Ch28 opioids

Question 1

Receptor Classes

Answer 1

• Mu: analgesia, respiratory depression, euphoria, sedation, dependence (most commonly activated)
• Kappa: analgesia and sedation
• Delta: send fastest pain impulse, inhibiting slows pain recepting

Question 2

Opioid Classification

Answer 2

•Pure Opioid Agonist: work to relieve pain by mimicking opioid peptides
Mu and kappa receptors
–Morphine: moderate to strong
–Codeine: moderate to strong

•Agonist-Antagonist Opioid:
–Alone: analgesia
+ pure opioid agonist = antagonist properties
–Pentazocine, nalbuphine, butorphanol,buprenorphine

•Pure Opioid Antagonist
–Narcan: anecdote to opioid overdose and opioid constipation
–Mu and kappa receptors
–No analgesia
–Reverses respiratory and CNS depression
–Methylnatrexone: Reverses constipation

Question 3

Morphine

Answer 3

Activate MU and Kappa receptors causing
–Analgesia
–Drowsiness
–Decreased cognition
–Decreased anxiety
–Provides sense of well being

General info:
•Relieves pain without effect senses
•No loss of consciousness
•Mimicks endogenous endorphins (agonist)
•Routes: IV, IM, epidural, intrathecal (spinal cord; epidural)
•Not very lipid soluble: no blood brain barrier
•Bioavailabilty: small

Side Effects:
•Respiratory depression
•Constipation
•Urinary Retention
•Orthostatic hypotension
•Emesis
•Cough suppression
•Tolerance/dependence

Question 4

fentanyl

Answer 4

• Duragesic patch, Actiq lollipop, Fentora, Onsoils, Subsys, lazanda
• 100 times strong as Morphine (mcg)
• Patches: elderly, forgetful, remove old, change q 3 days
• Lozenges: usually cancer, quick onset

Question 5

Meperidine: demerol

used in labor and delivery

Answer 5

• Short half life
• Many interactions
• Toxic if accumulation occurs
• Not drug of choice except early labor
• Contraindicated in gallbladder disease

Question 6

methadone

Answer 6

This is a opioid but doesnt not cause high, thats why its used in tx for addiction to trick body and not cause withdrawl

•Use:
–Addiction:
•40 mg wafers
•Occupies the receptors
•Avoid withdrawal

–Pain
•10 mg tablets
•Use small dose increases : avoid toxicity

• Narrow therapeutic window
• Long acting: OD tx must be prolonged
• Narcan not good antagonist

Question 7

hydromorphone

Answer 7

• Analgesia, sedation, euphoria
• Side effects: respiratory depression, constipation, Urinary retention, cough suppression
• Less analgesia/sedation than Morphine
• Lower abuse potential than Morphine

Question 8

codein

Answer 8

• 10% converts in Liver to Morphine
• Treats: Pain and cough suppression
• Oral: combined with APAP for potentiation affect
• 30 mg = 325 mg APAP (effect)

Question 9

Oxycodone (oxycontin)

Answer 9

•Efficacy equals codeine
•Short and long acting
•Short: Percocet (oxy + APAP), Percodan (oxy)
•Long: Oxycodone:
–30% immediate dump
–High risk of abuse
–Difficult to crush

Question 10

non opioid central acting analgesics

Question 11

tramadol

Answer 11

• Schedule IV (book is wrong)
• Both opioid and non-opioid actions
• Interactions: CNS depressants
• Suicidal Ideations
• Immediate release: tramadol
• Long Acting: Ultram

Question 12

clonidine

Answer 12

uses:
•Hypertension/pain

• Alpha2adrenergic agonist
• Adjunct therapy with Opioids
• CV side effects: severe hypotension, rebound hypertension, bradycardia