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Intravenous anaesthetic-hypnotic drugs Propofol Pentothal ...

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25/11/2010<br />

GABA A Receptor<br />

• Transmembrane<br />

pentamer composed of 2<br />

α, 2 β, and 1 γ or δ<br />

subunits<br />

• Each has a binding site for<br />

GABA<br />

• Benzodiazepines<br />

• Bind a cleft of α and γ<br />

subunits<br />

• Increases frequency of<br />

channel opening<br />

• Barbiturates, (propofol)<br />

• Bind α subunit<br />

• Increase duration of<br />

channel opening<br />

• Agonist: muscimol<br />

• Antagonist: bicuculine<br />

<strong>Propofol</strong> / Characteristics (1)<br />

1. 2,6-diisopropylphenol is used for induction and<br />

maintenance of general anaesthesia.<br />

2. It is prepared as a 1% or 2% isotonic oil-in-water<br />

emulsion, which contains egg lecithin, glycerol,<br />

and soybean oil.<br />

3. Bacterial growth is inhibited by either ethylenediaminetetraacetic<br />

acid or sulfite.<br />

4. Mode of action: Increases activity at inhibitory<br />

γ-aminobutyric acid (GABA) synapses.<br />

5

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