Pharmacology: Anxiety, Insomnia, Sedation, and Smoking Cessation

Central Nervous System Depressants Classification

  • Antianxiety Agents: Also known as anxiolytics, these medications are designed to manage states of nervousness and tension.

  • Sedative-Hypnotics: These agents are primarily used to induce sleep and treat insomnia.

Understanding Anxiety

  • Definition: Anxiety is characterized by feelings of nervousness, tension, and worry. It is considered an unpleasant feeling arising as a response to various threatening situations including physical, emotional, economic, social, or educational growth (e.g., test-taking).

  • Continuum of Anxiety: Anxiety exists on a spectrum, ranging from normal, situational stress to a full psychiatric classification as a disorder.

  • Neuroendocrine Factors:

    • Primarily involves the noradrenergic system.

    • May be caused by an excess of norepinephrine.

    • Likely associated with a depletion of gamma-aminobutyric acid (GABA).

  • Physical Symptoms of Hyperarousal:

    • Panic.

    • Restlessness.

    • Tremors.

    • Palpitations.

    • Hyperventilation.

  • Major Anxiety Disorders:

    • GAD: Generalized Anxiety Disorder.

    • OCD: Obsessive-Compulsive Disorder.

    • Panic Disorder.

    • PTSD: Post-Traumatic Stress Disorder.

    • SAD: Social Anxiety Disorder.

    • SAD: Seasonal Affective Disorder.

Non-Pharmacologic Management of Anxiety and Sleep

  • Therapeutic Interventions:

    • Psychotherapy.

    • Behavioral Modification Therapy.

    • Exercise.

    • Creating a calm environment.

    • Aromatherapy.

    • Laughter.

    • Complementary and Alternative Medicine (CAM).

    • Yoga.

  • Sleep Hygiene Protocols:

    • Follow a consistent routine.

    • Avoid doing other activities in bed (the bed is only for sleep).

    • Do not exercise immediately before bedtime.

    • Avoid stimulants or ethanol (ETOH) at night.

    • Avoid agitation or stressful activities before sleep.

    • Warm Milk: Often considered an urban legend, though it contains tryptophan.

Overview of Sleep and Insomnia

  • The Sleep Cycle:

    • Stage 1: Drowsiness with slow eye movement.

    • Stage 2: Eye movement ceases.

    • Stage 3: Deep sleep (non-REM).

    • Stage 4: Deep sleep (REM).

  • Psychological Complications of Insomnia:

    • Lower performance levels.

    • Slowed reaction times.

    • Increased risk of depression.

    • Increased risk of anxiety disorders.

  • Physiological Complications of Insomnia:

    • Overweight or obesity.

    • High blood pressure (hypertension).

    • Poor immune system function.

    • Risk of heart disease.

    • Risk of diabetes.

Benzodiazepines: Pharmacology and Use

  • Mechanism of Action: Benzodiazepines cause Central Nervous System (CNS) depression by binding with benzodiazepine receptors in the brain, which are involved in GABA binding sites.

  • Controlled Substance Status: Classified as Class IV substances.

  • Therapeutic Properties: Wide therapeutic range, but can lead to physical dependence.

  • Duration of Treatment Guidelines:

    • Benzos should be used for the shortest period possible.

    • For Anxiety: Managed for less than 4 months ($< 4\text{ months}$).

    • For Insomnia: Managed for less than 3 weeks ($< 3\text{ weeks}$).

  • Pharmacokinetics:

    • Routes: Oral and IV are preferred. IM can be used in emergency situations. Other routes include rectal and insufflation.

    • Distribution: Lipid-soluble agents that cross the blood-brain barrier.

    • Metabolism: Metabolized by the liver; half-lives vary between specific drugs.

  • Therapeutic Uses:

    • Relief of anxiety and sleep disorders.

    • Anticonvulsant properties.

    • Conscious sedation (provides short-term amnesia).

    • Preoperative sedation.

    • Prevention of agitation, seizures, and delirium tremens (DTs) during ethanol (ETOH) withdrawal.

    • Treatment of muscle spasms and status epilepticus.

    • Often used concurrently with SSRIs, antipsychotics, and mood stabilizers.

  • Contraindications and Cautions:

    • Contraindicated in individuals with sleep apnea.

    • Contraindicated in cases of severe respiratory depression.

    • Contraindicated in severe liver or kidney disease.

    • Use with caution in individuals with a history of drug abuse or ETOH use.

  • Benzodiazepine Withdrawal: Abrupt cessation after physical dependence has developed can cause withdrawal symptoms. Medications must be tapered and gradually discontinued.

  • Interactions:

    • Mixing with alcohol or other CNS depressants (like opioids) increases the risk of CNS depression.

    • Herbals such as kava-kava, valerian, or chamomile can increase sedative effects.

  • Specific Benzodiazepine Drugs:

    • Diazepam (Valium).

    • Alprazolam (Xanax).

    • Lorazepam (Ativan).

    • Chlordiazepoxide (Librium).

    • Clonazepam (Klonopin).

    • Midazolam (Versed).

  • Toxicity and Antidote:

    • Primary symptom of toxicity: Respiratory depression.

    • Antidote: Flumazenil (Romazicon).

Non-Benzodiazepine Antianxiety Agents

  • Buspirone (Buspar):

    • Profile: Usually non-sedating with no potential for abuse.

    • Action: Increases norepinephrine.

    • Therapeutic Use: Relief of anxiety.

    • Adverse Effects:

      • Cardiovascular: Chest pain, palpitations, tachycardia, hypertension, hypotension, syncope.

      • Vision: Blurred vision.

      • GI: Nausea, constipation, dry mouth.

      • CNS: Dizziness, drowsiness, incoordination.

    • Interactions: Grapefruit increases the risk of toxicity.

  • Nursing Interventions for Buspirone:

    • Assess chest pain, heart rate/rhythm, and BP.

    • Implement fall precautions (nonskid slippers).

    • Small frequent meals and frequent oral hygiene (non-alcohol based products) for dry mouth.

    • Increase fiber and fluids for constipation.

Other Pharmacologic Agents for Anxiety and Sleep

  • Other Anxiety Classifications:

    • SSRIs.

    • MAOIs.

    • Antihistamines.

    • Antipsychotics.

    • Beta Blockers.

  • Specific Sleep Aids:

    • Chloral hydrate (Noctec): Now off the market in the U.S.

    • Eszopiclone (Lunesta).

    • Ramelteon (Rozerem).

    • Zaleplon (Sonata).

    • Zolpidem (Ambien).

    • Hydroxyzine (Vistaril).

    • Melatonin.

    • Suvorexant (Belsomra): A newer drug classified as an orexin receptor antagonist.

  • Barbiturates:

    • Used for sedation, hypnosis, anesthesia, and inducing coma.

    • Example: Phenobarbital (Luminal).

Smoking Cessation Medications

  • Bupropion (Wellbutrin/Zyban): An antidepressant used to aid smoking cessation.

  • Varenicline (Chantix):

    • Solely a smoking deterrent.

    • Not a benzodiazepine or anxiolytic.

    • Mechanism: Nicotine receptor partial agonist.

    • Risk: Severe psychotic side effects.

  • Nicotine Substitutes: Replacing nicotine with specific nicotine delivery systems.

Nursing Functions and Education

  • Patient Education: Essential for all CNS depressants.

  • Paradoxical Response: Monitor for responses opposite to what is expected.

  • Pregnancy: Advise patients to avoid pregnancy while on these medications.

  • Dosing Philosophy: Start with the lowest possible dose for the shortest possible time.

  • Safety: Provide a safe environment with fall precautions, call bells within reach, and nonskid slippers. Advise patients not to drive or operate heavy machinery.

Case Studies and Clinical Questions

  • Case Study 1 (Thomas Downey):

    • Patient: 42-year-old male hospitalized for severe depression and insomnia.

    • History: Allergic to benzodiazepines. Vital Signs: HR 92bpm92\,bpm, Resp 22bpm22\,bpm, BP 139/89139/89, Pulse Ox 98%98\%. History of ankle fracture.

    • Clinical Consideration: Because he is allergic to benzos, alternative sleep aids must be chosen.

  • Medication Calculation (Clarissa Brown):

    • Order: Nafcillin (Nallpen) 1g1\,g IVPB every 6 hours.

    • Reconstitution: Add 3.4mL3.4\,mL to 1g1-g vial. Add to 50mL50\,mL of 0.9%NaCl0.9\%\,NaCl.

    • Administration: Over 15 minutes.

    • Calculation for IV Pump Flow Rate:

    • Rate (mL/hr)=50mL15min×60min/hr=200mL/hour\text{Rate (mL/hr)} = \frac{50\,mL}{15\,min} \times 60\,min/hr = 200\,mL/hour

  • NCLEX Question: For a client with severe GAD requiring immediate stabilization, Alprazolam (Xanax) is the most effective agent among the choices (Venlafaxine, Buspirone, Paroxetine) due to its rapid onset compared to antidepressants or buspirone.