2. PROPOFOL
Introduction: Propofol is an intravenous sedative-
hypnotic that was introduced for clinical use in 1977.
Since the introduction of propofol into cliical practice,
it has become the intravenous induction agents
include rapid induction of general anaesthesia.
3. Pharmacology: Propofol is commonly used for
conscious sedation, as an anaesthetic indiction agent
for the maintenance of general anaesthesia.
Propofol is a subsituted iso-propyl-phenol formulated
as a 1% aqueous solution. The propofol emulsion
formulation contain soybean oil, glycesol & egg
lecithin.
5. Mechanism of action
The mechanism of action of propofol is related to its
interaction with ‘gamma aminobutyric’ acid (GABA)
which is the principle inhibitory neurotransmitter in
the CNS.
Propofol works by increasing GABA mediated
inhibitory tone in the CNS.
Propofol decrease the rate of dissociation of the GABA
from the receptor, thereby increasing the duration of
GABA activated opening of the chloride channel
resulting hyperpolarization of the cell membrane.
6. Mechanism of Action
Propofol Activation of GABA receptor
Increase transmembrane cl conductance
Hyperpolarization of post synaptic membrane
Functional inhibition of the post synaptic membrane.
8. Pharmacokinetics
Bioavailability: N/A
Protein binding: 95%-99%
Metabolism: Liver
Onset of action: 15-30 seconds
Biological half life: 30-60 min
Duration of action: 5-10 min
Excretion: Liver
9. Indication
Starting or maintaining anaesthesia during certain
surgeries, tests or procedure.
Used for sedation.
ICU patients and mechanically ventilated patients.
Bronchodilation.
10. Contraindication
Hypersensityvity to propofol which contain: soybean
oil, egg or egg product.
Obsterical procedures.
It is not recommended for use in nursing mothers.
It is not recommended for anaesthesia in children
below the age of 3 yrs.
11. Interactions
Halothane, enflurane, isoflurane drug.
Narcotic drug such as: morphine, meperidine
Doxylamine drugs
Clonazepam drugs
Antidepressant such as:
amoxapine
amitriptyline
doxepin
Barbiturates such as:
pentobarbital
secobarbital
12. Side effects
Nausea
Cough
Burning or stining around the IV needle.
Itching or skin rash
Numbness or tingly feeling
Confusion
Agitation
Anxiety
Muscle pain
Discolored urine
13. Brand name in BangladeshBrand name Contains Dosage
form
Manufacture
POFOL I.V Propofol 10mg/ml I.V
injection
Popular
pharmaceuticals
FRESOFOL Propofol 10mg/ml I.V
injection
Fresenius kabi/HYE
impex international
RECOFOL Propofol 10mg/ml I.V
injection
Bayer Schering
oy/Tajarat
14. Doses
Usual adult dose for anaesthesia: Less
than 55 years:
Anaesthetic induction: 40 mg IV every 10 seconds until
induction onset.
Maintenance of Anaesthesia: IV infusion 100 to 200
mcg/kg/min.
cardiac anaesthesia:
Induction : 20 mg every 10 second until induction onset.
Maintenance: 100-150 mcg/kg/min
15. ICU sedation: initial continuous IV: 5mcg/kg/min
Maintenance: 5 to 50 mcg/kg/min.
Usual pediatric dose for anaesthesia:
3 to 16 years : Induction: 2.5 to 3.5 mg/kg over 20 to 30
second.
Maintenance: 125 to 300 mcg/kg/min.