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Central Nervous System

Depressants

Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.


CNS Depressants

Sedatives
• Drugs that have an inhibitory effect on the
CNS to the degree that they reduce:
– Nervousness
– Excitability
– Irritability
– without causing sleep

Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.


CNS Depressants

Hypnotics
• Calm or soothe the CNS to the point that they
cause sleep

Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.


CNS Depressants

Sedative-Hypnotics—dose dependent:
• At low doses, calm or soothe the CNS
without inducing sleep
• At high doses, calm or soothe the CNS
• to the point of causing sleep

Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.


Sedative-Hypnotics: Barbiturates

• First introduced in 1903, standard agents


for insomnia and sedation
• Habit-forming
• Only a handful commonly used today due
in part to the safety and efficacy of:
BENZODIAZEPINES

Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.


Sedative-Hypnotics: Barbiturates
Four categories:
• Ultrashort
– mephobexital, thiamylal, thiopental
• Short
– pentobarbital, secobarbital
• Intermediate
– aprobarbital, butabarbital
• Long
– phenobarbital
Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.
Sedative-Hypnotics: Barbiturates

Barbiturates have a very narrow therapeutic index.

Therapeutic Index
• Dosage range within which the drug is effective
but above which is rapidly toxic.

Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.


Sedative-Hypnotics: Barbiturates

Mechanism of Action
• Site of action:
– Brain stem (reticular formation)
– Cerebral cortex
• By inhibiting GABA, nerve impulses traveling in
the cerebral cortex are also inhibited.

Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.


Sedative-Hypnotics: Barbiturates

Drug Effects
• Low doses: Sedative effects

• High doses: Hypnotic effects


(also lowers respiratory rate)

Notorious enzyme inducers

Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.


Sedative-Hypnotics: Barbiturates

Therapeutic Uses
• Hypnotics
• Sedatives
• Anticonvulsants
• Surgical procedures

Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.


Sedative-Hypnotics: Barbiturates

Side Effects
Body System Effects
CNS Drowsiness, lethargy, vertigo
mental depression, coma

Respiratory Respiratory depression, apnea,


bronchospasms, cough

Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.


Sedative-Hypnotics: Barbiturates

Side Effects
Body System Effects
GI Nausea, vomiting, diarrhea

Other Agranulocytosis,
vasodilation, hypotension,
Stevens-Johnson syndrome

Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.


Sedative-Hypnotics: Barbiturates

Toxicology
• Overdose frequently leads to respiratory depression,
and subsequently, respiratory arrest.
• Can be therapeutic:
– Anesthesia induction
– Uncontrollable seizures: “phenobarbital coma”

Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.


Sedative-Hypnotics: Barbiturates
Drug Interactions
• Additive effects:
– ETOH, antihistamines, benzodiazepines,
narcotics, tranquilizers
• Inhibited metabolism:
– MAOIs will prolong effects of barbiturates
• Increased metabolism:
– Reduces anticoagulant response, leading to
possible clot formation
Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.
CNS Depressants: Benzodiazepines

Most frequently prescribed sedative-hypnotics


• Most commonly prescribed drug classes
• Favorable side effects
• Efficacy
• Safety

Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.


CNS Depressants: Benzodiazepines

Classified as either:
• Sedative-hypnotic or Anxiolytic

(Medication that relieves anxiety)

Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.


CNS Depressants: Benzodiazepines

Sedative-Hypnotic Type
• Long-Acting:
– flurazepam (Dalmane), quazepam (Doral)

• Short-Acting:
– estazolam (Prosom), temazepam (Restoril),
– triazolam (Halcion)

Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.


CNS Depressants: Benzodiazepines
Anxiolytic Type
• alprazolam (Xanax)
• chloridiazepoxide (Librium)
• diazepam (Valium)
• lorazepam (Ativan)
• midazolam (Versed)

zolpidem (Ambien) and zaleplon (Sonata)


(nonbenzodiazepine hypnotic agents, share characteristics)

Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.


CNS Depressants: Benzodiazepines

Mechanism of Action
• Depress CNS activity
• Affect hypothalamic, thalamic, and limbic
systems of the brain
• Benzodiazepine receptors

Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.


CNS Depressants: Benzodiazepines

Drug Effects
• Calming effect on the CNS
• Useful in controlling agitation and anxiety

Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.


CNS Depressants: Benzodiazepines
Therapeutic Uses
• Sedation
• Sleep induction
• Skeletal muscle relaxation
• Anxiety relief
• Treatment of alcohol withdrawal
• Agitation
• Depression
• Epilepsy
• Balanced anesthesia
Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.
CNS Depressants: Benzodiazepines

Side Effects
• Mild and infrequent
Headache Drowsiness
Dizziness Vertigo
Lethargy
Paradoxical excitement (nervousness)
“Hangover effect”

Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.


CNS Depressants:
Nursing Implications
• Before beginning therapy, perform a
thorough history regarding allergies, use
of other medications,health history, and
medical history.
• Obtain baseline vital signs and I & O,
including supine and erect BPs.
• Assess for potential disorders or conditions
that may be contraindications, and for
potential drug interactions.
Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.
CNS Depressants:
Nursing Implications
• Give 15 to 30 minutes before bedtime for
maximum effectiveness in inducing sleep.
• Most benzodiazepines (except flurazepam)
cause REM rebound and a tired feeling the
next day; use with caution in the elderly.
• Patients should be instructed to avoid
alcohol and other CNS depressants.

Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.


CNS Depressants:
Nursing Implications
• Check with physician before taking any other
medications, including OTC medications.
• It may take 2 to 3 weeks to notice improved
sleep when taking barbiturates.
• Abruptly stopping these medications,
especially barbiturates, may cause rebound
insomnia.

Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.


CNS Depressants:
Nursing Implications
• Safety is important
– Keep side rails up
– Do not permit smoking
– Assist patient with ambulation
(especially the elderly)
– Keep call light within reach

• Monitor for side effects

Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.


CNS Depressants:
Nursing Implications
• Monitor for therapeutic effects
– Increased ability to sleep at night
– Fewer awakenings
– Shorter sleep induction time
– Few side effects, such as hangover effects
– Improved sense of well-being because of
improved sleep

Copyright © 2002, 1998, Elsevier Science (USA). All rights reserved.

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