UNIT 9: ANALGESICS (Part 2) - OPIOIDS, OPIOID SUBSTITUTES, AND OPIOID ANTAGONISTS

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33 Terms

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• Morphine
• Methadone
• Fentanyl
• Hydromorphone, oxymorphone
• Meperidine
• Oxycodone
• Sufentanil, alfentanil, remifentanil
• Codeine
• Hydrocodone

OPIOID AGONISTS:

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OPIOID AGONISTS

Morphine

(OPIOID AGONISTS / MIXED OPIOID AGONIST-ANTAGONISTS)

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OPIOID AGONISTS

Methadone

(OPIOID AGONISTS / MIXED OPIOID AGONIST-ANTAGONISTS)

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OPIOID AGONISTS

Fentanyl

(OPIOID AGONISTS / MIXED OPIOID AGONIST-ANTAGONISTS)

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OPIOID AGONISTS

Hydromorphone, oxymorphone

(OPIOID AGONISTS / MIXED OPIOID AGONIST-ANTAGONISTS)

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OPIOID AGONISTS

Meperidine

(OPIOID AGONISTS / MIXED OPIOID AGONIST-ANTAGONISTS)

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OPIOID AGONISTS

Oxycodone

(OPIOID AGONISTS / MIXED OPIOID AGONIST-ANTAGONISTS)

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OPIOID AGONISTS

Sufentanil, alfentanil, remifentanil

(OPIOID AGONISTS / MIXED OPIOID AGONIST-ANTAGONISTS)

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OPIOID AGONISTS

Codeine

(OPIOID AGONISTS / MIXED OPIOID AGONIST-ANTAGONISTS)

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OPIOID AGONISTS

Hydrocodone

(OPIOID AGONISTS / MIXED OPIOID AGONIST-ANTAGONISTS)

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• Morphine
• Methadone
• Fentanyl

MECHANISM OF ACTION:
• Strong µreceptor agonists
• Variable affinity for delta and kappa receptors

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• Morphine
• Methadone
• Fentanyl

EFFECTS:
• Analgesia
• Relief of anxiety
• Sedation
• Slowed gastrointestinal transit

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• Morphine
• Methadone
• Fentanyl

CLINICAL APPLICATIONS:
• Severe pain
• Adjunct in anesthesia (fentanyl, morphine)
• Pulmonary edema (morphine only)
• Maintenance in rehabilitation programs (methadone only)

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• Morphine
• Methadone
• Fentanyl

PHARMACOKINETICS, TOXICITIES:
• First-pass effect
• Duration 1-4 h except methadone, 4-6 h
• Toxicity: respiratory depression,
• Severe constipation,
• Addiction liability,
• Convulsions

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Hydromorphone, oxymorphone

Like morphine in efficacy, but higher potency

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Meperidine

Strong agonist with anticholinergic effects

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Oxycodone

Dose-dependent analgesia

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Sufentanil, alfentanil, remifentanil

Like fentanyl but shorter duration of action

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• Codeine
• Hydrocodone

MECHANISM OF ACTION:
• Less efficacious than morphine
• Can antagonize strong agonists

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• Codeine
• Hydrocodone

EFFECTS:
• Like strong agonists
• Weaker effects

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• Codeine
• Hydrocodone

CLINICAL APPLICATIONS:
• Mild-moderate pain
• Cough (codeine)

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• Codeine
• Hydrocodone

PHARMACOKINETICS, TOXICITIES:
• Like strong agonists, toxicity dependent on genetic variation of metabolism

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• Buprenorphine
• Nalbuphine

MIXED OPIOID AGONIST-ANTAGONISTS:

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MIXED OPIOID AGONIST-ANTAGONISTS

Buprenorphine

(OPIOID AGONISTS / MIXED OPIOID AGONIST-ANTAGONISTS)

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Buprenorphine

MECHANISM ACTION:
• Partial µ agonist
• K antagonist

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Nalbuphine

(OPIOID AGONISTS / MIXED OPIOID AGONIST-ANTAGONISTS)

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Buprenorphine

EFFECTS:
• Like strong agonists but can antagonize their effects
• Also reduces craving for alcohol

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Buprenorphine

CLINICAL APPLICATIONS:
• Moderate pain
• Some maintenance rehabilitation programs

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Buprenorphine

PHARMACOKINETICS, TOXICITIES:
• Long duration of action 4-8 h
• May precipitate abstinence syndrome

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Nalbuphine

MECHANISM ACTION:
• K agonist • µ antagonist

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Nalbuphine

EFFECTS:
• Similar to buprenorphine

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Nalbuphine

CLINICAL APPLICATIONS:
• Moderate pain

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Nalbuphine

PHARMACOKINETICS, TOXICITIES:
• Like buprenorphine