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Chapter 4: Drugs for Pain, Fever,
and Inflammation
Copyright © 2010 Wolters Kluwer Health | Lippincott Williams & Wilkins
Conditions Commonly Treated by Pain,
Fever, and Inflammation Drugs
• Mild-to-moderate pain caused by injury or surgery
• Fever, headaches, & painful menstruation
• Rheumatoid arthritis
• Osteoarthritis
• Chronic pain associated with cancer, AIDS, multiple
sclerosis, or sickle cell disease
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Nonopioid Analgesics, Antipyretics, and
NSAIDs
• Analgesics: drugs that control pain without causing
patient to lose consciousness
–
Nonopioid: not derived from opium plant; do not cause physical
dependence in patients
–
Opioid: synthetic or derived from opium plan; may cause
physical dependence
• Nonsteroidal Anti-Inflammatory Drugs (NSAIDs)
–
Reduce redness, swelling, pain, & heat of inflammation
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Nonopioid Analgesics, Antipyretics, and
NSAIDs (cont’d)
• Nonopioid analgesics & NSAIDs
–
Stop body from producing prostaglandin, which has 2 effects:
• Analgesic effect: reduce pain response
• Anti-inflammatory effect: reduce inflammation
–
Are antipyretics, meaning they can reduce body temperature to
control fever
–
Four main groups:
• Salicylates
• Nonsalicylate analgesics
• NSAIDs
• Urinary tract analgesic phenazopyridine hydrochloride
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Nonopioid Analgesics, Antipyretics, and
NSAIDs (cont’d)
• Salicylates
–
Among most commonly used medications for controlling pain,
fever, & inflammation
–
Mainly used for following:
• Relieving mild-to-moderate pain
• Reducing fever
• Reducing inflammation from rheumatic fever, rheumatoid
arthritis, & osteoarthritis
–
Relieve headache & muscles at same time
–
Not effective for relieving pain of organs or smooth muscles or
controlling severe pain from trauma
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Nonopioid Analgesics, Antipyretics, and
NSAIDs (cont’d)
• Salicylates
• Adverse Reactions
–
Acetylsalicylic acid
–
Gastric distress
–
Choline magnesium
trisalicylate
–
Nausea
–
Vomiting
–
Bleeding tendencies
–
Choline salicylate
–
Diflunisal & salsalate
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Nonopioid Analgesics, Antipyretics, and
NSAIDs (cont’d)
• Acetaminophen
–
Belongs to a group of drugs called para-aminophenol (APAP)
derivatives
–
An OTC drug with analgesic & antipyretic properties
–
Affects central nervous system
–
Relieves fever by acting on hypothalamus
–
Does not have an anti-inflammatory effect
–
Does not affect way blood platelets work to form clots
–
Used to treat fever, headache, muscle ache, & general pain
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Nonopioid Analgesics, Antipyretics, and
NSAIDs (cont’d)
• Nonsteroidal Anti-Inflammatory Drugs
–
Typically used to combat inflammation
–
Have analgesic & antipyretic effects
–
May affect blood platelets, but effects are temporary
–
Are absorbed through GI tract
–
Two types
• Nonselective: block both COX-1 & COX-2 enzymes
• Selective: block only COX-2 enzymes
–
May cause higher risk for heart attack, stroke, or kidney
problems
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Nonopioid Analgesics, Antipyretics, and
NSAIDs (cont’d)
• Nonselective Nonsteroidal
Anti-Inflammatory Drugs
–
Nabumetone
–
Naproxen
–
Diclofenac
–
–
Etodolac, fenoprofen, &
flurbiprofen
Oxaprozin, piroxicam, &
sulindac
–
Misoprostol
–
Ibuprofen
–
Indomethacin
–
Ketoprofen, ketorolac, &
meloxicam
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Nonopioid Analgesics, Antipyretics, and
NSAIDs (cont’d)
• Adverse Reactions to
Nonselective Nonsteroidal
Anti-Inflammatory Drugs
–
Constipation
–
Diarrhea
–
Dizziness
–
Drowsiness
–
GI upset or pain
–
GI bleeding
–
Ulcers
–
Headache
–
Nausea
–
Rash
–
Visual disturbances
–
Vomiting
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Nonopioid Analgesics, Antipyretics, and
NSAIDs (cont’d)
• Selective Nonsteroidal Anti-Inflammatory Drugs
–
Reduce possibility of some adverse GI effects, such as ulcers,
compared with nonselective NSAIDs
–
Celecoxib (Celebrex) is only COX-2 inhibitor currently available
–
Used to relieve pain & inflammation associated with following:
• Osteoarthritis
• Rheumatoid arthritis
• Ankylosing spondylitis
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Nonopioid Analgesics, Antipyretics, and
NSAIDs (cont’d)
• Selective Nonsteroidal
Anti-Inflammatory Drugs
–
Celecoxib (Celebrex)
• Adverse Reactions
–
Dyspepsia
–
Nausea
–
Vomiting
–
GI ulcers
–
Hypertension
–
Fluid retention
–
Peripheral edema
–
Dizziness
–
Headache
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Nonopioid Analgesics, Antipyretics, and
NSAIDs (cont’d)
• Phenazopyridine Hydrochloride
–
A dye used in commercial coloring that helps relieve symptoms
associated with urinary tract infections, including:
• Pain
• Burning
• Urgency
• Frequency
–
Adverse reactions
• Yellow tinge to patient’s skin & whites of eyes
• Acute renal or hepatic failure
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Opioid Agonist and Antagonist Drugs
• Opioid Agonists
–
Controlled substances used to relieve or decrease pain without
causing patient to lose consciousness
–
Sometimes called narcotic agonists
• Opioid Antagonists
–
Drugs that work against opioid agonists to block their effects and
reverse adverse reactions, such as respiratory & CNS depression
• Mixed Opioid Agonist-Antagonists
–
Act like agonists & antagonists by relieving pain & reducing risk
of adverse reactions
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Opioid Agonist and Antagonist Drugs
(cont’d)
• Opioid Agonists
–
Mainly used to manage moderate-to-severe acute & chronic pain
–
Bind with opiate receptors in central, peripheral nervous systems
–
Mimic effects of endorphins, body’s natural opiates
–
Binding process has following effects:
• Antidiarrheal action
• Contraction of bladder & ureters
• Constriction of bronchial muscles
• Dilation of blood vessels
• Slowing of intestinal peristalsis & suppression of cough center
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Opioid Agonist and Antagonist Drugs
(cont’d)
• Opioid Agonists
–
Oxymorphone
–
Codeine
–
Propoxyphene
–
Fentanyl citrate
–
Remifentanil
–
Hydrocodone
–
Sufentanil
–
Hydromorphone
–
Levorphanol
–
Constipation
–
Meperidine
–
Flushing
–
Methadone
–
Orthostatic hypotension
–
Morphine
–
Pupil constriction
–
Oxycodone
• Adverse Reactions
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Opioid Agonist and Antagonist Drugs
(cont’d)
• Mixed Opioid Agonist-Antagonists
–
Relieve pain while reducing toxic effects & dependency
–
Affect CNS
–
Act in 2 ways at same time:
• At some receptor sites, they bind with receptor & produce
pain relief effect similar to other opioids
• At other sites, they block agonist action, reducing adverse
effects
–
Used for pain relief during childbirth & after surgery
–
Sometimes prescribed instead of opioid agonists because of
lower risk of drug dependence
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Opioid Agonist and Antagonist Drugs
(cont’d)
• Mixed Opioid AgonistAntagonists
• Adverse Reactions
–
Euphoria
–
Buprenorphine
–
Lightheadedness
–
Butorphanol & nalbuphine
–
Nausea
–
Pentazocine
–
Vomiting
–
Sedation
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Opioid Agonist and Antagonist Drugs
(cont’d)
• Opioid Antagonists
–
Counteract effects of opioids
–
Have strong attraction for opiate receptors
–
Don’t stimulate receptors, but fill up receptor sites so that
opioids can’t bind with them (competitive inhibition)
–
2 most common opioid antagonists:
• Naloxone
• Naltrexone
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Opioid Agonist and Antagonist Drugs
(cont’d)
• Adverse Reactions
–
Naloxone
• Nausea
• Vomiting
• Hypertension
• Tachycardia
–
Naltrexone
• Anxiety, depression,
disorientation,
dizziness, headache,
mood changes, or
nervousness
• Anorexia, diarrhea,
constipation, nausea,
thirst, GI pain, cramps,
vomiting
• Urinary frequency
• Edema, hypertension,
palpitations, phlebitis,
shortness of breath
• Liver toxicity
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Anesthetic Drugs
• Block perception of pain or cause a loss of feeling
• Allow individual to undergo surgery or other medical
procedures without distress & pain
• Three classes
–
General anesthetics
• Inhalation
• Intravenous
–
Local anesthetics
–
Topical anesthetics
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Anesthetic Drugs (cont’d)
• Inhalation Anesthetics
–
Used for surgery
–
Allow precise & quick control of depth of anesthesia
–
Most are liquid & volatile
–
Move from lungs to blood; are eliminated by lungs or liver
–
Work by depressing CNS
–
Effects
• Loss of consciousness
• Loss of responsiveness to sensory stimulation
• Muscle relaxation
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Anesthetic Drugs (cont’d)
• Inhalation Anesthetics
• Adverse Reactions
–
Desflurane
–
Ataxia
–
Enflurane, isoflurane, &
sevoflurane
–
Confusion
–
Depressed breathing &
circulation
–
Hypothermia
–
Nausea
–
Sedation
–
Vomiting
–
Nitrous oxide
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Anesthetic Drugs (cont’d)
• Intravenous Anesthetics
–
Typically used when patient needs general anesthesia for a short
period, such as outpatient surgery
–
Used to help induce general anesthesia more rapidly or
supplement inhalation anesthetics
–
Different types of drugs are used as intravenous anesthetics:
• Barbiturates
• Benzodiazepines
• Dissociatives
• Hypnotics
• Opiates
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Anesthetic Drugs (cont’d)
• Intravenous Anesthetics (& associated adverse
reactions)
–
Methohexital & Sufentanil
–
Thiopental: respiratory depression; hiccups, coughing, muscle
twitching; depressed cardiac function & peripheral dilation
–
Midazolam: CNS & respiratory depression, hypotension,
dizziness
–
Ketamine: irrational behavior, excitement, disorientation,
delirium, hallucinations, increased heart rate, hypertension
–
Etomidate: hiccups, coughing, muscle twitching
–
Propofol: respiratory depression
–
Fentanyl: CNS & respiratory depression, hypoventilation,
cardiac arrhythmias, muscle rigidity
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Anesthetic Drugs (cont’d)
• Local Anesthetics
–
Administered to prevent or relieve pain in a specific area of body
–
Often used as an alternative to general anesthesia for elderly or
debilitated patients
–
Two main groups: “amide” drugs & “ester” drugs
–
Uses
• To prevent & relieve pain from procedures, disease, injury
• To treat severe pain that topical anesthetics or analgesics
can’t relieve
• As an alternative to general anesthetics in surgery for older
patients & patients with respiratory disorders
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Anesthetic Drugs (cont’d)
• Local Anesthetics
–
–
Amide drugs
• Adverse Reactions
–
Shivering
• Bupivacaine
–
Positional headache
• Lidocaine
–
Pain
• Mepivacaine
–
Bradycardia
• Prilocaine
–
Hypotension
• Ropivacaine
–
Anxiety
–
Restlessness
–
Palpitations
–
Tachycardia
Ester drugs
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Anesthetic Drugs (cont’d)
• Topical Anesthetics
–
Are applied directly to unbroken skin or mucous membranes to
prevent or relieve minor pain
–
Most produce little systemic absorption
–
Many work by blocking nerve signals
–
Aren’t well absorbed into systemic circulation
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Anesthetic Drugs (cont’d)
• Topical Anesthetics
• Adverse Reactions
–
Lidocaine
–
A rash
–
Tetracaine
–
Itching
–
Benzocaine
–
Hives
–
Cocaine
–
Swelling of mouth & throat
–
Dyclonine & dibucaine
–
Breathing difficulty
–
Pramoxine
–
Aromatic compounds
–
Cooling effect
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