micafungin

Action and Spectrum

Actions and Spectrum: 

• micafungin is an antifungal agent that belongs to the echinocandin class of drugs. Its action mechanism involves inhibiting the synthesis of beta-1,3-D-glucan, a vital fungal cell wall component. This results in the weakening and eventual lysis of the fungal cell wall, leading to the death of the fungus. 
• micafungin has a broad spectrum of activity against various fungal species, including Candida and Aspergillus. It is primarily used to treat invasive candidiasis and invasive aspergillosis, two severe fungal infections that can affect immunocompromised patients, such as those undergoing chemotherapy, bone marrow transplantation, or solid organ transplantation. 

Drug Interaction

Adverse Reaction

Frequency defined 

>10% 

Headache 

Increased LFTs 

Nausea 

Phlebitis 

Pyrexia 

Rigors 

Vomiting 

Facial swelling 

Anemia 

Diarrhea 

Leukopenia 

Neutropenia 

Pruritus 

Rash 

Thrombocytopenia 

Vasodilation  

<1% 

Dizziness 

Delirium 

Somnolence 

Post-marketing reports 

Hemolytic anemia 

White blood cell count decreased 

Hepatic function abnormal 

Disseminated intravascular coagulation 

Hepatocellular damage 

Stevens-Johnson syndrome 

Hyperbilirubinemia 

Toxic epidermal necrolysis 

Hepatic disorder 

Black Box Warning

Contraindication / Caution

Contraindications/caution: 

Contraindications: 

• Hypersensitivity: micafungin should not be used in individuals with a known hypersensitivity to any component of the medication. 
• Hepatic impairment: micafungin is primarily metabolized in the liver, and patients with severe hepatic impairment may have difficulty metabolizing the medication. Thus, micafungin should be used cautiously in patients with moderate to severe hepatic impairment. 
• Pregnancy and lactation: The safety of micafungin in pregnant or lactating women has not been established. Therefore, micafungin should be used during pregnancy or lactation only if the potential benefit justifies the potential risk to the fetus or infant. 
• Pediatric population: The safety and efficacy of micafungin in children less than four months of age have not been established. 
• Concurrent use of certain medications: micafungin may interact with certain medications, including cyclosporine and tacrolimus, commonly used in transplant patients. Therefore, caution should be exercised when micafungin is used in patients taking these medications. 

Caution: 

• Renal impairment: The kidneys primarily eliminate micafungin, and patients with severe renal impairment may have difficulty eliminating the medication. Thus, micafungin should be used cautiously in patients with moderate to severe renal impairment. 
• Use in the elderly: Elderly patients may be more susceptible to adverse effects of micafungin due to age-related decline in renal function or other coexisting medical conditions. Therefore, caution should be exercised when using micafungin in elderly patients. 
• Fungal resistance: Overusing or misusing antifungal medications like micafungin may develop fungal resistance, making the medication less effective. Therefore, micafungin should be used only for treating fungal infections for which it is indicated and in the appropriate dosage and duration. 
• Liver function tests: micafungin may cause elevations in liver function tests, indicating liver damage. Therefore, liver function tests should be monitored regularly in patients receiving micafungin. 

Pregnancy / Lactation

Pregnancy consideration: The safety of micafungin in pregnant has not been established. 

Lactation:  

• The safety of micafungin during lactation has not been established, and there is limited information available regarding the excretion of micafungin in breast milk. 
• It is not known whether micafungin is excreted in human milk or if it affects the nursing infant. 

Pregnancy category: 

Category A: well-controlled and Satisfactory studies show no risk to the fetus in the first or later trimester.   

Category B: there was no evidence of risk to the fetus in animal studies, and there were not enough studies on pregnant women. 

Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.    

Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.    

Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.    

Category N: There is no data available for the drug under this category 

Pharmacology

Pharmacology: 

micafungin is a member of the echinocandin class of antifungal medications, which inhibit the synthesis of β(1,3)-D-glucan in the fungal cell wall. micafungin targets the enzyme 1,3-β-D-glucan synthase, responsible for producing β(1,3)-D-glucan. By inhibiting this enzyme, micafungin disrupts the formation of the fungal cell wall, leading to cell lysis and death. 

Pharmacodynamics: 

• The pharmacodynamics of micafungin involves inhibiting the synthesis of β(1,3)-D-glucan in the fungal cell wall. This disrupts the integrity of the fungal cell wall, causing osmotic instability and cell death. 
• micafungin has a concentration-dependent mode of action, meaning that higher drug concentrations are associated with more excellent antifungal activity. The minimum inhibitory concentration (MIC) is the lowest concentration of micafungin required to inhibit the growth of a particular fungal strain. 

Pharmacokinetics: 

Absorption 

micafungin is administered intravenously and unavailable in an oral formulation. After intravenous administration, micafungin is rapidly and extensively distributed into tissues.  

Distribution 

micafungin has a low plasma protein binding (~99% bound to albumin) and a large volume of distribution (approximately 0.3 L/kg), suggesting extensive distribution into tissues.  

Metabolism 

micafungin is minimally metabolized in the liver by arylsulfatase and other enzymes. The primary metabolite is M-1, which has little antifungal activity.  

Elimination and Excretion 

micafungin is primarily excreted unchanged in the bile, with a minor portion excreted in the urine. The elimination half-life of micafungin is approximately 14 hours in healthy adults but may be longer in patients with hepatic impairment. 

Adminstartion

Administration: 

• micafungin is administered intravenously over 1 hour, with the dosage and duration of treatment depending on the type and severity of the fungal infection being treated. 
• The recommended adult dose for candidemia and other invasive candidiasis is 100 mg once daily, with the duration of treatment ranging from 14 to 42 days or longer, depending on the response to therapy and the patient’s underlying clinical condition. 
• For esophageal candidiasis, the recommended dose is 150 mg once daily for two weeks. The recommended dose for preventing invasive Candida infections in patients undergoing hematopoietic stem cell transplantation is 50-100 mg once daily for the duration of neutropenia. 

Patient Information Leaflet

Patient information leaflet 

Generic Name: micafungin 

Why do we use micafungin? 

micafungin is a broad-spectrum antifungal medication that is indicated for the treatment of various fungal infections, including: 

• Candidemia: micafungin is approved for treating candidemia, a bloodstream infection caused by Candida species. It also treats other invasive Candida infections, such as disseminated candidiasis and candida peritonitis. 
• Esophageal candidiasis: micafungin is also approved for treating esophageal candidiasis, a fungal esophagus infection. 
• Invasive aspergillosis: micafungin is a salvage therapy for treating invasive aspergillosis, a severe infection caused by Aspergillus species. 
• Prophylaxis of Candida infections: micafungin is also used to prevent invasive Candida infections in patients undergoing hematopoietic stem cell transplantation.