Propofol
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Propofol (brand name Diprovan): an intravenous
anesthetic used to produce rapid induction of anesthesia with
a rapid emergence and with relatively low incidence of post-operative
nausea and vomiting.
Propofol is classified as a sedative-hypnotic and has become the
induction drug of choice for many procedures due to its rapid
induction, clearance, and low incidence of nausea compared to
other IV anesthetics. It is thought to act by interacting with
gamma-aminobutyric acid (GABA) and decreasing GABA’s rate
of disassociation from GABA-activated chloride ion channels, thereby
hyperpolarizing the cells and preventing further signaling. Potential
side effects may include decreases in blood pressure, heart rate,
respiratory rate, and cerebral blood flow. In addition, a sensation
of pain at the site of intravenous administration is a common
occurrence. Dosage is usually between 1.5 to 2.5 mg/kg IV and
unconsciousness (as established by unresponsiveness) is achieved
within 30 seconds to two minutes. Propofol does cross the placenta
but is quickly cleared from neonatal circulation. Propofol may
also be used as a continuously infused sedative during mechanical
ventilation in critically ill patients.
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Diprivan is a short-acting intravenous anesthetic
agent used for the induction of general anesthesia in adult patients and
pediatric patients older than 3 years of age; maintenance of general anesthesia
in adult patients and pediatric patients older than 2 months of age; and
intensive care unit (ICU) sedation for intubated, mechanically ventilated
adults.
Diprivan is approved for the induction and maintenance of anesthesia
in more than 50 countries.
Initial clinical trials were in 1977, in a form solubilised in cremophor
EL, but due to anaphylactic reactions it was withdrawn from the market.
It was subsequently reformulated as an aqueous emulsion in intralipid
and re-launched in 1986 by AstraZeneca with the brand name Diprivan
(Sometimes Diprovan). The current preparation is 1% Diprivan solubilised
with 2.25% glycerol, 10% soybean oil and 1.2% purified egg phospholipid,
and has a pH between 6.0 and 8.5 and a pKa of 11. Diprivan contains
EDTA as an antimicrobial agent. Newer generic formulations contain sodium
metabisulfite or benzyl alcohol. Diprivan is one of the few commonly-used
anesthetic drugs which can easily be identified by sight alone; it appears
as a highly opaque white fluid whereas nearly all other anesthetics
are clear and resemble water.
It is highly protein bound in vivo and is metabolised by conjugation
in the liver. Its rate of clearance exceeds hepatic blood flow, suggesting
an extrahepatic site of elimination as well. Its mechanism of action
is uncertain, but it is postulated that its primary effect may be at
the GABA-A receptor.
Aside from the hypotension and transient apnea following induction
doses, one of its most frequent side-effects is pain on injection, especially
in smaller veins. This pain can be mitigated by pretreatment or mixing
with intravenous lidocaine. Alternative formulations with a larger proportion
of medium-chain triglycerides (as opposed to Intralipid) appear to have
less pain on injection, possibly due to lower concentrations of free
aqueous Diprovan.
It appears to be safe for use in porphyria, and has not been known
to trigger malignant hyperpyrexia. The elimination half-life of Diprivan
has been estimated to be between 2-24 hours. However, its duration of
clinical effect is much shorter because Diprivan is rapidly distributed
into peripheral tissues.
source: wikipedia.org
common misspellings: diprovan, deprivan, deprovan, dipravan, dapravan, daprivan, dipervan, dipirvan, diprivin, dipravin, diprovin, dipriven, dipraven, propifil, propofil, pripofol, propafol, propafil, propophol
