Amphotericin B

What is Amphotericin B?

• Amphotericin B (Amphocin; Fungizone; Ambisome), is an antifungal polyene antibiotic obtained from a strain of Streptomyces nodosus.

Amphotericin B new

What are the uses of this medicine?

Amphotericin B (Amphocin; Fungizone; Ambisome), is specifically intended to treat potentially life-threatening fungal infections:

• aspergillosis, cryptococcosis (torulosis), North American blastomycosis, systemic candidiasis, coccidioido-mycosis, histoplasmosis, zygomycosis including mucormycosis due to susceptible species of the genera Absidia, Mucor and Rhizopus, and infections due to related susceptible species of Conidiobolus and Basidiobolus, and sporotrichosis.
• Amphotericin B may be useful in the treatment of American mucocutaneous leishmaniasis, but it is not the drug of choice as primary therapy.

Limittaions of use:

• Amphotericin B for Injection USP should be administered primarily to patients with progressive, potentially life-threatening fungal infections.
• This potent drug should not be used to treat noninvasive fungal infections, such as oral thrush, vaginal candidiasis and esophageal candidiasis in patients with normal neutrophil counts.

Amphotericin b

How does this medicine work?

• Amphotericin (am" foe ter' i sin) B is a polyene macrolide antibiotic that acts by binding to sterols in the plasma membranes of fungi causing the cells to leak, eventually leading to fungal cell death.

Amphotericin B shows a high order of in vitro activity against many species of fungi as fallows:

• Histoplasma capsulatum, Coccidioides immitis, Candida species, Blastomyces dermatitidis, Rhodotorula, Cryptococcus neoformans, Sporothrix schenckii, Mucor mucedo, and Aspergillus fumigatus.
• Candida albicans is generally quite susceptible to amphotericin B, non-albicans species may be less susceptible.
• Pseudallescheria boydii and Fusarium sp. are often resistant to amphotericin B.

Amphotericin-B-based-on-iodoacetyl-xtal-Mercury-3D-bs

Who Should Not Use this medicine ?

This medicine cannot be used in patients who:

• have shown hypersensitivity to amphotericin B or any other component in the formulation.

What drug interactions can this medicine cause?

• Tell your healthcare provider about all the medicines you take, including prescription and over-the-counter medicines, vitamins, and herbal supplements.

Be sure to mention any of the following:

• aminoglycoside antibiotics such as amikacin, gentamicin, or tobramycin (Bethkis, Kitabis Pak, Tobi)
• antifungals such as clotrimazole, fluconazole (Diflucan), itraconazole (Onmel, Sporanox), ketoconazole (Extina, Nizoral, Xolegel), and miconazole (Oravig, Monistat)
• corticotropin (H.P. Acthar Gel)
• cyclosporine (Gengraf, Neoral, Sandimmune)
• digoxin (Lanoxin)
• flucytosine (Ancobon)
• medications for the treatment of cancer such as nitrogen mustard
• pentamidine (Nebupent, Pentam)
• oral steroids such as dexamethasone, methylprednisolone (Medrol), and prednisone (Rayos)

Is this medicine FDA approved?

• Amphotericin B was approved by the FDA in 1971 and is currently widely used in the treatment of serious fungal infections. Amphotericin B is insoluble in water and is formulated for intravenous use by complexing it with lipotrophic molecules such as deoxycholate, liposomes or lipid complexes.

How should this medicine be used?

Recommended dosage:

• Therapy is usually initiated with a daily dose of 0.25 mg/kg of body weight.
• However, in those patients having severe and rapidly progressive fungal infection, therapy may be initiated with a daily dose of 0.3 mg/kg of body weight.
• In patients with impaired cardio-renal function or a severe reaction to the test dose, therapy should be initiated with smaller daily doses (i.e., 5 to 10 mg).
• Depending on the patient's cardio-renal status, doses may gradually be increased by 5 to 10 mg per day to final daily dosage of 0.5 to 0.7 mg/kg.

Sporotrichosis:

• Therapy with intravenous amphotericin B for sporotrichosis has ranged up to nine months with a total dose up to 2.5 g.

Aspergillosis:

• Aspergillosis has been treated with amphotericin B intravenously for a period up to 11 months with a total dose up to 3.6 g.

Rhinocerebral phycomycosis:

• A cumulative dose of at least 3 g of amphotericin B is recommended to treat rhinocerebral phycomycosis.

Administration:

• Amphotericin B is administered intravenously as an infusion.
• The medication is usually prepared as a sterile powder or a lipid-based formulation, which needs to be reconstituted or diluted before administration.
• Healthcare professionals will prepare the medication according to the instructions provided by the manufacturer.
• The dosage, infusion rate, and duration of treatment will be determined by the healthcare provider based on the specific fungal infection being treated, the patient's weight, renal function, and other factors.
• Amphotericin B infusions are typically given in a hospital or clinical setting under the supervision of healthcare professionals.
• The infusion may be given slowly over a few hours to minimize the risk of infusion-related reactions.

Pre-medication and Monitoring:

• To minimize infusion-related reactions, patients often receive pre-medication prior to the administration of amphotericin B. This may include medications such as antipyretics, antihistamines, corticosteroids, or antiemetics. The specific pre-medication regimen will be determined by the healthcare provider.
• Vital signs, including blood pressure, heart rate, and temperature, are monitored before, during, and after the infusion.
• Blood tests, including renal function tests and electrolyte levels, are performed regularly to monitor the patient's response to treatment and detect any potential adverse effects.

Reconstitution and Dilution:

• If amphotericin B is supplied as a powder, it needs to be reconstituted according to the manufacturer's instructions. This typically involves adding a specific volume of sterile water for injection to the vial.
• The reconstituted solution is then further diluted with a compatible infusion solution, such as normal saline or dextrose solution, to achieve the desired concentration for administration.
• The reconstituted and diluted solutions should be prepared aseptically, following proper sterile technique, to prevent contamination.

What are the dosage forms and brand names of this medicine?

This medicine is available in fallowing doasage form:

• As single vials providing 50 mg amphotericin B

This medicine is available in fallowing brand namesː

• Amphotericin is available in multiple forms and concentrations generically and under the brand names Amphocin and Fungizone (deoxycholate), Ambisome (liposome), Abelcet (lipid complex), and Amphotec (cholesteryl sulfate complex).

What side effects can this medication cause?

The most common side effects of this medicine include:

• General (body as a whole): fever (sometimes accompanied by shaking chills usually occurring within 15 to 20 minutes after initiation of treatment); malaise; weight loss.
• Cardiopulmonary: hypotension; tachypnea.
• Gastrointestinal: anorexia; nausea; vomiting; diarrhea; dyspepsia; cramping epigastric pain.
• Hematologic: normochromic, normocytic anemia.
• Local: pain at the injection site with or without phlebitis or thrombophlebitis.
• Musculoskeletal: generalized pain, including muscle and joint pains.
• Neurologic: headache.
• Renal:decreased renal function and renal function abnormalities.

Less common side effects may include:

• General (body as a whole): flushing.
• Allergic: anaphylactoid and other allergic reactions; bronchospasm; wheezing.
• Cardiopulmonary: cardiac arrest; shock; cardiac failure; pulmonary edema; hypersensitivity pneumonitis; arrhythmias, including ventricular fibrillation; dyspnea; hypertension.
• Dermatologic: rash, in particular maculopapular; pruritus. Skin exfoliation, toxic epidermal necrolysis, and Stevens-Johnson syndrome have been reported during post-marketing surveillance.
• Gastrointestinal: acute liver failure; hepatitis; jaundice; hemorrhagic gastroenteritis; melena.
• Hematologic: agranulocytosis; coagulation defects; thrombocytopenia; leukopenia; eosinophilia; leukocytosis.
• Neurologic: convulsions; hearing loss; tinnitus; transient vertigo; visual impairment; diplopia; peripheral neuropathy; encephalopathy; other neurologic symptoms.
• Renal: acute renal failure; anuria; oliguria.

What special precautions should I follow?

• Amphotericin B is frequently the only effective treatment available for potentially life-threatening fungal disease.
• Amphotericin B should be administered intravenously under close clinical observation by medically trained personnel.
• Acute reactions including fever, shaking chills, hypotension, anorexia, nausea, vomiting, headache, and tachypnea are common 1 to 3 hours after starting an intravenous infusion. These reactions are usually more severe with the first few doses of amphotericin B and usually diminish with subsequent doses.
• Rapid intravenous infusion has been associated with hypotension, hypokalemia, arrhythmias, and shock and should, therefore, be avoided.
• Amphotericin B should be used with care in patients with reduced renal function; frequent monitoring of renal function is recommended.
• Since acute pulmonary reactions have been reported in patients given amphotericin B during or shortly after leukocyte transfusions, it is advisable to temporarily separate these infusions as far as possible and to monitor pulmonary function.
• Leukoencephalopathy has been reported following use of amphotericin B.
• Whenever medication is interrupted for a period longer than 7 days, therapy should be resumed by starting with the lowest dosage level, e.g., 0.25 mg/kg of body weight, and increased gradually.
• It is not known whether amphotericin B is excreted in human milk. Because many drugs are excreted in human milk and considering the potential toxicity of amphotericin B, it is prudent to advise a nursing mother to discontinue nursing.
• Amphotericin B commonly causes mild to moderate serum aminotransferase elevations and can cause hyperbilirubinemia, but acute, clinically apparent drug induced liver injury from amphotericin B therapy is exceedingly rare.

What to do in case of emergency/overdose?

Symptoms of overdose may include:

• potentially fatal cardiac or cardiopulmonary arrest.

Management of overdosage:

• In case of overdose, call the poison control helpline of your country. In the United States, call 1-800-222-1222.

• Overdose related information is also available online at poisonhelp.org/help.
• In the event that the victim has collapsed, had a seizure, has trouble breathing, or can't be awakened, immediately call emergency services. In the United States, call 911.
• If an overdose is suspected, discontinue therapy and monitor the patient's clinical status (e.g., cardiorespiratory, renal, and liver function, hematologic status, serum electrolytes) and administer supportive therapy, as required.
• Amphotericin B is not hemodialyzable.

Can this medicine be used in pregnancy?

• Pregnancy Category B.
• Because animal reproduction studies are not always predictive of human response, and adequate and well-controlled studies have not been conducted in pregnant women, this drug should be used during pregnancy only if clearly indicated.

Can this medicine be used in children?

• Safety and effectiveness in pediatric patients have not been established through adequate and well-controlled studies.

What are the active and inactive ingredients in this medicine?

Active ingredient:

• amphotericin b

Inactive ingredients:

• deoxycholic acid
• sodium phosphate, dibasic
• sodium phosphate, monobasic, monohydrate
• phosphoric acid
• sodium hydroxide
• nitrogen

Who manufactures and distributes this medicine?

Manufactured for:

• XGen Pharmaceuticals DJB, Inc.
• Big Flats, NY

What should I know about storage and disposal of this medication?

• Prior to reconstitution Amphotericin B for Injection USP should be stored under refrigeration, 2˚ to 8˚C (36˚to 46˚F), protected against exposure to light.
• The concentrate may be stored in the dark, at room temperature for 24 hours, or at refrigerator temperatures for one week with minimal loss of potency and clarity.
• Any unused material should then be discarded.
• Solutions prepared for intravenous infusion (0.1 mg or less amphotericin B per mL) should be used promptly after preparation and should be protected from light during administration.

• Dailymed label info on Amphotericin B
• FDA Amphotericin B

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