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• Opioids Drugs -✓✓Drugs:
• Opioids - MOA -✓✓- Bind to "opiate receptors" in the brain, which
disrupts the transmission of pain signals in the CNS.
- Mimic actions of endogenous opiates
(endorphins, enkephalins, dynorphins).
- Primarily activate mu receptors, but also activate Kappa
• Opioids - Effect -✓✓* Relieve pain & induce euphoria
Also cause sedation, respiratory depression, miosis, constipation,
nausea, & suppress the cough reflex.
• Opioids - Uses -✓✓- Pain relief
- Cough suppression
- Relief of dyspnea
- Preoperative sedation
• Opioids - Side Effects -✓✓Hypotension
sedation
nausea
itching
miosis
muscle weakness
constipation
Urinary Retention
,Biliary Colic
Increased ICP
• Treatment of Opioid- Induced Constipation -✓✓methylnaltrexone
(Relistor)
naloxegol (Movantik)
Blocks opioid receptors in the GI tract
* Does not cross blood-brain barrier, so does not reverse analgesia
• Opioids - Drug Interactions -✓✓CNS depressants!
Anticholinergics
Drugs that lower BP
• Opioids - Contraindications/Warnings -✓✓Decreased respiratory
reserve
Labor and delivery
Inflammatory Bowel disease
Head Injury
• Opioids - Patient Educaiton -✓✓
• Opioid toxicity -✓✓3 signs:
- coma
- pinpoint pupils
- respiratory depression - may be fatal!
• Tolerance -✓✓a state in which a drug user needs larger amounts of the
drug to produce the same effect on the body
, • Physical Dependence -✓✓A state in which an abstinence syndrome
will occur if drug use is abruptly stopped
• Abuse -✓✓drug use that is inconsistent with medical or social norms
• Addiction -✓✓disease characterized by and individual pathologically
pursuing rewards and relief by substance use and other behaviors
• Full opioid agonists -✓✓- Good for severe pain
- May give a feeling of euphoria
Example: Morphin, codeine, hydromorphone
• Partial opioid agonists (Agonist-antagonist) -✓✓- Good for moderate
pain
- May act as antagonists at some receptors and
precipitate withdrawal.
Example: pentazocine, Suboxone, buprenorphine, nalbuphine
• Partial opioid agonists (Agonist-antagonist) Drugs: -✓✓Pentazocine
Suboxone
Buprenorphine
Nalbuphine
• Partial opioid agonists (Agonist-antagonist) Action -✓✓Acts as
antagonists at mu receptors, and agonists at kappa receptors
• Buprenorphine (Suboxone) Action: -✓✓Acts as a partial agonist at mu
receptors, and an antagonist at kappa receptors
• Medications for those with hx of Opioid abuse -
✓✓morphine/naltrexone (Embeda)