Tolsura

Generic name: itraconazole
Brand names: Onmel, Sporanox, Sporanox PulsePak, Tolsura
Drug class: Azole antifungals

Medically reviewed by  A Ras MD

What is Tolsura?

Tolsura is a prescription medicine used to treat the following fungal infections in adults: blastomycosis, histoplasmosis, and aspergillosis.
Tolsura is not for use for the treatment of fungal infections of the toenails or fingernails (onychomycosis).
Tolsura is not for use in place of other medicines that contain itraconazole.
It is not known if Tolsura is safe and effective in children.

Description

TOLSURA (itraconazole capsules) is an azole antifungal drug for oral use. Itraconazole is an equal mixture of four diastereomers (two enantiomeric pairs), each possessing three chiral centers. It may be represented by the following structural formula and nomenclature:

(±)-1-[(R*)-sec-butyl]-4-[p-[4-[p-[[(2R*,4S*)-2-(2,4-dichlorophenyl)-2-(1H-1,2,4-triazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy]phenyl]-1-piperazinyl]phenyl]-Δ2-1,2,4-triazolin-5-one mixture with (±)-1-[(R*)-sec-butyl]-4-[p-[4-[p-[[(2S*,4R*)-2-(2,4-dichlorophenyl)-2-(1H-1,2,4-triazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy]phenyl]-1-piperazinyl]phenyl]-Δ2-1,2,4-triazolin-5-one

or

(±)-1-[(RS)-sec-butyl]-4-[p-[4-[p-[[(2R,4S)-2-(2,4-dichlorophenyl)-2-(1H-1,2,4-triazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy]phenyl]-1-piperazinyl]phenyl]-Δ2-1,2,4-triazolin-5-one.

Itraconazole has a molecular formula of C35H38Cl2N8O4 and a molecular weight of 705.64. It is a white to slightly yellowish powder. It is insoluble in water, very slightly soluble in alcohols, and freely soluble in dichloromethane. It has a pKa of 3.70 (based on extrapolation of values obtained from methanolic solutions) and a log (n-octanol/water) partition coefficient of 5.66 at pH 8.1.

Each TOLSURA capsule contains 65 mg of itraconazole dispersed in a polymer matrix and encapsulated in a hard gelatin capsule. The inactive ingredients are colloidal silicon dioxide, hypromellose phthalate, magnesium stearate and sodium starch glycolate.

What is the most important information I should know about Tolsura?

Tolsura can cause serious side effects, including:

1. Congestive heart failure. Tolsura can cause congestive heart failure or make congestive heart failure that you already have worse. Stop taking Tolsura and call your doctor right away if you have any of these symptoms of congestive heart failure:

• shortness of breath
• swelling of your feet, ankles or legs
• sudden weight gain
• increased tiredness
• coughing up white or pink mucus (phlegm)
• fast heartbeat
• waking up at night more than normal for you

2. Heart problems and other serious medical problems. Serious medical problems that affect the heart and other parts of your body can happen if you take Tolsura with certain other medicines.

• Do not take Tolsura if you take any of the following medicines:
  • avanafil
  • disopyramide
  • dofetilide
  • dronedarone
  • eplerenone
  • ergot alkaloids (such as dihydroergotamine or ergotamine)
  • felodipine
  • irinotecan
  • isavuconazonium
  • ivabradine
  • lomitapide
  • lovastatin
  • lurasidone
  • methadone
  • midazolam (taken by mouth)
  • naloxegol
  • nisoldipine
  • pimozide
  • quinidine
  • ranolazine
  • simvastatin
  • ticagrelor
  • triazolam
• Do not take Tolsura if you have kidney or liver problems and take any of the following medicines:
  • colchicine
  • fesoterodine
  • solifenacin
• Do not take Tolsura:
  • if you have been told that an enzyme in your body, called CYP2D6, breaks down (metabolizes) certain medicines in your body too slowly.
  • if you are taking the medicine eliglustat and are also taking a medicine that slows the rate that your body breaks down (metabolizes) certain other medicines (CYP2D inhibitor). Ask your doctor or pharmacist if you take any of these medicines.

These are not complete lists of medicines that can interact with Tolsura. Tolsura may affect the way other medicines work, and other medicines may affect how Tolsura works. You can ask your pharmacist for a list of medicines that interact with Tolsura.
Before you start taking Tolsura, tell your doctor about all the medicines you take, including prescription and over-the-counter medicines, vitamins, and herbal supplements.
Before you start any new medicine, ask your doctor or pharmacist if it is safe to take it with Tolsura or within 2 weeks after stopping treatment with Tolsura.

3. Liver problems. Tolsura can cause serious liver problems which may be severe and lead to death. Stop taking Tolsura and call your doctor right away if you have any of these symptoms of liver problems:

• unusual fatigue
• loss of appetite
• nausea or vomiting
• your skin or the white part of your eyes turn yellow (jaundice)
• dark (tea-colored) urine
• light-colored stools (bowel movement)

For more information about side effects, see “What are the possible side effects of Tolsura?”

Who should not take Tolsura?

Do not take Tolsura if you:

• See “What is the most important information I should know about Tolsura?”
• are allergic to itraconazole or any of the ingredients in Tolsura. See the end of this Patient Information guide for a complete list of ingredients in Tolsura.

What should I tell my healthcare provider before taking Tolsura?

Before taking Tolsura, tell your doctor about all of your medical conditions, including if you:

• have heart problems.
• have lung problems.
• have kidney problems.
• have liver problems.
• have had an allergic reaction to a medicine used to treat a fungal infection.
• are pregnant or plan to become pregnant. It is not known if Tolsura will harm your unborn baby. Tell your doctor if you become pregnant during treatment with Tolsura.
• are breastfeeding or plan to breastfeed. Tolsura can pass into your breast milk. Talk to your doctor about the best way to feed your baby if you take Tolsura.

Before you start taking Tolsura, tell your doctor about all the medicines you take, including prescription and over-the-counter medicines, vitamins, and herbal supplements.
Especially tell your doctor if you take:

• a medicine to treat high blood pressure or certain other heart problems called a calcium channel blocker.
• a medicine to reduce acid in your stomach called a proton pump inhibitor, such as omeprazole.

How should I take Tolsura?

• Take Tolsura exactly as prescribed by your doctor. Your doctor will tell you how much Tolsura to take and when to take it.
• Tolsura must be taken with food.
• Tolsura capsules must be swallowed whole.
• Do not chew, crush or break Tolsura capsules.
• If you take too much Tolsura, call your doctor or go to the nearest hospital emergency room right away.

What should I avoid while taking Tolsura?

Tolsura can cause dizziness and vision problems. Do not drive or operate machinery until you know how Tolsura affects you. Tell your doctor if you get dizziness or vision problems.

What are the possible side effects of Tolsura?

Tolsura may cause serious side effects, including:

• See “What is the most important information I should know about Tolsura?”
• Nerve problems (neuropathy). Nerve problems have happened in some people who have taken Tolsura for longer than 3 months. Call your doctor right away if you have tingling or numbness in your hands or feet. Your doctor may stop your treatment with Tolsura if you have nerve problems.
• Hearing loss. Hearing loss can happen in some people who take Tolsura. Hearing loss usually improves when treatment with Tolsura is stopped, but hearing loss has been permanent in some people. Call your doctor if you have any changes in your hearing.

The most common side effects of Tolsura include:

• nausea
• rash
• vomiting
• swelling
• headache
• diarrhea
• fatigue
• fever
• itching
• high blood pressure
• abnormal liver blood tests
• stomach pain
• dizziness
• low blood potassium levels
• loss of appetite
• general feeling of discomfort
• decreased sex drive
• sleepiness
• elevated levels of a type of protein, called albumin, in your urine
• erectile dysfunction

These are not all the possible side effects of Tolsura.
Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

Label

PRINCIPAL DISPLAY PANEL – 65 MG CAPSULE BOTTLE LABEL

• NDC 51862-462-60
• TOLSURA®
  (Itraconazole Capsules)
• 65 mg
• Attention: Tolsura® is NOT interchangeable
  on a mg per mg basis with other
  formulations of itraconazole.
• Rx Only
  60 Capsules
• mayne pharma

What are the ingredients in Tolsura?

Active ingredient: itraconazole
Inactive ingredients: colloidal silicon dioxide, hypromellose phthalate, magnesium stearate and sodium starch glycolate.

SRC: NLM .