Propofol Fresenius

Active material: Propofol
When ATH: N01AX10
CCF: Preparation for intravenous anesthesia
When CSF: 21.01.02
Manufacturer: FRESENIUS KABI GERMANY GmbH (Germany)

Pharmaceutical form, composition and packaging

20 ml – ampoule (5) – packs cardboard.

Pharmacological action

Propofol is a fast-acting intravenous anesthetic for the introduction of general anesthesia and its maintenance, and for sedation of patients in intensive care. According to the general opinion, This causes an anesthetic effect on the level of non-specific lipid membranes. In most patients, general anesthesia occurs within 30-60 seconds. The duration of anesthesia, depending on the dose and concomitant medications, It is between 10 minutes before 1 o'clock. Patient awakens from anesthesia quickly and with a clear conscience. The ability to open the eyes appear over 10 minutes. The specific locations of specific adsorption is not installed.

When using Propofol for induction of anesthesia and to maintain it observed decrease in average blood pressure and slight changes in heart rate. Nonetheless, hemodynamic parameters normally remain relatively stable during maintenance of general anesthesia and the frequency of adverse hemodynamic changes low.

Although after the introduction of Propofol may occur respiratory depression, any effects qualitatively similar to those, that arise in the application of other intravenous anesthetic drugs, and easily controlled conditions in clinical.

Propofol reduces cerebral blood flow, reducing intracranial pressure and cerebral metabolism. The reduction in intracranial pressure was significantly higher in patients with a baseline value of intracranial pressure.

Pharmacokinetics

Of propofol 97% bound to plasma proteins. The kinetics of the drug after bolus intravenous injection may be presented in the form of a pattern of three parts: rapid distribution phase (half life 2-4 minutes), b-фаза (half life 30-60 minutes) и c-фаза (half life 200-300 minutes). During γ-phase reduction of the concentration of the drug in the blood is slow because of the slow redistribution of poorly perfused, probably, fatty tissue. In the clinical setting, this phase does not affect the time of awakening. Propofol is metabolized primarily in the liver by conjugation with the clearance around 2 l / min, but metabolism occurs also outside the liver. Clearance in children than in adults above. The half-life following intravenous infusion ranged from 277 to 403 minutes. Inactive metabolites are excreted mainly by the kidneys (about 88%). While maintaining anesthesia normally no significant accumulation of Propofol after surgical procedures of at least 5 hours. Within the recommended infusion rate is linear pharmacokinetics.

Testimony

Propofol primenyaetsya:

• in adults and children older than 1 months for total intravenous anesthesia, having a short-term action;
• in adults and children older than 1 month for the induction of anesthesia and to maintain it;
• in adults and children older than 16 years for sedation, receiving intensive care and on mechanical ventilation;
• adults in conscious, to provide sedation for surgical and diagnostic procedures.

Dosage regimen

It is used only intravenously. With the introduction of propofol at the disposal of the physician should be equipment, commonly used during anesthesia, including means of control of the cardiovascular system (ECG, pulse, oximetry) and resuscitation facilities.

Propofol Dose selected individually depending on the response of the patient to premedication. Usually, When using the drug requires additional administration of analgesic drugs.

Side effect

General

With the introduction of anesthesia may develop pressure reduction and the temporary cessation of breathing, that may manifest itself in severe, especially in patients with general deterioration. Less commonly observed movement epileptoformnye, convulsions and opisthotonus, sometimes in a few hours or days after administration. It was also reported cases of pulmonary edema. Sometimes waking consciousness is deteriorating again for a short time. In some cases, an allergic reaction in the presence of anaphylactic symptoms, such as severe hypotension, bronchospasm, swelling or erythema of the face. Against the background of the use of propofol and bradycardia occurred in some cases, cardiac arrest (asistolija). In very rare cases, the use of propofol for sedation in intensive care with doses higher 4 mg / kg / h was observed: raʙdomioliz, metabolic acidosis, hyperkalemia or heart failure. Very rarely following administration of propofol developed pancreatitis; but a causal relationship has not been confirmed clearly. Also notes postoperative fever, heat sensation of cold and euphoria. Against the background of the prolonged use of propofol may be a urine staining green or reddish-brown color, hinolnymi caused by metabolites of propofol and are not dangerous. There may be changes in sexual behavior, As with other anesthetics. After repeated administration of propofol observed mild thrombocytopenia.

Local

Usually, propofol is well tolerated. Often there is pain at the injection site, which can be reduced, mixing the drug with lidocaine or by injection into one of the large veins in the upper arm or elbow fossa. Rarely observed phlebitis and venous thrombosis. In some cases, after intravenous administration of propofol arose severe tissue reaction.

Contraindications

• govyshennaya sensitive to one component of the drug,
• pregnancy,
• Children up to age 1 of the month.

Propofol is contraindicated for the sedation of patients under the age of 16 years during intensive care. Elderly patients care, patients with impaired function of the heart, breath, kidney or liver disease, as well as patients with hypovolemia and epilepsy

Propofol should be administered with caution and reduced speed. If you have a heart, circulatory or respiratory failure should be compensated before administration of Propofol.

To apply caution in patients with severe heart failure and other serious diseases of the heart, if this is not provided extreme caution and intensive monitoring of the patient.

Particular caution should be exercised in relation to patients with high intracranial pressure and low mean arterial pressure, who are at increased risk of a significant fall of intracranial perfusion pressure.

Propofol is not recommended for use in patients, undergoing electroconvulsive therapy.

Pregnancy and lactation

Propofol crosses the placental barrier and can have a depressing effect on the fetus. For this reason, the drug is contraindicated during pregnancy, and in high doses to anesthesia during delivery, except for operations to end the pregnancy.

A small amount of propofol passes into breast milk. It is believed, that it is not dangerous for the baby, if the mother starts breastfeeding within a few hours after the administration of propofol.

Cautions

Propofol does not reduce vagal tone, and its use in some cases accompanied by bradycardia (sometimes expressed), and asystole. Prior to induction or during maintenance of anesthesia Propofol should consider intravenous anticholinergics, especially in cases presumably enhanced vagal tone or using Propofol together with other drugs, able to induce bradycardia.

To attenuate pain at the injection site during induction of anesthesia Propofol emulsion before administration of the drug can enter lidocaine. When using lidocaine should be considered, it can not be used in patients with hereditary porphyria.

Propofol may be used only doctors, trained in anesthesia and intensive care.

Efficacy and safety of propofol (Background) children under the age relaxation 16 years has not been studied. When unlicensed use of the drug for (Background) children under the age relaxation 16 years, reported cases of serious side effects, including death, Although a causal relationship in these cases is not installed. In particular, Cases of metabolic acidosis, giperlipidemii, rhabdomyolysis and / or cardiac failure. These effects are often observed in children with respiratory tract infections, treated in the intensive therapy unit dose, excess dose for adults. Similarly,, adult, receiving the drug for longer 58 hours at a 5 mg / kg / hour, Rarely, metabolic acidosis, rhabdomyolysis, hyperkalemia and / or rapidly progressive heart failure (in some cases, fatal). This rate exceeds the maximum rate 4 mg / kg / hour, recommended for use of the drug for the purpose of relaxation of patients under intensive care. Heart failure in such cases is usually not sensitive to maintenance therapy inotropes.

Overdose

Overdose can cause depression of the cardiovascular and respiratory systems. When the oppression of the respiratory system is recommended mechanical ventilation with oxygen, and for inhibition of the cardiovascular system of the patient must change position so, his head was above, and feet - below. If necessary, use a vasopressor agents, plazmozameschayuschie agents or solutions of electrolytes such Ringer.

Drug Interactions

Propofol can be used in conjunction with other drugs, commonly used for sedation, inhalation anesthesia, muscle relaxants or local anesthetic. Cases pharmacological incompatibility has not yet been registered. Reducing the dose required if, If general anesthesia is accompanied by local anesthesia.

The use of benzodiazepines, parasympatholytics or together with inhalation anesthetics propofol and prolong the anesthetic effect reduces the respiration rate.

After a joint opiate sedation may increase the frequency and duration of apnea.

Against the background of the introduction of suxamethonium or neostigmine may bradycardia and cardiac arrest.

Propofol in combination with these drugs, having hypotensive effect and affect breathing, may exacerbate these effects.

It should be taken into account, that the use of propofol for sedation background simultaneously with inhaled or other analgesics, can potentiate anesthesia and side effects of the cardiovascular system. The combined use of drugs with him, central nervous system depressants, eg, alcohol, general anesthetics or opioids leads to severe manifestations of sedation. If propofol combined with parenterally administered drugs, depresses the central nervous system, possible severe respiratory depression and cardiac activity.

After administration of fentanyl blood levels of Propofol temporarily increases. There is evidence, that the administration of fat emulsions, such, how Propofol, sick, receiving cyclosporine, It causes leukoencephalopathy.

Conditions and terms

Store at temperatures not above 25 ° C.

Do not freeze!

Shake before use!

Use only, if the emulsion is homogeneous, but the packaging is not damaged.

Shelf life. 3 year.