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Pharm 2024 > CNS Drugs: Opioids and Drugs of Abuse > Flashcards

CNS Drugs: Opioids and Drugs of Abuse Flashcards

Exam 4

1
Q

What are the 3 types of endogenous ligands?

A
  • Endorphins
  • Enkephalins
  • Dynorphins
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2
Q

What are the 2 types of neurons in hierarchical systems?

A

Relay neurons – relay signal to other parts of CNS
Circuit neurons – local, control

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3
Q

Relay neurons are _______. Which neurotransmitter(s) are included in this neuron type?

A

Excitatory (EPSP) - Glutamate and tachykinins

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4
Q

Circuit neurons are ________. Which neurotransmitter(s) are included in this neuron type?

A

Inhibitory (IPSP) – GABA, glycine, dopamine, and opioid peptides

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5
Q

What are the neurons included in the nonspecific (diffuse) systems?

A

NE, Dopamine, 5-HT, ACh

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6
Q

Diffuse activation is conducted by small, ___________ fibers

A

unmyelinated

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7
Q

ACh-secreting neurons have cell bodies located in the ______ and the _____, that project to the ______, _______, and _______

A

ventral telencephalon; pons
cerebrum, hippocampus, and thalamus

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8
Q

ACh secreting neurons can be linked to what 3 functions?

A
  • Learning and memory
  • Sleep wake cycles
  • Arousal and sensory information
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9
Q

What are the two components of pain?

A

Sensory and emotional

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10
Q

What are the 3 stimuli of pain?

A
  • Noxious chemical
  • Thermal
  • Mechanical
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11
Q

What are the 3 pathways of sensation transmission?

A
  1. Non-noxious mechanical stimulus (A beta) - all cutaneous mechanoreceptors, highly myelinated
  2. Noxious heat, mechanical stimuli (A delta) - sharp pain, initial reflex, highly myelinated
  3. Noxious chemical, heat, mechanical stimuli (C) - slow, burning pain, unmyelinated
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12
Q

What are the 2 methods of pain suppression?

A
  • Opioids – block pathway
  • Anti-inflammatory – suppress nociceptor signaling
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13
Q

What are the 2 pain pathways that respond to noxious chemicals?

A

Tissue damage – bradykinin
- Receptors – B1 (inflammatory) and B2 (constitutive)
- Activate PLA and PLC
AA Cascade – COX and LO - Prostaglandins

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14
Q

What is the most common opioid receptor subtype in the CNS?

A

μ (mu)

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15
Q

What are the 3 opioid receptor subtypes?

A

μ (mu), δ (delta), and Κ (kappa)

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16
Q

What is the medication that is a μ (mu) receptor antagonist?

A

naloxone (Narcan)

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17
Q

What are the 2 medications that are μ (mu) receptor full agonists?

A

morphine, fentanyl

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18
Q

What are the 2 medications that are μ (mu) receptor partial agonists?

A

codeine, oxycodone

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19
Q

What are the 5 functions of the μ (mu) opioid receptors?

A

Spinal analgesia, sedation, inhibition of respiration, slowed GI transit, modulation of hormone/NT release

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20
Q

μ (mu) receptors have the highest affinity to which endogenous opioid peptide?

A

endorphins

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21
Q

δ (delta) receptors have the highest affinity to which endogenous opioid peptide?

A

enkephalins

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22
Q

Κ (kappa) receptors have the highest affinity to which endogenous opioid peptide?

A

Dynorphins

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23
Q

What are the three pain tracts in the CNS? What are their main focuses?

A

Spinothalamic → primary pain pathway
Spinoreticular → emotional pain sensation
Spinomesencephalic → mu-opioid receptors

24
Q

Pharmacokinetics of opioids: absorption

A

Well absorbed (IM, SQ, Oral)
- Nasal, patch – avoid first pass effect
- Codeine: low 1st pass metabolism

25
Q

Pharmacokinetics of opioids: distribution

A

Highly perfused tissues – accumulation
- Brain, heart, kidney, liver
- Skeletal muscle – reservoir

26
Q

Pharmacokinetics of opioids: metabolism

A

Varied:
- Morphine – Phase II to active forms (M3G, M6G)
- Esters (heroin) – tissue esterases to morphine
- Other – Phase I (CYP3A4, CYP2D6)

27
Q

Pharmacokinetics of opioids: excretion

A

Mainly in urine

28
Q

What are the 3 opioid peptides?

A

enkephalins, endorphins, and dynorphin

29
Q

What is the MOA of opioids?

A
  1. Bind to receptors in brain and spinal cord
  2. Modulation of pain
  3. Receptor effects
    - Reduce neurotransmitter release (Glutamate, ACh, NE, serotonin, substance P)
    - Hyperpolarize postsynaptic neurons
30
Q

What are the 6 CNS effects of opioids?

A
  • Analgesia – sensory and emotional aspects
  • Euphoria (dysphoria)
  • Sedation
  • Respiratory depression - brainstem
  • Cough suppression
  • Miosis (always – marker)
31
Q

What are the CV effects of opioids?

A
  • Most have no direct effects
  • Bradycardia (CNS)
  • Meperidine (Demerol) - tachycardia
32
Q

What are the GI effects of opioids?

A

Constipation (ENS) – marked, no tolerance

33
Q

Which of the 2 side effects of opioids don’t change with tolerance?

A

miosis and constipation

34
Q

______ is an opioid antidiarrheal that only has CNS effects when given with _______

A

Loperamide (GI ABCB1)
Quinidine (ABCB1 inhibitor)

35
Q

List the 7 applications of opioids

A
  1. Analgesia
  2. ACS -MONA
  3. Acute pulmonary edema
  4. Cough
  5. Diarrhea
  6. Shivering
  7. Anesthesia
36
Q

What are the symptoms of opioid toxicity?

A
  • Dysphoric Reactions – Restlessness, tremor
  • Respiratory depression
  • Nausea and Vomiting
  • Increased intracranial pressure
  • Postural hypotension (worsened with hypovolemia)
  • Constipation
  • Urinary retention
  • Itch (parenteral)
37
Q

Differentiate between opioid tolerance, dependence and withdrawal

A

Tolerance - fairly rapid
Dependence - continuation despite negative effects, withdrawal symptoms if d/c’d
Withdrawal - Stems from Physical and Chemical dependence

38
Q

What are the symptoms of opioid withdrawal?

A
  • Rhinorhhea
  • Lacrimation
  • Yawning
  • Chills
  • Piloerection
  • Hyperventilation
  • Hyperthermia
  • Mydriasis
  • Muscle aches
  • N/V/D
  • Anxiety
  • Hostility
39
Q

______ is given for drug overdose

A

Naloxone (Narcan)

40
Q

_____ is given for alcohol withdrawal

A

Naltrexone

41
Q

Why should opioids be given sparingly in head injuries?

A

Opioids may enhance respiratory depression (lethal)

42
Q

Define Opioid Induced Hyperalgesia (OIH) and explain the mechanism

A

Increase pain sensation, distinct from original pain complaint that occurs in 30% of chronic use patients
Sensitization of muOR - MOR-1K (increases cAMP in cell)

43
Q

What is the treatment for Opioid Induced Hyperalgesia (OIH)?

A
  • Taper off opioids
  • Switch to alternative pathway (GABA analogs)
44
Q

What are the 3 structural classes of opioids?

A
  • Phenanthrenes
  • Phenylheptylamines
  • Phenylpiperidines
45
Q

What are the 3 Phenanthrenes that are strong opioid agonists?

A
  • Morphine, hydromorphone (Dilaudid)
  • Heroin (diacetylmorphine)
46
Q

What is the Phenylheptylamine that is a strong opioid agonist?

A

Methadone

47
Q

What are the 2 Phenylpiperidines that are strong opioid agonists?

A

Fentanyl and Meperidine (Demerol)

48
Q

Which opioid is the only opioid that causes tachycardia? How?

A

Meperidine (Demerol) - Antimuscarinic effects (tachycardia)

49
Q

What is the main use for Meperidine (Demerol)?

A

Post-op shivering

50
Q

What are the 2 cautions in administration of Meperidine (Demerol)?

A
  • Serotonin syndrome
  • Seizures - potentiate seizures for already exposed patients
51
Q

What are the 2 treatments for post-operative shivering?

A

Meperidine (Demerol) and Ondansetron

52
Q

What are the 3 Phenanthrenes that are moderate opioid agonists?

A
  • Codeine, oxycodone
  • More effective as combinations
    • Oxycodone + acetaminophen = Percocet
    • Oxycodone + Aspirin = Percodan
53
Q

What is the Phenylpiperidine that is a moderate opioid agonist?

A

Tramadol

54
Q

What are the 3 opioid antagonists?

A

Naloxone, naltrexone, naloxegol

55
Q

Buprenorphine (Buprenex) is a ______ agonist

A

partial

56
Q

Which partial opioid agonist can be used for post-op shivering?

A

Butorphanol (Stadol)

57
Q

What opioid can be used for cough suppression?

A

Dextromethorphan

Pharm 2024 (32 decks)

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