MYCAMINE
Clinical safety rating: caution
Comprehensive clinical and safety monograph for MYCAMINE (MYCAMINE).
Micafungin is an echinocandin antifungal that inhibits the synthesis of 1,3-β-D-glucan, an essential component of the fungal cell wall, leading to osmotic instability and cell death.
| Metabolism | Micafungin undergoes hepatic metabolism via arylsulfatase and catechol-O-methyltransferase pathways, with minor involvement of CYP450 enzymes. It is a substrate of CYP3A4 but not a major pathway. |
| Excretion | Primarily excreted unchanged via feces (approximately 28%) and to a lesser extent via urine (approximately 15%). Overall, elimination is primarily non-renal with biliary/fecal excretion as the major route. Less than 1% is excreted as metabolites. |
| Half-life | Terminal elimination half-life is approximately 14.3 hours (range 11–17 hours) in healthy adults. In pediatric patients, half-life is shorter (approximately 10–12 hours). Clinically, steady state is achieved by day 3 with daily dosing. |
| Protein binding | Highly protein bound (≥99%) primarily to albumin. Also binds to alpha-1-acid glycoprotein. Binding is linear over the therapeutic concentration range. |
| Volume of Distribution | Volume of distribution at steady state (Vdss) is approximately 0.39 L/kg (range 0.28–0.55 L/kg) in adults. This low Vd indicates limited extravascular distribution, consistent with high protein binding and primarily intravascular localization. |
| Bioavailability | Not applicable; mycamine (micafungin) is only available as an intravenous formulation. Oral bioavailability is negligible and not used clinically. |
| Onset of Action | Intravenous administration: Antifungal effects begin within hours following infusion; however, clinically significant antifungal activity is observed within 24–48 hours after the first dose. |
| Duration of Action | Duration of antifungal activity extends beyond the dosing interval due to prolonged half-life. With once-daily dosing, therapeutic concentrations are maintained throughout the 24-hour interval. Post-antifungal effect may persist for several hours after concentrations fall below MIC. |
| Molecular Weight | 1292.3 |
| Action Class | Fungal cell wall synthesis inhibitor (Echiocandins) |
| Brand Substitutes | Ibimica 50mg Injection, Micalan Injection, Micanfa 50mg Injection, Fungofine 50mg Injection, Micazar 50mg Injection, Micaggin 100mg Injection, Brumica 100mg Injection, Micafung Plus 100mg Injection |
100 mg IV once daily for invasive candidiasis; 150 mg IV once daily for esophageal candidiasis.
| Dosage form | INJECTABLE |
| Renal impairment | No dose adjustment required for any degree of renal impairment. |
| Liver impairment | No dose adjustment for mild-to-moderate hepatic impairment (Child-Pugh class A and B). Insufficient data for severe hepatic impairment (Child-Pugh class C); use with caution. |
| Pediatric use | For neonates and infants <4 months: weight <40 kg: 10 mg/kg IV once daily. For children ≥4 months and adolescents: weight <40 kg: 2 mg/kg IV once daily; weight ≥40 kg: 100 mg IV once daily. |
| Geriatric use | No specific dose adjustment required; consider age-related renal function decline, but no renal adjustment needed based on GFR. |
| 1st trimester | Limited human data; animal studies show no evidence of teratogenicity but use only if clearly needed. |
| 2nd trimester | May be used if benefit outweighs risk; no known association with fetal harm. |
| 3rd trimester | May be used if benefit outweighs risk; no known association with fetal harm. |
Clinical note
Comprehensive clinical and safety monograph for MYCAMINE (MYCAMINE).
| Placental transfer | Not studied in humans; in animal studies, detectable in fetal tissues. |
| Breastfeeding | Excretion into human milk unknown; caution due to potential for adverse effects in infant. Consider benefit of therapy versus risk. |
| Lactation Rating |
■ FDA Black Box Warning
None
| Serious Effects |
Hypersensitivity to micafungin or any component
| Precautions | Hepatic effects: elevations in AST, ALT, and bilirubin; monitor liver function, Rare cases of hepatic necrosis and hepatic failure, Renal effects: elevations in BUN and creatinine, Hypersensitivity reactions including anaphylaxis and exfoliative dermatitis, Risk of hemolytic anemia mediated by immune mechanisms |
| Food/Dietary | No clinically significant food interactions. Mycamine is administered intravenously; oral intake does not affect drug absorption. |
| Clinical Pearls |
Loading safety data…
| L3 (Moderately Safe) |
| Teratogenic Risk | Pregnancy Category C. Animal studies (rats at 0.5 mg/kg, rabbits at 1.25 mg/kg) showed fetal toxicity (reduced ossification, increased resorptions) at maternally toxic doses. No adequate human studies. Avoid in first trimester unless benefit outweighs risk; use only if clearly needed in second/third trimester. |
| Fetal Monitoring | Monitor liver function (AST, ALT, bilirubin) due to potential hepatotoxicity; renal function (serum creatinine) especially in compromised patients; signs of infusion-related reactions (rash, urticaria, hypotension). Fetal ultrasound if exposure during pregnancy. |
| Fertility Effects | No formal fertility studies in humans. In animal studies, slight increase in estrous cycle length in female rats but no effect on mating or fertility. Considered unlikely to significantly impair human fertility. |
| Mycamine (micafungin) is an echinocandin antifungal that inhibits beta-(1,3)-D-glucan synthase. It is used for candidemia, esophageal candidiasis, and prophylaxis in hematopoietic stem cell transplant recipients. Unlike azoles, it has minimal CYP interactions. Monitor LFTs due to potential hepatotoxicity. Dose adjustment not required in renal impairment. Infusion-related reactions (e.g., rash, hypotension) may occur; premedicate if needed. Invasive candidiasis: loading dose not required; doses up to 150 mg/day for endocarditis or osteomyelitis. |
| Patient Advice | Take this medication exactly as prescribed; it is given intravenously by a healthcare professional. · Report any signs of liver problems (yellowing skin/eyes, dark urine, abdominal pain) or allergic reactions (rash, itching, swelling, trouble breathing). · Inform your doctor if you have a history of liver disease or are pregnant/breastfeeding. · You may experience headache, nausea, or diarrhea; notify your doctor if severe. · Infusion reactions (flushing, fever, chills) can occur; tell your nurse if you feel unwell during the infusion. · Complete the full course of therapy even if you feel better to prevent recurrence. |