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Therapeutics III > Barker Pharmacology of Opiate Drugs > Flashcards

Barker Pharmacology of Opiate Drugs Flashcards

1
Q

Two types of alkaloids contained in opium

A

-Phenanthrenes
-Benzylisoquinolines

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2
Q

What are examples of phenanthrene opioids?

A

-Morphine
-Codeine
-Thebaine

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3
Q

What is the structure of phenanthrenes?

A

Three ring structure

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4
Q

Difference between opiates and opioids

A

-Opioids describe all kinds of opiates
-Opiates only describe naturally occurring opiates

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5
Q

How does the three position ether or ester substitution change the effect of the phenanthrene?

A

Produces decreased potency

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6
Q

How does the 6 position change the effect of the phenanthrene?

A

Increases activity

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7
Q

How does the 14 position OH change the effect of the phenanthrene?

A

Increases potency

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8
Q

How does the N-allyl change the effect of the phenanthrene?

A

Gives antagonist effect

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9
Q

What are the proteins that are cleaved into opioid peptides?

A

-Pro-opiomelanocortin (POMC)
-Preproenkephalin
-Predynorphin
-Nociceptin/orphanin FQ

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10
Q

What peptides does pro-opiomelanocortin create when cleaved?

A

beta-endorphin

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11
Q

What peptides does preproekephalin create when cleaved?

A

-Leu-enkephalin
-Met-enkaphalin

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12
Q

What peptides does preprodynorphin create when cleaved?

A

Dynorphin

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13
Q

How do opioids inhibit pain signals?

A

Inhibition of cAMP production through the Gi/o coupled receptors

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14
Q

What is the endogenous opioid for Mu receptors?

A

Endorphin

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15
Q

What is the endogenous opioid for kappa receptors?

A

Dynorphin

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16
Q

What is the endogenous opioid for delta receptors?

A

Enkephalin

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17
Q

What is the endogenous opioid for nociceptin, orphanin FQ receptors?

A

Nociceptin

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18
Q

What are sigma receptors?

A

Not opioid receptors

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19
Q

What are the presynaptic effects of opioids?

A

Inhibit calcium channel (Gi) decrease in neurotransmitter release

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20
Q

What are the postsynaptic effects of opioids?

A

-Activate GIRK channel (Gbetagamma)
-Efflux of K+ leads to hyperpolarization

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21
Q

Therapeutic use of beta-endorphins

A

-Analgesia for acute pain such as cancer pain, palliative care, and PCA
-Sedation
-Cough suppression in the medulla oblongata

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22
Q

Opioid-induced side effects

A

-Respiratory depression
-Constipation
-Pruritus (itch) (not allergic response)
-Addiction
-Urinary retention
-Nausea/vomiting
-Miosis

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23
Q

Can you use an opioid as an anti-diarrheal?

A

Yes, only opioids that can stay out of the CNS

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24
Q

What is the effect of the activation of kappa opioid receptors?

A

Dysphoric aversive effects

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25
Q

Potential uses of kappa opioid receptors

A

Treatment of addiction by reducing dopamine release by counterbalancing the effects of the mu opioid receptors

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26
Q

Effects of delta opioids

A

-Role in hypoxia/ischemia/stroke
-Reduce anxiety
-Treat alcoholism
-Relief hyperalgesia, chronic pain
-Side effect: seizures

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27
Q

How do opioids cause a release of dopamine?

A

-Opioid binds mu receptors
-Gi signaling inhibits neurotransmitter release
-Less GABA to activate GABAa
-Less inhibition of dopamine neuron activity
-Increase dopamine release
-Increased activation of dopamine receptors

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28
Q

Administration routes of opioids

A

-Intravenous
-Intra-axial: intrathecal, epidural
-Intra muscular
-Oral
-Topical/transdermal

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29
Q

How rapidly is morphine metabolized?

A

-Readily absorbed
-Undergoes first pass metabolism
-Bioavailability of 25%

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30
Q

How is morphine metabolized

A

In the liver morphine undergoes glucuronidation at the 3 and 6 position to form morphine-6-glucuronide which is a potent active metabolite

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31
Q

Which enzymes metabolize morphine?

A

-CYP2D6
-CYP3A4

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32
Q

How is morphine excreted?

A

-Glomerular filtration
-90% excreted in 24h

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33
Q

Which opioids are prodrugs?

A

-Heroin
-Codeine
-Tramadol

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34
Q

Which opioids do not produce active metabolites?

A

-Fentanyl
-Methadone

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35
Q

How is the onset and duration influenced for opioids?

A

Onset/duration is influenced by lipophilicity

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36
Q

What is codeine metabolized into?

A

-Hydrocodone
-Morphine

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37
Q

What is heroin metabolized into?

A

Morphine

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38
Q

How does the lipophilicity affect the onset/duration of morphine?

A

-Low lipophilicity
-Slower passage across BBB
-Prolonged duration of action

39
Q

How does the lipophilicity affect the onset/duration of fentanyl?

A

-High lipophilicity
-Rapid onset
-Short duration

40
Q

Which enzyme makes opioids starting with nor?

A

CYP3A4

41
Q

Which group of people is more likely to have the CYP2D6 ultra-rapid metabolizer phenotype?

A

People of North African descent

42
Q

What effects do people with the ultra-rapid metabolizing phenotype of CYP2D6 see when given codeine?

A

-Up to 50% higher plasma concentrations of morphine than extensive metabolizer
-Higher incidence of adverse effects

43
Q

Which group of people is more likely to have the CYP2D6 poor metabolizer phenotype?

A

-No therapeutic effect from codeine
-Same incidence of adverse effects

44
Q

How potent is fentanyl compared to other opioids?

A

-~100x potent over morphine
-~50x potent over heroin

45
Q

What is fentanyl used for?

A

-Palliative care
-Breakthrough pain

46
Q

What are the opioid agonists?

A

-Sufentanil, remifentanil, alfentanil
-Fentanyl
-Hydromorphone (Dilaudid), oxymorphone (Opana)
-Morphine
-Hydrocodone
-Oxycodone

47
Q

What are sufentanil, remifentanil, and alfentanil used for?

A

Anesthesia/sedation

48
Q

Why are sufentanil, remifentanil, and alfentanil not as powerful as fentanyl?

A

They are broken down by plasma esterases due to the ester linkage in their structure

49
Q

What makes hydromorphone and oxymorphone different from the other opioids?

A

No opioid-active metabolites

50
Q

Why is morphine preferred over oxycontin?

A

It is covered by medicare

51
Q

What is MScontin?

A

Extended release morphine

52
Q

What are the non-phenanthrene opioids?

A

-Tramadol
-Meperidine
-Methadone

53
Q

Tramadol clinical pearls

A

-Mild opiate analgesic
-Has SNRI properties
-Schedule 4

54
Q

What is tramadol used for?

A

-Management of mild neuropathic pain
-Painkiller used when you do not want to prescribe a stronger opioid

55
Q

What is meperidine used for?

A

Used to treat rigors

56
Q

Meperidine clinical pearls

A

-Has neurotoxic metabolite normeperidine devoid of analgesic
-Renally excreted - dangerous in patients with decreased renal function (accumulation)

57
Q

Side effects of meperidine

A

-Nervousness
-Tremors
-Muscle twitches
-Seizures

58
Q

When is meperidine recommended?

A

Not recommended without good justification

59
Q

What is methadone primarily used for?

A

-Opioid dependence
-Chronic pain

60
Q

Methadone clinical pearl

A

-Long duration of action/long half life (15-60hrs)/ fat solubility
-Prolonged QTc - unwanted effect
-NMDA antagonist

61
Q

Which opioids are used for cough suppression?

A

-Codeine
-Dextromethorphan

62
Q

Dextromethorphan clinical pearls

A

-Enantiomer of levomethorphan
-Limited opioid activity (not scheduled)
-At high doses acts as SSRI, NMDA antagonist

63
Q

Which drugs are used for anti-diarrheal?

A

-Diphenoxylate with atropine
-Loperamide
-Eluxadoline

64
Q

Loperamide clinical pearls

A

-Strong P-glycoprotein substrate - low BBB penetration
-Schedule 5/decontrolled=OTC

65
Q

Eluxadoline clinical pearls

A

-Irritable bowel syndrome with diarrhea
-Mu/kappa agonist, delta antagonist
-Enteric nervous system localization
-Schedule 4

66
Q

What are the opioids that act at Mu and kappa receptors?

A

-Pentazocine and butorphanol
-Nalbuphine
-Buprenorphine

67
Q

Pentazocine and butorphanol activity at receptors

A

K agonist and partial agonist/antagonism at Mu

68
Q

Pentazocine and butorphanol side effects

A

-Less dysphoria
-Hallucinations
-Increase in BP and HR

69
Q

How are pentazocine and butorphanol administered?

A

Parenterally

70
Q

Nalbuphine activity at receptors

A

Full agonist at k, antagonist at Mu

71
Q

Nalbuphine clinical pearls

A

-Antagonism of Mu receptors produces withdrawal in patients with addiction to opioids
-Parenterally administered

72
Q

Buprenorphine effects on receptors

A

-Partial mu agonist
-Weak kappa agonist
-delta antagonist

73
Q

When is buprenorphine primarily used?

A

Primary use in opioid replacement therapy

74
Q

Which drugs are used for preventative and acute management of ileus and constipation?

A

-Senna
-Polyethylene glycol
-Dioctyl sodium sulfosuccinate/docusate

75
Q

What is senna mechanism of action

A

Irritates colon - causes fluid secretion/colonic contraction

76
Q

Polyethylene glycol mechanism of action

A

Stool softener - osmotic increase in GI water content

77
Q

Dioctyl sodium sulfosuccinate/docusate mechanism of action

A

Stool softener, peristalsis when taking more than 400mg/day

78
Q

What effects can people develop tolerance too when taking opioids chronically?

A

-Analgesic effects
-Nausea
-Urinary retention
-Respiratory depression
-Euphoria

79
Q

What is opioid induced hyperalgesia?

A

Prolonged exposure to opiates causes formation of secondary pain pathways

80
Q

What symptoms do people not see any tolerance to?

A

-Constipation
-Itch
-Miosis

81
Q

What is the mechanism of action of methadone?

A

Full Mu opioid receptor agonist

82
Q

What is the indication of methdone?

A

Provide relief from tolerance due to a higher potency than morphine, oxycodone, and Dilaudid

83
Q

Methadone clinical pearls

A

-Slow acting
-Accumulates with repeated dose
-Elimination half-life (8-50hrs)
-Racemic mixuture ((+)=NMDA antagonist)
-Does not have three rings like morphine

84
Q

Buprenorphine mechanism of action

A

-Mu opioid receptor partial agonist
-Ceiling effect
-Blocks full agonist effect
-Antagonist by blocking effects of other narcotics
-Use 4hrs after last heroin use
-Provides some activation because of agonist effect to provide less withdrawal symptoms

85
Q

Side effect of subutex

A

Abuse potential

86
Q

Suboxone mechanism of action

A

Partially blocks agonist effects when taken IV

87
Q

Naltrexone clinical pearls

A

-Intramuscular injection
-Extended release
-Once monthly for IM
-PO is once daily dose
-Decent oral bioavailability
-Medium half-life
-Will cause withdrawal
-Works better if patient has been drug free for 1 month or more

88
Q

Naloxone clinical pearls

A

-IV or intranasal administered
-Limited oral bioavailability
-Rapid onset
-Short half-life
-Give multiple shots to avoid return of respiratory depression
-Presence of fentanyl and other synthetic opioids means even more doses
-Repeat dose every 2-5 minutes if not conscious
-Causes strong withdrawal

89
Q

Symptoms of neonatal abstinence syndrome

A

-Tremors
-Yawning
-Poor feeding
-Sweating
-Serious withdrawal in the baby
-Seizures may also occur in babies born to methadone users
-Some symptoms can last as long as 4 to 6 months
-Opioids can also be present in the breast milk
-Some hospitals may have Newborn Abstinence Scores to help the diagnosis

90
Q

Onset of neonatal abstinence syndrome

A

Symptoms may begin 24 to 48hrs after birth or as late as 5 to 10 days

91
Q

What medications cause neonatal abstinence syndrome?

A

Heroin and other opiates, including methadone

92
Q

Non-pharmacological treatment for neonatal abstinence syndrome

A

-Swaddling
-Hypercaloric formula
-Frequent feedings
-Observation - sleep, temperature, weight gain/loss, and change in symptoms
-Rehydration - IV fluids dehydration is severe

93
Q

Pharmacological treatment of neonatal abstinence syndrome

A

-Morphine sulfate - oral morphine diluted to 0.4 mg/ml
-Sublingual buprenorphine
-Methadone - 0.05 to 0.1 mg/kg/dose every 6 hours
-Morphine and buprenorphine linked with shorter hospital stay than methadone
-Clonidine may also be useful

Therapeutics III (42 decks)

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