Exam 3 - Lecture 31, Opioids

Question 1

OUD

Answer 1

Opioid use disorder, based on DSM

Question 2

Abstinence syndrome…

Answer 2

Withdrawal of opioid drug or blockade of its action by antagonist results in reduction of opioid receptor stimulation

subsides when endogenous opioid system recovers normal function

Question 3

Withdrawal syndrome

Answer 3

Physiological features identical whiter they’re due to discontinuation of drug or due to antagonist admin

Question 4

Time course: Precipitated withdrawal

Answer 4

occurs within minutes of antagonist admin and lasts only 2 hours

Question 5

Time course: Abstinence syndrome

Answer 5

after discontinuation of opioid admin is protracted

Question 6

Time course of withdrawal after last dose: 6-10hrs

Answer 6

Lacrimation (watery eyes), rhinorrhea (runny nose), yawning, sweating

Question 7

Time course of withdrawal after last dose: 12 -14 hours

Answer 7

restless sleep (yen)

Question 8

Time course of withdrawal after last dose: 20 hours

Answer 8

goose-flesh, mydriasis, agitation, tremors

Question 9

Time course of withdrawal after last dose: 36 - 48hrs

Answer 9

Peak of withdrawal symptoms

Insomnia, chills, cramps, vomiting, diarrhea, leg cramps, sweating, elevated HR and BP, fluid depletion (can lead to death if severe)

Question 10

Time course of withdrawal after last dose: 5 - 10 days

Answer 10

Withdrawal syndrome complete

Question 11

If give Single adequate dose opioid agonist in withdrawal process…

Answer 11

drug will abruptly terminate above symptoms and restore “normalcy”

Question 12

Morphine

Answer 12

Available as morphine sulfate and morphine HCL

Analgesic dose 10mg/70kg im or sc provide analgesia for 70% patients

Orally only 1/6 - 1/15 as effective as im or sc

Question 13

Codeine (methylmorphine)

Answer 13

Oral potency is 2/3 of parenteral, so oral admin more practical than morphine

Lower analgesic potency than morphine but can be enhanced by combo with aspirin

Less abuse potential, slower tolerance develop, less sedation and GI effects than morphine

Used as analgesic and anti-tussive

Question 14

Tramadol (Ultram)

Answer 14

Synthetic codeine analog

Mechanism:
Blockade 5HT reuptake with weak m-opioid agonist

No respiratory depressant or Cardio effects

Side effects:
Seizures
Risk of 5HT syndrome

Question 15

hydromorphone (Dilaudid)

Answer 15

5 - 10 times more potent than morphine with greater respiratory depressant action

Widely prescribed, high abuse potential

Question 16

Heroin (diacetylmorphine)

Answer 16

Preferred by addicts, must euphoric

High abuse

Not legally made in US

Question 17

Hydrocodone

Answer 17

found in Hycodan, Vicodin, Zohydro

Question 18

Oxycodone

Answer 18

combined w/ aspirin = Percodan
combined w/ acetaminophen = Percocet

Often used in Slow-release form (Oxycontin) for chronic pain

subject to widespread abuse, addicts crush for rapid high

Question 19

m receptor agonist, Adverse effects with acute use

Answer 19

Respiratory depression
Nausea and vomiting
Pruritus
Urticaria
Constipation
Urinary retention
Delirium
Sedation
Myoclonus
Seizures

Question 20

m receptor agonist, Adverse effects with chronic use

Answer 20

Hypogonadism
Immunosuppresion
Increased feeding
Increased Growth hormone secretion
Withdrawal effects
tolerance, dependence
Abuse, addiction
Hyperalgesia
Impairment while driving

Question 21

Meperidine (Demerol, Dolantin)

Answer 21

“equianalgesic doses”

Less potent than morhpine, more rapid onset of analgesia and shorter duration

Less constipation and urinary retention than morphine

No anti-jussive action

Tolerance and physical dependence of opioid type do develop with chronic use

Sever reactions w/ patients taking MAOI

Question 22

Fentanyl (Duragesic, Atiq)

Answer 22

Very potent, used in neurolept analgesia or manage of severe, chronic pain in cancer patient

Can cause fatal hypoventilation in children and adults

Question 23

Duragesic

Answer 23

Transdermal version of fentanyl used as means for chronic pain control

Question 24

Actiq

Answer 24

lozenge that dissolves in mouth, used for break-through cancer pain

Question 25

Sufentanil (Sufenta)

Answer 25

5-10 times more potent than fentanyl

used in anesthesiology by IV or epidural route

Question 26

Alfentanil (Alfenta)

Answer 26

Less potent but faster acting fentanyl, short duration

Used as IV anesthetic

Question 27

Remifentanil (Ultiva)

Answer 27

rapid onset, 1-2 min after iv injection and short duration (5-10 min) due to rapid metabolism by tissue cholinesterase

approved for opioid anesthetic analgesia

Question 28

Diphenoxylate (Lomotil, combined with atropine)

Answer 28

Constipating effect predominant

Used to treat diarrhea

Add atropine to deter abuse

Question 29

Loperamide (Imodium)

Answer 29

Anti-diarrheal agent but not combo with atropine

Lower abuse potential than diphenoxylate

Question 30

Methadone

Answer 30

Extended duration of action (t1/2 = 15-40hrs), useful in maintenance therapy of individuals dependent on opioids

similar abuse potential to morphine

Uses:
Pain relief
Treat opioid abstinence symptom (suppress withdrawal)
“Maintenance therapy” of heroin addicts

Question 31

Dextromethorphan

Answer 31

Similar cough suppression as codeine with no analgesia or respiratory depression

No potential for abuse due to no opioid subjective effects

no cross tolerance morphine

suggests that receptors in cough suppression are different from those mediating other opioid effects

Question 32

Pure opioid antagonist

Answer 32

No intrinsic activity

Naloxone (Narcan)
Naltrexone (Revia)

Question 33

Opioid agonist - antagonist

Answer 33

kappa agonist, weak mu antagonist

Nalorphine
Pentazocine
Butorphanol
Nalbuphine

Question 34

Partial mu agonist and kappa antagonist

Answer 34

Buprenorphine

Question 35

Mixed agonist/antagonist

Answer 35

acts as agonists and antagonists but at different receptors

Question 36

Naloxone

Answer 36

Small dose reverse or prevent all opioid effects.

Uses include:
treat respiratory depression opioid OD
Diagnosis of physical dependence on opioids
treatment of compulsive opioid use

Question 37

Naltrexone

Answer 37

greater potency by oral route than naloxone

useful in treatment of opioid users who are motivated to stay off drugs but high likelihood of relapse

Suggested as treatment for treating alcohol abuse

Question 38

Pentazocine

Answer 38

Kappa agonist, weak mu antagonist

Made in attempt to make analgesic low abuse potential

Has moderate abuse potential, may precipitate withdrawal in opioid dependent individuals

Used clinically for its analgesic properties, especially in situations where risk of drug dependence argues against other opioids

Question 39

Butorphanol

Answer 39

similar to pentazocine but lower psychotomimetic side effects

analgesic, relief of acute pain

nasal form for sever headaches

Kappa agonist, weak mu antagonist

Question 40

Buprenorphine

Answer 40

Highly lipophilic, 25-50 times more potent than morphine as mu agonist but less efficacious

partial mu agonist, but can display antagonism when full agonist is present

produces morphine-like respiratory depression and analgesia but with “ceiling effect”

subject to abuse, stop after long use leads to withdrawal syndrome

used as analgesic and maintenance drug for opioid-dependent subjects

mixed with naloxone to prevent abuse

prevent craving other drugs ie alc or cocaine