Académique Documents
Professionnel Documents
Culture Documents
• 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.
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.
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
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.
• 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
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.
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.
• 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.
• 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.