Non-Opioid Lecture Flashcards
Define Analgesia:
Absence of pain in response to a stimulus that is normally painful
Define Pain:
An unpleasant sensory or emotional experience associated with actual or potential tissue damage, or described in terms of such damage
Define Anesthesia:
Absence of all sensory modalities
3 endogenous responses to pain:
- Endorphins
- Enkephalins
- Dynorphins
Location and function of endorphins
Mainly concentrated in the central nervous system, activates opioid receptors, provides analgesia, euphoria at mu receptor
What was the first endorphin to be purified? What receptor does it activate?
Enkephalins, activates delta receptor
Dynorphins have a high affinity for which receptor?
kappa-opioid receptor
2 types of pain
- Dull, aching, inflammatory (NSAIDS most effective)
2. Sharp, piercing, lancinations (Opiates most effective)
Most dental pain is which of the two types?
Mostly dull,aching, inflammatory pain
- NSAIDS are most effective against this type of pain
Degrees of pain and what is most effective for each?
- Mild = Salicylates, NSAIDS most effective
- Moderate = Salicylates, NSAIDS most effective
- Severe = opiates are best
Locus of action for non-opioid analgesics and Mechanism?
- Act primarily at peripheral nerve endings
- Antipyretic effect mediated centrally
Mechanism: inhibit prostaglandin synthesis
Locus of action for opioid analgesics and mechanism?
- Act primarily within CNS
Mechanism: depress CNS which reduces response to pain (pain reaction)
T or F, All non-opioid analgesics work on the peripheral nervous system
True
T or F, Opiates = more side effects
True
Why are NSAIDS considered true analgesics?
They stop the pain from where it is occurring. Opiates are not considered true analgesics because they simply DIMINISH your awareness of pain, so they only act as analgesics (don’t feel the pain)
NSAIDS inhibit the synthesis of what? How is this done?
Inhibit prostaglandin synthesis
- Inhibit the important enzyme: cyclooxygenase (COX) so that prostaglandins are not formed
- Inhibit cytoprotective PG as well as PG associated with inflammation (These are the good guys that our bodies need)
3 main non-opioid analgesic classes that we talked about
- Salicylates = aspirin
- Non-steroidal anti-inflammatory drugs (NSAIDS) - includes ibuprofen
- Acetaminophen (Tylenol) = Not an NSAID. Classified as a miscellaneous analgesic
Why is Acetaminophen not considered an NSAID
It works on COX 3 in the CNS, and is not anti-inflammatory
How many different NSAIDS are approved in the U.S.
22
What are the affects of prostacyclin?
Vasodilation
Inhibits platelet aggregation
-*** Opposite of thromboxane effects
What are the effects of prostaglandins
Cytoprotective
Inflammatory mediators
What are the effects of thromboxane?
Vasoconstriction
Platelet aggregation
-*** Opposite of prostacyclin effects
COX 1 maintains what 5 things on a normal physiologic basis?
- Renal blood flow
- Body temperature
- Blood pressure
- Heart rate
- Reproduction
If you take NSAIDs and Aspirin, what happens by blocking COX?
Block formation of both cytoprotective prostaglandins and prostaglandins associated with inflammation (Blocks COX 1 and 2)
What adverse effect is present if COX 1 is blocked by aspirin or NSAIDS?
Decreases production of protective mucous = GI ulceration and bleeding.
**Remember: COX 1 regulates the amount of stomach acid produced. Stomach has thick mucous lining to protect gastric mucosa from HCl
- Chronic use of NSAIDS is associated with GI ulceration and bleeding
When is COX 2 produced?
Produced when you experience trauma and need inflammatory response for healing.
- This is the “inducible” form of COX
T or F, Blocking COX 2, like COX 1, will have an adverse effect on the stomach by blocking the cytoprotective prostaglandins.
False, COX 2 have no effect on the stomach = leave cytoprotective prostaglandins intact. They only alter prostaglandins associated with inflammation.
Drugs that block COX 2 are primarily used for what?
Arthritis
-***Celebrex is a common brand of COX 2 inhibitors used for arthritis
COX 3 is found where?
Only in the CNS
COX 3 function
It works centrally but has no anti-inflammatory effects. It does suppress prostaglandin synthesis.
- *** This is how acetaminophen works. Pain control but no anti-inflammatory effects
Why can tylenol be used for fever reduction?
It works centrally and can act on the hypothalamus
Non-selective NSAIDS block which COX?
Both COX-1 and COX-2
Selective NSAIDS block which COX?
Block COX-2 only. Only one available in US = celecoxib (Celebrex)
