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ORD Exam 1 > Narcotic Pharmacology > Flashcards

Narcotic Pharmacology Flashcards

1
Q

Three endogenous opioid receptors and transmitters:

A

Mu Receptor: Endorphins
Delta Receptor: Enkephalins and Endorphins
Kappa Receptor: Dynorphins

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2
Q

Mu receptor actions:

A
  • Good for acute pain
  • Strongest response
  • Spinal and Supraspinal Analgesia
  • Slow GI transit
  • Hormone release
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3
Q

Delta receptor actions:

A
  • Spinal and supraspinal analgesia

- Hormone release

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4
Q

Kappa receptor actions:

A
  • Only good for low level background pain not acute
  • Spinal and supraspinal analgesia
  • Psychomimetic -> Dysphoric Pain relief not euphoric
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5
Q

Endorphin Functions:

A
  • Modulate pain impulse in periphery
  • Stimulate release of ADH, prolactin, ACTH and GH
  • Inhibit release of LH, FSH, thyrotropin
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6
Q

Opiate receptors:

A
  • All are GPCR
  • Reduce inward Ca current
  • cAMP formation activating PKA
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7
Q

Morphine:

A
  • Opiates
  • Act on Mu Delta and Kappa
  • Central actions and peripheral actions
  • Sedation in humans
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8
Q

Peripheral Actions of Morphine (opiate): Cardiovascular system

A

-Mu receptor -> Bradycardia reduced preload and reduced dyspnea with pulmonary edema

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9
Q

Peripheral Actions of Morphine (opiate): Mast cells

A

-Histamine release from Mast Cells -> Transient hypotension and pruritus

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10
Q

Peripheral Actions of Morphine (opiate): GI tract

A

-Constipation, increased resting tone, decreased propulsive movement

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11
Q

Peripheral Actions of Morphine (opiate): Brain Biliary Urinary Lungs

A
  • Decreased breathing rate -> increased pCO2 -> brain vessels dilate -> increase in intracerebral pressure
  • Biliary tract spasm
  • Urethral and Ureter spams
  • Urinary retention
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12
Q

Morphine (opiate) respiratory suppression:

A

1st. ) Upper voluntary respiratory centers blocked
2nd. ) CO2 drive suppressed
3rd. ) O2 drive suppressed

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13
Q

Why do you not give oxygen to a patient with morphine O2 drive suppression?

A

The only reason they continue to breath is due to the oxygen drive, if you give them oxygen they will stop breathing on their own

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14
Q

What reverses the reduced preload and after load due to narcotics?

A

Naloxone -> Mu receptor inverse agonist (binds to the Mu receptor but instead of activating it, it causes the complete opposite reaction than normal agonists)

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15
Q

Narcotics to treat diarrhea:

A
  • Loperamide

- Diphenoxylate

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16
Q

Loperamide:

A
  • Diarrhea treatment
  • Does not achieve significant CNS levels
  • Only exposure is in the GI tract
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17
Q

Diphenoxylate:

A
  • Diarrhea treatment
  • Contains atropine
  • Atropine makes you sick to reduce addiction or abuse
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18
Q

Narcotic Analgesic Groups:

A
  • Morphine-like
  • Methadone
  • Phenylpiperidines (most effective)
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19
Q

Morphine-Like Structure Drugs: Opiates

A
  • Morphine
  • Hydromorphine
  • Oxomorphone
  • Codeine
  • Hydrocodone
  • Oxycodone
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20
Q

Tincture Opiates:

A
  • Laudanum (stonger)

- Paregoric

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21
Q

Hydromorphone:

A

Stronger than morphine

22
Q

Oxycodone/Hydrocodone:

A

More potent than morphine and longer half-life

23
Q

Codeine:

A
  • Less potent than morphine

- Body converts codeine to morphine

24
Q

Morphine Metabolism:

A

First pass of liver

25
Q

Methadone-like drugs: opiods

A
  • Methadone

- Diphenoxylate

26
Q

Methadone:

A
  • Slower progression of tolerance

- Less severe immediate physical withdrawal symptoms

27
Q

Diphenoxylate:

A
  • Contains atropine

- Antidiarrheal

28
Q

Fentanyl-Like: Opiods

A
  • Fentanyl
  • Remifentanil
  • Meperidine
  • Diphenoxylate
  • Loperamide
29
Q

Fentanyl:

A

Way more potent than morphine

30
Q

Remifentanil:

A
  • Short acting drug

- Used Post-Surgery

31
Q

Meperidine:

A
  • Anticholinergic
  • Can cause grand mal seizures
  • DRUG INTERACTIONS with MAO Inhibitors and SSRI
32
Q

Mixed Agonist-Antagonist Actions:

A
  • Mixed narcotic agonists of kappa receptors
  • Partial narcotic agonists or antagonist of mu receptors
  • Not effective pain relievers and will precipitate withdrawal
33
Q

Mixed Agonist-Antagonist Use:

A
  • Short term pain relief

- Not as much respiratory depression

34
Q

What are Mixed Agonist-Antagonists reversal resistant to?

A

Naloxone and other Mu-receptor antagonists bc they

35
Q

Morphine like Mixed agonist antagonists:

A
  • Nalbuphine

- Buprenorphine

36
Q

Other Mixed agonist antagonists:

A
  • Butorphanol

- Pentazocine

37
Q

Buprenorphine:

A
  • Partial agonist at mu receptor

- Binds and unbinds slowly from mu receptor

38
Q

Nalbuphine:

A
  • Less effect on respiratory depression
  • Precipitates acute withdrawal in physically dependent patients (mu antagonist)
  • Significant analgesia mediated through kappa receptor
39
Q

Tramadol:

A
  • Weak mu receptor agonist

- Inhibits reuptake of serotonin and norepinephrine in the braine

40
Q

Tapentadol:

A
  • Weak mu agonist

- Inhibits reuptake of norepinephrine in the brain

41
Q

Antitussives:

A
  • Codeine
  • Dextromethorphan
  • Benzonatate
42
Q

Codeine:

A
  • Mu mediated action

- NOT for children under 6

43
Q

Dextromethorphan:

A
  • Weak mu agonist
  • NOT for children under 6
  • NOT combined with SSRI or MAO
  • NMDA receptor agonist -> Dysphoria and Seizures
  • NOT NALOXONE reversible
44
Q

Benzonatate:

A
  • Not an Opiate
  • Local anesthetic
  • NOT for children under 6
45
Q

Treatment as antitussive for children under 6:

A

Teaspoon of honey

46
Q

Pure Mu Receptor Narcotic Antagonists:

A
  • Naloxone
  • Naltrexone
  • Methylnaltrexone
  • Alvimopan
47
Q

Naloxone:

A

Short acting

48
Q

Naltrexone:

A
  • Long acting

- Used for long term treatment of narcotic nicotine and ETOH dependence

49
Q

Methylnaltrexone and Alvimopan:

A
  • Used for mu receptor mediated constipation

- Dose not pass BBB so it does not affect analgesic affects in the brain

50
Q

Narcotic withdrawal symptoms:

A
  • Complete opposite of the initial effects of the drugs

- Urinary retention is the only symptom that occurs in withdrawal and initial drug use

51
Q

Tolerance:

A
  • Initially regulated by G protein -> deactivate opioid receptors, Arrestin activation
  • Later on is alteration of neurotransmitters

ORD Exam 1 (10 decks)

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