Posaconazole intravenous
Other products: Posaconazole
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Azole Antifungal
Dosing in kidney impairment
Dosage Modifications in Patients with Renal Impairment Avoid the use of posaconazole injection in patients with eGFR less than 50 mL/minute/1.73 m 2 , unless an assessment of the benefit/risk to the patient justifies its use. If the decision is made to use posaconazole injection in patients with eGFR less than 50 mL/minute/1.73 m 2 , closely monitor serum creatinine levels, and, if increases occur, consider changing to oral posaconazole therapy.
The recommended dosage of posaconazole injection in patients with eGFR 50 to 90 mL/minute/1.73 m 2 is the same as those with normal renal function.
Dosing in liver impairment
Hepatic Impairment No dosage adjustment is recommended for posaconazole injection in patients with mild, moderate, or severe hepatic impairment (Child-Pugh Class A, B, or C, respectively) [see Clinical Pharmacology]. However, a specific hepatic impairment study has not been conducted with the posaconazole injection.
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Preparation and administration
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Important Administration Instructions Posaconazole injection Administer via a central venous line, including a central venous catheter or peripherally inserted central catheter (PICC), by slow intravenous infusion over approximately 90 minutes [see [See table below.]
Preparation of Posaconazole Injection Preparation of Posaconazole Injection:
Remove the vial of posaconazole injection from the refrigerator and allow to equilibrate to room temperature prior to use.
To prepare the required dose, aseptically transfer one vial of posaconazole injection (containing 300 mg of posaconazole in 16.7 mL of solution) to an intravenous bag or bottle of one of the following compatible diluents to achieve a final posaconazole concentration between 1 mg/mL and 2 mg/mL: o 0.45% Sodium Chloride Injection o 0.9% Sodium Chloride Injection o 5% Dextrose Injection o 5% Dextrose and 0.45% Sodium Chloride Injection o 5% Dextrose and 0.9% Sodium Chloride Injection o 5% Dextrose and 20 mEq Potassium Chloride Injection Use of other diluents is not recommended because they may result in particulate formation.
Discard any unused posaconazole injection from the vial.
Parenteral drug products should be inspected visually for particulate matter prior to administration, whenever solution and container permit. Once admixed, the diluted posaconazole infusion solution ranges from colorless to yellow (variations of color within this range do not affect the quality of the product).
Immediately use the diluted posaconazole infusion solution, once admixed. If not used immediately, refrigerate (2 to 8°C (36 to 46°F)) the diluted posaconazole infusion solution up to 24 hours. Discard any unused portion. Incompatible Diluents Co-administration of drug products besides the infusion solutions or products stated above are not recommended because this may result in particulate formation.
The following diluents were determined to be incompatible with posaconazole injection; thus, do not dilute posaconazole injection with them:
Lactated Ringer’s Injection
Lactated Ringer’s and 5% Dextrose Injection
4.2% Sodium Bicarbonate Injection
Administration of Diluted Posaconazole Infusion Solution See Dosage and Administration for the preparation instructions for the diluted Posaconazole Solution. Important Administration Instructions for the Diluted Posaconazole Infusion Solution
Must administer diluted posaconazole infusion solution through a 0.22-micron polyethersulfone (PES) or polyvinylidene difluoride (PVDF) filter.
Administer diluted posaconazole infusion solution via a central venous line, including a central venous catheter (CVC) or peripherally inserted central catheter (PICC), by slow intravenous infusion over approximately 90 minutes [see Adverse Reactions]
If a CVC or PICC are not available, may administer diluted posaconazole solution once through a peripheral venous catheter by intravenous infusion over approximately 30 minutes to bridge the period during which a CVC or PICC are replaced, inserted, or unavailable for use (e.g., the CVC is being used for intravenous treatment with another product).
However, do not administer diluted posaconazole infusion solution more than once via peripheral venous catheter because in clinical trials, multiple peripheral infusions given through the same vein resulted in infusion site reactions [see Adverse Reactions] .
When multiple dosing is required, the infusion should be done via a central venous line. Additional Administration Instructions for the Diluted Posaconazole Infusion Solution
Administer diluted posaconazole infusion solution intravenously through the same intravenous line (or cannula) with the following compatible infusion solutions: o 0.45% Sodium Chloride Injection o 0.9% Sodium Chloride Injection o 5% Dextrose Injection o 5% Dextrose and 0.45% Sodium Chloride Injection o 5% Dextrose and 0.9% Sodium Chloride Injection o 5% Dextrose and 20 mEq potassium chloride Injection
Administer diluted posaconazole infusion solution intravenously at the same time through the same intravenous line (or cannula) with the following intravenous drug products prepared in 5% Dextrose Injection or 0.9% Sodium Chloride Injection: o Amikacin Sulfate Injection o Caspofungin Acetate for Injection o Ciprofloxacin Injection o Daptomycin for Injection o Dobutamine Injection o Famotidine Injection o Filgrastim Injection o Gentamicin Injection o Hydromorphone Hydrochloride Injection o Levofloxacin Injection o Lorazepam Injection o Meropenem for Injection o Micafungin for Injection o Morphine Sulfate Injection o Norepinephrine Bitartrate Injection o Potassium Chloride Injection o Vancomycin Hydrochloride for Injection
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- Posaconazole intravenous
Label text (17 paragraphs)
Table 15 and Table 17 include drugs with clinically important drug interactions when administered concomitantly with posaconazole and instructions for preventing or managing them. These recommendations are based on either drug interaction studies or predicted interactions due to the expected magnitude of interaction and potential for serious adverse reactions or loss of efficacy [see Clinical Pharmacology ( 12.3 )]. The following information was derived from data with Noxafil ® (posaconazole) oral suspension or another posaconazole tablet formulation unless otherwise noted.
All clinically important drug interactions with Noxafil ® (posaconazole) oral suspension, except for those that affect the absorption of posaconazole (via gastric pH and motility), are considered relevant to clinically important drug interactions with posaconazole injection [Clinical Pharmacology ( 12.3 )]. Consult the labeling of concomitantly used drugs to obtain further information about interactions with posaconazole.
Interaction Drug Interaction Rifabutin, phenytoin, efavirenz Avoid coadministration unless the benefit outweighs the risks ( 7.1 , 7.2 ) Other drugs metabolized by CYP3A4 Consider dosage adjustment and monitor for adverse effects and toxicity ( 7.2 ) Digoxin Monitor digoxin plasma concentrations ( 7.2 ) Fosamprenavir Monitor for breakthrough fungal infections ( 7.1 )
7.1 Effects of Other Drugs on Posaconazole Injection 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. Concomitant use of posaconazole with drugs that can decrease the plasma posaconazole concentrations should generally be avoided unless the benefit outweighs the risk. If such drugs are necessary, patients should be monitored closely for breakthrough fungal infections.
Table 15: Drug Interactions Affecting Posaconazole Injection When Administered Concomitantly with Other Drugs UDP-Glucuronidase Inducers Mechanism and Clinical Effect(s) Posaconazole is a UDP-glucuronosyltransferase substrate. Concomitant use of posaconazole with UDP-glucuronidase inducers may decrease posaconazole exposure [see Clinical Pharmacology ( 12.3 )] , which may reduce the effectiveness of posaconazole. Prevention or Management Efavirenz Avoid concomitant use of posaconazole with efavirenz, unless the benefit outweighs the risks. Rifabutin Avoid concomitant use of posaconazole with rifabutin unless the benefit to the patient outweighs the risk.
If concomitant use is needed, monitor closely for breakthrough fungal infections. See Table 17 for rifabutin monitoring considerations when posaconazole affects rifabutin via CYP3A4 inhibition. Phenytoin Avoid concomitant use of posaconazole with phenytoin unless the benefit to the patient outweighs the risk. If concomitant use is needed, monitor for breakthrough fungal infections. See Table 17 for phenytoin monitoring considerations when posaconazole affects phenytoin via CYP3A4 inhibition.
Fosamprenavir Mechanism and Clinical Effect(s) Concomitant use of posaconazole with fosamprenavir may lead to decreased posaconazole plasma concentrations [see Clinical Pharmacology ( 12.3 )] , which may reduce effectiveness of posaconazole. Prevention or Management If concomitant use of posaconazole with fosamprenavir is needed, monitor closely for breakthrough fungal infections.
7.2 Effects of Posaconazole Injection on Other Drugs Posaconazole is a strong CYP3A4 inhibitor. Therefore, concomitant use of posaconazole may increase plasma concentrations of drugs that are CYP3A4 substrates [see Clinical Pharmacology ( 12.3 )]. Table 17: Drug Interactions Affecting Drugs Administered Concomitantly with Posaconazole Injection Digoxin Clinical Effect(s) Increased digoxin plasma concentrations have been reported in patients who received concomitant posaconazole and digoxin. Prevention or Management Monitor digoxin plasma concentrations during concomitant use of posaconazole.
Glipizide Clinical Effect(s) No dosage modification of glipizide is needed when used concomitantly with posaconazole. However, glucose concentrations decrease in some patients concomitantly administered posaconazole and glipizide. Prevention or Management Increase monitoring of glucose concentrations when used concomitantly. CYP3A Substrates Immunosuppressants that are CYP3A4 Substrates Mechanism and Clinical Effect(s) Posaconazole is a strong CYP3A4 inhibitor. Therefore, plasma concentrations of CYP3A4 substrates may be increased by posaconazole use [see Clinical Pharmacology ( 12.3 )].
Prevention or Management Sirolimus Posaconazole is contraindicated with sirolimus [see Clinical Pharmacology ( 12.3 )]. Tacrolimus • At initiation of posaconazole treatment, reduce the tacrolimus dosage to approximately one-third of the original tacrolimus dosage. • Frequent monitoring of tacrolimus whole blood trough concentrations should be performed during and at discontinuation of posaconazole treatment and the tacrolimus dosage should be modified accordingly [see Warnings and Precautions ( 5.1 ) and Clinical Pharmacology ( 12.3 )]. Cyclosporine • At initiation of posaconazole treatment reduce the cyclosporine dosage to approximately three-fourths of the original dosage.
• Frequent monitoring of cyclosporine whole blood trough concentrations should be performed during and at discontinuation of posaconazole treatment and the cyclosporine dosage should be modified accordingly [see Warnings and Precautions ( 5.1 ) and Clinical Pharmacology ( 12.3 )]. CYP3A4 Substrates that Prolong QTc Interval Mechanism and Clinical Effect(s) Concomitant use of posaconazole with CYP3A4 substrates such as pimozide and quinidine may result in increased plasma concentrations of the CYP3A4 substrates leading to QTc interval prolongation and torsades de pointes [see Warnings and Precautions ( 5.2 )].
Prevention or Management Pimozide Concomitant use with posaconazole is contraindicated. Quinidine HMG-CoA Reductase Inhibitors (Statins) that are CYP3A4 Substrates Mechanism and Clinical Effect(s) Concomitant use of posaconazole with simvastatin increased simvastatin plasma concentrations which can lead to rhabdomyolysis [see Clinical Pharmacology ( 12.3 )]. Prevention or Management Atorvastatin, Lovastatin, Simvastatin Concomitant use with posaconazole is contraindicated.
Benzodiazepines that are CYP3A4 Substrates Mechanism and Clinical Effect(s) Concomitant use of posaconazole with midazolam increased midazolam plasma concentrations which could potentiate and prolong hypnotic and sedative effects [see Clinical Pharmacology ( 12.3 )]. Prevention or Management Midazolam, Alprazolam, Triazolam Closely monitor for adverse reactions associated with high plasma concentrations of benzodiazepines that are CYP3A4 substrates during concomitant use, and a benzodiazepine receptor antagonist should be available to reverse effects [see Warnings and Precautions ( 5.7 )].
Calcium Channel Blockers that are CYP3A4 Substrates Mechanism and Clinical Effect(s) Posaconazole may increase the plasma concentrations of calcium channel blockers that are substrates of CYP3A4. Prevention or Management Verapamil, Diltiazem, Nifedipine, Nicardipine, Felodipine Monitor frequently for adverse reactions and toxicity with concomitant use of posaconazole with calcium channel blockers that are CYP3A4 substrates. Dosage reduction of the calcium channel blocker may be needed.
Anti-HIV Drugs that are CYP3A4 Substrates Mechanism and Clinical Effect(s) Ritonavir and atazanavir are CYP3A4 substrates and posaconazole increased plasma concentrations of these drugs [see Clinical Pharmacology ( 12.3 )]. Prevention or Management Ritonavir and Atazanavir Monitor frequently for adverse reactions and toxicity of ritonavir and atazanavir during concomitant use. Antineoplastic Drugs that are CYP3A4 Substrates Mechanism and Clinical Effect(s) Posaconazole may increase plasma concentrations of oncology drugs that are CYP3A4 substrates, which may increase the risk of serious adverse reactions.
Prevention or Management Venetoclax CLL/SLL patients: Concomitant use of posaconazole with venetoclax during initiation and ramp-up phase is contraindicated. AML patients : With concomitant use, venetoclax dosage reduction and safety monitoring is recommended across all dosing phases [see Warnings and Precautions ( 5.11 )]. Vinca alkaloids (e.g., vincristine, vinblastine) Reserve concomitant use for patients with no alternative antifungal treatment options [see Warnings and Precautions ( 5.8 )]. Ergot Alkaloids Mechanism and Clinical Effect(s) Most of the ergot alkaloids are CYP3A4 substrates.
Posaconazole may increase the plasma concentrations of ergot alkaloids (ergotamine and dihydroergotamine) which may lead to ergotism. Prevention or Management Ergotamine, Dihydroergotamine Concomitant use with posaconazole is contraindicated.…
Contraindications
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 , 7.2 ) • CYP3A4 substrates (pimozide, quinidine): can result in QTc interval prolongation and cases of torsades de pointes (TdP) ( 4.3 , 5.2 , 7.2 ) • HMG-CoA Reductase Inhibitors Primarily Metabolized through CYP3A4 ( 4.4 , 7.2 ) • Ergot alkaloids ( 4.5 , 7.2 ) • Venetoclax: In patients with chronic lymphocytic leukemia (CLL) or small lymphocytic lymphoma (SLL) at initiation and during the ramp-up phase ( 4.6 , 5.11 , 7.2 )
4.1 Hypersensitivity Posaconazole is contraindicated in persons with known hypersensitivity to posaconazole or other azole antifungal agents.
4.2 Use with Sirolimus Posaconazole is contraindicated with sirolimus. Concomitant administration of posaconazole with sirolimus increases the sirolimus blood concentrations by approximately 9-fold and can result in sirolimus toxicity [see Drug Interactions ( 7.2 ) and Clinical Pharmacology ( 12.3 )].
4.3 QT Prolongation with Concomitant Use with CYP3A4 Substrates Posaconazole is contraindicated with CYP3A4 substrates that prolong the QT interval. Concomitant administration of posaconazole with the CYP3A4 substrates, pimozide and quinidine may result in increased plasma concentrations of these drugs, leading to QTc prolongation and cases of torsades de pointes [ see Warnings and Precautions ( 5.2 ) and Drug Interactions ( 7.2 ) ].
4.4 HMG-CoA Reductase Inhibitors Primarily Metabolized Through CYP3A4 Coadministration with the HMG-CoA reductase inhibitors that are primarily metabolized through CYP3A4 (e.g., atorvastatin, lovastatin, and simvastatin) is contraindicated since increased plasma concentration of these drugs can lead to rhabdomyolysis [see Drug Interactions ( 7.2 ) and Clinical Pharmacology ( 12.3 )] .
4.5 Use with Ergot Alkaloids Posaconazole may increase the plasma concentrations of ergot alkaloids (ergotamine and dihydroergotamine) which may lead to ergotism [ see Drug Interactions ( 7.2 ) ].
4.6 Use with Venetoclax Coadministration of…
Safety data
Reported adverse events (FAERS)
Liver injury (LiverTox)
E*Likelihood score E*: Unproved but suspected cause of clinically apparent liver injury.
Posaconazole is a potent triazole antifungal agent used in the prevention of invasive fungal infections due to aspergillosis and candida in high risk patients. Posaconazole therapy is associated with transient, asymptomatic serum aminotransferase elevations and is a suspected but rare cause of clinically apparent acute drug induced liver injury.
ABCDEA: well known cause; E: unlikely cause. [HD]: high doses only.
Pregnancy and lactation
Pregnancy
8.1 Pregnancy Risk Summary Based on findings from animal data, posaconazole may cause fetal harm when administered to pregnant women. Available data for use of posaconazole in pregnant women are insufficient to establish a drug-associated risk of major birth defects, miscarriage, or adverse maternal or fetal outcomes. In animal reproduction studies, skeletal malformations were observed when posaconazole was dosed orally to pregnant rats during organogenesis at doses ≥1.4 times the 400 mg twice daily oral suspension regimen based on steady-state plasma concentrations of posaconazole in healthy volunteers.
In pregnant rabbits dosed orally during organogenesis, doses of ≥ 3 times the clinical exposure caused an increase in resorptions ( see Data ). Based on animal data, advise pregnant women of the potential risk to a fetus. The estimated background risk of major birth defects and miscarriage for the indicated populations is unknown. All pregnancies have a background risk of birth defect, loss, or other adverse outcomes. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2 to 4% and 15 to 20%, respectively.
Data Animal Data: Posaconazole resulted in maternal toxicity (reduced food consumption and reduced body weight gain) and skeletal malformations (cranial malformations and missing ribs) when given orally to pregnant rats during organogenesis (Gestational Days 6 through 15) at doses ≥27 mg/kg (≥1.4 times the 400 mg twice daily oral suspension regimen based on steady-state plasma concentrations of drug in healthy volunteers). The no-effect dose for malformations and maternal toxicity in rats was 9 mg/kg, which is 0.7 times the exposure achieved with the 400 mg twice daily oral suspension regimen.
No malformations were seen in rabbits dosed during organogenesis (Gestational Days 7 through 19) at doses up to 80 mg/kg (5 times the exposure achieved with the 400 mg twice daily oral suspension regimen). In the rabbit, the no-effect dose was 20 mg/kg, while high doses of 40 mg/kg and 80 mg/kg (3 or 5 times the clinical exposure) caused an increase in resorptions. In rabbits dosed at 80 mg/kg, a reduction in body weight gain of females and a reduction in litter size were seen.
Lactation
8.6 Renal Impairment Posaconazole Injection Avoid use of posaconazole injection in patients with eGFR less than 50 mL/minute/1.73 m 2 unless the benefit/risk to the patient justifies its use. The inactive ingredient in posaconazole injection, Betadex Sulfobutyl Ether Sodium (SBECD) is expected to accumulate in patients with reduced renal function. Safety and effectiveness of posaconazole injection have not been established in patients with less than 50 mL/minute/1.73 m 2 . If treatment with posaconazole injection is unavoidable in patients with eGFR less than 50 mL/minute/1.73 m 2 , monitor serum creatinine levels.
If serum creatinine increases, consider changing to oral posaconazole therapy.
Breastfeeding (LactMed)
No information is available on the clinical use of posaconazole during breastfeeding. Because posaconazole is more than 98% bound to plasma proteins, the amount in milk is likely to be low. However, there is no published experience with posaconazole during breastfeeding, so an alternate drug may be preferred, especially while nursing a newborn or preterm infant.
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