Pharm Chapter 13 Notes PDF
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These notes cover Chapter 13 of a pharmacology textbook, focusing on drugs used for sedation and sleep. The chapter details sleep and sleep disorders, including insomnia. It also examines different types of sedative-hypnotic therapies and their effects on the body.
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Chater: 13: Drugs used for Sedation and Sleep Sleep and Sleep Pattern Disturbance Definition: Sleep is a natural state of unconsciousness that allows the body to rest and recover; it makes up about one-third of adult life. Importance of Sleep: Health benefits: ○ Support...
Chater: 13: Drugs used for Sedation and Sleep Sleep and Sleep Pattern Disturbance Definition: Sleep is a natural state of unconsciousness that allows the body to rest and recover; it makes up about one-third of adult life. Importance of Sleep: Health benefits: ○ Supports immune system and mental health. ○ Optimal duration: 7–8 hours for adults. Risks of inadequate sleep: ○ Increases risk of obesity, heart disease, and type 2 diabetes. ○ Less than 5 hours of sleep triples the risk of heart attacks. Phases of Sleep: 1. NREM Sleep (Non-Rapid Eye Movement): ○ Divided into 3 stages (N1, N2, N3): Stage N1: Lightest sleep; lasts a few minutes. Makes up 2–5% of total sleep. Stage N2: Light sleep with drifting sensations. 50% of total sleep. Stage N3: Deep, restful, dreamless sleep. Decreases blood pressure, breathing, and metabolism. 10–15% of total sleep in young adults. Diminishes with age. ○ Older adults spend less time in deep sleep (stage N3). 2. REM Sleep (Rapid Eye Movement): ○ Occurs after NREM, every 90 minutes. ○ Features: Dreaming, irregular breathing, increased heart rate. 20–25% of total sleep. Helps with stress release and emotional balance. Sleep Disorders: Insomnia Definition: Difficulty falling, staying asleep, or waking too early. Types: ○ Initial insomnia: Trouble falling asleep. ○ Intermittent insomnia: Waking frequently. ○ Terminal insomnia: Waking early without returning to sleep. Duration-based types: ○ Transient: Lasts a few nights. ○ Short-term insomnia: Lasts less than 3 weeks (causes: stress, illness, travel). ○ Chronic: Lasts over a month. Prevalence: ○ 10% of adults and 20% of older adults have chronic insomnia. ○ More common in women, older adults, and people with stress or mental health conditions (e.g., anxiety, depression). Causes of Insomnia: Lifestyle changes, stress, caffeine/alcohol, large meals before sleep, or illness. Effects of Insomnia: Fatigue, daytime drowsiness, and difficulty with work or daily tasks. Sedative-Hypnotic Therapy Key Definitions: Sedative: A drug that promotes relaxation and rest (may not induce sleep). Hypnotic: A drug that Induces sleep. Ideal Hypnotic Characteristics: Quick onset of restful, natural sleep. Proper duration for waking at a usual time. No “hangover” effects or habit formation (addiction). Note: No perfect hypnotic exists. Effects of Sedative-Hypnotics: Increase light sleep (N2 stage). Decrease REM sleep, leading to: ○ Mental imbalance if REM is reduced long-term. ○ REM rebound (restlessness/vivid dreams) when stopped. ○ ***Note to self: Rebound Sleep Definition: Rebound sleep refers to the body's way of compensating for sleep deprivation by spending more time in certain stages of sleep (usually NREM stage N3 or REM sleep) during subsequent sleep periods. Causes: ○ Sleep deprivation (not getting enough sleep). ○ Suppression of REM sleep (e.g., from stress, alcohol, or certain medications). Characteristics: ○ REM rebound: Increased intensity and duration of REM sleep after REM suppression. ○ NREM rebound: Body focuses on deep, restorative sleep (stage N3) after deprivation. Purpose: ○ Helps the body recover physically and mentally. ○ Restores balance in sleep patterns. Example: After staying awake for 24 hours, you may experience deeper and longer sleep during the next night to compensate for the loss. Types of Sedative-Hypnotic Drugs (*** They are classified into 2 groups): 1. Benzodiazepines. 2. Non-benzodiazepines. Uses: Temporary treatment of insomnia (***The primary uses of sleep meds). Reduce anxiety or promote relaxation before medical procedures. To improve sleep patterns for the temporary treatment of insomnia. Nursing Implications: 1. Assessment Check CNS function: Alertness, motor skills. Record vital signs: BP, pulse, respiration. Evaluate sleep patterns: Disruptions, hours, management. Assess anxiety levels: Is medication needed, or just emotional support? Examine external factors: Sleeping environment, caffeine, alcohol, activity levels. Monitor respiratory status: Avoid in patients with breathing issues. 2. Implementation Monitor vital signs regularly. Administer pre-op meds at specific time. Assess effects and adjust PRN meds as needed. 3. Education (Promote Good Sleep Hygiene): Maintain a consistent bedtime routine. Avoid caffeine, alcohol, and heavy meals before bed. Suggest warm milk before sleep. Ensure a comfortable sleep environment (quiet, dark, cool room). Encourage regular exercise but not close to bedtime. Teach stress management (e.g., relaxation techniques, soft music). Alternative Medications for Insomnia: Antidepressants: Amitriptyline, trazodone, mirtazapine. Anticonvulsants: Gabapentin, topiramate. Antipsychotics: Quetiapine, olanzapine. Note: Limited studies exist on their long-term use for insomnia. Risks: Dependence: Chronic use can lead to addiction. Adverse effects: Especially with long-term use. Disrupted sleep patterns may take weeks to normalize. Drug Therapy for Sleep Disturbance Drug Therapy for Sleep Disturbance: Benzodiazepines Key Points Benzodiazepines Overview ○ Commonly used for sedation, sleep induction, anxiety relief, and seizure control. ○ Safe with a wide margin between therapeutic and toxic doses. ○ Overdoses are usually not fatal unless mixed with other CNS depressants. How They Work ○ Act on GABA-A receptors in the brain. ○ Alpha-1 binding = sleep effects. ○ Alpha-2 binding = muscle relaxation, anxiety relief, and seizure control. Uses for Sleep Examples: Estazolam, flurazepam, quazepam, temazepam, triazolam. Effects: ○ Increase light sleep (N2 stage). ○ Decrease deep sleep (N3) and REM sleep. ○ Long-term use can disrupt normal sleep patterns, leading to tolerance and rebound insomnia. Short-term use (less than 4 weeks) is recommended. Special Uses Short-acting Benzodiazepines: ○ Midazolam: Quick onset, used for anesthesia and short procedures. ○ Lorazepam: Longer duration, used for pre-surgery anxiety. Antidote: Flumazenil reverses benzodiazepine effects but may cause seizures in certain patients. Adverse Effects 1. Common Effects ○ Drowsiness, sedation, lethargy ("morning hangover"). ○ Risk of impaired alertness for activities like driving or working. 2. Serious Effects ○ Confusion, agitation, hallucinations (especially in older adults or long-term users). ○ Blood dyscrasias (rare): Check blood regularly for signs like sore throat or fever. ○ Hepatotoxicity: Monitor liver tests for symptoms like jaundice or weakness. 3. Addiction & Withdrawal ○ Physical and psychological dependence possible with regular use. ○ Stopping suddenly can cause withdrawal (anxiety, seizures, delirium). ○ Gradual tapering (over 2–4 weeks) is required. Drug Interactions Alcohol, opioids, and sedatives increase toxic effects. Smoking and rifampin reduce effectiveness, requiring higher doses. Nursing Implications 1. Before Giving Benzodiazepines ○ Check vital signs (sitting and lying down BP). ○ Assess for liver disease or blood disorders. ○ Confirm not pregnant (high risk of birth defects). 2. Pregnancy & Breastfeeding ○ Avoid in the first trimester and while breastfeeding. 3. Monitoring ○ Watch for signs of overdose or excessive sedation. ○ Assess for dependency or misuse. Therapeutic Goals Light sedation for relaxation. Short-term sleep induction. Pre-surgery sedation with memory loss (amnesia). Nonbenzodiazepine Sedative-Hypnotic Agents Actions Main Function: Cause CNS depression to promote sleep or relaxation. Types: ○ Antihistamines: Diphenhydramine, doxylamine (used for mild insomnia). ○ Tricyclic Antidepressants: Doxepin (low doses affect histamine-1 receptors for sleep maintenance). ○ Benzodiazepine Receptor Agonists: Zaleplon, zolpidem, eszopiclone (short-term sleep aids with less REM sleep disruption). ○ Melatonin and Related Drugs: Melatonin (natural hormone for sleep, used for jet lag; OTC dietary supplement). Ramelteon, tasimelteon (stimulate melatonin receptors; used for specific sleep disorders like insomnia or non–24-hour sleep-wake disorder in blind patients). ○ Orexin Receptor Antagonists: Suvorexant, lemborexant (reduce wakefulness by blocking orexin receptors; schedule IV controlled substances, not for narcolepsy). ○ Herbal Medicine: Valerian (may prolong GABA action; unregulated potency). Uses Antihistamines: ○ For short-term mild insomnia. ○ Diphenhydramine and doxylamine commonly found in OTC sleep aids but cause tolerance and morning hangover. Doxepin (Unison): ○ Low doses for sleep promotion (can cause dry mouth, constipation). Orexin Receptor Antagonists: ○ Help with falling asleep and staying asleep. ○ Not suitable for narcoleptic patients. Melatonin: ○ Useful for jet lag and circadian rhythm issues. Ramelteon/Tasimelteon (causes excessive sedation): ○ Ramelteon: For insomnia with difficulty falling asleep. ○ Tasimelteon: Treats non–24-hour sleep-wake disorder in blind individuals. Benzodiazepine Receptor Agonists: (do not administer before/after a meal) ○ Zaleplon: Helps fall asleep; short duration (2-4 hrs), minimal hangover. ○ Zolpidem: Helps fall asleep and extends sleep; various forms for different sleep needs. ○ Eszopiclone: Longer duration (5-8 hrs); helps with nighttime/early morning awakenings but can cause morning hangover, especially in older adults. Adverse Effects Common: ○ Hangover, drowsiness, headache, muscle/joint pain, mental depression. ○ Transient restlessness, blurred vision, dizziness (may require dose adjustment). Serious: ○ Physical dependence (if used long-term). ○ Withdrawal symptoms: weakness, anxiety, delirium, seizures (requires gradual discontinuation). Special Populations: ○ Older adults or patients in severe pain may react paradoxically (e.g., excitement, restlessness). ○ Safety measures (e.g., bed rails) may be necessary. Interactions Drugs: ○ Enhanced toxicity with alcohol, antihistamines, narcotics, tranquilizers, cimetidine, and others. ○ Fluvoxamine: Inhibits metabolism of ramelteon/tasimelteon (causes sedation). ○ Rifampin: Reduces effectiveness of zolpidem, eszopiclone, ramelteon, and tasimelteon. Food: ○ High-fat meals slow absorption of zaleplon, zolpidem, eszopiclone, and ramelteon (take on an empty stomach for faster action). Nursing Implications Assessment: ○ Check baseline vitals, hepatic disease history, and pregnancy/breastfeeding status. Administration: ○ Take immediately before bed or after being in bed with difficulty falling asleep. ○ Avoid with heavy meals. Monitoring: ○ Watch for morning hangover or adverse effects (adjust dose if needed). ○ Gradual discontinuation to avoid withdrawal symptoms. Therapeutic Outcomes 1. Mild sedation. 2. Short-term use for sleep induction and maintenance.