copyright © 2015 cengage learning® 1 chapter 19 analgesics, sedatives, and hypnotics
TRANSCRIPT
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Copyright © 2015 Cengage Learning® 1Copyright © 2015 Cengage Learning®
Chapter 19Analgesics, Sedatives, and
Hypnotics
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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 over-the-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 long-
term 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• 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