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Pharm 3 > E1: Opiods > Flashcards

E1: Opiods Flashcards

1
Q

What are the endogenous opioid peptides?

A

Enkephalines, beta-endorphin, and dynorphin

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2
Q

How do beta-endorphins work?

A

Decreased pain transmission in the spinal cord and facilitate dopamine in reward system, causing euphoria

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3
Q

How do enkephalins work?

A

Decrease pain transmission in the spinal cord

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4
Q

How do dynorphins work?

A

Binds to Kappa receptors, may produce analgesia

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5
Q

What are the main effects of opioids?

A

Analgesia, sedation, euphoria, dysphoria

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6
Q

What receptors are involved in dysphoria?

A

Kappa and delta

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7
Q

What opioids are used for cough? Which does NOT suppress cough?

A
  • Codeine and dextromethorphan (no analgesia) used for cough
  • Meriperidine doesn’t suppress cough
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8
Q

What are the adverse effects of opioids?

A
  • Nausea and vomiting
  • Constipation
  • Urinary retention
  • itching
  • respiratory depression
  • postural hypotension
  • restlessness
  • dysphoria
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9
Q

Although tolerance developed to opioids, what effects of opioids do patients NOT become tolerant to?

A

Mitosis, constipation, and seizures

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10
Q

What can you use to reduce the symptoms of opiate withdrawal?

A

Clonidine or another opioid such as methadone

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11
Q

What is the treatment for opioid overdose?

A
  • Support respiration

- Narcan

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12
Q

What are the contraindications to opioids?

A
  • Use of a partial agonist with a full agonist
  • Head injuries
  • Pregnancy
  • impaired pulmonary function
  • impaired hepatic or renal function
  • some endocrine diseases
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13
Q

What is the MOA of morphine?

A

Strong agonist that stimulates all opioid receptors

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14
Q

How is Morphine metabolized?

A
  • In the liver by CYP2D6

- high first pass metabolism when injected

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15
Q

What are the side effects of morphine?

A

May cause itching or vomiting when injected due to histamine release

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16
Q

What is morphine metabolized to?

A

It is conjugated or glucuronide compounds

  • Morphine-6- glucuronide is potent analgesic
  • Morphine-3-glucuronide may cause adverse effects if it accumulates
17
Q

What is the MOA of Methadone?

A
  • Stimualtes mu receptors

- ma also block NMDA receptors and inhibit NE/Serotonin reuptake

18
Q

What is the use of methadone?

A
  • Traditionally used for maintenance treatment of addicts

- now commonly used in long term control of pain

19
Q

How long should Meperidine be used and why?

A
  • Should NOT be used for more than 48 hours in high doses or in renal failure due to accumulation of the metabolite normeperidine
  • Normeperidine can cause seizures
20
Q

What kind of drug should NOT be given with Meriperidine?

A

MAOIs- may cause serotonin syndrome

21
Q

What is the duration of action of methadone?

What about morphine/dilaudid?

A

Methadone: long

Morphine/dilaudid: 4-6 hours, fairly short half life

22
Q

What is the duration of action of Fentanyl?

A

-Short, which is why it has a high abuse potential

23
Q

What may fentanyl cause when given IV?

A

Truncal rigidity

24
Q

How is Fentanyl metabolized?

A

CYP3A4

25
Q

What is hydrocodone often combined with?

A

Tylenol

26
Q

Why doesn’t hydrocodone work well for patients taking SSRIs?

A

Hydrocodone requires conversion by CYP2D6 for some of the analgesic effect, and some SSRIs are CYP inducers

27
Q

Which opioids are metabolized to their active form by CYP2D6?

A

Codeine, oxycodone, and hydrocodone

28
Q

What is the MOA of Pentazocine/Naloxone?

A
  • Kappa receptor agonist

- Mu receptor partial agonist

29
Q

What are the potential side effects of Pentazocine/Naloxone?

A
  • Less sedating than other opioids
  • less respiratory depression and GI effects of other opioids
  • may cause dysphoria
30
Q

What is the MOA of Buprenorphine?

A

-Partial agonist of mu and maybe kappa

31
Q

What is the use of Buprenorphine?

A
  • Used for maintenance treatment of opioid addiction, decreases craving
  • combined with Naloxone
32
Q

What is the MOA of Tramadol?

A
  • weak mu agonist

- inhibits NE/serotonin ic reuptake

33
Q

What drugs cannot be combined with tramadol and why?

A
  • Antidepressants: seizures

- MAOIs, TCAs, SSRIs: may cause serotonin syndrome

34
Q

What is the MOA of Dextromethorphan?

A
  • Blocks NMDA receptors

- Decreases serotoninc reuptake: serotoninc syndrome with MAOIs

35
Q

What is Dextromethorphan used for?

A
  • Often combined with guafenisen for cough suppressant

- not an analgesic

36
Q

What drugs may precipitate withdrawal in opioid dependent individuals?

A

Opioid antagonists

37
Q

What is the DOC of opioid overdose?

A

Naloxone

38
Q

What is the used of Naltrexone?

A
  • used in treatment of opioid addicts, especially health care professionals
  • long acting preparation injected to treat addiction, but results may be better with Buprenorphine/Naloxone
  • will precipitate withdrawal in patients dependent on opioids

Pharm 3 (20 decks)

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