Propofol properties:
Lipid emulsion with pH of 7-8.5
Has Disodium edetate - preservative to inhibit bacterial and fungal growth
Generic prop contains what?
Sodium metabisulfite or benzyl alcohol - both preservatives to inhibit bacterial and fungal growth
What can sodium metabisulfite cause?
Allergic reaction specifically in patients w asthma
Opened syringes of prop should be discarded within___
6 hrs
Prop MOA:
GABAa receptor activation - causes Cl- to enter the cell resulting in hyperpolarization –> decreases action potential
Propofol DIRECTLY stimulates gaba (GABA MIMETIC) and causes increase in Cl in cell inhibits AP’s
Prop pharmacokinetics: Onset/duration
Distributes rapidly to brain (VRG)
Onset - 5-30 seconds
Rapid redistribution - duration of action 5-15m
prop pharmakokinetics Metabolism
In liver by CYP2B6, UFTHP4, CYP2C6
HIGHLY PROTEIN BOUND (98%)
- If given to patient plasma protein levels may increase increase the free active fraction and in turn increase effects
Elim half likfe - 1-2hrs
Prop Pharmacodynamics in brain
Decreases CBF, CMRO2, ICP, CPP
DUE TO decrease in MAP, metabolic rate, cerebral vasoconstriction
Prop dynamics CV
Decreases sympathetic tone and vasodilates –> lowers BP
Predictors - ASA III + IV
Age >50 - REDUCTION in dose by 50% in elderly over 80
Baseline MAP <70mmHG
Coadministration with fentanyl
Prop Respiratory dynamics:
DECREASE Tv
Minimal bronchodilating effect
Apnea - based on dose, speed of injection, patient characteristics and other resp. depressants
Prop other systems dynamics:
-Antiemetic effect - due to decreases in serotonin levels
Antipruritic effect
Pain on injection - reduced by Lidocaine 20-40mg pre-injection AND use of antecubital vein (Larger vein)
PROP numbers:
Induction Dose: 1-2mg/kg
Onset: 5-30 seconds
DOA: 5-15 mins
Elim half life: 1-2Hrs
Coadministration of prop with ____ can cause increase in propofol concentrations:
Midazolam - may also decrease metabolic clearance
Etomidate MOA:
GABA mimetic
Etomidate pharmacokinetics:
Lipid soluble
Distributes rapidly to brain and VRG - Onset - 5-30 seconds
Rapid redistribution - DOA - 5-15min
76% protein bound
Metabolized in liver by hepatic enzymes AND PLasma esterase - ester hydrolysis
Elim half life - 2-5 hours
CNS dynamics of etomidate:
Dose depenent CNS depression
Decreased CBF, ICP, CMRO2
CPP Remains the same - due to no decreases in MAP with adminstration (see cardiovascular effects)
Causes MYOCLONIA - sudden, generalized, asynchronous muscle contractions
Etomidate dynamics CV:
Hemodynamic stability when compared to prop - no sign. changes in HR, PAP, CI, SVR, SBP
ACTS as an agonist at alpha2 adrenoreceptors which can increase blood pressure
Etomidate dynamics respiratory:
Dose-dependent resp. depression
Decrease in MV, RR
Can cause apnea
Etomidate and adrenal gland:
Cause suppression of plasma cortisol for up to 24 hours after induction dose of etomidate due to inhibition of 11bhydroxylase enzyme
NEED to take caution when giving to septic patients
Septic patients - have adrenal insufficiency 2-3 times as long as nonseptic patients
Etomidate may increase mortality
Adverse effects of etomidate:
Myoclonia
Pain on injection (90%) d/t prop glycol
N/V (30-40%)
Contraindications of etomidate:
known sensitivity
Adrenal suppression
Acute porphyria
Etomidate numbers:
Induction dose: 0.2-0.3mg/kg
Onset: 5-30s
DOA: 5-15m
Elim halflife: 2-5hrs
Ketamine MOA:
Water soluble w a pH of 3.5-5.5
Class: Phencyclidine derivative
NMDA Antagonist - selective depression of afferent signals of pain perception to thalamus and cortex
Blocks GLUTAMATE from binding to receptor and causing rapid influx of NA, CA, and K
What is ketamine helpful in preventing?
Opioid induced hyperalgesia