Transcript Chapter 19

Chapter 19
Analgesics, Sedatives, and
Hypnotics
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1
Introduction
• Analgesics, sedatives, and hypnotics
– Depress central nervous system (CNS) action
to varying degrees
– Some drugs can be classified into more than
one category, depending on the dosage
• Analgesics: relieve pain
• Sedatives: calm, soothe, or produce sedation
• Hypnotics: produce sleep
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Introduction (cont’d.)
• The following slides discuss various
analgesics, sedatives, and hypnotics
– Refer to the chapter for specific side effects,
contraindications, and interactions
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Analgesics
• Pain is the most common reason for
patients to seek out medical care
– Most common types: back, neck, migraine,
and facial or jaw pain
– Is subjective: can be experienced or
perceived only by the individual subject
– Can be blocked by endorphins
• Endogenous analgesics produced within the body
as a reaction to severe pain or intense exercise
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Analgesics (cont’d.)
• Opioid analgesics
– Full or pure agonists, partial agonists, or
mixed agonist-antagonists
• Each bind to specific receptors with varying
degrees of action
• Classified as controlled substances
• Potential for abuse and psychological dependence
• Tend to cause tolerance and physiological
dependence
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Analgesics (cont’d.)
• Tramadol (Ultram)
– Centrally acting synthetic analog of codeine
with a dual mechanism of action
– Produces analgesia by weak inhibition of
norepinephrine and serotonin reuptake; is an
opioid receptor agonist
– Less potential for abuse or respiratory
depression (although both may occur)
– Currently not classified as a controlled
substance on the Federal level
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Analgesics (cont’d.)
• Nonopioid analgesics
– Many available without prescription as overthe-counter (OTC) medications
– Given for relieving mild to moderate pain,
fever, and anti-inflammatory conditions
– Used as a coanalgesic in severe acute or
chronic pain requiring opioids
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Analgesics (cont’d.)
– Salicylates (aspirin) are most commonly used
for their analgesic and antipyretic properties,
as well as for their anti-inflammatory action
– Acetaminophen has analgesic and antipyretic
properties, but very little effect on
inflammation
– Aspirin and acetaminophen are frequently
combined with opioids or with other drugs for
more effective analgesic action
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Analgesics (cont’d.)
• Salicylates and other NSAIDS
– Analgesic and anti-inflammatory actions
• Associated primarily with preventing formation of
prostaglandins and subsequent inflammatory
response that prostaglandins help to induce
• Acetaminophen (Tylenol)
– Used extensively to treat mild to moderate
pain and fever
• Very little effect on inflammation, but fewer
adverse side effects than salicylates
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Analgesics (cont’d.)
• Adjuvant analgesics
– May enhance analgesic effect with opioids
and nonopioids, produce analgesia alone, or
reduce side effects of analgesics
• Tricyclic antidepressants
– Treats fibromyalgia and nerve pain associated
with herpes, arthritis, diabetes, and cancer,
migraine or tension headaches, insomnia, and
depression
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Analgesics (cont’d.)
• Anticonvulsants (i.e., Neurontin and
Tegretol)
– Commonly used for management of nerve
pain associated with neuralgia, herpes zoster
(shingles), and cancer
– Implemented when patient describes pain as
“sharp,” “shooting,” “shock-like pain,” or
“lightning-like”
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Local Anesthetic
• Lidocaine patch (Lidoderm)
– Approved for management of postherpetic
neuralgia
– Can provide significant analgesia in other
forms of neuropathic pain
• Diabetic neuropathy and musculoskeletal pain
such as osteoarthritis and low back pain
– Provides pain relief through a peripheral effect
and generally has little, if any, central action
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Local Anesthetic (cont’d.)
• Antimigraine agents
– Simple analgesics, NSAIDs, and opioid
analgesics can be effective, especially if taken
at initial sign of migraine
• Serotonin receptor agonists (SRAs)
– Action: serotonin levels decrease, while
vasodilation and inflammation of blood vessels
in brain increase as migraine symptoms worsen
• Effective in treating associated nausea and vomiting
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Sedatives and Hypnotics
• Medications used to promote sedation in
smaller doses
– Promote sleep in larger doses
• Benzodiazepines (BZDs) and
nonbenzodiazepines
– Less abuse potential
– Withdrawal effects are observed after longterm use and respiratory depression (when
taken with alcohol) can be potentially fatal
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Sedatives and Hypnotics (cont’d.)
• Melatonin receptor agonist
– Ramelteon (Rozerem): first FDA-approved
prescription medication that acts on melatonin
receptor
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Mimics action of melatonin to trigger sleep onset
Dependence and abuse potential are eliminated
Not classified as a controlled substance
Works quickly, generally inducing sleep in less
than one hour
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