Q

compound in Imodium

A

Loperamide
(for GI spasms; drrha)

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47
Q

T/F
Fentanyl is a potent morphine agonist.

A

True

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48
Q

Which synthetics do not fit the expected synthetic nucleus

A

dont memorize, just know its different

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49
Q

Methadone

A

addict recovery (heroin)

“Turn a heroin addict into a methadone addict”
-Ron Dick

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50
Q

Which of these is no longer on the market?

A

Propoxyphene
DC’ed due to efficacy; no more effective than the Tylenol it was mixed with

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51
Q

PO morphine

A

MS contin

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52
Q

We often mix this opioid with other because its weak

A

codeine

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53
Q

Levorphanol is an opioid (agonist/antagonist)

A

agonist

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54
Q

T/F
Dextro structures have pain relief properties.

A

True
require large amounts tho

addicts try to purchase tons of Dextromethorphan

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55
Q

Morphine
Natural alkaloid from

A

Papaver somniferum

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56
Q

Morphine MoA

A

primarily at m receptors
(some k)

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57
Q

Agent by which all other opioid agonists are judged

A

morphine
(activity set at “1”)

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58
Q

T/F
Morphine induces its own metabolism.

A

true
leads to its rapid tolerance development

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59
Q

Why does the use of Morphine rise and fall through the years?

A

Dont want to create addicts vs treating pts pain

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60
Q

T/F
Heroin is a naturally occurring opioid, known as an alkaloid.

A

False
semi-synthetic

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61
Q

To make heroin, we acetylate which positions on morphine?

A

hydroxyl groups on positions 3 & 6

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62
Q

Heroin is ___ as potent as morphine

A

twice

(and more lipid soluble)

63
Q

T/F
Heroin in general is not approved for clinical use.

A

True
d/t high addiction liability

(Some states allow for intractable cancer pain; inpatient only)

64
Q

What gives codeine its potency?

A

10% of it is converted to morphine

does not have any notable potency at the receptor!

65
Q

T/F
Codeine does not have an analgesic effects.

A

False
Partially converted (10%) to morphine in the body, which is thought to account for the analgesic component

66
Q

Codeine MoA

A

Potent antitussive in the parent form.

CTZ cough control center in the brainstem

67
Q

Oxycodone (Oxycontin)

A

~2x potent > morphine (as an analgesic)

High euphoric liability

68
Q

T/F
You can crush ER Oxycodone

A

False
Many deaths d/t chewing ER form.

turns it into rapid release (by breaking down “beads” meant to be slowly removed by GIT)

Fatal dose if no tolerance

69
Q

Very potent synthetic morphine analgesic congener (5X)

A

Levorphanol

70
Q

Levorphanol
pros and cons

A

longer lasting
Less constipating (d/t the way it binds to GIT Mu)

potency restricts use (5x morphine)

71
Q

Dextromethorphan

A

dextro-rotary isomer (“no” analgesia)

effective antitussive

72
Q

This isomer has “no” analgesia

A

dextro-rotary

73
Q

Most widely used synthetic congener.

A

Meperidine

74
Q

Meperidine potency

A

Only one-tenth the mg. potency of morphine as an analgesic

(this doesn’t mean its more potent than codeine)

75
Q

T/F
Meperidine is more potent than codeine.

A

False

76
Q

Frequently abused since it does not cause miosis

A

Meperidine

Hard to detect abuse

77
Q

Which opioids’s metabolite can cause seizures?

A

Meperidine

Normeperidine: CNS stimulant ↓renal fxn = build-up → seizure risk

78
Q

Normeperidine lacks which group?

A

methyl

“nor” = without methyl group

79
Q

Contraindicated with MAOI therapy

A

meperidine

80
Q

Your pt is on certain drugs that lower seizure threshold. What should you NOT give for pain?

A

Meperidine

metabolite Normeperidine can cause seizures, risk is higher w/ concomitant use of drugs that lower seizure threshold

81
Q

monoamine oxidase inhibitors (MAOI)

A

Inhibit metabolism of Norepi

pt will have higher degree of CNS stimulation

DO NOT give with Meperidine

82
Q

equipotent to morphine

A

Methadone (Dolophine)

83
Q

Methadone (Dolophine)

A

same potency as morphine but less sedation

longer doA (slower elimination & can counter w/drawl symptoms

84
Q

Heroin addict Tx

A

Methadone (Dolophine)

85
Q

metabolizes Norepi

A

MAO monoamine oxidase

86
Q

Recovery/withdrawl
MoA

A

tolerance leads to oversensitive/overactive systems

increased CNS output (sweating)

cramping, N/V, diarrhea

87
Q

Methadone (Dolophine)
for addiction treatment

A

longer doA = dose less often

minimal sedation = addict can fxn

tightly controlled d/t difficult manufctrg

88
Q

Structurally related to Methadone, but less than one-tenth as potent per mg.

A

Propoxyphene (Darvon)

89
Q

T/F
Propoxyphene (Darvon)
lacks analgesic effects d/t its lack of similar properties to other opioId analgesics.

A

False
yes it sucks as pain relief
but
it has properties similar to other Opioid analgesics

90
Q

Fentanyl (Sublimaze)
chemically r/t ___

A

meperidine

Fentanyl = piperidine = similar to meperidine

91
Q

Fentanyl is __x as potent an analgesic as Morphine

A

80

92
Q

T/F
Fentanyl’s main advantage is its higher potency compared to morphine.

A

False
Main advantage is it’s short half-life of redistribution (12.5 min.).

93
Q

Fentanyl
half-life of redistribution

A

12.5 min

94
Q

Fentanyl’s …. is partially responsible for its abuse potential.

A

short half-life of redistribution (12.5 mins)

fast recovery

95
Q

Fentanyl distribution after administration

A

Very lipid soluble so redistribute brain to fat fast

96
Q

Piperidines vs morphine
relative potencies

A

Sufentanil 800x
Fentanyl 80x
Remifentanil 80x
Alfentanil 20x

97
Q
A
98
Q

Fentanyl routes

A

IV, epidural, transdermal

99
Q

Fent vs remifent

A

remi is selective m-receptor agonist. (vs fentanyl)

100
Q

T/F
esterases are solely found in blood.

A

False
all over the place
liver

101
Q

Differs from other fentanyl derivatives by having an ester-linkage

A

remifent

102
Q

T/F
Remifentanil has a short duration of action due to hydrolysis by tissue esterases.

A

False
non-specific esterases

103
Q

Remi vs. fent
benefits

A

Remi:
shorter duration
more exact titration
rapid recovery

even faster than fentanyl!

104
Q

What makes remifent a good adjunct for induction and/or maintenance in pediatric patients?

A

Peds & neonates have esterases
vs liver enzymes which take time

105
Q

Etorphine (Immobilon, M99)

A

Veterinary-use only

1000X morphine potency

large animal immobilizer

Toxic to humans, one drop on skin can be fatal
d/t ↑↑↑↑ L. sol

Dihydroetorphine (less L sol) used in China as a painkiller, it appears to be less addictive(??)

106
Q

Opioid Antagonists
affinity
intrinsic activity

A

Have receptor affinity but “no” intrinsic activity.

107
Q

Opioid Antagonists
MoA

A

mainly block m receptors
(some k blockade also).

108
Q

affinity but lesser degree of intrinsic activity

A

partial agonist/antagonist

109
Q

What effects do Opioid Antagonists counter?

A

analgesic
respiratory
euphoric
miosis
hypotension
smooth muscle fx

…of opioids AND endogenous b-endorphin and enkephalins

110
Q

T/F
Opioid Antagonists are unable to counter effects from endogenous opioids.

A

False

111
Q

Opioid Antagonists elicit (excitatory/inhibitory) effects.

A

excitatory
could cause seizure in someone who is seizure prone and not in opioid OD

112
Q

Naloxone

A

pure antagonist (mostly m)

usually IV

Complete reversal

113
Q

Nalaxone vs Naltrexone

A

Naltrexone:
similar, but longer half-life
can be given orally
mainly for alcoholics (↓ ethanol intoxication pleasure)

not true 100% antagonist

114
Q

Naltrexone (Revia)

A

similar to naloxone, but longer half-life
can be given orally
mainly for alcoholics (↓ ethanol intoxication pleasure)

not true 100% antagonist

115
Q

Use is to control N&V from opioid agonists

A

Methylnaltrexone (Relistor)

116
Q

Methylnaltrexone (Relistor

A

quat = ionized
**peripheral opioid antagonism

No CNS withdrawal effects**

Use is to control N&V from opioid agonists

117
Q

treat alcoholics by decreasing ethanol intoxication pleasure

A

Naltrexone (Revia)

118
Q

Almivopan (Entereg)

A

oral
m selective peripheral antagonist

approved for post-op ileus

119
Q

Nalmefene (Opvee)

A

analog of naltrexone
nasal spray opioid antagonist
rescue agent for opioid OD

↓ ETOH pleasure

µ and δ antagonist
κ receptor partial agonist

120
Q

Nalmefene (Opvee)
MoA

A

µ and δ antagonist
κ receptor partial agonist

Opioid OD rescue
decrease ETOH pleasure

121
Q

Buprenorphine (Buprenex) shares structural components of …

A

Codeine and Naltrexone

122
Q

Buprenorphine (Buprenex)

A

partial agonist/antagonist

High affinity: mu
weaker max response than other agonists

123
Q

T/F
As a partial agonist/antagonist, Buprenorphine (Buprenex) elicits a weaker maximal response than other agonists and thus cannot relieve pain.

A

False
still has good analgesia, just not as much

124
Q

T/F
Buprenorphine elicits a weaker maximal response than other agonists, so addicts take more of it to get the same effect as stronger substances”

A

FALSE
Partial agonist will never give full effect

125
Q

Can we use Buprenorphine (Buprenex) to counteract addiction?

A

yes

less abuse potential
counteracts Heroin & Morphine addiction w/o causing full-blown withdrawal symptoms

126
Q

limits ability of Naloxone to reverse

A

Buprenorphine (Buprenex)
Slow dissociation from receptors increases duration (8 hrs)

Naloxone has to “wait” for free receptors

127
Q

T/F
Buprenorphine (Buprenex) can precipitate a withdrawal reaction.

A

True
Can displace other mu agonists (antagonistic action)

prevent agonist from beinding = w/drawl

128
Q

Buprenorphine (Buprenex)
uses

A

Heroin & Morphine addictn
moderates severe pain
epidural

129
Q

Mixed Opioid Agonist/Antagonists

A

Nalorphine (Nalline)
Pentazocine
Nalbuphine

130
Q

Nalorphine (Nalline)

A

Veterinary use only

mu antagonist
K weak agonist

blocks m receptor analgesia & euphoria
stimulates k analgesia & sedation

Large doses: ~dysphoria & hallucinations

131
Q

Pentazocine used with ___ to limit abuse

A

Naloxone

132
Q

have similar actions, but are stronger k mediated analgesics than nalorphine

A

Pentazocine
Nalbuphine

133
Q

Tramadol (Ultram)

A

structural similarities to Opioids and NSAIDs

Racemic: diff enantiomers cause each action

Less addiction liability

134
Q

Tramadol (Ultram)
MoA

A

parent compound & active metabolite have:
moderate mu affinity
weak k & d affinity

block re-uptake of serotonin & norepi in central synapses
↓
decreases pain info transmission in brain

135
Q

its analgesic effect is not entirely reversed by Naloxone

A

Tramadol

parent compound & active metabolite have:
moderate mu affinity
weak k & d affinity

naloxone = primarily mu

136
Q

Tramadol SEs

A

dizziness, sedation, seizures and hallucinations

N/V common = limited periop use

increased risk of bleeding if taken with Warfarin

epileptogenic effects

137
Q

T/F
Like other opioids, tramadol is a controlled substance d/t its potency.

A

False
d/t abuse potential

138
Q

Naloxone acts primarily at __ receptors.

A

mu

139
Q

Tramadol’s analgesic strength is comparable to which agent?

A

Codeine-Acetaminophen agents

140
Q

limited periop use d/t N/V

A

tramadol

141
Q

body synthesizes __% of norepi; __% is reused

A

make 20%
reuse 80%

142
Q

Blocking reuptake

A

blocks carrier that brings it back in

compound builds up & stimulates post-synaptic neuron

initial increased stimulation
eventual depletion (b/c we only synthesize 20%)

143
Q

serotonin is also known as

A

5HT
5-hydroxytryptamine

*Note: 5HT3 is a type of serotonin receptor)

144
Q

increased risk of bleeding if taken with Warfarin

A

tramadol

possibly d/t NSAID component

145
Q

causes abuse potential

A

euphoria and sedative effects

146
Q

T/F
Tachyphylaxis develops as higher and higher doses are required to achieve the same euphoria

A

False
Rapid tolerance develops

147
Q

T/F
Many “addicts” only continue to take the opioids to avoid the uncomfortable withdrawal symptoms.

A

True

148
Q

T/F
More prescription abuse than illicit substances.

A

True

149
Q

single largest cause of prescription deaths in US, 2011 -2012.

A

Opana (oxymorphone) ER

150
Q

Rapid Detox

A

Anesthesia + Potent Opioid Antagonist for 6-8 H

Unconscious during w/drawl SEs

151
Q

T/F
Opioids can be used alone or as an adjuvant to anesthesia.

A

True

152
Q

neuroleptic anesthesia

A

butyrophenone (droperidol:
D2 blocker; antiemetic properties)
+
opioid (fentanyl)
+
nitrous oxide, etc.

153
Q

peptide-type opioid receptor agonists

A

pain relief

target receptor sub-types

cant give PO (denatured in stomach)

154
Q

Transplantation of adrenal medullary chromaffin cells

A

chromaffin cells (secrete opioid peptides) into subarachnoid space
long-term pain relief to chronic sufferers w/o exogenous opioid SE’s.

C cells survive for a certain time
No major SE bc endogenous

Daddy Pharm (13 decks)

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