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TxWes Spring '25: Anesthesia Pharm > Pain & Opioids Exam 2 > Flashcards

Pain & Opioids Exam 2 Flashcards

1
Q

What are opioids effects on the CO₂ medullary center?

A

Opioids inhibit the CO₂ medullary center.

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2
Q

Differentiate opioids from narcotics.

A
  • Opioids: all exogenous substances that bind to endogenous opioid receptors.
  • Narcotic: any substance that can produce physical dependence (stupor).
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3
Q

What two types of opioid chemical structures are there?

A
  • Phenanthrenes
  • Benzylisoquinolines
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4
Q

What types of drugs are Phenanthrenes? What types of drugs are benzylisoquinolines?

A

Phenanthrenes: Morphine, codeine, thebaine
Benzylisoquinoline: Papaverine, noscapine

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5
Q

What is papaverine mostly used for?

A

Treating intra-arterial barbiturate administration (dilates the highly constricted artery).

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6
Q

What portions of the brain are the source of descending inhibitory signals? (3)

A
  • Periaqueductal gray (PAG)
  • RVM
  • Dorsal horn
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7
Q

What endogenous substances have the same effect as opioids?

A
  • Endorphins
  • Enkephalins
  • Dynorphines
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8
Q

Presynaptic inhibition of what neurotransmitters occurs with opioid administration?

A
  • ACh
  • Dopamine
  • NE
  • Substance P
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9
Q

How do opioids modulate pain at the cellular level?

A
  • Agonizes opioid receptors in pre/post synapse
  • hyperpolarization of cells
  • decreased neurotransmission (ACh, NE, dopamine, Substance P)
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10
Q

Where are opioid receptors located in the brain?

A
  • PAG
  • Locus Coeruleus
  • RVM (rostral ventral medulla)
  • Hypothalamus
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11
Q

Where is the primary site of opioid receptors in the spinal cord?

A
  • interneurons
  • Substantia gelatinosa (aka Laminae 2)
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12
Q

Where is/are opioid receptors found outside the CNS?

A
  • Sensory neurons
  • immune cells
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13
Q

What are the four (most important) types of opioid receptors?

A
  • Μu1 (μ₁)
  • Μu2 (μ₂)
  • Κappa (κ)
  • Delta (δ)
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14
Q

Which opioid receptor(s) is/are responsible for respiratory depression & physical dependence?

A
  • Μu2
  • delta δ
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15
Q

Which receptors are responsible for constipation?

A

Mu 2 > delta

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16
Q

Which receptors can cause urinary retention? Are there any receptors that cause diuresis when bound?

A
  • Retention: Μu1 and delta δ
  • Diuresis: Kappa κ
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17
Q

All opioid receptors induce analgesia at both the brain and the spinal cord. T/F?

A

False
Μu2 receptors only cause analgesia at the spinal cord level.

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18
Q

What opioid receptors have low abuse potential when bound?

A
  • Μu1
  • Kappa κ
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19
Q

Which opioid receptor is responsible for euphoria, bradycardia, hypothermia, and miosis when bound?

A

Mu1

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20
Q

What agonists bind to each of the four opioid receptors?

A
  • Mu1 & Mu2 = endorphins, morphine, synthetics.
  • κ = dynorphins.
  • δ = enkephalins.
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21
Q

Describe the adverse side effects of opioids on the cardiovascular system.

A
  • ↓BP, venous return, and CO
  • ↓HR or histamine release = ↓BP
  • +N2O or benzo = CV depression
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22
Q

What possible cardiovascular benefits do opioids provide?

A

Myocardial ischemia protection (decrease oxygen demand)

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23
Q

What are the respiratory effects of opioids? What would symptoms of overdose be?

A

Depressed CNS response to CO₂ causing a right shift of PaCO₂ (↑)
Overdose = apnea, miosis, coma

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24
Q

What drug is given to treat apnea from opiod overdose?

A
  • Physostigmine
  • inhibits acetylcholinesterase
  • increased ACh levels
  • reverses ventilatory depresson but not analgesia
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25
What would cause a leftward shift in PaCO₂? What would cause a rightward shift?
Leftward: **Metabolic acidosis** (to breathe off all that CO₂) Rightward: **sleep**, **opiates**, **anesthesia**
26
Why should caution be used when administering opioids to **head trauma** patients?
Opioids ↓CBF and possibly ICP
27
What **musculoskeletal** abnormality occurs with opioid administration? What makes this condition worse? How is it treated?
* **Skeletal chest wall and abdominal muscle rigidity**. * Mechanical ventilation * **Muscle relaxants and/or naloxone**
28
What are sphincter of Oddi spasms? Which drugs can cause this?
**Biliary smooth muscle spasm** * Fentanyl (99%) * Morphine (53%) * Meperidine (61%)
29
How are opioid-induced **sphincter of Oddi spasm’s** treated?
* **Naloxone 40 mcg** * **Glucagon (2mg IV given incrementally)** and causes no opioid antagonism. * **atropine 0.2 mg** * **nalbuphine 10 mg** * **NTG 50 mcg**
30
What drugs should be used for ERCP cases?
Non-opioids (multimodal approach w/ NSAIDs, gabapentin, etc.)
31
How long does it take (generally) to develop tolerance to opioids? What causes tolerance?
* **2-3 weeks** * **morphine = 25 days** * Downregulation (desensitized and **decreased number of opioid receptor**)
32
What is the dosage of morphine? When does it peak? How long does it last?
* 1 - 10 mg IV * Peak: 10 - 20 minutes * Duration: 4-5 hours
33
How is morphine **metabolized**? What is the active metabolite and its significance?
* **Glucuronic acid** conjugation in the liver * **Morphine-6-glucuronide** = active analgesic causing late resp depression
34
What would occur with morphine overdose in a **renal failure** patient?
Prolonged ventilatory depression.
35
What receptors does **meperidine** agonize?
* μ and κ receptors * α2 receptors as well
36
What are the **analogues** of **meperidine**? What other drugs does meperidine have a similar organic structure to?
* Fentanyl & it’s derivatives * **Lidocaine** & **Atropine**
37
How potent is Meperidine? How long does it last?
10% as potent as morphine Duration: 2-4 hours
38
What is the **primary indication** for **meperidine**? What dose is used?
**Post-operative shivering** **12.5mg IV**
39
When should meperidine not be used?
**Bronchoscopies** (promotes coughing)
40
How potent is fentanyl?
75 - 125 x morphine.
41
What is the **blood-brain equilibration** of fentanyl?
**6.4 minutes** Potent with rapid onset and ↑ lipid solubility.
42
What percent of fentanyl is subject to **lung first-pass effect**?
* **75%** * **Reservoir** for drug * results in decreased amount of active drug
43
Where is fentanyl metabolized?
Liver via CYP3A Principal metabolite: Norfentanil.
44
How does fentanyl dosing change for the **elderly** or **liver cirrhosis**?
**No change** in elderly or cirrhotic patients.
45
Describe what the graph below is showing.
**Fentanyl** has the greatest **context-sensitive half-time** of any of the fentanyl derivatives.
46
What is the analgesia dosage of fentanyl? Induction dose?
Analgesia: **1-2 mcg/kg IV** Induction: **1.5-3 mcg/kg IV**
47
1mg of PO fentanyl is equivalent to?
5mg IV morphine
48
What is the **intrathecal** dosage of fentanyl?
25 mcg
49
What is the adult transmucosal dose of fentanyl?
Adult: 5 - 20 mcg/kg Pediatric: 15 - 20 mcg/kg
50
What is the transdermal dose of fentanyl?
75 - 100 μg (18 hours steady delivery)
51
What is the fentanyl dose as **adjunct** with **volatile anesthetics**?
2-20 mcg/kg IV
52
What the side effects of fentanyl?
* ↓BP & ↓CO * Can cause seizures * modestly increase ICP
53
How much more potent is **sufentanil** than fentanyl?
5-12 times more potent.
54
How much of sufentanil is subject to lung first pass effects?
60%
55
How much of sufentanil is protein bound? What protein is it bound to?
**92.5%** **α-1 acid glycoprotein bound**
56
What is the analgesia dose of sufentanil?
Analgesia: 0.1 - 0.4 μg/kg IV
57
What is the induction dose of sufentanil?
18.9 mcg/kg IV
58
What is the sufentanil intraop dose? Infusion dose?
intraop: 0.3 - 1μg/kg IV infusion: 0.5 - 1μg/kg/hr IV.
59
What are side effects of sufentanil?
* bradycardia * decreased CO * chest and abdominal wall rigidity
60
What is the potency and onset of alfentanil?
**1/5th less** potent than fentanyl Onset: **1.4 min** > fentanyl/sufentanil
61
What is the alfentanil induction dose?
* **Induction**: 150 - 300 μg/kg IV * **Laryngoscopy**: 15 - 30 μg/kg IV * **Maintenance**: 25 - 150 μg/kg/hr IV with inhaled anesthetics.
62
Alfentanil is **contraindicated** for? Why?
* Parkinson's disease * acute dystonia
63
What receptor affinity does remifentanil have? What is its potency?
* selective μ opioid agonist * **15-20x** as potent as alfentanil (= fentanyl)
64
What is remifentanil’s structure and why is it important?
**Ester Structure** = hydrolyzed by **plasma** & **tissue esterases**
65
What are the pharmacokinetics of remifentanil?
* **Rapid onset & offset** (15 mins), very titratable, no accumulation. * Clearance: **3-4L/min** **(8x faster than alfentanil)** * Peak: **30-60 seconds** (fastest fentanyl derivative).
66
What is the **induction** dose of remifentanil?
1 μg/kg IV over 1 min
67
What is the **maintenance** dosing of remifentanil?
0.25-1 mcg/kg IV or **0.005 - 2 μg/kg/min IV**
68
What is the E1/2 time of remifentanil?
6.3 minutes (99.8%)
69
How potent is hydromorphone? What is the dose?
**5x more** potent than morphine **0.5mg IV → 1-4 mg total**
70
What benefits does hydromorphone have over morphine?
No histamine release & no active metabolites.
71
Why is codeine not given IV?
Histamine induced **hypotension**
72
What is the E 1/2 time of codeine?
3-3.5 hours
73
What is the dose of codeine for cough suppression? Analgesia dose?
Cough: **15mg** Analgesia: **60mg** (= about 5mg morphine).
74
Which opioid is most cleared?
Remifentanil (3-4L/min)
75
Which opioid(s) is/are the most protein bound?
**Sufentanil, alfentanil, & remifentanil** Least = morphine.
76
Which opioid is the highest percent **non-ionized**?
Alfentanil
77
Morphine tends to relieve _____ type pain more than _____ type pain.
Dull: sharp
78
Opioid + N2O or benzos can lead to?
CV depression (CO & BP)
79
What negative effect does post-op shivering have?
increased metabolic demand 500%
80
What is the metabolism profile for **alfentanil**? (metabolized by and metabolite)
metabolized by hepatic p450 metabolite: noralfentanil
81
How potent is tramadol?
5-10x less than morphine
82
Tramadol receptor? Dose?
* µ with weak κ & δ * 3 mg/kg PO * interaction with coumadin
83
What is methadone used for?
* Opioid withdrawal * chronic pain

TxWes Spring '25: Anesthesia Pharm (13 decks)

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