🐾 Anestofol solution, 5% vial 10 ml

Anestofol refers to preparations for noninhalation general anesthesia.
Propofol, a component of the drug, is 2,6-diisopropylphenol, causes rapid general anesthesia due to non-specific action at the level of lipid membranes of CNS neurons.
The mechanism of action of propofol is based on the potentiation of gamma-aminobutyric acid in the GABA receptor, which facilitates the inhibitory impulse and delays the time of closure of the chloride ion channel.
When propofol is injected intravenously anesthesia occurs within approximately 30-60 seconds, without pronounced signs of agitation. Propofol has antiemetic effect.
It readily crosses histohematic barriers, including the placental and the BBB. It penetrates into breast milk in small amounts. Propofol is largely (97-98%) bound to plasma proteins, primarily to glycoprotein and to a lesser extent to plasma albumin.
Pharmacokinetics of propofol after bolus administration is described in a three-part model.
The first phase is characterized by rapid distribution of the active substance (half-life of 2-4 min), the second phase by rapid elimination of propofol (half-life of 30-60 min); followed by a longer, final phase characterized by redistribution of propofol from weakly perfused tissues into the blood.
Propofol is well distributed and rapidly eliminated from the body (total clearance is 0.03 – 0.07 l/min).
Propofol is quickly metabolized mainly by conjugation in the liver (by 90-95%) with the formation of inactive metabolites, providing “easy exit” from anesthesia in the animal. It is excreted mainly by the kidneys and bile (up to 10% unchanged). No cumulative effect is observed even after multiple administration of the drug.
The risk of painful sensations along the vein is minimized due to lidocaine contained in the drug.
Lidocaine has a local anesthetic effect, prevents generation of impulses in the endings of sensitive nerves and impulse conducting along the nerve fibers.
Propofol refers to highly dangerous substances according to the degree of impact on the body (2nd class of hazard according to GOST 12.1.007-76).

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