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Anxiolytics & sedative-hypnotics: Nursing Pharmacology

Notes

Notes

ANXIOLYTICS AND SEDATIVE-HYPNOTICS, PART 1
DRUG NAME
Short-acting (-azolam):
alprazolam (Xanax)
midazolam (Nayzilam)

Intermediate-acting 
(-azepam):
lorazepam (Ativan)
clonazepam (KlonoPIN)

Long-acting (-azepam):
diazepam (Valium)
butabarbital,

pentobarbital 
(Nembutal sodium),

phenobarbital
CLASS
Benzodiazepines
Barbiturates
MECHANISM OF ACTION
  1. Bind to GABAA receptors
  2. ↑ frequency of Cl- channel opening; ↑ Cl-  influx
  3. Membrane hyperpolarization;
    ↓ neuronal excitability
  1. Bind to GABAA receptors
  2. ↑ duration of Cl- channel opening; ↑ Cl-  influx
  3. Membrane hyperpolarization; ↓ neuronal excitability
INDICATIONS
  • Anxiety
  • Preoperative sedation
  • Anesthesia induction
  • Sedation for mechanical ventilation
  • Alcohol withdrawal syndrome
  • Status epilepticus
  • Anxiety
  • Preoperative sedation
  • Convulsions
  • Induced coma


ROUTE(S) OF ADMINISTRATION
PO, IV, IM, SC, SL, PR
PO, IV, IM
SIDE EFFECTS
  • Headache, sedation, dizziness
  • Blurred vision, dry mouth
  • Urinary incontinence, constipation
  • Leukopenia
  • Paradoxical stimulation
  • Tolerance, dependence, and withdrawal symptoms
  • Headache, somnolence, confusion
  • CNS depression, hallucinations, vertigo
  • Nausea, vomiting, diarrhea
  • Asthenia, ataxia
  • Paradoxical stimulation
  • Tolerance, dependence, and withdrawal symptoms
  • Stevens-Johnson syndrome
CONTRAINDICATIONS AND CAUTIONS
  • Myasthenia gravis
  • Concomitant use with other CNS depressants
  • Acute narrow-angle glaucoma
  • Pregnancy, breastfeeding
  • Concomitant use with other CNS depressants
  • Hypotension, laryngospasm, bronchospasm
NURSING CONSIDERATIONS
Assessment and monitoring
  • Vital signs - include orthostatic hypotension assessment
  • Weight
  • LOC
  • Laboratory values: CBC, hepatic, renal, cardiac function
  • Current medications
  • Side effects - report to provider and intervene if necessary
  • Administer IV dose slowly

Client education

  • Teach the client to monitor for and report side effects
  • Avoid hazardous activities like driving until response is known
  • Keep clients who receive parenteral doses in bed for at least three hours to ensure safety
  • 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
Assessment and monitoring
  • Vital signs - include orthostatic hypotension assessment
  • Weight
  • LOC
  • Laboratory values: CBC, hepatic, renal, cardiac function
  • Current medications
  • Side effects - report to provider and intervene if necessary
  • Have resuscitative equipment nearby
  • Phenobarbital for long-term anticonvulsant therapy - monitor serum folate levels
  • Administer IV dose slowly

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
  • Can reduce the efficacy of oral contraceptives
  • Make position changes slowly to reduce effects of orthostatic hypotension
  • Promptly report flu-like symptoms or a rash which could indicate Stevens-Johnson syndrome
ANXIOLYTICS AND SEDATIVE-HYPNOTICS, PART 2
DRUG NAME
zolpidem (Ambien),
zaleplon,
eszopiclone (Lunesta)

buspirone
CLASS
Hypnotic;
Non-benzodiazepines
Miscellaneous anxiolytics
MECHANISM OF ACTION
  1. Bind to GABAA receptors
  2. ↑ frequency of Cl- channel opening; ↑ Cl-  influx
  3. Membrane hyperpolarization;
    ↓ neuronal excitability
  1. Bind to and activate 5-HT1 receptors
  2. Bind to and block DA2 receptors
INDICATIONS
Insomnia
Anxiety
ROUTE(S) OF ADMINISTRATION
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
Assessment and monitoring
  • Vital signs
  • Weight
  • LOC
  • Laboratory values: CBC, hepatic, renal, cardiac function
  • Current medications
  • Side effects - report to provider and intervene if necessary

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 sleep-walking and sleep-driving may occur
Assessment and monitoring
  • Vital signs
  • Weight
  • LOC
  • Laboratory values: CBC, hepatic, renal, cardiac function
  • Current medications
  • Side effects - report to provider and intervene if necessary

Client education
  • Teach the client to monitor for and report side effects
  • Avoid hazardous activities like driving until response is known
  • Notify provider if chronic abnormal movements like dystonia, motor restlessness, or involuntary movement of facial or cervical muscles occurs
  • Avoid large amounts of grapefruit


Transcript

Anxiolytics and sedative-hypnotics are medications that act as central nervous system depressants that reduce tension and induce calm or sleep, and are primarily used to relieve anxiety, as well as insomnia.

It’s important to note that the preferred medications for the long-term management of anxiety are typically selective serotonin reuptake inhibitors, or SSRIs for short, due to their low abuse potential and dependence.

But, medications that can be used for the short-term management include benzodiazepines, barbiturates, and miscellaneous anxiolytics.

First, let’s start with benzodiazepines. These medications are usually taken orally, but some of them can also be administered intravenously, intramuscularly, subcutaneously, sublingually, or even rectally.

Now, based on the overall duration of action, benzodiazepines can be subdivided into three main groups.

The first group includes short-acting benzodiazepines, which typically end in -azolam, such as alprazolam and midazolam; the second group covers intermediate-acting benzodiazepines that end in -azepam, like lorazepam and clonazepam; and finally, the third group includes long-acting benzodiazepines that also end in -azepam, such as diazepam.

In addition to treating anxiety and insomnia, benzodiazepines are also indicated for treatment for status epilepticus, where a person has ongoing or multiple seizures for over 5 minutes.

Other important indications include preoperative sedation, induction of general anesthesia sedation for mechanical ventilation, and alcohol withdrawal syndrome.

Now, benzodiazepines work by binding to GABAA receptors, increasing the frequency at which they open up to let chloride ions into the cell. The influx of negatively charged chloride ions makes the neuron less responsive to stimuli.

Now, benzodiazepines can cause side effects like headache, sedation, and dizziness; as well as blurred vision and dry mouth.

Also, despite being a central nervous system depressant, benzodiazepines can cause paradoxical stimulation in certain parts of the brain, leading to symptoms such as fast speech, excitement, and restlessness.

In rare cases, clients might experience urinary incontinence, constipation, or even develop leukopenia, which can lead to fever, malaise, and sore throat.

Finally, if used continuously over long periods of time, benzodiazepines can lead to tolerance, dependency, and abuse.

So, when the medication is discontinued, the client may experience withdrawal symptoms, which include anxiety, tremors, tachycardia, hypertension, agitation, delirium, and life-threatening seizures.

As far as contraindications go, benzodiazepines should be avoided in individuals with myasthenia gravis, since they can exacerbate myasthenic symptoms.

Other contraindications include severe liver impairment, and acute narrow-angle glaucoma, and must not be combined with other CNS depressants, such as alcohol.

Finally, benzodiazepines should be avoided during pregnancy, breastfeeding and in individuals diagnosed with sleep apnea.

Now, let’s switch our focus to barbiturates that can be used as anxiolytics or sedative-hypnotics, such as butabarbital, pentobarbital, and phenobarbital, which can be administered orally, intravenously, or intramuscularly.

Barbiturates also bind GABAA receptors, but in contrast to benzodiazepines, they increase the duration of their opening, thereby increasing the influx of chloride ions.

As a result, the neuron becomes less responsive to stimuli. Besides anxiety, barbiturates can also be used for preoperative sedation, anesthesia induction, convulsions, and to induce coma in life-threatening conditions, such as increased intracranial pressure.

Barbiturates can cause side effects like headache, somnolence, confusion, hallucinations, and vertigo, and CNS depression may even lead to coma or death.

Some clients can experience bradycardia, hypotension, and syncope; while others might experience respiratory depression and even apnea.

Common gastrointestinal problems include nausea, vomiting, and constipation; while important musculoskeletal side effects include asthenia, or lack of energy and physical weakness; and ataxia, which refers to a lack of coordination and muscle control.

Just like benzodiazepines, barbiturates can also cause paradoxical stimulation, as well as tolerance and dependence, which can be followed by withdrawal symptoms.

Finally, on rare occasions, clients treated with barbiturates can develop a life-threatening rash called Stevens-Johnson syndrome.

Important contraindications include concomitant administration of barbiturates with other CNS depressants, such as alcohol and benzodiazepines; as well as hypotension; laryngospasm, and bronchospasm.

Finally, we have miscellaneous anxiolytics, which include nonbenzodiazepine sedative-hypnotics and buspirone.

First, let’s focus on nonbenzodiazepines: zolpidem, zaleplon, and eszopiclone, which are often referred to as ZZZ medications.

These medications are taken orally and they are called nonbenzodiazepines because they have a different chemical structure to the benzodiazepines, but the same mechanism of action.

The most common side effects associated with nonbenzodiazepines include headache, hot flashes, anxiety, nausea, and vomiting. Also, some clients might present with ataxia and erectile dysfunction.

Additionally, nonbenzodiazepines have a boxed warning about abnormal sleep behaviors like sleep-walking or engaging in other activities while not fully awake.

Sources
  1. "Mosby's 2021 Nursing Drug Reference" Mosby (2021)
  2. "Pharmacology: A Patient-Centered Nursing Process Approach (8e)" Elsevier Health Sciences (2014)
  3. "Focus on Nursing Pharmacology" LWW (2019)
  4. "Saunders Comprehensive Review for the NCLEX-RN Examination" Saunders (2019)