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4. Pharm III > 1- Opioids > Flashcards

1- Opioids Flashcards

1
Q

What is the role of endogenous opioid peptides?

A

Released in response to pain and lead to decreased responsiveness to pain

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2
Q

Endogenous opioids are found in areas of the brain involved in what?

A

Reward system

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3
Q

What are the 3 endogenous opioids?

A

Enkephalins, beta-endorphins, dynorphin

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4
Q

What is the role of enkephalins? (endogenous opioid)

A

↓ pain transmission in spinal cord

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5
Q

What is the role of beta-endorphins? (endogenous opioids)

A

↓ pain and facilitate DA → euphoria

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6
Q

What is the role of dynorphin? (endogenous opioid)

A

Bind to kappa receptors → analgesia or dysphoria

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7
Q

What are the effects of binding to the mu (𝝁) receptor?

A

Analgesia, euphoria, sedation, SE

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8
Q

What are the effects of binding to the kappa (𝜿) receptor?

A

Analgesia OR dysphoria (individual variance)

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9
Q

What are the effects of binding to the delta (𝛅) receptor?

A

Dysphoria

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10
Q

All opioid receptors are coupled to Gi/O. This leads to ↓ cAMP, ↓ release of excitatory NTs (in dorsal horn) by closing Ca voltage channels on presynaptic terminal and ultimately leads to what?

A

↓ neuronal activity in pain pathways

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11
Q

Opioids have a direction action at what tissue?

A

Inflamed and damaged

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12
Q

Opioids remove inhibition in periaqueductal grey area, resulting in what?

A

Release of endogenous opioids

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13
Q

What is the effect of opioids on GABA?

A

Block release → activation of descending pathway that inhibits pain transmission → ↓ pain transmission

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14
Q

What is the contribution of only mu (𝝁) receptors with respect to opioid activity?

A

Open K channels → hyperpolarization → inhibit nerve transmission → harder for neurons to respond to pain signals

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15
Q

Opioid effects are dependent on what?

A

Receptor distribution in the individual

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16
Q

What is the effect of opioids with respect to analgesia?

A

↓ sensation & reaction to pain, tolerance develops quickly

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17
Q

Are opioids used as sleep aids?

A

No- quality of sedation different

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18
Q

With respect to sedative effects, opioid overdose leads to what?

A

Graded depression of cortical function: mental clouding/ sedation → hypnosis/ stupor → coma → death

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19
Q

How can opioids lead to emesis?

A

Stimulate chemoreceptor trigger zone (CTZ), depression of cough reflex

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20
Q

When is respiratory depression more common w/ opioid use and what condition may this effect be useful in?

A

More common in OD, useful in pulmonary edema

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21
Q

Because opioids can result in elevated intracranial pressure, you should be cautious with use in who?

A

Pts with head trauma

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22
Q

What effect of opioids does not develop tolerance and why is this beneficial?

A

Miosis, can be used as dx tool

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23
Q

Do opioids have the potential to increase or decrease body temp?

A

Decrease

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24
Q

When can truncal rigidity occur with the use of opioids and what might this complicate?

A

If given too quickly, may interfere w/ respiration or attempts to ventilate patient

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25
Q

How can truncal rigidity with use of opioids be prevented?

A

Injecting slowly or using NM blockers

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26
Q

What are the CV effects of opioids?

A
  • No direct effect (possible bradycardia)
  • Hypotension from CNS depression or histamine release
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27
Q

What significant GI effect is seen with opioids?

A

Constipation (proactively tx/edu)

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28
Q

How do opioids affect the GU system?

A

Antidiuretic effect, increase sphincter and urethral tone

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29
Q

What populations should you avoid use of opioids with due to their effects on the GU system?

A

Avoid in pts w/ BPH or in pts passing kidney stone

(antidiuretic effect and increase sphincter and urethral tone)

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30
Q

What is the effect of opioids on the uterus?

A

Prolonged labor

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31
Q

What are the endocrine effects of opioids?

A

Increases AHD, prolactin, somatotropin

Inhibits LH

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32
Q

Opioids result in histamine release which may result in flushing, itching, or sweating. Is this considered an opioid allergy?

A

NO

(more common if injected)

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33
Q

How can the effects of histamine release from opioids be treated/ prevented?

A

Antihistamines

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34
Q

What are the SEs of opioids? (8)

A

N/V (take w/ food)

Constipation

Urinary retention

Itching

Respiratory depression

Postural hypotension

Restlessness

Dysphoria

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35
Q

When is respiratory depression (SE of opioids) worse and when should this lead to caution?

A

Worse w/ higher doses (dangerous if naive users)

Caution in pulmonary disease

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36
Q

When does tolerance to opioids develop?

A

Chronic use, occurs rapidly and more common w/ drugs that have lower efficacy → higher doses needed

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37
Q

To what opioid effects can an individual develop tolerance? (5)

A

Analgesia, sedation, euphoria, N/V, respiratory depression

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38
Q

To what opioid effects can an individual NOT develop tolerance? (3)

A

Miosis, constipation, seizures

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39
Q

Due to the fact that physical dependence to opioids can develop, when might withdrawal occur?

A

If stopped abruptly

(physical dependence due to desensitization of 𝝁 receptors)

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40
Q

How can physical dependence to opioids be decreased?

A

W/ use of NMDA receptor antagonists

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41
Q

When does hyperalgesia occur with opioid use?

A

Chronic use

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42
Q

How can hyperalgesia be decreased with chronic opioid use?

A

NMDA receptor antagonist

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43
Q

Do patients who develop a tolerance to opioids have an addiction?

A

Not necessarily, but patients with addiction are also tolerant

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44
Q

In addiction with opioids, the brain responds by decreasing dopamine receptors. What does this result in?

A

Substance doesn’t provide as much pleasure anymore but craving for it is worse

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45
Q

What is defined as compulsive use of drugs (in spite of adverse consequences) that are no longer required medically?

A

Addiction

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46
Q

Abondoning responsibilities, constipation, depression, mood swings, slurred speech, poor coordination, needle marks from injection, and infections from injection are all signs of what?

A

Addiction

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47
Q

Addiction to opioids is more likely under what circumstance?

A

If UNDERprescribed, pt develops severe pain → relieved by opioids → reinforcement and reward pathway activated

48
Q

What is important to prevent addiction to opioids?

A

Stay ahead of the pain

49
Q

The following are sxs of what?

Dysphoria, anxiety, insomnia, anorexia, yawning, chills, goosebumps, vomiting, diarrhea, rhinorrhea, lacrimation, increased BP/ HR/ temp, muscle aches/ twitches

A

Opioid withdrawal

50
Q

Sxs of opioid withdrawal can be reduced with the use of what?

A

Clonidine (or another opioid- Methadone)

51
Q

Opioid antagonists can precipitate what if dependent?

A

Withdrawal

52
Q

What are the signs of opioid overdose?

A

CNS depression, respiratory depression, pinpoint pupils (may dilate if severely hypoxic)

53
Q

How do you treat opioid overdose?

A

Supporting respiration + opioid antagonist (Narcan)

54
Q

What are the routes of administration for opioids? (5)

A

Patient controlled analgesia, transdermal patch, intranasal spray, buccal-lollipop, sublingual

55
Q

In order to maximize effectiveness, opioids should be combined with what?

A

Non-opioids

56
Q

What is the protocol for opioid use in terminal illness?

A

Use enough drug to control pain and relieve suffering

57
Q

Aside from analgesia, what are the clinical uses of opioids?

A

Acute pulmonary edema, relief of cough, treatment of diarrhea, anesthesia

58
Q

How are opioids used in anesthesia?

A

General- adjunct to control pain

Spinal- epidural with local anesthetics

59
Q

What drug interactions should you be cautious of with use of opioids?

A

Sedative hypnotics, antipsychotics, MAO inhibitors, CYP2D6 inhibitors

60
Q

Opioids + sedative hypnotics will have what what effects?

A

Increased CNS and respiratory depression

61
Q

Opioids + antipsychotics will have what effects?

A

Sedation

62
Q

What are the contraindications to opioid use? (5)

A
  • Partial agonist + full agonist
  • Head injuries (increased IC pressure)
  • Pregnancy
  • Impaired pulmonary/ hepatic/ renal fxn
  • Some endocrine diseases
63
Q

When does withdrawal occur with opioids?

A

Abrupt discontinuation after chronic treatment, or with administration of an antagonist or partial agonist

64
Q

Relapse with opioids is often prevented with what?

A

Another opioid (buprenorphine or methadone)

65
Q

Why do addicts often go back to using drugs?

A

Not b/c drugs are working but b/c they don’t want withdrawl or lack of drug causes dysphoria

66
Q

What opioid gets into the brain well, can be injected, snorted or smoked, and is commonly abused because it produces euphoria?

A

Heroin

67
Q

What opioid stimulates all opioid receptors, is a strong agonist, and produces all of the effects of opioids?

A

Morphine

68
Q

What is the use of Morphine and what route of administration is most effective?

A

Severe pain (ER long acting if chronic/ terminal pain)

More effective when injected due to high first pass metabolism

69
Q

What opiois has rapid onset after parenteral administration, max analgesic action w/i 1 hr of injection and duration of analgesia of ~4-6 hrs?

A

Morphine

70
Q

Morphine is primary excreted via what?

A

In the urine as metabolites

71
Q

How is morphine metabolized?

A

In liver by CYP2D6

72
Q

What are the SEs of morphine if injected?

A

Itching or vomiting

73
Q

Morphine and other opioids readily cross the placental barrier and can affect the fetus how?

A

Respiratory depression or drug dependence with chronic use

74
Q

Why is Hydromorphone a good alternative to morphine? (3)

A

More potent, metabolites don’t accumulate so good if renal dysfunction, less likely to cause histamine release and itching

75
Q

What opioid has a long half life/ duration of actio, stimulates mu receptors, and may also block NMDA receptors and inhibit NE/5-HT reuptake?

A

Methadone

76
Q

What is the use of Methadone? (3)

A

Maintenance treatment of addicts, long-term control of pain, low does used to prevent withdrawal sxs (withdrawal milder but prolonged)

77
Q

What opioid is effective in “hard-to-treat” types of pain?

A

Methadone

78
Q

What are the SEs of Meperidine (Demerol)?

A

Euphoria, tachycardia, pupil dilation

(Normeperidine can cause seizures)

79
Q

What is the caution with Meperidine (Demerol)?

A

Do not use for > 48 hrs, in high doses, or in renal failure (due to accumulation of metabolites)

80
Q

What is the use of Meperidine (Demerol)?

A

Obstetrics- less respiratory depression in baby

(also no cough suppression)

81
Q

What is the caution with Meperidine (Demerol) and MAOIs or other anti depressants?

A

Serotonin syndrome

82
Q

What opioid is very lipid soluble, highly potent, has a short duration of action and half life, and high abuse potential?

A

Fentanyl

83
Q

What is the use of Fentanyl?

A

Short surgical procedures (w/ midazolam), longer surgeries (good CV profile)

84
Q

What are the SEs of Fentanyl?

A

Truncal rigidity (if given rapidly IV), drug interactions (CYP3A4)

85
Q

What are available routes of admin for Fentanyl?

A

IV, transdermal patches, lollipops

86
Q

What opioids is used for mod to severe pain, often combined w/ acetaminophen, given orally/ well absorbed, and has a fairly short half life and duration of action?

A

Hydrocodone and Oxycodone

87
Q

Conversion by what is needed for some of the analgesic effect of Hydrocodone?

A

CYP2D6 (therefore doesn’t work as well in some pts on SSRIs)

88
Q

Why is it recommended to prescribe Hydrocodone, Oxycodone or Codeine w/o acetaminophen?

A

Risk of acetaminophen toxicity

89
Q

Oxycodone, Hydrocodone, and Codeine must be metabolized by what in order to become active and to increase analgesic effectiveness?

A

CYP2D6

90
Q

How has oxycodone changed to decrease abuse potential?

A

Delivery forms modified, Naloxoen or naltrexone added to prevent effect if injected

91
Q

What is the use of Codeine?

A

Cough suppresant, mild to mod pain

92
Q

What is the caution with Codeine?

A

Shouldn’t be used in small children

93
Q

What opioids are generally given orally in combo with acetaminophen or aspirin?

A

Codeine, Oxycodone, Hydrocodone

94
Q

How can genetic differences in CYP2D6 lead to different drug effects?

A

Ultra metabolizers (convert more than they should)

Extensive metabolizers (normal)

Poor metabolizers (basically useless)

95
Q

What opioid is a kappa receptor agonist, and a mu receptor partial agonist?

A

Pentazocine/ naloxone

96
Q

What is the use of Pentazocine/ naloxone?

A

Moderate pain, oral or injected

97
Q

What are the benefits of using Pentazocine/ naloxone over some other opioids?

A

Fewer SEs (less sedating, resp depression, and GI effects)

98
Q

What are the cautions with use of Pentazocine/ naloxone?

A

May cause dysphoria, may cause withdrawl in pts dependent on opioids (partial mu agonist)

99
Q

What opioid is a partial agonist on mu and has a ceiling effect (therefore not causing much euphoria)?

A

Buprenorphine

100
Q

What is the use of Buprenorphine?

A

Maintenance treatment of opioid addiction- decreases craving for drug

101
Q

Buprenorphine is typically combined with what other drug?

A

Naloxone

102
Q

What is the MOA of Tramadol?

A

Weak mu agonist, inhibits NE/5-HT reuptake (contributes to analgesic effect)

103
Q

What is the use of Tramadol?

A

Mild to mod pain

104
Q

What drug interactions should you be cautious of when using Tramadol?

A

Combo with antidepressants- seizures

Combo with MAOIs, TCAs, SSRIs- serotonin syndrome

105
Q

What is the MOA for Dextromethorphan?

A

Blocks NMDA receptors, decreases 5-HT reuptake

106
Q

What is the use of Dextromethorphan?

A

Cough suppressant (not an analgesic)

107
Q

What drug is associated with abuse in teenages and has even caused some deaths (robotripping)?

A

Dextromethorphan (in some OTC meds)

108
Q

With respect to SEs, what is a benefit of Dextromethorphan?

A

Not likely to cause constipation

109
Q

What is the MOA of opioid antagonists?

A

Bind to opioid receptors and prevent agonists from acting

110
Q

When will mixed opioid agonists/ antagonists exert their effects?

A

Alone will cause stimulation of receptor

Antagonism if other stronger agonist used concurrently

111
Q

What is the DOC for opioid overdose?

A

Narcan (reverses resp depression, consciousness, awareness of pain, miosis, constipation)

112
Q

How is Narcan administered?

A

Must be injected, give until pupils dilate

113
Q

What is the duration of action of Narcan?

A

Short (2 hrs)

114
Q

What is the use for Naltrexone?

A

Treatment of opioid addicts (esp HCPs), decreases craving in recovering alcoholics

115
Q

What are the pharmacokinetics of Naltrexone?

A

Effective orally and long-acting

Long acting prep injected to treat addiction

116
Q

What effect might Naltrexone have in patients dependent on opioids?

A

Will precipitate withdrawal

117
Q

What is the caution with use of Naltrexone chronically?

A

Liver toxicity (concern in alcoholics)

4. Pharm III (16 decks)

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