NU 578 - Unit 2
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
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
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
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
