Amphotericinum In

General characteristics. Structure:

Lyophilisate for preparation of solution for infusions in the form of the porous mass of yellow color, inodorous, or almost inodorous, is hygroscopic; let's dissolve in water and 5% glucose solution with formation of a colloid system.

Ointment for external use of yellow color, a homogeneous consistence.

Active ingredient:    1 g Amphotericinum In 30 000 PIECES

Excipients: liquid paraffin, polysorbate 80, vaseline medical.

Pharmacological properties:

Antifungal antibiotic of a broad spectrum of activity from group of polyenes. It is produced by an actinomyce of Streptomyces nodosus. Renders fungicidal or a fungistasis depending on concentration in biological liquids and sensitivity of the activator.
The mechanism of effect of drug is based on its ability to contact sterola (ergosterola) which are in a cellular membrane sensitive to Amphotericinum In a mushroom. Permeability of a membrane is as a result broken, and intracellular components get to extracellular space.
It is active concerning mushrooms of the sort Candida, Histoplasma capsulatum, Cryptococcus neoformans, Aspergillus, Coccidioides immitans, Blastomyces dermatitidis, Sporothtrix schenckii, Fonsecaea, and also leyshmaniye.

Pharmacokinetics. Distribution

It is distributed in most bodies and fabrics, in cerebrospinal fluid is not defined. Linkng with proteins of plasma makes 90%.

Removal

It is removed by kidneys, very slowly. 2-5% of the entered dose are removed in an active form. It can be found in urine within 7 weeks after cancellation.

Indications to use:

For parenteral and inhalation use

— GIT candidiasis, intestinal kandidonositelstvo;

— candidiasis of internals;

— the chronic granulematozny and disseminated candidiasis forms;

— coccidioidosis;

— cryptococcosis;

— histoplasmosis;

— North American zymonematosis;

— chromomycosis;

— mold mycoses;

— aspergillosis;

— sporotrichosis.

For external use

— candidiasis of skin and mucous membranes.

Route of administration and doses:

External use
Ointment is applied on affected areas of skin a thin layer 2-4 Course of treatment at candidiasis of folds of skin - 1-3 weeks, at an intertrigo at children - 1-2 weeks, at defeat of interdigital intervals and a paronychia - 2-4 weeks.

Features of use:

In case of development of anemia treatment by Amphotericinum In should be stopped.

In the course of treatment systematic control of function of a liver, kidneys, pictures of peripheral blood and level of potassium in a blood plasma is necessary.

Ointment should not be applied under occlusive bandages.

In the absence of effect of ointment use Amphotericinum In in 1-2 weeks it is necessary to specify the diagnosis and further tactics of treatment.

Side effects:

For parenteral use
From the alimentary system: nausea, vomiting, pains in epigastriums, a loss of appetite, increase in activity of liver enzymes.
From system of a hemopoiesis: anemia, leukopenia, thrombocytopenia.
From TsNS and peripheral nervous system: headache, polyneuropathy, sight illegibility, diplopia.
From cardiovascular system: arterial hypotension, arterial hypertension, arrhythmia, changes of an ECG.
From an urinary system: a renal failure, including increase in concentration of creatinine in blood serum, a proteinuria, an azotemia, a hypopotassemia, acidosis.
Allergic reactions: skin rash, an itch, a Quincke's edema, a bronchospasm (at inhalation use), allergic contact dermatitis (at external use).
From water and electrolytic balance: hypopotassemia.
Local reactions: at in introduction - thrombophlebitis; at inhalation use - irritation in a throat, cough, cold.
Others: fervescence, fever.
For external use
At ointment use - a burning sensation, prickings, a dermahemia; seldom - a xeroderma.

Interaction with other medicines:

At simultaneous use of Amphotericinum In with potentially nefrotoksichny antibiotics, cyclosporine, diuretics the risk of development of nephrotoxic action increases.

At simultaneous use with the medicines oppressing function of marrow the risk of development of anemia and other hematologic disturbances increases.

Amphotericinum of B can cause strengthening of effects of cardiac glycosides (especially against the background of deficit of potassium in an organism) and not depolarizing muscle relaxants.

At simultaneous use with flutsitoziny Amphotericinum In reduces clearance of the last thereof the toxic effects caused flutsitoziny can amplify.

Processing of skin the means containing benzyl alcohol before ointment imposing In can lead Amphotericinum to drug precipitation.

Contraindications:

— the expressed abnormal liver functions;

— the expressed renal failures;

— diseases of the hemopoietic system;

— diabetes mellitus;

— hypersensitivity to drug components.

 

Use of the drug AMPHOTERICINUM In at pregnancy and feeding by a breast
Amphotericinum In gets through a placenta. Adequate and strictly controlled researches of safety and efficiency of use of drug for pregnant women were not conducted. Use of drug is possible only if the estimated advantage for mother exceeds potential risk for a fruit.

It is unknown whether Amphotericinum In with breast milk is allocated. Therefore in need of use in the period of a lactation it is necessary to resolve an issue of the breastfeeding termination.

 

Use at abnormal liver functions
It is contraindicated at the expressed abnormal liver functions.

 

Use at renal failures
It is contraindicated at the expressed renal failures.

 

Use for children
The daily dose of Amphotericinum In for children and teenagers depends on age.

Overdose:

Now about cases of overdose of the drug Amphotericinum In it was not reported.

Storage conditions:

List B. Drug should be stored in the dry, protected from light place, at a temperature from 2 to 8 °C. A period of validity of the lyophilized powder - 4 years. Unused solution for infusions is not subject to storage. The solution for inhalations which remained in a bottle can be used during 24 h at storage in the refrigerator.

Issue conditions:

According to the recipe

Packaging:

15 g - aluminum (1) - packs cardboard.
30 g - aluminum (1) - packs cardboard.