Posaconazole

Posaconazole delayed-release tablets, posaconazole injection, and posaconazole oral suspension are prescription medicines used to help prevent and treat fungal infections that can spread throughout your body (invasive fungal infections). These infections are caused by fungi called Aspergillus or Candida. Posaconazole is used in people who have an increased chance of getting these infections due to a weak immune system. These include people who have:

• had a hematopoietic stem cell transplantation (bone marrow transplant) with graft versus host disease
• a low white blood cell count due to chemotherapy for blood cancers (hematologic malignancy)

Posaconazole oral suspension is also used to treat severe yeast infections of the mouth and throat caused by Candida called oropharyngeal candidiasis (OPC). Posaconazole oral suspension can be used as the first treatment for OPC, or as another treatment for OPC after itraconazole or fluconazole treatment has not worked.

This medication may be prescribed for other uses. Ask your doctor or pharmacist for more information.

Tell your healthcare provider about all of the medications you take including prescription and non-prescription medicines, vitamins, and herbal supplements.

Do not take posaconazole if you are taking any of the following medicines:

• sirolimus
• pimozide
• quinidine
• certain statin medicines that lower cholesterol (atorvastatin, lovastatin, simvastatin)
• ergot alkaloids (ergotamine, dihydroergotamine)

​Also, you should tell your healthcare provider if you:

• are taking certain medicines that lower your immune system like cyclosporine or tacrolimus
• are taking certain drugs for HIV infection, such as ritonavir, atazanavir, efavirenz, or fosamprenavir. Efavirenz and fosamprenavir can cause a decrease in the posaconazole levels in your body. Efavirenz and fosamprenavir should not be taken with posaconazole.
• are taking midazolam, a hypnotic and sedative medicine

Ask your healthcare provider or pharmacist if you are not sure if you are taking any of these medicines.

Do not start taking a new medicine without talking to your healthcare provider or pharmacist.

Posaconazole may cause serious side effects, including:

• drug interactions with cyclosporine or tacrolimus. If you take posaconazole with cyclosporine or tacrolimus, your blood levels of cyclosporine or tacrolimus may increase. Serious side effects can happen in your kidney or brain if you have high levels of cyclosporine or tacrolimus in your blood. Your healthcare provider should do blood tests to check your levels of cyclosporine or tacrolimus if you are taking these medicines while taking posaconazole. Tell your healthcare provider right away if you have swelling in your arm or leg or shortness of breath.
• problems with the electrical system of your heart (arrhythmias and QTc prolongation). Certain medicines used to treat fungus called azoles, including posaconazole may cause heart rhythm problems. People who have certain heart problems or who take certain medicines have a higher chance for this problem. Tell your healthcare provider right away if your heartbeat becomes fast or irregular.
• liver problems. Some people who also have other serious medical problems may have severe liver problems that may lead to death, especially if you take certain doses of posaconazole. Your healthcare provider should do blood tests to check your liver while you are taking posaconazole. Call your healthcare provider right away if you have any of the following symptoms of liver problems:
  • itchy skin
  • nausea or vomiting
  • yellowing of your eyes
  • feeling very tired
  • flu-like symptoms
• increased amounts of midazolam in your blood. If you take posaconazole with midazolam, posaconazole increases the amount of midazolam in your blood. This can make your sleepiness last longer. Your healthcare provider should check you closely for side effects if you take midazolam with posaconazole.

Keep this and all medicines out of the reach of children.

• Store posaconazole delayed release tablets at room temperature between 68°F to 77°F (20°C to 25°C).
• Keep posaconazole delayed-release tablets in a tightly closed container.
• Do not freeze posaconazole oral suspension.
• Posaconazole injection can be stored up to 24 hours refrigerated.
• Safely throw away medicine that is out of date or no longer needed.

Antifungal; azole (triazole derivative).1 2 3 4 5 6

It is very important that your doctor check your progress at regular visits. This will allow your doctor to see if the medicine is working properly and to decide if you should continue to take it. Blood tests will be needed to check for unwanted effects.

You should not use atorvastatin (Lipitor®), lovastatin (Mevacor®), pimozide (Orap®), quinidine (Quinaglute®), simvastatin (Zocor®), sirolimus (Rapamune®), or ergotamine medicines (eg, bromocriptine, dihydroergotamine, ergonovine, ergotamine, methylergonovine, methysergide, Cafergot®, Ergomar®, Wigraine®). Using any of them together with posaconazole may increase the chance of unwanted effects.

posaconazole can cause changes in heart rhythms, such as a condition called QT prolongation. It may change the way your heart beats and cause fainting or serious side effects in some patients. Contact your doctor right away if you have any symptoms of heart rhythm problems, such as fast, pounding, or irregular heartbeats.

Check with your doctor right away if you have pain or tenderness in the upper stomach, pale stools, dark urine, loss of appetite, nausea, unusual tiredness or weakness, or yellow skin or eyes. These could be symptoms of a serious liver problem.

Check with your doctor right away if you have severe diarrhea or vomiting while using posaconazole.

Do not take other medicines unless they have been discussed with your doctor. This includes prescription or nonprescription (over-the-counter [OTC]) medicines and herbal or vitamin supplements.

• Antifungal Agent, Oral

Prophylaxis of invasive Aspergillus and Candida infections: Suspension and delayed-release tablets (13 years and older) and injection (18 years and older): Prophylaxis of invasive Aspergillus and Candida infections in patients who are at high risk of developing these infections due to being severely immunocompromised (eg, hematopoietic stem cell transplant [HSCT] recipients with graft-versus-host disease [GVHD] or those with prolonged neutropenia secondary to chemotherapy for hematologic malignancies).

Oropharyngeal candidiasis: Suspension (13 years and older): Treatment of oropharyngeal candidiasis (including patients refractory to itraconazole and/or fluconazole)

Suspension: Oral: Shake well before use. Administer with provided measured dosing spoon during or within 20 minutes following a full meal; patients who are unable to eat a full meal may take each dose with an oral liquid nutritional supplement; or acidic carbonated beverage (eg, ginger ale). Consider an alternative antifungal in patients unable to eat a full meal or tolerate a liquid nutritional supplement or acidic carbonated beverage and who do not have the option of taking the delayed-release tablet or injection.

Tablets (delayed release): Oral: Swallow tablets whole; do not divide, crush, dissolve, or chew. Administer with food.

Closely monitor patients with severe diarrhea or vomiting for breakthrough fungal infections.

Injection: Infuse over 90 minutes via a central venous line. Do not administer IV push or bolus. Must be infused through an in-line filter (0.22-micron polyethersulfone [PES] or polyvinylidene difluoride [PVDF]). Infusion through a peripheral line should only be used as a one-time infusion over 30 minutes in a patient who will be receiving a central venous line for subsequent doses, or to bridge a period during which a central venous line is to be replaced or is in use for another infusion. Note: In clinical trials, multiple peripheral infusions given through the same vein resulted in infusion-site reactions.

Adverse events have been observed in animal reproduction studies.

• Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)

• Patient may experience abdominal pain, constipation, cough, lack of appetite, joint pain, back pain, or insomnia. Have patient report immediately to prescriber signs of electrolyte problems (mood changes, confusion, muscle pain or weakness, abnormal heartbeat, seizures, lack of appetite, or severe nausea or vomiting), signs of liver problems (dark urine, fatigue, lack of appetite, nausea, abdominal pain, light-colored stools, vomiting, or jaundice), signs of high blood sugar (confusion, fatigue, increased thirst, increased hunger, polyuria, flushing, fast breathing, or breath that smells like fruit), abnormal heartbeat, angina, tachycardia, severe dizziness, passing out, vision changes, severe diarrhea, severe nausea, severe vomiting, shortness of breath, swelling of arms or legs, chills, pharyngitis, severe headache, nosebleed, bruising, bleeding, abnormal vaginal bleeding, severe loss of strength and energy, mouth irritation, or mouth sores (HCAHPS).

• Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions.

Intended Use and Disclaimer: Should not be printed and given to patients. This information is intended to serve as a concise initial reference for health care professionals to use when discussing medications with a patient. You must ultimately rely on your own discretion, experience, and judgment in diagnosing, treating, and advising patients.

IV:
Moderate or severe renal dysfunction (estimated glomerular filtration rate [eGFR] less than 50 mL/min): The injection should be avoided unless benefit justifies risk.

Comments: Serum creatinine levels should be monitored closely; if levels increase, switching to oral posaconazole therapy should be considered.

Oral:
Mild to moderate renal dysfunction (eGFR 20 to 80 mL/min/1.73 m2): No adjustment recommended.
Severe renal dysfunction (eGFR less than 20 mL/min/1.73 m2): No adjustment recommended; patients should be monitored closely for breakthrough fungal infections.