Anxiolytic-hypnotics agents are used to alter an individual’s responses to environmental stimuli. These agents are referred to as anxiolytics (prevent feelings of tension or fear), sedatives (help patient feel calm and unaware of their environment), and hypnotics (help patients sleep).

Table of Common Drugs and Generic Names


Here is a table of commonly encountered diuretic agents, their generic names, and brand names:

ClassificationsGeneric NameBrand Name
Benzodiazepines used as Anxiolytic-HypnoticsalprazolamXanax
chlordiazepoxideLibrium
clonazepamKlonopin
diazepamValium
lorazepamAtivan
oxazepamSerax
triazolamHalcion
Barbiturates used as Anxiolytic-HypnoticsamobarbitalAmytal sodium
butabarbitalButisol
pentobarbitalNembutal
phenobarbitalLuminal
Other Anxiolytic-Hypnotic Drugsbuspirone
diphenhydramineBenadryl
meprobamateMiltown
promethazinePhenergan
zolpidemAmbien

Manifestation Spotlight: Anxiety, Sedation, and Hypnosis


Anxiety is described as a feeling of tension, nervousness, and apprehension which typically involves unpleasant reactions to a stimulus both real and imaginary. It is accompanied by sympathetic nervous system reactions like fast heartbeat, rapid breathing, flushing, and sweating. Anxiety can be mild, moderate, or severe.

Sedation is the loss of awareness and reaction to environmental stimuli. However, this may be desirable for restless and irritable patients. This is also beneficial for patients who are about to undergo surgery.

Hypnosis is the further depression and sleep of the central nervous system (CNS) which usually results from extreme sedation. In this state, the person no longer senses or reacts to incoming stimuli.

Benzodiazepines Used as Anxiolytic-Hypnotics


Description

  • This is the most frequently used anxiolytic drug because it can lyse or break the feeling of anxiety without causing much sedation and are less likely to make patients physically dependent.

Therapeutic Action

  • By acting on the limbic system and the reticular activating system (RAS), it causes the gamma-aminobutyric acid (GABA) to be more effective in interfering neuron firing. GABA stabilizes the postsynaptic cell which leads to an anxiolytic effect at a dose lower than required to induce sedation and hypnosis. However, the exact mechanism of action is not clearly understood.

Indications

  • Indicated for the treatment of the following conditions: anxiety disorders, alcohol withdrawal, hyperexcitability and agitation, and preoperative relief of anxiety and tension to aid in balanced anesthesia.

Children

  • Response of children to these agents is unpredictable so indication of this drug to the younger population remains to be a challenge.
  • Children may be inappropriately aggressive, tearful, and irritable.
  • Only clonazepam, clorazepate, and diazepam have established pediatric dosage. Possible dried secretions and their effect on breathing must always be assessed carefully.

Adults

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  • If drug is indicated for insomnia, they should be cautioned that drug is for short-term use only. Other methods to help induce sleep such as strict implementation of set bedtime, warm bath, and a back rub must be encouraged before prescribing this drug.
  • It should be advised that activities such as driving, sports, and making legal decisions should be avoided when taking this drug.
  • Liver function should be evaluated before and during therapy.
  • Use of this drug in pregnant and lactating women is contraindicated.

Older adults

  • Older adults are more susceptible to drug adverse effects like hallucinations and sedation.
  • Dosage should be reduced and careful monitoring for toxicity is instituted.
  • Like adults, liver and renal function should be monitored closely.
  • Non-drug measures to reduce anxiety should be encouraged.

Pharmacokinetics

RouteOnsetPeakDuration
Oral30-60 min1-2 h3 h
IM15-30 min30-45 min3 h
IV1-5 min30 min15-60 min
RectalRapid1.5 h3 h
T1/2: 20-80 h
Metabolism: liver
Excretion: urine

Contraindications and Cautions

  • Allergy to benzodiazepines. Prevent severe hypersensitivity reactions.
  • Psychosis. Can be exacerbated by sedation
  • Acute narrow-angle glaucoma, shock, coma, acute alcoholic intoxication. Can be exacerbated by the depressant effects of these drugs.
  • Pregnancy. Associated with development of cleft lip or palate, inguinal hernia, cardiac defects, microcephaly, and pyloric stenosis when taken in the first trimester of pregnancy. Neonatal withdrawal syndrome may also result.
  • Lactation. Potential adverse effects to the neonate (e.g. sedation)
  • Elderly, debilitated. Possibiliy of unpredictable reactions
  • Renal or hepatic dysfunction. May alter metabolism and excretion of drugs resulting in direct toxicity.

Adverse Effects

  • CNS: sedation, drowsiness, depression, lethargy, blurred vision, headache, apathy, light-headedness, amnesia, confusion, mild paradoxical excitatory reactions in the first two weeks of therapy
  • CV: hypotension, hypertension, arrhythmias, palpitations
  • GI: dry mouth, constipation, nausea, vomiting, elevated liver enzymes
  • GU: urinary retention and hesitancy, loss of libido, changes in sexual functioning
  • Hematological: blood dyscrasias, anemia
  • Local injection sites can develop phlebitis, local reactions, and thrombosis.
  • Withdrawal syndrome caused by abrupt cessation of drugs is characterized by nausea, headache, vertigo, malaise, and nightmares.

Interactions

  • Alcohol, other CNS depressants: increased risk of CNS depression
  • Cimetidine, oral contraceptives, disulfiram: increased effects of benzodiazepines
  • Theophylline, ranitidine: decreased therapeutic effects of benzodiazepines
  • Flumazenil is the antidote of benzodiazepine.

Nursing Considerations

Here are important nursing considerations when administering this drug:

Nursing Assessment

These are the important things the nurse should include in conducting assessment, history taking, and examination:

  • Assess for the mentioned cautions and contraindications (e.g. drug allergies, hepatorenal diseases, psychosis, glaucoma, etc.) to prevent any untoward complications.
  • Perform a thorough physical assessment to establish baseline data before drug therapy begins, to determine effectiveness of therapy, and to evaluate for occurrence of any adverse effects associated with drug therapy.
  • Monitor results of laboratory tests (e.g. renal and liver functions tests, complete blood count (CBC), etc.) to monitor effectiveness of the therapy and provide prompt treatment to developing complications.

Nursing Diagnoses

Here are some of the nursing diagnoses that can be formulated in the use of this drug for therapy:

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Implementation with Rationale

These are vital nursing interventions done in patients who are taking anxiolytic-hypnotics:

  • Administer intravenous diuretics slowly to prevent severe changes in fluid and electrolytes.
  • Do not mix intravenous drugs in solution with any other drugs to avoid potential drug-drug interactions.
  • Maintain patients who receive parenteral benzodiazepines in bed for at least 3 hours to ensure patient safety.
  • Monitor patient response to drugs through vital signs, weight, serum electrolytes and hydration to evaluate effectiveness of drug therapy.
  • Monitor hepatic and renal function and CBC for long-term therapies to detect dysfunction and to arrange to taper and discontinue drug if dysfunction occurs.
  • Provide safety measures (e.g. adequate lighting, raised side rails, etc.) to prevent injuries.
  • Educate client on drug therapy to promote compliance.

Evaluation

Here are aspects of care that should be evaluated to determine effectiveness of drug therapy:

  • Monitor patient response to therapy (e.g. controlled anxiety, sleep, etc).
  • Monitor for adverse effects (e.g. hypotension, blood dyscrasias, hepatorenal dysfunction, etc).
  • Evaluate patient understanding on drug therapy by asking patient to name the drug, its indication, and adverse effects to watch for.
  • Monitor patient compliance to drug therapy.

Barbiturates Used as Anxiolytic-Hypnotics


Description

  • These were once the sedative-hypnotic drugs of choice but newer anxiolytics have replaced them. Barbiturates have high risk for addiction and dependency.

Therapeutic Action

  • These are general CNS depressants that inhibit neuronal impulse conduction in the ascending RAS, depress the cerebral cortex, alter cerebellar function, and depress motor output. Therefore, they can cause sedation, hypnosis, anesthesia, and even coma.

Indications

  • Generally indicated for anxiety, sedation, insomnia, paresthesia, and seizures.
  • Parenteral forms may be used for treatment of acute manic reactions.

Children

  • Barbiturates have established pediatric dosage but must be used with caution because children often have unexpected responses.
  • Children may be inappropriately aggressive, tearful, and irritable.
  • Possible dried secretions and their effect on breathing must always be assessed carefully.

Adults

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  • If drug is indicated for insomnia, they should be cautioned that drug is for short-term use only.
  • Other methods to help induce sleep such as strict implementation of set bedtime, warm bath, and a back rub must be encouraged before prescribing this drug.
  • It should be advised that activities such as driving, sports, and making legal decisions should be avoided when taking this drug.
  • Liver function should be evaluated before and during therapy.
  • Use of this drug in pregnant and lactating women is contraindicated.

Older adults

  • Older adults are more susceptible to drug adverse effects like hallucinations and sedation.
  • Dosage should be reduced and careful monitoring for toxicity is instituted.
  • Like adults, liver and renal function should be monitored closely.
  • Non-drug measures to reduce anxiety should be encouraged.

Pharmacokinetics

RouteOnsetPeakDuration
Oral15 min30-60 min10-16 h
IM, subcutaneous10-30 min4-6 h
IVUp 10 15 min5 min4-6 h
T1/2: 79 h
Metabolism: liver
Excretion: urine

Contraindications and Cautions

  • Allergy to barbiturates. Prevent severe hypersensitivity reactions.
  • History of addiction to sedative-hypnotic drugs: barbiturates are more addicting than most other anxiolytics
  • Latent or manifest euphoria. May be exacerbated by drug effects
  • Marked hepatic impairment or nephritis. May alter the metabolism and excretion of drugs
  • Respiratory distress and dysfunction. Exacerbated by CNS depression caused by drugs.
  • Pregnancy. Associated with congenital abnormalities
  • Lactation. Has potential for adverse effects on the infant.
  • Acute or chronic pain. Can cause paradoxical excitement which can mask other symptoms
  • Seizure disorder. Abrupt withdrawal of barbiturates can precipitate status epilepticus
  • Chronic hepatic, cardiac, and respiratory diseases. Can be exacerbated by the depressive effects of these drugs.

Adverse Effects

  • CNS: drowsiness, somnolence, lethargy, ataxia, vertigo, “hangover” feeling, thinking abnormalities, paradoxical excitement, anxiety, hallucinations
  • CV: bradycardia, hypotension, syncope
  • Respiratory: serious hypoventilation, respiratory depression
  • Hypersensitivity reactions: rash, serum sickness, Steven-Johnson syndrome
  • Development of physical tolerance and psychological dependence

Interactions

  • Alcohol, other CNS depressants (e.g. antihistamines, tranquilizers, etc.): increased risk of CNS depression
  • Phenytoin: altered response to phenytoin
  • Monoamine oxidase (MAO) inhibitors: increased serum levels of barbiturates
  • Oral anticoagulants, digoxin, corticosteroids, tricyclic antidepressants (TCAs), oral contraceptives, acetaminophen, metronidazole, carbamazepine: reduced effectivity of these drugs because of enzyme induction effect of barbiturates

Nursing Considerations

Here are important nursing considerations when administering this drug:

Nursing Assessment

These are the important things the nurse should include in conducting assessment, history taking, and examination:

  • Assess for the mentioned cautions and contraindications (e.g. drug allergies, hepatorenal diseases, seizure disorders, etc.) to prevent any untoward complications.
  • Perform a thorough physical assessment to establish baseline data before drug therapy begins, to determine effectiveness of therapy, and to evaluate for occurrence of any adverse effects associated with drug therapy.

Nursing Diagnoses

Here are some of the nursing diagnoses that can be formulated in the use of this drug for therapy:

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  • Impaired gas exchange related to respiratory depression
  • Disturbed thought processes and sensory perception related to CNS effects
  • Risk for injury related to CNS effects

Implementation with Rationale

These are vital nursing interventions done in patients who are taking anxiolytic-hypnotics:

  • Administer intravenous diuretics slowly because rapid administration may cause cardiac problems.
  • Do not mix intravenous drugs in solution with any other drugs to avoid potential drug-drug interactions.
  • Taper dose as ordered because abrupt withdrawal can precipitate seizure attacks.
  • Provide comfort measures (e.g. small, frequent meals, access to bathroom facilities, orientation, etc.) to help patient tolerate drug effects
  • Provide safety measures (e.g. adequate lighting, raised side rails, etc.) to prevent injuries.
  • Educate client on drug therapy to promote compliance.

Evaluation

Here are aspects of care that should be evaluated to determine effectiveness of drug therapy:

  • Monitor patient response to therapy (e.g. controlled anxiety, sleep, etc).
  • Monitor for adverse effects (e.g. hypotension, dependence, hepatorenal dysfunction, etc).
  • Evaluate patient understanding on drug therapy by asking patient to name the drug, its indication, and adverse effects to watch for.
  • Monitor patient compliance to drug therapy.

Practice Exam: Anxiolytic and Hypnotic Drugs


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Questions


1. What drug refers to the ability to help patient feel calm and unaware of his environment?

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A. Anesthesia
B. Sedatives
C. Hypnotics
D. Anxiolytics

2. The most commonly used anxiolytics.

A. Benzodiazepines
B. Diphenhydramine
C. Barbiturates
D. Buspirone

3. Which of the following medical condition(s) can be considered as contraindication(s) to use of anxiolytics and hypnotics?

A. Psychosis
B. Alcoholic intoxication
C. Acute gastroenteritis
D. Both A and B

4. What is the antidote of benzodiazepine?

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A. Theophylline
B. Ranitidine
C. Flumazenil
D. Benadryl

5. Abrupt withdrawal of barbiturates can precipitate what medical condition?

A. Ascites
B. Hypertensive crisis
C. Status epilepticus
D. Coma

Answers & Rationale


1. Answer: B. Sedatives.

Hypnotic effect helps patients sleep and anxiolytic effect helps patients relieve feelings of tension and fear.

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2. Answer: A. Benzodiazepines.

They are the most commonly used anxiolytics because they can lyse or break the feeling of anxiety without causing much sedation and are less likely to make patients physically dependent.

3. Answer: D. Both A & B. 

Psychosis can be exacerbated by the sedative effect of the drug. On the other hand, alcoholic intoxication can be exacerbated by depressant effects of these drugs.

4. Answer: C. Flumazenil

5. Answer: C. Status epilepticus

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