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Pharmacology > Opioids > Flashcards

Opioids Flashcards

1
Q

morphine is the

A

prototypic opioid agonist

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2
Q

opioid

A

all compounds that work on opioid receptors

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3
Q

opiate

A

naturally occurring alkaloid from the opium poppy

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4
Q

when did the opioid crisis start

A

1990s-ish

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5
Q

pain that occurs when nerve endings are activated by tissue damage or inflammation

A

nociceptive pain

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6
Q

often a result of injury, protective response

A

nociceptive pain

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7
Q

abnormal processing of stimuli from the peripheral or central nervous systems

A

neuropathic

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8
Q

no functional purpose, described as burning, electric shock

A

neuropathic pain

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9
Q

physical pain that is caused, increased, or prolonged by mental, emotional or behavioral factors

A

psychogenic pain

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10
Q

pathophysiology of nociceptive pain (5 steps)

A
  1. site of injury
  2. chemicals release that allow neurotransmission along ascending nerve to dorsal horn
  3. impulse follows spinothalamic tract to brain
  4. pain perceived by brain
  5. impulse travels descending path to make a motor response
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11
Q

opioid receptors are located in the

A

CNS, GI tract, bladder

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12
Q

most of the adverse side effects are due to

A

peripheral stimulation of opioid receptors

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13
Q

opioid receptors inhibits response at dorsal horn

A

dorsal root ganglia

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14
Q

opioid receptors reduce neurotransmitter release and decreases signaling and inhibit post synaptic neuron signaling

A

dorsal root ganglia

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15
Q

opioid receptors simulates endogenous opioid system

A

cerebral cortex

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16
Q

controls pain, reward, and addicitive behaviors

A

cerebral cortex

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17
Q

opioid receptors mimics the action of endorphins, enkephalins, dynomorphins in the

A

cerebral cortex

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18
Q

what are the opioid receptor types

A
  1. Mu
  2. Delta
  3. Kappa
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19
Q

what is the primary opioid receptor

A

Mu

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20
Q

are specific agonists available for opioid receptors?

A

no

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21
Q

this receptor is located in the CNS at supraspinal and spinal sites and the PNS in the GI tract, cardiovascular, and immune systems

A

Mu receptors

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22
Q

primary use for opioid mu receptor

A

analgesia

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23
Q

side effects of mu receptor

A

respiratory depression, sedation, pruritus, euphoria, miosis (pinpoint), decreased GI motility, urinary rentention, physical dependence, hormone changes, stimulate dopamine/acetylcholine release

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24
Q

chronic use of opioids can lead to

A

immunosuppression

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25
Q

what opioid receptor is located primarily within the dorsal horn of the spinal cord and brain stem

A

Kappa receptor

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26
Q

effects of kappa opioid receptor

A

modest analgesia

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27
Q

adverse effects of kappa receptor (7)

A

diuresis, dysphoria, sedation, resp depression, bradycardia, decreased GI motility, hallucunations

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28
Q

what opioid receptor is primary located in the brain and is a binding site for endogenous peptides

A

Delta receptor

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29
Q

effects of delta receptor

A

some analgesia

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30
Q

adverse effects of delta receptor (6)

A

dysphoria, delusions, hallucinations, dependence, hormonal changes, dopamine release

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31
Q

pure opioid agonists stimulate the (which receptor)

A

mu receptor

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32
Q

pure opioid receptors are the most potent ____

A

analgesics

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33
Q

in a pure opioid agonist, as the dose increases the analgesia increases in a _____ _____ _____

A

log linear fashion

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34
Q

the degree of analgesia is limited by

A

side effects

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35
Q

start ____ and go ____

A

low, slow

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36
Q

you should start with a ____ ____ pure opioid agonist when prescribing medication

A

short acting

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37
Q

classes of pure opioid agonists

A

phenanthrene, phenylpiperidine, diphenylheptane

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38
Q

example of phenanthrene

A

morphine, oxycodone, hydrocodone

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39
Q

example of phenylpiperidine

A

fentanyl

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40
Q

example of diphenylheptane

A

methadone

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41
Q

things to consider when using opioids for pain management (5)

A

pharmacokinetic profile, ROA, setting, patient history, adverse effects

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42
Q

through what system are opioids metabolized?

A

CYP 450 system

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43
Q

by using the CYP 450 system to metabolize opioids, this causes an increase ____ for _____ _____

A

risk, drug interactions

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44
Q

many metabolites are excreted ____

A

renally

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45
Q

what type of medication is codeine

A

very weak mu receptor agonist

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46
Q

codeine is ingested as the “inactive” form of the drug, turning into ___ when activated. Codeine is known as a ____.

A

morphine, prodrug

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47
Q

where is codeine converted into morphine and how?

A

liver. Codeine –> CYP2D6 –> morphine

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47
Q

in normal metabolizers what percent of codeine is converted to morphine?

A

10%

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48
Q

what percentage of Caucasians and Asian/African Americans lack the ability to metabolize codeine into morphine?

A

6-10% Caucasians
2-5% Asian / African American

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49
Q

if someone lacks the ability to metabolize codeine into morphine there is no _____ ____

A

therapeutic benefit

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50
Q

what percent of people are ultra rapid metabolizers covert codeine to >10% morphine

A

1%

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51
Q

if you are an ultra rapid metabolizer, you are at increased risk for what

A

respiratory depression

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52
Q

contraindications of codeine? (2ish)

A

Children, children especially after a tonsillectomy

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53
Q

at lower doses codeine can suppress the ___ ____

A

cough reflex

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54
Q

what is made of Tylenol #3/#4

A

acetaminophen/codeine
(#3 = mg codeine, #4 = 60mg tylenol)

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55
Q

a complex response involving the central and peripheral nervous system as well as the smooth muscle of the bronchial tree

A

cough relfex

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56
Q

this opioid medication is known as the gold standard opioid

A

morphine

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57
Q

how is morphine available?

A

Oral, SQ, IV, IM, Intrathecal

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58
Q

if someone has chronic pain and has tried quite a few other pain medications, what type of morphine would you prescribe?

A

oral sustained release: MS contin (12 hours)
oral extended release: Kadian (12-24hrs)

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59
Q

is IV morphine short or long acting?

A

short acting, rapid onset

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60
Q

what types of morphine isnt really recommended due to

A

IM & SQ

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61
Q

what is peak onset time for IV morphine and its duration time?

A

onset is 20 minutes, duration is 3-5 hours

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62
Q

what is morphine used for (2)

A

pulmonary edema, pain relief

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63
Q

what opioid medication has lower affinity for mu receptor

A

hydrocodone

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64
Q

true or false: hydrocodone is mostly combined with something else

A

true

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65
Q

hydrocodone + acetaminophen =

A

Vicodin, Norco, Lorect

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66
Q

hydrocodone + ibuprofen =

A

Vicoprofen

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67
Q

hydrocodone is weaker than

A

oxycodone

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68
Q

what opioid medication has a higher affinity for the mu receptor

A

oxycodone

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69
Q

oxycodone + acetaminophen =

A

Percocet(pill), Roxicet (oral solution)

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70
Q

Oxycodone + ASA =

71
Q

peak and duration for Percodan

A

1 hour, 4-5 hr duration

72
Q

OxyContin is ___ ____

A

controlled release

73
Q

what is peak and duration for OxyContin

A

3-4 hour peak, 12 hour duration

74
Q

hydromorphone =

75
Q

what opioid is a strong opioid agonist

A

hydromorphone

76
Q

hydromorphone has similar _____ as morphine but a higher _____

A

efficacy, potency

77
Q

how is hydromorphone available?

A

PO, SQ, IM, IV, PR

78
Q

what method of admin is hydromorphone NOT recommended in?

79
Q

can hydromorphone be used in a PCA form?

80
Q

true/false: hydrocodone is also available in dilaudid HP

81
Q

hydrocodone oral peak & duration

A

30-90 minutes, 4-5 hours

82
Q

hydrocodone IV peak

A

10-20 minutes

83
Q

risk of hydrocodone

A

prolonged QT, increased risk of seizures

84
Q

how is hydrocodone eliminated

85
Q

contraindications of hydrocodone?

A

kidney disease

86
Q

meperidine =

87
Q

meperidine uses what type of metabolism?

A

hepatic P450 metabolism

88
Q

what product is made from the hepatic P450 metabolism in meperidine?

A

normeperidine

89
Q

accumulation of normeperidine in the blood leads to

A

sezuires, renal failure

90
Q

how is meperidine administered?

A

PO, IM, SQ, IV

91
Q

when can meperidine (demerol) be fatal?

A

when used with MAOIs

92
Q

is meperidine recommended as a first line agent?

93
Q

what is one unique factor regarding overdose of meperidine?

A

naloxone does not reverse metabolite (can worsen seziures)

94
Q

fentanyl =

A

duragesic, fentora (DANGER)

95
Q

what opioid is a very potent agent, 50-100 times more potent than morphine and 30-50 times more potent than heroin?

96
Q

should you give fentanyl to an opiate naive patient for chronic pain treatment?

A

absolutely NOT

97
Q

IV effect time/duration

A

immediate effect, 30-60 min duration

98
Q

duragesic ROA =

A

transdermal

99
Q

duragesic has a (short/long) halflife and the patch is worn for ___ hours

A

long, 72 hours

100
Q

fentora ROA =

101
Q

fentora is often used for

A

breakthrough pain in oncology patients

102
Q

what is unique about fentanyl? (and also crazy scary for doctors and first responders)

A

absorbed through the skin

103
Q

what opioid is used in managing chronic pain and treating opioid addiction

104
Q

mechanism of action of methadone (3)

A
  1. Mu agonist
  2. N-methyl-D-aspartate (NMDA antagonist)
  3. NE and 5HT re-uptake inhibitor
105
Q

half life of methadone

A

12-40 hours

106
Q

adverse side effects methadone

A

pronlonged QT, conversion between products NOT linear

107
Q

what opioid is a non-opioid synthetic analgesic and barely stimulates the mu receptor?

A

tramadol (ultram)

108
Q

mechanism of action of tramadol

A
  1. very mild mu agonist
  2. reduces re-uptake of NE and 5-HT
109
Q

what are some positives to taking tramadol vs other opioids?

A
  1. less resp depression
  2. less histamine release
110
Q

side effects of tramadol

A
  1. N/V
  2. constipation
  3. HA & dizzy
  4. SERATONIN SYNDROME
  5. SEIZURES
111
Q

contraindications of tramadol

A

a patient who takes SSRI’s

112
Q

potentially life-threatening condition associated with increased serotonergic activity in the CNS

A

serotonin syndrome

113
Q

clinical manifestations of serotonin syndrome (2)

A
  1. AMS
  2. Agitation
114
Q

Autonomic symptoms of Serotonin Syndrome (5)

A
  1. Tachycardia
  2. Hyperthermia
  3. sweating
  4. diarrhea
  5. mydriasis (dilated pupil)
115
Q

neuromuscular hyperactivity in serotonin syndrome =

A

hyperreflexia

116
Q

higher doses of opioids are associated with higher risk of ______

117
Q

a value assigned to opioids to represent their relative potencies

A

Miligram Morphine Equivalent (MME)

118
Q

what is the reason for calculating the MME?

A

can assess how much opioids a patient is recieving

119
Q

if >50 MME/day the risk of overdose _____

120
Q

1 opioid side efecct

A

constipation

121
Q

why do opioids cause constipation? (3)

A
  1. decreases intestinal secretions
  2. decrease peristalsis
  3. increased smooth muscle tone
122
Q

does a tolerance develop with constipation and taking opioids?

123
Q

treatments for constipation while taking opioids (4)

A
  1. scheduled stimulant laxative
  2. increase fluid intake
  3. exercise
  4. peripherally acting opioid antagonists
124
Q

what opioid side effect stimulates receptors of the medulla called the chemoreceptor trigger zone

A

Nausea/Vomiting

125
Q

does N/V while taking opioids get worse with constipation?

126
Q

can you build a tolerance to opioid caused N/V?

A

yes, 3-4 days

127
Q

what opioid side effect should you start at a low dose to avoid?

128
Q

name the opioid side effect based on these factors:
1. CNS depressant
2. dose dependent
3. tolerance builds in 1-3 days

129
Q

pathognomonic sign of opioid overdose =

A

miosis (pinpoint pupils)

130
Q

are there any major side effects of the cardiac system at low doses

A

usually not

131
Q

high doses of opioids can cause these cardiac symptoms (2)

A
  1. bradycardia
  2. hypotension
132
Q

do you develop a tolerance to urinary retention when taking opioids?

A

either/or, its a surprise :)

133
Q

what is the main cause of death from an opioid overdose?

A

respiratory depression

134
Q

does tolerance develop in respiratory depression

135
Q

respiratory depression is ____ _____

A

dose dependent

136
Q

treatment of adverse opioid side effects (2)

A
  1. hold opioid
  2. naloxone
137
Q

Mechanism of action of naloxone

A
  1. antagonizes both mu 1&2
  2. rapid onset, short half-life
138
Q

gradual loss of effect with repeated doses =

139
Q

when is tolerance typically seen?

A

2-3 mo of use

140
Q

patients on chronic opioid therapy should consider ___ ____ to avoid tolerance

A

opioid rotation

141
Q

what side effects develop a tolerance

A

sedation, resp depression, N/V, +/- urinary retention

142
Q

adaptation which produces withdrawal when drug is stopped

A

physical dependence

143
Q

strong desire or a sense of compulsion to take a drug, progressive neglect of alternative pleasures of interests because of drug use, increased amount of time spent obtaining drug

A

psychological dependence or addiction

144
Q

a primary chronic disease of brain reward, motivation, memory, and related circuitry

A

addiction (per the american society of addiction medicine)

145
Q

what does addiction cause

A

pathologic pursuit of reward and relief through substance use and other behaviors

146
Q

severity and duration depends on quantity, type, frequency, and duration of opioid use

A

withdrawal

147
Q

symptoms of withdrawal occur with ____ cessation and ____ when on chronic opioids

A

abrupt, chronic

148
Q

removal of inhibition =

A

increases neurotransmission

149
Q

withdrawal symptoms

A

abd pain, diarrhea, HTN, lacrimation, rhinorrhea, goosebumps, pupillary dilation, hyperventilation, pain/irritability, dysphoria/depression, restlessness and insomnia, forgetfulness

150
Q

diphenoxylate (lomotil) is used to treat

151
Q

what type of license must you have to prescribe lomotil and what schedule drug is it?

A

DEA, its a schedule 5

152
Q

what is in lomotil that makes it an opioid like product?

A

Diphenoxylate

153
Q

Diphenoxylate is insoluble so it stays in the ____ _____

154
Q

what is loperamide (imodium) used for?

A

diarrhea treatment

155
Q

loperamide is an ____ ______

A

opioid agonist

156
Q

does loperamide stay in the GI tract?

157
Q

high doses of loperamide can interact with the ____

158
Q

people often misuse ____ & ______ to get a small high and end up with ______

A

loperamide & diphenoxylate, f ton of constipation

159
Q

what is dextromethorphan (delsym, DM) used for?

A

anti-tussive

160
Q

what is in dextromethorphan?

A

dextro-isomer of codeine

161
Q

effects of dextromethorphan are _____ by opioid antagonists but in high doses interacts with ____ and causes _____

A

unaffected, CNS, euphoria

162
Q

what are 3 non-analgesic uses of opioids (3 meds)

A
  1. Diphenoxylate
  2. Loperamide
  3. Dextromethorphan
163
Q

opioid antagonists

A

compete with opioid receptors

164
Q

what is the primary opioid antagonist?

165
Q

effects of opioid antagonists (3)

A
  1. reverse agonists
  2. deterrent to use
  3. different medications have different pharmacokinetic profiles
166
Q

examples of opioid antagonists (4)

A
  1. naloxone
  2. Naltrexone
  3. Naloxegol
  4. Methylnaltrexone
167
Q

important characteristics about naloxone (4)

A
  1. rapid reverse of opioid OD
  2. Low PO bioavail (give nasal, IV, IM, etc)
  3. rapid onset
  4. SHORT duration of action (often give multiple doses)
168
Q

side effects of naloxone (4)

A
  1. projectile vomiting
  2. agitation
  3. HTN
  4. Tachycardia
169
Q

do you need a perscription for naloxone?

A

no, available at pharmacy, in most AEDs and EMTs/Police carry

170
Q

important characteristics about Naltrexone (reVia, Vivitrol) (5)

A
  1. opioid & alcohol addiction
  2. NOT given with opioid agonists (reverses effect)
  3. NOT for use during acute withdrawl
  4. given for cravings
  5. available oral and IM
171
Q

side effects of naltrexone

A

depression, suicide risk, hepatotoxicity, insomnia, N/V

172
Q

important charcateristics of Naloxegol (moveantik)

A
  1. naloxone + polyethylene glycol polymer
  2. works ONLY within GI (too large to leave)
  3. available PO
173
Q

important characteristics of methylnaltrexone (relistor)

A
  1. quaternary derivative of naltrexone
  2. works ONLY in GI (positive charge keeps in GI)
  3. available SC
174
Q

both Naloxegol and Methylnaltrexone treat opioid ______

A

constipation

Pharmacology (7 decks)

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