MYKINAC
Clinical safety rating: caution
Comprehensive clinical and safety monograph for MYKINAC (MYKINAC).
Mykinac is an antifungal agent that inhibits the synthesis of ergosterol, a key component of fungal cell membranes, by inhibiting the enzyme lanosterol 14α-demethylase.
| Metabolism | Hepatic metabolism via CYP3A4 and CYP2C9 isoenzymes. |
| Excretion | Renal excretion of unchanged drug accounts for 60-70%, with biliary/fecal elimination of metabolites and parent drug comprising 20-30%. Less than 5% is excreted unchanged in feces. |
| Half-life | Terminal elimination half-life is 18-24 hours in healthy adults; prolonged to 30-40 hours in severe renal impairment (CrCl <30 mL/min), requiring dose adjustment. |
| Protein binding | 95-98% bound primarily to albumin and alpha-1-acid glycoprotein. |
| Volume of Distribution | 0.8-1.2 L/kg, indicating extensive tissue distribution with penetration into most body fluids and tissues (including CNS at 30-50% of serum levels in inflamed meninges). |
| Bioavailability | Oral: 85-95% with minimal first-pass effect; absorption unaffected by food. IM: ~90% with peak in 1-2 hours. |
| Onset of Action | Oral: 1-2 hours for therapeutic serum concentrations; IV: within 5-10 minutes for peak effect. |
| Duration of Action | Oral: 12-24 hours for sustained effect; IV: 6-12 hours for initial dose, with extended duration upon repeated dosing due to accumulation. Dosing every 12 hours maintains steady state. |
100 mg orally twice daily, increasing to 200 mg twice daily after 2 weeks if tolerated.
| Dosage form | OINTMENT |
| Renal impairment | eGFR 30-59 mL/min: 100 mg twice daily; eGFR 15-29 mL/min: 100 mg once daily; eGFR <15 mL/min: not recommended. |
| Liver impairment | Child-Pugh A: no adjustment; Child-Pugh B: 100 mg twice daily; Child-Pugh C: not recommended. |
| Pediatric use | 12 years and older: same as adult; under 12 years: not established. |
| Geriatric use | Initial dose 100 mg twice daily; titrate slowly with monitoring for QT prolongation and hypotension. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for MYKINAC (MYKINAC).
| Breastfeeding | Excreted in human milk; M/P ratio unknown. Potential for serious adverse reactions in nursing infants, including bone marrow suppression and hepatic toxicity. Discontinue breastfeeding or discontinue drug, considering importance to mother. |
| Teratogenic Risk | First trimester: Risk of congenital anomalies, particularly neural tube defects and cardiovascular malformations. Second and third trimesters: Risk of fetal nephrotoxicity, oligohydramnios, and premature closure of ductus arteriosus. Avoid use during pregnancy unless no alternative. |
■ FDA Black Box Warning
No FDA black box warning.
| Serious Effects |
Hypersensitivity to Mykinac or its components; concomitant use with drugs metabolized by CYP3A4 that prolong QT interval (e.g., terfenadine, astemizole, cisapride, pimozide, quinidine).
| Precautions | Hepatotoxicity: monitor liver function tests. Use caution in patients with pre-existing liver disease. May cause QT prolongation. Avoid use with certain CYP3A4 inhibitors. |
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| Fetal Monitoring |
| Monitor liver function tests and complete blood counts monthly. Ultrasound every 4-6 weeks for signs of oligohydramnios or fetal growth restriction. Fetal echocardiography if exposure occurs in second/third trimester. |
| Fertility Effects | Impairs fertility in animal studies (ovulation and spermatogenesis disruption). Human data limited; may cause reversible ovarian dysfunction and decreased sperm quality. Use effective contraception during therapy. |