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CNS Drugs Flashcards

Test 4 (71 cards)

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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
Differentiate between the Spinothalamic, Spinoreticular, Spinomesencephalic tracts
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
26
What is the most common receptor target for opioids?
mu
27
Codeine is a _______ and is converted to _______
prodrug morphine **some morphine produced anytime you take codeine**
28
What is the function of the mu receptor subtype?
**Endorphins** spinal analgesia sedation slowed GI
29
What is the function of the kappa receptor subtype?
**Dynorphins** associated with negative psychosis effects
30
Describe opioid Pharmcokinetics
Significant 1st pass effects highly perfused in tissues (esp. skeletal) excreted in urine
31
Which opioid has a high PO bioavailability?
Codeine
32
Describe Morphine metabolism
Uses phase 2 converts to more active forms: M3G, M6G
33
Heroin metabolizes to ______ with _______ enzyme
morphine tissue esterase
34
What enzymes are mostly used in phase 1 metabolism?
CYP3A4 CYP2D6
35
What is the MOA in opioids?
**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
What the effects of opioids on the CNS? What is the marker symptoms?
Analgesia euphoria sedation respiratory depression cough suppression **miosis <-- MARKER**
37
T/F: Miosis isn't always present in exogenous opioids
F always present
38
What are CV and GI effects with opioids?
Bradycardia Constipation
39
Meperidine (Demerol) causes ______cardia
tachy
40
What are the things we should assess with pain?
1, What's causing it? (Pathology) 2. Pt history 3. Duration of pain
41
Opioids are more effective for ______ pain
severe, constant/chronic
42
Why would we need to use opioids in infants?
Renal or biliary colic
43
What is the acronym for Acute coronary syndrome?
**For MI & Angina** MONA Morphine Oxygen Nitoglycerin Aspirin
44
Describe Tx for Acute Pulomary Edema
**Sometimes anxiety induced** Giving an opioid MOA: - reduce anxiety - reduce preload & after load **Give lasix alt therapy**
45
What as signs of opioid toxicity?
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
Differentiate between tolerance and dependence in opioids
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
What causes addiction?
Increased tolerance + dependence
48
What system does addiction activate?
Dopamine mesolimbic system
49
How does tolerance happen?
-Receptor phosphorylation -Uncoupling of G-proteins -cAMP -internalization
50
What has no degrees to tolerance (immune to tolerance)?
Miosis Constipation Seizures Nalaxone
51
Describe Opioid Induced Hyperalgesia
(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
You should avoid ____ in head injuries
opioids
53
_____ is for opioid overdose & _____ is for alcohol withdrawal
Nalaxone (Narcan) Naltrexone
54
What are the 3 structures associated with opioids?
Phenanthrenes Phenylheptylamines Phenylpiperidines
54
T/F: Opioids during pregnancy has no lasting effects
F Can cause fetal dependence
55
What opioids are Phenanthrenes?
Morphine Dilaudid Codeine Oxycodone Percadan/Percoce
56
Which opioids are Phenylheptylamines?
Methadone
57
Which opioids are Phenylpiperidines?
Fentanyl Meperidine (Demerol) Tramadol
58
Drugs: Morphine, Hydromorphone (Dilaudid)
Class: Opioid -Strong agonist -Phenanthrenes Uses: Severe pain **Dilaudid works 5x stronger than morphine**
59
Drugs: Methadone
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
What drug is used for Heroine rehab?
Methadone
61
Drugs: Fentanyl, Meperidine
Class: Opioid -Strong agonist -Phenylpiperidines Fentanyl: 100x more potent than morphine meperidine: causes tachycardia - neg. inotrope -**major use for post op shivering**
62
What drugs are used for post op shivering? Why do we need to reduce this?
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
Drugs: Codeine, Oxycodon, Percadan/Percocet
Class: Opioid -Moderate agonist -Phenanthrenes More effective as combinations Oxycodon + Acetaminophen = Percocet Oxycodon + aspirin = Percodan
64
What is a Percocet?
Oxycodon + Acetaminophen
65
What is a Percodan?
Oxycodon + aspirin
66
Drugs: tramadol
Class: Opioid -Moderate agonist -Phenylpiperidines **Also has SNRI activity** Makes you happier Is a racemic mixture
67
Drugs: Buprenorphine
Class: Opioid -Partial agonist Uses: Opioid abuse
68
Drugs: Butorphanol
Class: Opoid -Partial agonist Uses: post op shivering
69
Drugs: Dextromethorphan
Class: Opioid -Weak agonist Uses: Cough (Antitussive)
70
Drugs: Naloxone, Naltrexone, Naloxegol
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)

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