Transcript Chapter 15 - Dr. Gerry Cronin

Focus on
PHARMACOLOGY
ESSENTIALS FOR HEALTH PROFESSIONALS
CHAPTER
15
Analgesic,
Antipyretic, and
Anti-Inflammatory
Agents
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Mechanism of Action of Acetaminophen Animation
Mechanism of Action of Morphine Animation
Mechanism of Action of Oxycodone Animation
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Terms
• Analgesics: relieve pain without
significantly disturbing consciousness or
altering actions of sensory nerves
• Antipyretics: reduce fever
• Some of these types of drugs also have
anti-inflammatory properties
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Pain
• Central nervous system’s reaction to
potentially harmful stimuli
characterized by physical discomfort
– Acute: severe pain with sudden onset;
serves as early warning to seek medical
help to prevent damage to body
– Chronic: lasting a long time or marked by
frequent recurrence
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Pain Stimuli
• May result from inflammatory process
that causes tissue injury
– Histamine, prostaglandins, serotonin, and
bradykinin are released and initiate action
potential along sensory nerve fiber.
– Nociceptors (pain receptors) are activated
and message sent to brain cortex.
– Appropriate autonomic and reflect
responses are activated.
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Figure 15-1
Reflex responses to pain.
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Neurotransmitters
• Endorphins and enkephalins are
neurotransmitters that can bind with
opiate receptors in the CNS and inhibit
transmission of pain impulses.
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Figure 15-2
Endogenous analgesic compounds released after pain stimuli.
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Nonsteroidal Anti-Inflammatory
Drugs (NSAIDs)
• Group of drugs that include salicylates
and antipyretics
• Used to relieve inflammation, swelling,
stiffness, and joint pain of arthritis;
treat menstrual cramps, gout attacks,
bursitis, tendonitis, sprains, and muscle
strains
• Mechanism of action: believed to act by
blocking prostaglandin synthesis
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Aspirin (Bayer, Others): Uses
• Most common salicylate
• Used as an antipyretic and analgesic to
relieve pain of headache, fever,
muscular aches and pains
• One of safest and most effective drugs
to relieve fever
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Aspirin: Adverse Effects
• Uncommon: dyspepsia, nausea,
vomiting, occult bleeding
• Serious: massive GI hemorrhage at
high doses and in elderly patients
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Aspirin: Contraindications
• Avoid in patients with GI disturbances,
particularly hemorrhaging ulcers.
• Use with caution in patients on
anticoagulant therapy or who are
taking uricosurics.
• Aspirin interacts with antidiabetic drugs
and oral anticoagulants.
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Aspirin and Reye’s Syndrome
• Use of aspirin in treatment of fever in
children who have chickenpox may
cause Reye’s syndrome.
• Aspirin should not be prescribed for
children who have upper respiratory
viral infections or chickenpox.
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Salicylates and GI Bleeding
• Elderly patients who are vulnerable to
GI bleeding should not take salicylates.
• Patients should request emergency help
for bloody urine, loss of hearing or
vision, confusion, convulsions, diarrhea,
difficulty swallowing, dizziness, severe
drowsiness, increased thirst, nausea or
vomiting.
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Aspirin: Patient Information
• Advise menstruating women to avoid
aspirin if menstrual bleeding is heavy.
• Advise pregnant women to avoid
aspirin in last trimester and during
lactation.
• Instruct patients to discontinue aspirin
1 week before or after surgery.
• Instruct patients to avoid drinking
alcohol while taking aspirin.
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Ibuprofen (Motrin, Advil): Uses
• Nonsalicylate used for analgesic, antiinflammatory, and antipyretic activities
• Rheumatoid arthritis, osteoarthritis,
and arthritis
• Mild to moderate pain, dysmenorrhea,
and fever
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Ibuprofen: Adverse Effects
• Common: nausea, occult blood loss,
peptic ulceration, diarrhea,
constipation, abdominal pain,
dyspepsia, flatulence, heartburn,
decreased appetite
• Serious: azotemia, cystitis, hematuria,
aplastic anemia, hypoglycemia,
hyperkalemia
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Ibuprofen: Contraindications
• Avoid in pregnant patients and those
with angioedema, nasal polyps, or
bronchospastic reaction to NSAIDs.
• Use cautiously in patients with GI
disorders, hepatic or renal disease,
hypertension, or preexisting asthma.
• Ibuprofen may interact with
antihypertensives, furosemide, and
thiazide diuretics.
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Ibuprofen: Patient Information
• Breastfeeding women should not take
ibuprofen.
• Advise patients to notify their physician
if blood appears in stool, vomitus, or
urine, or if they have a new skin rash,
pruritus, or jaundice.
• Warn patients not to consume alcohol
or take aspirin or other NSAIDs with
ibuprofen.
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Indomethacin (Indocin): Uses
• Treatment of rheumatoid arthritis,
rheumatoid spondylitis, osteoarthritis,
bursitis, tendonitis, gouty arthritis, and
patent ductus arteriosus in premature
infants
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Indomethacin: Adverse Effects
• Common: GI ulceration, hemorrhage,
GI bleeding, increased pain in
ulcerative colitis, gastritis, nausea, and
vomiting
• Serious: hepatic toxicity, aplastic
anemia, hemolytic anemia, asthma,
urticaria, depression, mental confusion,
coma, convulsions
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Indomethacin: Contraindications
• Avoid in patients with history of aspirinor NSAID-induced asthma, rhinitis, or
urticaria.
• Avoid in pregnant or breastfeeding
women.
• Use cautiously in patients with epilepsy,
parkinsonism, and hepatic or renal
disease.
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Indomethacin: Contraindications
• Interacts with aminoglycosides,
cyclosporine, methotrexate,
antihypertensives, furosemide, and
thiazide diuretics
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Indomethacin: Patient Information
• Advise patients to notify their physician
if they develop skin rash, breathing
problems, or visual disturbances (signs
of hypersensitivity).
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Selective COX-2 Inhibitors:
Mechanism of Action
• One group of NSAIDs that selectively
inhibits cyclooxygenase-2 (COX-2)
(enzymes required to produce
prostaglandins from arachidonic acid;
appear to be made in macrophages in
response to local tissue damage)
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Table 15-1
Selective COX-2 Inhibitors
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COX-2 Inhibitors: Uses
• Celecoxib (Celebrex): treatment of
osteoarthritis and rheumatoid arthritis
• Newer COX-2 inhibitor, meloxicam
(Mobic) is labeled for treatment of
osteoarthritis.
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COX-2 Inhibitors: Adverse Effects
• Common: abdominal pain, dyspepsia,
diarrhea
• Serious: myocardial infarction and
stroke
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COX-2 Inhibitors:
Contraindications
• Use cautiously in patients with asthma,
hypertension, lower extremity edema,
congestive heart failure, or fluid
retention, and in pregnant or lactating
women.
• Avoid in patients with hepatic
impairment or advanced renal disease.
• Interacts with ACE inhibitors,
fluconazole, and lithium.
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COX-2 Inhibitors:
Patient Information
• Advise patients to report unexplained
weight gain, skin rash, nausea, fatigue,
lethargy, jaundice, flu-like symptoms,
black tarry stools, or upper GI distress
• Instruct patients to avoid aspirin, other
NSAIDs, alcohol, and tobacco when
taking meloxicam. Avoid celecoxib
during the third trimester of pregnancy
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Acetaminophen (Tylenol):
Mechanism of Action
• Thought to be inhibition of
prostaglandin in peripheral nervous
system, making sensory neurons less
likely to receive pain signals
• Acetaminophen blocks peripheral pain
impulses to lesser degree than other
NSAIDs; lacks anti-inflammatory action
of salicylates.
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Acetaminophen: Uses
• Treatment of musculoskeletal pain,
headache, dysmenorrhea, myalgias,
neuralgias, arthritic and rheumatic
conditions
• Reduces fever and discomfort of
common cold and viral infections
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Acetaminophen: Adverse Effects
• Usually well-tolerated in therapeutic
doses
• Long-term use: skin eruptions and
urticaria, hypotension, hepatotoxicity
• Overdose: hepatotoxicity, coma,
internal bleeding (antidote is
acetylcysteine)
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Acetaminophen: Contraindications
• Use cautiously in children younger than
3 years.
• Avoid in patients with alcoholism,
malnutrition, or thrombocytopenia.
• Safety during pregnancy and lactation
is not established.
• Interacts with barbiturates,
carbamazepine, phenytoin, and
rifampin
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Acetaminophen:
Patient Information
• Advise patients to avoid alcohol
because regular consumption of alcohol
and acetaminophen may cause severe
liver damage and even death.
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Mechanism of Action of
Acetaminophen Animation
Click on the screenshot to view an animation showing the mechanism of
action of acetaminophen.
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Opiates: Mechanism of Action
• Opiates: drugs derived from opium
poppies; morphine and codeine
• Opioid: general term referring to
natural, synthetic, or endogenous
morphine-related substances
• Analgesic effects produced by binding
to opioid receptors (mu, kappa, and
delta); mostly affect mu receptors
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Table 15-2
Classifications of Opioid Analgesics
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Table 15-2 (continued) Classifications of Opioid Analgesics
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Table 15-2 (continued) Classifications of Opioid Analgesics
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Table 15-2 (continued) Classifications of Opioid Analgesics
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Morphine (Astramorph, Others):
Uses
• Management of all types of moderate to
severe pain
• Derivatives are used for cough
inhibition, treatment of GI pain,
relieving pain of myocardial infarction
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Morphine: Adverse Effects
• Common: nausea and vomiting,
constipation, dry mouth, biliary tract
spasms, dizziness, sedation, pruritus
• Serious: respiratory depression
• Physical and psychological dependence
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Morphine: Contraindications
• Avoid in patients with asthma,
emphysema, head injury, increased
intracranial pressure, severe liver or
kidney dysfunction, acute ulcerative
colitis, or convulsive disorders.
• Use cautiously in patients with prostatic
hypertrophy.
• Interacts with alcohol, monoamine
oxidase inhibitors, meperidine
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Morphine: Patient Information
• Instruct patients not to take morphine
if breathing rate is less than 12 breaths
per minute or systolic blood pressure is
less than 110 mm Hg.
• Advise patients to request symptomatic
relief for constipation and to drink
plenty of water.
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Mechanism of Action of Morphine
Animation
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action of morphine.
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Codeine: Uses
• Used to induce sleep in presence of
mild pain
• Used as analgesic, sedative, hypnotic,
antiperistaltic, and antitussive
• Commonly given in combination with
aspirin, acetaminophen, and other
agents (Schedule III drug in
combination)
• Schedule II drug (alone)
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Codeine: Adverse Effects
• Common: postural hypotension, nausea
and vomiting, constipation, miosis
• Serious: cortical and respiratory
depression
• Tolerance, dependence, and addiction
can occur
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Codeine: Contraindications
• Avoid in patients with respiratory
insufficiency, bronchial asthma, and
increased intracranial pressure.
• Interacts with alcohol, cimetidine,
antidepressants, and neuroleptics
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Codeine: Patient Information
• Instruct patients to take only as
directed because overuse can lead to
dependence.
• Advise patients to avoid alcohol and
other CNS depressants.
• Advise patients that urine retention and
constipation can occur and to rise
slowly from lying position to avoid
dizziness.
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Hydrocodone (Hycodan):
Mechanism of Action
• Morphine derivative similar to codeine
• Suppresses cough reflex by direct
action on cough center in medulla
• Acts as CNS depressant to relieve
moderate to severe pain
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Hydrocodone: Uses
• Used to relieve nonproductive cough
and to relieve moderate to severe pain
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Hydrocodone: Adverse Effects
• Common: dry mouth, nausea and
vomiting, constipation, sedation,
dizziness, drowsiness
• Serious: respiratory depression
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Hydrocodone: Contraindications
• Avoid in patients with hypersensitivity
or in lactating women.
• Use cautiously in patients with asthma,
emphysema, history of drug abuse, and
respiratory depression.
• Interacts with alcohol and other CNS
depressants
• Can be used in children younger than 1
year and in pregnant women
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Hydrocodone:
Patient Information
• Instruct patients to avoid hazardous
activities.
• Advise patients to drink plenty of fluids
and to take only as directed.
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Oxycodone (OxyContin):
Mechanism of Action
• Precise mechanism not clear
• Binds to specific receptors in various
sites of CNS to alter both perception of
pain and emotional response to pain
• Oxycodone is as potent as morphine
and 10–12 times more potent than
codeine.
• Schedule II drug
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Oxycodone: Uses
• Relief of moderate to severe pain
(bursitis, dislocations, simple fractures,
other injuries)
• Postoperative and postpartum pain
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Oxycodone: Adverse Effects
• Common: euphoria, dysphoria, lightheadedness, dizziness, sedation,
anorexia, nausea and vomiting,
constipation
• Serious: jaundice, hepatotoxicity,
respiratory depression
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Oxycodone: Contraindications
• Avoid in pregnancy and lactation, and
in children.
• Use cautiously in patients with
alcoholism, renal or hepatic disease,
viral infections, ulcerative colitis,
gallbladder disease, head injury, acute
abdominal conditions, hypothyroidism,
prostatic hypertrophy, and respiratory
depression.
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Oxycodone: Contraindications
• Interacts with antidepressants,
anxiolytics, antihistamines, pain
relievers, seizure medications, and
muscle relaxants
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Oxycodone:
Patient Information
• Instruct patients to avoid hazardous
activities and alcohol.
• Advise patients to take the drug in the
form prescribed without crushing,
chewing, or breaking.
• Advise patients to take only the dose
prescribed.
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Mechanism of Action
of Oxycodone Animation
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action of oxycodone.
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Age Differences in Narcotic
Metabolism
• Metabolism of narcotics is slower in
elderly patients, leading to possible
confusion and respiratory depression.
• Children and infants eliminate narcotics
at a different rate than do adults, so
dosing is difficult.
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Opioid Antagonists
• Naloxone (Narcan): prescribed for
narcotic overdose, reversal of narcotic
respiratory depression
• Naltrexone (Trexan, ReVia): adjunct for
maintaining opioid-free state in
detoxified addicts; management of
alcohol dependence
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Buprenorphine (Buprenex):
Mechanism of Action
• Synthetic centrally acting narcotic
analgesic
• Opiate agonist–antagonist
• Has high affinity for mu-opioid
receptors (agonist action)
• Acts as antagonist at kappa-opiate
receptors in CNS
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Buprenorphine: Uses
• Treatment of moderate to severe
postoperative pain
• Administered for pain associated with
cancer, accidental trauma, urethral
calculi, myocardial infarction
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Buprenorphine: Adverse Effects
• Common: sedation, drowsiness,
vertigo, dizziness, headache, amnesia,
euphoria, insomnia
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Buprenorphine: Contraindications
• Safety during pregnancy, lactation, and
in children younger than 13 years is not
established
• Interacts with alcohol and diazepam
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Buprenorphine:
Patient Information
• Instruct patients to avoid driving or
engaging in hazardous activities.
• Advise patients to avoid alcohol and
other CNS depressants.
• Advise female patients to not breast
feed.
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Fentanyl (Duragesic, Sublimaze)
• Analgesic and sedative used during
operative and perioperative periods
• Interacts with alcohol, other CNS
depressants, monoamine oxidase
inhibitors
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Fentanyl (Duragesic, Sublimaze)
• Instruct postoperative patients to
report muscle rigidity or weakness;
unusual postoperative muscle
movement of the extremities, eyes, or
neck; or breathing difficulties.
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Meperidine (Demerol)
• Synthetic opioid that acts on the CNS
and organs composed of smooth
muscle
• Principally induces analgesia and
sedation
• Used preoperatively, to treat moderate
to severe pain, as obstetric analgesia
and to support anesthesia
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Meperidine: Adverse Effects
• Common: dizziness, sedation, nausea
and vomiting, sweating
• Serious: respiratory depression or
arrest, circulatory depression, shock,
cardiac arrest
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Meperidine: Contraindications
• Avoid in patients taking monoamine
oxidase inhibitors.
• Use cautiously in patients taking other
opioid analgesics, general anesthetics,
phenothiazines, sedatives, tricyclic
antidepressants, and other CNS
depressants.
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Meperidine:
Patient Information
• Advise patients to move carefully and
avoid smoking.
• Instruct patients to avoid driving and
other hazardous activities until
drowsiness and dizziness have passed.
• Instruct patients to avoid alcohol and to
not breast feed.
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Methadone (Dolophine)
• Synthetic opioid analgesic that binds
with opiate receptors in the CNS,
altering perception and emotional
response to pain
• Used for relief of moderate to severe
pain and for detoxification of opioid
addicts
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Methadone (Dolophine)
• Adverse effects, contraindications, and
patient teaching similar to those of
fentanyl
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Pentazocine (Talwin)
• Synthetic narcotic agonist–antagonist
analgesic (Schedule IV)
• Action similar to morphine
• For control of moderate to severe pain,
preoperative analgesia or sedation, and
as supplement to surgical anesthesia
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Pentazocine (Talwin)
• Adverse effects, contraindications,
patient information similar to those of
other opioids
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