Abelcet (amphotericin B lipid complex)
Last reviewed · Source: First Databank (FDB) drug data
Overview
Amphotericin B, a macrocyclic polyene, is an antifungal agent.
Amphotericin B is an antifungal antibiotic produced by Streptomyces nodosus. The drug is commercially available as amphotericin B formulated with sodium desoxycholate (conventional amphotericin B) and amphotericin B liposomal (lipid formulation). The lipid formulation contains a lipid-based drug delivery system that may improve the toxicity profile of amphotericin B, but also can affect pharmacokinetics and functional properties of the drug.
Amphotericin B liposomal contains amphotericin B intercalated into a unilamellar bilayer liposomal membrane composed of hydrogenated soy phosphatidylcholine (HSPC), cholesterol, distearoylphosphatidylglycerol, and alpha-tocopherol.
Amphotericin B usually is fungistatic in action at concentrations obtained clinically, but may be fungicidal in high concentrations or against very susceptible organisms. Amphotericin B exerts its antifungal activity principally by binding to sterols (e.g., ergosterol) in the fungal cell membrane. As a result of this binding, the cell membrane is no longer able to function as a selective barrier and leakage of intracellular contents occurs.
Cell death occurs in part as a result of permeability changes by which monovalent ions (sodium, potassium, hydrogen, and chloride) leak out of the cell. Binding to sterols in mammalian cells (such as certain kidney cells and erythrocytes) may account for some of the toxicities reported with conventional amphotericin B therapy.
The pharmacokinetics of amphotericin B vary substantially depending on whether the drug is administered as conventional amphotericin B (formulated with sodium desoxycholate) or amphotericin B liposomal, and pharmacokinetic parameters reported for one amphotericin B formulation should not be used to predict the pharmacokinetics of any other amphotericin B formulation. The manufacturers' literature and specialized references should be consulted for information regarding the absorption, distribution, or elimination of amphotericin B administered as amphotericin B liposomal.
After an initial IV infusion of 1-5 mg of amphotericin B daily, with dosage gradually increased to 0.4-0.6 mg/kg daily, plasma concentrations ranging from approximately 0.5-2 mcg/mL were reported. Following a rapid initial decrease, plasma concentrations plateau at about 0.5 mcg/mL. The pharmacokinetics of amphotericin B following administration of amphotericin B liposomal are nonlinear, with greater than proportional increases in serum concentrations observed with dosage increases from 1 mg/kg daily to 5 mg/kg daily.
Steady state concentrations of amphotericin B are attained within 4 days of initiating amphotericin B liposomal.
Amphotericin B concentrations attained in inflamed pleura, peritoneum, synovium, and aqueous humor following IV administration of conventional amphotericin B reportedly are about 60% of concurrent plasma concentrations. Penetration into vitreous humor is low. Following administration of amphotericin B liposomal mean trough concentrations of amphotericin B, although variable, generally remain constant with repeated daily administration over the dosage range of 1-5 mg/kg per day.
Following IV administration of conventional amphotericin B, CSF concentrations of the drug rarely exceed 2.5% of concurrent serum concentrations. Low concentrations of amphotericin B are attained in amniotic fluid. It is not known whether amphotericin B is distributed into milk.
Amphotericin B is more than 90% bound to plasma proteins.
The metabolic fate of amphotericin B in humans has not been fully elucidated. Following IV administration of conventional amphotericin B in patients whose renal function is normal prior to therapy, the initial plasma half-life is approximately 24 hours. After the first 24 hours, the rate at which amphotericin B is eliminated decreases and an elimination half-life of approximately 15 days for conventional amphotericin B has been reported.
Conventional amphotericin B is eliminated very slowly (over weeks to months) by the kidneys. Over a 7-day period, the cumulative urinary excretion of a single dose of conventional amphotericin B is about 40% of the administered drug. It has been estimated that only about 2-5% of a total dose of amphotericin B is excreted in urine unchanged.
When conventional IV amphotericin B therapy is discontinued, the drug can be detected in the urine for at least 7 weeks due to its slow disappearance. The elimination half-life of amphotericin B liposomal ranges on average from 7-10 hours, although based on concentrations assessed 49 days after the final dose, mean half-lives ranged from 100-153 hours. This elimination half-life is likely due to a slow redistribution of amphotericin from tissues.
Amphotericin B is not hemodialyzable.
USES: This medication is used to treat a variety of serious fungal infections. It is often used in patients who cannot tolerate or who do not respond to the regular amphotericin treatment. It works by stopping the growth of fungi.
Generic name: amphotericin B lipid complex
Pronunciation: (AM-foe-TER-i-sin/LIP-id)
Reference product & biosimilars
No reference, biosimilar or interchangeable associated with this drug.
Today’s intelligence on Abelcet
Indications
The following indications are listed for Abelcet:
- Aspergillosis
- Blastomycosis
- Candida Peritonitis
- Candidal Endocarditis
- Candidal Meningitis
- Candidal Septicemia
- Candidemia
- Candidiasis
- Coccidioidomycosis
- Cryptococcal Septicemia
- Cryptococcosis
- Disseminated Candidiasis
- Disseminated Sporotrichosis
- Fungal Endocarditis
- Fungal Infection Of Lung
- Fungal Meningitis
- Fungal Sepsis
- Fungal Urinary Tract Infection
- Histoplasmosis
- Leishmaniasis
- Mucormycosis
- Pulmonary Cryptococcosis
- Rhinocerebral Phycomycosis
Also known as: Blastomycotic Infection, Busse-Buschke Disease, California Disease, Candida Species Peritonitis, Candida Spp. Peritonitis, Candidal Infection, Candidal Sepsis, Candidosis, Coccidioidal Granuloma, Cryptococcal Infection, Cryptococcal Sepsis, Darling's Disease, Disseminated Candidosis, Disseminated Moniliasis, Endocardial Candidiasis, Endocardial Moniliasis, Fungal Pneumonia, Fungal Septicemia, Gilchrist's Disease, Infection With Cryptococcus Neoformans, Meningeal Candidiasis, Meningeal Moniliasis, Moniliasis, Mycotic Pneumonia, Mycotic Sepsis, Mycotic Septicemia, North American Blastomycosis, Phycomycetosis, Phycomycosis, Posada-Wernicke Disease, Posadas Disease, Posadas Mycosis, Pulmonary Busse-Buschke Disease, Pulmonary Cryptococcal Infection, Pulmonary Torulosis, Rhinocerebral Mucormycosis, Rhinocerebral Phycomycetosis, Rhinocerebral Zygomycosis, Septic Candidiasis, Septic Moniliasis, Torulosis, Uti Due To A Fungus, Zygomycosis.
Dosing
Amphotericin B is available as conventional amphotericin B (formulated with sodium desoxycholate) or amphotericin B liposomal (AmBisome(R)); dosage is expressed as amphotericin B.
Dosage of amphotericin B varies depending on whether the drug is administered as conventional amphotericin B (formulated with sodium desoxycholate) or amphotericin B liposomal. Dosage recommendations for the specific formulation being administered should be followed.
No dosing information is available for this tab.
No dosing information is available for this tab.
No dosing information is available for this tab.
Drug interactions
Systematic drug interaction studies have not been performed to date using amphotericin B liposomal. The fact that drug interactions reported with conventional IV amphotericin B could also occur with the lipid formulation of the drug should be considered.
There are no contraindication interactions for this drug.
There are no severe interactions for this drug.
There are no moderate interactions for this drug.
Contraindications
*Hypersensitivity to amphotericin B or any other component in the respective formulation. The manufacturers of conventional amphotericin B and amphotericin B liposomal suggest that use of these drugs can be considered in patients with hypersensitivity if the clinician determines that the benefits of such therapy outweigh the risks.
There are no contraindication contraindications for this drug.
There are no severe contraindications for this drug.
There are no moderate contraindications for this drug.
Adverse reactions
The most commonly reported adverse effects reported with conventional amphotericin B include fever (sometimes accompanied by chills), malaise, weight loss, hypotension, tachypnea, anorexia, nausea, vomiting, diarrhea, dyspepsia, cramping epigastric pain, normochromic, normocytic anemia, pain at the injection site (with or without phlebitis or thrombophlebitis), generalized pain (including muscle/joint pains), headache, and decreased renal function and renal function abnormalities (e.g., azotemia, hypokalemia, hyposthenuria, renal tubular acidosis, nephrocalcinosis).
In a study of amphotericin B liposomal as empiric therapy in adults, the only adverse effects reported more frequently than with conventional IV amphotericin B and in >=20% of patients were diarrhea and rash. Amphotericin B liposomal is associated with a lower overall incidence of chills, changes in blood pressure, tachycardia, hypoxia, hypokalemia, and various adverse effects related to renal toxicity than the conventional formulation of the drug.
There are no severe adverse reactions for this drug.
There are no less severe adverse reactions for this drug.
Precautions
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Although safety and efficacy of conventional IV amphotericin B in pediatric patients have not been established through adequate and well-controlled studies, the drug has been used effectively to treat systemic fungal infections in pediatric patients without unusual adverse effects. The manufacturers state that the lowest effective dosage of the drug should be employed whenever conventional IV amphotericin B is used in pediatric patients.
IV amphotericin B liposomal has been administered to pediatric patients 1 month to 16 years of age without any unusual adverse effects. In clinical studies of 302 pediatric patients, there were no differences in efficacy or safety of IV amphotericin B liposomal when compared to adult patients. In a large, double-blind study comparing the safety and efficacy of amphotericin B liposomal and conventional IV amphotericin B, the incidence of chills, vomiting, hypokalemia, or hypertension in patients 16 years of age or younger ranged from 10-37% in those receiving amphotericin B liposomal and from 21-68% in those receiving the conventional formulation of the drug.
Safe use of amphotericin B during pregnancy has not been established. Conventional IV amphotericin B has been used to treat systemic fungal infections or visceral leishmaniasis in a limited number of pregnant women without obvious adverse effects to the fetus. While reproduction studies in rats and rabbits using conventional amphotericin B or amphotericin B liposomal have not revealed evidence of harm to the fetus, rabbits receiving amphotericin B liposomal dosages equivalent to 0.5-2 times the usual human dosage experienced a higher rate of spontaneous abortions than the control group. However, animal reproduction studies are not always predictive of human response. There are no adequate or controlled studies to date using any amphotericin B formulation in pregnant women, and these drugs should be used during pregnancy only when clearly needed.
It is not known whether amphotericin B is distributed into human milk. Because many drugs are distributed into human milk and because of the potential for serious adverse reactions to amphotericin B in nursing infants if it were distributed, a decision should be made whether to discontinue nursing or the drug, taking into account the importance of the drug to the woman.
Although clinical experience to date indicates that dosage modification is unnecessary when amphotericin B liposomal is used in geriatric patients, the manufacturer recommends that these patients be carefully monitored while receiving the drug.
While safety and efficacy of conventional IV amphotericin B and amphotericin B liposomal have not been studied specifically in geriatric patients, no unusual age-related adverse effects have been reported when the drugs were used in patients 65 years of age or older. Although dosage modifications are usually unnecessary, carefully monitor during treatment.
ICD codes
No ICD codes are available for this drug.
Formulary status
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Last reviewed · Source: First Databank (FDB) drug data
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