Propofol

Physical & Chemical Properties:

• Class: Non Barbiturate
• Chemical name as 2,6 di-isopropylphenol.
• Available as 1% and 2% milky white solution.
• It is lipid soluble & water insoluble
• Composition:
• Egg lecithin(1.2%) + Glycerol(2.25%) + Soyabean Oil(10%).
• (Oil based is painful. Therefore injection of propofol should be
preceded or mixed with lignocaine.)
• Fospropofol is a water-based preparation but not widely available.
• As egg is a good media for bacterial growth, chances
of contamination of opened vial are very high.
• In fact, there have been death reports following the use
of contaminated solution of propofol.
• Although the recent formulations of propofol contains
antimicrobial agents like disodium edetate or sodium
metabisulfite but they also does not guarantee
immunity against contamination therefore after
opening it is mandatory to discard the Propofol vial
within 6 hours.
 Mechanism of action:
i. Stimulate GABA (inhibitory neurotransmitter)
ii. Inhibit glycine receptors
iii. Inhibit 5HT receptors (explains its antiemetic effects)

Propofol binds to ꞵ subunit of GABA-A receptor & ᵧ2 subunit also

contribute to modulatory effects of propofol on GABA-A.
Prevents dissociation of GABA from the receptor
This causes prolonged activation of the receptor . Chloride influx
occurs as a result causing hyperpolarization & inhibition of post
synaptic neurons.
Pharmacokinetics: Induction is achieved in one arm brain
circulation time, i.e. 15 seconds. Consciousness is regained after
2-8 minutes due to rapid redistribution.
Elimination half-life is 2-4 hours; recovery is rapid and
associated with less hangover than thiopentone.
Dose: 1.5-2.5 mg/kg
Route: iv
Metabolism: Mainly metabolized in liver but significant (30%)
extrahepatic metabolism also occurs in kidneys. A part of
Propofol is also metabolized in lungs. Clearance rate is 10 times
more rapid than thiopentone therefore recovery is rapid. All
metabolic products of propofol are inactive.
 Systemic effects
CVS Hypotension followed by Bradycardia
RESPI Apnea (Higher incidence 25-30%)
Bronchodilation in COPD patients
Depresses upper airway reflexes (preferred for surgeries done
under LMA without muscle relaxant)
CNS Loss of consciousness, Anticonvulsant but Grand mal epilepsy
have been reported in few cases
ICP & CMR
EYE IOP
GIT Antiemetic ((even more effective than ondansetron for
postoperative nausea and vomiting)
IMMUNOLOGIC Antipruiritic (can be used for the treatment of cholestatic
pruritus)
 Uses
l. Because of its shorter half life it is the agent of choice for
induction.
2. Because of its early and smooth recovery, inactive
metabolites and antiemetic effects it is the iv agent of choice
for day care surgery.
3. Along with opioids (Remifemanil) propofol is the agent of
choice for total intravenous anesthesia (TIVA).
4. Propofol infusion can be used to produce sedation in ICU.
5. It is the agent of choice for induction in susceptible
individuals for malignant hyperthermia.
 Antiemetic Cardiovascular
Antipruiritic stability

Advantages

Rapid & Smooth

Bronchodilator recovery, Early
Ambulatory(4hrs)
 Disadvantages:
Apnea Less stability of Increased risk of
solution (<6hrs) aspiration because of
inhibition of airway
reflexes
Hypotensi Expensive Addiction (since it
on raises Dopamine level)
Painful Chances of sepsis with Propoful Infusion
contaminated solution Syndrome
is high
 Propofol Infusion Syndrome:
• It is rare but is a lethal complication.
• It is usually seen if propofol infusion is continued for more than
48 hours.
• More common in children.
• It occurs because of the failure of free fatty acid metabolism
caused by propofol.
• It is associated with severe metabolic acidosis (lactic acidosis),
acute cardiac failure, cardiomyopathy, skeletal myopathy,
hyperkalemia, lipemia and hepatomegaly.
 Obstetrics:
Contrary to past, can be
Shock used since induction dose
doesn’t affect APGAR.

Contraindications

Egg/Soy Allergy: can safely

Children: receive Propofol.
Not recommended for long Since egg allergy id due to
term infusion in children egg white (albumin) not
<16 Years lecithin (which is prepared
from yolk)
 References:
- Short textbook of Anesthesia by Ajay Yadav – 6th Edition

- Thank You