Diazepam Flashcards
Brand Name
Valium
Class
Benzo
Structure
Benzene ring fused w/ 7 member diazepine ring
mechanism of action
potentiates binding of GABA to the GABA-A receptor, keeping the Cl- channels open and hyperpolarizing the cell, making it resistant to excitation
pharmacokinetics PB Lipid solubility VD elimination
highly PB highly lipid soluble large VD (0.7-1.7L/Kg) rapidly crossed BBB and placenta elimination - conjugated CYP450, excreted urine
pharmacokinetics
onset
doa
T1/2
onset - 30-60 sec
doa - prolonged
T1/2 - 21-37 hrs
active metabolite
desmethyldiazepam
most active, lasts 48-96 hrs
side effects
lowers CBF & CMRO2
does not cause isoelectric EEG
preserves CO2 response but flattens curve
neuroprotective
lowers SVR, BP, CO with induction dose
dose dependent decrease in RR and TV
does NOT attenuate SNS response to DVL
can cause hypersensitivity and paradoxical excitation
contraindications
early pregnancy
decrease dose for hepatic/renal impairment
use with caution in elderly (increased sensitivity)
DO NOT give with glaucoma
dose
pre-med 0.2 mg/kg IV; 10-15 mg PO
induction: 0.5-1 mg/kg IV
other
least potent benzo
pain on injection (propylene glycol)
does not effect NMB dose