What is/are Posaconazole?
Posaconazole is a triazole antifungal drug marketed in the United States, the European Union, and in other countries by Schering-Plough under the trade name Noxafil. In Canada, posaconazole is marketed by Schering-Plough under the trade name Posanol.
It is used to treat invasive infections by Candida species, Mucor, and Aspergillus species in severely immunocompromised patients. Clinical evidence for its utility in treatment of invasive disease caused by Fusarium species (fusariosis) is limited.
Two studies suggest posaconazole may be superior to other triazoles, such as fluconazole or itraconazole, in the prevention of invasive fungal infections, although it may cause more serious side effects.
There is also some indication that posaconazole may be the most effective treatment for both chronic and acute Chagas disease, showing much better efficacy than benznidazole. Schering-Plough is currently recruiting participants for a phase 2 clinical trial in Argentina to test its efficacy against asymptomatic, chronic Chagas.
- Headache with chest pain and severe dizziness, fainting, fast or pounding heartbeats;
- Slow heartbeats;
- Signs of an infection such as fever, chills, sore throat, flu symptoms, vomiting, mouth sores;
- Pale skin, easy bruising or bleeding, feeling light-headed or short of breath, rapid heart rate, trouble concentrating;
- Low potassium (confusion, uneven heart rate, extreme thirst, increased urination, leg discomfort, muscle weakness or limp feeling);
- Feeling like you might pass out;
- Nausea, upper stomach pain, itching, loss of appetite, dark urine, clay-colored stools, jaundice (yellowing of the skin or eyes); or
- Dangerously high blood pressure (severe headache, blurred vision, buzzing in your ears, anxiety, chest pain, shortness of breath, seizure).
Less serious side effects of posaconazole may include:
- Mild headache, dizziness;
- Tired feeling
- Swelling of your ankles or feet;
- Diarrhea, constipation, stomach pain;
- Joint or muscle pain; or
- Sleep problems (insomnia).
Mechanism of action
Posaconazole works by disrupting the close packing of acyl chains of phospholipids, impairing the functions of certain membrane-bound enzyme systems such as ATPase and enzymes of the electron transport system, thus inhibiting growth of the fungi. It does this by blocking the synthesis of ergosterol by inhibiting of the enzyme lanosterol 14α-demethylase and accumulation of methylated sterol precursors. Posaconazole is significantly more potent at inhibiting 14-alpha demethylase than itraconazole.
This article uses material from the Wikipedia article Posaconazole, which is released under the Creative Commons Attribution-Share-Alike License 3.0.