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Neuro II > Opioid Narcotics > Flashcards

Opioid Narcotics Flashcards

1
Q

In general, how do opioids cause their effect on the pre and post synaptic neurons and what does this result in?

A

Pre-> blunt Ca2+ influx into cells
Post-> drive K+ out of cells

Results in decrease glutamate release

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2
Q

What is unique to Buprenorphrine compared to fentanyl and morphine?

A
  • partial agonist, where as the other two are full agonists

- more potent!!

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3
Q

What is the clinical utility of mu receptor agonists?

A

Analgesia (tissue injury=acute injury > nerve injury)

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4
Q

What are the common effects by Mu agonist stimulation?

A

Analgesia, CNS and respiratory depression, miosis, constipation.

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5
Q

What type of patients is the use of morphine contraindicated in and why?

A

Brain injury and emphysema patients. Morphine depresses respiration and decrease sensitivity to [CO2]

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6
Q

Name the six group 1 full agonists

A

Morphine, Methadone, Meperidine, Hydromorphone, Oxymorphone, Levorphanol

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7
Q

Name the three group 2 short-acting full agonists

A

Fentanyl, Sulfentanil, Remifentanyl

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8
Q

Name the two group 3 codeine-related agonists

A

Hydrocodone, oxycodone

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9
Q

What must a physician be aware of when switching a patient from a parenteral opioid to an oral form?

A

Bioavailability and Potency.

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10
Q

How is morphine metabolized?

A
  • Strong first pass effect.
  • Inactive metabolite–> Normophine by CYP3A4
  • Active metabolite–> M-3 and M-6 Glucouronamide by UGT 1A1/ 2B7
    - -> Hydromorphone by dehydrogenase enzyme
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11
Q

What are the characteristics of Methadone?

A
  • Full Mu agonist
  • Loner t1/2 (about 27 hours)
  • Better oral absorption
  • useful for withdrawal/ maintenance, detoxification.
  • Can effect cardiac electrical conduction–> incrase QT interval.
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12
Q

What are the characteristics of Meperidine?

A
  • Eye–> pupil dilation (difficult to detect abusers)

- Toxic metabolite Normeperidine accumulates and can cause seizure activity.

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13
Q

What are the characteristics of Sulfentanil?

A
  • Short-acting full agonist

- binds all three opioid receptors

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14
Q

What are the characteristics of Remifentanyl?

A
  • Very short acting
  • Metabolized by plasma and tissue esterases.
  • Used in OBGYN for birth
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15
Q

What are the characteristics of Fentanyl?

A
  • Rapid onset and distribution (lipophilic)
  • Short duration of action
  • Transdermal and transmucosal administration
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16
Q

What are the characteristics of Codeine?

A
  • Partial agonist
  • reliable oral absorption
  • analgesia for moderate pain
  • anti-tussive- cough relief (Mu-independently)
17
Q

What is the metabolism of codeine?

A

Codeine–> morphine via CYP2D6, active metabolite. Plus inactive norcodeine.

18
Q

What must be considered when giving kids codeine?

A

-the possibility that they are ultra-fast metabolizers. This can lead to fatal respiratory depression.

19
Q

What are the active metabolites of heroin and codeine?

A

Morphine

20
Q

What is the active metabolite of oxycodone?

A

Oxymorphone

21
Q

What is the active metabolite of meperidine?

A

Normeperidine, which is toxic.

22
Q

What are the active metabolites of Hydromorphone, Oxymorphone, and Fentanyl?

A

There are none.

23
Q

What opioids can be used in the GI tract as anti-diarrheals?

A
  • Loperamide and Diphenyoxylate.

- Any opioid can be used but these have poor solubility and low risk for abuse.

24
Q

What are the characteristics of Tramadol?

A
  • Moderate Mu agonist
  • Active metabolite is N-desmethyl
  • Reliable oral absorption
  • Inhibits catecholamine reuptake
  • associated with seizures
25
Q

What are the characteristics of Pentazocine?

A
  • Mixed kappa and mu agonist, delta antagonist
  • supra-spinal analgesia
  • side effects includ tachycardia and hallucinations
26
Q

What are the characteristics of Buprenorphrine?

A
  • Mu partial agonist/ kappa and delta antagonist
  • used for analgesia
  • can precipitate withdrawal in abusers
27
Q

What is characteristic of opioid overdose?

A

-decreased respiration

28
Q

What is the treatment for opioid overdose?

A

1) IV Naloxone (Mu receptor antagonist)

2) Naltrexone PO (has long duration of action)

29
Q

What opioid agonst can be used post-operatively to treat pain without causing constipation and putting the patient at risk for obstruction?

A

Methylnaltrexone

Neuro II (6 decks)

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