Sedative Hypnotics

Sedative

Reduce anxiety & exert calming effect. effective agents produce a CNS depression not greater than therapeutic goal

Hypnotic Agent

produce drowsiness & encourage sleep & a greater degree of CNS depression than a sedative

Benzodiazepines

Produce calming effects followed by drowsiness leadin to sleep and at higher concentrations coma.
No surgical anesthsia or fatal respiratory depression.

Barbiturates

produce a dose dependent CNS depression. Produce calming, sleep , drowsiness unconsciousness, surgical anesthesia, coma and eventually fatal depression of cardiovascular & respiratory systems.

Benzodiazepines Mechanism

Increase the frequency of channel openings in the presence of GABA & increase the affinity of GABA for the receptors. Binds to Gaba -A (BZ1 & BZ2).

Barbiturates

Increase mean open time of channel in the presence of GABA, can act directly as agonists at high concentratiom, & can increase affinity of GABA.

Benzodiazepines
Uses & Adverse effects

Uses: Anxiolytics, Hypnotics, antiepileptics, muscle relaxants, adjuncts to anesthesia and to alleviate the symtoms of alcohol withdrawal.

Adverse Effects: prolong use leads to tolerance & dependence. All should be presribed for short peroids.

Benzodiazepines Caution

w/COPD, OSA, Children & Hepatic dsyfunction. Few w/CV problems but may decrease BP & increase HR. FATAL if taken w/other depressants like alcohol or barbiturates. All BDZ can be abused.

Diazepam(Valium)

Drug Class:
Benzodiazepines Agonists

Pharmacokinetics:
Rapid absorbed & onset
wide distrubuted given orally

Metabolism: Hepatic

Excreted: Urine

Metabolites:
(2)desmethyldiazepam & oxazepam

Side Effects:
residual drowsiness

Uses:
Anxiety
STATUS epilepticus, Anesthesia,
Alcohol W/D

Duration: Long 1-3 days

Admin: IV or ORAL