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Neuro-Psych Exam II > Pain Drugs > Flashcards

Pain Drugs Flashcards

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
Q

Name two antidiarrheal opioids with NO CNS activity

A
  1. Diphenoxylate

2. Loperamide (Immodium)

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26
Q

Describe 6 effects of opioid withdrawal

A
  1. Rebound phenomenon
  2. Hyperalgesia
  3. Hyperventilation
  4. Mydriasis
  5. Diarrhea
  6. Dysphoria
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27
Q

3 Drugs to NOT co-administer with opioids

A
  1. Phenothiazines
  2. MAOIs
  3. TCAs
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28
Q

3 Contraindications to opioid use

A
  1. Hepatic insufficiency
  2. Resp insufficiency
  3. Head injury
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29
Q

Codeine:
MOA
Therapeutic use (2)

A 
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
Q

Which CYP is responsible for metabolism of Codeine?

A

O-demethylation

CYP2D6 metabolism

31
Q

What are the predominant ADRs w/ methadone use (2)

A
  1. Constipation

2. Biliary spasms

32
Q

What is the therapeutic use or methadone? (2)

Social problem associated with methadone use?

A
  1. Pain
  2. Opiate withdrawal

*Drug of Abuse= WV #1 OD

33
Q

What is the MOA of Methadone?

A

Strong u agonist

*No K activity

34
Q

Important feature of methadone metabolism and 2 reasons why it is useful?

A

Long t1/2–>

  1. Single daily dose
  2. Slower tolerance (meet craving w/out opioid use)

*Levels out cravings and is self tapering

35
Q

Heroine:
MOA
Use

A

Morphine Precursor; strong agonist

* Drug of Abuse; look for miosis

36
Q

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?

A

Heroin (DAM)–> 6-MAM–> M

  • 6- MAM & DAM > morphine @ BBB.
  • 6-MAM = urine metabolite
37
Q

Hydromorphone:
MOA
Therapeutic Use

A

Strong u agonist

*Treatment of severe pain

38
Q

Hydrocodone + Acetaminophen:
MOA
Therapeutic use
Social Implications

A

Orally equipotent to morphine (same as morphine)
Tx: severe pain or cough
* Drug of Abuse, esp with extended release version

39
Q

Oxycodone:
MOA
Therapeutic Use

A

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
Q 
Fentanyl (+ derivatives ending in "il"): 
MOA 
Therapeutic Use (2)
Advantage over morphine
Social implications
A

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
Q

Meperidine:
MOA
Therapeutic Use
Drug-Drug Interactions

A

Strong u agonist–synthetic

Tx: Obstetrics

DDI: MAOIs–> CNS excitement w/ resp depression and delirium

42
Q

Describe how Meperidine causes CNS excitement at toxic doses–why is this exceptionally dangerous?

A

Normeperidine (metabolite at toxic doses) will cause CNS excitement

*THIS CAN NOT BE BLOCKED BY NALOXONE

43
Q

What drug is metabolized by CYP2D6?

Describe implications for slow vs. fast metabolizers.

Which patient population must be exceptionally careful with this drug?

A

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
Q

Buprenorphine:
MOA
Therapeutic Use
ROA

A

Mixed u agonist/ k antagonist
Tx: Opioid dependence/ withdrawal in preggos
ROA: Sublingual

45
Q

Diphenoxylate:

Therapeutic Use

A

Opioid agonist; antidiarrheal

46
Q

Loperamide:

Therapeutic use

A

Opioid agonist; antidiarrheal

47
Q 
Tramadol: 
MOA
Therapeutic Use 
Social Implicatios
ADRS
A

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
Q 
Naloxone: 
MOA 
Therapeutic Use
ROA
Metabolism
A

Opioid Antagonist

Tx: OD in ER, instant withdrawal
ROA: IM/ IV
Metabolism: Short t1/2; fast acting

49
Q 
Naltrexone:
MOA
ROA 
Therapeutic Use
Special feature:
A

Opioid Antagonist
ROA: Oral
Tx: Opioid gentle withdrawal, ETOH withdrawal
Short t1/2

50
Q

Nalmefene
MOA
Therapeutic Use

A

Opioid Antagonist

Rarely used due to long t 1/2

51
Q 
Dextromethorphan: 
MOA 
Therapeutic use 
ADR
Social implications
A

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
Q

Clonadine:
MOA
Therapeutic use (3)

A 
A2 adrenergic agonist: 
^NE @ synapse in dorsal horn
Tx: 
1. Neuropathic pain 
2. Cancer pain 
3. Adjunct therapy
53
Q

Amitriptyline:
MOA
Therapeutic Use
ADR

A

TCA (^NE + 5-HT)
Neuropathic pain

***SUICIDE

54
Q

Venlafaxine:
MOA
Therapeutic Use

A

SNRI (^NE + 5-HT)

Neuropathic pain

55
Q

Duloxetine:
MOA
Therapeutic Use

A

SNRI (^NE + 5-HT)

Neuropathic pain

56
Q

Are SSRIs effective at treating pain?

A

NO need BOTH NE and 5HT

57
Q

Gabapentin + Pregabalin:
MOA (2)
Therapeutic Use
Drug-Drug Interaction

A 
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
Q

Carbamazepine:
MOA
Therapeutic Use

A

Blocks VGNa+ Channels

Tx: 1st line trigeminal neuralgia

59
Q

Lidocaine:

Therapeutic Use

A

Local anesthetic (topical)

60
Q

Capsaicin:
MOA
Therapeutic Use

A

Chilli pepper alkaloid
TRPV1 antagonist

Tx: Topical anesthetic

61
Q

Ketamine:

MOA

A

Blocks NMDA–> Blocks glu signals

62
Q 
Baclofen: 
MOA 
Therapeutic Uses (2)
ADRs (2)
DD Interactions
A

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
Q

Diazepam:
MOA
Therapeutic Use

A

BDZ

Tx: Spasms

64
Q

Carisoprodol:

Therapeutic Use

A

Tx: Acute MSK pain

*Rarely used

65
Q

Cyclobenzaprine:
Therapeutic Use (2)
Pharmacokinetics
ADRS

A

TX: Acute MSK spasms + pain, TMJ
Kinetics: Long t1/2
ADRS: Similar to TCAs, careful with elderly pts

66
Q

Metaxalone:
Therapeutic Use
ADRs
Contraindications

A

Tx: Muscle discomfort
ADRs: Jaundice*
CI: Liver impairment

67
Q

Methocarbamol:
Therapeutic Use (2)
ADRs
Kinetics

A

Tx: Muscle spasm, tetanus*

ADRs: CNS drowsiness + multiple system effects; careful with elderly

Kinetics: Rapid onset

68
Q

Tizanadine:
MOA
Therapeutic Use (3)

A

A2 Agonist

Tx: Tension HA*, muscle spasms, low back pain

69
Q

List the Centrally Active Muscle relaxants (6)

With which population must we be careful when administering these drugs?

A
  1. Baclofen
  2. Diazepam
  3. Cyclobenzaprine
  4. Metaxalone
  5. Methocarbamol
  6. Tizanadine

ELDERLY PEOPLE

70
Q

What is the first line treatment for neuropathic pain (other than trigenminal neuralgia)?

A

Antidepressants/ Ca++ channel alpha-2-delta ligands

Neuro-Psych Exam II (11 decks)

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