Mycamine^® (Lyophilisate) Instructions for Use

ATC Code

J02AX05 (Micafungin)

Active Substance

Micafungin (Rec.INN registered by WHO)

Clinical-Pharmacological Group

Antifungal drug

Pharmacotherapeutic Group

Antifungal agent

Pharmacological Action

Antifungal agent, an echinocandin derivative. The mechanism of action is associated with the inhibition of the synthesis of 1,3-β-D-glucan, which is a component of the fungal cell wall and is not contained in mammalian cells.

Activity of micafungin has been demonstrated in vivo in models of mucosal candidiasis and disseminated candidiasis. Micafungin increased the survival of immunosuppressed mice in a model of disseminated candidiasis and/or reduced the severity of fungal lesions.

Clinical studies have shown the efficacy of micafungin in the treatment of esophageal candidiasis and for the prevention of candidiasis after hematopoietic stem cell transplantation.

It is not known whether Micafungin causes drug resistance.

The efficacy of micafungin against other types of fungi has not been established.

Pharmacokinetics

There is a linear relationship between the AUC value and the dose of micafungin in the range of daily doses of 50-150 mg.

The binding of micafungin to plasma proteins is high – more than 99% in vitro and does not depend on plasma concentration in the concentration range of 10-100 µg/ml. It binds predominantly to albumin, but at therapeutic concentrations it does not competitively displace bilirubin from albumin binding sites. To a lesser extent, Micafungin binds to alpha₁-acid glycoprotein. In patients with esophageal candidiasis in the dose range of 50-150 mg/day, the mean V_d was 0.39±0.11 L/kg.

Some pathways of micafungin metabolism are catalyzed by CYP450 isoenzymes.

It is excreted mainly in the feces.

Indications

Treatment of esophageal candidiasis.

Prevention of candidiasis in patients after hematopoietic stem cell transplantation.

ICD codes

Dosage Regimen

Administer intravenously as an infusion. Do not administer by bolus injection.

For treatment of esophageal candidiasis, the recommended dose is 150 mg once daily.

For prophylaxis of candidiasis in patients undergoing hematopoietic stem cell transplantation, the recommended dose is 50 mg once daily.

Determine the duration of therapy individually based on the patient’s clinical response and microbiological findings.

Reconstitute the lyophilisate with 0.9% Sodium Chloride Injection or 5% Dextrose Injection. Gently swirl the vial; do not shake vigorously.

Further dilute the reconstituted solution in an IV infusion bag containing 0.9% Sodium Chloride or 5% Dextrose to a final concentration of 0.5 mg/mL to 4 mg/mL.

Administer the infusion over 1 hour. More rapid infusion may result in more frequent histamine-mediated reactions.

Inspect the solution visually for particulate matter and discoloration prior to administration. Discard if cloudiness or precipitate is observed.

No dosage adjustment is required for patients with renal impairment or for elderly patients.

Use in patients with hepatic impairment only after a careful benefit-risk evaluation.

Adverse Reactions

From the hematopoietic system leukopenia, neutropenia, thrombocytopenia, anemia, lymphopenia, eosinophilia.

From the digestive system nausea, abdominal pain, vomiting, decreased appetite, hyperbilirubinemia, increased activity of ALP, AST, ALT, LDH, constipation, dyspepsia.

From the CNS headache, dizziness, drowsiness, delirium.

From metabolism hypokalemia, hypophosphatemia, hypomagnesemia.

Allergic reactions rash, itching, facial swelling, facial redness, increased body temperature, chills.

Contraindications

Hypersensitivity to micafungin.

Use in Pregnancy and Lactation

Adequate and strictly controlled clinical studies of the safety of micafungin during pregnancy have not been conducted. Use during pregnancy is possible only if the intended benefit to the mother outweighs the potential risk to the fetus and only in established cases of extreme necessity.

It is not known whether Micafungin is excreted in human breast milk. Use during lactation is possible only in cases where the intended benefit to the mother outweighs the potential risk to the breastfed infant.

In experimental studies, visceral abnormalities and miscarriages were observed when micafungin was administered to rabbits at doses that were 4 times higher than the therapeutic doses recommended for humans. Micafungin did not cause fertility impairment in animals.

Micafungin is excreted in the breast milk of lactating rats.

Use in Hepatic Impairment

Micafungin should be used only after a thorough assessment of the expected benefit and the existing risk of therapy in patients with impaired liver function.

Special Precautions

Micafungin should be used only after a thorough assessment of the expected benefit and the existing risk of therapy in patients with impaired liver function, in the presence of clinical and laboratory data of hemolysis or hemolytic anemia.

With caution, under careful clinical supervision and with monitoring of plasma concentrations, Micafungin should be used simultaneously with sirolimus, nifedipine.

Drug Interactions

The AUC of sirolimus increased by 21% without changing its C_max in plasma at steady state when taking micafungin, compared with taking sirolimus alone.

The AUC and C_max in plasma of nifedipine increased by 18% and 42%, respectively, at steady state when taking micafungin, compared with taking nifedipine alone.

Storage Conditions

Store at 2°C (36°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.