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Central Nervous System Depressants

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

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

CNS Depressants
Sedative-Hypnoticsdose 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

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

Sedative-Hypnotics: Barbiturates
Four categories:
Ultrashort
mephobexital, thiamylal, thiopental

Short
pentobarbital, secobarbital

Intermediate
aprobarbital, butabarbital,amobarbital

Long
Phenobarbital,mephobarbital

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.

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.

Barbiturates and benzodiazepines act similarly to produce depression of central nervous system function and behavior. Both classes of drugs enhance the ability of the inhibitory neurotransmitter, gamma aminobutyric acid (GABA), to activate a type of receptors known as GABA-A receptors. These drugs increase the effectiveness of GABA by altering the receptor so that GABA can bind more easily, an effect known as allosteric regulation. Activation of the GABA-A receptor opens an ion channel, allowing negatively charged chloride ions to enter the cell, producing an inhibition of

GABA is the main inhibitory neurotransmitter in the central nervous system (CNS)..

Sedative-Hypnotics: Barbiturates
Drug Effects
Low doses: Sedative effects

High doses: Hypnotic effects (also lowers respiratory rate)

Sedative-Hypnotics: Barbiturates
Therapeutic Uses
Hypnotics Sedatives Anticonvulsants Surgical procedures

Sedative-Hypnotics: Barbiturates
Side Effects Body System
CNS

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

Respiratory

Sedative-Hypnotics: Barbiturates
Side Effects Body System
GI Other

Effects
Nausea, vomiting, diarrhea Agranulocytosis, vasodilation, hypotension, Stevens-Johnson syndrome

Sedative-Hypnotics: Barbiturates
Toxicology
Overdose frequently leads to respiratory depression, and subsequently, respiratory arrest. Can be therapeutic: Anesthesia induction Uncontrollable seizures: phenobarbital coma

Sedative-Hypnotics: Barbiturates
Drug Interactions
Additive effects: antihistamines, benzodiazepines, narcotics, tranquilizers Inhibited metabolism: MAOIs will prolong effects of barbiturates Increased metabolism: Reduces anticoagulant response, leading to possible clot formation

CNS Depressants: Benzodiazepines


Most frequently prescribed sedativehypnotics
Most commonly prescribed drug classes Favorable side effects Efficacy Safety

Classified as either: Sedative-hypnotic or Anxiolytic

CNS Depressants: Benzodiazepines

(Medication that relieves anxiety)

CNS Depressants: Benzodiazepines


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

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

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)

Miscellaneous sedative-hypnotic agents


chloral hydrate dexmedetomidine diphenhydramine doxylamine eszopiclone

CNS Depressants: Benzodiazepines


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

CNS Depressants: Benzodiazepines


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

CNS Depressants: Benzodiazepines


Therapeutic Uses
Sedation Sleep induction Skeletal muscle relaxation Anxiety relief Treatment of alcohol withdrawal Agitation Depression Epilepsy Balanced anesthesia

CNS Depressants: Benzodiazepines


Side Effects
Mild and infrequent
Headache Drowsiness Dizziness Lethargy Vertigo

Paradoxical excitement (nervousness) Hangover effect

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.

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.

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.

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

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