Friday 8 April 2016

Benzodiazepines | Crack PGIMER 22 MAY 2016


Which is true regarding benzodiazepines

A. GABA agonist
B. Diazepam isa short acting benzodiazepine
C. Diazepam causes lesser respiratory depression
D. Nitrazepam is metabolized in liver
E. Diazepam has higher abuse potential than Midazolam


The Answer is. (C) Diazepam causes lesser respiratory depression (D) Nitrazepam is metabolized in liver
•Benzodiazepines act on BZD receptors of GABA-BZD receptor-chloride channel complex, modulates BID receptors, increases the frequency of Cl Channel opening induced by submaximal concentration of GABA. Thus it is not GABA agonist, it is GABA facilitatory but no mimetic action
• Coma, respiratory depression though rare, can occur with ultra short acting agents-Like Midazolam, Triazolam
• The dependence producing liability of BZDs is low. They are rarely used
• Agents that are absorbed rapidly and are lipid soluble such as diazepam, have rapid onset of action and higher abuse potential
• Midazolam; extremely rapid absorption ; more liable for abuse
• Diazepam has rapid onset of action
• Benzodiazepines are metabolised in liver by dealkylation and hydroxylation

Note: Diazepam undergoes entero hepatic circulation