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Pharmacology Test #4 > Pharmacology of Opioid Analgesics > Flashcards

Pharmacology of Opioid Analgesics Flashcards

1
Q

Analgesia definition

A

block pain neurotransmission; antinociception

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2
Q

Anesthesia definition

A

block sensory neurotransmission; pain, motor and autonomic pathways

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3
Q

Nociception definition

A

pain sensation

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4
Q

qd

A

once daily

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5
Q

bid

A

twice a day

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6
Q

Q12

A

every 12 hrs

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7
Q

tid

A

three times a day

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8
Q

qid

A

four times a day

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9
Q

What happens when tissue is damaged

A

release of cytokines, chemical mediators

increase vascularization, sensitize somatosensory nervous system, promote recovery

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10
Q

Types of pain

A

thermal, mechanical, and chemical

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11
Q

Co-morbidities with chronic pain

A

anxiety, depression, insomnia/disrupted sleep, activation of glia, hyperalgesia, allodynia

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12
Q

How are pain signals transmitted

A

pain signals are transmitted to the CNS where different aspects of the pain signal are processed by specific brain regions

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13
Q

Assigns aversive or pleasurable qualities to pain

A

nucleus accumbens

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14
Q

Involved with fear processing associated with pain expectation

A

amygdala

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15
Q

important for determining what action should be taken to deal with pain (fight or flight)

A

frontal cortex

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16
Q

Key brain regions expression opioid receptors

A
  1. periagueductal gray (PAG)
  2. rostral ventral medulla (RVM)
  3. dorsal root ganglion (drg)/dorsal horn
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17
Q

Two types of alkaloids that opium contains

A
  1. Phenanthrenes

2. Benzylisoquinolines

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18
Q

Mu opioid receptor structures can be divided into

A

phenanthrene and non-phenanthrene alkaloids

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19
Q

Phenanthrene opioids primarily show differences where

A

at the 3 and 6 position

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20
Q

How is antagonist of phenanthrene opioids conferred

A

conferred by bulky side groups indicated in the red circle

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21
Q

Why is it worthwhile to switch between phenanthrene and non-phenanthrene opioids in patients that are not responsive/show strong side effects to one type

A

it is suggested that some patients respond better to phenanthrene than non-phenanthrene opioids and vice versa

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22
Q

Phenanthrenes

A

morphine, hydrocodone, buprenorphine, naloxone

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23
Q

Non-phenanthrenes

A

tramadol, meperidine, fentanyl, and methadone

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24
Q

Metabolism of phenanthrene opioids occurs primarily by

A

glucorinidation at the 3 and 6 position

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25
Q

Activity of morphine-6-glucoronide

A

metabolite that is still pharmacologically active

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26
Q

Where is morphine/phenanthrenes metabolized

A

large hepatic (CYP2D6) and can be impaired by patients with liver disease or genetic difference in the make up of their liver enzymes

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27
Q

Where is morphine/phenanthrenes excreted?

A

excreted through the kidneys by glomerular filtration

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28
Q

Describe opioid receptors

A

G protein-coupled receptors
family A- peptide receptors
Gi/o - coupled (inhibition of cAMP production)

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29
Q

Three types of opioid receptors

A

Mu, Kappa, Delta, Nociceptin orphanin FQ receptor

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30
Q

Are there currently kappa or delta opioid-selective FDA approved drugs

A

No

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31
Q

Therapeutic targets for the mu opioid receptor

A

analgesia (not acute sharp localized pain, not neuropathic pain, cancer pain, peripheral, PCA)
sedation
antitussive (supress cough reflex)

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32
Q

Natural ligand for the mu opioid receptor?

A

beta-endorphine (endogenous morphine)
pro-opiomelanocortin (POMC)
“runners high”

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33
Q

Side effects from the mu opioid receptor

A

respiratory depression, constipation, pruritis, tolerance/dependent, urinary retention, nausea/vomiting, muscle rigidity, miosis

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34
Q

Kappa opioid receptor are involved in what type of feedback loop

A

negative feedback loop, inhibiting the release of dopamine

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35
Q

Describe the negative feedback loop with the kappa opioid receptor

A

initial release of dopamine causes transcription of dynorphin, the endogenous kappa opioid agonist; release of dynorphin will activate presynaptic Kappa receptors on dopaminergic terminals, inhibiting further release of dopamine

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36
Q

Endogenous kappa opioid agonist

A

dynorphin

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37
Q

Kappa opioid receptor has potential for use of treatment of

A

addiction

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38
Q

Salivinorin A

A

Kappa opioid receptor agonist, not an alkaloid

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39
Q

Delta opioid receptors are being considered as target for

A

anxiety, depressive and alcohol use disorders, preventing ischemic damage

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40
Q

Natural ligands for the delta opioid receptor

A

enkephalins

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41
Q

Endogenous peptides released during hibernation act on which receptors

A

delta receptors

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42
Q

When are delta opioid receptors upregulated

A

during chronic stimulation, such as during chronic inflammation and nerve damage, thus making it an interested target for treatment of chronic pain

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43
Q

Effect of Mu opioid receptor activation

A

analgesia, euphoria and mood effects, respiratory depression, miosis, neuroendocrine regulation, decreased GI motility, autonomic regulation, tolerance and withdrawal

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44
Q

Endogenous Mu opioid receptor peptide affinity

A

Endorphins

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45
Q

Effect of Kappa opioid receptor activation

A

analgesia, diuresis, sedation, dysphoria and psychotomimetic, less miosis, less respiratory depression, little dependence

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46
Q

Effect of Delta opioid receptor activation

A

analgesia, mood, hypoxia, chronic pain, alcohol addiction

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47
Q

Effect of Orphanin opioid-receptor-like sybtype 1 (ORL1), Nociceptin receptor activation

A

controversy actions, opposes classic mu effects, mediate pain

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48
Q

Endogenous ORL1, Nociceptin peptide affinity

A

Nociceptin/Orphanin FQ

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49
Q

Opioids bind to

A

opioid receptors which are G-protein coupled receptors

50
Q

All opioid receptors are

A

Gi/o-coupled causing inhibition of adenylyl cyclase induced cAMP production

51
Q

Opioid receptors also activate which channels (besides G-protein coupled)

A

GIRK channels (G-protein activated inwardly rectifying potassium channels) causing hyperpolarization, inhibiting neurotransmitter release

52
Q

Where are opioid receptors located on the neuron

A

located both presynaptic and postsynaptic

53
Q

Presynaptic inhibition of neurotransmitter release is mediated by

A

inhibition of calcium uptake

54
Q

Postsynaptic inhibition of pain transmission is by

A

inducing hyperpolarization throgh activation of GIRK channels -> effux of K+

55
Q

Clinically used opioid receptor agonists (strongest)

A

sufentanil, remifentanyl, fentanyl, hydromorphone (Dilaudid), morphine, hydrocodone, oxycodone

56
Q

Opioid receptor agonists used most often in surgical settings

A

sufentanil, remifentanyl, fentanyl

57
Q

Opioid receptor agonists used most often post-surgically

A

hydromorphone and morphine

58
Q

Orally available opioid receptor agonists

A

hydrocodone (Lortab/Vicodin/Norco) and Oxycodone (oxycontin/percocet)

59
Q

Clinical used opiod receptor agonists not as strong

A

Methadone, Meperidine (Demerol), Codeine, Tramadol (Ultram), Loperamide (Imodium), Propoxyphene (Darvon)

60
Q

Meperidine (Demerol) used to treat

A

rigors

61
Q

Tramadol (Ultram) used when

A

painkiller used when you don’t want to prescribe a stronger opioid

62
Q

Loperamide (Imodium) used as

A

an anti-diarrheal

63
Q

Why is risk of dependence low with Loperamide (Imodium)

A

PgP substrate -> low BBB penetration -> doesn’t get into the CNS with risk of dependence is lower

64
Q

When is Propoxyphene (Darvon) used

A

withdrawn due to heart rhythm abnormalities

65
Q

Non phenanthrene opioids

A

Tramadol (Ultram), Tapentadol (Nucynta), Meperidine (Demerol)

66
Q

Tramadol (Ultram), Tapentadol (Nucynta) have what kind of properties

A

SNRI properties; 5HT/NE reuptake inhibitor, stimulate 5HT release

67
Q

Activate metabolite of Meperidine (Normeperidine) can do what?

A

can accumulate and cuase CNS irritability and myoclonic seizures

68
Q

When is Meperidine recommended?

A

not recommended without good justification; dangerous in patients with decreased renal function

69
Q

Opioids with NMDA action

A

Methadone and Levorphanol

70
Q

Methadone

A

primarily used for opioid dependence; NMDA antagonist; chronic pain; long duration of action

71
Q

Levorphanol

A

analgesic half-life is shower than the serum half-life of drug; NMDA antagonist; neuropahtic pain

72
Q

Why is antagonism at NMDA receptors useful?

A

NMDA receptors are upregulated in chronic pain

73
Q

What is upregulated during chronic pain establishment

A

AMPA and NDMA receptors

74
Q

Buprenorphine

A

partial mu agonist, weak K agonist and delta antagonist; long acting; low tolerance, dependence and addiction, used to treat opioid withdrawal in addiction therapy

75
Q

Buprenorphine as a partial agonist can activate?

A

mu receptors and cause euphoria and analgesia to a lesser extent than a full agonist like morphine would

76
Q

If a patient is already using a full agonist buprenorphine will work as a

A

antagonist and can thus induce some withdrawal signs

77
Q

Partial mu antagonists

A

Naloxone (Narcan) and Naltrexone (Revia/vivitrol)

78
Q

Which opioids are used for surgery and why?

A

fentanyl, sufentanil, remifentanil

fast onset, short duration

79
Q

Which opioids are used postop and for epidurals and why?

A

hydromorphone (dilaudid) and morphine

4-5X more potent than morphine, greater half life than fentanyl

80
Q

Which opioids are used for management of pain and why?

A

oxycodone, hydrocodone, oxycontin, and zohydro

oral bioavailability, greater half life than fentanil

81
Q

Which opioid is used for terminal cancer pain and why?

A

morphine

low cost, history of knowledge, risk of dependence not an issue in a terminal cancer patient

82
Q

Which opioid is used for opioid intolerance and why?

A

Merperidine (Demerol)
constipation less common than with morphine; seizure, delirium, neurotoxic, metabolites not blocked by NTX; MAO inhibitors contraindicated

83
Q

Administration routes of opioids

A

IV, intramuscular, intraaxial, intrathecal, epidural, oral, topical/transdermal/transmucosal

84
Q

Why are opioids like remifentanyl, sufentanil useful for inducing and maintaining surgial analgesia/anesthesia?

A

they reach peak plasma level quickly and are quickly excreted

85
Q

Rationales for opioid rotation

A
  1. lack of initial efficacy, despite titration to acceptable levels
  2. decreased efficacy over time (tolerance)
  3. side effects that cannot be tolerated or adequately remedied
  4. insurance coverage and cost constraints
86
Q

How do you calculate an equianalgesic dose?

A
  1. convert each opioid to equi-analgesic morphine dose
  2. combine morphine equivalents to calculate total daily opioid dose
  3. calculate daily equivalent dose of new opioid
87
Q

At a low dose, opioids will cause

A

euphoria and pain relief

88
Q

At a high dose of opioids, patients will experience

A

constipation, miosis, urinary retention, itch and respiratory depression

89
Q

Major side effect of prolonged opioid use

A

constipation

90
Q

Major strategy of dealing with opioid induced constipation (OIC)

A

peripherally restricted opioid antagonists

91
Q

Preventive and acute management of ileus and constipation

A

senna, polyethylene glycol (Miralax) and dioctyl sodium sulfosuccinate/docusate

92
Q

Senna

A

Irritates colon, causes fluid secretion/colonic contraction

93
Q

Polyethylene glycol (Miralax)

A

stool softener; osmotic increase in GI water content

94
Q

Dioctyl sodium sulfosuccinate/docusate

A

stool softener; peristalsis greater than 400 mg/day

95
Q

Peripherally restricted my opioid antagonists

A

Methylnaltrexone (Relistor), Alvimopan (Entereg), Naloxegol (Movantik), and Naldemedine

96
Q

Is opioid induced itch an allergic reaction?

A

No

97
Q

What causes opioid induced pruritis?

A

heteromer of a mu opioid receptor splice variant and the gastrin releasing peptide receptor

98
Q

Opioid tolerance

A

analgesic effects, nausea, urinary retention, respiratory depression, euphoria

99
Q

Biggest risk of death with opioid tolerance in which people

A

biggest risk of death in withdrawn patients/users (addicts that relapse)

100
Q

Changes seen with tolerance

A

increased dose required to produce equivalent effect
receptor adaptation
decreased receptor number
decreased coupling to effector

101
Q

Changes seen with hyperalgesia

A

compensatory changes

altered excitability of target neurons

102
Q

Neurotransmitters involved with opioid induced hyperalgesia

A

NMDA, cholecystokinin, dynorphin, substance P

103
Q

What causes persistent inhibition of adenylyl cyclase with opioid tolerance

A

activation of MORs by morphine and many other Mu opioid receptor agonists does not lead to strong phosphorylation and desensitization of the receptor

104
Q

In response to maintain homeostasis in opioid tolerance, what does the cell do?

A

the cell upregulates adenylyl cyclase -> causes an increase in cAMP production leading to cellular tolerance to t he opioid effect

105
Q

Honestly just go learn the opioid tolerance mechanism really well

A

It’s too complicated to put into flashcards

106
Q

Signs of opioid induced hypersensitivity

A

pain not relieved (exacerbated) by opioid
diffuse pain
cold pressor test (emerge arm in ice bath and check time to withdraw)

107
Q

What to do with signs of OIH?

A 
switch opioid class
phenanthrenes vs non-phenanthrenes
108
Q

Opioid detox

A

switch to clonidine/diazepam

109
Q

Use extreme caution when administering opioid to patients with

A

compromised respiratory function

chronic bronchitis, asthma, emphysema

110
Q

Opioids and seizure disorders

A

opioids may aggravate pre-exisint seizure problems

111
Q

Opioid drug-drug interactions

A 
Depressants (alcohol, benzos, barbituarates)
Antipsychotics
TCA antidepressants
Antihistamines
Meperidine (MAOs, SSRIs)
112
Q

Symptoms of morphine and heroin overdose

A

coma, depressed respiration, pinpoint pupils (miosis), needle marks, mixed poisonings

113
Q

Treatment for acute opioid overdose

A

restore respiration, maintain CV function, Naloxone (opioid antagonist)

114
Q

FDA approved opioids to treat opioid abuse

A

methadone, buprenorphine, suboxone, zubsolv

115
Q

Suboxone

A

buprenorphine + maloxone

116
Q

The presence of naloxone in suboxone is used as

A

an abuse deterrent

117
Q

What do some opioids for treating diarrhea contain as an abuse deterrent?

A

atropine

118
Q

Agonist maintenance to treat opioid addiction

A

methadone maintenance therapy; cross tolerance to heroin can reduce illicit drug use

119
Q

Partial agonist therapy for opioid addiction

A

buprenorphine; cross tolerance; pharmacologically blocks effects of opiate agonists

120
Q

Antagonist therapy for opioid addiction

A

naltrexone; long-term treatment; does not alleviate cravings

121
Q

Should you prescribe opioids?

A

Yes but with proper awareness, monitoring, communications with the patient

122
Q

Opioids to treat alcohol use disorders

A

Naltrexone, Nalmefene

Pharmacology Test #4 (9 decks)

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