Products
Propofol is commercially available as an emulsion for injection or infusion (Disoprivan, generic). It has been approved in many countries since 1986.
Structure and properties
Propofol obtained by distillation (C12H18O, Mr = 178.3 g/mol, 2,6-diisopropylphenol) is a colorless to pale yellow, clear liquid that is sparingly soluble in water and miscible with hexane and methanol. The liquid in commercially available ampoules is a milky-white emulsion (1-2%). It belongs to the group of phenols.
Effects
Propofol (ATC N01AX10) has anesthetic properties. It is short-acting, intravenous, with rapid onset of action; sedative, relaxant, euphoric, sexually disinhibitory, and aphrodisiac.
Indications
For induction and maintenance of general anesthesia and for sedation of ventilated adults during intensive care. Propofol is also used off-label for headache and migraine, but is not approved for this purpose.
Abuse
Propofol is also abused because of its sedative, relaxing, mildly euphoric, sexually disinhibitory, and aphrodisiac effects. It is popular in part because of its rapid onset of action and short duration of action. In addition, it is not a narcotic and is therefore easier to obtain for abuse. It probably does not lead to physical dependence, but it does lead to psychological dependence. Abuse is potentially life-threatening, even at therapeutic concentrations. Especially if injected rapidly, it can cause a drop in blood pressure, as well as respiratory arrest with hypoxia. Another possible cause of death is pulmonary edema. Therefore, concomitant misuse of other respiratory depressant substances such as benzodiazepines and opioids is probably also problematic. A number of deaths have been described in the literature, including suicides and homicides. Frequently, the victims were health care professionals (especially anesthesiologists, nurses). The death of Michael Jackson is also related to the use of propofol. According to media reports, Jackson’s personal physician, Dr. Conrad Murray, administered propofol to Jackson. Jackson also took numerous other drugs, including benzodiazepines.
Contraindications
- Hypersensitivity
- For sedation of children under 16 years of age in the intensive care unit.
For complete precautions, see the drug label.
Interactions
Fentanyl may increase blood levels of propofol. Ciclosporin: leukoencephalopathy has been reported.
Adverse effects.
Very common:
- Local pain at the injection site
Common:
- Bradycardia (slow pulse rate)
- Hypotension (low blood pressure)
- Temporary apnea (respiratory arrest)
- Nausea and vomiting, headache after awakening (nausea, however, less common than with inhalation anesthetics)
Overdose
Respiratory depression, cardiovascular depression, also with fatal outcome.
