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Neuroscience > Neuroscience Week 3: Opioid Actions > Flashcards

Neuroscience Week 3: Opioid Actions Flashcards

1
Q

Understand the general pharmacokinetics of opioid compounds

A

Oral/Parenteral potency ratio

Absorption - routes of administration

Distribution - localize to highly perfused tissues

Metabolism

Excretion

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2
Q

Examples of strong opioid agonists

A
  • Morphine
  • Oxycodone (AKA oxycontine)
  • Fentanyl
  • Methadone
  • Meperidine
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3
Q

Examples of partial opioid agonists

A
  • Codeine
  • hydrocodone
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4
Q

Examples of mixed opioid agonist-antagonist actions

A

Buprenorphine

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5
Q

Other clinical uses of Opioid Analgesics:

Treating dyspnea from acute pulmonary edema

A

Morphine

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6
Q

Other clinical uses of Opioid Analgesics:

Example for antitiussive

A

Dextromethorphan

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7
Q

antitussive Definition

A

To prevent or relieve a cough

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8
Q

Other clinical uses of Opioid Analgesics:

Example for anti-diarrhea

A
  • Diphenoxylate
  • Loperamide
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9
Q

Other clinical uses of Opioid Analgesics:

Examples for shivering

A

Meperidine

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10
Q

Other clinical uses of Opioid Analgesics:

adjuncts to anesthesia

A

Fentanyl (regional)

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11
Q

Positive effects of opioids on CNS

A

Analgesia

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12
Q

Adverse effects of opioids on CNS

A
  • Mental clouding & Sedation
  • Respiratory depression
  • Antidiuresis
  • Emesis
  • Bradycardia
  • Miosis
  • constipation
  • seizures
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13
Q

Opioid antagonists

A
  • Naloxone
  • Naltrexone
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14
Q

Opioid drug interactions

A

Sedative-hypnotics - increased respiratory depression (CNS depression)

Antipsychotic tranquilizers - increased sedation and accentuates cardiovascular effects (antimuscarinic and α-blocking actions

Monoamine oxidase inhibitors - increased for hyperpyrexic coma and hypertension

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15
Q

Oral/Parenteral Potency Ratio

A

1st pass metabolism (elimination) upon oral administration

Parenteral route: elsewhere than mouth or alimentary canal; e.g. IV, IM, Sub, Q, intrathecal, etc)

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16
Q

Example of low to parenteral ratio

A

Morphine

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17
Q

Example of high oral to parenteral ratio

A

Methadone

18
Q

Codeine Absorption

A
  • reduced 1st pass metabolism, remains effectively orally
  • acts as a partial agonist at the mu receptor
  • High O/P ratio
19
Q

Oxycodone Absorption

A

moderate 1stpass metabolism, but remains effective orally Acts as a moderately strong agonist at the mu receptor. Medium O/P ratio In sustained release form:OxyContin In tablets containing acetaminophen: Percocet

In tablets containing aspirin: Percodan

20
Q

Other routes of administration

A

Nasal insufflation

of some opioids can result in rapid therapeutic blood levels by avoiding 1st pass elimination

•

Oral mucosa via lozenges

•

Transdermal via transdermal patches, which can deliver potent analgesics over many days

21
Q

Opiods are converted mostly to?

A

Opioids are converted mostly to polar metabolites (e.g. glucuronides

22
Q

How are opioids typically distributed?

A

Opioids rapidly leave the blood compartment and localize in

highest concentrations in highly perfused tissues such as:

Brain

Lungs

Liver

Kidney

Spleen

23
Q

Opioids and muscle

A

Concentrations in skeletal muscle may be lower, but muscle can

serve as a main reservoir due to its bulk

24
Q

Opiods and fatty tissue

A

Low blood flow in fatty tissue but accumulation occurs with highly lipophilic drugs in fatty tissue especially after frequent high dose delivery eg fentanyl

25
Q

Morphine Metabolism

A

Pay special attention to renal failure resulting in high circulating levels

26
Q

Fentanyl metabolism

A
27
Q

Fentanyl Absorption

A

Absorption: Highly lipophilic and slowly metabolized via transdermal route. Transdermal system: improved iontophoretic (localized electric current) allowing needle-free delivery.

28
Q

Polar metabolits such as glucoronide conjugates: M3G and H3G are excreted how?

A

In the urine

small amounts are present in the bile; a very minor amount of the excretory process

29
Q

Remifentanil Metabolism

A

bolus IV dose for a very quick procedure (cataract removal)

30
Q

Codeine is metabolized to

A

Codeine demethylated → morphine

31
Q

Hydrocodone is metabolized to

A

Hydrocodone → hydromorphone → H3G

32
Q

Oxycodone is metabolized to?

A

Oxycodone → Oxymorphone → O3G

33
Q

Codeine

hydrocodone

Oxycodone

Metabolism

A
34
Q

Poor metabolizers of codeine

A

wont experience an effect as codeine itself doesnt have strong affinity to the mu receptor

35
Q

clinical uses of opioids

A
36
Q

Mild-moderate agonist Clinical Use of Opioids

A
37
Q

Clinical uses of other opioids

A
38
Q

Opioid effects and tolerance

A
39
Q

Opioid Drug Interactions

A
40
Q

Non-opioid Therapeutics used to manage pain

A

draw attention to gabapentin and pregabalin

ketamine

tramadol however it is a weak mu opiod agonist

Neuroscience (96 decks)

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