Micafungin Sodium

Pronunciation: MYE-ka-FUN-jin SOE-dee-um
Class: Antifungal agent

Trade Names

Mycamine
- Powder for injection 50 mg

Pharmacology

Inhibits synthesis of 1,3-B-D-glucan, an essential component of fungal cell walls, but not present in mammalian cells.

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Pharmacokinetics

Absorption

C _max with 100 mg dose to steady state is approximately 10 mcg/mL. C _max with 8 mg/kg for 7 days is approximately 61 mcg/mL.

Distribution

More than 99% protein bound, primarily to albumin, and to a lesser extent to alpha-1 acid glycoprotein.

Metabolism

Metabolized by arylsulfatase, catechol-O-methyltransferase, and hydroxylation; catalyzed by CYP-450 isoenzymes.

Elimination

The half-life is 14 to 17 h. Fecal excretion is major route of elimination (71%).

Special Populations

No dosage adjustment is needed.

Moderate (Child-Pugh score 7 to 9): AUC and C _max were reduced about 22% compared with healthy hepatic function. No dosage adjustment needed.

No overall differences in safety and efficacy were observed in subjects 65 yr of age and older compared with younger patients.

No dosage adjustment is required based on gender.

No dosage adjustment is required based on race.

Indications and Usage

Treatment of esophageal candidiasis; prophylaxis of Candida infections in patients undergoing hematopoietic stem cell transplantation (HSCT); treatment of patients with candidemia, acute disseminated candidiasis, Candida peritonitis, and abscess.

Contraindications

Known hypersensitivity to echinocandins or any component of the product.

Dosage and Administration

IV 100 mg once daily by slow infusion over 1 h.

IV 150 mg once daily by slow infusion over 1 h.

IV 50 mg once daily by slow infusion over 1 h.

General Advice

• For IV infusion only. Not for oral, intradermal, subcutaneous, IM, IV bolus, or intra-arterial administration.
• Reconstitute powder for injection by adding 5 mL of sodium chloride 0.9% injection (without a bacteriostatic agent) or dextrose 5% injection to vial. To minimize excessive foaming, gently dissolve powder by swirling the vial until a clear solution is obtained. Do not vigorously shake vial. Final concentration is approximately micafungin 10 mg/mL (50 mg vial) or 20 mg/mL (100 mg vial).
• For treatment of esophageal candidiasis, add micafungin 150 mg from 3 of the 50 mg vials reconstituted with 15 mL of diluent to 100 mL of sodium chloride 0.9% injection or dextrose 5% injection.
• For prophylaxis of Candida infections, add micafungin 50 mg from 1 vial reconstituted with 5 mL of diluent to 100 mL of sodium chloride 0.9% injection or dextrose 5% injection.
• Do not mix or co-infuse with other medications.
• Visually inspect reconstituted solution before use. Do not use if particulate matter, cloudiness, or discoloration is noted.
• Flush existing IV line with sodium chloride 0.9% injection prior to infusing micafungin.
• Administer by IV infusion over 1 h. More rapid infusions may result in more frequent histamine-mediated reactions.
• Reconstituted solution contains no preservative. Discard any unused solution.

Storage/Stability

Store unopened vials at controlled room temperature (59° to 86°F). Reconstituted micafungin solution may be stored in the original vial at room temperature (77°F) for up to 24 h. Diluted infusion solution can be stored at room temperature (77°F) for 24 h. Protect diluted infusion solution from light.

Drug Interactions

Plasma levels may be elevated by micafungin, increasing the pharmacologic effects and adverse reactions.

Sirolimus AUC increased, but not C _max .

Laboratory Test Interactions

None well documented.

Adverse Reactions

Cardiovascular

Tachycardia (25%); hypertension (21%); hypotension (19%); flushing (11%); atrial fibrillation, bradycardia (4%).

CNS

Pyrexia (45%); headache (42%); insomnia (36%); fatigue (30%); anxiety (22%); dizziness (13%).

Dermatologic

Rash (26%); pruritus (18%); erythema (11%); decubitus ulcer (6%).

EENT

Epistaxis (12%).

GI

Diarrhea (71%); nausea (70%); vomiting (66%); constipation (30%); abdominal pain, anorexia (27%); dyspepsia (25%); decreased appetite (21%).

Genitourinary

Acute renal failure and renal function impairment (postmarketing).

Hematologic-Lymphatic

Neutropenia (76%); thrombocytopenia (72%); febrile neutropenia (37%); anemia (36%); aggravated anemia (5%); decreased WBCs, hemolytic anemia, vascular disorder (postmarketing).

Hepatic

Abnormal hepatic function, hepatic disorder, hepatocellular damage, hyperbilirubinemia (postmarketing).

Lab Tests

Increased blood alkaline phosphatase (8%); increased AST (6%); increased ALT (5%); abnormal LFTs (4%).

Metabolic-Nutritional

Hypomagnesemia (50%); hypokalemia (49%); fluid overload, hypocalcemia (17%); fluid retention, hyperglycemia (16%); hypoglycemia (7%); hypernatremia (6%).

Musculoskeletal

Rigors (26%); back pain (5%).

Respiratory

Cough (23%); dyspnea (13%); epistaxis (6%); pneumonia (5%).

Miscellaneous

Mucosal inflammation (76%); peripheral edema (21%); phlebitis (19%); bacteremia (16%); septic shock (8%); sepsis (6%).

Precautions

Pregnancy

Category C .

Lactation

Undetermined

Children

Safety and efficacy not established.

Hypersensitivity

Isolated cases of serious hypersensitivity (anaphylaxis and anaphylactoid) reactions have occurred. Monitor patient for signs of allergic reaction. Discontinue therapy. Be prepared to treat appropriately.

Renal Function

Elevated BUN and creatinine as well as isolated cases of renal function impairment or acute renal failure have been reported.

Hepatic Function

Abnormal liver function tests may occur.

Hematologic

Acute intravascular hemolysis and hemoglobinuria may occur.

Overdosage

Symptoms

None reported.

Patient Information

• Advise patient or caregiver that medication will be prepared and administered by health care provider in a hospital setting.
• Advise patient to immediately report any discomfort at injection site or vein above the injection site.
• Instruct patient to report any of the following to health care provider: chills, fever, flushing, itching, nausea, rash, any unusual or unexplained symptoms.

Copyright © 2009 Wolters Kluwer Health.