Propofol

hh

1. Made by
RaselMahbub
Dept.Ofpharmacy
JagannathUniversity
01915923493

2. PROPOFOL
Introduction: Propofolis an intravenous sedative-
hypnotic that was introduced for clinical use in 1977.
Since the introduction of propofolinto cliicalpractice,
it has become the intravenous induction agents
include rapid induction of general anaesthesia.

3. Pharmacology: Propofolis commonly used for
conscious sedation, as an anaestheticindictionagent
for the maintenance of general anaesthesia.
Propofolis a subsitutediso-propyl-phenol formulated
as a 1% aqueous solution. The propofolemulsion
formulation contain soybean oil, glycesol& egg
lecithin.

4. Structure: Propofol

5. Mechanism of action
The mechanism of action of propofolis related to its
interaction with ‘gamma aminobutyric’ acid (GABA)
which is the principle inhibitory neurotransmitter in
the CNS.
Propofolworks by increasing GABA mediated
inhibitory tone in the CNS.
Propofoldecrease the rate of dissociation of the GABA
from the receptor, thereby increasing the duration of
GABA activated opening of the chloride channel
resulting hyperpolarizationof the cell membrane.

6. Mechanism of Action
Propofol Activation of GABA receptor
Increase transmembraneclconductance
Hyperpolarizationof post synaptic membrane
Functional inhibition of the post synaptic membrane.

7. Mechanism of Action

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 anaesthesiaduring certain
surgeries, tests or procedure.
Used for sedation.
ICU patients and mechanically ventilated patients.
Bronchodilation.

10. Contraindication
Hypersensityvityto propofolwhich contain: soybean
oil, egg or egg product.
Obstericalprocedures.
It is not recommended for use in nursing mothers.
It is not recommended for anaesthesiain children
below the age of 3 yrs.

11. Interactions
Halothane, enflurane, isofluranedrug.
Narcotic drug such as: morphine, meperidine
Doxylaminedrugs
Clonazepamdrugs
Antidepressant such as:
 amoxapine
 amitriptyline
 doxepin
Barbiturates such as:
 pentobarbital
 secobarbital

12. Side effects
Nausea
Cough
Burning or stiningaround the IV needle.
Itching or skin rash
Numbness or tingly feeling
Confusion
Agitation
Anxiety
Muscle pain
Discolored urine

13. Brand name in Bangladesh
Brand name Contains Dosage
form
Manufacture
POFOLI.V Propofol10mg/ml I.V
injection
Popular
pharmaceuticals
FRESOFOL Propofol10mg/ml I.V
injection
Freseniuskabi/HYE
impexinternational
RECOFOL Propofol10mg/ml I.V
injection
Bayer Schering
oy/Tajarat

14. Doses
Usual adult dose for anaesthesia: Less
than 55 years:
Anaestheticinduction: 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.