Amphotericin B


Concise Prescribing Info
Indications/Uses
Listed in Dosage.
Dosage/Direction for Use
Adult : PO Oral candidiasis Dissolve 1 lozenge in the mouth 4 times/day after meals and at bedtime for 7-14 days. IV Severe systemic fungal infections As conventional amphotericin B: Test dose 1 mg infused over 20-30 minutes. Then, initially, 0.25 mg/kg/day, gradually increase to 1 mg/kg/day, according to response and tolerance. In seriously ill patients, gradually increase dose up to a total of 1.5 mg/kg/day or on alternate days. Doses are given via slow infusion over 2-6 hours. Max total daily dose: 1.5 mg/kg. If treatment is interrupted for more than 7 days, restart at 0.25 mg/kg daily and increase slowly. As liposomal amphotericin B: Test dose 1 mg infused over 10 minutes, then 3 mg/kg once daily given via infusion over 30-60 minutes. Max: 5 mg/kg/day. As lipid complex amphotericin B: In patients not responding to conventional amphotericin B or to other antifungal drugs: Test dose 1 mg infused over 15 minutes, then 5 mg/kg once daily via infusion at a rate of 2.5mg/kg/hour. Duration of treatment: At least 14 days. Empiric treatment of presumed fungal infection in febrile neutropenic patients As liposomal amphotericin B: Test dose 1 mg infused over 10 minutes, then 3 mg/kg once daily given via infusion over 30-60 minutes. Max: 5 mg/kg daily. Visceral leishmaniasis As liposomal amphotericin B: A total dose of 21-30 mg/kg via infusion given over for 10-21 days.
Dosage Details
Intravenous
Severe systemic fungal infections
Adult: As conventional amphotericin B: Test dose 1 mg infused over 20-30 minutes. Then, initially, 0.25 mg/kg daily, gradually increase to 1 mg/kg daily, according to response and tolerance. In seriously ill patients, gradually increase dose up to a total of 1.5 mg/kg daily or on alternate days. Doses are given via slow infusion over 2-6 hours. Max total daily dose: 1.5 mg/kg. If treatment is interrupted for more than 7 days, restart at 0.25 mg/kg daily and increase slowly. As liposomal amphotericin B: Test dose 1 mg infused over 10 minutes, then 3 mg/kg once daily given via infusion over 30-60 minutes. Max: 5 mg/kg daily. As lipid complex amphotericin B: In patients not responding to conventional amphotericin B or to other antifungal drugs: Test dose 1 mg infused over 15 minutes, then 5 mg/kg once daily via infusion at a rate of 2.5mg/kg/hour. Duration of treatment: At least 14 days.

Intravenous
Visceral leishmaniasis
Adult: As liposomal amphotericin B: A total dose of 21-30 mg/kg via infusion given over for 10-21 days.

Intravenous
Fungal infection
Adult: As empiric treatment of presumed infection in febrile neutropenic patients: As liposomal amphotericin B: Test dose 1 mg infused over 10 minutes, then 3 mg/kg once daily given via infusion over 30-60 minutes. Max: 5 mg/kg daily.

Oral
Oral candidiasis
Adult: As lozenge: Dissolve 1 lozenge in the mouth 4 times daily for 7-14 days.
Reconstitution
Conventional amphotericin B: Reconstitute with 10 mL sterile water for inj (without preservatives); further dilute with dextrose 5% inj. Liposomal amphotericin B: Reconstitute with 12 mL sterile water for inj (without preservatives); further dilute with dextrose 5% to a final concentration of 1-2 mg/mL. Lipid complex amphotericin B: Dilute with dextrose 5% to a concentration of 1 mg/mL.
Incompatibility
Incompatible with NaCl 0.9% or electrolyte solutions.
Contraindications
Hypersensitivity.
Special Precautions
Patient receiving leukocyte transfusion. Renal impairment. Pregnancy and Lactation. Lipid-based and conventional formulations should not be used interchangeably.
Adverse Reactions
Significant: Anaphylactic reactions, infusion reactions (e.g. fever, shaking, chills, hypotension. anorexia, nausea, vomiting, headache, and tachypnoea), leucoencephalopathy, anaemia, nephrotoxicity, myocardial toxicity, acute pulmonary toxicity.
Blood and lymphatic system disorders: Leukocytosis, leucopenia, thrombocytopenia, hyperbilirubinaemia.
Cardiac disorders: Chest pain, tachycardia, dyspnoea.
Gastrointestinal disorders: Diarrhoea, epigastric pain, stomach cramps, constipation.
Infections and infestations: Infection, sepsis.
Injury, poisoning and procedural complications: Arachnoiditis, injection site pain, phlebitis.
Investigations: Raised serum alkaline phosphatase, ALT, AST, creatinine, BUN.
Metabolism and nutrition disorders: Peripheral oedema, oedema, hypokalaemia, hypomagnesaemia, hypocalcaemia, hyponatraemia, hypervolaemia.
Musculoskeletal and connective tissue disorders: Back pain.
Nervous system disorders: Neuralgia, paraesthesia.
Psychiatric disorders: Delirium, insomnia, anxiety, confusion.
Renal and urinary disorders: Azotaemia, renal tubular acidosis, nephrocalcinosis, urinary retention, haematuria.
Respiratory, thoracic and mediastinal disorders: Cough.
Skin and subcutaneous tissue disorders: Skin rash, pruritus.
Vascular disorders: Flushing, hypertension.
IV/Parenteral: B
MonitoringParameters
Monitor renal function frequently during therapy; BUN and serum creatinine every other day while tapering doses and weekly thereafter; electrolytes, primarily K, Mg; LFT, CBC, PT/PTT, temperature, input and output. Monitor for signs of hypokalaemia.
Overdosage
Symptoms: Potentially fatal cardiac or cardiopulmonary arrest. Management: Symptomatic and supportive treatment.
Drug Interactions
May potentiate nephrotoxicity with nephrotoxic drugs (e.g. ciclosporin). Increased risk of hypotension, bronchospasm, and nephrotoxicity with antineoplastics. Increased risk of hypokalaemia with corticosteroids, corticotropin, loop and thiazide diuretics. May increase the toxicity of flucytosine and digitalis. May enhance the curariform effect of skeletal muscle relaxants (e.g. tubocurarine).
Lab Interference
Liposomal amphotericin B: May cause falsely elevated serum phosphate result using PHOSm assay.
Action
Description: Amphotericin B, is a polyene antifungal antibiotic which interferes with cell membrane permeability by binding to ergosterol, causing intracellular content leakage and eventually cell death.
Pharmacokinetics:
Absorption: Little to no absorption from the gastrointestinal tract. Time to peak plasma concentration: Within 1 hour after a 4- to 6-hour dose (conventional).
Distribution: Crosses placenta. Distributed in the aqueous humor, bile, pericardial fluid, pleural fluid, and synovial fluid (conventional); high concentration in the liver, spleen, and lung (lipid complex). Volume of distribution: 0.1-0.16 L/kg (liposomal); 4 L/kg (conventional); 131 L/kg (lipid complex). Plasma protein binding: 90% (conventional).
Excretion: Via urine (2-5% as biologically active form [conventional]; 0.9% [lipid complex]). Elimination half-life: 15 days (conventional); 7-10 hours (liposomal); 173 hours (lipid complex).
Chemical Structure

Chemical Structure Image
Amphotericin B

Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 5280965, Amphotericin b. https://pubchem.ncbi.nlm.nih.gov/compound/Amphotericin-b. Accessed Sept. 24, 2020.

Storage
Store between 2-8°C. Protect from light. Do not freeze. Reconstituted conventional amphotericin B soln: Stable for not more than 8 hours when stored at room temp or for 24 hours when stored between 2-8°C. Reconstituted liposomal amphotericin B soln: Stable for 24 hours when stored between 2-8°C. Reconstituted lipid complex amphotericin B soln: Stable for 6 hours when stored at room temp or for 48 hours when stored between 2-8°C. Lozenge: Store below 25°C.
MIMS Class
ATC Classification
J02AA01 - amphotericin B ; Belongs to the class of antibiotics. Used in the systemic treatment of mycotic infections.
A01AB04 - amphotericin B ; Belongs to the class of local antiinfective and antiseptic preparations. Used in the treatment of diseases of the mouth.
References
Abelcet 100 mg (Leadiant Biosciences, Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 04/09/2020.

Abelcet Lipid Complex 5 mg/mL Concentrate for Dispersion for Infusion (Teva Pharma B.V.). MHRA. https://products.mhra.gov.uk/. Accessed 04/09/2020.

AmBisome Liposomal 50 mg Powder for Dispersion for Infusion (Gilead Sciences International Limited). MHRA. https://products.mhra.gov.uk/. Accessed 04/09/2020.

AmBisome Liposome for Injection (Astellas Pharma US, Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 04/09/2020.

Amphostal 50 mg Powder for Sterile Concentrate (Stallion Laboratories PVT. LTD.). MIMS Philippines. http://www.mims.com/philippines. Accessed 07/09/2020.

Amphotericin B Injection, Powder, Lyophilized, for Solution (X-GEN Pharmaceuticals, Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 04/09/2020.

Anon. Amphotericin B (Conventional). Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 04/09/2020.

Anon. Amphotericin B (Lipid Complex). Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 04/09/2020.

Anon. Amphotericin B (Liposomal). Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 04/09/2020.

Anon. Amphotericin B. AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com. Accessed 04/09/2020.

Buckingham R (ed). Amphotericin B. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 04/09/2020.

Fungizone 50 mg Power for Sterile Concentrate (Cheplapharm Arzneimittel GmbH). MHRA. https://products.mhra.gov.uk/. Accessed 04/09/2020.

Joint Formulary Committee. Amphotericin B. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 11/09/2020.

Disclaimer: This information is independently developed by MIMS based on Amphotericin B from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2020 MIMS. All rights reserved. Powered by MIMS.com
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