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Pharmacology and Medical Chemistry I > Exam 3 - Lecture 31, Opioids > Flashcards

Exam 3 - Lecture 31, Opioids Flashcards

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1
Q

OUD

A

Opioid use disorder, based on DSM

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2
Q

Abstinence syndrome…

A

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

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3
Q

Withdrawal syndrome

A

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

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4
Q

Time course: Precipitated withdrawal

A

occurs within minutes of antagonist admin and lasts only 2 hours

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5
Q

Time course: Abstinence syndrome

A

after discontinuation of opioid admin is protracted

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6
Q

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

A

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

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7
Q

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

A

restless sleep (yen)

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8
Q

Time course of withdrawal after last dose: 20 hours

A

goose-flesh, mydriasis, agitation, tremors

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9
Q

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

A

Peak of withdrawal symptoms

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

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10
Q

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

A

Withdrawal syndrome complete

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11
Q

If give Single adequate dose opioid agonist in withdrawal process…

A

drug will abruptly terminate above symptoms and restore “normalcy”

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12
Q

Morphine

A

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

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13
Q

Codeine (methylmorphine)

A

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

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14
Q

Tramadol (Ultram)

A

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

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15
Q

hydromorphone (Dilaudid)

A

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

Widely prescribed, high abuse potential

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16
Q

Heroin (diacetylmorphine)

A

Preferred by addicts, must euphoric

High abuse

Not legally made in US

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17
Q

Hydrocodone

A

found in Hycodan, Vicodin, Zohydro

18
Q

Oxycodone

A

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

19
Q

m receptor agonist, Adverse effects with acute use

A 
Respiratory depression
Nausea and vomiting
Pruritus
Urticaria
Constipation
Urinary retention
Delirium
Sedation
Myoclonus
Seizures
20
Q

m receptor agonist, Adverse effects with chronic use

A 
Hypogonadism
Immunosuppresion
Increased feeding
Increased Growth hormone secretion
Withdrawal effects
tolerance, dependence
Abuse, addiction
Hyperalgesia
Impairment while driving
21
Q

Meperidine (Demerol, Dolantin)

A

“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

22
Q

Fentanyl (Duragesic, Atiq)

A

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

Can cause fatal hypoventilation in children and adults

23
Q

Duragesic

A

Transdermal version of fentanyl used as means for chronic pain control

24
Q

Actiq

A

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

25
Q

Sufentanil (Sufenta)

A

5-10 times more potent than fentanyl

used in anesthesiology by IV or epidural route

26
Q

Alfentanil (Alfenta)

A

Less potent but faster acting fentanyl, short duration

Used as IV anesthetic

27
Q

Remifentanil (Ultiva)

A

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

28
Q

Diphenoxylate (Lomotil, combined with atropine)

A

Constipating effect predominant

Used to treat diarrhea

Add atropine to deter abuse

29
Q

Loperamide (Imodium)

A

Anti-diarrheal agent but not combo with atropine

Lower abuse potential than diphenoxylate

30
Q

Methadone

A

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

31
Q

Dextromethorphan

A

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

32
Q

Pure opioid antagonist

A

No intrinsic activity

Naloxone (Narcan)
Naltrexone (Revia)

33
Q

Opioid agonist - antagonist

A

kappa agonist, weak mu antagonist

Nalorphine
Pentazocine
Butorphanol
Nalbuphine

34
Q

Partial mu agonist and kappa antagonist

A

Buprenorphine

35
Q

Mixed agonist/antagonist

A

acts as agonists and antagonists but at different receptors

36
Q

Naloxone

A

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

37
Q

Naltrexone

A

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

38
Q

Pentazocine

A

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

39
Q

Butorphanol

A

similar to pentazocine but lower psychotomimetic side effects

analgesic, relief of acute pain

nasal form for sever headaches

Kappa agonist, weak mu antagonist

40
Q

Buprenorphine

A

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

Pharmacology and Medical Chemistry I (30 decks)

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