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Flashcards about Insomnia and Pharmacologic Therapy
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Insomnia Definition
Subjective perception of difficulty with sleep initiation, duration, consolidation, or quality that occurs despite adequate opportunity for sleep, resulting in some form of daytime impairment.
First-Line Insomnia Therapies
Nonpharmacologic interventions such as stimulus control, relaxation training, or sleep restriction.
Insomnia Prevalence
More common in women, older adults (up to 65% of those 65+), and individuals with comorbidities such as pulmonary disease, heart failure, neurologic disease, painful conditions, and psychiatric disorders.
Benzodiazepines Mechanism
Modulate the γ-aminobutyric acid (GABA)A receptor in neurons, causing hyperpolarization of the cell, leading to sedation, decreased anxiety, muscle relaxation, and retrograde amnesia.
Benzodiazepines Adverse Effects
Disrupt sleep quality by distorting sleep architecture, diminish deep sleep time, high risk of physical dependence (15-40% report severe withdrawal), rebound insomnia, increased anxiety. Contraindicated in pregnancy, breastfeeding, sleep apnea, and chronic pulmonary disease.
Z-Drugs Mechanism
Bind more selectively to certain subunits of the GABAA receptor, primarily targeting the sedative effect of the receptor rather than the anxiolytic effect.
Z-Drugs Adverse Effects
Memory loss, dizziness, disinhibition, gastrointestinal upset, hallucinations, complex sleep-related behaviors (e.g., sleep driving, sleep eating). May cause stimulation, euphoria, and anxiolysis in some patients.
Eszopiclone (Lunesta)
Cyclopyrrolone drug used to improve sleep latency and is particularly well-suited for sleep maintenance given its long half-life; may cause unpleasant taste.
Zaleplon (Sonata)
A pyrazolopyrimidine drug with an extremely short half-life, indicated for improving sleep latency but not sleep maintenance.
Melatonin Agonists
Regulate the sleep-wake cycle; disruption or decreased production can contribute to insomnia, especially with time zone changes, shift work, or aging.
Ramelteon (Rozerem)
A melatonin agonist approved by the FDA for insomnia related to sleep latency. Has few adverse effects and is not habit forming. May decrease risk of hospital-associated delirium in older adults.
Doxepin (Silenor)
A tricyclic antidepressant FDA approved for sleep maintenance difficulties. Likely works through antagonism of the histamine H1 receptor. Favorable adverse effect profile even with long-term use.
Antihistamines in Pregnancy
Doxylamine (category A) and diphenhydramine (category B) are first-line therapies for insomnia in pregnant women because they may be effective for nausea and insomnia and are generally considered safe.
Suvorexant (Belsomra)
An orexin receptor antagonist that regulates the sleep arousal cycle. Common adverse effect is daytime somnolence. High cost and addictive potential make it a non-preferred first-line treatment.
Gabapentin (Neurontin) and Pregabalin (Lyrica)
Antiepileptics that have been found to improve sleep, particularly useful for insomnia due to restless legs syndrome. Pregabalin may also improve sleep quality, but evidence is limited.
Insomnia Treatment Algorithm
Behavioral interventions are the mainstay. If pharmacologic intervention is needed, tailor approach based on insomnia type (sleep-onset, sleep-maintenance, insomnia in older adults, depression and insomnia).