Expiration date: 06/2025
Structure and Composition:
Lyophilized powder for solution for infusion 1 vial of 50000 units.
Amphotericin B 50 mg
in bottles of 10 ml in a cardboard pack 1 bottle.
Ointment 1 g
amphotericin B 30000 IU
in tubes of 15 and 30 g in the paper cartons 1 tube.
Description pharmaceutical form:
Lyophilized powder for solution for infusion - a porous mass of yellow, odorless or almost odorless. Hygroscopic.
Ointment - yellow ointment.
Characteristic:
Sterile complex polyene antifungal antibiotic amphotericin B, produced by the actinomycete Streptomyces nodosus, with sodium deoxycholate, and buffer, which consists of amphotericin B, sodium phosphate monobasic and bilateral. It is inactivated by light, atmospheric oxygen. Soluble in water and 5% glucose solution to form colloidal systems, DMSO, insoluble in ether, chloroform, 96% alcohol.
Pharmachologic effect:
Associated with sterols (ergosterol) cell membrane of sensitive fungi. As a result of disrupted membrane permeability and intracellular components fall into the extracellular space.
Pharmacokinetics:
The on / in the introduction is distributed in most of the organs and tissues of the body, it is not defined in the cerebrospinal fluid. It penetrates through the placenta. Plasma protein binding is 90%. Report the news, very slowly, 2-5% in the active form. It can be detected in urine for 7 weeks after the cancellation.
When applied topically - is practically not absorbed.
Description of the pharmacological actions:
It has fungicidal or fungistatic effect depending on the concentration in biological fluids and susceptibility. It is active against many pathogenic fungi, including Candida spp., Histoplasma capsulatum, Cryptococcus neoformans, Aspergillus spp. or Leishmania.
Indications:
Candidiasis of the gastrointestinal tract, intestinal kandidonositelstvo, candidiasis of the internal organs, and chronic granulomatous form of disseminated candidiasis, coccidiosis, cryptococcosis, histoplasmosis, North American blastomycosis, chromomycosis, mold mycosis, sporotrichosis.
Contraindications:
Hypersensitivity to amphotericin B and others. Components of the preparation, expressed human liver and kidneys, blood system diseases, diabetes.
For the ointment - hypersensitivity to amphotericin B.
Application of pregnancy and breastfeeding:
Be wary of pregnancy (adequate and well-controlled studies of the safety in pregnant women has not carried out). At the time of treatment should stop breastfeeding (known whether amphotericin B penetrates into breast milk).
Side effect:
The on / in the introduction:
From the nervous system and sensory organs: headache, polyneuropathy, blurred vision, diplopia.
Cardio-vascular system and blood (blood, hemostasis): arterial hypo- or hypertension, arrhythmia, ECG changes, anemia, leukopenia, thrombocytopenia.
From the digestive tract: nausea, vomiting, diarrhea, epigastric pain, elevated liver enzymes.
With the genitourinary system: renal dysfunction, including increasing the concentration of creatinine in serum, proteinuria, azotemia, acidosis.
Allergic reactions: skin rash, pruritus, angioedema, bronchoconstriction (inhalation).
Other: fever, chills, loss of appetite, disturbance of electrolyte composition of blood, including hypokalemia, hypomagnesemia thrombophlebitis at the injection site by inhalation possible sore throat, cough, runny nose.
When applied topically, no side effects characteristic of systemic action, but may cause allergic reactions.
Drug Interactions:
While the use of potentially nephrotoxic antibiotics, cyclosporin, diuretics increases the risk of nephrotoxicity. In an application with the means oppressive bone marrow, radiation therapy increases the risk of anemia and others. Hematological disorders. It could enhance effects of cardiac glycosides (especially against the background of potassium deficiency in the body) and non-depolarizing muscle relaxants peripheral. In an application with flucytosine lowers the ride height of the latter, as a result may increase the toxicity of flucytosine.
Dosage and administration:
. B / drip (20-30 drops / min) for 3-6 hr solution is prepared under sterile conditions immediately prior to use: the vial is added 5-10 ml of water for injection (sterile syringe through a puncture the rubber stopper, pre-treating it with alcohol ). For I / O administration, the concentration of 100-125 IU per 1 ml of solvent. The mixture was stirred until complete dissolution of the powder, the solution from the vial using a sterile needle dial syringe and poured into a bottle with 400 ml of sterile 5% glucose solution (in the amount of solvent to be dissolved up to 50,000 IU of antibiotic). The solution is prepared and protected from bright light indoors. In case of using the drug does not precipitate.
Individually adjusted dose rate of 250 U / kg. Prior to the introduction of pre-administered 100 U / kg (to identify individual tolerability) with good tolerance, lack of side effects and if necessary increase the dose up to 1000 IU / kg.
Before each administration set and exact mass of the patient, calculate the dose (250 IU drug per 1 kg of patient weight of 75 kg body weight).
The average total dose per course of treatment - 1500000-2000000 units (18-20 injections). The drug is administered in a day or 1-2 times a week (risk of accumulation). Duration of treatment - not less than 4-8 weeks (to prevent recurrence).
Children designate in the following daily doses (U / kg):
At the age of 1-3 years: 1 to 5 injections - 75-150 U / kg from 6 to 10 injections - 100-250 U / kg from 11 to 15 infusions - 150-350 U / kg from 16 to 20 infusions of 175- 400 U / kg.
At the age of 4-7 years: 1 to 5 injections - 100-200 U / kg from 6 to 10 injections - 150-300 U / kg from 11 to 15 infusions - 175-400 U / kg from 16 to 20 injections - 200 -500 U / kg.
At the age of 8-12 years: 1 to 5 injections - 125-250 U / kg from 6 to 10 injections - 175-300 U / kg from 11 to 15 infusions - 200-450 U / kg from 16 to 20 injections - 225 -600 U / kg.
At the age of 13-18 years: 1 to 5 injections - 150-300 U / kg from 6 to 10 injections - 200-400 U / kg from 11 to 15 infusions - 225-500 U / kg from 16 to 20 injections - 250 -700 U / kg.
The first course of treatment - 20 drip / infusion 2 times a week, 1 month after the break, repeat the course. The degree and amount of side effects decreases with intermittent course of treatment (30-40 injections for 5-6 months).
When intolerance daily and course doses lower and increase the interval between administration of the drug. Repeated courses of treatment is initiated with smaller doses.
Inhalation. The solution is prepared immediately before use based 50,000 U per 10 ml of sterile water for injection. Inhalation is performed 1-2 times per day duration - 15-20 min at the rate of 1000-2000 IU / kg. When using inhalers, working only on inhalation, the single dose is reduced to 5 ml (25,000 IU). The course of treatment - 10-14 days, a second course - 7-10 days. The remaining solution in the vial used for inhalation for 24 hours under the condition of its storage in a refrigerator.
Ointment. Locally, put a thin layer 1-2 times a day (up to 4 times). The course of treatment - at least 10 days.
Precautionary measures:
The on / in the introduction of the drug to reduce the severity of side effects appoint antipyretics and antihistamines, vitamins, ascorbic acid, NSAIDs, iron preparations, potassium and others. In the course of treatment requires systematic monitoring of renal function, liver, the blood potassium level blood. When the symptoms of anemia treatment with amphotericin B should be discontinued. For better portability antibiotic in solution for inhalation it is recommended to add 10-15 drops of glycerin health.
