Fusidanate® (Fuzidanat)

Composition Pharmacodynamics Indications Carefully Contraindications Dosing and Administration Side effects Form release / dosage
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Active substanceFusidic acidFusidic acid
Dosage form: & nbspPowder for solution for infusion
Composition:
Active substance:
Sodium fusidate (in terms of fusidic acid) 500 mg
Solvent:
Disodium edetate dihydrate (in terms of disodium edetate) 5.0 mg
Sodium hydrogen phosphate dihydrate 196.0 mg
Citric acid monohydrate - 10.0 mg
Water for injections up to 10 ml

Description:
powder white or white with a yellowish hue; .
solvent - clear colorless or light yellow solution.

Pharmacotherapeutic group:antibiotic of polycyclic structure
ATX: & nbsp

D.09.A.A.02   Fusidic acid

Pharmacodynamics:
Pharmacodynamics. Fusidic acid belongs to the group of fusidins, antimicrobial compounds that act as inhibitors of protein synthesis in a bacterial cell. .. By blocking the elongation of factor G, they prevent its binding to ribosomes andguanosine triphosphate, which interrupts the release of energy necessary for protein synthesis and leads to the death of the bacterial cell. Fusidic acid has a high, -. activity against staphylococci, 'including Staphylococcus aureus, 1 Staphylococcus1 epidermidis, including methicillin-resistant (oxacillin) strains, Neisseria meningitides, Neisseria gonorrhoeae, Haemophylus spp., Moraxella spp. and Corinebacterium spp.
In the concentration of 0,03-3,13'mg / l inhibits almost all Staphylococcus aureus strains. Less active against Streptococcus spp., Including Streptococcus pneumoniae, is not active against Escherichia coli, Salmonella spp., Proteus spp., Other
gram-negative bacteria, protozoa and fungi. There is no cross resistance for fusidic acid; acts on strains of staphylococci, resistant to other antibiotics. Fusidic acid is characterized by low toxicity. It is used when other antibiotics are contraindicated, for example, if there is an allergy to penicillins and other antibiotics, as well as with kidney failure.

Pharmacokinetics:
. After a single infusion of 500 mg for more than 2 hours - the maximum concentration of fusidic acid 'in the serum is about 50 μg / ml. With repeated infusions every 8 hours for 2-3 days, cumulation of the drug is observed,while the maximum concentration of fusidic acid in the serum reaches 60-120 μg / ml
. Half-life is about 10-15 hours; The connection with proteins (albumin) is more than 95%. It is well distributed in tissues with low and high blood supply. High bactericidal .. concentrations that exceed the minimum inhibitory concentration for staphylococci. (0,03-3,13 mg / l), are created in the skin and subcutaneous tissue, cartilage and-connective tissue, heart tissues, lungs, liver, kidneys, bones, synovial fluid, eye tissues, purulent discharge , sputum, sequestrants; scabs, in the contents, abscesses, including abscesses of the brain .. Fusidic acid is metabolized in the liver. It is excreted mainly with bile through the intestine, to a lesser extent - by the kidneys. Penetrates through the placenta and in small amounts - in; breast milk.

Indications:
Bacterial infections caused by fusidic acid-sensitive microorganisms: pneumonia, lung abscess, pleural empyema, bacterial endocarditis, sepsis, mucoviscidosis, osteomyelitis, skin infections. and soft tissues (pyoderma wound infection, infected burns).

Contraindications:
Hypersensitivity to any of the components of the drug, 'simultaneous reception with statins (risk of rhabdomyolysis). .

Carefully:
If there is a violation of the liver function, obstruction of the biliary tract, impaired transport, and metabolism of bilirubin, the presence of jaundice, during treatment with hepatotoxic drugs; when combined with lincomycin and rifampicin, in newborns with jaundice, acidosis, and also in premature or newborns with other severe diseases.

Pregnancy and lactation:
Fusidanate® is not recommended for use during pregnancy. If you need to use the drug during lactation, breastfeeding is discontinued.

Dosing and Administration:
Fusidanate® is administered intravenously by drip.
The average dose for adults weighing more than 50 kg is 500 mg 3 times a day. Average dose
for children and adults with a body weight of less than 50 kg - 6-7 mg / kg 3 times a day.
In patients with renal insufficiency, as well as those on hemodialysis correction of the dose is not required.
The recommended duration of treatment is 3-6 days, with a subsequent transition;
on taking oral forms of fusidic acid
The solution is prepared ex tempore by dissolving 500 mg of powder. Fusidanate® in 10 ml.
/ of the attached buffer solution, and then the resulting solution is diluted in 500 ml of 0.9%
/ solution of sodium chloride. Children use 10% instead of 0.9% sodium chloride solution: solution of dextrose. In adults weighing less than 50 kg and children, a single dose corresponds to 6-7 ml of the resulting solution per 1 kg of body weight. The Fusidanate solution is introduced,
- drip intravenously directly into large veins or through a catheter into the central veins. The rate of administration in adults is 60-80 cap / min, in children 10-15. cap / min ..
The duration of the introduction through the catheter into the central vein is more than 2 hours; in the superficial vein - not less than 6 hours: -After the end of the infusion, it is necessary to inject / 30.5 ml of a 0.9% solution of sodium chloride or 5% of a solution of dextrose.
A mixture of Fusidan ® with buffer solution can not be administered without further dilution, this solution can be used only once, the remains of unused solution should be destroyed.
Side effects:
The incidence of side effects when using fusidic acid for infusions was 3: 10,000 courses of treatment. The side effects are listed in the order decrease in frequency.
Local reactions', thrombophlebitis, spasm of veins.
Gastrointestinal tract: nausea, diarrhea, abdominal pain, vomiting.
Common symptoms: malaise, fatigue, asthenia, drowsiness, anorexia.
Skin and soft tissues: rash (erythematous, maculopapular, pustular), itching, hives. .
Hepatobiliary system increases the concentration of bilirubin, alkaline phosphatase, transaminase, jaundice, hepatic-renal syndrome.
Organ hematopoiesis, leukopenia, thrombocytopenia, pancytopenia, anemia, hemolysis of erythrocytes (with rapid administration).
Urinary system renal failure.
Immune systems allergic reactions, anaphylactic reactions.

Overdose:
About cases of an overdose of fusidic acid is unknown.
Probable symptoms of acute overdose: gastrointestinal disorders, changes in the liver (change'biochemical indicators, jaundice)
Treatment symptomatic "and maintenance therapy.Hemodialysis is not effective. '
Interaction:
It is pharmaceutically incompatible with kanamycin, gentamicin, vancomycin, carbenicillin, with amino acid solutions, with donor (whole) blood, - with infusion solutions containing lipids, with solutions for peritoneal dialysis,with concentrated (> 20%) solutions of dextrose and calcium-containing drugs.
Fusidanate solution. is compatible with the following infusion solutions: ;
0.9% solution of sodium chloride for intravenous infusions (1-2 mg / ml); .
5% dextrose solution for intravenous infusions (1-2 mg / ml)
Ringer lactate solution (1 mg / ml)
sodium lactate solution for intravenous infusions (1 mg / ml); '
. 0.18,% sodium chloride solution and 4% dextrose solution for intravenous
infusions (1 mg / ml);
0,3% potassium chloride solution and 5% solution, dextrose for intravenous infusions (1 mg / ml) .-,
With the concomitant administration of Fusidanat® with drugs whose metabolism is linked to the cytochrome CYP3A4 system, there may be a mutual inhibition of metabolism., When combined with Fusidan® with inhibitors, 3-hydroxy-3-methylglutaryl coenzyme A reductase, such as statins , the concentration in the blood plasma of both drugs increases, as a result, the risk of rhabdomyolysis 'A' increases. Concomitant use with Fusidanat® increases plasma concentrations of blood - 'cyclosporine, anticoagulants - coumarin derivatives (dose adjustment is required, when combined with Fusidanate®, as well as when it is withdrawn), HIV protease inhibitors (ritonavir and saquinavir).When combined with glycopeptides, fluoroquinolones, antagonism of action is observed.
In the simultaneous use of fusidic acid with other antistaphylococcal antibiotics, for example, penicillin-resistant penicillins, ampicillin, methicillin, cloxacillin, flucloxacillin, cephalosporins, erythromycin, rifampicin, lincomycin, additive or synergistic effects are observed.

Special instructions:
Fusidanate® can not be administered intramuscularly or subcutaneously
If in combination with Fusidanate® another antibiotic is prescribed for the parenteral
introduction, then solutions are introduced separately.
It is not recommended to appoint Fusidan® to patients receiving "drugs," - inhibiting CYP3A4.
In the process of treatment, liver function should be monitored, especially in patients who are "simultaneously receiving hepatotoxic drugs, with liver diseases, with obstruction of the biliary tract, or in combination with drugs that have the same fusidic acid release route, for example , (with lincomycin and rifampicin.If during the treatment with fusidanate ® develops hyperbilirubinemia with jaundice or, without it,as well as the activity of 'liver enzymes' (transaminase alkaline phosphatase) increases, the drug should be canceled.' Increase in activity, liver enzymes and jaundice are usually quickly reversible after drug withdrawal. Jaundice is more common in cases of rapid intravenous injection or exceeding the dose.
Because Fusidanat®. competitively inhibits the binding of bilirubin to a protein, it should be used with caution in patients with impaired transport and bilirubin metabolism. Cases of nuclear jaundice in newborns were not observed, however, "the drug should be administered with caution to newborns with jaundice, acidosis, premature, and also newborns with other serious diseases."
Adverse reactions from the hematopoiesis mainly concern the white. germ of hematopoiesis and are observed with prolonged use of the drug, usually more than 15 days, and when it is abolished, they undergo reverse development.
The risk of developing acute renal failure is usually present in patients with jaundice in the presence of predisposing factors.
In rare cases; at. srchetannom. application with inhibitors of 3-hydroxy-3-methylglutaryl-coenzyme A reductase as a result of rhabdomyolysis' in blood plasma -
the activity of creatine phosphokinase increases, muscle weakness and myalgia are observed, so these patients should be carefully monitored.
In severe infections requiring long-term antibacterial therapy, Fusidan® can be administered in combination with other antistaphylococcal antibiotics, such as penicillin-resistant penicillins, ampicillin, methicillin, cloxacillin, flucloxacillin, cephalosporins, erythromycin, rifampicin, lincomycin,
- additive or synergistic effect.
. With a rapid infusion of fuzidanat ® causes spasm of veins, thrombophlebitis and hemolysis of red blood cells.
'1 ml of the Fusidanate® solution contains 3.1 mmol of sodium and 1.1 mmol of phosphate.

Effect on the ability to drive transp. cf. and fur:
Fusidanat® does not affect the ability of the patient to drive vehicles and perform other potentially dangerous activities that require an increased concentration of attention and speed of psychomotor reactions
Form release / dosage:Powder for solution for infusion 500 mg
Packaging:
A drug
500 mg of active substance into 10 ml glass vials, hermetically sealed with rubber stoppers, crimped with aluminum or imported 'or' combined 'caps (aluminum with safety, plastic' caps)
Solvent (nitrate buffer): '
10 ml (solvent in bottles of glass (type I) with a capacity of 10 ml, hermetically sealed with rubber stoppers, crimped with aluminum or imported or combined caps (aluminum with safety plastic '
\ lids) vial with the drug, 1 bottle with a solvent and instruction, for use packaged in a pack of cardboard. ,
1 vial with the drug, 1 vial with solvent is packaged in a contour mesh package. One contour pack of cells and, the instructions for use are packed in a pack of cardboard.

Storage conditions:
In the dark place at a temperature of no higher than 25 ° C. Keep out of the reach of children.

Shelf life:
3 years.
Do not use after expiration date
Terms of leave from pharmacies:On prescription
Registration number:PL-000626
Date of registration:23.09.2011
The owner of the registration certificate:ABOLMED, LLC ABOLMED, LLC Russia
Manufacturer: & nbsp
Representation: & nbspABOLmed Ltd. ABOLmed Ltd. Russia
Information update date: & nbsp27.09.2015
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