Amphotericin B (Amphotericinum B)

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

Antifungal means

Included in the formulation
  • Ambiz®
    powder d / infusion 
    Gilead Science International Co., Ltd.     United Kingdom
  • Amphotericin B
    lyophilizate d / infusion 
    SYNTHESIS, OJSC     Russia
    • Included in the list (Order of the Government of the Russian Federation No. 2782-r of 30.12.2014):

    VED

    АТХ:

    J.02.A.A.01   Amphotericin B

    Pharmacodynamics:

    Disrupts membrane barrier functions by linking with its sterol component. Causes lysis of sensitive fungi: Candida spp., Histoplasma capsulatum, Cryptococcus neoformans, Aspergillus spp., Leishmania.

    Pharmacokinetics:

    The drug is not practically absorbed from gastrointestinal tract. It binds to blood proteins by 90%. Practically not dialyziruetsya, easily penetrates into the tissues (except body fluids and serous cavities), passes through the placenta. Metabolized, in bile and urine, about 98% of amphotericin is present in the form of metabolites. It is excreted by the kidneys slowly, half-life is 15 days. Traces of the drug after cancellation are found in the body for several more weeks.

    When topical application in the form of an ointment is not practically absorbed.

    Indications:

    Fungal infections (including cancer patients with neutropenia): disseminated cryptococcosis, cryptococcal meningitis (including in patients with AIDS in combination with flucytosine); meningitis caused by other fungi, invasive and disseminated aspergillosis, North American blastomycosis,disseminated forms of candidiasis, intestinal candidiasis, coccidioidosis, paracoccidioidosis, histoplasmosis, fricomycosis, chromomycosis, mold mycosis, disseminated sporotrichosis, hyalogomycosis, chronic mycetoma, abdominal infections (including peritonitis), endocarditis, endophthalmitis, fungal septicemia (with candidemia in patients without neutropenia comparable in effectiveness with fluconazole), fungal infections of the urinary tract.

    Visceral leishmaniasis (as a primary treatment, including those with immunodeficiency), American skin-visceral leishmaniasis.

    ICD-10

    I.B20-B24.B20.4   The disease caused by HIV, with manifestations of candidiasis

    I.B20-B24.B20.5   The disease caused by HIV, with manifestations of other mycoses

    I.B35-B49.B37.8   Candidiasis of other localizations

    I.B35-B49.B37.7   Candida septicemia

    I.B35-B49.B37.1   Pulmonary Candidiasis

    I.B35-B49.B37.0   Candidiasis stomatitis

    I.B35-B49.B38   Coccidioidomycosis

    I.B35-B49.B39   Histoplasmosis

    I.B35-B49.B40   Blastomycosis

    I.B35-B49.B42   Sporotrichosis

    I.B35-B49.B43   Chromomycosis and pheomycotic abscess

    I.B35-B49.B44   Aspergillosis

    I.B35-B49.B45   Cryptococcosis

    I.B35-B49.B45.2   Cutaneous Cryptococcosis

    I.B35-B49.B45.1   Cerebral Cryptococcosis

    I.B35-B49.B45.0   Pulmonary cryptococcosis

    I.B35-B49.B48   Other mycoses, not elsewhere classified

    I.B35-B49.B48.7   Opportunistic fungal infections

    II.C81-C96.C84   Peripheral and cutaneous T-cell lymphomas

    Contraindications:

    Individual intolerance.

    Expressed violations of the liver and kidneys.

    Diseases of the hematopoietic system.

    Diabetes.

    Carefully:No data.
    Pregnancy and lactation:

    With caution in pregnancy (adequate and strictly controlled safety studies in pregnant women are not performed).

    FDA Action Category - B.

    For the period of use of the drug from breastfeeding should be discarded, since it is not known whether amphotericin B penetrates into breast milk.

    Dosing and Administration:

    Intravenously drip for 2-6 hours; the active substance concentration is 0.1 mg / ml.

    Trial dose - 1 mg (base) - diluted in 20-50 ml of 5% dextrose solution and administered intravenously for 20-30 minutes or more under the control of blood pressure, pulse and body temperature every 30 minutes for 2-4 hours.

    Treatment begins with the introduction of low doses (5-10 mg) and, increasing them by 5-10 mg per day, bring to a daily dose of 0.5-0.7 mg / kg. When using the drug every other day, the dose should not exceed 1.5 mg / kg.

    Intracavitary instillation: 5 mg (base) in 10-20 ml of a 5% solution of dextrose is administered for 3-5 minutes, then 50 mg (base) in 10-20 ml of 5% dextrose solution for 3-5 minutes every day . 8-12 hours after instillation, 20 ml of a 5% solution of acetylcysteine ​​are injected and continuous slow suction is carried out overnight.

    Side effects:

    Nervous system and sensory organs: headache, polyneuropathy, double vision and blurred vision.

    The cardiovascular system: arterial hypo- or hypertension, arrhythmia, changes ECG.

    Blood: anemia, leukopenia, thrombocytopenia.

    Digestive system: pain in the stomach, nausea, vomiting, decreased appetite, diarrhea, increased activity of hepatic enzymes.

    Genitourinary system: impaired renal function, increased serum creatinine concentration, proteinuria, azotemia, acidosis.

    Allergic reactions: skin rash, itching, angioedema, bronchospasm (with inhalation of the drug).

    Others: increased body temperature, chills, a violation of electrolyte blood.

    Locally: thrombophlebitis at the injection site; with inhalation - perspiration in the throat, cough, runny nose; with topical application - allergic reactions are possible.

    Overdose:

    In case of an overdose observed increased side effects, possible cardiac arrest and respiration. Symptomatic treatment is prescribed.

    Interaction:

    Glycosides of digitalis, antidepolarizing muscle relaxants, diuretics (excretory potassium) - increased toxicity of digitalis preparations, increased neuromuscular blockade.

    Zalcitabine - a decrease in its renal excretion.

    Corticotropin, glucocorticoids, mineralocorticoids - severe hypokalemia.

    Nephrotoxic drugs (antibacterial drugs, immunosuppressants, antineoplastic agents), diuretics (excretory potassium) - increased risk of nephrotoxic action, electrolyte disturbances.

    Antifungal agents (derivatives of azoles) - antagonism.

    Medications that depress the bone marrow, radiation therapy - an increased risk of oppression hemopoiesis.

    Flucytosine is a synergistic action with a simultaneous increase in the toxicity of flucytosine.

    Special instructions:

    To combat side effects, antipyretic and antihistamines, vitamins B, ascorbic acid, non-steroidal anti-inflammatory drugs, preparations of iron, potassium, etc.

    It is necessary to control the function of the kidneys, liver, blood composition and potassium level in the blood.When symptoms of anemia appear, amphotericin B treatment should be discontinued.

    Instructions
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