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Pharmacology > Opioid lecture part 2 > Flashcards

Opioid lecture part 2 Flashcards

1
Q

3 Types of opioid drugs

A
  1. Agonists - elicit receptor responses of opiate receptors
  2. Pure Antagonists - no inherent action after binding to receptor but block any agonist activity
  3. Agonist/Antagonists - drugs having mixed effects
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2
Q

Morphine is what type of opioid drug?

A

Pure agonist

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3
Q

Pure agonists are activated via what receptors

A

Mu and Kappa activated

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4
Q

Which type of opioid drug has unlimited analgesia

A

Pure Agonist

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5
Q

With continued exposure of tissues to high concentrations of opioid agonists, what happens to the potency of the drug?

A

Potency of the drug declines so that progressively higher concentrations are required to produce the same degree of analgesia

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6
Q

Partial agonists are partial ? activation and weak ? antagonist?

A

Partial Mu activation

Weak Kappa antagonist

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7
Q

T or F, Partial agonist have unlimited analgesia?

A

False, Good analgesia but limited effect

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8
Q

T or F, Partial agonist drugs are commonly used in dentistry

A

False, not typically

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9
Q

Agonist/Antagonist drugs have what receptor antagonist and what receptor agonist?

A 
Mu = antagonist
Kappa = agonist
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10
Q

Which type of opioid drug is used as sedative prior to surgery; supplement to surgical anesthesia

A

Agonist/Antagonist

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11
Q

Pure Antagonists are what receptor antagonists

A

Mu and Kappa

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12
Q

How much analgesia does Pure antagonists have?

A

No analgesia

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13
Q

What drug is a good example of a pure antagonist?

A

naloxone (Narcan)

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14
Q

How is naloxone used in dentistry and in general?

A

ANTIDOTE

  • used in dentistry to reduce overdose of opiates (used during conscious sedation
  • Used for complete or partial reversal of opioid depression (including respiratory depression)
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15
Q

How are opioids absorbed?

A

Most are well-absorbed orally

  • Lungs
  • Nasal and oral mucosa
  • Intact skin (patches)
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16
Q

How are opioids excreted?

A

As metabolites in urine

17
Q

Duration of action for opioids?

A

Orally = most produce analgesia for 4-6 hours

18
Q

Metabolism of opioids?

A

Conjugation with glucuronic acid in liver

19
Q

Can opioids be passed to fetus?

A

Yes produces respiratory depression in fetus if taken by mother

20
Q

4 Desired clinical effects of opioid drugs

A
  1. Potent analgesia
  2. Sedation and euphoria
  3. Cough suppression
  4. GI effects
    - increase smooth muscle tone
    - decrease propulsion and motility
    - used for treatment of diarrhea
21
Q

ADVERSE reactions of opioid drugs

A
  1. Physical addiction
  2. Respiratory depression (dose-related)
  3. Nausea and vomiting (emesis)
  4. Constipation
  5. Miosis (pinpoint pupils)
  6. Urinary retention
  7. CNS effects
  8. Cardiovascular
  9. Biliary tract constriction
  10. Histamine release
  11. Pregnancy and lactation
  12. Physical dependency/addiction
  13. Tolerance
  14. Pharmacologic effect may also be an adverse reaction
  15. Severity of side effects is proportional to efficacy
  16. Overdose
  17. Withdrawal
22
Q

Which drugs are considered FDA pregnancy category C and can cross into breast milk

A

Morphine and Codeine

23
Q

Major symptom of overdose

A

respiratory depression

Also: pinpoint pupils, coma

  • Treated with antagonist = naloxone
24
Q

What are the hypersensitivity reactions to opioids

A

Most are dermatologic

If true allergy, AVOID

25
Q

Clinical indications for opioids in dentistry and medicine?

A

Dentistry

  • Analgesia
  • Sedation

Medicine

  • Analgesia
  • Sedation
  • Cough suppression
  • Diarrhea
26
Q

Drugs used in dentistry are derivatives of what?

A

Morphine and Codeine are derived from opium alkaloids

Heroin = synthesized morphine product

27
Q

Name pure agonist drugs

A
  1. Morphine
  2. Oxycodone
  3. hydrocodone
  4. codeine
  5. dihydrocodeine
  6. propoxyphene (withdrawn from US market in Nov. due to cardiac arrhythmias)
  7. meperidine
  8. hydromorphone
  9. methadone
  10. fentanyl
  11. heroin
28
Q

Name the mixed agonists/antagonists drugs

A
  1. pentazocine
  2. butorphanol
  3. nalbuphine
  4. buprenorphine
29
Q

Which drug is a mixed agonist/antagonist that is equally as potent as morphine

A

Methadone (C-II)

  • Inhibits ascending pain pathways
  • Produces generalized CNS depression
  • Long duration of action
  • ** Initially used as a maintenance regimen for heroin abuse = FDA approved detoxication and maintenance programs
30
Q

How quickly can the pure antagonist effects occur when an antidote is given

A

Within 1-2 minutes; 1-4 hours duration of action

31
Q

Two examples of pure antagonists

A
  1. naltrexone - antidote given orally or IM

2. naloxone - in dental office, IV to reverse overdose of fentanyl and meperidine (sedation)

32
Q

Most widely used route of administration for morphine

A

IM

  • Oral morphine is poorly absorbed
  • Not used in dentistry
  • Used primarily for post-recovery pain
33
Q

Describe the morphine chemical structure

A

Piperidine ring structure = 6 sided

- Needed to bind to opiate (mu) receptor

34
Q

What is the most widely abused drug by hospital personnel?

A

meperidine (Demerol)

- Excellent analgesic, but addictive

35
Q

T or F, meperidine has No Misois.

A

True

  • Addicts use this drug because it masks the pinpoint pupils that they would get from abusing morphine
36
Q

Primary side effects of Demerol?

A 
Nausea
Respiratory Depression (risk for death in addicts)
37
Q

Is Demerol used in dentistry?

A

Yes,
IV sedation (not as potent as fentanyl)
- Wider margin of safety
- 25 mg IV dose

Orally for moderate to severe pain

  • 50-100 mg orally q 4 hours as needed
  • 3-4 hour duration of action

Pharmacology (24 decks)

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