copyright © 2013, 2010 by saunders, an imprint of elsevier inc. chapter 34 sedative-hypnotic drugs
TRANSCRIPT
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Copyright © 2013, 2010 by Saunders, an imprint of Elsevier Inc.
Chapter 34
Sedative-Hypnotic Drugs
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2Copyright © 2013, 2010 by Saunders, an imprint of Elsevier Inc.
Sedative-Hypnotic Drugs
Drugs that depress CNS function Primarily used to treat anxiety and insomnia Antianxiety agents or anxiolytics Distinction between antianxiety effects and
hypnotic effects is often a matter of dosage
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3Copyright © 2013, 2010 by Saunders, an imprint of Elsevier Inc.
Sedative-Hypnotic Drugs
Benzodiazepines Benzodiazepine-like drugs Ramelteon: a melatonin agonist Barbiturates
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4Copyright © 2013, 2010 by Saunders, an imprint of Elsevier Inc.
Benzodiazepines
Drugs of choice to treat insomnia and anxiety Used to induce general anesthesia Used to manage seizure disorders, muscle spasm,
panic disorder, and withdrawal from alcohol Most familiar member: diazepam (Valium) Most prescribed: lorazepam and alprazolam Safer than general CNS depressants Lower potential for abuse Produce less tolerance and physical dependence Fewer drug interactions
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Benzodiazepines
Overview of pharmacologic effects Central nervous system Cardiovascular system Respiratory system
Molecular mechanism of action Pharmacokinetics
Absorption and distribution Metabolism Time course of action
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Benzodiazepines
Therapeutic uses Anxiety Insomnia Seizure disorders Muscle spasm Alcohol withdrawal Panic disorder Perioperative applications
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Benzodiazepines
Adverse effects CNS depression Anterograde amnesia Sleep driving Paradoxical effects Respiratory depression Abuse Use in pregnancy and lactation Other adverse effects
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Benzodiazepines
Drug interactions CNS depressants
Tolerance and physical dependence Tolerance
• With prolonged use, tolerance develops to some effects but not others
Physical dependence• Can cause physical dependence, but the incidence of
substantial dependence is low
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Benzodiazepines
Acute toxicity Oral overdose Intravenous toxicity General treatment measures Treatment with flumazenil
Preparations, dosage, and administration Preparations and dosage Routes
• Orally• Parenterally (IM and IV)
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Benzodiazepine-like Drugs
Zolpidem (Ambien) Sedative-hypnotic Short-term management of insomnia
Zaleplon (Sonata) New class of hypnotics, pyrazolopyrimidines Short-term management of insomnia Prolonged use does not appear to cause tolerance
Eszopiclone (Lunesta) Is the S-isomer of zopiclone For treating insomnia No limitation on how long it can be used
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Ramelteon: Melatonin Agonist
Brand name: Rozerem Relatively new hypnotic Activation of melatonin receptors Approved for chronic insomnia: difficulty with
sleep onset Rapid onset (about 30 minutes)
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Barbiturates
Three classifications Ultrashort-acting (thiopental) Short- to intermediate-acting (secobarbital) Long-acting (phenobarbital)
Mechanism of action Binds to the GABA receptor–chloride channel
complex
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Barbiturates
Pharmacologic effects CNS depression Cardiovascular effects Induction of hepatic drug-metabolizing enzymes
Tolerance and physical dependence Tolerance
• Develops to many—but not all—of the CNS effects• Very little tolerance develops to respiratory depression
Physical dependence
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Fig. 34–2. Induction of hepatic microsomal enzymes by barbiturates.
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Barbiturates
Pharmacokinetics Lipid solubility has a significant impact Rapid onset and brief duration
Therapeutic uses Seizure disorders Induction of anesthesia Insomnia Other uses
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Barbiturates
Drug interactions CNS depressants Interactions resulting from induction of
drug-metabolizing enzymes Chloral hydrate Meprobamate
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Barbiturates
Adverse effects Respiratory depression Suicide Abuse Use in pregnancy Exacerbation of intermittent porphyria Hangover Paradoxical excitement Hyperalgesia
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Barbiturates
Acute toxicity Symptoms
• Respiratory depression• Coma• Pinpoint pupils
Treatment• Removal of barbiturate from the body• Maintenance of an adequate oxygen supply to the brain
Administration Oral Intravenous Intramuscular
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Fig. 34–3. Development of tolerance to the toxic and subjective effects of barbiturates.
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Miscellaneous Sedative-Hypnotics
Basic pharmacologic profile Nonselective CNS depressants Actions much like those of barbiturates Acute overdose resembles poisoning with
barbiturates Avoid during pregnancy and lactation
Chloral hydrate Meprobamate Paraldehyde
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Management of Insomnia
Sleep physiology Sleep phases
Basic management principles Cause-specific therapy Nondrug therapy
Drugs used for treatment Hypnotic drugs
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Sleep Physiology
Sleep phases Rapid-eye-movement (REM) Non–rapid-eye-movement sleep (NREM)
• I = Relatively light sleep• II = Relatively light sleep• III = Deep sleep• IV = Deep sleep
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Basic Management Principles
Cause-specific therapy Treatment is highly dependent on the cause
Nondrug therapy Therapy with hypnotic drugs
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Drugs Used for Treatment of Insomnia
Drugs used for treatment Benzodiazepines Benzodiazepine-like drugs: zolpidem, zaleplon,
and eszopiclone Ramelteon Trazodone Doxepin Antihistamines Alternative medicines