Level 1

Benzodiazepine

1. in the short-term treatment of anxiety
2. in the treatment of status epilepticus
3. for muscle spasm in tetanus and other spastic conditions
4. for alcohol withdrawal, and for
5. premedication and
6. sedation during endoscopy and procedures performed under local
anaesthesia.

Solution: Clear, yellow solution and as a white oil-in-water emulsion for injection
containing 5 mg/ml.

Tab: 2/5/10 mg
Syrup: 0.4/1 mg/ml
Supp: 10 mg

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

Diazepam has kappa-opioid agonist activity in vitro, which may explain the
mechanism of benzodiazepine-induced spinal analgesia

CVS A transient decrease in the blood pressure and a slight decrease in
the cardiac output may occur, following the intravenous administration of
diazepam. The coronary blood flow is increased, secondary to coronary
arterial vasodilation; a decrease in myocardial oxygen consumption has also
been reported.
RS Large doses cause respiratory depression; hypoxic drive is depressed to
a greater degree than is hypercarbic drive.DIAzEPAM 101
CNS Diazepam is anxiolytic and decreases aggression, although paradoxical
excitement may occur. sedation, hypnosis, and anterograde amnesia occur
after the administration of diazepam. The drug has anticonvulsant and analgesic properties, and depresses spinal reflexes.

Depression of the CNs, including drowsiness,
ataxia, and headache, may complicate the use of diazepam. Rashes, gastrointestinal upsets, and urinary retention have also been reported. Tolerance
and dependence may occur with prolonged use of benzodiazepines; acute
withdrawal of benzodiazepines in these circumstances may produce insomnia, anxiety, confusion, psychosis, and perceptual disturbances. Intravenous
diazepam is highly irritant to veins; the oil-in-water preparation is less so.

Diazepam is rapidly absorbed after oral administration; the bioavailability is 86–100%. Absorption after intramuscular administration is
slow and erratic.

99%

0.8–1.4 l/kg

Hepatic to active metabolites.

Major metabolite is desmethyldiazepam (half life 100hrs). other metabolites are oxazepam
(which is further metabolized by glucuronidation) and temazepam.

urine as oxidized and
glucuronide derivatives; <1% is excreted unchanged.

elimination half-life is 20–40 hours.

- potentiates non-depolarizing muscle relaxants.
- adsorbed onto plastic
- not removed by dialysis.

The adult oral dose is 2–60 mg/day
in divided doses; the initial intravenous dose is 10–20 mg, increasing according to clinical effect.

Sedative / Hypnotic
Benzodiazepine

Sedative / Hypnotic