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Pharmacology Block 3 > Opiods > Flashcards

Opiods Flashcards

1
Q

What pathway inhibits the spinothalamic tract, causing pain relief?

A

Periaqueductal Grey - inhibits the ascending pathway

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2
Q

The Kappa receptor binds what endogenous opoid?

A

Dynorphin

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3
Q

What endogenous opoids bind the Mu-receptor?

A

Enkephalin and B-endorphin

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4
Q

What does the peptide pro-opoidmelanocortin get cleaved into?

A

B-endorphin and ACTH

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5
Q

What does the delta receptor bind?

A

Enkephalins

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6
Q

What receptor does Morphine bind to and what are secondary messengers?

A

Morphine binds the Mu-receptor, activating Gi-coupled receptor decreasing cAMP, decreasing Ca+2, inhibiting neurotrasmitter release of ascending tract.

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7
Q

What are the two most important qualities of an opoid dictating their effectiveness?

A

Lipophilicity and Elimination

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8
Q

Which two opoids are considered prodrugs?

A

Herion and Codeine

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9
Q

What are common effects of opiods?

A
  • Analgesia
  • Cough Suppresion
  • Decreases GI Motility
  • Euphoria
  • Endocrine Effects, increased ADH and decreased LH
  • Pupillary Constriction - no tolerance
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10
Q

What is the most concerning side effect of Opoids?

A

Respiratory Depression

  • decreases sensitivity of chemoreceptors
  • additive with other depressing drugs
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11
Q

Why would giving Morphine to someone with Gall stones cause them more pain?

A

Due to opoids ability to tighten sphincter tone.

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12
Q

Why would it be beneficial to give opoids to an individual who is having an MI?

A

Opoids decrease the myocardial oxygen demand, helping when there is ischemia occurring.

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13
Q

What are the effects of the Mu-receptor, other than inhibition of ascending pain pathways?

A

Decrease GI Motility
Decrease LH release
Increase ADH release
Induce Nausea in the postrema area of brain

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14
Q

What would you have to do if you were prescribing a pain-relieving dose of Morphine to a patient from IV to PO usage?

A

Multiple it by 3x, because the bioavailability is 1/3 of ingested dose.

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15
Q

What opoids work on the Mu-receptor?

A

Morphine, Heroin, Codeine, Oxycodone, Hydrocodone, Methadone, Meperidine, and Fentanyl

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16
Q

What drug has the highest abuse potential and is more lipophilic compared to Morphine?

A

Heroin

17
Q

What opoid is a prodrug that is converted to Morphine and typically used in combination with Acetaminophen?

A

Codeine – typically more mild-moderate pain

18
Q

What opoids are used for moderate-severe pain, usually combined with Tylenol?

A

Oxycodone and Hydrocodone

19
Q

What opiod is used to treat chornic pain and/or opiod abuse?

A

Methadone - equal to morphine, longer duration and better bioavailability

20
Q

What opiod is similar potency to Morphine, but has a shorter lasting effects and toxic metabolites?

A

Meperidine, toxic metabolites and interacts with MAO inhibitors.

21
Q

What short acting opiod is used in transdermal patches for long lasting pain relief?

A

Fentanyl

22
Q

What is an opiod that is about 2-3x more potent than Morphine?

A

Hydromorphone

23
Q

What opiod is mix-action, Mu-antagonist and a Kappa-agonist?

A

Nalbuphine - can cause withdrawal symptoms in dependent patients. Minimal euphoria. IV use only.

24
Q

What opiod can be combined with Naloxone to treat opiod dependence?

A

Buprenorphine

25
Q

Alone what kind of effects does Buprenorphine have?

A

Partial Mu-agonist, used for moderate-severe pain. Less dependence forming.

26
Q

If a patient overdosed on opiods what can reverse the effects immediately?

A

Naloxone

27
Q

How does Naloxone work?

A

High Affinity for Mu-receptor - antagonist preventing effects. Short duration.

28
Q

What is a long acting drug used for opiod and alcohol abuse?

A

Naltrexone

29
Q

What is a NMDA receptor antagonist that is a cough suppressant?

A

Dextromethorphan

30
Q

What does Tramadol do and what is it used for?

A

Tramadol is a weak Mu-receptor agonist and blocks NE/Serotonin uptake. Mild-moderate pain.

31
Q

If you are tolerate to one Mu-agonist how are the other opiod Mu-agonists effected?

A

All Mu-agonists undergo tolerance. Cross Tolerant.

32
Q

What effects do patient’s become tolerant of first?

A

nausea/vomiting.

Then gradually, pain relief, euphoria, respiratory depression, and endocrine effects

33
Q

What effects are unphased by tolerance?

A

Miosis and Constipation (Suppressed GI-motility)

34
Q

What are the symptoms of Opiod withdrawal?

A

First - restlessness, sweating, yawning
Second - piloerection, involuntary movements, n/v, depression
End effects, restless sleep and hyperactivity
Takes 7-10 Days Total - Nonlethal

Pharmacology Block 3 (19 decks)

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