Kinetics of propofol following intravenous bolus injection can be presented as a model of three parts: a fast distribution phase parabolan (half-life 4.2 minutes) β-phase elimination (half-life of 30-60 minutes) and γ-phase of elimination (half-life of 200-300 minutes). During lowering of γ-phase concentration of propofol in the blood is slow due to long adipose redistribution. In the clinical setting, this phase does not affect the time of awakening. The central volume of distribution is 0,2-0,79 l / kg, the equilibrium volume of distribution – 1,8-5,3 l / kg. Propofol predominantly metabolized by conjugation in the liver and in liver clearance is about 2 L / min. Higher clearance in children than in adults. The half-life after intravenous infusion ranged from 277 to 403 minutes. Inactive metabolites are excreted mainly by the kidneys (about 88%). Only 0.3% of the injected drug is excreted unchanged in the urine.
When the maintenance of general anesthesia in normal mode no significant accumulation of propofol after surgical procedures l of at least 5 hours.
Within the recommended rates of infusion of propofol pharmacokinetics is linear in nature.
Indications for use:
- Induction and maintenance of general anesthesia in adults and children older than 1 month;
- Sedation patients on mechanical ventilation (ALV), in adults and children older than 16 years;
- Sedation of patients in mind during surgical and diagnostic procedures in adults in conscious, alone or in combination with a local anesthetic.
- hypersensitivity to propofol or any of the components;
- Pregnancy and lactation (up to 24 hours after use of propofol);
- Children up to age 1 month;
- Propofol Kabi 10 mg / ml is not recommended for sedation in children aged up to 16 years inclusive;
- Propofol Kabi 10 mg / mL are not recommended for use in patients undergoing electroconvulsive therapy.
As with other means to neingalyatsionnyh general anesthesia, caution should be exercised in relation to patients with cardiovascular, respiratory, renal or hepatic impairment, as well as for patients with epilepsy, hypovolemia, lipid metabolism disorders or in parabolan debilitated patients.
In patients with impaired function of the heart, lung, kidney or liver disease, elderly and handicapped people, patients with hypovolemia or epilepsy, patients with disorders of consciousness should be administered at a reduced speed. Before you start applying should get compensation of cardiovascular or respiratory failure and hypovolemia. You must make sure that he gets the antiepileptic therapy before anesthesia in a patient with epilepsy. Although several studies have demonstrated the efficacy of propofol in the treatment of status epilepticus, it can also increase the risk of seizures.
Patients with severe heart failure and other severe heart disease can be administered only with extreme caution and under constant surveillance.
Special caution should be exercised in patients with impaired lipid metabolism and other conditions under which you must carefully administered fat emulsion. If the patient is receiving parenteral nutrition, it is necessary to take into account the amount of fat when. In 1.0 ml of emulsion contained 0.1 grams of fat. In the treatment in the intensive care unit after 3 days is necessary to determine the lipid concentration. Taking into account the higher dose in patients with obesity, you should consider the risk of hemodynamic disturbances.
Particular caution should be exercised in patients with a high intracranial pressure and a low mean arterial pressure, given the increased risk of a significant fall of intracranial perfusion pressure.
Patients with increased intracranial pressure should appoint adequate treatment to improve perfusion brain pressure.
particular caution should be observed when using for anesthesia in infants and children up to 3 years, although currently there is no evidence that the pharmacodynamics and pharmacokinetics of propofol in these children different from children -x over 3 years.
Pregnancy and breast-feeding
Parabolan crosses the placental barrier and can have a dampening effect on the fetus. Is contraindicated in pregnancy, and in high doses for general anesthesia or to maintain anesthesia during delivery.
Exceptions are abortion operation.