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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
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
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.
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.
Sedative-Hypnotics: Barbiturates
Drug Effects
Low doses: High doses: Sedative effects
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: 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.
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.
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.
(nervousness)