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Intro to Principles of Drug Action > Pharmacology of Opioid > Flashcards

Pharmacology of Opioid Flashcards

1
Q

What opioids are considered to be in the class “high efficacy analgesics” (strong agonist)?

A

-morphine
-fentanyl
-methadone
-meperidine
-oxycodone
-hydromorphone

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2
Q

What opioids are considered to be in the class “low-medium efficacy oral analgesics” (mild-moderate agonist)?

A

-codeine
-hydrocodone
-tramadol

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3
Q

What opioids are considered to be in the class “mixed receptor agonist/antagonist”?

A

-buprenorphine
-nalbuphine

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4
Q

What drugs are opioid antagonist?

A

-naloxone
-naltrexone

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5
Q

What drug are non-analgesic opioids?

A

-dextromethorphan
-loperamide

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6
Q

What are the therapeutic effects of opioids?

A

-analgesia (pain relief)
-cough suppression (mediated by DM receptors- not opioids)
-anesthesia
-sedation
-euphoria
-diarrhea treatment
-acute pulmonary edema

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7
Q

Define: Equi-analgesia

A

all “full-agonists” (high efficacy) can achieve same maximal effect if dose is adjusted for binding affinity and route administration. morphine milligram equivalents (MME) is used to calculate and compare total daily dose of opioids (1mg morphine/day= 1MME)

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8
Q

How do opioids cause analgesia?

A

-increase the pain threshold
-increase the pain tolerance

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9
Q

Describe: Methadone

A

long-acting, replacement therapy to treat heroin addiction

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10
Q

Describe: Meperidine

A

short-term therapy (<48 hours) due to toxic metabolite

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11
Q

What are the indications of high efficacy opioid analgesics?

A

-severe pain
-adjunct in anesthesia (fentanyl, morphine)
-pulmonary edema (morphine only)

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12
Q

What are the indications of low-medium efficacy opioid analgesics?

A

-mild-moderate pain
-cough suppression (codeine)

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13
Q

Describe: Codeine

A

used for anti-tussive and anti-diarrheal effects (usually, not for pain)

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14
Q

Describe: Tramadol

A

also blocks reuptake of NE or serotonin

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15
Q

Describe: Buprenorphine

A

partial agonist at mu and antagonist at kappa, longer duration of action(4-8h), commonly paired with naloxone (suboxone) for treatment of opioid addiction

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16
Q

Describe: Nalbuphine

A

agonist at kappa receptors and antagonist at mu, commonly used to reverse pruritis (itchy skin) that is a side effect of opioid agonists

17
Q

What are the indications of mixed agonist/antagonist?

A

moderate pain

18
Q

What is the cause of death from an opioid overdose?

A

respiratory depression

19
Q

What are the symptoms of opioid overdose?

A

the triad: coma, respiratory depression, pinpoint pupils

20
Q

Contraindications: Opioids

A

-impaired pulmonary function= may exacerbate symptoms
-head injuries
-pregnancy
-substance abuse history
-impaired hepatic/renal function
-use caution when combining with sedative-hypnotics or antipsychotic tranquilizer

21
Q

What is the main route of metabolism for opioids?

A

glucuronidation and demethylation in the liver

22
Q

What is the duration of action of opioids?

A

3-4 hours

23
Q

What is the antidote for opioid overdose?

A

opioid antagonists

24
Q

What drugs are opioid antagonists?

A

-naloxone (Narcan)
-naltrexone

25
Q

Describe: Naloxone

A

-opioid antagonist
-duration of action= 1-2 hours, may need to repeat doses when treating an overdose, can be administered: (injection (healthcare professional), auto injector, nasal spray(Narcan) (OTC))

26
Q

What drugs are peripherally-acting mu-opioid receptor antagonists?

A

-methylnaltrexone
-alvimopan
-naloxegol
-naldemedine

27
Q

What is the clinical use of peripherally-acting mu-opioid antagonists?

A

opioid induced constipation

28
Q

What can induce opioid withdraw?

A

-stopping opioid doses
-antagonists (ex naloxone)
-mixed agonist/antagonists (ex buprenorphine)

29
Q

What is the timeline of opioid withdraws?

A

begins 6-10h after last dose, peak at 36-48 hours, and subsides in 5-7 days- not life threatening, but very uncomfortable

30
Q

What are the symptoms of opioid withdraw?

A

-early symptoms= “flu-like”, watery eyes, runny nose, yawning, goosebumps
-late symptoms= restlessness and irritability, nausea and vomiting, increase heart rate and blood pressure, chills and sweating, muscle aches, diarrhea, mydriasis (pupil dilation), drug cravings

31
Q

What are symptoms of opioid withdrawal in neonates?

A

-blotchy skin coloring
-diarrhea
-excessive or high pitched crying
-rapid breathing
-poor feeding
-sleep problems

32
Q

Describe: Naltrexone

A

-opioid antagonist
-long duration of action (>10h)

33
Q

Describe: Methadone

A

-slow acting mu-opioid agonist
-long duration of action (t1/2= 4-130h)= daily dosing at a clinic
-replacement therapy

34
Q

Describe: Buprenorphine

A

-partial agonist of mu receptors, antagonists at kappa and delta (less efficacious than morphine)
-replacement therapy
-long duration of action (t1/2=40h)

35
Q

What type of pain can opioids treat?

A

-nociceptive pain (associated with injury and/or inflammation)
-acute nociceptive pain (use with chronic pain is associated with tolerance and dependence)
-cancer pain

36
Q

What are the CDC Guidelines for use of opioids for chronic pain?

A
  1. opioids are not first-line or routine therapy for chronic pain
  2. establish goals
  3. discuss benefits and risks and availability of nonopioid therapies
  4. use immediate-release opioids when starting
  5. prescribe no more than needed
  6. do not prescribe ER/LA opioids for acute pain
  7. follow-up and re-evaluate risks and reduce dose or taper to discontinue if needed
  8. check PDMP for high dosages and prescriptions from other providers
  9. use urine testing
  10. avoid using benzodiazepines with opioids
  11. arrangement treatment for opioid use disorder if needed
37
Q

What signaling proteins are activated when opioid agonists bind to mu receptors?

A

G(i/o) signaling pathway which is responsible for pain-relieving effects and beta-arrestin that is responsible for the unwanted side effects: euphoria (addiction), respiratory depression, and gastrointestinal effects

38
Q

Describe: Oliceridine (Olincyk)

A

-MOA: selective full agonist at mu receptors, suggested it could be a biased agonist
-indication: acute severe pain for when IV analgesics are required but alternative treatment is inadequate

Intro to Principles of Drug Action (11 decks)

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