🐾 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).

Indications

Anestofol 5% is used for euthanasia of dogs and cats whose physical suffering cannot be relieved by medication.

Composition

Anestofol 5% contains propofol 50 mg and lidocaine hydrochloride 50 mg as active substances in 1 ml, and as excipients: tocopherol acetate 7 mg, L-arginine 1 mg, sodium metabisulfite 1 mg, macrogol 15 hydroxyesterate 270 mg, trilon B 0.1 mg, dimethylacetamide 150 mg, benzyl alcohol 0.01 ml and water for injection up to 1 ml.

How to take, the dosage

Propofol passes through the placental barrier, therefore Anestofol 1% is contraindicated for anesthesia in pregnant dogs when it is planned to save the litter, but the drug may be used for anesthesia during caesarean section.
Propofol is excreted with the milk therefore after Anestofol 1% use in lactating bitches the pups should be allowed to the mother not earlier than after 3 hours.
The drug should be used with caution in animals with serious decompensated diseases of cardio-vascular and respiratory systems, kidneys and liver as well as in hypovolemia and severe general state.
Anestofol 1% is administered only intravenously in the following doses:
for short-term anesthesia:
– without premedication – 0.5-0.7 ml of the drug per 1 kg of animal weight, which corresponds to 5-7 mg of propofol per 1 kg of animal weight;
– with premedication – 0.4 ml of the drug per 1 kg of animal weight, which corresponds to 4 mg of propofol per 1 kg of animal weight;
for main anesthesia the drug is administered slowly until the desired depth of anesthesia in a dose up to 8 mg of propofol per 1 kg of the animal weight depending on the species and individual sensitivity of the animal. Further, to maintain adequate anesthesia during the entire period of surgical intervention Anestofol 1% is administered at a dose of 10 mg/kg/hr. Taking into account that propofol has a pronounced hypnotic, but weak analgesic effect, prolonged cavity operations and osteosynthesis should be performed with simultaneous use of analgesic drugs;
for induction anesthesia before inhalation anesthesia Anestofol 1% is administered in the same dose as for short-term anesthesia. It should be noted that the initial concentration of anesthetic gas when using Anestofol 1% should be higher than when using barbiturates.
Propofol does not have sufficient vagolytic effect, its use may be accompanied by chronotropic effect manifested by marked bradycardia or development of asystole, therefore it is recommended to administer choline drugs, in particular – atropine before Anestofol 1% application.
If pronounced arterial hypotension occurs against the background of propofol administration it may be necessary to administer infusion solutions to correct the circulating blood volume and decrease the rate of propofol infusion.
Before using Anestofol 1% for anesthesia, if possible, the animal should be kept on a starvation diet for 18-24 hours.
To reduce the single dose of the drug, simultaneous use of other drugs that depress the central nervous system, in particular medetomidine (Domitor, Dorben, Meditin), fentanyl or xylazine (Xila, Rometar, Xylanit, etc.For euthanasia Anestofol 5% is administered intravenously in dogs and cats with a dose of 1 ml of the drug per 2.5-5 kg of animal weight, which corresponds to 10-20 mg of propofol per 1 kg of animal weight.
No peculiarities of action were revealed during the first use or in case of withdrawal of the drug.
The drug dosing regimen should be avoided.
Side effects after administration of Anestofol 1% in accordance with the instructions are extremely rare.
Excitation and vomiting may be observed in a small number of animals (5-10%) during the withdrawal from anesthesia.
Also Anestofol 1% administration may cause short-term apnea and drop in blood pressure.
Anestofol 1% and 5% is compatible with muscle relaxants, inhalation and noninhalation anesthetics, with drugs used in premedication, analgesics, but it may increase the suppressive effect on respiration and decrease blood pressure.
Anestofol 1% and 5% is not intended for use in productive animals.

Special Instructions

When working with Anestofol 1% and 5% you should follow general rules of personal hygiene and safety precautions provided for when working with drugs. When working with the drug it is forbidden to drink, smoke and eat. After handling the drug wash your hands with soap and water.
In case of accidental contact of the drug with the skin or mucous membranes of the eyes they should be rinsed with plenty of running water. People with hypersensitivity to the drug components should avoid direct contact with Anestofol 1% and 5%.
In case of allergic reactions or accidental ingestion of the drug the patient should immediately contact a medical institution (have the instructions for use or the label).
Empty bottles of Anestofol 1% and 5% may not be used for domestic purposes, they must be disposed of with household waste.