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Owenpharm Block 3 > Opioids > Flashcards

Opioids Flashcards

1
Q
  1. What are the three major groups of endogenous opioid peptides and what are they pre-cursors?
  2. Where are the Leucine and Methionine Enkephalins dristibuted through CNS?
  3. Beta-endorphins come from where and are associated with what?
A
  1. Enkephalins (pre: proenkephalin), Endorphins (pre: proopiomelanocortin), Dynorphins (pre: prodynorphin)
  2. Widely distributed, especially in interneurons, including those associated with pain pathways
  3. Beta-endorphins occur in the hypothalamus and n. solitarius and pituitary. It is co-released with ACTH in response to stress.
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2
Q
  1. What is the endogenous ligand for the MU receptor?
  2. What is the endogenous ligand for the KAPPA receptor?
  3. What is the endogenous ligand for the DELTA receptor?
A
  1. MU: Enkephalins, B-endorphins
  2. KAPPA: Dynorphins
  3. DELTA: Enkephalins, B-endorphins
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3
Q
  1. What are the drug ligands for the MU receptor?
  2. What is the drug ligand for the KAPPA receptor?
  3. What is the drug ligand for the DELTA receptor?
A
  1. MU: Morphine, Fentanyl, Methadone, Meperidine, Buprenorphine
  2. KAPPA: Nalbuphine
  3. DELTA: NONE
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4
Q

What is the mechanism of action for morphine?

A

Morphine binds MU receptor → G-protein reduction in cAMP → blocks calcium entry and opens K+ channels → decreased Ca concentration decreases neurotransmitter release

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5
Q
  1. What receptors in what area of the brain might be involved in Opioid dependance?
  2. What may be responsible for the dysphoric actions of nalbuphine?
A
  1. MU and DELTA receptors in the limbic areas
  2. KAPPA receptors in the limbic structures
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6
Q
  1. What is referred to by “narcotic”?
  2. What is referred to by “opiate”?
A
  1. Any drug that produces a stuporous, sleep-like state & may or may not be analgesic.
  2. Drugs derived from opium or have a morphine-like pharmacological profile
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7
Q
  1. What is the relative oral absorption for morphine compared to IV?
  2. What affects the onset of action of opioids?
A
  1. Approximately 1/3
  2. Degree of lipophilicity (Heroin highly lipophilic)
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8
Q
  1. What is the difference between Morphine and Codeine?
  2. Why is Codeine less efficacious than Morphine?
  3. How is Heroin associated with Morphine?
A
  1. Codeine is a methylated pro-drug for Morphine.
  2. Not all of the Codeine is converted to Morphine but may still bind in the Codeine form
  3. It is diacetylmorphine and is converted to monoacetyl-morphine
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9
Q

How do opioids create cough suppression? Which drugs are commonly used for this?

A

They suppress brainstem cough centers (may not be mediated by opioid receptors)
Codeine and Dextromethorphan

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10
Q

How are opioids used for an antidiarrheal effect? What unwanted side effect is associated with this?

A

Peripheral MU receptors on GI nerves. Same effect can cause constipation.

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11
Q

Why do opiates cause nausea?

A

Stimulation of CTZ (chemoreceptor trigger zone) in area postrema. More significant effect when standing.

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12
Q

What are the endocrine effects of Opiates?

A
  1. Decreased LH release - MU mediated
  2. Increased ADH secretion - MU mediated
  3. Decreased ADH secretion - KAPPA mediated
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13
Q

Why do opiates cause miosis (pupillary constriction)?

A

They stimulate the Edinger-Westphal nucleus of the oculomotor nerve.
There is no tolerance to this effect.

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14
Q
  1. What is the oral to parenteral potency ratio of Morphine?
  2. What is the duration of analgesia for Morphine?
A
  1. 3-4 to 1 potency for oral to parenteral
  2. Duration of analgesia is 4-5 hours.
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15
Q
  1. What is the relative potency of Methadone?
  2. What is the relative duration of action?
  3. What is it primarily used for?
A
  1. Methadone is equipotent with morphine.
  2. It has a longer duration of action than morphine.
  3. It is used in the treatment of opioid abuse and chronic pain
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16
Q
  1. What is the relative potency of Fentanyl?
  2. What is the relative duration of action?
  3. How is it primarily available?
A
  1. Fentanyl is 100X as potent as morphine.
  2. It is short-acting - 1 to 1.5 hours
  3. It is available in injectable form and transdermal patch

(Considered “medical heroin”)

17
Q
  1. What is the relative duration of Meperidine?
  2. Why isn’t it used as much anymore?
A
  1. It has a shorter duration of analgesia than Morphine
  2. It forms a toxic metabolite that can accumulate with frequent use. It has significant interactions with MAO-I’s.
18
Q
  1. What is the indication for Codeine?
  2. How much Codeine is required to reach a Morphine like efficacy?
A
  1. Mild to moderate pain
  2. Morphine life efficacy NOT achievable at any dose of Codeine
19
Q
  1. What are two oral preparations of opioids that are commonly used for moderate to severe pain?
  2. Which one is more commonly combined with an NSAID or acetaminophen?
A
  1. Oxycodone and Hydrocodone
  2. Hydrocodone
20
Q

What is the relative potency of Hydromorphone compared to morphine?

A

2-3X as potent

21
Q
  1. What is the mechanism of action of Nalbuphine?
  2. What is its relative efficacy and potency?
  3. What is the advantage to Nalbuphine over Morphine?
  4. What is the drawback to Nalbuphine?
  5. What is its limitation in administration?
A
  1. MU-antagonist and KAPPA-agonist
  2. Similar to Morphine.
  3. Little euphoria and low abuse potential
  4. Can precipitate withdrawal in opiate dependent patients.
  5. Only available by injection.
22
Q
  1. What drug is a partial MU-agonist but 20-50x more potent than morphine?
  2. What are the components of Suboxone?
A
  1. Buprenorphine
  2. Buprenorphine and Naloxone
23
Q
  1. What is the mechanism for Naloxone?
  2. What is the duration of action?
A
  1. High affinity MU-antagonist. Lower affinity for KAPPA and DELTA.
  2. 1-2 hours
24
Q

What drug is a long acting (24+ hrs.) opioid antagonist? What is it used for?

A

Naltrexone. It is used in treatment of alcoholism and opiate addiction.

25
Q
  1. What is the mechanism/function for Dextromethorphan?
  2. What is the mechanism for Tramadol?
A
  1. Not a MU agonist like its isomer levorphanol but is a cough suppressant with some NMDA antagonism.
  2. Weak MU-agonist and blocks NE and 5-HT uptake.
26
Q
  1. What opioid side effect do patients generate rapid tolerance to?
  2. What side effects do patients generate little or no tolerance to?
  3. What side effects do patients gradually generate tolerance to?
A
  1. Nausea and vomiting
  2. Miosis and Constipation
  3. Analgesia, Euphoria, Respiratory depression, endocrine dysfunction.
27
Q
  1. What withdrawal symptoms develop after 6-12 hrs?
  2. What symptoms develop after 12-24 hrs?
A
  1. Restlessness, lacrimation, rhinorrhea, sweating, yawning
  2. Above plus irritability, tremor, dilated pupils, anorexia, piloerection
28
Q

What makes alcohol withdrawal life threatening but opiate withdrawal not life threatening?

A

There is no risk of convulsions/seizures or encephalopathy with opiate withdrawal like there is with alcohol withdrawal.

Owenpharm Block 3 (8 decks)

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