Exam 3 - Lecture 31, Opioids Flashcards by Patryk Lasiuk

OUD

Opioid use disorder, based on DSM

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Abstinence syndrome…

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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Withdrawal syndrome

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

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Time course: Precipitated withdrawal

occurs within minutes of antagonist admin and lasts only 2 hours

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Time course: Abstinence syndrome

after discontinuation of opioid admin is protracted

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

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

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

restless sleep (yen)

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Time course of withdrawal after last dose: 20 hours

goose-flesh, mydriasis, agitation, tremors

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

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

Withdrawal syndrome complete

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If give Single adequate dose opioid agonist in withdrawal process…

drug will abruptly terminate above symptoms and restore “normalcy”

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Morphine

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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Codeine (methylmorphine)

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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Tramadol (Ultram)

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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hydromorphone (Dilaudid)

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

Widely prescribed, high abuse potential

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Heroin (diacetylmorphine)

Preferred by addicts, must euphoric

High abuse

Not legally made in US

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Hydrocodone

found in Hycodan, Vicodin, Zohydro

Oxycodone

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

m receptor agonist, Adverse effects with acute use

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

m receptor agonist, Adverse effects with chronic use

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

Meperidine (Demerol, Dolantin)

“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

Fentanyl (Duragesic, Atiq)

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

Can cause fatal hypoventilation in children and adults

Duragesic

Transdermal version of fentanyl used as means for chronic pain control

Actiq

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

Sufentanil (Sufenta)

5-10 times more potent than fentanyl used in anesthesiology by IV or epidural route

Alfentanil (Alfenta)

Less potent but faster acting fentanyl, short duration Used as IV anesthetic

Remifentanil (Ultiva)

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

Diphenoxylate (Lomotil, combined with atropine)

Constipating effect predominant Used to treat diarrhea Add atropine to deter abuse

Loperamide (Imodium)

Anti-diarrheal agent but not combo with atropine Lower abuse potential than diphenoxylate

Methadone

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

Dextromethorphan

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

Pure opioid antagonist

No intrinsic activity Naloxone (Narcan) Naltrexone (Revia)

Opioid agonist - antagonist

kappa agonist, weak mu antagonist Nalorphine Pentazocine Butorphanol Nalbuphine

Partial mu agonist and kappa antagonist

Buprenorphine

Mixed agonist/antagonist

acts as agonists and antagonists but at different receptors

Naloxone

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

Naltrexone

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

Pentazocine

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

Butorphanol

similar to pentazocine but lower psychotomimetic side effects analgesic, relief of acute pain nasal form for sever headaches Kappa agonist, weak mu antagonist

Buprenorphine

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