FUNGIZONE
Clinical safety rating: caution
Comprehensive clinical and safety monograph for FUNGIZONE (FUNGIZONE).
Binds to ergosterol in fungal cell membranes, forming pores that increase permeability, leading to leakage of intracellular contents and cell death.
| Metabolism | Not metabolized; excreted slowly via urine and bile. |
| Excretion | Primarily fecal (40-50%) via biliary elimination without metabolism; renal excretion of unchanged drug is minimal (<5% in 24 hours). |
| Half-life | Terminal elimination half-life is approximately 15 days (range 10-20 days) after a single dose; with prolonged therapy, a prolonged terminal half-life of up to 15 days reflects slow redistribution from tissue depots. |
| Protein binding | Approximately 90-95% bound, primarily to albumin and alpha-1-acid glycoprotein. |
| Volume of Distribution | Vd is approximately 4 L/kg (range 2-6 L/kg), indicating extensive tissue binding and distribution into organs such as liver, spleen, lungs, and kidney. |
| Bioavailability | Oral: <5% (negligible, not clinically useful); IV: 100% (complete); topical: not applicable (local effect, minimal systemic absorption). |
| Onset of Action | IV: Onset of antifungal effect occurs within 1-2 days, but clinical response typically seen after 3-7 days; topical: antifungal effects begin within 24-48 hours. |
| Duration of Action | IV: Antifungal activity persists for several days to weeks due to slow elimination; detectable levels may be found up to 4-6 weeks after cessation. Topical: duration varies with application regimen. |
| Action Class | Fungal cell membrane active agent |
| Brand Substitutes | Neotericin 50mg Injection, Amfocan 50mg Injection, Amtericin 50mg Injection, Fungitericin Injection, Mycoflu Injection |
IV: 0.25-1 mg/kg/day as a single infusion; for aspergillosis, up to 1.5 mg/kg/day; maximum daily dose 1.5 mg/kg.
| Dosage form | CREAM |
| Renal impairment | GFR >50 mL/min: no adjustment; GFR 10-50 mL/min: increase dosing interval to every 24-36 hours; GFR <10 mL/min: every 24-48 hours, consider alternative agent due to nephrotoxicity. |
| Liver impairment | Child-Pugh A: no adjustment; Child-Pugh B: reduce dose by 50%; Child-Pugh C: avoid use due to risk of hepatotoxicity. |
| Pediatric use | IV: 0.25-1 mg/kg/day; for severe infections up to 1.5 mg/kg/day; maximum 1.5 mg/kg/day. |
| Geriatric use | Start at lower end of dosing range (0.25 mg/kg/day); monitor renal function closely; adjust dose based on creatinine clearance. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for FUNGIZONE (FUNGIZONE).
| Breastfeeding | Amphotericin B is excreted into human breast milk in very small amounts; the milk-to-plasma ratio (M/P) is estimated at <0.1. However, its oral bioavailability is negligible (<5%), so systemic exposure to the nursing infant is minimal. The American Academy of Pediatrics considers amphotericin B compatible with breastfeeding. Monitor infant for diarrhea or rash, though adverse effects are unlikely. |
| Teratogenic Risk | FUNGIZONE (amphotericin B deoxycholate) is classified as FDA Pregnancy Category B. Animal studies have not demonstrated teratogenic effects; however, no adequate and well-controlled studies exist in pregnant women. Administration during the first trimester is associated with a theoretical risk of embryo-fetal toxicity only at maternally toxic doses. During the second and third trimesters, the drug crosses the placenta minimally, and no specific fetal malformations have been consistently reported. Use only if clearly needed and if the potential benefit outweighs the unknown fetal risks. |
■ FDA Black Box Warning
Amphotericin B should be used primarily for treatment of patients with progressive and potentially life-threatening fungal infections; it is not intended for noninvasive forms of fungal disease. The drug should be administered by intravenous infusion only, and dosage should be individualized. Hospitalization is recommended during the initial course of therapy.
| Serious Effects |
["Hypersensitivity to amphotericin B or any component of the formulation","Severe bone marrow suppression (relative)"]
| Precautions | Nephrotoxicity, infusion-related reactions (fever, chills, rigors, hypotension, bronchospasm), cardiotoxicity (arrhythmias), hepatotoxicity, anaphylaxis, electrolyte disturbances (hypokalemia, hypomagnesemia), and bone marrow suppression. |
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| Fetal Monitoring | Monitor maternal renal function (serum creatinine, BUN), electrolytes (potassium, magnesium, calcium, sodium), liver function tests, and complete blood counts every 1-2 weeks. Assess for infusion-related reactions (fever, rigors, hypotension, hypoxemia) during administration. In pregnancy, monitor fetal growth and well-being via ultrasound and non-stress tests if maternal condition warrants; no specific fetal monitoring is mandatory for the drug itself. |
| Fertility Effects | Amphotericin B has not been studied for its effects on human fertility. Animal studies (rats) at high doses have shown reduced fertility and impaired spermatogenesis at toxic doses. In humans, no data suggest significant impairment of fertility at therapeutic doses, but caution is advised in patients of reproductive potential. |