Pharm Benzos Flashcards
Names of benzos
Librium Diazepam Serax Lorazepam Midazolam-1976
Moa benzos
Activation of GABAA receptor complex and enhancement of gaba mediated chloride currents
Neurons hyper polarized and less excitable
GABA continues to bind and is needed to work
Benzo that has best affinity and efficacy
Midazolam
Benzo moa almost exclusively on post synaptic nerve endings in CNS, the greatest density is in the?
Cerebral cortex,
Effects of benzos with corresponding area of brain
Anxiolytic- amygdala, hippocampus, límbico áreas
Sedation- brain stem and cortical receptors
Anticonvulsant
Muscle relaxation- spinal cord
Amnesia-forebrain and hippocampus
Benzos vs barbs
Less tolerance Less abuse potential Greater margin of safety against overdose Fewer and less dig drug interactions Do not induce enzymes
Less tolerance?
Not sure if true, data from pt reported
Imidazole ring at pH 4?
Basic formulation water soluble, does not require lipid vehicle(like propofol)
Open ring
Imidazole ring at pH of body
Ring closes and midazolam becomes lipophilic
Despite rapid passage into the brain, midazolam has a ______ effect site equilibrium. _______ protein bound.
Slower, highly
Benzo CNS effects
Decrease CMRO2 and CBF(lesser extent than barbs)
Cannot produce isoelectric (flat) eeg
Little to no change in icp
Potent anticonvulsant
Paradoxical excitement occurs in <1% of pts receiving versed
Cv system effects
Dose dependent decrease in systemic blood pressure
CO is not changed ( why no change in ICP)
BP response d/t decrease SVR
Does not prevent sympathetic response with intubation
Respiratory effects benzos
Minimal, does dependent decrease in ventilation
Decrease in vent response to co2(effect chemoreceptors)
Transient apnea after rapid IV dose(synergistic and additive with opioids) worst with sleep apnea
Depression of swallowing reflex
Decrease in upper airway activity
Side effect benzo
Allergic reactions- extremely rare
Anterograde amnesia
Ativan infusions not recommended d/t propylene glycol cause cardiovascular complications
Over sedation SLEEP NOT RESTORATIVE
Cause for pain on injection of diazepam and Ativan
Propylene glycol solvent