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Prescribing Information
VFEND® I.V. (voriconazole) for Injection
VFEND® Tablets (voriconazole)
VFEND® (voriconazole) for Oral Suspension
Dosage and Administration
Return to the VFEND Product Center

Administration
VFEND Tablets or Oral Suspension should be taken at least one hour before, or one hour following, a meal.

VFEND I.V. for Injection requires reconstitution to 10 mg/mL and subsequent dilution to 5 mg/mL or less prior to administration as an infusion, at a maximum rate of 3 mg/kg per hour over 1-2 hours (see Intravenous Administration).NOT FOR IV BOLUS INJECTION

Use of VFEND I.V. with other Parenteral Drug Products

Blood products and concentrated electrolytes VFEND I.V. must not be infused concomitantly with any blood product or short-term infusion of concentrated electrolytes, even if the two infusions are running in separate intravenous lines (or cannulas). Electrolyte disturbances such as hypokalemia, hypomagnesemia and hypocalcemia should be corrected prior to initiation of VFEND therapy (see PRECAUTIONS).

Intravenous solutions containing (non-concentrated) electrolytes VFEND I.V. can be infused at the same time as other intravenous solutions containing (nonconcentrated) electrolytes, but must be infused through a separate line.

Total parenteral nutrition (TPN) VFEND I.V. can be infused at the same time as total parenteral nutrition, but must be infused in a separate line. If infused through a multiple-lumen catheter, TPN needs to be administered using a different port from the one used for VFEND I.V.

Use in Adults

Invasive aspergillosis and serious fungal infections due to Fusarium spp. and Scedosporium apiospermum:

For the treatment of adults with invasive aspergillosis and infections due to Fusarium spp. and Scedosporium apiospermum, therapy must be initiated with the specified loading dose regimen of intravenous VFEND to achieve plasma concentrations on Day 1 that are close to steady state. On the basis of high oral bioavailability, switching between intravenous and oral administration is appropriate when clinically indicated (see CLINICAL PHARMACOLOGY). Once the patient can tolerate medication given by mouth, the oral tablet form or oral suspension form of VFEND may be utilized. (See Table 17.)

Candidemia in nonneutropenic patients and other deep tissue Candida infections:

See Table 17. Patients should be treated for at least 14 days following resolution of symptoms or following last positive culture, whichever is longer.

Esophageal Candidiasis
See Table 17. Patients should be treated for a minimum of 14 days and for at least 7 days following resolution of symptoms.

Table 17
Recommended Dosing Regimen

Comp

Dosage Adjustment
If patient response is inadequate, the oral maintenance dose may be increased from 200 mg every 12 hours to 300 mg every 12 hours. For adult patients weighing less than 40 kg, the oral maintenance dose may be increased from 100 mg every 12 hours to 150 mg every 12 hours. If patients are unable to tolerate 300 mg orally every 12 hours, reduce the oral maintenance dose by 50 mg steps to a minimum of 200 mg every 12 hours (or to 100 mg every 12 hours for adult patients weighing less than 40 kg).

If patients are unable to tolerate 4 mg/kg IV, reduce the intravenous maintenance dose to 3 mg/kg every 12 hours.

Phenytoin may be coadministered with VFEND if the intravenous maintenance dose of VFEND is increased to 5 mg/kg every 12 hours, or the oral maintenance dose is increased from 200 mg to 400 mg every 12 hours (100 mg to 200 mg every 12 hours in adult patients weighing less than 40 kg) (see CLINICAL PHARMACOLOGY, PRECAUTIONS – Drug Interactions).

When voriconazole is coadministered with efavirenz, the voriconazole maintenance dose should be increased to 400 mg Q12h and the efavirenz dose should be decreased to 300 mg Q24h (see CLINICAL PHARMACOLOGY and PRECAUTIONS — Drug Interactions).

Duration of therapy should be based on the severity of the patient's underlying disease, recovery from immunosuppression, and clinical response.

Use in Geriatric Patients
No dose adjustment is necessary for geriatric patients.

Use in Patients with Hepatic Insufficiency
In the clinical program, patients were included who had baseline liver function tests (ALT, AST) up to 5 times the upper limit of normal. No dose adjustment is necessary in patients with this degree of abnormal liver function, but continued monitoring of liver function tests for further elevations is recommended (see WARNINGS).

It is recommended that the standard loading dose regimens be used but that the maintenance dose be halved in patients with mild to moderate hepatic cirrhosis (Child-Pugh Class A and B).

VFEND has not been studied in patients with severe hepatic cirrhosis (Child-Pugh Class C) or in patients with chronic hepatitis B or chronic hepatitis C disease. VFEND has been associated with elevations in liver function tests and clinical signs of liver damage, such as jaundice, and should only be used in patients with severe hepatic insufficiency if the benefit outweighs the potential risk. Patients with hepatic insufficiency must be carefully monitored for drug toxicity.

Use in Patients with Renal Insufficiency
The pharmacokinetics of orally administered VFEND are not significantly affected by renal insufficiency. Therefore, no adjustment is necessary for oral dosing in patients with mild to severe renal impairment (see CLINICAL PHARMACOLOGY – Special Populations).

In patients with moderate or severe renal insufficiency (creatinine clearance <50 mL/min), accumulation of the intravenous vehicle, SBECD, occurs. Oral voriconazole should be administered to these patients, unless an assessment of the benefit/risk to the patient justifies the use of intravenous voriconazole. Serum creatinine levels should be closely monitored in these patients, and, if increases occur, consideration should be given to changing to oral voriconazole therapy (see DOSAGE and ADMINISTRATION).

Voriconazole is hemodialyzed with clearance of 121 mL/min. The intravenous vehicle, SBECD, is hemodialyzed with clearance of 55 mL/min. A 4-hour hemodialysis session does not remove a sufficient amount of voriconazole to warrant dose adjustment.

Intravenous Administration
VFEND I.V. For Injection:

Reconstitution
The powder is reconstituted with 19 mL of Water For Injection to obtain an extractable volume of 20 mL of clear concentrate containing 10 mg/mL of voriconazole. It is recommended that a standard 20 mL (non-automated) syringe be used to ensure that the exact amount (19.0 mL) of Water for Injection is dispensed. Discard the vial if a vacuum does not pull the diluent into the vial. Shake the vial until all the powder is dissolved.

Dilution
VFEND must be infused over 1-2 hours, at a concentration of 5 mg/mL or less. Therefore, the required volume of the 10 mg/mL VFEND concentrate should be further diluted as follows (appropriate diluents listed below):

1. Calculate the volume of 10 mg/mL VFEND concentrate required based on the patient's weight (see Table 18).

2. In order to allow the required volume of VFEND concentrate to be added, withdraw and discard at least an equal volume of diluent from the infusion bag or bottle to be used. The volume of diluent remaining in the bag or bottle should be such that when the 10 mg/mL VFEND concentrate is added, the final concentration is not less than 0.5 mg/mL nor greater than 5 mg/mL.

3. Using a suitable size syringe and aseptic technique, withdraw the required volume of VFEND concentrate from the appropriate number of vials and add to the infusion bag or bottle. Discard Partially Used Vials.

The final VFEND solution must be infused over 1-2 hours at a maximum rate of 3 mg/kg per hour.

Table 18
Required Volumes of 10 mg/mL VFEND Concentrate

Comp

VFEND I.V. for Injection is a single dose unpreserved sterile lyophile. Therefore, from a microbiological point of view, once reconstituted, the product should be used immediately. If not used immediately, in-use storage times and conditions prior to use are the responsibility of the user and should not be longer than 24 hours at 2º to 8ºC (36º to 46ºF). This medicinal product is for single use only and any unused solution should be discarded. Only clear solutions without particles should be used.

The reconstituted solution can be diluted with:

9 mg/mL (0.9%) Sodium Chloride USP
Lactated Ringers USP
5% Dextrose and Lactated Ringers USP
5% Dextrose and 0.45% Sodium Chloride USP
5% Dextrose USP
5% Dextrose and 20 mEq Potassium Chloride USP
0.45% Sodium Chloride USP
5% Dextrose and 0.9% Sodium Chloride USP

The compatibility of VFEND I.V. with diluents other than those described above is unknown (see Incompatibilities below).

Parenteral drug products should be inspected visually for particulate matter and discoloration prior to administration, whenever solution and container permit.

Incompatibilities:

VFEND I.V. must not be diluted with 4.2% Sodium Bicarbonate Infusion. The mildly alkaline nature of this diluent caused slight degradation of VFEND after 24 hours storage at room temperature. Although refrigerated storage is recommended following reconstitution, use of this diluent is not recommended as a precautionary measure. Compatibility with other concentrations is unknown.

VFEND for Oral Suspension

Reconstitution
Tap the bottle to release the powder. Add 46 mL of water to the bottle. Shake the closed bottle vigorously for about 1 minute. Remove child-resistant cap and push bottle adaptor into the neck of the bottle. Replace the cap. Write the date of expiration of the reconstituted suspension on the bottle label (the shelf-life of the reconstituted suspension is 14 days at controlled room temperature 15-30ºC[59-86ºF]).

Instructions for use
Shake the closed bottle of reconstituted suspension for approximately 10 seconds before each use. The reconstituted oral suspension should only be administered using the oral dispenser supplied with each pack.

Incompatibilities
VFEND for Oral Suspension and the 40 mg/mL reconstituted oral suspension should not be mixed with any other medication or additional flavoring agent. It is not intended that the suspension be further diluted with water or other vehicles.

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VFEND Safety Information
 

Important Safety Information

Most frequently reported adverse events (all causalities) in therapeutic trials were visual disturbances, fever, rash, vomiting, nausea, diarrhea, headache, sepsis, peripheral edema, abdominal pain, and respiratory disorder. Treatment-related adverse events that most often led to discontinuation in clinical trials were elevated LFTs, rash, and visual disturbances.

VFEND treatment–related visual disturbances are common. The effect of VFEND on visual function is not known if treatment continues beyond 28 days. There have been post-marketing reports of prolonged visual adverse events, including optic neuritis and papilledema. These events occurred primarily in severely ill patients who had underlying conditions and/or concomitant medications, which may have caused or contributed to the events. If treatment continues beyond 28 days, visual function should be monitored. Patients should be advised not to drive at night when taking VFEND and to avoid potentially hazardous tasks if they perceive any change in vision.

VFEND is contraindicated with terfenadine, astemizole, cisapride, pimozide, quinidine (since increased plasma concentrations of these drugs can lead to QT prolongation and rare occurrences of torsade de pointes), sirolimus, rifampin, rifabutin, carbamazepine, long-acting barbiturates, ergot alkaloids, and St. John’s Wort (Hypericum perforatum). VFEND is also contraindicated with ritonavir (400 mg every 12 hours). If VFEND is coadministered with efavirenz, the VFEND maintenance dose should be increased to 400 mg every 12 hours and the efavirenz dose should be decreased to 300 mg every 24 hours. When treatment with VFEND is stopped, the initial dosage of efavirenz should be restored.

There have been uncommon cases of serious hepatic reactions during treatment with VFEND (clinical hepatitis, cholestasis, and fulminant hepatic failure, including fatalities). LFTs should be evaluated at the start of and during the course of therapy. Patients have rarely developed serious cutaneous reactions, such as Stevens-Johnson syndrome, during treatment with VFEND.

Pregnancy Category D.

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