Brand Name
Diprivan
General Therapeutic Class
IV anesthetic
Sedative/Hypnotic
Pharmacological / Chemical Class
Alkylphenol Derivative
MOA
Binds to Beta subunits (Beta-2 and Beta-3) allosterically on postsynaptic GABA-A receptor increasing affinity of endogenous GABA to the receptor resulting in increased Chloride conductance and hyperpolarization. It increases the duration and frequency of channel opening resulting in hypnosis, immobility, and amnesia. In higher doses it may bind directly to GABA-A
Uses
TIVA
Induction
Antiemetic qualities
Outpatient surgery
Endoscopy
MAC (sedation)
ICU sedation
Contraindications?
Known anaphylactic reaction to Eggs/Soy/propofol
Precautions
Hypovolemic state, Trauma, shock, severe hemodynamic instability
Lipid metabolism disorders
CV disease
Volume of distribution
Very large
Effect of Volume of distribution on desired effect
Rapidly redistributes (offset)
Context sensitive half-life for infusions up to 8 hours?
Approximately 40 mins (ideal)
Cardiac effects
decreased contractility
Therefore decreased CO
Vascular effects
Decreased Preload
Decreased SVR
Decreased BP/MAP
CNS effects
Decreased CBF
Decreased ICP
Decreased CMRO2
Antiemetic effects
Neuroprotective (increases seizure threshold)
Resp effects
results in hypoventilation and apnea (Dose dependent)
Decreases Hypoxic and Hypercapnic drive
Pain on injection?
Yes, likely due to kinin system; Pretreat with lidocaine
Other adverse effects?
PRIS
dosing > 5mg/kg/hr for 48 hours
Rhabdo, hyperkalemia, hypertriglyceremia, end organ damage (Renal, Cardiac)
Histamine Release?
No
Allergic reactions?
Not clinically seen; contraindicated if known anaphylactic reaction to drug, generic (sulfa), egg lethicin/soy lethicin
Induction Dose
1-2.5 mg/kg
Sedation (MAC) dose
25-75 mcg/kg/min
General anesthesia maintenance infusion dose
100-200 mcg/kg/min
Onset
30 seconds due to high lipophilicity and rapid distribution to VRO
Duration
Dose dependent
5-15 mins
Dosing Adjustments: Elderly
less