Diazepam remains a popular oral drug for preoperative medication of adults and is the benzodiazepine most likely to be selected for management of delirium tremens and treatment of local anesthetic induced seizures. This is considered to be one of the diazepam uses that are very common. Production of skeletal muscle relaxation by diazepam is often […]
Diazepam effects produce minimal depressant effects on ventilation with 0.2 mg/kg IV dose in Respiration system. The slight increase in PaCO2 is due primarily to a decrease in tidal volume. Nevertheless, nearly, small doses of diazepam (<10 mg IV) have produced apnoea. Combination of diazepam with other CNS depressants (opioids, alcohol) or administration of this
Diazepam metabolism is carried out by hepatic microsomal enzymes using an oxidative pathway of N-demethylation with the production of desmethyldiazepam, oxazepam, and to a lesser extent temazepam as metabolites. Desmethyl diazepam is metabolized more slowly than oxazepam and is only slightly less potent than diazepam. These metabolites contribute to the sustained effect of diazepam. The
Diazepam half life could be observed during rapid absorption from the gastrointestinal tract after oral administration, reaching peak concentrations in about 1 hour in adults and within 15 to 30 minutes in children. There is rapid uptake of diazepam into the brain, followed by redistribution to inactive tissue sites. The Vd of diazepam is large,
The sedative effect of benzodiazepines and opiods is potentiated by other CNS depressants including alcohol, barbiturates, inhaled and injected anesthetics, and opioids. Anesthetic requirements for inhaled and injected anesthetics are decreased by benzodiazepines and opiods . Benzodiazepines decrease the MAC value of inhaled anesthetics. Benzodiazepines, especially midazolam, potentiate the ventilatory depressant effects of opioids, though
Benzodiazepine half life is commonly administered through oral, intramuscular and intravenous routes. Intramuscular absorption of diazepam is erratic, whereas midazolam and benzodiazepine half life have good bioavailability through this route. Diazepam and lorazepam are well absorbed from gastrointestinal tract. However, meals and antacids may decrease absorption from the gastrointestinal tract. Midazolam has also been used
The sedative effects of benzodiazepine receptors are due to activation of α-1 subunits of GABA receptors. The anxiolytic activity associated with the benzodiazepine is due to α-2 subunit activity. The GABAA receptor is large, providing attachment sites for GABA, benzodiazepines, barbiturates, etomidate, propofol, and alcohol. This property explains the pharmacologic synergy of these substances and
Benzodiazepines uses are many. Preoperative medication for anxiolysis and sedation is one where it finds its usage. Midazolam has replaced diazepam as the most commonly administered benzodiazepine in the preoperative period for preoperative medication and intravenous (IV) sedation. Furthermore, the context-sensitive half-times for diazepam and lorazepam are prolonged; and so they are used where prompt
Among the common benzodiazepines that are used in anesthesia today are three: namely diazepam, midazolam and lorazepam. Benzodiazepines produce varying degree of anxiolysis, sedation, anticonvulsant actions and anterograde amnesia. Benzodiazepines also produce some degree of skeletal muscle relaxation but that is not sufficient for surgical procedures; and they also do not decrease the dose requirements
Benzodiazepines effects appear to produce all their pharmacologic effects by facilitating the actions of gamma-amino butyric acid (GABA). The area where it causes it effect is the principal inhibitory neurotransmitter in the CNS by enhancing their affinity towards GABA receptors leading to increased chloride conductance and hyperpolarization of the postsynaptic cell membrane, and thereby rendering
