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Spring 2024 Therapeutics 3 > Final Opiate Drugs > Flashcards

Final Opiate Drugs Flashcards

1
Q

What is an alkaloid?

A

Plant derived compound with a basic nitrogen

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2
Q

What are the two types of alkaloids contained in opium?

A

Phenanthrenes

Benzylisoquinolines

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3
Q

What are the Phenanthrene drugs?

A

Morphine
Codeine
Thebaine

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4
Q

What are the Benzylisoquinoline drugs?

A

Noscapine
Papaverine

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5
Q

What are opiates?

A

The opioids that are naturally occurring
-plant derived compounds

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6
Q

Substitutions at the 3 position of the phenanthrene ring do what?

A

Ethers or Esters produce DECREASED potency

(codeine)

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7
Q

Substitutions at the 6 position of the phenanthrene ring do what?

A

INCREASE activity

(hydromorphone or hydrocodone)

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8
Q

Substitutions at the 14 position of the phenanthrene ring do what?

A

OH has increased potency (oxycodone)

N-allyl gives antagonist or mixed antagonists (naloxone or naltrexone)

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9
Q

What are the non-phenanthrenes?

A

Tramadol
Meperidine
Fentanyl
Methadone

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10
Q

What are the genes that encode endogenous opioids?

A

Pro-opiomelanocortin (POMC)

Preproenkephalin

Preprodynorphin

Nociceptin/Orphanin FQ

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11
Q

What opioid receptors does the pro-opiomelanocortin (POMC) gene encode?

A

B-endorphin works on Mu receptors

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12
Q

What opioid receptors does the preproenkephalin gene encode?

A

Leu-Enkephalin = delta receptors

Met-enkephalin= mu and delta receptors

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13
Q

What opioid receptors does the preprodynorphin gene encode?

A

Dynorphin works on kappa receptors

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14
Q

What opioid receptors does the nociceptin/orphanin FQ gene encode?

A

Nociceptin, completely different mechanism

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15
Q

What affects do the opioid receptors have on ion channels?

A

Open GIRK potassium channels (postsynaptic)

Close calcium channels to decrease neurotransmitter release (presynaptic)

*K leaving hyperpolarizes the cell and makes it more difficult for the neuron to fire
*reduces pain signaling

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16
Q

Which opioid receptor specifically is responsible for the hyperpolarization of the cell?

A

Mu receptors

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17
Q

What are the opioid receptors?

A

Mu (M-morphine)
Kappa (K-ketocyclazocine)
Delta (D- deference - where it was identified)

Nociceptin (orphanin FQ receptor)

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18
Q

What is the endogenous opioid of Mu receptors?

A

Endorphin

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19
Q

What is the endogenous opioid of Kappa receptors?

A

Dynorphin

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20
Q

What is the endogenous opioid of Delta receptors?

A

enkephalin

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21
Q

What are beta-endorphins?

A

Endogenous morphine

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22
Q

What are the therapeutic uses of the beta-endorphins?

A

Analgesia:
-Not as effective for chronic pain, better for breakthrough pain
-Used for patient-controlled analgesia

Sedation

Antitussive

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23
Q

Opioid-induced side effects are mostly what kind of effects?

A

On-target effects

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24
Q

What are the common side effects of opioids?

A

-Respiratory Depression
-Constipation
-Pruritus (itching) *not an allergic response
-Addiction
Urinary retention
-Nausea/Vomiting
-Miosis (pinpoint pupils)

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25
Q

Would you use an opioid as an anti-diarrheal?

A

Yes
-one that stays out of CNS and in the GI tract

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26
Q

Activation of kappa opioid receptors has what affect?

A

Dysphoric and Aversive

-negative effect, kappa opioid receptor agonists can be combined with mu opioid agonists to reduce the addiction potential

-decreases dopamine release

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27
Q

Which opioid receptor may be useful to combat opioid addiction?

A

Kappa receptors

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28
Q

Which opioid receptor does not have any FDA approved agonists?

A

Delta receptor

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29
Q

What are the uses of the delta opioid receptor?

A

-Reduce anxiety
-Reduce depression
-Treat alcoholism
-Relief hyperalgesia, chronic pain

-May protect against hypoxia, ischemia, and stroke

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30
Q

What side effect is associated with delta opioid receptors?

A

Seizures

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31
Q

What two areas of the brain are important for reward and linked to addiction?

A

Ventral Tegmental Area

Nucleus Accumbens

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32
Q

How do opioids function in the brain to increase reward?

A

Opioid binds the mu receptor

Gi signaling inhibits neurotransmitter release

Less GABA to activate GABA A

Less inhbition of dopamine activity

Increased dopamine release and increased dopamine receptor activation

(mu receptor reduces GABA release which increases dopamine release)

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33
Q

Which opioid drug shows a slower and more sustained peak?

A

Morphine (longer half life)

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34
Q

What is the % bioavailability of morphine?

A

25%

*first pass metabolism

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35
Q

What is morphine a substrate of?

A

CYP2D6

CYP3A4

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36
Q

How does liver disease affect the half-life of morphine?

A

Increased half-life with liver disease

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37
Q

What % of morphine is excreted in 24h?

A

90%

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38
Q

Which opioids are prodrugs?

A

Heroin
Codeine
Tramadol

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39
Q

What is the inactive metabolite of codeine and what active metabolites is it changed to?

A

Inactive: Norcodeine

Active: Hydrocodone, Morphine

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40
Q

What is the active metabolite of tramadol?

A

O-desmethyltramadol

*not a pharmaceutical opioid

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41
Q

What is the inactive metabolite of heroin and what active metabolite is it changed to?

A

Inactive: Normorphine

Active: Morphine

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42
Q

What is the lipophilicity of morphine and how does this impact its passage across the BBB and its duration of action?

A

Low Lipophilicity
Slow passage across BBB
Long duration of action

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43
Q

What is the lipophilicity of fentanyl and how does this impact its onset and duration of action?

A

High lipophilicity
Rapid onset
Short duration

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44
Q

CYP3A4 makes what opioids?

A

(FOUR) makes opioids starting with NOR

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45
Q

What are nor opioid metabolites?

A

-Made by CYP3A4
-Less active
-Nor= without a methyl group (demethylated)

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46
Q

What enzyme activates codeine to morphine?

A

CYP2D6

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47
Q

What are the 4 possible CYP2D6 metabolizers?

A

PM: poor metabolizers
IM: intermediate metabolizers
EM: extensive metabolizers
UM: ultra-rapid metabolizers

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48
Q

Ultrarapid metabolizers of CYP2D6 would experience what effects with codeine?

A

Activate codeine at a much higher rate, would have more adverse effects

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49
Q

Poor metabolizers of CYP2D6 would have what effects with codeine?

A

No therapeutic effect

*more common in caucasians

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50
Q

True or False: Fentanyl is a low potency opioid

A

FALSE
-very potent

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51
Q

When is fentanyl used?

A

Palliative care

Breakthrough pain

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52
Q

What side effect is a concern with fentanyl?

A

Respiratory depression

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53
Q

The majority of opioids are what schedule?

A

Schedule II

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54
Q

The opioids Sufentanil, Remifentanil, and Alfentanil undergo what breakdown in the body?

A

Breakdown by plasma esterases due to ester linkage

55
Q

What is the extended-release form of morphine?

A

MScontin

56
Q

What is Lortab/Vicodin/Norco?

A

Hydrocodone + Acetaminophen

57
Q

What is Percocet?

A

Oxycodone + Acetaminophen

58
Q

Besides analgesia, what other property does Tramadol have?

A

SNRI

59
Q

When would we use Tramadol?

A

When you do not want to prescribe a stronger opioid

-Used for neuropathic pain

60
Q

What is an important point to remember about Meperidine?

A

Has a toxic metabolite: Normeperidine

(CYP3A4)
*metabolite is not an analgesic

61
Q

When would we use Meperidine?

A

Not recommended without good justification because of toxic metabolite

-Treats rigors (shivering)

62
Q

Who should not receive Meperidine?

A

Patients with decreased renal function

63
Q

When do we use Methadone?

A

For opioid dependence

64
Q

What is the MOA of methadone?

A

NMDA antagonist

-This is an ion channel glutamate receptor that is important for the conduction of pain signals
-Blocking this receptor blocks pain coming into the spinal cord and brain

65
Q

What opioids can be used for cough/antitussive effects?

A

-Codeine
-Dextromethorphan (limited opioid activity)

66
Q

Which opioids can be used as anti-diarrheal?

A

Diphenoxylate with atropine

Loperamide

Eluxadoline

67
Q

Which opioids act as both Mu and Kappa receptors and what are they used for?

A

Moderate Pain

-Pentazocine
-Butorphanol
-Nalbuphine
-Buprenorphine (mainly used in opioid replacement therapy)

68
Q

Which drug can cause colonic contraction?
(used to manage constipation caused by opioids)

A

Senna

69
Q

What are the side effects of opioids that show limited or no tolerance (will not go away as the body adapts to the drug)?

A

**Constipation
-Itch
-Miosis (pin pupils)

70
Q

Which treatment for opioid dependence is a full agonist?

A

Methadone

71
Q

What are the clinical pearls of methadone?

A

*Slow acting
-Accumulates with repeated dosing

72
Q

What is the main function of Methadone in preventing opioid use?

A

Provides relief from withdrawal symptoms

73
Q

Which treatment for opioid dependence is a partial agonist?

A

Buprenorphine

74
Q

Why is Buprenorphine a partial agonist?

A

Partially agonizes (activates) mu opioid receptors to prevent withdrawal

But also blocks the full agonist effects of opioids

75
Q

What are the trade names of Buprenorphine?

A

Subutex *abuse potential

Suboxone (also contains naloxone to block agonist effects when taken IV)

76
Q

What treatment for opioid dependence is an antagonist?

A

Naltrexone

77
Q

How is Naltrexone administered?

A

IM injection

-ER release
-Once monthly

*also po daily form with decent bioavailability

78
Q

When should patients take Naltrexone?

A

Works best if patient has been drug free for 1 month and the risk for withdrawal is decreased

**This drug will cause withdrawal if taken during active opioid addiction

79
Q

True or False: Naloxone and Naltrexone are interchangeable

A

False!!!

Naloxone: Antidote to overdose
Naltrexone: Blocks reinforcement of opioids

80
Q

What are the clinical pearls of Naloxone?

A

IV or intranasal administration

Limited oral bioavailability

Rapid onset

*Short half-life

81
Q

What are the clinical pearls of Naltrexone?

A

Decent oral bioavailability

PO administration

Medium half-life (longer word, longer half-life)

82
Q

If 1 shot of Naloxone (Narcan) does not bring an overdosed patient cack to consciousness, how long should we wait before administering another dose?

A

Repeat doses every 2-5 mins if not conscious

83
Q

What is a concerning symptom of neonatal abstinence syndrome in babies?

A

Seizures in babies of methadone users

84
Q

True or False: Opioids can be present in breast milk

A

True

85
Q

What drugs can be used in neonatal abstinence syndrome and are linked with shorter hospital stays?

A

Morphine

Buprenorphine

86
Q

What are the signs of opioid overdose vs opioid withdrawal?

A

Overdose:
-Sedation
-Pinpoint pupils
-Decreased respiratory rate

Withdrawal:
-Insomnia
-Dilated pupils
-Increased respiratory rate

87
Q

What is the reversal agent for opioid overdose?

A

Naloxone (Narcan)

88
Q

What is the MOA of Naloxone?

A

Opioid antagonist

89
Q

What forms is naloxone available in?

A

IV
Nasal Spray

90
Q

What is a risk with using naloxone?

A

Can cause opioid withdrawal

91
Q

When should naloxone be prescribed?

A

Together with opioids

In patients at risk for overdose
–History of overdose
–History of substance use disorder
–High opioid doses (>50 morphine equiv)
–*Concurrent benzodiazepine use (“pams”)

92
Q

How often can doses of naloxone spray be given?

A

Every 2-3 minutes

93
Q

Which drugs can be used to treat symptoms of opioid withdrawal?

A

Clonidine
Buprenorphine
Methadone

94
Q

Which opioid is metabolized to morphine and by what?

A

Codeine

by CYP2D6

95
Q

Poor metabolizers of codeine will get what effect?

A

NO effect

(needs to be activated)

96
Q

Ultra-rapid metabolizers of codeine will get what effect?

A

Overdose and Toxicity

*especially in children, can cause death

97
Q

Who should not receive codeine?

A

Breastfeeding mothers

Children <12

98
Q

What is the boxed warning for tramadol?

A

Use of CYP 450 3A4 inducers, 3A4 inhibitors, and 2D6 inhibitors with tramadol require careful consideration of effect on the parent drug and metabolite

99
Q

What schedule is Tramadol?

A

IV

100
Q

What side effect is most common with morphine compared to other opioids?

A

Itching

101
Q

When should morphine use be avoided?

A

*Morphine and it metabolites are renally excreted

-avoid in Stage 4 or 5 chronic kidney disease

102
Q

What boxed warning is associated with morphine?

A

Avoid alcohol while taking ER capsules

103
Q

What boxed warning is associated with Hydromorphone (Dilaudid)?

A

Warning about dosing errors when prescribing, dispensing, and administering

*Oral solution: Do not confuse mg with mL

*IV: Do not confuse high potency solution (10mg/ml) with others (1,2, or 4)

104
Q

What is Norco made up of?

A

Hydrocodone (5, 7.5, or 10mg)

Acetaminophen (325mg)

105
Q

Which forms of oxycodone are abuse deterrent?

A

ER capsule, tablets

106
Q

What is the name for the combination product of oxycodone and acetaminophen?

A

Percocet

107
Q

When might fentanyl be a good treatment option?

A

For a fast on/off pain treatment

*In renal impairment (not excreted by kidneys)

108
Q

What dosage forms does fentanyl come in?

A

Buccal tablet
Sublingual liquid
Lozenge
**Injectable solution
Patch

109
Q

What symptom is LESS of an issue with fentanyl?

A

Hypotension

110
Q

When can non-injectable fentanyl be used?

A

ONLY in patients who are opioid tolerant

111
Q

What is considered “opioid tolerant”?

A

Taking morphine 60mg per day (or equivalent) for at least 1 week

112
Q

When using the fentanyl patch dosing chart, what is an important point to remember?

A

*Can only use the chart to go from oral to transdermal and not the other way around

-because there is a built-in buffer to prevent overdose

113
Q

What are the counselling points for the fentanyl patch?

A

Do not cut patches

Do not let the patch get too warm while wearing

Apply one patch every 72 hours

114
Q

What is the last line opioid treatment for chronic pain?

A

Methadone (Methadose)

(used primarily to treat addiction)

115
Q

What significant side effect is associated with Methadone (Methadose)?

A

QTc prolongation

116
Q

What are the clinical pearls to remember for Meperidine (Demerol)?

A

-Not used much, many SE
-Avoid in elderly
-Avoid in renal impairment
-Caution in hepatic impairment

NEVER USE THIS

117
Q

What patients should not receive tramadol?

A

History of seizure

118
Q

Which opioids have non-po options?

A

Morphine
Hydromorphone (Dilaudid)
Fentanyl (Duragesic)

Methadone but not used commonly
Meperidine but not used

119
Q

Which opioids have long-acting formulations?

A

Tramadol
Morphine
Hydromorphone
Hydrocodone
Oxycodone

120
Q

If a patient has an allergy to an opioid, what other opioids can be used?

A

Fentanyl
Methadone
Meperidine
Tramadol

(do not have an allergic cross reaction)

121
Q

Which opioids can we not convert to oral morphine?

A

Codeine
Methadone
Tramadol

122
Q

The CDC guideline for prescribing opioids applies to which patients?

A

Outpatients > 18 years old
Acute, Subacute, or Chronic pain

NOT:
-sickle cell disease pain
-caner pain
-palliative or end of life care

123
Q

True or False: Nonopioid therapies are at least as effective as opioids for many types of acute pain

A

True

124
Q

What is the 1st recommendation when considering prescribing opioids?

A

Maximize non-pharm and non-opioid options FIRST

(also preferred for subacute and chronic pain)

125
Q

What is the second recommendation when considering prescribing opioids?

A

Always start with immediate-release opioid options, never long-acting

Prescribe the lowest effective dose of opioids (especially in naiive patients)

For patients already receiving opioids: weigh benefits and risks when changing opioid dosage
-if they do not outweigh risks, gradually taper down dose

126
Q

What is the third recommendation in opioid prescribing?

A

-When used for acute care, do not prescribe a greater quantity than needed for the expected duration of pain severe enough to require opioids

-Evaluate benefits vs risks with patients 1-4 weeks into starting therapy

-Regularly reevaluate risks vs benefit

127
Q

What is the fourth recommendation for opioid prescribing?

A

Implement strategies to mitigate risk (naloxone)

Occasionally review the patient’s history of controlled substance prescriptions to determine if the patient is receiving dosages or combinations that put them at risk for overdose

Consider toxicology testing to assess for other prescribed or nonprescribed substance use

Caution with concurrent prescription of opioids and benzodiazepines

Treat opioid use disorder

Do not do detoxification without medications for opioid use disorder

128
Q

What is the tapering schedule that should be followed to taper off opioids?

A

On for more than a year: decrease dose by 10% each month

On for less than a year: decrease dose by 10% each week

129
Q

What is the max day-supply of opioids a physician can prescribe if it is their first time prescribing opioids to the patient and there are no extenuating circumstances?

A

7 day supply

130
Q

True or False: Hospitalized patients can only have one order of an opioid for each severity of pain

A

True

(severe, moderate, mild)

131
Q

What is the treatment for low back pain?

A

Non-pharm

1st Line:
–Acetaminophen
–NSAID

2nd Line:
–SNRI
–TCAs

132
Q

What is the treatment for osteoarthritis?

A

Non-pharm

1st Line:
–Acetaminophen
–NSAIDs

2nd Line:
–Intra-articular hyaluronic acid
–Capsaicin

133
Q

What is the treatment for fibromyalgia?

A

Non-pharm

FDA-approved: Pregabalin, Duloxetine

Other: TCA, Gabapentin, Venlafaxine

134
Q

What is the treatment for neuropathic pain?

A

1st line:
–SNRIs
–Gabapentin/Pregabalin

2nd Line:
–Topical Lidocaine
–TCAs

Spring 2024 Therapeutics 3 (24 decks)

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