Opiods

Question 1

Pain

Answer 1

Unpleasant sensory and emotional experience with actual or potential tissue damage

Question 2

Nociceptors (pain receptors)

Answer 2

Free nerve ending with cells bodies outside the SC —> certain threshold reached before signal triggered —> threshold reached and signal passes along axon into the SC

Question 3

What sense pain/ primary target of opioids!

Answer 3

Dorsal root ganglion

Question 4

Opioid receptors and natural pain chemicals

Answer 4

Mu (MOP) receptors- endorphins
Kappa (KOP)- dynorphin
Delta (DOP)- encephalin

Question 5

Opioid receptor locations

Answer 5

MOP and KOP- brain, SC and peripheral sensory neurons
DOP- brain and peripheral sensory neurons

Question 6

Major effect of opioids receptors

Answer 6

Analgesia (spinal and supraspinal)

Question 7

MOP effects

Answer 7

Respiratory depression
Decreased GI motility, biliary secretions, urine voiding reflex, uterine contractions
Increased appetite
Euphoria
Antidiuresis
Miosis/ mydriasis
Nausea/ vomiting
Immunimodulation

Question 8

KOP receptor major effects

Answer 8

Decreased GI motility
Increased appetite
Sedation
Diuresis (increased ADH release)
Miosis / mydriasis

Question 9

DOP receptor major effects

Answer 9

Increased appetite
Immunomodulation

Question 10

Opioids MOA

Answer 10

Opioids bind to spinal and supraspinal receptors —> inhibit adenylyl cyclase (decrease CAMP) —> activation of K+ ion channels and hyperpolarization —> inhibits excitatory NT release

Question 11

Opioid therapeutic uses

Answer 11

Analgesia
Sedation
Calming and euphoria
Diarrhea, decreased GI motility
Induction and maintenance of anesthesia

Question 12

Agonist opioids

Answer 12

Morphine
Methadone
Hydromorphone
Fentanyl
Tramadol

Question 13

Mixed agonist/ antagonist opioids

Answer 13

Butorphanol
Buprenorphine

Question 14

Antagonist/ reversal of opioids

Answer 14

Naloxone

Question 15

Morphine PE

Answer 15

Analgesia, emetics , miosis, decreased GI motility

Question 16

Morphine therapeutic uses

Answer 16

Acute pain, anesthetic premedication, antitussive

Question 17

Adverse effects of morphine

Answer 17

Hyperexcitability, hypotension, cerebral hemorrhage or edema
Anaphyloid rx (mast cell degranulation)

Question 18

Methadone

Answer 18

Synthetic OPIOD
Slower elimination than morphine

Question 19

Methadone therapeutic uses

Answer 19

Preanesthetic, algesia

Question 20

Methadone adverse effects

Answer 20

Sedation, vomiting, constipation, respiratory depression

Question 21

Hydromorphone

Answer 21

5x analgesia potency of morphine
Replaced oxymorphone

Question 22

Hydromorphone therapeutic uses

Answer 22

Analgesia, preanesthetic and anesthetic

Question 23

Hydromorphone adverse effects

Answer 23

Panting (cool down) and bradycardia, dose dependent excitement, cerebral hemorrhage or edema

Question 24

Fentanyl PK

Answer 24

More rapid onset than morphine but shorter duration
75-125 x more potent

Question 25

How do you measure fentanyl?

Answer 25

MICROGRAMS!!

Question 26

Fentanyl therapeutic uses

Answer 26

Analgesia (continuous infusion), anesthetic induction in dogS Neuroletanalgesia

Question 27

Adverse affects of fentanyl

Answer 27

Motor response Panting, defecation, flatulence, bradycardia, salivation

Question 28

Tramadol

Answer 28

Synthetic analog of codeine MOP agonist (weak) and inhibits serotonin and NE uptake @ synapse

Question 29

Tramadol PK

Answer 29

Active metabolite is desmethyltramadol

Question 30

Tramadol therapeutic affects

Answer 30

Analgesic, antitussive in dogs and cats

Question 31

Butorphanol

Answer 31

Agonist-Antagonist High affinity for MOP receptors but not activity (antagonist) High affinity for KOP receptors

Question 32

Butorphanol therapeutic uses

Answer 32

Opiod reversal (antagonist), analgesic, antitussive *short duration of efficacy limits its use as a primary*

Question 33

Buprenorphine

Answer 33

Most generally useful analgesic in dogs and cats (30x potency of morphine) Longer duration of action than other opiods

Question 34

Buprenorphine MOA

Answer 34

High affinity for MOP but only partial agonist KOP antagonist

Question 35

Buprenorphine therapeutic uses

Answer 35

Analgesia for mild to moderate pain in small animals (buccal/ transmucosal admin in cats)

Question 36

Simbadol for Cats

Answer 36

Buprenorphine long acting SQ Slow release SQ prep Offers 24 hour surgical pain control for cats (1x/day)

Question 37

Zorbium for Cats

Answer 37

Buprenorphine Transdermal First FDA approved long acting transdermal for bupren for cats 4 days, single dose

Question 38

Naloxone

Answer 38

Pure opiate antagonist High affinity for MOP receptors High doses will reverse DOP and KOP

Question 39

Naloxone PK

Answer 39

Duration of action less than agonists Repeated administration for opioid reversal (monitor and redose)

Question 40

Naloxone therapeutic uses

Answer 40

Reversal of opioid induced respiratory depression Treat shocks (IV and IM, nasal) Extralabel use in dogs and cats

Question 41

Adverse effects of naloxone

Answer 41

CNS sedation Respiratory and cardiac depression

Question 42

Naloxone contraindicated

Answer 42

Shock Severe cranial trauma and diseases associated with respiratory compromise

Question 43

Continuous opioid use

Answer 43

If given longer than 5-7 days they'll get withdrawal signs (nausea, aggregation, vocalization, vomting, hyperactivity) after discontinuing the drug or antagonist administered

Question 44

Opioid scheduling

Answer 44

Morphine and other pure: 2 Bupren: 3 Buto: 4 (2-5, low potential of abuse)