EXAM #3: OPOID ANALGESICS Flashcards
What types of disease are opioid analgesics in to delay or arrest the disease process?
Autoimmune disease e.g. RA
Where do opioid analgesics exert their MOA?
Ascending:
1) At the damaged/inflammed peripheral nerve
2) Dorsal horn/ spinal cord
3) Thalamus
Descending pathways
What are the effects of opoids?
- Euphoria
- Analgesia
- Sedation
- Anti-diarrheal
- Cough suppression
What is opium?
Exudate from poppy seeds
What is an opiate?
Drug extracted from the exudate of a poppy seed
What is an opoid?
Natural or synthetic drug that binds to opoid receptors w/ agonist effects
What is a narcotic?
General term to categorize drugs that treat moderate to severe pain
What are the endogenous opoids?
Endorphins
Enkephalins
Dynorphins
Agonism of what subtype of opoid receptor produces the MOST analgesia?
Mu
Kappa and delta do produce some analgesia
What is the difference between Mu1 and Mu2?
Mu1= outside the CNS Mu2= inside the CNS
What is morphine metabolized to? What is unique about the metabolites?
Morphine undergoes glucuronidation to two products:
1) Morphine-3-glucuronide (90%)
2) Morphine-6-glucuronide (10%)
Morphine 6-glucuronide is MORE potent than morphine
What are heroin and codeine metabolized to?
Morphine
What happens upon Mu opoid receptor activation to produce analgesia?
- Mu opoid receptors are GPRCs coupled to Gi subunits
- Decreased adenylyl cyclase
- Decreased cAMP
–>Less intracellular Ca++ and increased K+ opening i.e. INHIBITION or neurotransmission
How do opoid analgesics inhibit the ascending pain pathways?
1) Inhibition of afferent pain transmission
2) Blocked peripheral effects
3) Blocked dorsal horn of the spinal cord
How do opioid analgesics affect the descending pain pathways?
Block inhibitory GABAergic interneurons
This leads to ENHANCED INHIBITION of nociceptive processing*
What is unique about the analgeisa produced by opioid analgesics?
Reduce BOTH the sensory and affective components of pain