Opioid Agonists and Antagonists Flashcards

1
Q

Prototype

A

Morphone

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2
Q

morphine indications

A

… Clinical indication: moderate to severe pain

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3
Q

morphine pharmacokinetics and dynamics

A
† ½ life 2-4 h
† Oral doses 50% as effective as parenteral
† Least lipophilic
† Active mebolite M6G
† Causes histamine release
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4
Q

Morphine is the lest

A

liphophilic

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5
Q

morphine has low penetration of

A

BBB

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6
Q

Hydromorphine (Dilaudid) is a

A

Semisynthetic, derived from morphine

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7
Q

Hydromorphine (Dilaudid) indications

A

moderate to severe pain

† Good choice for patient with renal disease

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8
Q

Hydromorphine (Dilaudid) pharmacokinetics

A

† ½ life 1-3 hours
† Oral doses <50% as effective as IV
† No active metabolites
… Similar analgesic and SE profile to morphine

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9
Q

dilaudided is usefull to prevent

A

shivering

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10
Q

Meperidine (Demerol) - Indications

A

† Moderate to severe pain, anesthesia adjunct, OB
analgesia, pre-op sedation
† Avoid in renal failure, seizure history, elderly
† Not appropriate for chronic pain management

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11
Q

Meperidine (Demerol) pharmacokinetics

A

† ½ life 2.5-4h

† Active metabolite (1/2 life 15-30h)

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12
Q

Meperidine (Demerol) SE

A

… S.E.: may precipitate tremors, myoclonus, seizures

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13
Q

Fentanyl - Indications

A

† Moderate to severe chronic or break through pain
† 80x more potent than morphine
† The fentanyl patch should only be used by patients who
are opioid-tolerant and have chronic pain that is not well
controlled with other pain medicines.

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14
Q

Fentanyl administration

A

Administration: oral, IV, neuraxial, lozenge, patch

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15
Q

Fentanyl overdose signs

A

Overdose signs: dyspnea or slow or shallow breathing; slow
heartbeat; severe sleepiness; cold, clammy skin; trouble
walking or talking; or feeling faint, dizzy, or confused

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16
Q

Methadone - Indications

A

† Heroin addiction, severe pain, suppression of opioid

withdrawal symptoms, neuropathic pain?

17
Q

Methadone phamacokinetics and Dynamics

A

† Long half life: 72 hours
† Dosing decreased after 72 hours to prevent extreme
side effects
† Difficult to determine equlanalgesic conversion

18
Q

Codeine - Indications

A

† Mild to moderate pain, analgesia, antidiarrheal,

antitussive

19
Q

codeine - phamacokinetics and dynamics

A

† Administered orally or IV
† Often combined with acetaminophen
† Ethnic differences: Hispanic and Mediterranean ring
countries not able to metabolize to morphine

20
Q

codeine SE

A

constipation, N&V

21
Q

Hydrocodone - Indications

A

† Moderate to severe pain, antitusssive

† May be useful short term in acute pain

22
Q

Hydrocodone - P&D

A

† Half life: 3-4 h
† Duration: 4-8 h
† Often combined with acetaminophen or ibuprofen
(Vicodin or vicoprofen)

23
Q

Oxycodone (Oxycontin, Percocet) Clinical Indications

A

† Moderate to severe pain

24
Q

Oxycodone Pharmacokinetics and Dynamics

A
† Oral route only
† Onset 40-60 minutes
† Half life: 2-3h
† Duration 3-6h
† Often combined with acetaminophen, ibuprofen
25
Q

Opioids to Avoid

A
… Meperidine (Demerol)
† Active metabolite
† Metabolite ½ life 72 h
… Prop yp ox hene
† Active metabolite nonpropoxyphene
† Half life 15 h
26
Q

Opioid Angonist-Antagonists Clinical Indication

A

moderate to severe pain

27
Q

Opioid Angonist-Antagonists - MOA

A

MOA: activate 1 type of receptor while blocking

another

28
Q

Opioid Angonist-Antagonists agents

A

† Buprenorphine
† Butorphenol
† Nalbuphine*
† Pentazocine*

29
Q

Opioid Angonist-Antagonists - ADR

A

Adverse reactions less common than with true agonists

30
Q

Suboxone

A

… buprenorphine and naloxone

31
Q

Suboxone - Indications

A

Clinical indications

† Used to treat opiate addiction

32
Q

Suboxone - SE

A

Similar side effects and precautions to opiates

33
Q

Suboxone cannont

A

Cannot stop abruptly, will trigger withdrawal