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Pharmacology - Fall 2024 > Opioids > Flashcards

Opioids Flashcards

1
Q

What are the two opioid antagonists? What are their uses?

A

Naloxone - Overdose antidote (short duration, supportive therapy still needed)
Naltrexone - EtOH abuse.

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2
Q

What is Buprenorphine used for?

A

Opioid abuse (partial agonist)

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3
Q

What is Dextromethorphan’s use?

A

Anti-tussive

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4
Q

Which phenanthrenes are moderate agonists & more useful with acetaminophen or aspirin?

A

Oxycodone & codeine

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5
Q

How much can shivering increase O₂ consumption?
By what mechanism does meperidine treat shivering?

A

500%
↑ kappa receptor agonism & serotonergic effects.

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6
Q

What is the most potent fentanyl derivative?

A

Carfentanil (10,000:1 morphine ratio)

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7
Q

What is the primary use of Meperidine?
What cardiac effects are seen with it?

A

Post-op shivering
neg inotrope, + chronotrope

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8
Q

What is methadone’s usefulness?
Why is this?

A

Suppression of opioid withdrawal symptoms (and chronic pain)
Long Half-Life = 25-50 hours

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9
Q

What is heroin used for in the UK?

A

Palliative Care

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10
Q

What structure is indicated in the figure below?
What types of opioids are associated with this structure?

A

Phenylpiperidine
Fentanyl & Meperidine

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11
Q

What structure is indicated in the figure below?
What opioids are seen with this structure?

A

Phenylheptylamine
Very strong (Methadone)

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12
Q

What structure is indicated in the figure below?
What strength is typically seen with these opioids?

A

Phenanthrene
Very strong (morphine, hydromorphone, heroine)

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13
Q

What can occur when opioids are given to a pregnant mother?

A

Fetal Dependence

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14
Q

Why are opioids partially contraindicated in head injuries?

A

↑ Resp depression

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15
Q

What is the treatment for opioid induced hyperalgesia?

A

Wean opioid
GABA analogs

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16
Q

What is the mechanism for opioid induced hyperalgesia?

A

Sensitization of MuOR-1K variant & ↑cAMP

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17
Q

What is opioid induced hyperalgesia?
How many patients will experience this?

A

Increased pain response secondary to chronic use
30% of chronic users develop this

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18
Q

What symptoms would be seen in severe opioid withdrawal?

A

Mydriasis
Hyperthermia
N/V/D
Anxiety/Hostility

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19
Q

What mild symptoms might be seen from opioid withdrawal?

A

Piloerection
Hyperventilation
Lacrimation
Rhinorrhea
Yawning

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20
Q

How quickly does opioid tolerance build?
What is the probable mechanism for this?

A

Rapidly
β-arrestin pathway

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21
Q

What drug is indicated for post-operative shivering?

A

Demerol (meperidine)

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22
Q

Why is morphine used in Acute Coronary syndrome?

A

↓ anxiety
↓ HR (and thus metabolic demand)
↓ pain

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23
Q

What is the treatment for Acute Coronary Syndrome?

A

Morphine
Oxygen
Nitroglycerin
Aspirin

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24
Q

What drug can cause respiratory depression when given with loperamide?
Why?

A

Quinidine
Blocks ABCB1 so loperamide accumulates and affects CNS.

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25
Q

What does Loperamide do? Why?

A

Antidiarrheal opioid with no CNS effects due to GI ABCB1 clearance.

26
Q

Is tolerance developed to the constipatory effects of opioids?

A

No

27
Q

What effects may opioids have on the cardiovascular system?
What is the exception?

A

Indirect CNS bradycardia
Meperidine (Demerol) has antimuscarinic traits = ↑HR.

28
Q

What symptom of opioid organ system effects is always present with opioid use & no tolerance develops to it?

A

Miosis (pupillary constriction)

29
Q

Which opioid receptors are responsible for analgesia?
Which opioid receptor is responsible for CNS respiratory depression & dependence/addiction?

A

Mu, delta, & kappa.
Mu

30
Q

What opioid pathway leads to decreased effect & opioid tolerance?

A

G-protein independent pathway with ERK, JNK & β-arrestin.

(ERK = E receptor Kinase, JNK = Janus Kinase)

31
Q

How do μ(mu) opioid receptors suppress pain?

A

Gᵢ = ↓AC → ↓cAMP = ↑pK⁺, ↓pCa⁺⁺ = Hyperpolarized neuron.

32
Q

Where are mu opioid receptors located on neurons?

A

Pre-synaptic & post-synaptic neurons

33
Q

What type of receptor are opioid receptors?

A

Gᵢ GPCRs

34
Q

What mediator is utilized with κ(kappa) receptors?

A

Dynorphins

35
Q

Differentiate full agonist, partial agonists, & antagonists of the opioid receptors. Give examples for each.

A

Full Agonists (strong to moderate effect) morphine, fentanyl, etc.
Partial Agonists (moderate to mild effect) codeine, oxycodone, etc.
Antagonists (Reversal) Naloxone

36
Q

What are the other opioid receptors aside from μ(mu) opioid receptors?

A

δ(delta) & κ(kappa) receptors.

37
Q

What is the primary opioid and endogenous ligand receptor?
What endogenous ligands are used by this receptor?

A

μ(mu) opioid receptors
Endorphins

38
Q

Which spinal tract is suppressive to painful stimuli?

A

Spinomesencephalic through μ(mu) opioid receptors in the periaqueductal gray matter.

39
Q

What are the three pain tracts of the CNS (discussed in lecture)?

A

Spinothalamic
Spinoreticular
Spinomesencephalic

40
Q

What mediators of pain (discussed in lecture) are released in response to tissue damage?

A

Bradykinin
Prostaglandins
Glutamate
Substance P

41
Q

What fiber type can suppress fast pain?

A

Aβ through suppression of Aδ fast pain.

42
Q

Most pain receptors are _____ ______ endings.

A

free nerve

43
Q

Is most pain signaling hierarchical or diffuse?

A

Hierarchical

44
Q

Tachykinins use _________ __ receptors and have a __________ effect on pain signaling.

A

Substance P; excitatory

45
Q

What CNS effects does ACh have?

A

Learning & Memory
Sleep-wake cycles
Arousal & sensory information

46
Q

Which area of the brain is associated with ACh diffusion?
What neurotransmitter does ACh have a similarity to in the CNS?

A

Pontine Nuclei
Serotonin/Melatonin

47
Q

Which diffuse system area of the brain is associated with NE?

A

Locus Coeruleus

48
Q

Where is dopamine produced?

A

Substantia Nigra & Ventral Tegmental Area

49
Q

Where is serotonin produced?

A

Raphe Nuclei

50
Q

How do non-specific, diffuse systems differ from relay systems?

A

Monoamine Transmitters used (NE, Dop, 5-HT)
Slower
Diffuse throughout the CNS. (en-passant synapses used)

51
Q

How does an axoaxonic interaction differ from a feedback or feed-forward neuron interaction?

A

Inhibition/excitation occurs at the axon rather than the neuron body.

52
Q

Are feed-forward & feed-back systems inhibitory or excitatory?

A

They can be both.

53
Q

Explain the mechanism of a feed-forward response.

A

Neuron A excites an interneuron which then inhibits Neuron

54
Q

Explain the mechanism of a feed-back response.
What is the purpose of this system?

A

Excitatory neuron depolarizes an inhibitory interneuron which suppresses the initial excitatory neuron.
Seizure prevention from constant excitatory stimulation.

55
Q

What specific type of neuron is pertinent to feed-forward & feed-back responses in relay systems?

A

Interneurons

56
Q

What are hierarchical systems?

A

Multiple Neurons linked to one another for signaling.

57
Q

What are the three endogenous ligands pertinent to pain signaling?

A

Endorphins (1°)
Enkephalins (pain signaling)
Dynorphins (pain signaling)

58
Q

Naloxegol

A
  • Opioid antagonist
  • derivative of morphine
  • naloxegol (gut)
59
Q

tramadol

A

Phenylpiperidines classification
- has SNRI activity
- racemic mixture
- safer alternative

considered moderate agonist.

60
Q

percadan/percocet

A

oxycodone + acetaminophen = percocet

oxycodone + aspirin = percodan

these combination are said to be more effective than codeine & oxycodone alone. (phenanthrenes)

61
Q

dilaudid

A

Hydromorphone (phenanthrenes)

strong agonist for severe pain

Pharmacology - Fall 2024 (10 decks)

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