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Copyright © 2012 Wolters Kluwer Health | Lippincott Williams & Wilkins
Chapter 15
Drugs Relieving Anxiety and Promoting Sleep
Chapter 15
Drugs Relieving Anxiety and Promoting Sleep
Copyright © 2012 Wolters Kluwer Health | Lippincott Williams & Wilkins
QuestionQuestion
• What system in the brain is responsible for emotion?
– A. Amygdala system
– B. Reticular system
– C. Limbic system
– D. Ventricular system
Copyright © 2012 Wolters Kluwer Health | Lippincott Williams & Wilkins
AnswerAnswer
• C. Limbic system
• Rationale: The limbic system in the brain is known to be primarily responsible for emotions.
Copyright © 2012 Wolters Kluwer Health | Lippincott Williams & Wilkins
Emotions and Neurotransmitters Emotions and Neurotransmitters
• The limbic system in the brain is known to be primarily responsible for emotions.
• The amygdala receives incoming sensory signals and then communicates with the frontal lobes of the brain.
• The amygdala can signal the brain that a threat is present and set off a fear response or anxiety.
• Another part of the brain, the hippocampus, is responsible for processing threatening or traumatic stimuli.
• The brain sends its messages to the body by way of the nervous system.
Copyright © 2012 Wolters Kluwer Health | Lippincott Williams & Wilkins
GABA Cell ReceptorsGABA Cell Receptors
Copyright © 2012 Wolters Kluwer Health | Lippincott Williams & Wilkins
Sleep Sleep
• Sleep is a time of bodily rest, although the brain remains active.
• There are two phases:
– No rapid eye movements (NREM)
– Rapid eye movements (REM)
Copyright © 2012 Wolters Kluwer Health | Lippincott Williams & Wilkins
Sleep (cont.)Sleep (cont.)
• NREM stages of sleep are further divided into
– Stage 1—light sleep; muscles relax; brain waves are irregular and rapid.
– Stage 2—brain waves are larger than in stage 1, with bursts of electrical activity.
– Stages 3 and 4—deep sleep, with even larger, slower brain waves called delta waves.
Copyright © 2012 Wolters Kluwer Health | Lippincott Williams & Wilkins
Sleep (cont.)Sleep (cont.)
• A number of physiologic changes occur during sleep.
• The amount of sleep needed by a person varies throughout the life span, with infants requiring the most sleep and adults requiring the least.
Copyright © 2012 Wolters Kluwer Health | Lippincott Williams & Wilkins
Anxiety Anxiety • Anxiety is a feeling of unease that something bad or
undesirable may happen.
• Some anxiety is normal; it is a protective mechanism.
• Anxiety becomes pathologic when it is severe and chronic and interferes with a person’s ability to function in normal life.
• Anxiety disorders can become progressively worse if they are untreated.
• Anxiety commonly occurs in combination with other mental or physical illnesses.
Copyright © 2012 Wolters Kluwer Health | Lippincott Williams & Wilkins
Sleep Disorders Sleep Disorders
• Between 50 and 70 million Americans have a sleep disorder.
• These disorders are many and may include the following problems:
– Narcolepsy—sudden irresistible sleep attacks of unknown origin lasting from seconds to minutes, two to six times a day
– Sleep apnea—a group of disorders characterized by cessation of breathing during sleep
– Sleepwalking—getting up and walking about while still asleep
Copyright © 2012 Wolters Kluwer Health | Lippincott Williams & Wilkins
Sleep Disorders (cont.)Sleep Disorders (cont.)
• These disorders are many and may include the following problems (cont.):
– Night terrors—occur only in children, with periods of fright, crying, moaning, or screaming after a brief time asleep
– Excessive daytime sedation
– Insomnia
Copyright © 2012 Wolters Kluwer Health | Lippincott Williams & Wilkins
Selective Serotonin Reuptake Inhibitors Selective Serotonin Reuptake Inhibitors
• Selective serotonin reuptake inhibitors (SSRIs) are a class of antidepressant drugs, some of which are now considered first-line therapy for anxiety disorders.
• Low serotonin levels are known to be present in severe stress and in many mood and anxiety-related disorders.
• SSRIs indirectly increase the amount of the neurotransmitter serotonin available in the synapses.
• SSRIs are generally well tolerated with few adverse effects.
Copyright © 2012 Wolters Kluwer Health | Lippincott Williams & Wilkins
Tricyclic Antidepressants Tricyclic Antidepressants
• The tricyclic antidepressants (TCAs) are another class of antidepressants.
• TCAs are as effective as the SSRIs in treating most anxiety disorders.
• TCAs work by affecting the regulation of serotonin or norepinephrine in the brain.
• TCAs have a higher adverse effect profile than SSRIs, which limits their use as antidepressants.
Copyright © 2012 Wolters Kluwer Health | Lippincott Williams & Wilkins
Monoamine Oxidase Inhibitors Monoamine Oxidase Inhibitors
• Monoamine oxidase inhibitors (MAOIs) are the oldest class of antidepressants.
• The MAOIs used to treat anxiety disorders are phenelzine (Nardil), tranylcypromine (Parnate), and isocarboxazid (Marplan).
• These drugs are occasionally prescribed for panic disorder and social phobia.
Copyright © 2012 Wolters Kluwer Health | Lippincott Williams & Wilkins
Monoamine Oxidase Inhibitors (cont.)Monoamine Oxidase Inhibitors (cont.)
• Monoamine oxidase is the enzyme that degrades serotonin in the synapse.
• By inhibiting the enzyme, higher levels of serotonin can remain in the synapse and be active.
• The MAOIs are associated with a significant risk of a serious drug–food interaction.
Copyright © 2012 Wolters Kluwer Health | Lippincott Williams & Wilkins
Beta-BlockersBeta-Blockers
• Beta-blockers are adrenergic drugs most frequently used for a wide variety of cardiac conditions.
• Among other actions, they slow the heart rate.
• This helps the patient with some types of anxiety who may be uncomfortable and highly aware of the tachycardia and palpitations.
Copyright © 2012 Wolters Kluwer Health | Lippincott Williams & Wilkins
Benzodiazepines Benzodiazepines
• Benzodiazepines are used for a number of therapeutic effects.
• As a class, benzodiazepines appear to potentiate the effects of GABA.
• The result is more CNS depression than would normally be found.
• Benzodiazepines bind to specific receptor sites to produce their effects.
• As a drug class, benzodiazepines have a high margin of safety.
Copyright © 2012 Wolters Kluwer Health | Lippincott Williams & Wilkins
QuestionQuestion
• Benzodiazepines are used to treat which of the following condition(s)?
– A. Anxiety
– B. Seizures
– C. Alcohol withdrawal
– D. All of the above
Copyright © 2012 Wolters Kluwer Health | Lippincott Williams & Wilkins
AnswerAnswer
• D. All of the above
• Rationale: Benzodiazepines are used for the following: anxiety relief, sleep promotion, anticonvulsant effects, muscle relaxation, treatment of acute alcohol withdrawal, induction of general anesthesia, preoperative sedation, and conscious sedation.
Copyright © 2012 Wolters Kluwer Health | Lippincott Williams & Wilkins
Lorazepam: Core Drug Knowledge Lorazepam: Core Drug Knowledge
• Pharmacotherapeutics
– Used in treating anxiety disorders and insomnia
• Pharmacokinetics
– Administered: parenterally or orally. Distribution: body tissues. Metabolism: liver. Excreted: kidneys.
• Pharmacodynamics
– Increases the effects of GABA
Copyright © 2012 Wolters Kluwer Health | Lippincott Williams & Wilkins
Lorazepam: Core Drug Knowledge (cont.)Lorazepam: Core Drug Knowledge (cont.)
• Contraindications and precautions
– Hypersensitivity, psychoses, acute narrow-angle glaucoma, and use in children younger than 6 months
• Adverse effects
– Mild drowsiness, ataxia, confusion, respiratory disturbances, bradycardia, and hypotension
• Drug interactions
– Several drug interactions
Copyright © 2012 Wolters Kluwer Health | Lippincott Williams & Wilkins
Lorazepam: Core Patient Variables Lorazepam: Core Patient Variables • Health status
– Asses for renal and hepatic impairment
• Life span and gender
– Pregnancy Category D
• Lifestyle, diet, and habits
– Assess the patient for the use of other CNS depressants.
• Environment
– Oral formulation can be given in any environment.
• Culture and inherited traits
– Longer T½ in Asians
Copyright © 2012 Wolters Kluwer Health | Lippincott Williams & Wilkins
Lorazepam: Nursing Diagnoses and Outcomes Lorazepam: Nursing Diagnoses and Outcomes • Risk for Injury related to drowsiness and other adverse
effects
– Desired outcome: The patient will not sustain an injury while on lorazepam.
• Anxiety related to disease process
– Desired outcome: The patient will achieve symptom control.
• Deficient Knowledge related to newly prescribed drug therapy
– Desired outcome: The patient will learn the actions and adverse effects of lorazepam and how to safely self-administer the drug.
Copyright © 2012 Wolters Kluwer Health | Lippincott Williams & Wilkins
Lorazepam: Planning and InterventionsLorazepam: Planning and Interventions
• Maximizing therapeutic effects
– Give at scheduled intervals throughout the day.
• Minimizing adverse effects
– If GI distress occurs, administer lorazepam with food.
– Monitor for paradoxical reactions and stop the drug if they occur.
– Dilute injectable lorazepam with an equal volume of compatible solution.
Copyright © 2012 Wolters Kluwer Health | Lippincott Williams & Wilkins
Lorazepam: Teaching, Assessment, and EvaluationsLorazepam: Teaching, Assessment, and Evaluations
• Patient and family education
– Caution against use of alcohol with this drug.
– Discuss side effects of medication.
• Ongoing assessment and evaluation
– Lorazepam therapy is effective if the patient reports a reduction in feelings of anxiety.
– Throughout therapy, assess for therapeutic response and onset of adverse effects.
Copyright © 2012 Wolters Kluwer Health | Lippincott Williams & Wilkins
QuestionQuestion
• Lorazepam has a ________ duration of action?
– A. Short
– B. Intermediate
– C. Long
– D. Varies with route of administration
Copyright © 2012 Wolters Kluwer Health | Lippincott Williams & Wilkins
AnswerAnswer
• A. Short
• Rationale: Lorazepam has a short duration of action; therefore, divide the daily dosage for treating anxiety into two or three doses and administer the drug throughout the day.
Copyright © 2012 Wolters Kluwer Health | Lippincott Williams & Wilkins
Buspirone Buspirone
• Buspirone (BuSpar) is an azaspirodecanedione that is not chemically or pharmacologically related to the benzodiazepines.
• It is used to treat symptoms of anxiety, although exactly how it works is unknown.
• Optimum relief of anxiety usually occurs after 3 to 4 weeks of treatment.
• Buspirone is intended for short-term therapy; patients who have been treated with buspirone for up to 1 year have not required a dosage increase to maintain therapeutic effect.
Copyright © 2012 Wolters Kluwer Health | Lippincott Williams & Wilkins
Hydroxyzine Hydroxyzine
• Hydroxyzine (Vistaril) is a miscellaneous antianxiety drug.
• It exerts CNS depressant activity in subcortical areas.
• It rapidly produces a feeling of calm and relieves anxiety without impairing mental alertness.
• It may be coadministered with a narcotic to control pain while minimizing the nausea that may be an adverse effect from the narcotic.
Copyright © 2012 Wolters Kluwer Health | Lippincott Williams & Wilkins
Meprobamate Meprobamate
• Meprobamate (Equanil) is also used for short-term management of anxiety symptoms.
• Meprobamate has selective effects at multiple sites within the CNS, including the thalamus and the limbic system.
• It may also inhibit multineuronal spinal reflexes.
• It has mild tranquilizing properties and some anticonvulsant and muscle-relaxant properties.
• Meprobamate can produce several CNS adverse effects.
• Meprobamate is a Pregnancy Category D drug.
Copyright © 2012 Wolters Kluwer Health | Lippincott Williams & Wilkins
EszopicloneEszopiclone
• Eszopiclone (Lunesta) is a nonbenzodiazepine hypnotic.
• The drug induces sleep quickly, prevents waking during the night.
• Eszopiclone is believed to achieve its therapeutic effect from interaction with GABA-receptor/benzodiazepine-receptor complexes.
• It is the only drug for insomnia that is approved for long-term use (up to 6 months of use).
• Eszopiclone has a rapid onset (within 1 hour) and is metabolized in the liver and excreted in the urine.
• The most common adverse effects of eszopiclone after 6 weeks of use were headache, prolonged drowsiness, and an unpleasant taste.
Copyright © 2012 Wolters Kluwer Health | Lippincott Williams & Wilkins
Zaleplon Zaleplon
• Zaleplon (Sonata) is a sedative for short-term use (up to 28 days).
• Although a nonbenzodiazepine and not chemically related to the benzodiazepines, it does interact with the GABA–benzodiazepine (BZ) complex.
• The most common adverse effects of zaleplon are drowsiness, dizziness, light-headedness, and difficulty with coordination. Zaleplon is a Pregnancy Category C drug.
• Zaleplon may lead to dependency, and rebound insomnia is possible.
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Zolpidem Zolpidem
• Zolpidem (Ambien) is used for short-term treatment of insomnia—generally not for more than 7 to 10 days.
• It induces sleep rapidly and should be taken immediately before going to bed.
• Although zolpidem is not chemically related to the benzodiazepines, it does interact selectively with the GABA–BZ receptor complex and shares some pharmacologic properties with the benzodiazepines.
• Zolpidem generally preserves all of the sleep stages and has only minor effects on REM sleep.
• The most common adverse effects from zolpidem are headache, prolonged drowsiness, and dizziness.
Copyright © 2012 Wolters Kluwer Health | Lippincott Williams & Wilkins
Ramelteon Ramelteon
• Melatonin receptor agonists stimulate the same receptor sites as endogenous melatonin.
• Ramelteon (Rozerem) is used in the treatment of insomnia when the patient has difficulty falling asleep.
• Ramelteon has high affinity at two specific melatonin receptors.
• Common adverse effects of ramelteon include headache, daytime sleepiness, dizziness, tiredness, nausea, worsening insomnia, and colds.
Copyright © 2012 Wolters Kluwer Health | Lippincott Williams & Wilkins
Trazodone Trazodone
• Trazodone (Desyrel) is an atypical antidepressant.
• This drug causes significant sedation as an adverse effect.
• Trazodone is most commonly used to promote sleep.
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Chloral Hydrate Chloral Hydrate
• Chloral hydrate is a nonbarbiturate hypnotic used to induce sleep and to cause preoperative sedation.
• It can be used as an adjunct to opiates and analgesics in pain control.
• In therapeutic doses, chloral hydrate has little effect on respirations, blood pressure, or reflexes.
• It does produce numerous adverse effects in the CNS.
Copyright © 2012 Wolters Kluwer Health | Lippincott Williams & Wilkins
Barbiturates Barbiturates
• Barbiturates such as phenobarbital (Bellatal), secobarbital (Seconal), and pentobarbital (Nembutal) were used to treat insomnia before the availability of the benzodiazepines.
• Although they are effective for short-term treatment of insomnia, they are also highly habit forming.
• Patients can develop tolerance and physical and psychological dependence on the drugs.