Opioids

Question 1

-any drug, natural or synthetic, that acts at opioid receptors

Answer 1

opioids

Question 2

-derived from opium poppy, contains many opiate compounds including morphine and codeine

Answer 2

opiates

Question 3

• at least 3 receptor types (mu, kappa, delta)
• all are Gprotein coupled
• close calcium channels, reducing evoked transmitter release (presynaptic)
• open potassium channels, hyperpolarizing membranes (postsynaptic)

Answer 3

morphine

Question 4

_____ receptors produce analgesic, sedative, and euphoric effects of opiates, as well as most of untoward side effects

Answer 4

mu

Question 5

_____ receptors appear to contribute to analgesia at spinal levels

Answer 5

delta

Question 6

____ receptors may also contribute to analgesia, but primarily results in dysphoria

Answer 6

kappa

Question 7

• opioid receptors in peripheral tissues
• dorsal horn of spinal cord (IPSPs, inhibition of NT release)
• ventral caudal thalamus

Answer 7

afferent pain transmission from periphery to CNS

Question 8

• periaqueductal grey matter
• rostral ventral medulla
• dorsal horn of the spinal cord

Answer 8

pain modulating descending paths from the CNS

Question 9

• analgesia
• euphoria/dysphoria
• sedation
• respiratory depression
• cough suppression
• miosis (parasympathetic, cholinergic)
• truncal rigidity
• nausea and vomiting

Answer 9

CNS effects of opioids

Question 10

• arterial and venous dilation
• constipation
• biliary colic
• decreased RBF
• decreased uterine tone
• endocrine alterations: increase ADH, prolactin, somatotropin, decreased LH
• histamine: flushing, sweating, rashes and itching

Answer 10

peripheral effects of opioids

Question 11

• acute or chronic pain (analgesic, no apparent max dose, less effective for neuropathy)
• acute pulm edema or MI, decreases sensation of crisis
• cough, antitussive
• diarrhea
• anesthesia, preop meds

Answer 11

uses of opioids

Question 12

• respiratory depression (primary cause of death)
• dysphoria
• nausea, vomiting
• constipation
• seizures at high doses, delta mediated

Answer 12

opioid toxicity

Question 13

• clinically apparent in 2 weeks
• develops to euphoria, resp depression, analgesia, sedation, nausea, cough suppression, antidiuresis
• minimal or none to constipation, seizures, miosis

Answer 13

tolerance

Question 14

dysphoria, rinorrhea, lacrimation, yawning, chills, vomiting, diarrhea, anorexia, insomnia, anxiety, hostility
-no tolerance but craving can persist

Answer 14

opioid withdrawal

Question 15

equal to 10mg morphine

Answer 15

equianalgesic dose

Question 16

morphine, methadone, meperidine, hydromorphone, oxymorphone, fentanyl, alfentanil

Answer 16

high efficacy analgesics (severe pain, trauma, post surgical)

Question 17

• poor oral bioavailability

- duration 4-5 hours

Answer 17

morphine

Question 18

• longer acting, 6 hours, plasma half life 24 hours
• good oral bioavailability
• used as maintenance in opioid addicts

Answer 18

methadone

Question 19

• medium acting 2-4 hours
• antimuscarinic, may cause tachycardia
• metabolized to active metabolite
• psychoactive, can cause seizures

Answer 19

meperidine

Question 20

• short acting, 1hr
• 100X more potent than morphine
• acts at mu receptors
• poor oral bioavailability
• transdermal available

Answer 20

fentanyl

Question 21

• very short acting, 15-45min
• very potent, parenteral only
• for brief, painful procedures

Answer 21

alfentanil

Question 22

codeine, hydrocodone, oxycodone, propoxyphene, tramadol

Answer 22

low to medium efficacy analgesics

Question 23

low efficacy, metabolized into morphine by CYP2D6

Answer 23

codeine

Question 24

full agonist, moderate/high efficacy

Answer 24

oxycodone

Question 25

- propoxyphene like metabolites, inhibits NE and 5HT reuptake - may have efficacy for neuropathic pain

Answer 25

tramadol

Question 26

- believed to have less addictive potential and risk of respiratory depression - used for moderate to severe pain - also used for opioid addiction

Answer 26

partial or mixed agonist-antagonist analgesics

Question 27

- mu partial agonist | - maintenance of opioid dependance as depot or in combo with naloxone

Answer 27

buprenorphine

Question 28

buprenorphine, butorphanol, nalbuphine, pentacozine

Answer 28

partial or mixed agonist-antagonist analgesics

Question 29

-antidiarrheals, poor permeation of BBB

Answer 29

diphenoxylate, loperamide

Question 30

codeine and dextromethorphan

Answer 30

antitussives

Question 31

- opioid antagonist used for acute overdose - 1-2 hr duration - high affinity for mu receptors - used in combo with buprenorphine for maintenance of opioid dependance, and in combo with oxycodone for chronic pain

Answer 31

naloxone, for acute opioid overdose

Question 32

used to prevent relapse in recovering addicts, or buproprion for weight loss

Answer 32

naltrexone

Question 33

methylnaltrexone or naloxegol, poor BBB penetration

Answer 33

opioid antagonist, used for constipation

Question 34

many opioids have low bioavailability due to 1st pass metabolism, except which two?

Answer 34

methadone and codeine

Question 35

______ is more potent than morphine but has poor BBB permeability, glucoronidated

Answer 35

M-6G

Question 36

______ and ______ are metabolized into morphine

Answer 36

codeine and heroin

Question 37

- head injuries - pregnancy - impaired pulm function - hepato or renal compromised patients - endocrine disorders

Answer 37

contraindications of opioids

Question 38

pure agonists and mixed-agonist/antagonist _______ analgesia, can precipitate withdrawal symptoms

Answer 38

decrease

Question 39

opioids + other sedative hypnotics ______ sedation and respiratory depression

Answer 39

increase

Question 40

opioids + antipsychotics _____ sedation and respiratory depression, _____ risk of seizures

Answer 40

increase, increase

Question 41

opioids + MAOIs ______ risk of hyperpyrexic coma and hypertension

Answer 41

increase