Level 1

- Imidazole ring in its structure - Accounts for water solubility And rapid metabolism
- 2-3x potent Diazepam

Clear solution pH 3.5 (IV/IM), Tablet
pKa 6.5 – 89% un-ionized

increases the sensitivity GABAA receptors which open (via GABA) and allow Cl influx
causing hyperpolarisation
- Influx of Cl- into nerve cell
- Hyperpolarised, preventing conduction

CNS: Sedative, reduces epileptiform activity,
increases confusion and disorientation, amnesic properties more prominent than
sedative eff¬ects
CVS: minor hypotension has been reported

Resp: respiratory depression - synergistic with opioids

A : IV,PO,In,IM
poor oral bioavailability 45%

hepatic via CYP3A4, and glucuronidation
active metabolite

excreted in urine (as glucuronide conjugated metabolites)

half life 1-4 hrs
prolonged in cirrhosis, CRF, CCF, obesity, elderly

2-2.5mg initially then 1mg boluses to eff¬ect

- Benzodiazepine
- Imidazole ring in its structure - Accounts for water solubility And rapid metabolism
- 2-3x potent Diazepam

Sedative, amnesic+ anxiolytic,
antiepileptic

lipid soluble at physiological pH (pKa 6.5).
high lipid sol crosses BBB

Anticonvulsant
Sedative-Hypnotic

Respiratory depression and excessive sedation with overdosage
Same CYP as alfentanil (increases effect)

highly protein bound (95%)

small-mod Vd = 1-2 L/kg
high lipid sol crosses BBB

Sedative / Hypnotic

Respiratory depression and excessive sedation with overdosage
Same CYP as alfentanil (increases e¬ffect)

95%

1-2 L/kg