Amphotec

1 What is Amphotec?

Brand: Amphotec

Generic: Amphotericin B Cholesteryl Sulfate Complex (Intravenous Route)

Amphotericin B (AMB) is widely used as an antifungal drug in order to treat subcutaneous and systemic mycoses.

This antifungal drug is a polyene antibiotic which alters cell membrane permeability by binding to ergosterol, thus causing leakage of cell components and subsequent fungal cell death.

Like fungi, leishmania has a high percentage of ergosterol and is susceptible to this antifungal antibiotic.

Amphotericin B cholesteryl sulfate complex is one of the newer AMB formulations. It is preferably used to overcome serious infections, such as aspergillosis, caused by a variety of fungi.

This medicine is available in powder form that is later dissolved in sterile water at the time of injection. You can get this product only with your doctor’s prescription.

2 What to Know Before Using

Amphotericin B (AMB) is obtained from Streptomyces nodosus. It is active against a wide range of yeasts and fungi – Candida albicans, Histoplasma capsulatum, Cryptococcus neoformans, Blastomyces dermatitidis, Coccidioides immitis, Torulopsis, Rhodotorula, Aspergillus, Sporothrix, etc. Dermatophytes are inhibited in vitro, but concentrations of AMB attained in the infected skin are low and ineffective.

It is fungicidal at high and static at low concentrations.

There are some new amphotericin B formulations. In an attempt to improve the tolerability of intravenous infusion of AMB, 3 new lipid formulations of AMB have been produced. They are:

  • Amphotericin B lipid complex (ABLC): contains 35% AMB incorporated in ribbon-like particles of dimyristoyl phospholipids.
  • Amphotericin B colloidal dispersion (ABCD): disc shaped particles containing 50% each of AMB and cholesteryl sulfate are prepared as an aqueous dispersion.
  • Liposomal amphotericin B (L-AMB): it has been produced to improve the tolerability of i.v. infusion of AMB, reduce its toxicity and achieve targeted delivery. It consists of 10% AMB incorporated in uniform sized (60-80 nM) unilamellar liposomes made up of lecithin and other biodegradable phospholipids.

If you are about to start this drug therapy, the risk and benefit ratio should be considered. This is a decision that your doctor will make with your active participation.

There are some important factors such as drug interaction, metabolic impairment, hypersensitivity reaction, pregnancy, lactation etc. which may alter the desired therapeutic effects of such medications.

Sometimes the presence of other health disorders affects the beneficial effects of this medicine and even may cause serious complications.

Make sure you mention your doctor if you have any other medical problems. The use of AMB liposome is contraindicated in patients with known hypersensitivity. This drug should not be given to the patients receiving antineoplastics.

In addition, certain drugs should not be used concurrently with such medications. It is always recommended to consult with your doctor if you are in need of some drugs for another health problem in order to avoid unwanted serious drug interactions.

Moreover, animal reproduction studies performed have failed to demonstrate a risk to the fetus and there are no adequate and well-controlled studies in pregnant women. Thus, this medicine can be used during pregnancy if clearly needed.

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3 Proper Usage

Amphotericin B (AMB) is the most effective drug for various types of systemic mycoses and is the gold standard of antifungal therapy.

The frequency of your daily drug administration and the duration of drug therapy depend on the particular medical problem for which you are taking the medicine. That’s why; the therapeutic dose may vary with patient’s condition or requirement.

In order to treat aspergillosis, both adults and children are usually treated with 3 to 4 milligrams amphotericin B cholesteryl sulfate complex per kilogram (1.36 to 1.81 mg per pound) of body weight, injected slowly into a vein, once in a day.

In general, such medications are given to the patients in a hospital. You should take this medicine in time until the prescribed course is finished.

If you miss any dose of this medicine, you should take it as soon as possible. But if it is time for your next dose, then you should skip the missed dose and go back to your regular treatment schedule.

You should store the medicine in a closed container at room temperature away from heat, moisture, and direct light. All kinds of medicines should be kept out of the reach of children.

Further, outdated medicines should be disposed of by an appropriate way.

4 Precautions to Take

Regular visits are recommended to make sure this medicine is working properly or not while you are receiving a drug therapy.

Additionally, you should be careful in order to avoid the unwanted drug interactions and other toxicity that may arise because of concurrent use of AMB with certain medicines.

It is safe to consult your doctor when you are in need of medicines for anther health problem. On the contrary, you should tell your healthcare professional if you are taking any of the medicines listed below. It will help your doctor in making a decision to pick up the appropriate drug.

There are some drug interactions associated with AMB which is discussed below:

  • Aminoglycosides, vancomycin, cyclosporine and other nephrotoxic drugs enhance the renal impairment caused by AMB.
  • Flucytosine has supra-additive action with AMB in the case of fungi sensitive to both (AMB increases the penetration of 5-FC into the fungus).
  • Rifampicin and minocycline, though not antifungal in their own right, potentiate AMB action.

Moreover, this drug should be used with great care in patients with renal and hepatic impairment and during pregnancy. Monitoring of renal and liver functions should be carried out to assess the condition of the patient.

5 Potential Side Effects

There are some unwanted side-effects associated with each drug that usually do not need medical attention.

These side-effects usually go away during the treatment episode as your body adjusts to the medicine. Your healthcare professional may advise you about the ways how to prevent or reduce those unwanted side-effects.

Sometimes you may need to consult with the doctor if you feel any serious toxic effects. Indeed, the toxicity of AMB is high but these effects are less likely to occur when the liposomal preparation is used.

Following side-effects are quite alarming and warrant immediate medical help:

Acute reaction: this occurs with each infusion and consists of chills, fever, aches and pain all over, nausea, vomiting and dyspnea lasting for 2-5 hours, probably due to the release of cytokines (IL, TNF-alpha).

When these are severe – the dose is increased gradually. Usually, the intensity of reaction decreases with continued medication. Injection of hydrocortisone 0.6 mg/kg with the infusion may reduce the intensity of the reaction. Thrombophlebitis of the injected vein can occur.

Long-term toxicity: nephrotoxicity is the most important. It occurs fairly uniformly and is dose-related: manifestations are –azotemia, reduced GFR, acidosis, hypokalemia, and inability to concentrate urine. It reverses slowly and often incompletely after stoppage of therapy.

Anaemia: most patients develop slowly progressing anaemia which is due to bone marrow depression. It is largely reversible.

CNS toxicity occurs only on intrathecal injection –headache, vomiting, nerve palsies, etc.

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