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CNS Depressants

CNS Depressants

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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: • High doses: Sedative effects

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
CNS

Effects
Drowsiness, lethargy, vertigo mental depression, coma Respiratory depression, apnea, bronchospasms, cough

Respiratory

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

Sedative-Hypnotics: Barbiturates
Side Effects
Body System
GI Other

Effects
Nausea, vomiting, diarrhea 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 ―Hangover effect‖

(nervousness)

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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