Amphotericin B [lipid complex] - instructions for use, dose, side effects, contraindications

Clinical and pharmacological group: & nbsp

Included in the formulation

АТХ:

J.02.A.A.01 Amphotericin B

Pharmacodynamics:

A polyene macrocyclic antibiotic, depending on the sensitivity of the pathogen and the concentration of the drug in biological fluids, can exert a fungicidal or fungistatic action, binds to ergosterols in the cell membrane of sensitive fungi.

Active for most strains Histoplasma capsulatum, Coccidioides immitis, Paracoccidioides braziliensis, Candida spp., Blastomyces dermatitidis, Rhodotorula spp., Cryptococcus neoformans, Sporothrix schenckii, Mucor mucedo, Rhizopus spp., Absidia spp., Basodiobolus ranarum, Aspergillus fumigatus. Moderately active against some protozoa: Leishmania braziliensis, Leishmania mexicana, Naegleria fowleri. Amphotericin B is usually stable Pseudallescheria boydii, Fusarium spp., the drug is ineffective against bacteria, rickettsia, viruses.

Pharmacokinetics:

It is distributed in most organs and tissues of the body, it penetrates the placenta. In the cerebrospinal fluid is not determined. 90% bound to plasma proteins. Very slowly excreted by the kidneys, can be found in the urine within 7 weeks after the end of treatment.

Indications:

- Severe systemic and / or deep mycoses in children and adults;

- Disseminated cryptococcosis and cryptococcal meningitis;

- Invasive and disseminated aspergillosis;

- Coccidioidomycosis;

- North American blastomycosis;

- Histoplasmosis and hyalogomycosis;

- Mukromycosis and chronic mycetoma;

- Visceral leishmaniasis in children and adults and American cutaneous visceral leishmaniasis;

- Systemic mycoses in patients with AIDS and in patients with immunodeficiency;

- Prevention of invasive fungal infections (including malignant neoplasms, transplantation of parenchymal organs and bone marrow).

ICD-10

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.B38 Coccidioidomycosis

I.B35-B49.B39 Histoplasmosis

I.B35-B49.B40 Blastomycosis

I.B35-B49.B44 Aspergillosis

I.B35-B49.B44.7 Disseminated Aspergillosis

I.B35-B49.B45 Cryptococcosis

I.B35-B49.B45.1 Cerebral Cryptococcosis

I.B35-B49.B45.7 Disseminated cryptococcosis

I.B35-B49.B46.5 Mucormycosis, unspecified

I.B35-B49.B47 Mycetoma

I.B35-B49.B48.8 Other specified mycoses

I.B35-B49.B49 Mycosis, unspecified

I.B50-B64.B55.0 Visceral leishmaniasis

I.B50-B64.B55.2 Skin and mucous leishmaniasis

II.C76-C80.C76 Malignant neoplasm of other and inaccurately marked localizations

III.D80-D89.D84.9 Immunodeficiency, unspecified

XXI.Z40-Z54.Z51.1 Chemotherapy for neoplasm

XXI.Z80-Z99.Z94.9 Presence of transplanted organ and tissue, unspecified

Contraindications:

- Individual intolerance;

- Severe violations of the liver and kidneys;

- Diseases of the hematopoietic system;

- Diabetes.

Carefully:

With extreme caution, it is necessary to use the drug in combination with nephrotoxic agents.

Pregnancy and lactation:

Action category for the fetus by FDA - С. The safety of the drug during pregnancy and lactation is not established. Its use during pregnancy is possible only if the intended benefit to the mother is higher than the potential risk to the fetus. Not recommended for use during breastfeeding.

Dosing and Administration:

Intravenously, drip for 30-60 minutes, the average course dose of the drug is 1-3 g and is achieved during 2-4 weekspruce.

With systemic fungal infections Therapy is started with 1 mg / kg in day, if necessary, can be increased to 3 mg / kg in day, in severe cases - up to 5 mg / kg in day.

For the prevention of invasive fungal diseases in the transplantation of parenchymatous organs the drug is prescribed at 1 mg / kg in day within 5 days after transplantation.

Patients with HIV-infection complicated with disseminated cryptococcosis, by 3 mg / kg for 42 days.

In the treatment of visceral leishmaniasis the drug is prescribed at 1-1.5 mg / kg in day for 21 days or 3 mg / kg in day within 10 days.

For the prevention of invasive fungal infections in patients with neutropenia caused by chemotherapy or the use of high doses glucocorticosteroids, the drug is administered at a dose of 2 mg / kg in day until the neutrophil level is restored to 0.5×10⁹/ l.

When the drug is prescribed for elderly patients, dose adjustment is not required.

The infusion solution is prepared immediately before use and can be stored for 1-2 hours at room temperature.

Side effects:

Digestive system: nausea, vomiting, increased activity of hepatic enzymes.

Urinary system: possibly a temporary decrease in renal function (increased serum creatinine concentration, azotemia, hypokalemia, acidosis).

Others: in rare cases possible fever, chills, headaches. A characteristic symptom is the occurrence of pain in the lower back in a few minutes after the start of the infusion (passes independently after the procedure).

Overdose:

In case of an overdose, it is important to urgently cancel the drug and carefully monitor the kidney function.

Interaction:

With simultaneous use with diuretics, potentially nephrotoxic antibiotics, cyclosporine, the risk of developing nephrotoxic action is increased.

Simultaneous appointment with bone marrow suppressants, radiotherapy increases the risk of anemia and other blood problems.

The drug increases the toxicity of cardiac glycosides and antidepolarizing agents.

With simultaneous use increases the toxicity of flucytosine.

Joint application with glucocorticoids can lead to increased hypokalemia.

Special instructions:

The likelihood of toxic effects increases with prolonged treatment with the drug.

A regular (once a week and more often) laboratory monitoring of kidney, liver and hematopoiesis is needed.

The drug is administered to the patient on hemodialysis only after completion of the dialysis procedure.

Instructions

Amphotericin B [lipid complex] (Amphotericinum B [complexus lipidus])