Posaconazole

Table of contents

  • Brand Names
  • Drug Combinations
  • Chemistry
  • Pharmacologic Category
  • Mechanism of Action
  • Therapeutic Use
  • Unlabeled Use
  • Pregnancy and Lactation Implications
  • Contraindications
  • Warnings and Precautions
  • Adverse Reactions
  • Genes that may be involved
  • Inhibits
  • Drug Interactions
  • Nutrition/Nutraceutical Interactions
  • Dosage
  • Pharmacokinetics and Pharmacodynamics
  • Special Considerations

Brand Names

Europe

Austria: Noxafil, Posaconazole (d); Belgium: Noxafil; Czech Republic: Noxafil, Posaconazole (d); Denmark: Noxafil; Estonia: Noxafil; Finland: Noxafil; France: Noxafil; Germany: Noxafil, Posaconazole (d); Greece: Noxafil; Hungary: Noxafil, Posaconazole (d); Ireland: Noxafil; Italy: Noxafil; Latvia: Noxafil; Lithuania: Noxafil; Luxembourg: Noxafil, Posaconazole (d); Malta: Noxafil, Posaconazole (d); Netherlands: Noxafil, Posaconazole (d); Poland: Noxafil, Posaconazole (d); Portugal: Noxafil, Posaconazole (d); Romania: Noxafil, Posaconazole (d); Slovakia: Noxafil; Slovenia: Noxafil; Spain: Noxafil; Sweden: Noxafil, Posaconazole (d); UK: Noxafil.

North America

Canada: Posanol; USA: Noxafil.

Drug combinations

Posaconazole, Mometasone, and Orbifloxacin

Chemistry

Posaconazole: C~37~H~42~F~2~N~8~O~4~. Mw: 700.78. (1) 3H-1,2,4-Triazol-3-one, 4-[4-[4-[4-[[5-(2,4-difluorophenyl)tetrahydro-5-(1H-1,2,4-triazol-1-ylmethyl)-3-furanyl]methoxy]phenyl]-1-piperazinyl]phenyl]-2-(1-ethyl-2-hydroxypropyl)-2,4-dihydro-, [3R-[3α(1S*,2S*),5α]]-; (2) 4-[p-[4-[p-[[(3R,5R)-5-(2,4-Difluorophenyl)tetrahydro-5-(1H-1,2,4-triazol-1-ylmethyl)-3-furyl]methoxy]phenyl]-1-piperazinyl]phenyl]-1-[(1S,2S)-1-ethyl-2-hydroxypropyl]-Δ^2^-1,2,4-triazolin-5-one. CAS-171228-49-2 (1999).

Pharmacologic Category

Antifungals; Azoles. (ATC-Code: J02AC04).

Mechanism of action

Interferes with fungal cytochrome P450 (latosterol-14α-demethylase) activity, decreasing ergosterol synthesis and inhibiting fungal cell membrane formation.

Therapeutic use

Prophylaxis of invasive Aspergillus and Candida infections in severely-immunocompromised patients. Treatment of oropharyngeal candidiasis (including patients refractory to itraconazole and/or fluconazole).

Pregnancy and lactiation implications

Teratogenic in animal studies. There are no adequate, well-controlled studies in pregnant women. Use only if benefit to mother justifies potential risk to fetus during pregnancy or breast-feeding.

Unlabeled use

Salvage therapy of refractory invasive fungal infections. Mucormycosis.

Contraindications

Hypersensitivity to posaconazole or any component of the formulation. Co-administration of cisapride, ergot alkaloids, pimozide, quinidine, or sirolimus.

Warnings and precautions

Use with caution in hypersensitivity to other azole antifungal agents (cross-reaction may occur). Hepatic dysfunction occurred (use with caution in hepatic impairment). Use caution in increased risk of arrhythmia (concurrent QTc-prolonging drugs, hypokalemia). Breakthrough fungal infections in severe diarrhea or vomiting might occur. Use caution in severe renal impairment. Levels of cyclosporine may significantly increase if used concomitantly with posaconazole and may result in rare serious adverse events (e.g. nephrotoxicity, leukoencephalopathy, and death). High potential for interactions in patients receiving drugs that decrease absorption or increase metabolism of posaconazole.

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