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According to uses
Anxiolytics
Lorazepam Oxazepam Alprazolam
Chlordiazepoxide Diazepam Prazepam
Clonazepam
Hypnotics
short: Triazolam
Intermediate:
Lorazepam , Estazolam
Temazepam Nitrazepam
Long: Flurazepam, Quazepam
Preanesthetics
Diazepam - Midazolam
Mechanism of Action
Slower absorption
e.g. lorazepam & oxazepam, temazepam (LOT)
Can be given parenterally
Chlordiazepoxide - Diazepam (IV only NOT IM)
Lorazepam - Midazolam (IV or IM)
Bzs are widely distributed.
Cross placental barrier during pregnancy
and are excreted in milk (Fetal & neonatal
depression).
Redistribution from CNS to skeletal muscles,
adipose tissue) (termination of action).
All benzodiazepines are metabolized in the
liver to active compounds
Anxiolytic action.
Depression of cognitive and psychomotor function.
o Liver disease
o Old people.
Precautions
Side Effects
Nausea
Dizziness
Imidazopyridine derivative.
Acts on benzodiazepine receptors (BZ 1) &
facilitate GABA mediated neuronal inhibition.
Its action is antagonized by flumazenil.
Rapidly absorbed from GIT and metabolized to
inactive metabolites via liver CYT P450.
Short duration of action ( 2- 4 h).
has no muscle relaxant effect.
has no anticonvulsant effect.
Minimal psychomotor dysfunction
Minimal tolerance & dependence.
Minimal rebound insomnia.
Its efficacy is similar to benzodiazepines.
Minor effect on sleep pattern, but high
doses suppress REM.
Respiratory depression occur at high doses in
combination with other CNS depressant as
ethanol.
Adverse Effects
Dizziness
GIT upset
Drowsiness
Uses
a hypnotic drug for short term treatment of
insomnia.
Drug Interactions
Inducers
Rifampicin, phenytoin, carbamazepine
Inhibitors
Cimetidine, erythromycin
Zaleplon
Binds to BZs receptors and facilitate GABA
actions.
Rapid absorption
Short onset of action
Short duration of action (1 hr)
Metabolized by liver microsomal enzymes
CYP3A4
Metabolism is inhibited by cimetidine.
Decreases sleep latency
Little effect on sleep pattern
Potentiates action of other CNS depressants
(alcohol).
Dose reduction as before.
Used as hypnotic drug
Advantages
Less impairment of pyschomotor and
cognitive functions than BZs or zolpidem.
5HT1A agonists
Buspirone