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Pharm > CNS Drugs > Flashcards

CNS Drugs Flashcards

Test 4

1
Q

What are opioids used for?

A

Pain relief
Antianxiety
sedation

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2
Q

List the endogenous opioids and their subtypes. Which opioids favor which subtype?

A

Endogenous opioids:
-Endorphins
-Enkephalins
-Dynorphins

Mu: Endorphins >

Delta: Enkephalins >

Kappa: Dynorphins>

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3
Q

What are your neuron types? what is the neurotransmitter associated with this?

A
  1. Relay (Excitatory) neurons: Glutamate
  2. Circuit (Inhibitory) neurons: GABA & Glycine
    – considered negative feed-forward or feedback
    -“axoaxonic”
  3. Monoamine neurotransmission: NE, Dopamine, 5-HT
  4. Slow conduction (Slow pain)
    –en passant synapses
    -small lightly myelinated or unmyelinated fibers
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4
Q

Where is dopamine released from?

A

Substantia nigra & ventral tegmental area

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5
Q

Where is NE released from?

A

Locus coeruleus

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6
Q

Where is Serotonin released from?

A

Raphe Nuclei

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7
Q

What is Alzheimer’s linked to?

A

Deterioration of the system the spreads Ach it includes: Pontine nuclei, Fornix, & cingulate gyrus

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8
Q

Where is Ach produced?

A

Pontine nuclei

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9
Q

What do tachykinins work on?

A

Substance P receptor on the pain signaling pathway

It is EXCITATORY

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10
Q

What neurotransmitters are amino acids?

A

GABA
Glycine
Glutamate

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11
Q

What neurotransmitters are Peptides?

A

Opioid peptides
Tachykinins

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12
Q

What neurotransmitters are monoamines?

A

Serotonin
NE
Dopamine

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13
Q

What neurotransmitter is a choline ester?

A

Ach

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14
Q

Which neurotransmitters are a part of the hierarchal vs diffuse?

A

hierarchal:
GABA
Glycine
Glutamate
Opioid peptides
Tachykinins

diffuse:
Ach
Serotonin
NE
Dopamine

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15
Q

What are the 2 components of pain?

A

Sensory
emotional

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16
Q

pain causes an _______ which means we want to do something about it

A

affective sensation

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17
Q

What are the causes of pain?

A

Noxious chemical
thermal
mechanical

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18
Q

Describe pain receptors

A

“Free nerve endings” –> “nociceptors”

At the beginning of these receptor that are Leukotriene-R, prostaglandin-R, Serotonin-R, etc

They all have different neurochemical markers

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19
Q

Describe low-threshold mechanoreceptors

A

allows foe fine tune movements when grazed

–not used for pain–

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20
Q

Where is pain processed?

A

Somatosensory cortex

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21
Q

What type of fiber is used for pressure, fast pain, & slow pain?

A
  1. pressure: A-beta fiber: highly myelinated
  2. fast pain: A-delta fiber: highly myelinated
  3. slow pain: C fiber: unmyelinared
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22
Q

Compare C & A fibers

A

A-fibers: Large; can suppress pain signaling (both fast pain on A-delta fibers with pressure & slow pain on C-fibers)

C-fibers: small; can overcome suppression by A-fibers if pain is strong enough

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23
Q

What neurotransmitters cause pain in relation to the “noxious chemicals” when there is tissue damage? Explain this process

A

Bradykinin
Prostaglandins
Cytokines

Tissue damage –> release of WBC (Mast cells, Neutrophils, macrophages) –> degranulation –> Bradykinin & Activated AA –> COX –> PG

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24
Q

Which bradykinin receptor is inflammatory?

A

B1

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25
Q

Differentiate between the Spinothalamic, Spinoreticular, Spinomesencephalic tracts

A

Spinothalamic: Primary
-Spinal cord -> medulla - pons -> synapses at thalamus - ends at somatosensory cortex

Spinoreticular: Emotional pathway
-Passes through reticular formation of the pons -> ends in the somatosensory cortex

Spinomesencephalic: Pain suppression pathway
-Doesnt completely suppress all the pain
-Terminates at the periaqueductal gray matter

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26
Q

What is the most common receptor target for opioids?

A

mu

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27
Q

Codeine is a _______ and is converted to _______

A

prodrug

morphine

some morphine produced anytime you take codeine

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28
Q

What is the function of the mu receptor subtype?

A

Endorphins

spinal analgesia
sedation
slowed GI

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29
Q

What is the function of the kappa receptor subtype?

A

Dynorphins

associated with negative psychosis effects

30
Q

Describe opioid Pharmcokinetics

A

Significant 1st pass effects

highly perfused in tissues (esp. skeletal)

excreted in urine

31
Q

Which opioid has a high PO bioavailability?

32
Q

Describe Morphine metabolism

A

Uses phase 2

converts to more active forms: M3G, M6G

33
Q

Heroin metabolizes to ______ with _______ enzyme

A

morphine

tissue esterase

34
Q

What enzymes are mostly used in phase 1 metabolism?

A

CYP3A4
CYP2D6

35
Q

What is the MOA in opioids?

A

GCPR: G(i) -> decreases cAMP:

  1. Mu-Opioid-R on postsynapse is coupled to a K+ ion channel & depolarizes the cell
  2. MOR on presynapse: prevents Ca++ entry into the cell which prevents exocytosis of excitatory neurotransmitters
    -prevents pain stimuli from progressing
36
Q

What the effects of opioids on the CNS? What is the marker symptoms?

A

Analgesia
euphoria
sedation
respiratory depression
cough suppression
miosis <– MARKER

37
Q

T/F: Miosis isn’t always present in exogenous opioids

A

F

always present

38
Q

What are CV and GI effects with opioids?

A

Bradycardia

Constipation

39
Q

Meperidine (Demerol) causes ______cardia

40
Q

What are the things we should assess with pain?

A

1, What’s causing it? (Pathology)
2. Pt history
3. Duration of pain

41
Q

Opioids are more effective for ______ pain

A

severe, constant/chronic

42
Q

Why would we need to use opioids in infants?

A

Renal or biliary colic

43
Q

What is the acronym for Acute coronary syndrome?

A

For MI & Angina

MONA

Morphine
Oxygen
Nitoglycerin
Aspirin

44
Q

Describe Tx for Acute Pulomary Edema

A

Sometimes anxiety induced

Giving an opioid MOA:
- reduce anxiety
- reduce preload & after load

Give lasix alt therapy

45
Q

What as signs of opioid toxicity?

A

Dysphoric reactions (restlessness, tremors)
Respiratory depression
N/V
Increased ICP
postural hypotension
constipation
urinary retention
itch (associated w/ mast cell degranulation caused by opioids)

46
Q

Differentiate between tolerance and dependence in opioids

A

tolerance: happens rapidly –> leads to dependence
-needing more to have the same effects as before

dependence: continuing to take despite negative effects
-stopping will cause withdrawal symptoms

47
Q

What causes addiction?

A

Increased tolerance + dependence

48
Q

What system does addiction activate?

A

Dopamine mesolimbic system

49
Q

How does tolerance happen?

A

-Receptor phosphorylation
-Uncoupling of G-proteins
-cAMP
-internalization

50
Q

What has no degrees to tolerance (immune to tolerance)?

A

Miosis
Constipation
Seizures
Nalaxone

51
Q

Describe Opioid Induced Hyperalgesia

A

(OIH)

Increased pain sensation from original pain

MOA: sensitization/mutation in MOR -> increases in cAMP & increases in excitatory neurotransmitters

Tx: taper off opioids & with to GABA analogs (antiseizure meds)

52
Q

You should avoid ____ in head injuries

53
Q

_____ is for opioid overdose & _____ is for alcohol withdrawal

A

Nalaxone (Narcan)

Naltrexone

54
Q

What are the 3 structures associated with opioids?

A

Phenanthrenes
Phenylheptylamines
Phenylpiperidines

54
Q

T/F: Opioids during pregnancy has no lasting effects

A

F

Can cause fetal dependence

55
Q

What opioids are Phenanthrenes?

A

Morphine
Dilaudid
Codeine
Oxycodone
Percadan/Percoce

56
Q

Which opioids are Phenylheptylamines?

57
Q

Which opioids are Phenylpiperidines?

A

Fentanyl
Meperidine (Demerol)
Tramadol

58
Q

Drugs: Morphine, Hydromorphone (Dilaudid)

A

Class: Opioid
-Strong agonist
-Phenanthrenes

Uses: Severe pain

Dilaudid works 5x stronger than morphine

59
Q

Drugs: Methadone

A

Class: Opioid
-Strong agonist
-Phenylheptylamines

Uses: Chronic pain
-if you have a tolerance to morphine
-to help people get off heroine

ADME: CYP3AP phase 1
half life: 25-50 hours
duration: 4-6 hours

60
Q

What drug is used for Heroine rehab?

61
Q

Drugs: Fentanyl, Meperidine

A

Class: Opioid
-Strong agonist
-Phenylpiperidines

Fentanyl: 100x more potent than morphine

meperidine: causes tachycardia
- neg. inotrope
-major use for post op shivering

62
Q

What drugs are used for post op shivering? Why do we need to reduce this?

A

Meperidine (Demerol)
Ondansetron (Zofran): 5-HT3 antagonist
Butorphanol

Post op shivering decreases healing where you need to heal at because O2 is being used up by shivering

63
Q

Drugs: Codeine, Oxycodon, Percadan/Percocet

A

Class: Opioid
-Moderate agonist
-Phenanthrenes

More effective as combinations

Oxycodon + Acetaminophen = Percocet

Oxycodon + aspirin = Percodan

64
Q

What is a Percocet?

A

Oxycodon + Acetaminophen

65
Q

What is a Percodan?

A

Oxycodon + aspirin

66
Q

Drugs: tramadol

A

Class: Opioid
-Moderate agonist
-Phenylpiperidines

Also has SNRI activity
Makes you happier

Is a racemic mixture

67
Q

Drugs: Buprenorphine

A

Class: Opioid
-Partial agonist

Uses: Opioid abuse

68
Q

Drugs: Butorphanol

A

Class: Opoid
-Partial agonist

Uses: post op shivering

69
Q

Drugs: Dextromethorphan

A

Class: Opioid
-Weak agonist

Uses: Cough (Antitussive)

70
Q

Drugs: Naloxone, Naltrexone, Naloxegol

A

Class: Opioid antagonist

Uses: naloxone:opioid overdose
-naltrexone: alcohol withdrawal
-naloxegol: Increase GI motility when taking opioid

Short duration

Little effect in the absence of agonist (wont do anything if there’s nothing in your system)

Pharm (30 decks)

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