Opiates

Question 1

what is the mechanism of action by which opiates exert their effects ?

Answer 1

• opiates are μ-opioid receptor agonists
  (“μssage parlor”)

-activation of opiate receptors leads to opening of K+ ion channel causing hyperpolarization
(“open banana barrels in the back”)

-activation of opiate receptors closes Voltage Dependent Ca+2 channel
(“closed Calci-YUM ice cream cooler next to bananas”)

-closure of Voltage Dependent Ca+2 channel prevents release of neurotransmitters basically stopping the pain signaling in the brain

(“worker disconnecting presynaptic wire from icecream cooler”)

Question 2

Name the Semi Synthetic opiates and classify them according to their strength

Answer 2

Strong
Heroin
Oxycodone

Weak/Intermediate
Dihydrocodeine

Mixed Agonist/Antagonist

Buprenorphine
Nalbuphine

Question 3

Names of opiates agonists

Answer 3

Fentanyl (opioid analgesic)
(“Fantasy”)

Morphine (opioid analgesic)
(“More fun”)

Tramadol
(“Distant tram”)

(a weak μ-opioid receptor agonist used to manage chronic pain)

Question 4

Tramadol properties

(“synthetic weak/intermediate”)

Answer 4

a weak μ-opioid receptor agonist used to manage chronic pain

• inhibits reuptake of norepinephrine and serotonin
  (“North-South”)

(“Distant tram”)

Question 5

Loperamide
(“Lop-eared rabbit”)

Diphenoxylate
(“Dolphins”)

properties

Answer 5

μ-opioid receptors are located in the GI tract delay stool transit

• can be used as antidiarrheals
  (“Removed muddy slippers”)
• Loperamid increases colonic phasic segmentation → increase stool transit time
  (“Loping back and forth”)

Question 6

Codeine
(“Barcode”)

Orphan
(“dextromethorphan”)

Properties

Answer 6

Opioid antitussives

• dextromethorphan antagonizes NMDA receptors
  (“Tethered nomadic camel”)

Question 7

Opiates Side Effects

Answer 7

cause CNS depression (e.g.sedation)
(“Cerebral towel”)

-opiates can cause respiratory depression
(“Deflated lung vest”)

-opiates cause miosis (constricted pupils)
(“Constricted hood”)

-can cause constipation
(“Plunger”)

-can cause biliary colic (contract biliary smooth muscle)
(“Biliary tree”)

-patients may develop tolerance to opiates

(“All are welcome”)

• tolerance does not develop for miosis or constipation
  (“Out of order””)

​-opiate induced hyperalgesia can occur with chronic use
(“Causing pain”)

-opioid withdrawal
(“Anxious, hot, and moist”)

• rhinorrhea
• lacrimation
• yawning
• hyperventilation
• hyperthermia
• muscle aches
• vomiting
• diarrhea
• anxiety

Question 8

Methadone
(“DONE timer”)

Properties

Answer 8

long acting opioid used to attenuate withdrawal symptoms

• methadone and buprenorphine have a long half lives used in opioid detoxification
  (“Long tapering flag”)

Question 9

Buprenorphine

Properties

Answer 9

long acting partial μ-opioid agonist used to attenuate withdrawal symptoms

Question 10

partial μ-opioid agonists

Buprenorphine
Nalbuphine
​Butorphanol

Properties

Answer 10

partial μ-opioid agonists can induce withdrawals

Question 11

Naloxone use

(“No lax zone”)

Answer 11

μ-opioid antagonist used to reverse acute opioid toxicity

• can precipitate withdrawals

Question 12

Naltrexone use

(“No tricks zone”)

Answer 12

μ-opioid antagonist

helps maintain abstinence in heroin addicts
(“no tricks zone just results”)

helps reduce cravings for alcohol and nicotine
(“Tempting alcohol”)

naltrexone can help with weight loss
(“Getting fit”)

Question 13

Name the Synthetic Opiates

Answer 13

Strong

Meperidine
Fentanyl
Methadone

Weak/ Intermediate

Diphenoxylate
Loperamide
Tramadol