Used for intravenous infusion for procedural sedation.
A sedative without analgesic properties.
A gamma-aminobutyric acid receptor modulator.
May accumulate unpredictably.
High dose or prolonged use may lead to the potentially fatal porpofol infusion syndrome.
When used for endoscopy procedures reduces procedural recovery times, improves procedure throughput and increases the efficiency of endoscopy units.
Has been associated with seizures, and brief agitation.
Propofol
A short-acting medication that results in a decreased level of consciousness and lack of memory for events.
Marketed as Diprivan.
It is used for starting and maintenance of general anesthesia, sedation for mechanically ventilated adults, and procedural sedation.
It is used for induction and maintenance, and in some cases, of general anesthesia, having largely replaced sodium thiopental.
Can also be administered as part of an anaesthesia maintenance, called total intravenous anesthesia using either manually-programmed infusion pumps or computer-controlled infusion pumps in a process called target controlled infusion
It is also used for status epilepticus if other medications have not worked.
Administered by injection into a vein.
Maximum effect takes about two minutes to occur and it typically lasts five to ten minutes.
Pregnancy category US: B (No risk in non-human studies)
Protein binding 95–99%.
Metabolism is by liver glucuronidation.
Onset of action 15–30 seconds.
Elimination half-life 1.5–31 hours.
Duration of action 5–10 minutes.
Excretion by liver
Common side effects include: irregular heart rate, low blood pressure, burning sensation at the site of injection, and the stoppage of breathing.
Serious side effects may include seizures, addiction, and propofol infusion syndrome with long-term use.
It appears to be safe for using during pregnancy.
It is not recommended during cesarean section.
Not a pain medication.
Can be used with opioids.
Works, at least, partly via a receptor for GABA.
Can be used to sedate individuals who are receiving mechanical ventilation but are not undergoing surgery, such as patients in the intensive care unit.
In the critically ill patients, it is superior to lorazepam both in effectiveness and overall cost.
Recovery from propofol is more rapid than sodium thiopental for starting anesthesia.
Use in procedural sedation results in a faster recovery compared to midazolam.
Widely used for sedation of infants and children undergoing MRI, because of its fast induction and recovery time.
It can also be combined with opioids or benzodiazepines, and ketamine.
Recreational use by self-administration is relatively rare due to its potency and the level of monitoring required for safe use, and steep dose-response curve makes recreational use of propofol very dangerous, and deaths are reported.
Recreational use provides short term effects include mild euphoria, hallucinations, and disinhibition.
Long-term use can result in addiction.
Intravenous injection is associated with pain, especially in smaller veins.
Activation of the pain receptor, TRPA, found on sensory nerves causes the pain and can be mitigated by pretreatment with lidocaine.
There is great variability in individuals response to propofol, at times showing profound sedation with small doses.
Side effects include: low blood pressure related to vasodilation, transient apnea following induction doses, and cerebrovascular effects.
It has more pronounced hemodynamic effects compared to many intravenous anesthetic agents.
Reports of blood pressure drops of 30% or more are thought to be at least partially due to
Inhibition of sympathetic nerve activity, may cause blood pressure drops of 30%.
The hypotension effect is related to dose and rate of propofol administration.
The hypotension effect may also be potentiated by opioid analgesics.
Can cause decreased systemic vascular resistance, myocardial blood flow, and oxygen consumption, by vasodilation.
Green discolouration of the urine has been reported.
By depressing the central inspiratory drive, it may produce significant decreases in respiratory rate, minute volume, tidal volume, mean inspiratory flow rate, functional residual capacity, and apnea.
Drug administration can diminish cerebral blood flow, cerebral metabolic oxygen consumption, and intracranial pressure, and can decrease intraocular pressure by as much as 50% in patients with normal intraocular pressure.
Rarely associated with dystonia.
Mild myoclonic movements are common.
Can induce priapism in some individuals.
May suppress REM sleep stage and to worsen the poor sleep quality in some patients.
Should be administered when appropriately trained staff and facilities for monitoring are available, as well as proper airway management, a supply of supplemental oxygen, artificial ventilation, and cardiovascular resuscitation.
A rare, but serious, side effect is propofol infusion syndrome, a potentially lethal metabolic derangement in critically ill patients after a prolonged infusion of high-dose substance in combination with catecholamines and/or corticosteroids.
Has several mechanisms of action: through potentiation of GABAA receptor activity and therefore acting as a GABAA receptor positive allosteric modulator, thereby slowing the channel-closing time, and at high doses, propofol may be able to activate GABAA receptors in the absence of GABA, behaving as a GABAA receptor agonist as well.
It is highly protein-bound and is metabolized by conjugation in the liver, and has a half-life of elimination estimated to be between 2 and 24 hours.
Its duration of clinical effect is much shorter, because it is rapidly distributed into peripheral tissues.
A single dose of IV propofol typically wears off within minutes.
It is a versatile drug that can be given for short or prolonged sedation, as well as for general anesthesia.
Generally not associated with nausea.
Its rapid onset and recovery along with its amnestic effects have led to its widespread use for sedation and anesthesia.
Diprivan contains EDTA, a common chelation agent, that also acts bacteriostatically against some bacteria.
A water-soluble prodrug form, fospropofol is rapidly broken down by the enzyme alkaline phosphatase to form propofol.
Lusedra, this new formulation may not produce the pain at injection site that often occurs with the traditional form of the drug.