Opioid Narcotic Analgesics Flashcards

1
Q

Endorphins

A

Mu Rc (supra-spinal analgesia)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

Dynorphins

A

Kappa Rc (spinal analgesia)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

Enkephalins/Endorphins

A

Delta Rc

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

Mu opioid Rc - Full agonist

A
  1. Fentanyl (more potent)

2. Morphine

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

Partial agonist (Mu)/mixed (Mu/K/delta)

A
  1. Buprenorphine (partial agonist/mixed)

2. Pentazocine (mixed)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

Mu opioid Rc - antagonist

A
  1. Naloxone
  2. Naltrexone
    BOTH inhibit heroin, morphine, fentanyl –> ANTIDOTE for opioid overdose
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

Tolerance to morphine

A

Response dec over time –> increase dose or different opioid
NO TOLERANCE TO - miosis, constipation
Contraindication - brain injury, emphysema

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

Group 1
Full agonists
Parenteral/Oral

A
  1. Morphine (low oral:parenteral ratio)
  2. Methadone (high O:P ratio)
  3. Meperidine
  4. Hydromorphine
  5. Oxymorphine
  6. Levorphanol (high O:P ratio)
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

Group 2
Full agonists
Short acting

A
  1. Fentanyl
  2. Sufentanil (Mu, K, delta)
  3. Remifentanyl - VERY short acting
  4. Alfentanil
    This group is 100x more potent than morphine and methadone
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

Group 3

Partial agonists

A
  1. Codeine - high O:P ratio; low efficiency; give higher dose
  2. Hydrocodone - usually given with acetaminophen
  3. Oxycodone - usually given with acetaminophen
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

Morphine

A

CYP 3A4 = normorphine (INACTIVE)
UGT 1A1/2B7 = Morphine-3-glucuronide and Morphine-6-glucuronide (ACTIVE)
Dehydrogenase = Hydromorphone (ACTIVE)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

Methadone

A
  • useful for withdrawal/maintenance, detoxification
  • affects electrical conduction of heart - QT interval prolonged in overdose/long term trt
  • block K channel –> delayed repol (HERG channels)
  • longer half life than morphine
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

Meperidine

A
  • eye: dilation
  • Normeperidine (toxic) accumulates –> seizures
    Fentanyl –> meperidine –> morphine
    (faster –> slower onset)
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

Remifentanyl

A
  • childbirth analgesia
  • metab by plasma and tissue esterases (rapid in fetus)
  • RAPID onset/SHORT acting
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

Fentanyl (lollipop)

A
  • RAPID onset/SHORT duration (Lipophilic)
  • transmucosal
  • used for ‘break through pain’ due to morphine
  • transdermal patch delivery (slow onset)
  • NO active metabolite (like Hydromorphone and oxymorphone)
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

Codeine

A
  • less chance for resp depression
  • moderate pain analgesia
  • 50% oral absorption
  • anti-tussive –> cough relief (Mu independent)
    Adverse effect - sleep apnea and death in kids
  • CYP 3A4 = norcodeine (INACTIVE)
  • UGT 2B7 - codeine-6-glucuronide (ACTIVE)
17
Q

Safer anti-tussive

A

Dextromethophan

  • not analgesic/not addictive
  • relieves cough INDEPENDENT of opioid Rc
18
Q

Minimal abuse - Gut & opioids

A
  1. Loperamide

2. Diphenoxylate

19
Q

Loperamide

Diphenoxylate

A
  • anti-diarrheals
  • poor solubility
  • poor BBB penetration
20
Q

Tramadol

A
  • Mu-desmethyl (active metabolite)
  • 70% bioavailability
  • inhibit catecholamine release
  • can cause seizures
  • treats moderate/uncontrolled/persisting pain
21
Q

Pentazocine

A
  • supra-spinal analgesia
  • precipitates ‘withdrawal’
  • tachycardia, hallucinations
22
Q

Buprenorphine

A
  • precipitates ‘withdrawal’

- detox/maintained in combo with Naloxone

23
Q

Abuse potential opioids

A

Heroin

  • di-acetylmorphine
  • penetrates BBB rapidly –> euphoria
24
Q

Naloxone (IV)

A
  • reverses coma/resp depression

- NOT ABSORBED FROM GUT

25
Q

Naltrexone (PO)

A
  • long duration in overdose

- 45 hrs for single dose

26
Q

Acetaminophen

A

Liver toxicity!!!

27
Q

Methylnaltrexone

A
  • quaternary derivative of naltrexone
  • cannot cross BBB
  • acts peripherally –> inhibits opioid induced decrease in GI motility
  • DECREASES CONSTIPATION
  • DOES NOT affect opioid analgesic affects