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Neuro-Psych Exam II > Pain Drugs > Flashcards

Pain Drugs Flashcards

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1
Q

What is the #1 pharmacological treatment for somatic (as opposed to neuralgic) Pain?

A

OTC Non-Opioid Analgesics

NSADIS, ASA, Acetaminophen, Cox-2 Inhibitors

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2
Q

Non-Opioid Analgesics:

MOA
Uses (5)

A

Targets the inflammatory component of pain cascade

Tx:

  1. Mild-moderate pain, esp somatic
  2. Soft tissue injury
  3. Strains/ Sprains
  4. HA
  5. Arthritis
    * Can be used synergistically with opioids
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3
Q

Acetaminophen:

Side effects and contraindications

A

SE: Hepatotoxic, #1 cause of liver failure in US

CI: Liver disease, Alcoholics

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4
Q

NSAIDS + ASA:

Side effects and contraindications

A

SE: Gastric ulcers, Inhibit platelet agg.
CI: Don’t mix NSAIDS w/ ASA in pts on Cardioprotective ASA
Don’t give NSAIDs in third trimester of pregnancy

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5
Q

Opioid Agonist Drugs:

MOA (5)

A
  1. Activate inward K+ channels
  2. Inhibit Ca++ channels
  3. Inhibit adenylyl cyclase
  4. Inhibit release of substance P
  5. Synaptic remodeling by MAP kinase
    * All work the same
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6
Q

Where are u receptors located? (3)

A
  1. CNS
    (neocortex, amygdala, thalamus, n. accumbens, hippocampus)
  2. Myenteric plexus (GI)
  3. Vas Deferens
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7
Q

What are the physiological effects of opioid action at u receptors? (5)

A
  1. Supraspinal analgesia
  2. Miosis
  3. GI stasis
  4. Respiratory depression
  5. Euphoria, dependence
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8
Q

Selective endogenous activators of u receptors (3)

A
  1. Endomorphin-1 & 2
  2. Enkephalins
  3. Beta-endorphin
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9
Q

2 important selective u ANTAGONISTS

A
  1. Naloxone

2. Naltrexone

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10
Q

Where are the K receptors located? (5)

A

Only in CNS

  1. Cerebral cortex
  2. Nucleus Accumbens
  3. Claustrum
  4. Hypothalamus
  5. SC
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11
Q

What are the physiological effects of activating the K receptors?

A
  1. SC analgesia
  2. Miosis
  3. Sedation
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12
Q

What is the endogenous activator of K receptors?

A

Dynorphins

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13
Q

What are 6 selective drug AGONISTS of u receptors?

A
  1. Morphine
  2. Fentanyl
  3. Methadone
  4. Meperidine
  5. Oxycodone
  6. Hydromorphone
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14
Q

What are 3 selective drug agonists of K receptors?

A
  1. Butorphanol
  2. Pentazocine
  3. Nalbuphine
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15
Q

What is the ultimate effect of long term opioid use on the nervous system?

A

Synaptic remodeling

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16
Q

Morphine:

Classification
MOA (2)
Therapeutic Use (3)

A 
C: Strong agonist 
MOA: 
*Strongest agonist of u receptors 
*Agonist of K receptors in spinal cord only 
Uses: 
*Moderate to severe acute or chronic pain 
1. Acute pulm. edema 
2. MI pain 
3. Preanesthetic
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17
Q

ROA for All Opioid Agonists (5)

A
  1. SQ
  2. IM
  3. oral
  4. suppository
  5. pump
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18
Q

ADR for all Opioid Agonists (4)

A
  1. Nausea, vomiting, constipation
  2. Miosis
  3. Respiratory Depression = OD
    * Give ventilation + nalox
  4. Tolerance- pain/ mood only, not above ADRs

NOT FIRST LINE DRUGS**

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19
Q

1 reason for death by opioid overdose

A

respiratory depression

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20
Q

Describe why opioid agonist possess abuse potential (esp. morphine)

A

u, K**agnonists–> euphoria/dysphoria–> abuse

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21
Q

How do opioid agonist (esp. morphine) induce n/v?

When is this important to consider?

A

Direct action on CTZ outside the BBB

*Must consider when administering morphine as pre-surgical analgesic so as to admin anti-emetic

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22
Q

How do we diagnose opioid intoxication?

A

Miosis ensues due to EW nucleus excitation; persists regards of light stimulation

*Pathogmonic

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23
Q

How do opioids like morphine induce respiratory depression?

A

Direct action on brainstem: decrease sensitivity to CO2

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24
Q

What is the most prominent GI side effect caused by opioid use?

Agonizing which receptors mediates this effect?

A

CONSTIPATION*

Mediated by u and delta activity

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25
Name two antidiarrheal opioids with NO CNS activity
1. Diphenoxylate | 2. Loperamide (Immodium)
26
Describe 6 effects of opioid withdrawal
1. Rebound phenomenon 2. Hyperalgesia 3. Hyperventilation 4. Mydriasis 5. Diarrhea 6. Dysphoria
27
3 Drugs to NOT co-administer with opioids
1. Phenothiazines 2. MAOIs 3. TCAs
28
3 Contraindications to opioid use
1. Hepatic insufficiency 2. Resp insufficiency 3. Head injury
29
Codeine: MOA Therapeutic use (2)
``` Morphine Precursor: metabolized by *CYP2D6 to ACTIVE form MOA: Acts on medulla to induce anti-tussive effects (dec. CNS sensitivity to cough stimuli; dec. mucosal secretion) Tx: 1. Antitussive 2. Mild Analgesic ```
30
Which CYP is responsible for metabolism of Codeine?
O-demethylation | CYP2D6 metabolism
31
What are the predominant ADRs w/ methadone use (2)
1. Constipation | 2. Biliary spasms
32
What is the therapeutic use or methadone? (2) Social problem associated with methadone use?
1. Pain 2. Opiate withdrawal *Drug of Abuse= WV #1 OD
33
What is the MOA of Methadone?
Strong u agonist | *No K activity
34
Important feature of methadone metabolism and 2 reasons why it is useful?
Long t1/2--> 1. Single daily dose 2. Slower tolerance (meet craving w/out opioid use) *Levels out cravings and is self tapering
35
Heroine: MOA Use
Morphine Precursor; strong agonist | * Drug of Abuse; look for miosis
36
Describe the course of heroine metabolism to morphine. What about heroine's metabolites makes it so risky for abuse? Which metabolite is found in urine?
Heroin (DAM)--> 6-MAM--> M * 6- MAM & DAM > morphine @ BBB. * 6-MAM = urine metabolite
37
Hydromorphone: MOA Therapeutic Use
Strong u agonist *Treatment of severe pain
38
Hydrocodone + Acetaminophen: MOA Therapeutic use Social Implications
Orally equipotent to morphine (same as morphine) Tx: severe pain or cough * Drug of Abuse, esp with extended release version
39
Oxycodone: MOA Therapeutic Use
Strong u agonist Tx: moderate to severe pain, often in combination with NSAIDS/ non-opiate drugs *Drug of abuse, esp with extended release version
40
``` Fentanyl (+ derivatives ending in "il"): MOA Therapeutic Use (2) Advantage over morphine Social implications ```
Strong u agonist--synthetic Tx: 1. Surgery pre/post anesthesia (IV admin) 2. Treatment chronic pain in opioid tolerant patients (patch or lozenge) *Less N/V than morphine Social: Heroin may be laced w/ fentanyl = ^^ death
41
Meperidine: MOA Therapeutic Use Drug-Drug Interactions
Strong u agonist--synthetic Tx: Obstetrics DDI: MAOIs--> CNS excitement w/ resp depression and delirium
42
Describe how Meperidine causes CNS excitement at toxic doses--why is this exceptionally dangerous?
Normeperidine (metabolite at toxic doses) will cause CNS excitement *THIS CAN NOT BE BLOCKED BY NALOXONE
43
What drug is metabolized by CYP2D6? Describe implications for slow vs. fast metabolizers. Which patient population must be exceptionally careful with this drug?
Codeine (inactive if enzyme is deficient) slow metabolizers--codeine is ineffective analgesic fast metabolizers--rapid conversion to morphine, overdose *Preggos or breastfeeding: infant overdose if she is slow and baby is fast
44
Buprenorphine: MOA Therapeutic Use ROA
Mixed u agonist/ k antagonist Tx: Opioid dependence/ withdrawal in preggos ROA: Sublingual
45
Diphenoxylate: | Therapeutic Use
Opioid agonist; antidiarrheal
46
Loperamide: | Therapeutic use
Opioid agonist; antidiarrheal
47
``` Tramadol: MOA Therapeutic Use Social Implicatios ADRS ```
Inhibits 5-HT + NE Reuptake; unrelated to opiates but partially inhibited by naloxone Tx: Moderate pain (esp in dogs) *Drug of abuse ADRs: Similar to opiates
48
``` Naloxone: MOA Therapeutic Use ROA Metabolism ```
Opioid Antagonist Tx: OD in ER, instant withdrawal ROA: IM/ IV Metabolism: Short t1/2; fast acting
49
``` Naltrexone: MOA ROA Therapeutic Use Special feature: ```
Opioid Antagonist ROA: Oral Tx: Opioid gentle withdrawal, ETOH withdrawal Short t1/2
50
Nalmefene MOA Therapeutic Use
Opioid Antagonist | Rarely used due to long t 1/2
51
``` Dextromethorphan: MOA Therapeutic use ADR Social implications ```
Synthetic morphine derivative w/ NMDA activity in high doses Tx: Antitussive--Suppresses response of cough center; elevates threshold ADR: Hepatotoxic *Robotripping in teens *Not reversible with naloxone
52
Clonadine: MOA Therapeutic use (3)
``` A2 adrenergic agonist: ^NE @ synapse in dorsal horn Tx: 1. Neuropathic pain 2. Cancer pain 3. Adjunct therapy ```
53
Amitriptyline: MOA Therapeutic Use ADR
TCA (^NE + 5-HT) Neuropathic pain ***SUICIDE
54
Venlafaxine: MOA Therapeutic Use
SNRI (^NE + 5-HT) | Neuropathic pain
55
Duloxetine: MOA Therapeutic Use
SNRI (^NE + 5-HT) | Neuropathic pain
56
Are SSRIs effective at treating pain?
NO need BOTH NE and 5HT
57
Gabapentin + Pregabalin: MOA (2) Therapeutic Use Drug-Drug Interaction
``` MOA: 1. Block alpha-2-delta ligands 2. Decrease activity in Ca++ channels Tx: Neuropathic pain DDI: Potentiate opioids, do not admin together--they are commonly co-abused ```
58
Carbamazepine: MOA Therapeutic Use
Blocks VGNa+ Channels Tx: 1st line trigeminal neuralgia
59
Lidocaine: | Therapeutic Use
Local anesthetic (topical)
60
Capsaicin: MOA Therapeutic Use
Chilli pepper alkaloid TRPV1 antagonist Tx: Topical anesthetic
61
Ketamine: | MOA
Blocks NMDA--> Blocks glu signals
62
``` Baclofen: MOA Therapeutic Uses (2) ADRs (2) DD Interactions ```
GABA Agonist Tx: spasticity, hiccups ADRS: 1. CNS depression 2. BLACK BOX warning--rapid withdrawal causes hyperpyrexia, rabdo and other bad stuff DDIs: Do not coadmin with other CNS depressants
63
Diazepam: MOA Therapeutic Use
BDZ Tx: Spasms
64
Carisoprodol: | Therapeutic Use
Tx: Acute MSK pain | *Rarely used
65
Cyclobenzaprine: Therapeutic Use (2) Pharmacokinetics ADRS
TX: Acute MSK spasms + pain, TMJ Kinetics: Long t1/2 ADRS: Similar to TCAs, careful with elderly pts
66
Metaxalone: Therapeutic Use ADRs Contraindications
Tx: Muscle discomfort ADRs: Jaundice* CI: Liver impairment
67
Methocarbamol: Therapeutic Use (2) ADRs Kinetics
Tx: Muscle spasm, tetanus* ADRs: CNS drowsiness + multiple system effects; careful with elderly Kinetics: Rapid onset
68
Tizanadine: MOA Therapeutic Use (3)
A2 Agonist Tx: Tension HA*, muscle spasms, low back pain
69
List the Centrally Active Muscle relaxants (6) With which population must we be careful when administering these drugs?
1. Baclofen 2. Diazepam 3. Cyclobenzaprine 4. Metaxalone 5. Methocarbamol 6. Tizanadine ELDERLY PEOPLE
70
What is the first line treatment for neuropathic pain (other than trigenminal neuralgia)?
Antidepressants/ Ca++ channel alpha-2-delta ligands

Neuro-Psych Exam II (11 decks)

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