Opioid Analgesics

Front 1

Opioids

Back 1

1. Morphine
2. Methadone- long-acting synthetic opioid

Front 2

Opioid Receptors

Back 2

1. Mu receptors- for euphoria and analgesia
2. Delta receptors
3. Kappa receptors- analgesia and dysphoria
4. Orphan receptor

Front 3

Endogenous Opioids

Back 3

1. Enkephalins- bind to both mu and delta
2. Dynorphins- bind to kappa
3. Beta-Endorphins- bind to mu and delta
**All of the clinically relevant are MU AGONISTS

Front 4

Opioid Agonists: Opium alkaloids and derivatives

Back 4

1. Morphine
2. Heroin
3. Hydromorphone
4. Codeine and mixtures containing codeine
5. Hydrocodone

Front 5

Morphine

Back 5

1. Mu agonist
2. Not given orally b/c of huge First Pass Effect
3. Mu opioids reduce the activity of the ascending pathways, so you don't perceive pain
4. Descending pathway will slow your response to pain

Front 6

Desirable Properties of Morphine

Back 6

1. Effective analgesia over a wide dosage range
2. Effect on mood (relief of anxiety)
3. Sedation- ex: used when getting a tooth pulled

Front 7

Three biggest Side Effects of Morphine

Back 7

1. RESPIRATORY DEPRESSION- opioids put the respiratory center of your brain to sleep, so brain can't tell the body when to breathe
2. DEPRESSION OF COUGH REFLEX
3. CONSTIPATION

Front 8

Other Side Effects (or Undesirable Properties) of Morphine

Back 8

1. Sedation
2. Mental clouding (ex:inability to concentrate)
3. Dysphoria
4. Dizziness (primarily on ambulation)
5. Nausea and vomiting
6. Circulatory depression (OH)
7. Biliary tract spasms
8. Uretreral and vesical spasms
9. Urinary retention
10. Behavioral dependence
11. Physical dependence
12. Tolerance to some effects

Front 9

Opioid Agonists: Synthetic Compounds

Back 9

1. Meperidine- has a convulsant metabolite (meperidine)
2. Fentanyl
3. Methadone
4. Propoxyphene- crappy analgesic

Front 10

Methadone

Back 10

1. Synthetic agonist
2. Half-life of 24 hours
3. Widely used for opioid dependents

Front 11

Opioid Antagonists

Back 11

1. Naloxone (Narcan)
2. Naltrexone (Trexan)

Front 12

Naloxone (Narcan)

Back 12

1. Opioid antagonist
2. Half-life of about 30 minutes, so must be readministered
3. Found on every crash cart in every hospital

Front 13

Naltrexone (Trexan)

Back 13

1. Opioid antagonist
2. Half-life of 24 hours
3. Good oral efficacy, and also comes in an injectable form

Front 14

Mixed Agonist-Antagonists

Back 14

1. Pentazocine
2. Butorphanol
3. Nalbuphine
4. Dexocine
5. Buprenorphine
6. Tramadol

Front 15

Buprenorphine

Back 15

1. Partial mu agonist
2. Given for dependence
3. Has a 48 hour half-life, so sometimes it is used in the place of Methadone

Front 16

Metabolism of Opioids

Back 16

P450-2D6 system in the liver; converts codeine to morphine and oxycodone to oxymorphone

Front 17

Signs of Opioid Overdose

Back 17

1. Pinpoint pupils
2. Decreased respiration
3. Loss of consciousness