Opioid Analgesics

Question 1

Typical Pharmacologic Approaches to Chronic Pain (4)

Answer 1

Opioid Analgesics
NSAID’s
Glucocorticoids
DMARD’s

Question 2

Prototype opioid agent

Answer 2

Morphine

Question 3

Opioids are used to produce what effects? (5)

Answer 3

euphoria
analgesia
sedation
relief from diarrhea
cough suppression

Question 4

Opium

Answer 4

greek word meaning juice –> exudate from poppy seeds containing 20 biologically active components including morphine and codeine

Question 5

opiates

Answer 5

drug extracted from poppy exudate

morphine and codeine

Question 6

Opioid

Answer 6

natural or synthetic drug that binds to OPIOID RECEPTORS to produce AGONIST EFFECTS

Question 7

Narcotic

Answer 7

pharmacological compounds used to treat moderate to severe pain

Question 8

Natural Opioids occur as (5)

Answer 8

morphine
codeine

endogenous –> endorphins, enkephalins, dynorphins

Question 9

Three Major Endogenous Opioid Receptors

Analgesic properties associated primarily with?

Answer 9

Mu –> 1 and 2 - analgesic responses
Kappa
Delta

Question 10

Pharmacokinetics for all opioids

Answer 10

absorption - well absorbed from GI - experience 1st pass effect

metabolism - Hepatic glucuronidation primarily

Latency to onset decreases from transdermal to pulmonary inhalation

Question 11

Morphine metabolism important notes

Answer 11

Morphine converted to M6G and M3G

M6G has significant analgesic properties

Question 12

Mechanisms of Analgesia (3)

Answer 12

Gi/Go coupling

Inhibits adenylyl cyclase - decreased cAMP

Reduces intracellular Ca - leads to Decreased neurotransmitter release

Increase post-synaptic K channel opening - hyperpolarization

Question 13

Mechanisms of Analgesia with Ascending Pain Pathways (3)

Answer 13

Inhibition of AFFERENT PAIN TRANSMISSION

Decreases EXCITABILITY OF PERIPHERAL SENSORY NEURONS

Blocks pain signaling both pre-synaptically and post-synaptically in DORSAL HORN

Question 14

Mechanism of Analgesia with Descending Pain pathways

Answer 14

BLOCKS INHIBITORY GABA INTERNEURONS

leads to ENHANCED INHIBITION OF NOCICEPTIVE PROCESSING

Question 15

3 Sites of Action of Opioids in Descending Pain Pathways

Answer 15

Periaqueductal Gray Area
Rostral ventral medulla
Locus coeruleus

Question 16

Analgesia affects both _____ and _____ aspects of pain

Answer 16

sensory

affective

Question 17

Opioids affect breathing how?

What clinical scenario should the be used with caution?

why?

Answer 17

cause respiratory depression

head trauma

reflexive cerebral vasodilation

Question 18

Pupils with opioids

Answer 18

pin-point (constricted)

Question 19

GI effects with opioids

Answer 19

constipation

Question 20

Opioid effects on _____ release can lead to urticaria, itching, diaphoresis, and vasodilation

Answer 20

HISTAMINE

Question 21

Drug Interactions of Opioids

Answer 21

CNS Depressants
MES Inducers
MAOI's 
Mixed agonist-antagonists
Antagonists

Question 22

What is the major drug that negatively interacts with MAOI?

Answer 22

MEPERIDINE

hyperpyrexic reaction

Question 23

Strong Agonists (8)

Answer 23

Morphine
Hydromorphone
Oxymorphone
Methadone
Meperidine
Fentanyl
Sufentanil
Heroin

Question 24

Moderate Agonists (3)

Answer 24

Codeine
Oxycodone
Hydrocodone

Question 25

Mixed Agonist/Antagonist (4)

Answer 25

Buprenorphine
Butorphanol
Nalbuphine
Pentazocine

Question 26

Other Opioid Agonists

Answer 26

Dextromethorphan
Diphenoxylate
Loperamide
Tramadol

Question 27

Opioid Antagonists

Answer 27

Naloxone
Naltrexone
Nalmefene

treatment of OVERDOSE

Question 28

Which Mixed Agonists/Antagonists activate kappa and block mu? (3)

Answer 28

Butorphanol
Nalbuphine
Pentazocine

Question 29

Hydromorphone vs morphine

Answer 29

7 to 10x more potent

Question 30

Fentanyl notes

Answer 30

TRANSDERMAL PATCH available

72 hours release

80x more potent than morpheine

Question 31

Codeine (3 important notes)

Answer 31

less euphoria
lower abuse potential
can produce significant sedation

Question 32

Naloxone

Answer 32

REVERSES ACUTE OPIOID OVERDOSE

can produce reversal of CNS and respiratory depression WITHIN 30 SECONDS

Question 33

Naltrexone vs Naloxone

Answer 33

takes longer to take effect but LASTS LONGER

maintenance drug of opioid addiction

Question 34

Withdrawal symptoms can occur within?

usually subside within?

Answer 34

6 to 10 hours

5 days

Question 35

Methadone

Answer 35

primary intervention to treat opioid addiction

MILDER WITHDRAWAL SYMPTOMS