Barbiturates Flashcards
Barbiturates Mechanism of Action
Interaction with GABA A (alpha subunit) receptor, directly activate chloride ion channels, increasing their duration of opening (increases efficacy of GABA), hyperpolarization of postsynaptic cell membranes, also blocks AMPA receptor (glutamate)
Barbiturates Protein Binding
83%
Barbiturates Lipid Solubility
High - rapid into CNS, uptake in 30 seconds & prompt awakening after single dose
Barbiturates Metabolism
Hepatic
Barbiturates Excretion
Renal
Barbiturates CV Effects
Decrease: SBP, CO & SVR - cardiac depression & increased venous capacitance, Increase: HR (rebound)
Barbiturates Pulmonary Effects
Respiratory depression, apnea, return with slow RR & tidal volume
Barbiturates CNS Effects
Decrease: CBF, ICP, CMRO2
Barbiturates Renal
Modest decrease in blood flow & GFR
Barbiturates pH effects
Metabolic acidosis increase effects, metabolic alkalosis decreases effects of barbs, & respiratory acidosis has much less effect
Thiopental supplied as
25 mg/mL
Methohexital supplied as
10 mg/mL
Induction dose of thiopental
3-5 mg/kg
Induction dose of methohexital
1-1.5 mg/kg (20-30mg/kg rectal)
Barbiturates Be aware of
May cause hyperalgesia, can cause histamine release, Extravasation causes tissue sloughing, do not mix with succ (will make “concrete”), intraarterial injection causes severe vasoconstriction, induces the P450 system, contraindicated in patients with acute intermittent porphyria