Daptomycin - instructions for use, reviews, analogs and formulations (powder for the preparation of a solution for 300 mg and 500 mg infusion) medicines for the treatment of furuncles, abscesses and endocarditis in adults, children and pregnancy. Composition

In this article, you can read the instructions for using the drug Daptomycin. Presented are reviews of visitors to the site - consumers of this medication, as well as opinions of doctors specialists on the use of Daptomycin in their practice. A big request is to actively add their feedback on the drug: the medicine helped or did not help get rid of the disease, which were observed complications and side effects, possibly not declared by the manufacturer in the annotation. Analogues of Daptomycin in the presence of existing structural analogues.Use for the treatment of furuncles, abscesses, pyoderma and staphylococcal endocarditis in adults, children, as well as during pregnancy and lactation. Composition of the preparation.

Daptomycin - antibiotic, cyclic lipopeptide of natural origin. It is active only against gram-positive bacteria. The mechanism of action of Daptomycin is based on the fact that in the presence of calcium ions it binds to the cell membrane (both in the growth phase of the bacterial cell and at rest), causes its depolarization, which leads to a rapid inhibition of protein, DNA and RNA synthesis and cell death with a minor lysis.

Daptomycin rapidly exhibits bactericidal activity (concentration-dependent) against sensitive Gram-positive microorganisms. The group of highly sensitive microorganisms includes: Staphylococcus aureus, Staphylococcus haemolyticus, coagulase-negative staphylococci, Streptococcus agalactiae (streptococcus), Streptococcus dysgalactiae subsp equisimilis, Streptococcus pyogenes, group G streptococci, Clostridium perfringens, Peptostreptococcus spp. The group of resistant microorganisms includes naturally resistant gram-negative microorganisms.

Daptomycin is effective in patients with complicated skin and soft tissue infections (wound infections, subcutaneous abscesses), with bacteremia caused by Staphylococcus aureus (staphylococcus), including methicillin-resistant strains (infective endocarditis, including early postoperative endocarditis)

Composition

Daptomycin + excipients

Pharmacokinetics

In experimental studies, daptomycin is not practically absorbed into the blood by oral administration. With a single or repeated admission, daptomycin is predominantly distributed in well-vascularized tissues and less penetrates the blood-brain and placental barrier. Daptomycin reversibly binds to human plasma proteins regardless of concentration. In healthy volunteers, binding to proteins is approximately 90%, including in cases of impaired renal function. It is excreted mainly by the kidneys. In a single application, 78% of daptomycin is excreted in the urine and 5% - with feces. About 50% of the dose is excreted unchanged in the urine.

Indications

• abscess of skin and soft tissues (limited purulent inflammation);
• phlegmon (diffuse purulent inflammation);
• furuncle (purulent inflammation of the hair follicle, sebaceous gland and adjacent connective tissue);
• carbuncle (accumulation of several furuncles in one area of ​​the skin);
• Folliculitis (isolated inflammation of several hair follicles);
• sycosis (chronic inflammation of the hair follicles);
• impetigo (chronic pustular skin disease);
• Septicemia caused by Staphylococcus aureus (sepsis);
• acute and subacute infective endocarditis (inflammation of the inner shell of the heart);

Forms of release

Lyophilizate for the preparation of a solution for infusions of 350 mg in a vial.

Lyophilizate for the preparation of a solution for infusions of 500 mg in a vial.

Instructions for use and dosing regimen

Daptomycin is administered by intravenous infusion for at least 30 minutes.

For complicated infections of the skin and soft tissues, the recommended adult dose is 4 mg / kg once a day for 7-14 days or until the infection disappears. With the development of bacteremia caused by Staphylococcus aureus, 6 mg / kg of the drug are prescribed once a day.

When bacteremia caused by Staphylococcus aureus, including established or putative infective endocarditis, the recommended dose for adults - 6 mg / kg 1 time a day for 2-6 weeks at the discretion of the attending physician.

Patients over 65 years old in the absence of severe renal dysfunction should be administered with caution at a dose of 4 or 6 mg / kg 1 time per day.Since the experience of using Daptomycin in patients older than 65 years is limited, care must be taken when using the drug in this category of patients.

Since the effectiveness and safety of Daptomycin in children and adolescents (under 18 years of age) is not established, the drug is not recommended for use in this category of patients.

Rules for the preparation and administration of a solution of Daptomycin

1. To prepare a solution for intravenous administration with a concentration of 50 mg / ml of daptomycin:

• 350 mg of the lyophilizate is dissolved in 7.0 ml of a 0.9% solution of sodium chloride or sterile water for injection;
• 500 mg of lyophilizate is dissolved in 10.0 ml of a 0.9% solution of sodium chloride or sterile water for injection.

Preparation of Daptomycin solution is carried out under aseptic conditions.

It is necessary to remove the polypropylene "flip of" cap to detect the central part of the rubber plug. 7 or 10 ml of a 0.9% solution of sodium chloride or sterile water for injection is injected into the vial through the center of the rubber stopper, directing the needle to the wall of the vial. The bottle should be gently rotated to ensure complete dissolution of the drug, then leave it for 10 minutes.The vial is then gently shaken for 5 minutes until the desired clear reconstituted solution is obtained. To avoid foaming, the vial should not be shaken vigorously. Complete dissolution of the lyophilizate usually occurs within 15 minutes.

Before the introduction of Daptomycin, the quality of dissolution of the preparation and the color of the solution should be visually checked. Daptomycin solution should be from pale yellow to light brown in color. If the color changes or the appearance of undissolved visible particles, the preparation should not be used.

The chemical and physical stability of the dissolved drug in the vial is maintained for 4 hours at a temperature of up to 30 degrees Celsius; 12 hours at a temperature of up to 25 degrees Celsius; up to 48 hours - at a temperature of 2-8 degrees Celsius.

2. The resulting solution of Daptomycin is diluted with 50 ml of 0.9% sodium chloride solution and administered intravenously dropwise (in the form of droppers) for 30 minutes.

The chemical and physical stability of the diluted solution in the infusion bags is maintained for 12 hours at a temperature of up to 25 degrees Celsius or 24 hours at a temperature of up to 25 degrees Celsius.

From a microbiological point of view, a diluted solution of the drug for intravenous administration should be used immediately after preparation. If the prepared infusion solution is not used immediately, the storage time should not exceed 24 hours at a temperature of 2-8 degrees Celsius.

The total shelf life of the solution of daptomycin in the vial and the diluted solution of the drug in the infusion bag should not exceed 12 hours at a temperature of 25 degrees Celsius or 24 hours at a temperature of 2-8 degrees Celsius.

3. After a single injection of Daptomycin, the unused solution of the drug remaining in the vial can not be re-applied.

4. After using the product, disposal of all materials should be carried out properly.

Do not mix Daptomycin with glucose-containing solutions.

Side effect

• fungal infections;
• urinary tract infections;
• thrombocytosis (increase in the number of platelets in the blood);
• anemia (decrease in the concentration of hemoglobin in the blood);
• eosinophilia (an increase in the eosinophil count in the blood);
• anorexia (eating disorder);
• hyperglycemia (increased blood glucose);
• anxiety;
• insomnia;
• headache;
• dizziness;
• paresthesia (impaired skin sensitivity);
• a taste disorder;
• supraventricular tachycardia (increased heart rate);
• extrasystole (violation of the heart rhythm);
• tides;
• decrease or increase in blood pressure;
• nausea;
• vomiting;
• diarrhea;
• constipation;
• abdominal pain;
• dyspepsia (heaviness in the abdomen, early satiety);
• glossitis (inflammation of the tongue);
• jaundice;
• urticaria (rash);
• itching;
• myositis (inflammation of skeletal muscles);
• muscle weakness;
• Myalgia (pain in the muscles);
• arthralgia (joint pain);
• rhabdomyolysis (destruction of muscle cells);
• impaired renal function;
• vaginitis;
• eosinophilic infiltrates in the lungs;
• vesicle-bullous rash (vesicles);
• swelling in the oropharynx;
• anaphylaxis;
• postinfusion reactions;
• fever;
• chills;
• wheezing;
• systemic hyperemia;
• fainting;
• metallic taste in the mouth;
• angioedema;
• DRESS-syndrome (rash + eosinophilia + systemic manifestations);
• reaction at the injection site;
• cough;
• increased activity of hepatic enzymes (ALT, AST, APF);
• violation of electrolyte balance;
• increase in creatinine in blood plasma;
• increased myoglobin.

 Contraindications

• children and adolescents under 18;
• hypersensitivity to daptomycin.

It is not used to treat pneumonia.

Application in pregnancy and lactation

Application in pregnancy is possible only in cases where the expected benefit for the mother exceeds the potential risk to the fetus.

It is not known whether Daptomycin is excreted in human milk. If it is necessary to use lactation, breastfeeding should be discontinued.

In experimental studies, Daptomycin does not adversely affect the course of pregnancy, embryo, fetus, labor and postnatal development.

Use in children

The safety and efficacy of Daptomycin in children and adolescents under the age of 18 years have not been studied.

Application in elderly patients

With caution appoint Daptomycin to patients older than 65 years.

special instructions

With caution apply Daptomycin in patients with impaired renal function (creatinine clearance less than 80 ml per minute), obesity, severe impaired liver function (more than 9 points on the Child-Pugh scale), patients older than 65 years.

In patients with severe renal dysfunction (creatinine clearance less than 30 ml per minute) is used only in those cases when the expected benefit from therapy exceeds the possible risk.This requires a correction of the dosing regimen.

In patients with severe renal insufficiency, an increase in the concentration of Daptomycin in the blood plasma, leading to an increased risk of myopathy.

If suspected to develop a mixed infection (including gram-negative and anaerobic microorganisms), Daptomycin should be combined with appropriate antibiotics.

In case of deeply localized infections, appropriate surgical intervention should be carried out immediately (including wound repair, prosthesis removal, valve prosthetics) to achieve a clinical effect.

Since the development of antibiotic-associated colitis and moderate to severe pseudomembranous colitis (life-threatening conditions) has been noted with almost all antibacterial drugs, consideration should be given to the possibility of developing these undesirable phenomena when using Daptomycin and to monitor the condition of patients with diarrhea during treatment or shortly afterwards its endings.

During the treatment period, the level of activity of creatine phosphokinase should be carefully monitored.In patients with muscle symptoms of unknown etiology and a significant increase in the activity of this enzyme, treatment with Daptomycin should be discontinued.

When Daptomycin is used together with drugs that cause myopathy, it is necessary to monitor the activity of creatine phosphokinase more than once a week and to provide monitoring for patients in order to timely detect any symptoms that indicate the development of myopathy.

In case of symptoms of peripheral neuropathy, patients should be examined and treatment of Daptomycin should be considered.

Impact on the ability to drive vehicles and manage mechanisms

The effect of the drug on the ability to drive vehicles and work with mechanisms has not been studied. However, given the safety profile of Daptomycin, the negative impact on the ability to perform potentially hazardous activities requiring increased concentration and speed of psychomotor reactions is unlikely.

Drug Interactions

Daptomycin is not metabolized or is slightly metabolized with the participation of CYP450 isoenzymes.

The experience of simultaneous use of Daptomycin with drugs, the use of which may be accompanied by myopathy, is limited. However, there have been several cases of increased activity of creatine phosphokinase and the development of rhabdomyolysis in patients receiving Daptomycin together with drugs that cause myopathy. Use Daptomycin together with drugs that cause myopathy, should only be in cases where the benefits of therapy exceed the possible risk.

Since the excretion of Daptomycin occurs mainly through renal filtration, its plasma concentration may increase with simultaneous use with drugs that reduce renal filtration (including non-steroidal anti-inflammatory drugs). In addition, when Daptomycin is used with these drugs, it is possible to develop pharmacodynamic interaction due to the cumulative effect on renal function.

It is necessary to use with caution the use of Daptomycin along with potentially nephrotoxic drugs, providing additional regular monitoring of kidney function in all patients (regardless of the initial state of renal function).

Analogues of the drug Daptomycin

Structural analogs for the active substance:

• Cubicin.

Analogues on the pharmacological group (antibacterial drugs for systemic use):

• Amintaks;
• Bactroban;
• Baneocin;
• Bioparox;
• Bonderm;
• Vellobaktin B;
• Wilimixin;
• Heliomycin;
• Gramicidin C;
• Grammidine;
• Kansamin;
• Coxerin;
• Colistin;
• Cubicin;
• Maiser;
• Monural;
• Ovea;
• Polizhinaks;
• Polymyxin B;
• Subvixin;
• Supirocin;
• Triassept;
• Uronormin F;
• Urophosfabol;
• Urofoscin;
• Fosmicin;
• Fosfomycin;
• Phosphorol is a rhombus;
• Fugentin;
• Fusidanate;
• Fusiderm;
• Fusidic acid;
• Fusidine sodium;
• Fusimet;
• Fucidin;
• Fucitalmic;
• Cyclo plus;
• Cyclomycin plus;
• Cyclorin;
• Cycloserin;
• Ecofomurals.

Callback of a surgeon

Of the positive aspects of Daptomycin, a rapid bactericidal action against most gram-positive bacteria (staphylococci, streptococci, enterococci), which are often resistant to other antibiotics, should be noted. In particular, if 10 years ago for the treatment of pyoderma, furunculosis in a hospital Vancomycin was successfully used, now it is already ineffective, and Kubitsin (the trade name Daptomycin) completely replaces it.The main disadvantage is a pronounced nephrotoxic effect, so with great caution appoint it for problems with the kidneys and the elderly. Often and allergic reactions, so it is contraindicated in allergic patients.

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