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PDA Block 3 > Opioids > Flashcards

Opioids Flashcards

1
Q

What is Pain?

A

Pain is a subjective symptom or an unpleasant sensory and/or emotional experience that is typically associated with actual or potential tissue damage from mechanical or thermal causes or disease

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2
Q

Which ascending tract sends information about pain and temperature

A

Spinothalamic tract

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3
Q

Where does the descending pain-inhibitory pathway originate

A

The midbrain

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4
Q

A-delta and C fibers terminate in the ______ ____ of the spinal cord and transmit _______ and ______ pain

A

Dorsal horn; somatic; visceral

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5
Q

Describe the descending pathways

A
  • Originate in the periaqueductal gray region of the midbrain and nuclei of the rostro-ventral medulla
  • Project to dorsal horn and release norepinephrine, serotonin and enkephalin
  • Inhibit the activity of ascending pain pathways
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6
Q

What are the endogenous opioid peptides

A

Endorphins
Enkephalin
Dynorphins

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7
Q

Three major classes of opioid receptors (g-protein coupled receptors)

A

Mu receptor
Kappa receptor
Delta receptor

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8
Q

Mu receptor
Endogenous ligands:
Drugs:

A

Endogenous ligands: Enkephalins, β-endorphin

Drugs: Morphine, fentanyl, methadone, meperidine, oxycodone, buprenorphine,

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9
Q

Kappa receptor
Endogenous ligands:
Drugs:

A

Endogenous ligands: Dynorphins

Drugs: Nalbuphine, butorphanol and pentazocine

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10
Q

Delta receptor
Endogenous ligands:
Drugs:

A

Endogenous ligands: Enkephalins

Drugs: none

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11
Q

Localization of opioid receptors

A

Found in the periaqueductal gray, dorsal horns of spinal cord, medulla and hypothalamus - also peripheral organs such as GI system and heart

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12
Q

Mu and delta receptors in limbic areas may be involved in ______ _______

A

Drug dependence

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13
Q

Kappa receptors in limbic structures may be involved in ______ actions of kappa agents

A

dysphoric

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14
Q

Narcotic

A

A term used to refer to morphine like drugs and some other abused substances - drugs that produce a stuporous sleeplike state and may or may not be analgesic

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15
Q

Opiates

A

Drugs that are derived from opium or have a morphine like pharmacological profile

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16
Q

Opioid

A

Refers to all opiates, agonist-antagonists and endogenous peptides

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17
Q

Which drugs undergo extensive first pass metabolism

A

Morphine and naloxone

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18
Q

Which opioid drugs are activated by metabolism

A

Codeine and heroin

19
Q

Duration of action is related to both _______ and _______ _____

A

Lipohilicity; elimination rate

20
Q

Effects of Opioid agonists

A

1) Analgesia (alleviating pain)
2) Cough suppression
3) Antidiarrheal effect and constipation (mu receptors on GI nerves)
4) Euphoria
5) Sedation
6) Respiratory depression (side effect) - decrease in the sensitivity of chemoreceptors in brainstem to CO2
7) Nausea
8) Endocrine Effects
9) Miosis (Edinger Westphal nucleus)

21
Q

Which drugs are less efficacious in alleviating pain

A

Codeine and propoxyphene

22
Q

Which opioids are used for cough suppression

A

Codeine, hydrocodone and dextromethorphan

23
Q

What are the endocrine effects of opioids

A
  • Decreased release of LH - mu receptor

- ADH secretion is increased by mu stimulation and decreased by Kappa stimulation

24
Q

Opioid agonists (8)

A

1) Oxycodone
2) Codeine
3) Morphine
4) Heroin
5) Hydrocodone
6) Methadone
7) Fentanyl
8) Meperidine

25
Q 
Morphine
Receptor:
Oral to Parenteral ratio:
Administration:
Duration of analgesia:
A

Receptor: mu agonist
Oral to Parenteral ratio: 3 or 4 to 1
Administration: Available in injectable, oral, oral sustained release and suppository forms - sustaine release preparation
Duration of analgesia: 4-5 hours

26
Q

Heroin
More _____ than Morphine
Converted to ______ and ______
Abuse potential:

A

More lipophilic than Morphine
Converted to 6-mono-acetyl morphine and morphine
Abuse potential: High

27
Q

Codeine, Hydrocodone and Oxycodone
Which of these does not reach morphine like efficacy?
These drugs are often used in combination with what?
Which of these drugs are available as sustained release preparations?

A

Codeine;
NSAIDS or acetaminophen;
Oxycodone and Hydrocodone

28
Q 
Methadone
Receptor:
Duration of action:
Administration (most common):
Use:
A

Receptor: mu agonist
Duration of action: longer than morphine
Administration (most common): has good oral availability
Use: treatment of opioid abuse and chronic pain

29
Q

Meperidine - a phenylpiperidine
Duration of action:
What does this drug form:
Interactions:

A

Duration of action: shorter duration of analgesia than morphine
What does this drug form: forms toxic metabolite, normeperidine, that can accumulate with frequent use
Interactions: with MAO inhibitors

30
Q 
Fentanyl - structurally related to meperidine
Receptor:
Duration of action:
Potency in comparison to morphine:
Availability:
A

Receptor: mu agonist
Duration of action: short acting - 1-1.5 hours
Potency in comparison to morphine: 100 x as potent
Availability: injectable form and as transdermal patches

31
Q

How potent is Hydromorphone compared to morphine

A

2-3 X as potent

32
Q

Mixed-Action Agonist/Antagonist (2)

A

1) Nalbuphine

2) Buprenorphine

33
Q 
Nalbuphine
Receptors:
Efficacy:
Abuse potential:
Availability:
A

Receptors: mu antagonist and kappa agonist
Efficacy: similar to morphine
Abuse potential: low
Availability: only in injectable form

34
Q

Buprenorphine
Receptors:
Use:
Administration:

A

Receptors: Partial mu agonist
Use: Treatment of moderate to severe pain
Administration: Oral or patch

35
Q

Opioid Antagonists (2)

A

1) Naloxone

2) Naltrexone

36
Q 
Naloxone
Receptors:
Administration:
Duration of action:
Use:
A

Receptors: High affinity for mu receptors, less for kappa and delta
Administration: greater activity parenterally than orally
Duration of action: 1 to 2 hours (short)
Use: Treat opioid overdoses - decrease parenteral abuse liability

37
Q

Naltrexone
Administration:
Use:

A

Administration: Orally active with long half life
Use: Treatment of alcoholism and opiate addiction

38
Q

Dextromethorphan

A

dextro isomer of levorphanol. Antitussive, but not analgesic. Also is an NMDA antagonist

39
Q

Tramadol

A

Weak mu agonist - also blocks NE and 5-HT uptake

  • Used for mild to moderate pain
  • Available for oral use including a sustained release preparation
40
Q

Tolerance of Opioids

A

Tolerance develops to most of the effects of the opioids
- Rapid = emetic action
- Moderate Rate = analgesic, respiratory, euphoria and endocrine effects
- Little or no tolerance - constipation and miosis
Cross tolerance

41
Q

Physical dependence on opioids

A

Continuous exposure to opioids results in development of physical dependence. When drug administration is stopped, the body functions abnormally

42
Q 
Symptoms of withdrawal based on time
6-12 hours:
12-24 hours:
24-27 hours:
Later:
A

6-12 hours: Drugs seeking behavior; restlessness, lacrimation, rhinorrhea
12-24 hours: Restless sleep for several hours; irritability, tremor, dilated pupils, anorexia
24-27 hours: Increased intensity of above, plus weakness, depression, nausea - possible electrolyte imbalance
Later: Above symptoms alternate with restless sleep with gradual decrease in activity – Delayed growth and development in infants born to addicted mothers may be detected for up to 1 year

43
Q

Signs of Opioid abuse

A

1) Euphoria
2) Craving
3) Drug-seeking behavior
4) Withdrawal

44
Q

Treatment of opioid abuse:

A

1) Methadone
2) Suboxone
3) Naltrexone

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