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HS 81: Pharmacology

Anxiolytic and Hypnotic Drugs


States affected by Anxiolytic and Hypnotic Drugs
• Anxiety
• Sedation
• Hypnosis
Anxiety
-is a feeling of tension, nervousness, apprehension, or fear that usually unpleasant
reactions to a stimulus, whether actual or unknown.
-is often accompanied by signs and symptoms of the sympathetic stress reaction,
which may include sweating, fast heart rate, rapid breathing, and elevated blood pressure.
Mild Anxiety
-a common reaction, may serve as a stimulus or motivator in some situations.

• When anxiety becomes overwhelming or serve, it can interfere with the activities of
daily living and lead to medical problems related to chronic stimulation of the
sympathetic nervous system.
• A severely anxious person may be afraid to leave the house or to interact with other
people.
Anxiolytic drugs
-are drugs that are used to lyse or break the feeling of anxiety.
Sedation
-the loss of awareness and reaction to environmental stimuli.
-may be desirable in patients who are restless, nervous, irritable, or overreacting to
stimuli.
-an axiolytic, it may frequently lead to drowsiness.

• The choice of anxiolytic drug depends on the situation in which it will be used,
keeping the related adverse effects in mind.
Hypnosis
-a result of extreme sedation through the depression and sleep of the central nervous
system.
-an extreme state of sedation, in which the person no longer senses or react to
incoming stimuli.

Hypnotics
-are used to help people fall asleep by causing sedation.
-drugs that are effective hypnotics act on the reticular activating system (RAS) and
block the brain’s response to incoming stimuli.
Benzodiazepines
-the most frequently used axiolytic drugs, prevent anxiety without causing much
associated sedation.
-they are less likely to cause physical dependence than many of the older
sedatives/hypnotics that are used to relieve anxiety.

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Therapeutic Actions: It acts in the limbic system and the RAS to make gamma-aminobutyric
acid (GABA) more effective, causing interference with neuron firing. GABA stabilizes the
postsynaptic cell. This leads to an anxiolytic effect at doses lower than those required to
induced sedation and hypnosis. The exact mechanism of action is not clearly understood.
Indication: It is indicated for the treatment of the following conditions: anxiety disorders,
alcohol withdrawal, hyper excitability and agitation, and preoperative relief of anxiety and
tension to aid in balanced anesthesia.

Pharmacokinetics: They are well absorbed from the gastrointestinal tract, with peak levels
achieved in 30 minutes to 2 hours. They are lipid soluble and well distributed throughout the
body, crossing the placenta and entering breast milk. They are metabolized extensively in
the liver. Patients with liver disease must receive a smaller dose and be monitored closely.
Excretion is primarily through the urine.

Contraindications: Contraindications include allergy to any benzodiazepine; psychosis, which


could be exacerbated by sedation; and acute narrow-angle glaucoma, shock, coma, or acute
alcoholic intoxication, all of which could be exacerbated by the depressant effects of these
drugs.
• Sedatives/hypnotics are contraindicated in pregnancy because a predicatble
sundrome of cleft lip or palate, inguinal hernia, cardiac defects, microcephaly, pyloric
stenosis occurs when they are taken in the first trimester.
• Neonatal withdrawal syndrome may also result.
• Breastfeeding is also a contraindication because of potential adverse effects on the
neonate.
Cautions: They are used cautiously in elderly or debilitated patients because of the
possibility of unpredictable reactions and in cases of renal or hepatic dysfunction, which may
alter the metabolism and excretion of these drugs, resulting in direct toxicity.

Adverse Effects: The adverse effects are associated with the impact of these drugs on the
central and peripheral nervous systems. Nervous system effects include sedation,
drowsiness, depression, lethargy, blurred vision, headaches, apathy, light-headedness, and
confusion.
• Mild paradoxical excitatory reactions may occur during the first 2 weeks of therapy.
• GI: dry mouth, constipation, nausea, vomiting, and elevated liver enzymes may
result.
• CV: hypotension, hypertension, arrhythmias, palpitations, and respiratory difficulties.
• Hemat: blood dyscrasias and anemia
• GU: urinary retention and hesitancy, loss of libido, changes in sexual functioning.
• Local: phlebitis, local reactions, and thrombosis may occur at local injection sites.
• Misc: Nausea, headache, vertigo, malaise, and nightmares.
Some Benzodiazepines
Drug Name Dosage/Route Usual Indications
alprazolam 0.25-0.5 mg PO t.i.d. up to 1-10mg/day PO have been used; Anxiety: panic attacks
(Xanax) reduced dosage in elderly. Onset: 30 minutes
Duration: 4-6h
Special Considerations: Taper after long-
term therapy.
diazepam Adult: 2-10 mg PO b.i.d. to q.i.d.; 0.2 mg/kg PR; or 2-30mg IM b.i.d Anxiety; alcohol withdrawal; muscle
(Valium) or IV 2-2.5mg PO b.i.d. for elderly patients relaxant; antiepileptic; antitetanus;
Pediatric: 1-2.5 mg PO t.i.d.; 0.3-0.5 mg/kg PR; or 1-3mg IM or IV preoperative anxiolytic
Onset: 5-60 min

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Duration: 3 h
Special Considerations: Monitor injection
sites; drug of choice if route change is
anticipated; taper after long-term
therapy.
lemazepam 15-30 mg PO at bedtime Hypnotic; treatment of insomnia
(Restoril) Onset: varies
Duration: 4-6h
Special Considerations: Taper after long-
term therapy
triazolam 0.125-0.5 mg PO at bedtime Hypnotic; treatment of insomnia
(Halcion) Onset: varies
Duration: 2-4h
Special considerations: Monitor liver and
renal function, CBC; taper after long-term
therapy
Clinically Important Drug-Drug Interactions
• The risk of CNS depression increases if benzodiazepines are taken with alcohol or
other CNS depressants, so such combinations should be avoided.
• The effects of benzodiazepines increases if they are taken with cimetidine, oral
contraceptives, or disulfiram. If any of these drugs are used with benzodiazepines,
patients should be monitored and the appropriate dosage adjustments made.
• Finally, the impact of benxodiazepines may be decreased if they are given with
theophylines or ranitidine. If either of these drugs is used, dosage adjustment may be
necessary.

Nursing Considerations for Patients Receiving Benzodiazepines


Assessment: History and Examination
• Assess for known allergies to benzodiazepines; impaired liver or kidney function,
which could alter the metabolism and excretion of a particular drug; any condition
that might be exacerbated by the depressant effects of the drugs; and pregnancy
and lactation.
• Assess for potential adverse effects.
• Assess for the following: temperature and weight; skin color and lesions; affect,
orientation, reflexes, and vision; pulse, blood pressure, and perfusion; respiratory
rate, adventitious sounds, and presence of chronic pulmonary disease; and bowel
sounds on abdominal examination.
Nursing Diagnoses
• Disturbed Thought Processes and Disturbed Sensory Perception (Visual, Kinesthetic)
related to CNS effects
• Risk for injury related to CNS effects
• Disturbed sleep pattern related to CNS effects
• Deficient Knowledge regarding drug therapy
Implementation with Rationale
• Do not administer intra-arterially because serious arteriospasm and gangrene could
occur. Monitor injection sites carefully for local reactions to institute treatment as
soon as possible.
• Do not mix intravenous (IV) drugs in solution with any other drugs to avoid potential
drug-drug interactions.
• Give parenteral forms only if oral forms are not feasible or available, and switch to
oral forms, which are safer and less likely to cause adverse effects, as soon as
possible.

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• Give IV drugs slowly because these agents have been associated with hypotension,
bradycardia, and cardiac arrest.
• Arrange to reduce the dosage of narcotic analgesics in patients receiving a
benzodiazepine to decrease potentiated effects and sedation.
• Maintain patients who receive parenteral benzodiazepines in bed for a period of at
least 3 hours.
• Monitor hepatic or renal function as well as CBC during long-term therapy to detect
dysfunction and to arrange to taper and discontinue drug if dysfunction occurs.
• Taper dosage gradually after long-term therapy, especially in epileptic patients.
• Provide comfort measures to help patients tolerate drug effects, such as having them
void before dosing, instituting a bowel program as needed, giving food with the drug
if GI upset is sever, environmental control, and orientation.
• Provide thorough patient teaching, including drug name, prescribed dosage,
measures for avoidance of adverse effects, and warning signs that may indicate
possible problems.
• Instruct patients about the need for periodic monitoring and evaluation to enhance
patient knowledge about drug therapy and to promote compliance.
• Offer support and encouragement to help the patient cope with the diagnosis and the
drug regimen.
Evaluation
• Monitor patient response to the drug (alleviation of signs and symptoms of anxiety;
sleep; sedation)
• Monitor for adverse effects (sedation, hypotension, cardiac arrhythmias, hepatic or
renal dysfunction, blood dyscrasias).
• Evaluate effectiveness of teaching plan (patient can give the drug name, dosage,
possible adverse effects to watch for, specific measures to help avoid adverse
effects, and the importance of continued follow-up).
• Monitor effectiveness of comfort measures and compliance with regimen.
Barbiturates
-were once the sedative/hypnotic drugs of choice.
-not only is likelihood of sedation and other adverse effects greater with these drugs,
but the risk of addiction and dependence is also greater.

Therapeutic Actions: They are greater CNS depressants that inhibit neuronal impulse
conduction in the ascending RAS, depress the cerebral cortex, alter cerebellar function, and
depress motor output. Thus, they can cause sedation, hypnosis, anesthesia, and in extreme
cases, coma.
Indications: They are indicated for relief of the signs and symptoms of anxiety, for sedation,
insomnia, preanesthesia, and seizures. Parenteral forms, which reach peak levels faster and
have a faster onset of action, may be used for treatment of acute manic reactions and many
forms of seizures.

Pharmacokinetics: They are absorbed well, reaching peak levels in 20 to 60 minutes. They
are metabolized in the liver to varying degrees, depending on the drug, and excreted in the
urine. The longer-acting barbiturates tend to be metabolized slower and excreted to a
greater degree unchanged in the urine. The barbiturates are known to induce liver enzyme
systems, increasing the metabolism of the barbiturate broken down by that system, as well

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as that of any other drug that may be metabolized by that enzyme system. Patients with
hepatic or renal dysfunction require lower doses of the drug to avoid toxic effects and should
be monitored closely. Barbiturates are lipid soluble; they readily cross the placenta and
enter breast milk.

Contraindications: They are contraindicated to alert to any barbiturate and a previous


history of addiction to sedative/ hypnotic drugs because the barbiturates are more addicting
than most other axiolytics.
• Latent or manifest porphyria, which may be exacerbated; marked hepatic
impairment or nephritis, which may alter the metabolism and excretion of these
drugs
• Respiratory distress or severe respiratory dysfunction, which could be exacerbated
by the CNS depression caused by these drugs.
• Pregnancy is a contraindication because of potential adverse effects on the fetus;
congenital abnormalities have been reported with barbiturate use.
Cautions: They are cautiously used in patients with acute or chronic pain because
barbiturates can cause paradoxical excitement, masking other symptoms; with seizure
disorders because abrupt withdrawal of a barbiturate can precipitate status epileptics; and
with chronic hepatic, cardiac, or respiratory diseases, which could be exacerbated by the
depressive effects of these drugs. Care should be taken with lactating women because of
the potential for adverse effects on the infant.

Adverse Effects: The adverse effects caused by barbiturates are more severe than those
associated with other, newer sedatives/hypnotics. They are no longer considered the
mainstay for the treatment of anxiety.
• Development of physical tolerance and psychological dependence is more likely with
the barbiturates than with other anxiolytics.
• Related to general CNS depression
• CNS: drowsiness, somnolence, lethargy, ataxia, vertigo, a feeling of a “hangover”
thinking abnormalities, paradoxical excitement, anxiety, and hallucinations.
• GI: nausea, vomiting, constipation, diarrhea, and epigastric pain may occur.
• CV: bradycardia, hypotension (particularly with IV administration), and syncope.
• Resp: hypoventilation, respiratory depression, and laryngospasm may also result,
particularly with IV administration.
• Derm: rash
• Misc: serum sickness, Stevens-Johnson syndrome, which is sometimes fatal, may also
occur.

Clinically Important Drug-Drug Interactions


• Increased CNS depression results if these agents are taken with other CNS
depressants, including alcohol, antihistamines, and other tranquilizers.
• If other CNS depressants are used dosage adjustments are necessary.
• There often is an altered response to phenytoin if it is combined with barbiturates;
evaluate the patient frequently if this combination cannot be avoided.
• If barbiturates are combined with monoamine oxidase (MAO) inhibitors, increased
serum levels and effects occur.

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• If the older sedatives/hypnotcs are combined with MAO inhibitors, patients should be
monitored closely and necessary dosage adjustments made.
• Because of an enzyme-induction effect of barbiturates in the liver, the following
drugs may not be as effective as desired:
o Oral anticoagulants, digoxin, tricyclic antidepressants (TCAs), corticosteroids,
oral contraceptives, estrogens, acetaminophen, metronidazole,
phenmetrazine, carbamazepine, beta-blockers, griseofulvin,
phyenylbutazones, theophyllines, quinidine, and doxycycline. If these agents
are given in combination with barbiturates, patients should be monitored
closely; frequently dosage adjustments may be necessary to achieve the
desired therapeutic effect.

Nursing Considerations for Patients Receiving Barbiturates


Assessment: History and Examination
• Similar with the assessment done in patients receiving benzodiazepine.
Nursing Diagnoses
• Disturbed Thought Process and Disturbed Sensory Perception (Visual, Auditoyr,
Kinesthetic, Tactile) related to CNS effects
• Risk for Injury related to CNS effects
• Impaired Gas Exchange related to respiratory depression
• Deficient Knowledge regarding drug therapy
Implementation
• Do not administer these drugs intra-arterially because serious arteriospasm and
gangrene could occur.
• Monitor injection sites carefully for local reactions.
• Do not mix IV drugs in solution with any other drugs to avoid potential drug-drug
interactions.
• Give parenteral forms only if oral forms are not feasible or available, and witch to oral
forms as soon as possible to avoid serious reactions or adverse effects.
• Give IV medications slowly because rapid administration may cause cardiac
problems.
• Provide standby life-support facilities in case of severe respiratory depression or
hypersensitivity reactions.
• Taper dosage gradually after long-term therapy, especially in epileptic patients.
• Provide comfort measures to help patients tolerate drug effects, such as having them
void before dosing, instituting a bowel program as needed, giving food with the drug
if GI upset is sever, environmental control, and orientation.
• Provide thorough patient teaching, including drug name, prescribed dosage,
measures for avoidance of adverse effects, and warning signs that may indicate
possible problems.
• Instruct patients about the need for periodic monitoring and evaluation to enhance
patient knowledge about drug therapy and to promote compliance.
• Offer support and encouragement to help the patient cope with the diagnosis and the
drug regimen.
Evaluation

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• Monitor patient response to the drug (alleviation of signs and symptoms of anxiety;
sleep; sedation)
• Monitor for adverse effects (sedation, hypotension, cardiac arrhythmias, hepatic or
renal dysfunction, blood dyscrasias).
• Evaluate effectiveness of teaching plan (patient can give the drug name, dosage,
possible adverse effects to watch for, specific measures to help avoid adverse
effects, and the importance of continued follow-up).
• Monitor effectiveness of comfort measures and compliance with regimen.

Other Anxiolytic and Hypnotic Drugs


• Other Drugs are used to treat anxiety or to produce hypnosis that do not fall into
either the benzodiazepines or the barbiturate group. Such medication include the
following:
o Paraldehyde (Paral), a very old drug, is still used orally and rectally to sedate
the patients with delirium tremens or psychiatric conditions characterized by
extreme excitement. It is rapidly absorbed and metabolized in the liver. It
cannot be stored in plastic containers or dispensed with a plastic spoon or
syringe.
o Meprobamate (Miltown) is an older drug that is used to manage acute anxiety
for up to 4 months. It works in the limbic system and thalamus and has some
anticonvulsant properties and central nervous system muscle relaxing effects.
o Chloral hydrate (Aquachloral) is frequently used to produce nocturnal sedation
or preoperative sedation. Its mechanism of action is unknown.
o Zaleplon (Sonata) and zolpidem (Ambien) both of which cause sedation, are
used for the short-term treatment of insomnia. They are thought to work by
affecting serotonin levels in the sleep center near the RAS. Patient should be
going to bed and able to stay there for 4 to 8 hours when taking these drugs.
o Dexmedetomidine (Precedex) is given intravenously at a starting dose of
1mcg/kg over 10 minutes and then a controlled infusion for up to 24 hours. It
is used for sedation of newly intubated and mechanically ventilated patients
in an ICU.
o Eszopiclone(Lunesta) is a new agent used to treat insomnia. It is thought to
react with GABA sites near benzodiazepine receptors.
o Antihistamines (promethazine [Phenergan], diphenhydramine [Benadryl] can
be very sedating in some people. They are used as preoperative medications
and postoperatively to decrease the need for narcotics. Patients need to be
monitored for thickened respiratory secretions and breathing difficulties, a
problem that can cause concern after anesthesia.
o Buspirone (BuSpar), a newer antianxiety agent, has no sedative,
anticonvulsant, or muscle-relaxant properties, and its mechanism of action is
unknown.
o Ramelteon (Rozerem), introduced in 2005, is the first of a new class of
sedatives/hypnotics, the melatonin receptor agonists. This drug stimulates
melatonin receptors, which are thought to be involved in the maintenance of
circadian rhythm and the sleep-wake cycle. It is used for the treatment of
insomnia characterized by difficulty with sleep onset. It is rapidly absorbed
with peak levels in 30 to 90 minutes. It is metabolized in the liver and

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excreted in the feces and urine. It should be administered 30 minutes before


bed. Patients should be monitored for depression and suicidal ideation.

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