Pharm 2025 > Opioids > Flashcards

Opioids Flashcards

(54 cards)

Study These Flashcards
1
Q

List endogenous opioids

A

Endorphins
Enkephalins
Dynorphiins

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2
Q

Endorphin target

A

μ (mu)

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3
Q

Enkephalins target

A

δ (delta)

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4
Q

Dynorphins Target

A

Κ (kappa)

Effect- Dec Gi transit

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5
Q

Relay neurons

A

Signal to other parts fo CNS can use EPSP- glutamate

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6
Q

Nonspecific (Diffuse) Neuron System

A

NE, Dopaine, 5-HT released by neuclei= diffuse activation (slower)

Non-hierarchyactic- acts in diff areas of brain

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7
Q

Components fo pain

A

Sensory
Emotional

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8
Q

Opioid Peptides

A

Mu, Delta, Kappa receptors= inhibitory (prevent pain signaling in somatosensory cortex)

hierarchical system

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9
Q

Three fibers for transmission of sensation

A

1) Nociceptors- free nerve endings pain receptors

A(Beta) fibers- light touch (fast)
A(delta)- fast pain
C fiber- slower pain

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10
Q

Hierarchical System

A

Neurons- relay & circuit neurons

(Neuron to Neuron)

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11
Q

Circuit Neurons

A

Local control

(IPSP)= GABA, Glycine
Negative feed forward or feedback
Axoaxonic- interacts w axon

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12
Q

ACh in CNS

A

Diffuse system= memory, sleep, sensory information

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13
Q
A
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14
Q

What is released during tissue damage? What do they activate?

A

Bradykinin, Arachidonic acid - prostaglandins

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15
Q

Noxious Chemicals

A

Tissue damage – bradykinin
Receptors – B1 (inflammatory) and B2 (constitutive)
Activate PKA and PKC

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16
Q

Affective Sensation? Travels through what tracts?

A

Want to do something about

Sphinothalamic vs Spinorecticular

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17
Q

Spinoreticular allows us to ID what?

A

Travels through reticular formation of the pons=

Location of pain; slower

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18
Q

Spinothalamic

A

Pain- spinal cord neuron- reflex arch- thalamus- post-central gyrus

Fastest travel of pain

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19
Q

Spinomesencephalic pathway

A

Familiarization of pain; rich in μ (mu)

goes through PAG (DIC pathway)- endorphins & enkephalins

(gate theory)

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20
Q

Full agonist: μ (mu)

A

Morphine
Fentanyl

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21
Q

Partial Agonsit : μ (mu)

A

Codeine & Oxycodone

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22
Q

Antagonist : μ (mu)

23
Q

Opioid Pharmcokinetics

Study These Flashcards
A

A: Well absorbed–

D: Highly perfused in tissues- accumulation

M: Varies

E: Mainly Urine

24
Q

Which opioid drug has a low 1st pass metabolism?

Study These Flashcards
A

Codeine (Prodrug- activated to morphine as active drug)

25
Morphine metabolism
Phase II to active forms
26
Opioid MOA
Bind to receptors in brain & spinal cord= hyper polarize postsynaptic neurons Dec neurotransmitter release--> Glutamate, ACh, NE, serotonin, Substance P
27
Normal μ (mu) pathway ?
μ (mu)= GPCR = G(i) = dec cAMP= block Ca channels= activates K channels to hyper polarize cell= suppress add NT release
28
G protein independent signaling of μ (mu) causes?
Additional G-protein independent things that are activated= cause side effects of opioids
29
Opioid system effects- CNS
Analgesia Miosis (ALWAYS) Euphoria or dysphoria Sedation, Resp depression Cough suppression Constipation
30
What can meperidine cause?
Tachycardia
31
Loperamide CNS effects?
Opioid- antidiarrheal Typically No CNS effects Given w quinidine then ABCB1 Inhibitor = may have CNS effect
32
Opioid Toxicity
Resp Depression Dysphoric Rx N/V Inc intracranial pressure Hypotension Constipation Itch
33
Opioid Tolerance
Related to desensitization response; need more when on long term therapy
34
Dependence
Withdrawal symptoms; r/t dopamine mesolimbic system
35
What 3 things can tolerance not be associated with?
Constipation, Meiosis, Convulsion , Naloxone/Naloxegol
36
Withdrawal s/s
HTN, mydrasis, Anxiety, Hostility Yawning, hyperventilation
37
Opidoid Induced Hyperalgesia; MOA?
Inc pain sensation; distinct from original pain complaint MOA: 1) Sensitization of mu- opioid receptor (no long signaling) 2) MOR-1K- splice variant muOR- inc cAMP in cell
38
Tx OIH?
Taper off opioids Alt. pain pathway - GABA analogs
39
3 classes of Opoids
Phenanthrenes Phenylheptylamines Phenylpiperidines
40
Phenanthrenes- Strong Agonist Ex? Use?
Morphine, Hydromorphone Heroin Use- severe pain
41
Phenylheptylamines- Agonist? Use? Half life?
Methadone Use- Chronic pain; opioid abuse Shorter duration analgesia; long half life
42
Phenylpiperidine- Strong Agonist?
Fentanyl Meperidine (Demerol)
43
Meperidine- Use? MOA? Can Induce?
MOA- antimuscarinic effects Use- Post-op shivering Induce- Serotonin syndrome, seizures
44
Carfentanil- elephant tranquilizer
45
Post-op shivering Causes
Cool OR IV fluids Paralytic- inhibition of muscle movement
46
Shivering is an issue why?
Inc O2 consumption by 500%
47
Tx for post-operative shivering
Meperidine- inc K-opioid, serotonergic effect Ondansetron - 5-HT3 antagonist
48
Moderate Agonists- Phenanthrenes
Codeine, oxycodone Oxy + aspirin = percodan Oxy + Acetaminophen= percocet
49
Phenylpiperidines- Moderate Agonist
Tramadol- SNRI activity; safer Loperamide
50
Partial Agonists opioid? Use for what tx?
Buprenorphine (Buprenex) Tx for Opioid abuse Butorphanol (Stadol)= Tx post-op shivering
51
Cough opioid drug ?
Dextromethorphan
52
Opioid antagonists?
Derivatives of morphine- Naloxone, Naltrexone, naloxegol Effects in 1-3 min & short duration; little effect in absence of agonist
53
Normal Opioid CV effects
Usually bradycardia ; no direct effects
54
Opioid Use Cautioned in what type of patients?
Head injuries, Prego, Impaired Pulmonary function
Pharm 2025
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