2014年3月15日，Noxafil（posaconazole，泊沙康唑）静脉注射剂（intravenous，IV，18mg/ml）获FDA批准，这是一种新配方Noxafil。FDA于2013年11月授予Noxafil IV新药申请（NDA）优先审查资格。此外，Noxafil（posaconazole，100 mg）缓释片于2013年11月获FDA批准，同时默沙东还销售Noxafil（40mg/mL）口服混悬液。
Noxafil注射液、缓释片及口服混悬液，均适用于因免疫功能严重低下而具有高风险的侵袭性曲霉菌和念珠菌感染的患者，如患有移植物抗宿主病（GVHD）的造血干细胞移植（HSCT）受者，或那些因化疗导致长期的中性粒细胞减少（低白细胞计数）的恶性血液病患者。
Noxafil注射液适用于18岁及以上患者，Noxafil缓释片和口服混悬液适用于13岁及以上患者。这些药物均用于高危患者预防侵袭性曲霉菌和念珠菌感染。
默沙东计划在4月中旬将Noxafil静脉注射剂推向市场。

NOXAFIL INJECTION Rx
Generic Name and Formulations:
Posaconazole 18mg/mL; preservative-free.

Company:
Merck & Co., Inc.
Indications for NOXAFIL INJECTION:
Prophylaxis against invasive Aspergillus and Candida infections, in patients at high risk due to being severely immunocompromised, such as hematopoietic stem cell transplant recipients with Graft vs. Host Disease (GVHD) or those with hematologic malignancies with prolonged neutropenia due to chemotherapy.

Adult Dose for NOXAFIL INJECTION:
Give by slow IV infusion over ~90mins via central venous line (including central venous catheter or PICC); if unavailable, may give via peripheral venous catheter over ~30mins only as a single dose in advance of central line placement. ≥18yrs: 300mg twice daily on Day 1, then 300mg once daily starting on Day 2 until recovery from neutropenia or immunosuppression.

Children's Dose for NOXAFIL INJECTION:
<18yrs: not established.

See Also:
NOXAFIL

NOXAFIL ORAL SUSPENSION

Pharmacological Class:
Azole antifungal.

Contraindications:
Hypersensitivity to other azole antifungal agents. Concomitant sirolimus, ergot alkaloids, or HMG-CoA reductase inhibitors (eg, atorvastatin, lovastatin, simvastatin). Drugs that cause QT prolongation and are metabolized by CYP3A4 (eg, quinidine, pimozide).

Warnings/Precautions:
Tabs and oral susp are not interchangeable. Inj: avoid in moderate or severe renal impairment (eGFR <50mL/min); if needed, monitor and consider switching to oral therapy if creatinine levels increase. Proarrhythmic conditions. Correct potassium, calcium, magnesium levels before starting. Evaluate and monitor liver function tests before and during therapy; consider discontinuing if liver disease occurs. Patients who cannot eat a full meal or tolerate an oral nutritional supplement, or those with severe renal impairment, severe diarrhea, vomiting, or >120kg: monitor for breakthrough fungal infections. Pregnancy (Cat.C). Nursing mothers: not recommended.

Interactions:
See Contraindications. Avoid drugs that lower posaconazole levels (eg, rifabutin, phenytoin, efavirenz, fosamprenavir); monitor for breakthrough fungal infections. Potentiates calcineurin-inhibitors (eg, cyclosporine, tacrolimus); monitor trough levels frequently during and at discontinuation of posaconazole; adjust tacrolimus or cyclosporine doses. Potentiates CYP3A4 substrates (eg, ritonavir, atazanavir, calcium channel blockers, vinca alkaloids, rifabutin, phenytoin), digoxin; monitor and consider dose reduction. Prolonged hypnotic and sedative effects with concomitant midazolam or other benzodiazepines (eg, alprazolam, triazolam). Monitor glucose levels with glipizide. Susp: avoid concomitant cimetidine, esomeprazole, metoclopramide; if needed, monitor for breakthrough fungal infections.

Adverse Reactions:
Fever, diarrhea, nausea, vomiting, headache, hypokalemia, cough, rigors, fatigue, anorexia, hypertension, abdominal pain, constipation, rash; lab abnormalities (eg, anemia, neutropenia, thrombocytopenia, increased liver enzymes), arrhythmias, QT prolongation.

Metabolism:
Hepatic (CYP3A4).

Elimination:
Fecal (major), renal.

Generic Availability:
NO

How Supplied:
Tabs—60; Susp—105mL (w. dosing spoon); Vials—1