Daptomycin (Daptomycinum)

Pharmacodynamics Pharmacokinetics Indications Carefully Contraindications Dosing and Administration Side effects
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Clinical and pharmacological group: & nbsp

Other antibiotics

Included in the formulation
  • Kubitsin
    lyophilizate d / infusion 
    Novartis Pharma AG     Switzerland
    • АТХ:

    J.01.X.X   Other antibacterial drugs

    J.01.X.X.09   Daptomycin

    Pharmacodynamics:

    The preparation is a cyclic lipopeptide of natural origin. It has the property in the presence of calcium ions to bind to the cell wall of Gram-positive bacteria, which leads to its depolarization. As a result, there is a violation of protein, DNA and RNA synthesis of the microorganism with its subsequent death.

    Pharmacokinetics:

    When the drug is administered in doses of 4-12 mg / kg 1 time per day for 14 days, the pharmacokinetics of daptomycin are mostly linear in nature; equilibrium concentration is achieved after 3 days.

    Poorly penetrates through blood-brain and placental barriers. It binds to plasma proteins by 90%. Minor biotransformation occurs with the help of cytochrome P450. Elimination by the kidneys is 78%, of which 50% is unchanged, and also through the gastrointestinal tract - 5%.

    Indications:

    Bacteremia caused by Staphylococcus aureus (including presumed or established infective endocarditis), complication of infection of soft tissues and skin.

    ICD-10

    I.A30-A49.A41   Other septicemia

    I.B95-B97.B95.6   Staphylococcus aureus as the cause of diseases classified elsewhere

    IX.I30-I52.I33   Acute and subacute endocarditis

    XII.L00-L08.L01   Impetigo

    XII.L00-L08.L02   Abscess of skin, boil and carbuncle

    XII.L00-L08.L03   Phlegmon

    XII.L00-L08.L08.0   Pyoderma

    Contraindications:

    Hypersensitivity, period of lactation, children's age.

    Carefully:

    Chronic liver disease, kidney disease, obesity, age over 65, pregnancy.

    Pregnancy and lactation:

    Action category for the fetus by FDA - B. Qualitative and well-controlled studies on humans and animals have not been conducted. Apply if the benefit to the mother exceeds the risk to the fetus. It is not known whether daptomycin with human breast 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, childbirth and postnatal development.

    Dosing and Administration:

    Introduction by intravenous infusion (within 30 minutes). The dose is 4-6 mg per kilogram 1 time per day. With long-term treatment, the dose is selected individually by the treating physician. Duration of treatment is from 1 to 6 weeks.

    Side effects:

    From the side of the circulatory system: thromboses, anemia, eosinophilia.

    From the side of metabolism: hyperkalemia, anorexia.

    From the nervous system: dizziness, headache, taste disorders, paresthesia, anxiety, insomnia.

    From the gastrointestinal tract: diarrhea, vomiting, nausea, abdominal pain, constipation, glossitis, dyspepsia, hepatitis.

    On the part of the reproductive system: vaginitis.

    From the side of the urinary tract: impaired renal function.

    Infectious diseases: fungal infections, urinary tract infections.

    From the immune system: hypersensitivity, anaphylaxis, rash, infiltrates in the lungs, systemic hyperemia, angioedema, chills, fever, itching, swelling sensation of the nasopharynx.

    From the musculoskeletal system: muscle weakness, myositis, arthralgia, rhabdomyolysis.

    Other: reactions at the site of administration of the drug, pain, cough, impaired laboratory parameters of the liver, blood.

    Overdose:

    Not described. Treatment: symptomatic therapy and medical supervision. Daptomycin is slowly eliminated from the body by hemodialysis (about 15% of the dose taken is withdrawn after 4 hours) or by peritoneal dialysis (about 11% of the administered dose is removed after 48 hours).

    Interaction:

    At simultaneous reception with the preparations having nefrotoksicheskie properties - aggravation nefrotoksicheskogo effect. Since daptomycin release 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, including selective COX-2 inhibitors). In addition, when daptomycin is used with these drugs, it is possible to develop pharmacodynamic interaction due to the cumulative effect on renal function.

    Simultaneous reception with funds that contribute to the development of myopathy - increases the activity of creatine phosphokinase and the risk of rhabdomyolysis.

    Special instructions:

    If there is a suspicion that patients have a mixed infection, it is necessary to combine the drug with other antibiotics.

    During the treatment period it is necessary to carefully monitor the level of creatine kinase in patients.

    In case of development of peripheral neuropathy in patients, it is necessary to cancel the drug.

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