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Opioids: Difference between revisions
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Analgesia Effect of Opioid Receptors<ref>Modified from Millers Anaesthesia</ref> | |||
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|style="width: 28%"|'''Mu''' | |style="width: 28%"|'''Mu''' | ||
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|- | |- | ||
| | |ฮฒ-Endorphin | ||
|Agonist | |Agonist | ||
|Agonist | |Agonist | ||
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|Antagonist | |Antagonist | ||
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|+Opioid receptors and their endogenous ligands and precursors | |||
!Receptor | |||
!Precursor | |||
!Peptide | |||
|- | |||
|DOP | |||
|Pro-enkephalin | |||
|[Met]-enkephalin | |||
[Leu]-enkephalin | |||
|- | |||
|KOP | |||
|Pro-dynorphin | |||
|Dynorphin-A | |||
Dynorphin-B | |||
|- | |||
|NOP | |||
|POMC | |||
Unknown | |||
|ฮฒ-Endorphin | |||
Endomorphin-1 | |||
Endomorphin-2 | |||
|- | |||
|MOP | |||
|Pre-pro-nociceptin | |||
|N/OFQ | |||
|} | |||
== Mechanisms of Analgesia == | |||
== Specific Opioids == | |||
== Opioid Potency Comparison == | |||
== Renal Failure == | |||
== Liver Failure == | |||
== Variation in Sensitivity == | |||
== See Also == | |||
[[Opioid Deprescribing]] | |||
[[Category:Pharmacology]] | [[Category:Pharmacology]] |
Revision as of 21:01, 24 June 2021
This article is a stub.
Classification
Classification by receptor affinity
- Opioid Agonists - Morphine, Codeine, Meperidine, Fentanyl, Sufentanil, Remifentanil, Methadone, Tramadol
- Opioid Agonist/Antagonists & Partial Agonists - Pentazocine, Nalbuphine, Butorphanol, Buprenorphine
- Opioid Antagonists - Nalorphine, Naloxone, Naltrexone, Naltrindole, Nalmefene
Classification by Exogenous Opioids Strength
According to the strength or potency based on the plasma concentrations at which they exert their effects. C50 or the plasma concentration causing a 50% effect.
- Strong Opioids include fentanyl, sufentanil, and remifentanil
- Weak opioids include codeine and tramadol
- Intermediate group includes morphine, methadone, oxycodone, and buprenorphine
Classification by synthetic process
- Naturally occurring compounds - Morphine, Codeine, Thebaine, Papaverine
- Semi-synthetic compounds - Diamorphine (heroin), Dihydromorphone, Buprenorphine, Oxycodone
- Synthetic compounds - Pethidine, Fentanyl, Methadone, Alfentanil, Remifentanil, Tapentadol
Pharmacology
Mu | Delta | Kappa | |
Mu1 - Analgesia
Mu2 - Sedation, vomiting, respiratory depression, pruritis, euphoria, anorexia, urinary retention, physical dependence. |
Analgesia, spinal analgesia | Analgesia, sedation, dyspnoea, psychomimetic effects, miosis, respiratory depression, euphoria, dysphoria, dyspnoea | |
Endogenous Peptides | |||
---|---|---|---|
Enkephalins | Agonist | Agonist | |
ฮฒ-Endorphin | Agonist | Agonist | |
Dynorphin A | Agonist | Agonist | |
Agonists | |||
Morphine | Agonist | Weak Agonist | |
Codeine | Weak Agonist | Weak Agonist | |
Fentanyl | Agonist | ||
Meperidine | Agonist | Agonist | |
Methadone | Agonist | ||
Antagonists | |||
Naloxone | Antagonist | Weak Antagonist | Antagonist |
Naltrexone | Antagonist | Weak Antagonist | Antagonist |
Receptor | Precursor | Peptide |
---|---|---|
DOP | Pro-enkephalin | [Met]-enkephalin
[Leu]-enkephalin |
KOP | Pro-dynorphin | Dynorphin-A
Dynorphin-B |
NOP | POMC
Unknown |
ฮฒ-Endorphin
Endomorphin-1 Endomorphin-2 |
MOP | Pre-pro-nociceptin | N/OFQ |
Mechanisms of Analgesia
Specific Opioids
Opioid Potency Comparison
Renal Failure
Liver Failure
Variation in Sensitivity
See Also
- โ Modified from Millers Anaesthesia