Ampholip conc. d/r-ra d/inf. 5 mg/ml vials. 10 ml

Ampholip has fungicidal and / or fungistatic effect depending on the concentration in biological fluids and susceptibility. The mechanism of action of Amphotericin B is based on its ability to bind to sterol (ergosterol), located in the cell membrane sensitive to amphotericin The fungus. As a result of disrupted membrane permeability and intracellular components fall into the extracellular space.

Is active in vitro against most strains of Histoplasma capsulatum, Coccidioides immitis, Candida spp., Blastomyces dermatitidis, Rhodotorula, Cryptococcus neoformans, Sporothrix schenkii, Mucor mucedo, Aspergillus spp.

Is distributed in the majority of organs and tissues, cerebrospinal fluid is determined in a minor amount. Plasma protein binding is 90%. Excreted by the kidneys, very slowly. 2-5% of the administered dose is excreted in the active form. It can be detected in the urine within 7 weeks after drug withdrawal.

Active substance:
Amphotericin B [lipid complex]

Manufacturer

Bharat Sirams End Vaksins Limited, India

Prescribing

Children by a physician, pregnant by a doctor, for adults on prescription

Composition

1 ml concentrate for solution for infusion contains: active substance
: amphotericin B lipid complex (in terms of amphotericin B)
5 mg Excipients: dimyristoyl phosphatidylcholine, dimyristoyl phosphatidylglycerol, sodium chloride, water for injection

Indications

• systemic treatment of severe and / or profound mycosis in children (including premature infants with low birth weight) and adults, including .: disseminated candidiasis; disseminated cryptococcosis and cryptococcal meningitis; invasive and disseminated aspergillosis; coccidioidomycosis; North American blastomycosis; histoplasmosis; gialogifomikoz; mucormycosis; chronic mycetoma; visceral leishmaniasis in children and adults (as primary therapy, including in patients with immune deficiency); American cutaneous visceral leishmaniasis;
• the treatment of systemic fungal infections in AIDS patients and immunocompromised patients, including arisen as a result of anticancer therapy;
• prophylaxis of invasive fungal infections, including in neutropenic patients with malignancy, as well as the transplantation of parenchymal organs and bone marrow (both children and adults).

Contraindications

• hypersensitivity to amphotericin B and other ingredients;
• severe violations of the liver and kidneys;
• disorders of the hematopoietic system (anemia, agranulocytosis);
• diabetes.

Side effects

On the part of the gastrointestinal tract and liver: nausea, vomiting (less than 3%); increase in liver enzymes. Generally, impaired liver function is not progressing with increasing dose. In patients after liver transplantation may be a significant increase in alkaline phosphatase levels.

From the urinary system: there are reports of transient decline of renal function, including increased creatinine concentration in blood serum, azotemia, hypokalemia, acidosis.

Other: rarely – fever, chills, headaches. There have been reports of the occurrence of pain in the back and chest, in rare cases – strong. A characteristic symptom is the occurrence of pain in the lower back in a few minutes after the start of infusion.

How to accept, acceptance rate and dosage

In / in, drip for 30-60 minutes. At occurrence of side reactions infusion time must be increased to 90-120 min. The recommended concentration of active substance is 1mg / ml. The average exchange rate dose is 1-3 and g is reached for 2-4 weeks.

In systemic mycosis treatment usually begin with a dose of 1 mg / kg / day, which is gradually increased if necessary up to 3 mg / kg / day, in some cases – to 5 mg / kg / day

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For the prevention of invasive fungal disease when transplanting parenchymal organs Ampholip administered for 5 days after transplantation at dose of 1 mg / kg / day.

Patients with HIV infection complicated by disseminated cryptococcosis, a drug administered in a daily dose of 3 mg / kg for 42 days. After the end of the main course due to the risk of infection recurrence may be required more prolonged maintenance therapy.

In the treatment of visceral leishmaniasis Ampholip used at a dose of 1-1.5 mg / kg / day for 21 day or 3 mg / kg / day for 10 days. In immunocompromised patients can also use a dose of 1-1.5 mg / kg / day for 21 days, but after the main course due to the risk of recurrence of infection may be necessary supportive therapy or repeated courses of treatment.

For the prevention of invasive fungal infections in patients with neutropenia caused by chemotherapy or high doses of corticosteroids, the drug is administered in a dose of 2 mg / kg / day until neutrophil recovery levels of up to 0.5 x 10 ⁹ / l.

Babies drug administered in doses comparable to those used in adults, per 1 kg of body weight.

In appointing the drug elderly patients dose adjustment is required.

The method for preparing an infusion solution

Immediately before use, the drug should be stored at 1-2 h RT.

For infusion solution bottle should be thoroughly shake – up sediment disappearance and add to a 5% dextrose solution for intravenous use. Ready-to-use infusion solution should have a concentration of 1mg / ml.

Storage conditions

In the dark place at a temperature of 2-8 ° C (do not freeze).

Active substance

Amphotericin B [lipid complex]

Interaction

It increases the efficacy and toxicity of anticoagulants, nitrofurans; theophylline and sulfonylureas (extend half-life);

reduces the effectiveness of ethinyl estradiol (the risk of breakthrough bleeding).

inhibitors of microsomal oxidation in the liver (including cimetidine, non-narcotic analgesics, antidepressants) slow the metabolic rate, increase in the serum concentration (increased toxicity). Inductors microsomal oxidation in the liver (including phenytoin, rifampin, barbiturates, carbamazepine) accelerate biotransformation in the liver (lower efficiency).

When applied simultaneously with flucytosine Ampholip be appreciated that Ampholip can amplify the toxic effect of flucytosine by increasing the cellular uptake and reduction of renal excretion.

Pharmaceutical interaction

Ampholip incompatible with heparin, and other physiological solutions containing electrolytes. The drug can not be mixed with other drugs. The presence of bacteriostatic additives (including benzyl alcohol) may lead to precipitation of the drug.

Special conditions

The likelihood of toxicity increases with prolonged treatment of drug Ampholip.

During the use of the drug requires regular (at least 1 time per week) Laboratory monitoring of renal function, hepatic and hemopoietic system. With extreme caution should be used Ampholip patients receiving concomitant nephrotoxic drugs.

When administered with a diabetes drug, patients should be taken into account that Ampholip 1 vial contains approximately 900 mg of sucrose.

Introduction Ampholip patients on hemodialysis, is possible only after the completion of dialysis treatment.

In appointing Ampholip patients taking potassium supplements, you need to carefully monitor the level of potassium and magnesium in the blood plasma.

Back pain, periodically appearing at / in the introduction, is held after stopping the infusion, or by decreasing the rate of administration, and typically does not occur again.

Despite the fact that during the period of treatment Ampholip there were no significant changes in the blood clotting system, please note that when applying Ampholip in a conventional dosage form may cause hemolysis.

When using a system for on / in the previously established for other purposes, the system must be rinsed with a 5% glucose solution for injection. If this is not possible, then Ampholip should be administered through a separate system.

Pregnancy and lactation

The safety of the drug during pregnancy and lactation has not been established.

The use of the drug during pregnancy is possible only when the intended benefits to the mother outweighs the potential risk to the fetus. If necessary, use during lactation should decide the issue of termination of breastfeeding.

Overdose

Treatment: In case of overdose, immediately stop the drug and carefully monitor renal function

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Weight	0.043 kg
Expiration date	2 years.
Dosage form	Infusion solution