"Amphotericin B": instruction, mechanism of action. Patients' feedback about the drug

Fungal skin lesions bring considerable discomfort to the patient. Moreover, such diseases are contagious. Therefore, when the first signs of fungus appear, you should always contact a specialist. After the delivery of medical tests and other examinations the doctor is obliged to appoint effective medications to the patient.

Very often, various ointments and tablets are used to treat fungal diseases. However, most doctors claim that such a pathological condition is better treated with intravenous injections. After injections, the drug will immediately begin to affect the microorganisms, which show special sensitivity to it.

The most effective and effective means for eliminating fungal diseases include the drug "Amphotericin B". The instruction, release forms and reviews about this medicine will be presented below.

Form, composition, description and packaging of antibiotic

You can buy the drug in the following forms:

• Lyophilisate "Amphotericin B". The reviews say that this form of the drug is a porous, hygroscopic, yellow mass without a pronounced odor. It is designed to prepare an infusion solution. The active component of this drug is amphotericin B. As auxiliary constituents, substances such as monosodium phosphate and desoxycholic acid are used. On sale this medication comes in 10 ml vials and packs of cardboard.

• Ointment "Amphotericin B". The use of this agent is shown as an additional drug in complex therapy. Antifungal ointment is used only externally. It has a yellow color and contains the same active substance. As for the additional components, they use vaseline oil, medical Vaseline and polysorbate 80. They can be purchased in tubes of 30 or 15 g.

The mechanism of action of the antifungal drug

What is the drug "Amphotericin B"? Instructions for use (tablets with the same active substance found quite problematic) reports that it is a macrocyclic polyene antibiotic with antifungal activity. It is produced by Streptomyces nodosus, and also has a fungistatic and fungicidal effect (depends on the concentration of the drug in biological fluids and the sensitivity of the pathogen).

After getting the medicine into the bloodstream, it binds to the sterols that are in the cell membranes of the fungus that is sensitive to the drug. As a result of such an impact, their permeability is disrupted and the intracellular components are removed to the extracellular space.

The drug "Amphotericin B" is active against many strains and is moderately active against simple fungi.

Also it should be noted that Fusarium spp. And Pseudallescheria boydii. In addition, this drug is ineffective against rickettsia, bacteria and viruses.

Kinetic properties of the drug

Now you know what constitutes an antifungal drug, such as "Amphotericin B". The mechanism of action of this agent was described above.

After intravenous administration of the drug in a single dose in the blood immediately creates its effective concentration, which persists throughout the day. With plasma proteins, this drug binds to 90 percent.

The medicament in question is distributed in the liver, lungs, kidneys, spleen, muscles, adrenal glands and in other organs and tissues. Its concentration in pleural effusion, synovial and peritoneal fluids, as well as aqueous humor reaches 2/3 of the concentration in the blood.

The ways of metabolism of this agent are unknown. In urine and bile, about 98 percent of the drug is present in the form of metabolites. It is withdrawn slowly, through the kidneys. The initial half-life of the drug in adults is 24 hours, in children 6-40 hours, and in newborns 20-60 hours. The final half-life is 15 days.

Indications of antibiotic

What diseases treats the drug Amphotericin B? It is prescribed for progressive, life-threatening fungal infections that have been caused by sensitive microorganisms:

• Histoplasmosis, disseminated cryptococcosis, coccidioidosis;
• Cryptococcal meningitis, paracoccidioidosis, chromomycosis;
• Meningitis caused by other fungi, North American blastomycosis;
• Disseminated and invasive aspergillosis, fikomycosis (zygomycosis);
• Disseminated form of candidiasis, hyalogomycosis;
• Fungal mycosis, chronic mycetoma;
• Disseminated sporotrichosis, infections of the abdominal cavity (including peritonitis);
• Endophthalmitis, endocarditis, fungal sepsis;
• Visceral leishmaniasis, fungal infections of the urinary tract;
• American skin-visceral leishmaniasis.

Contraindications antifungal agents

Consider what conditions prohibit the use of the drug Amphotericin B (tablets from fungi with a similar name are not produced). According to the instruction, this remedy is contraindicated:

• With chronic renal failure;
• With hypersensitivity;
• During the period of breastfeeding.

With caution this medication is used for kidney diseases (including glomerulonephritis), amyloidosis, liver cirrhosis, hepatitis, anemia, agranulocytosis, pregnancy and diabetes.

Amphotericin B lyophilizate: instructions for use

To prepare an intravenous solution, the preparation is used with an initial concentration of 5 mg / ml. Using a sterile syringe, 10 ml of water for injection is introduced into the vial with the medicine. Further, its contents are shaken until a clear, colloidal liquid forms.

Intravenously, the drug is administered within half an hour under the control of blood pressure, body temperature and pulse of the patient. If the drug is well tolerated, its recommended daily dosage is 0.25-0.3 mg per kg of body weight (depending on the severity of the disease).

With heart and vascular diseases, hypersensitivity and insufficient kidney function, treatment starts with small doses (5-10 mg), which gradually increase by 5-10 mg per day and adjusted to 0.5-0.7 mg per kg.

With sporotrichosis, the course dose of the drug is 2.5 g, and the duration of therapy is at least 9 months.

In aspergillosis, the dosage is 3.6 g, and the duration of treatment is at least 11 months.

Children at the beginning of therapy are given 0.25 mg per kg of body weight per day, and then gradually increase to the maximum dose (1 mg per kg).

Ointment "Amphotericin B": instructions for use

Tablets under a similar trade name in pharmacies are not sold. Therefore, to replace this medication you should consult a doctor.

If you need to use the "Amphotericin B" ointment, apply a thin layer to the affected areas twice a day. The treatment course depends on the available indications:

• With candidiasis skin folds - about 1-3 weeks;
• With diaper rash in children - about 7-14 days;
• At paronychia and lesions of interdigital spaces - 2-4 weeks.

Side effects

The drug "Amphotericin B" can cause the following side effects:

• Headaches, convulsions, peripheral neuropathy, transitory vertigo, encephalopathy;
• Decreased appetite, vomiting, dyspepsia, nausea, gastralgia, diarrhea, hepatotoxicity, acute hepatic insufficiency, jaundice, hepatitis, melena, hemorrhagic gastroenteritis;
• Normochromic normocytic anemia, leukopenia, clotting disorder, thrombocytopenia, agranulocytosis, hemolytic anemia, eosinophilia, leukocytosis;
• Impaired vision, loss of hearing, diplopia, tinnitus;
• Tachypnea, dyspnea, pulmonary edema, arrhythmia and allergic pneumonitis;
• Decrease or increase in blood pressure, itching, changes in ECG indicators, cardiac arrest, shock, heart failure;
• Anaphylactoid reactions, sneezing, nephrogenic diabetes insipidus, bronchospasm, nephrocalcinosis, rash, exfoliative dermatitis, toxic epidermal necrolysis
• Renal dysfunction, hypokalemia, hypostenuria, renal tubular acidosis, Stevens-Johnson syndrome, acute renal failure, oliguria, anuria;
• Thrombophlebitis and burn at the injection site;
• Fever, myalgia, weight loss, arthralgia, general weakness.

Cases of overdose

When administering large doses of medication, the patient may experience a stop in breathing and heart failure. Therefore, during the therapy should strictly adhere to the recommended dosage. It is also necessary to monitor the work of respiratory and cardiac activity, kidney and liver function, the picture of peripheral blood, as well as the content of electrolytes in it.

Compatibility with other medicines

The drug "Amphotericin B" can strengthen or weaken the effect of other drugs, as well as increase their toxicity. In this regard, this medication with caution is prescribed in complex therapy.

When appointing the said remedy, the patient should be sure to inform his doctor about taking other medications. Otherwise, the use of "Amphotericin B" (intravenous) may be detrimental to the health and overall well-being of a person.

Special Recommendations

• The drug "Amphotericin B" should be used only to treat life-threatening and progressive fungal infections.
• With prolonged use, the likelihood of developing toxic effects increases.
• When anemia occurs, use of the drug should be discontinued.

Reviews

Now you know how the drug "Amphotericin B" works. Suspension with this name in pharmacies is not for sale. Therefore, for oral administration, you should choose another medication with a similar effect.

According to most patients, this means effectively copes with the task. It perfectly treats fungal skin lesions, eliminating the patient's physical and psychological discomfort.

The main drawback of this drug is the presence of a large number of side effects. In the course of treatment with this agent, unwanted reactions can be manifested by any organs and systems. Therefore, it should be used only on special indications.