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Narcotics and Analgesics

Pharmacology
By Linda Self
Pain
Universal, complex, subjective
experience
Number one reason people take
medication
Generally is related to some type of
tissue damage and serves as a
warning signal
Scope of the Problem
Increases as Baby Boomers age
25 million people suffer acute pain
related to surgery or injury
Chronic pain affects 250 million
Americans
Is a multibillion dollar industry
Much ignorance exists about this
complaint
Gate Control Theory of Pain
Gate control theory of pain is the idea
that physical pain is not a direct
result of activation of pain receptor
neurons, but rather, its perception is
modulated by interaction between
different neurons
Gate Control Theory of Pain
Nerve fibers (A delta (fast channels))
and C fibers (slow channels) transmit
pain impulses from the periphery
Impulses are intercepted in the dorsal
horns of the spinal cord, the
substantia gelatinosa
In this region, cells can be inhibited
or facilitated to the T-cells (trigger
cells)
Gate Control Theory of Pain cont.
When cells in the substantia
gelatinosa are inhibited, the gate to
the brain is closed
When facilitated, the gate to the
brain is open
Gate Control Theory of Pain
Similar gating mechanisms exist in
the nerve fibers descending from the
thalamus and the cortex. These areas
of the brain regulate thoughts and
emotions. Thus, with a pain stimulus,
ones thoughts and emotions can
actually modify the pain experience.
Pathophysiological Response
Tissue damage activates free nerve
endings (nociceptors) of peripheral
nerves
Pain signal is transmitted to the
spinal cord, hypothalamus, and
cerebral cortex
Pain is transmitted to spinal cord by
A-delta fibers and C fibers
Pathophysiological Response
A-delta fibers transmit fast, sharp,
well-localized pain signals
C fibers conduct the pain signal
slowly and produce poorly localized,
dull, or burning type of pain
Thalamus is the relay station for
incoming stimuli, incl. pain
Pain Fibers and Pathways
A delta fibers found in the skin and muscle,
myelinated, respond to mechanical stimuli.
Produce intermittent pain.
C fibers distributed in the muscle as well as
the periosteum and the viscera. These
fibers are unmyelinated, conduct thermal,
chemical and strong mechanical stimuli.
Produce persistent pain.
Inhibitory and Facilitatory
Mechanisms
Neurotransmitterschemicals that exert
inhibitory or excitatory activity at post-
synaptic nerve cell membranes. Examples
include: acetylcholine, norepinehprine,
epinephrine, dopamin, and serotonin.
Neuromodulatorsendogenous opiates.
Hormones in brain. Alpha endorphins, beta
endorphins and enkephalins. Help to relieve
pain.
Opioid Receptors
Opioid receptorsbinding sites not
only for endogenous opiates but also
for opioid analgesics to relieve pain.
Several types of receptors: Mu,
Kappa, Delta, Epsilon and Sigma.
Mu Receptors
Location: CNS incl. brainstem, limbic
system, dorsal horn of spinal cord
Morphine sulfate and morphine
sulfate agonists bind to Mu receptors
Sources of Pain
Nociceptivefree nerve endings that
receive painful stimuli
Neuropathic damaged nerves
Narcotic Analgesics
Relieve moderate to severe pain by
inhibiting release of Substance P in
central and peripheral nerves;
reducing the perception of pain
sensation in brain, producting
sedation and decreasing emotional
upsets associated with pain
Narcotic Analgesics
Can be given orally, IM, sub q, IV or
even transdermally
Orally are metabolized by liver,
excreted by kidneycaution if
compromised
Morphine and meperidine produce
metabolites
Widespread effects: CNS, Resp., GI
NarcoticsMechanisms of Action
Bind to opioid receptors in brain and
SC and even in periphery
Indications for Use
Before and during surgery
Before and during invasive diagnostic
procedures
During labor and delivery
Tx acute pulmonary edema
Treating severe, nonproductive cough
Contraindications to Use
Respiratory depression
Chronic lung disease
Chronic liver or kidney disease
BPH
Increased intracranial pressure
Hypersensitivity reactions
Changing Philosophy on Pain
Undermedicated
Titrate to comfort
Management Considerations
age-specific considerations
Morphine often drug of choicenon-
ceiling. Other nonceiling drugs
include: hydromorphone, levorphanol
and methadone
Use non-narcotic when able
Combinations may work by different
mechanisms thus greater efficacy
(e.g. Tylenol w/codeine)
Route selections
Oral preferred
IV most rapidPCA allows self
administration. Basal dosage. More
effective, requires less dosing.
Epidural, intrathecal or local injection
Can use rectal suppositories or
transdermal routes
Dosage
Dosages of narcotic analgesics should
be reduced for clients receiving other
CNS depressants such as other
sedative-type drugs, antihistamines
or sedating antianxiety medications
Scheduling
Give narcotics before encouraging
turning, coughing and deep breathing
in post-surgical patients
Automatic stop orders after 72h
In acute pain, narcotic analgesics are
most effective when given
parenterally and at start of pain
Individual Drugs
Agonists have activity on mu and
kappa opioid receptors
Agonist/antagonists have agonist
activity in some receptors;
antagonists in others. Have lower
abuse potential than pure agonists;
because of antagonismcan produce
withdrawal symptoms
Antagonists are antidote drugs
Agonists
Alfenta (alfentanil)short duration
Codeine
Sublimaze or Duragesic (Fentanyl)short
duration
Dilaudid (hydromorphone)
Demerol (meperidine)preferred in urinary
and biliary colic, less resp. depression
newborns
Morphine
OxyContin
Agonists cont.
Darvon (propoxyphene)
Ultram (tramadol)
Methadone
Agonists/Antagonists
Have lower abuse potential than pure
agonists
Buprenex (buprenorphine)
Nubain (nalbuphine)
Talwin (pentazocine)
Stadol (butohanol)also in nasal
spray
Antagonists
Revex (nalmefene)longer duration
of action than Narcan
Narcan (naloxone)
ReVia (naltrexone)-used in
maintenance of opiate-free states in
opiate addicts
Dietary and Herbal Supplements
Zostrix (capsaicin)from cayenne
peppers; topical indicated for post-
herpetic neuralgia, neuropathic
pain=Substance P
Cancer
Give on a regular schedule
Oral, rectal and transdermal are preferred
over IV
Oxycodone and a non-narcotic analgesic
may have additive effects
MS or other for severe pain
Long acting for chronic pain with fast acting
meds for break-through pain
May use TCAs, anti-emetics, stool regimen
Management of Withdrawal
Symptoms
Methadone
Clonidine (norepinephrine)
Gradually decrease dosing so not to
cause withdrawal s/s
Analgesic,Antipyretic, and Anti-
inflammatory Drugs
Mechanism of actioninactivate
cyclo-oxygenases, enzymes required
for the production of prostaglandins
ASA and traditional NSAIDs
inhibit both COX 1 and COX 2
COX 1 is present in all tissues esp.
GI, kidneys, endothelial cells and in
platelets
Cox 1 cont.
Prostaglandins important in:
1. Protection of kidneys and stomach
2. Regulate vascular tone and platelets
in CV system
COX 2
Found in brain, bone, kidneys, GI
tract, and the female reproductive
system
Overall, prostaglandins produced by
COX 2 are associated with pain and
inflammation
Actions of the COXs
Act on hypothalamus to decrease response
to pyrogens and reset the thermostat
Prevent prostaglandins from increasing the
pain and edema produced by other
substances released by damaged cells
COX 1-Antiplatelet activity for life of
platelet7-10 days plus interfere w/blood
coagulation and increase risk for bleeding
Indications for Use
Treat mild to moderate pain or
inflammation
Musculoskeletal disorders; HA;
dysmenorrhea, minor trauma and
surgery
Low dose ASA for risk of MI or stroke
Celebrex is indicated for familial
polyposis
Contraindications to Use
PUD
GI or bleeding disorders
Hypersensitivity reactions
Impaired renal function
If allergic to ASA
In children, ASA contraindicated in
presence of viruses=Reyes syndrome
Celebrex if allergic to sulfonamides
Reyes
Seen in children under 15 after an
acute viral illness
Results in encephalopathy, fatty
infiltration of the liver, pancreas,
kidneys, spleen, and lymph nodes
Cause is unknown
Contraindications
Toradol (ketoralac) not used in labor
and delivery or during any major
surgery
OTC preps contraindicated in
alcoholics due to possible liver
damage
Aspirin (ASA)
Home remedy for headaches, colds,
influenza and other respiratory
infections
For fever
For inflammation
ASA and COX 2 are ok, COX 2 have
little effect on platelet function
ASA cont.
Poisoning can occur with large doses.
Saturate the metabolic pathway, slow
elimination and cause drug accumulation
If overdose, measure serum levels
Recognize s/s: N/V, fever, fluid and lyte
deficiencies, tinnitus, decreased hearing,
hyperventilation, confusion, visual
changes>>>>delirium, stupor and coma
ASA salicylism
Gastric lavage
Activated charcoal
IV bicarbonate so more rapid
excretion
hemodialysis
NSAIDS
Propionic acid derivatives such as
ibuprofen, ketoprofen (Orudis),
naproxen and fenoprofen (Nalfon)
Acetic acid derivatives include
indomethacin (Indocin), sulindac
(Clinoril) and tolmetin (Tolectin)---
these drugs have more severe
adverse reactions than the proprionic
acid derivatives
NSAIDS
IV indomethacin is approved for the
tx of patent ductus arteriosus in
premature infants.
Remember: patent ductus is a
communication between the
pulmonary artery and the aorta
NSAIDS
Toradol (ketoralac) is used only for
pain. Is the only NSAID that can be
given by injection. Use limited to 5
days as can cause bleeding.
Oxicam drugs include Mobic
(meloxacam) and Feldene (piroxicam)
Celebrex (celecoxib)
Affect bleeding only while drug is still
in the system
Effects of Nonsteroidals on Other
Drugs
Decrease effects of ACEI, beta
blockers and diuretics
Affect sodium and water retention
Inhibit renal prostaglandin synthesis
Acetaminophen
Equal in effectiveness to ASA in
analgesic and antipyretic effects
Lacks anti-inflammatory actions
Ethanol induces drug-metabolizing
enzymes in liver. Resulting rapid
metabolism of acetaminophen
produces enough toxic metabolite to
exceed glutathione. Need glutathione
to inactivate toxic metabolites. P. 114
Acetaminophen Poisoning
Toxicity occurs with 20g or more.
Creates toxic metabolite that is inactivated
by glutathione.
OD supply of glutathione is depleted and
toxic metabolite damages liver cells
Not to exceed 4g/day
Treatmentgastric lavage, charcoal,
antidote is Mucomyst (acetylcysteine).
Provides cysteine, a precursor to
glutethione.
Drugs used in Gout and
Hyperuricemia
Zyloprim (allopurinol)prevents or
treats hyperuricemia
Uric acid is formed by purine
metabolism and an enzyme xanthine
oxidase. Allopurinol prevents
formation by inhibiting xanthine
oxidase.
Antigout Medications
Colchicineused to treat or prevent acute
attacks of gout. Drug of choice for acute
attacks. Decreases inflammation by
affecting leukocytes.
Benemid (probenecid) increases urinary
excretion of uric acid. Not effective in acute
attacks.
Anturane (sulfinpyrazone) uricosuric similar
to Benemid. Not for acute attacks.
Guidelines for Treating Gout
Maintenance drugs are Zyloprim,
Benemid and Anturane
Colchicine needed for several weeks
to prevent acute attacks while serum
levels are being lowered
Need high fluid intake, alkaline urine
to prevent renal calculi
Drugs Used for Migraines
Selective serotonin 5-HT1 receptor
agonists
Increase serotonin in the brain
Constrict blood vessels
Contraindicated in patients with
history of MI,, angina, uncontrolled
htn.
Drugs used for migraines
Drugs vary in onset with sub q
sumatriptan acting the most rapidly
and starting within 10 minutes; most
clients get relief within 1-2 hours
Drugs are metabolized in the liver by
monoamine oxidase or by cytochrome
p450 enzymes; sub q administrations
causes more adverse effects than the
oral drugs
Migraine Meds
Ergotamine tartrateergot alkaloid
used only in tx of migraine
Work by constricting blood vessels
Most effective when given sublingual
or by inhalation
Contraindicated in pregnancy, htn,
PVD, CAD, renal or hepatic disease
and even in severe infections
Guidelines for Treating Migraine
Start out with acetaminophen,
aspirin, or other NSAIDs
Moderate to severe migraines,
sumatriptan or other related drugs
are useful
For severe and frequent migraines,
prophylaxis is indicated. Use ASA and
NSAIDs.
Guidelines for Treating migraines
For menstrual migraines, start tx one
week before and during menses
Other drugs indicated for tx include
beta adrenergic blocking agents such
as Inderal
Guidelines for Treating Arthritis
Control pain and inflammation
Rest, exercise,and PT
OsteoarthritisCOX1, COX2,
glucosamine, intraarticular injections
of corticosteroids or hyaluronic acid
(Synvisc) to act as shock absorber
Rheumatoid Arthritis
NSAIDs
Corticosteroids
Immunosuppressantsmethotrexate
Enbrel, Remicade and Arava. Affect
tumor necrosis factor and other
cytokines.
Questions or Discussion