Opioids like morphine bind to opioid receptors in the brain, spinal cord, and digestive tract to relieve pain. They inhibit neurotransmitter release and can cause respiratory depression, nausea, drowsiness, tolerance, and addiction with long term use. Narcotic analgesics are classified into categories including morphine derivatives, synthetic morphine derivatives, and narcotic antagonists. NSAIDs like ibuprofen and naproxen inhibit prostaglandin production to reduce pain and inflammation but can cause gastric upset and kidney damage. COX-2 inhibitors selectively inhibit COX-2 to reduce inflammation with fewer gastrointestinal side effects. Acetaminophen's mechanism is unknown but it is used for fever and pain relief, though can
Analgesics: Narcotic, Non-Narcotic, and Mechanisms of Action
1. ANALGESIC
S
NARCOTIC & OPIOID
narke----any substance that relieved pain, dulled the
senses, or induced sleep.
Opiate receptors are distributed widely in the brain,
and are found in the spinal cord and digestive tract.
narcotic=substance that binds to opiate receptors or
illicit substance
pain will give release of opiates (endorphins and
enkephalins, dynorphin)
Act like inhibitory transmitters… yields less pain.
2. ANALGESICS
opium poppy used by Egyptians,Greeks, Romans.
morphine=purified constituent of opium----
Morpheus---Greek god of dreams….euphoria
MOA----these drugs interact with specific receptor sites and
have effect on CNS, acting on receptors located on
neuronal cell membranes. The presynaptic action of opioids to
inhibit neurotransmitter release is considered to be their
major effect in the nervous system. also acts on gut wall and
joints.
Even in therapeutic doses, narcotic analgesics can cause
respiratory depression, nausea, and drowsiness. Long
term administration produces tolerance, psychic, and
physical dependence called addiction. These drugs are
commonly prescribed to manage pain, but can also be
prescribed to treat diarrhea (Lomotil) or severe cough (codeine).
3. ANALGESICS
Narcotic agents may be classified into four categories:
1--Morphine and codeine-- natural alkaloids of opium.
2---Synthetic derivatives of morphine such as heroin.
3--- Synthetic agents which resemble the morphine
structure.
4---Narcotic antagonists which are used as antidotes
for overdoses of narcotic analgesics.
4. ANALGESIC
S
opioids --- bind to presynaptic nerve terminal calcium channels.
this shortens action potential and yields inhibitied
neurotransmitter release.
opioids---bind to postsynaptic receptors in ascending
pain pathway yields reduced action potential
opioids---cause increased transmission of the descending
inhibition of spinal nociceptive conduction.
Schedule II/III controlled drugs.
adverse reaction----respiratory depression, constipation,
confusion, naseau, euphoria
consider----addiction and tolerance. federal and state laws
for processing, dispensing, maintaining records.
5. ANALGESICS
examples--
acet w codeine----tylenol w codeine
codeine---Codeine
fentanyl-----Duragesic patch
hydrocodone----Hycodan
acet w hydrocodone----Lortab
hydromorphone----Dilaudid
meperidine---Demerol
methadone----Dolophine
morphine----MS Contin
oxycodone----Oxycontin
acet w oxycodone----Percocet
pentazocine---Talwin
acet w propoxyphene----Darvocet
6. NON-NARCOTIC
ANALGESIC
NSAIDs
Nonsteroidal Antiinflammatory Drugs:
prostaglandins have 20 carbon chain that includes
5 carbon ring.
Make a prostaglandin-------cell injury releases arachidonic acid.
cyclooxygenase will convert AA into PG. This irritates
nerve endings, yields pain and inflammation.
COX 1and COX2 hit different sites on AA.
COX1 makes PG for kidney function,stomach protection
mucous, blood clotting.
COX2 makes PG for pain,heat, swelling.
Most NSAID attack COX1 and COX2.
8. NON-NARCOTIC
ANALGESICCOX2 inhibitor
indications----rheumatoid arthritis, osteoarthritis,
menstration cramps, acute pain
reactions------GI issues, fluid retention
example-
only celecoxib/Celebrex
vioxx and bextra removed from production--MI,strokes
Aspirin-
moa---redcued fever by increased skin blood flow and inhibit
prostaglandin
indications--
pain, inflammation, fever
9. NON-NARCOTIC
ANALGESICaspirin reactions---
stomach ulcer, anemia, tinnitus, confusion, prolonged labor
consider----not given to children exposed to chickenpox.(reyes
syndrome)
avoid with warfarin
Acetominophen---
moa-----exact mechanism unknown
indications----fever, pain, inflammation
reaction----avoid with warfarin, liver damage
Selective 5HT(5-hydroxytryptamine) receptor agonists---
Also called serotonin receptors. Found in CNS and PNS.
These receptors cause vasoconstriction which redirects cerebral
bloodflow.
Examples---sumatriptan/imitrex
Zolmitriptan/zomig
10. NON-NARCOTIC
ANALGESICaspirin reactions---
stomach ulcer, anemia, tinnitus, confusion, prolonged labor
consider----not given to children exposed to chickenpox.(reyes
syndrome)
avoid with warfarin
Acetominophen---
moa-----exact mechanism unknown
indications----fever, pain, inflammation
reaction----avoid with warfarin, liver damage
Selective 5HT(5-hydroxytryptamine) receptor agonists---
Also called serotonin receptors. Found in CNS and PNS.
These receptors cause vasoconstriction which redirects cerebral
bloodflow.
Examples---sumatriptan/imitrex
Zolmitriptan/zomig