Anxiolytics and Sedative-Hypnotics

ANXIOLYTICS AND SEDATIVE-HYPNOTICS, PART 1

DRUG NAME CLASS

  • Benzodiazepines
  • Barbiturates

MECHANISM OF ACTION

  1. Benzodiazepines

    • Bind to GABA A receptors
    • Effects:
      • ↑ frequency of Cl⁻ channel opening
      • ↑ Cl⁻ influx
      • Resulting in membrane hyperpolarization
      • ↓ neuronal excitability
  2. Barbiturates

    • Bind to GABA A receptors
    • Effects:
      • ↑ duration of Cl⁻ channel opening
      • ↑ Cl⁻ influx
      • Resulting in membrane hyperpolarization
      • ↓ neuronal excitability

INDICATIONS

  • Benzodiazepines:

    • Anxiety
    • Preoperative sedation
    • Anesthesia induction
    • Sedation for mechanical ventilation
    • Alcohol withdrawal syndrome
    • Status epilepticus
  • Barbiturates:

    • Anxiety
    • Preoperative sedation
    • Convulsions
    • Induced coma

ROUTE(S) OF ADMINISTRATION

  • Benzodiazepines:

    • Short-acting (-azolam):
    • alprazolam (Xanax)
    • midazolam (Nayzilam)
    • Intermediate-acting (-azepam):
    • lorazepam (Ativan)
    • clonazepam (KlonoPIN)
    • Long-acting (-azepam):
    • diazepam (Valium)
  • Barbiturates:

    • butabarbital
    • pentobarbital (Nembutal sodium)
    • phenobarbital

SIDE EFFECTS

  • Benzodiazepines:

    • Headache
    • Sedation
    • Dizziness
    • Blurred vision
    • Dry mouth
    • Urinary incontinence
    • Constipation
    • Leukopenia
    • Paradoxical stimulation
    • Tolerance, dependence, and withdrawal symptoms
  • Barbiturates:

    • Headache
    • Somnolence
    • Confusion
    • CNS depression
    • Hallucinations
    • Vertigo
    • Nausea, vomiting, diarrhea
    • Asthenia
    • Ataxia
    • Paradoxical stimulation
    • Tolerance, dependence, withdrawal symptoms
    • Stevens-Johnson syndrome

CONTRAINDICATIONS AND CAUTIONS

  • Benzodiazepines:

    • Myasthenia gravis
    • Concomitant use with other CNS depressants
    • Acute narrow-angle glaucoma
    • Pregnancy, breastfeeding
  • Barbiturates:

    • Concomitant use with other CNS depressants
    • Hypotension
    • Laryngospasm
    • Bronchospasm

NURSING CONSIDERATIONS

  1. Assessment and Monitoring:

    • Vital signs including orthostatic hypotension assessment
    • Weight
    • Level of consciousness (LOC)
    • Laboratory values: CBC, hepatic, renal, cardiac function
    • Current medications
    • Side effects - report to provider and intervene if necessary
    • Have resuscitative equipment nearby
  2. Client Education:

    • Teach the client to monitor for and report side effects
    • Avoid hazardous activities like driving until response is known
    • Provide safety measures like raising side-rails and ensuring adequate lighting
    • Make position changes slowly to reduce effects of orthostatic hypotension
    • Avoid grapefruit juice if taking alprazolam or midazolam therapy
    • Administer IV dose slowly

ANXIOLYTICS AND SEDATIVE-HYPNOTICS, PART 2

DRUG NAME CLASS

  • Hypnotic; Non-benzodiazepines
  • Miscellaneous anxiolytics
    • Examples:
    • zaleplon
    • eszopiclone (Lunesta)
    • buspirone

MECHANISM OF ACTION

  1. Bind to GABA A receptors

    • Effects include increased frequency of Cl⁻ channel opening and increased Cl⁻ influx
    • Resulting in membrane hyperpolarization and decreased neuronal excitability
  2. Bind to and activate 5-HT1 receptors

  3. Bind to and block D2 receptors

INDICATIONS

  • Insomnia
  • Anxiety

ROUTE(S) OF ADMINISTRATION

  • Oral (PO)

SIDE EFFECTS

  • Headache
  • Hot flashes
  • Drowsiness
  • Anxiety
  • Nausea, vomiting
  • Ataxia
  • Erectile dysfunction
  • Tolerance, dependence, and withdrawal symptoms
  • Headache, sedation, dry mouth

CONTRAINDICATIONS AND CAUTIONS

  • Concomitant use with other CNS depressants
  • Hepatic / renal impairment

NURSING CONSIDERATIONS

  1. Assessment and Monitoring:

    • Vital signs
    • Weight
    • Level of consciousness (LOC)
    • Laboratory values: CBC, hepatic, renal, cardiac function
    • Current medications
    • Side effects - report to provider and intervene if necessary
  2. Client Education:

    • Teach the client to monitor for and report side effects
    • Avoid hazardous activities like driving until response is known
    • Provide safety measures like raising side-rails and ensuring adequate lighting
    • Take only if able to get a full night’s sleep (7–8 hrs)
    • Dangerous sleep behaviors like sleepwalking and sleep-driving may occur
    • Notify provider if chronic abnormal movements like dystonia, motor restlessness, or involuntary movement of facial or cervical muscles occurs
    • Avoid large amounts of grapefruit.

AUTHOR INFORMATION

  • Filip Vasiljević, MD
  • Kimberly Clay, BSN, RN
  • Illustrator: Robyn Hughes, MScBMC
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