解热镇痛抗炎药 antipyretic-analgesic and anti-inflammatory drugs
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解热镇痛抗炎药 Antipyretic-analgesic and Anti-inflammatory Drugs. Pain Treatment. Analgesics Antipyretic-analgesic and anti-inflammatory drugs*. Pain. An unpleasant experience associated with actual or potential tissue damage. Pain Physiology. Neurochemistry. Ion Fluxes (H + / K + ). - PowerPoint PPT PresentationTRANSCRIPT
解热镇痛抗炎药
Antipyretic-analgesic Antipyretic-analgesic and Anti-inflammatory Dand Anti-inflammatory Drugsrugs
Pain Treatment
Analgesics
Antipyretic-analgesic and
anti-inflammatory drugs*
An unpleasant experience
associated
with actual or potential
tissue damage.
PainPain
Pain Physiology
Ion FluxesIon Fluxes(H(H++/ K/ K++))Ion FluxesIon Fluxes(H(H++/ K/ K++))
NeurochemistryNeurochemistryNeurochemistryNeurochemistryTissue InjuryTissue InjuryTissue InjuryTissue Injury
Mast Mast CellCell
Mast Mast CellCell
SensitizedSensitizedNociceptorNociceptorSensitizedSensitizedNociceptorNociceptor
Aspartate, Neurotensin, Glutamate, SubstanceSubstance PAspartate, Neurotensin, Glutamate, SubstanceSubstance P
To brainTo brainTo brainTo brain
HistamineHistamineHistamineHistamine
BradykininBradykininBradykininBradykinin
LeukotrienesLeukotrienesLeukotrienesLeukotrienes
DorsalDorsalhornhorn
DorsalDorsalhornhorn
ProstaglandinsProstaglandinsProstaglandinsProstaglandins
Pain TransmissionPain TransmissionPain TransmissionPain Transmission
Pain Pain perceptionperceptionPain Pain perceptionperception
Spinal Spinal cordcord
Spinal Spinal cordcord
EnkephalinEnkephalininter-inter-neuronneuron
EnkephalinEnkephalininter-inter-neuronneuron
NociceptorNociceptorNociceptorNociceptor
DescendingDescendingpathwaypathway
DescendingDescendingpathwaypathway
AscendingAscendingpathwaypathway
AscendingAscendingpathwaypathway
Descending Pain Control Pathways
Descending Descending impulseimpulse
Descending Descending impulseimpulse
EnkephalinEnkephalinEnkephalinEnkephalin
OpioidOpioidreceptorreceptor
OpioidOpioidreceptorreceptor
Opportunities for Pain Treatment
At the receptor Along the nerve At receptors in spinal column an
d brain
Acute vs chronic Nociceptive vs Neuropathic
PainPain
Acute vs. Chronic PainAcute vs. Chronic PainAcute vs. Chronic PainAcute vs. Chronic Pain
C fibers:C fibers:dull, aching, burning paindull, aching, burning painC fibers:C fibers:dull, aching, burning paindull, aching, burning pain
Dorsal Dorsal rootroot
ganglionganglion
Dorsal Dorsal rootroot
ganglionganglionTo brainTo brainTo brainTo brain
A-delta fibers:A-delta fibers:sharp,shooting painsharp,shooting painA-delta fibers:A-delta fibers:sharp,shooting painsharp,shooting pain
Ascending Ascending pain pain
pathwaypathway
Ascending Ascending pain pain
pathwaypathway
Tissue Tissue injuryinjury
Tissue Tissue injuryinjury
Spinal Spinal cordcord
Spinal Spinal cordcord
Nociceptive Pain
Ascending Ascending pain pain
pathwaypathway
Ascending Ascending pain pain
pathwaypathway
Nerve Nerve injuryinjury
Nerve Nerve injuryinjury Spinal Spinal
cordcordSpinal Spinal cordcord
Neuropathic Pain
Principles of Pain Management Gold standard: patient determines severity Tradition: pain has been undertreated Prevention or early treatment best Pain kills Pain is real Balance pain relief with side effects of drug
s
Antipyretic-analgesic and Anti-inflammatory Drugs
Non-steroidal anti-inflammatory
drugs, NSAIDs.
Aspirin-like drugs.
Mechanism of NSAIDs
Arachidonic acid, AA
Prostaglandin, PGLeukotrienes, LTs
PGE2 PGF2 PGI2 TXA2
PLAPLA22
phospholipid
COXCOX
NSAIDs
Salicylates Aspirin and NSAIDs Anti-inflammatory Inhibits cyclooxygenase pathway
for breakdown of arachidonic acid to prostaglandins and thromboxane
Ibuprofen, Naprosyn & naproxen COX-2 inhibitors
Acetaminophen Inhibits synthesis of prostaglandin i
n CNS but not in periphery.
No anti-inflammatory or anti-platelet effects but good for mild pain and to reduce fever
Adverse reactions rare. Overdose may cause liver disease esp in persons who regularly consume alcohol.
Antidepressants in neuropathic pain Ergotamine in migraine headache Anticonvulsants in neuropathic pain or migra
ne headache NMDA antagonists for neuropathic pain Centrally acting alpha2 agonists such as cloni
dine Anesthetics (lidocaine or bupivicaine) (ketami
ne) Radiopharmaceuticals for cancer bone pain
Other Pain Management Drugs
NMDA
N-methyl-D-aspartate N-methyl-D-aspartate (NMDA) (NMDA) receptor opens receptor opens channel for channel for CaCa++++ influx. influx. This can lead to nerve dThis can lead to nerve damage and pain. amage and pain.
MemantineMemantine blocks blocks the NMDA receptor. the NMDA receptor. Phase II study: diabPhase II study: diabetic subjects with netic subjects with neuropathic pain expeuropathic pain experienced 29% less erienced 29% less pain than placebo-tpain than placebo-treated subjects.reated subjects.
CaCa++++CaCa++++
NerveNerve
An Alpha 2 Agonist?An Alpha 2 Agonist?
Reuptake pump
Reuptake pump
NENE
RR
NENE NENEPost-
synaptic cell
Post-synaptic
cell
Alpha 2 presynaptic receptor
Alpha 2 presynaptic receptor
RR
RR
RR
NENEPost-
synaptic cell
Post-synaptic
cell
Alpha 2 presynaptic receptor
Alpha 2 presynaptic receptor
When stimulated, When stimulated, they inhibit nerve they inhibit nerve transmission. transmission.
NENE
RR
Post-synaptic
cell
Post-synaptic
cell
Alpha 2 presynaptic receptor
Alpha 2 presynaptic receptor
Clonidine given epidurally or Clonidine given epidurally or orally blocks pain messages orally blocks pain messages from neuropathic origin.from neuropathic origin.
A highly lipid soluble drug, what is the cA highly lipid soluble drug, what is the chance that epidurally-placed clonidine whance that epidurally-placed clonidine would get into the blood stream? ould get into the blood stream?
NENE
RR
RR
Post-synaptic
cell
Post-synaptic
cell
Alpha 2 presynaptic receptor
Alpha 2 presynaptic receptor
What would the SNS blockade What would the SNS blockade do to the blood pressure?do to the blood pressure?
NENE
RR
RR
Post-synaptic
cell
Post-synaptic
cell
Alpha 2 presynaptic receptor
Alpha 2 presynaptic receptor