Posaconazole Delayed-release

Generic Name: posaconazole delayed-release

Azole Antifungal [EPC]Over-the-Counter (OTC)

Brand Names:

Posaconazole

11 DESCRIPTION Posaconazole is an azole antifungal agent. Posaconazole is available as delayed-release tablet intended for oral administration. Posaconazole is designated chemically as 4-[4-[4-[4-[[ (3 R ,5 R )-5- (2,4-difluorophenyl)tetrahydro-5- (1 H -1,2,4-triazol-1-ylmethyl)-3-furanyl]methoxy]phenyl]-1-piperazinyl]phenyl]-2-[(1 S ,2 S )-1-ethyl-2-hydroxypropyl]-2,4-dihydro-3 H -1,2,4-triazol-3-one with an empirical formula of C 37 H 42 F 2 N 8 O 4 and a molecular weight of 700.8.

Overview

11 DESCRIPTION Posaconazole is an azole antifungal agent. Posaconazole is available as delayed-release tablet intended for oral administration. Posaconazole is designated chemically as 4-[4-[4-[4-[[ (3 R ,5 R )-5- (2,4-difluorophenyl)tetrahydro-5- (1 H -1,2,4-triazol-1-ylmethyl)-3-furanyl]methoxy]phenyl]-1-piperazinyl]phenyl]-2-[(1 S ,2 S )-1-ethyl-2-hydroxypropyl]-2,4-dihydro-3 H -1,2,4-triazol-3-one with an empirical formula of C 37 H 42 F 2 N 8 O 4 and a molecular weight of 700.8.

Uses

1 INDICATIONS AND USAGE Posaconazole delayed-release tablets is an azole antifungal agent indicated as follows: ( 1 ) Posaconazole delayed-release tablets are indicated for the prophylaxis of invasive Aspergillus and Candida infections in patients who are at high risk of developing these infections due to being severely immunocompromised, such as hematopoietic stem cell transplant (HSCT) recipients with graftversushost disease (GVHD) or those with hematologic malignancies with prolonged neutropenia from chemotherapy as follows: ( 1.2 ) Posaconazole delayed-release tablets : adults and pediatric patients 13 years of age and older ( 1 ) 1.2 Prophylaxis of Invasive Aspergillus and Candida Infections Posaconazole is indicated for the prophylaxis of invasive Aspergillus and Candida infections i...

Dosage

2 DOSAGE AND ADMINISTRATION Posaconazole oral suspension is not substitutable with posaconazole delayed-release tablets due to the differences in the dosing of each formulation. ( 2.1 ) Administer posaconazole delayed-release tablets with or without food. ( 2.1 ) Table 1. Recommended Dosage in Adult Patients and Pediatric Patients aged 13 years and older Indication Dosage Form, Dose and Duration of Therapy Prophylaxis of invasive Aspergillus and Candida infections Posaconazole Delayed-Release Tablets: Loading dose : 300 mg (three 100 mg delayed-release tablets) twice a day on the first day. ( 2 ) Maintenance dose : 300 mg (three 100 mg delayed-release tablets) once a day, starting on the second day. Duration of therapy is based on recovery from neutropenia or immunosuppression.

Side Effects

6 ADVERSE REACTIONS The following serious and otherwise important adverse reactions are discussed in detail in another section of the labeling: Hypersensitivity [see Contraindications ( 4.1 )] Arrhythmias and QT Prolongation [see Warnings and Precautions ( 5.2 )] Hepatic Toxicity [see Warnings and Precautions ( 5.4 )] Adult Patients : Common adverse reactions in studies with posaconazole in adults are diarrhea, nausea, fever, vomiting, headache, coughing, and hypokalemia. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Chartwell RX, LLC at 1-845-232-1683 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch .

Interactions

7 DRUG INTERACTIONS Posaconazole is primarily metabolized via UDP glucuronosyltransferase and is a substrate of p­ glycoprotein (P-gp) efflux. Therefore, inhibitors or inducers of these clearance pathways may affect posaconazole plasma concentrations. Coadministration of drugs that can decrease the plasma concentrations of posaconazole should generally be avoided unless the benefit outweighs the risk. If such drugs are necessary, patients should be monitored closely for breakthrough fungal infections. Posaconazole is also a strong inhibitor of CYP3A4. Therefore, plasma concentrations of drugs predominantly metabolized by CYP3A4 may be increased by posaconazole [see Clinical Pharmacology ( 12.3 )] .

Warnings

5 WARNINGS AND PRECAUTIONS Calcineurin-Inhibitor Toxicity: Posaconazole increases concentrations of cyclosporine or tacrolimus; reduce dose of cyclosporine and tacrolimus and monitor concentrations frequently. ( 5.1 ) Arrhythmias and QTc Prolongation: Posaconazole has been shown to prolong the QTc interval and cause cases of TdP. Administer with caution to patients with potentially proarrhythmic conditions. Do not administer with drugs known to prolong QTc interval and metabolized through CYP3A4. ( 5.2 ) Electrolyte Disturbances: Monitor and correct, especially those involving potassium (K + ), magnesium (Mg ++ ), and Calcium (Ca + ) before and during posaconazole therapy. ( 5.3 ) Hepatic Toxicity: Elevations in liver tests may occur. 4 CONTRAINDICATIONS Known hypersensitivity to posaconazole or other azole antifungal agents. ( 4.1 ) Coadministration of posaconazole with the following drugs is contraindicated; Posaconazole increases concentrations and toxicities of: Sirolimus ( 4.2 , 5.1 , 7.1 ) CYP3A4 substrates (pimozide, quinidine): can result in QTc interval prolongation and cases of torsades de pointes (TdP) ( 4.3 , 5.2 ,...

Storage

16 HOW SUPPLIED/STORAGE AND HANDLING 16.1 How Supplied Posaconazole delayed-release tablets are available as yellow, coated, oblong tablets, debossed with “100” on one side containing 100 mg of posaconazole. Bottles with child-resistant closures of 60 delayed-release tablets (NDC 62135-429-60).

Frequently Asked Questions

What is Posaconazole Delayed-release used for?

1 INDICATIONS AND USAGE Posaconazole delayed-release tablets is an azole antifungal agent indicated as follows: ( 1 ) Posaconazole delayed-release tablets are indicated for the prophylaxis of invasive Aspergillus and Candida infections in patients who are at high risk of developing these infections due to being severely immunocompromised, such as hematopoietic stem cell transplant (HSCT) recipients with graftversushost disease (GVHD) or those with hematologic malignancies with prolonged neutropenia from chemotherapy as follows: ( 1.2 ) Posaconazole delayed-release tablets : adults and pediatric patients 13 years of age and older ( 1 ) 1.2 Prophylaxis of Invasive Aspergillus and Candida Infections Posaconazole is indicated for the prophylaxis of invasive Aspergillus and Candida infections i...

What are the side effects of Posaconazole Delayed-release?

6 ADVERSE REACTIONS The following serious and otherwise important adverse reactions are discussed in detail in another section of the labeling: Hypersensitivity [see Contraindications ( 4.1 )] Arrhythmias and QT Prolongation [see Warnings and Precautions ( 5.2 )] Hepatic Toxicity [see Warnings and Precautions ( 5.4 )] Adult Patients : Common adverse reactions in studies with posaconazole in adults are diarrhea, nausea, fever, vomiting, headache, coughing, and hypokalemia. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Chartwell RX, LLC at 1-845-232-1683 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch .

What are the important warnings for Posaconazole Delayed-release?

5 WARNINGS AND PRECAUTIONS Calcineurin-Inhibitor Toxicity: Posaconazole increases concentrations of cyclosporine or tacrolimus; reduce dose of cyclosporine and tacrolimus and monitor concentrations frequently. ( 5.1 ) Arrhythmias and QTc Prolongation: Posaconazole has been shown to prolong the QTc interval and cause cases of TdP. Administer with caution to patients with potentially proarrhythmic conditions. Do not administer with drugs known to prolong QTc interval and metabolized through CYP3A4. ( 5.2 ) Electrolyte Disturbances: Monitor and correct, especially those involving potassium (K + ), magnesium (Mg ++ ), and Calcium (Ca + ) before and during posaconazole therapy. ( 5.3 ) Hepatic Toxicity: Elevations in liver tests may occur. 4 CONTRAINDICATIONS Known hypersensitivity to posaconazole or other azole antifungal agents. ( 4.1 ) Coadministration of posaconazole with the following drugs is contraindicated; Posaconazole increases concentrations and toxicities of: Sirolimus ( 4.2 , 5.1 , 7.1 ) CYP3A4 substrates (pimozide, quinidine): can result in QTc interval prolongation and cases of torsades de pointes (TdP) ( 4.3 , 5.2 ,...

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Medical Disclaimer

This drug information is for educational purposes only and should not replace professional medical advice. Drug information is sourced from the FDA National Drug Code Directory and Structured Product Labeling. Always consult with a healthcare provider before starting, stopping, or changing any medication.