Propofol

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The active ingredient propofol is the youngest and yet the most widely used anesthetic agent worldwide. Because of its memory-switching off (amnestic) and consciousness-switching off (hypnotic) effect, it is used for the quick and reliable induction and maintenance of anesthesia during an operation. It is very well tolerated and is therefore also used for calming (sedation). Here you can read everything you need to know about the effects, side effects and use of Propofol.

This is how Propofol works

In general, the goal of anesthesia is to eliminate pain (analgesia) and consciousness (hypnosis) during an operation. Furthermore, the muscles should relax and natural reflexes suppressed (vegetative damping). At the beginning of anesthesia, loss of consciousness is induced with a hypnotic (sleeping pill) such as propofol.

How exactly propofol develops its sleep-like effect is not fully understood. The active ingredient can switch off nerve cells for a short time and thus inhibits certain brain regions, namely the hippocampus, which is responsible for memory, and a region of the cerebral cortex (prefrontal cortex), which is responsible for short-term and long-term memory and decision-making. Propofol also prevents the spinal cord from transmitting signals.

Propofol is given directly into a vein (intravenously) as an anesthetic and is therefore called an injection anesthetic. Other injection anesthetics include barbiturates, etomidate and ketamine. There are also anesthetics for inhalation, the so-called inhalation anesthetics (such as isoflurane, sevofulran and desflurane). Injection anesthetics work faster than inhalation anesthetics and are therefore very suitable for starting anesthesia.

Propofol absorption and excretion

After propofol is injected into the patient's vein, it first enters the tissues with the best blood circulation, such as the brain, in the bloodstream. Deep hypnosis occurs within 30 seconds of the patient. The active ingredient is then quickly redistributed to other tissues with less blood supply. As a result of this redistribution, the anesthetic effect in the brain ends within five to ten minutes - consciousness is regained. This can be prevented by giving propofol continuously during an operation.

One then speaks of total intravenous anesthesia. In the liver and kidneys, the active ingredient is finally quickly biochemically converted and broken down and then excreted. Half of it is eliminated from the body after about two hours. A small amount of propofol can also escape through the air we breathe.

When is Propofol used?

Propofol is the most widely used intravenous anesthetic for adults and children. It is very well tolerated: patients describe falling asleep and waking up comfortably. Vomiting and nausea, which often occur after surgery, are very rare with propofol.

In anesthesia medicine, propofol is artificially administered to:

Induction of anesthesia
Calming (sedation) of adults during surgery
Sedation during targeted (interventional) interventions, for example in endoscopy

The active ingredient is still used as an agent for epilepsy (anticonvulsant).

This is how propofol is used

Propofol is given intravenously (IV). It gets directly into the patient's vein via a syringe (injection) or infusion and is therefore effective very quickly. If the concentration in the blood plasma is low, it has a soporific (sedating) and memory-switching-off (amnetic) effect. In contrast, unconsciousness (hypnosis) is achieved with higher concentrations of active ingredients. If the concentration is increased further, the patient becomes unable to move (immobile).

This prevents unwanted reflexes, for example caused by the surgeon cutting the skin. Even higher concentrations of propofol are needed to suppress pain-induced stress reactions such as an increase in blood pressure and heart rate. If the anesthetic is used in too low a dose, the patient may regain consciousness during the anesthesia.

Because propofol has no analgesic effect, a pain reliever (analgesic) must always be administered, such as the highly effective opioid fentanyl. But an appropriate means to relax the muscles (muscle relaxant) is always required. The dosage is calculated based on the age and body weight of the patient and the duration of use.

What are the side effects of Propofol?

Propofol, like any drug, can have side effects. These include:

Slowed breathing (respiratory depression) to respiratory arrest (apnea)
Release of the messenger substance histamine and thus intolerance reactions
increased infections due to a weakening of the immune system

You may experience pain at the injection site during the injection.

Propofol infusion syndrome occurs very rarely (with long-term administration), which among other things leads to severe cardiovascular disorders - often even fatal. This side effect can occur especially in children after long-term sedation with propofol for more than two days. This undesirable effect is also possible in adults. To avoid the syndrome, propofol must not be used for more than seven days. The patient should be under constant medical supervision.

What should be considered when using propofol?

Propofol is very well tolerated. Propofol can be used in newborns from the 31st day of life. For long-term sedation in the intensive care unit, however, it is only suitable for patients older than 16 years.

It should also be noted that propofol can slow the heartbeat and lower blood pressure. Therefore, special caution is required in patients with cardiovascular weakness or reduced blood volume (hypovolaemia).

Some substances, such as the strong pain reliever fentanyl or benzodiazepines, can prolong and intensify the effect of propofol.

Propofol in pregnancy

The anesthetic can easily pass through the placenta to the unborn child. A mutagenic effect has not yet been observed.According to the current state of knowledge, the agent does not cause any malformations (no teratogenic risk). In higher doses, however, it is likely to have a negative effect on the child's circulation.

According to experts from the Berlin Charité, propofol can still be used throughout pregnancy in certain situations. Doctors use it, for example, to induce general anesthesia before a caesarean section.

For longer interventions lasting at least three hours, the treating physicians carefully weigh up whether propofol is still the most suitable anesthetic agent. Propofol is not suitable for sedation for several days during pregnancy.

In principle, doctors only give anesthetics during pregnancy if it is necessary. It is best to convey your concerns to the doctor and get detailed information about the necessity and risks.

Propofol while breastfeeding

If propofol is given to nursing mothers, very small amounts of it pass into breast milk. According to the Pharmacovigilance and Advice Center for Embryonic Toxicology of the Berlin Charité (embryotox), this does not, however, constitute an additional breastfeeding break.

Clinical experience has so far shown no side effects in breastfed children after their mothers have been anesthetized.

However, some manufacturers of the drug Propofol recommend a 24-hour break from breastfeeding. It is best to clarify this with your doctor - he can provide an individual assessment.

How to get drugs with propofol

Propofol is available with a prescription in the form of ampoules or vials. The active ingredient is usually dissolved in an emulsion made from soybean oil. The required dosage is determined and administered by a doctor.

Since when has propofol been known?

Propofol was first synthesized around 1970 and tested in a clinical study by doctors Kay and Rolly as early as 1977. It was not until 1989 that it was finally approved on the market in Germany for anesthesia and in 1993 also for sedation in intensive care medicine.