tolsura - 1au3b422k9zdqzddw3my51gg-wpengine.netdna-ssl.com · limitations of use not for treating...
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Introduction
Brand name: Tolsura
Generic name: Itraconazole
Pharmacological class: Azole antifungal
Strength and Formulation: 65mg; capsules
Manufacturer: Mayne Pharma US
How supplied: Caps—60
Legal Classification: Rx
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Tolsura
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Indication
Blastomycosis
Histoplasmosis
Aspergillosis in patients who are intolerant
of or refractory to amphotericin B
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Limitations of Use
Not for treating onychomycosis
Not interchangeable or substitutable
with other itraconazole products due to
dosing differences
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Dosage & Administration
Swallow whole
Take with food
Doses >130mg should be given in 2
divided doses
Blastomycosis, histoplasmosis: 130mg
once daily, may increase by 65mg
increments; max 260mg/day
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Dosage & Administration
Aspergillosis: 130mg once daily; max
260mg/day
Life-threatening conditions: give loading
dose of 130mg three times daily for first 3
days, followed by the appropriate treatment
dose; continue for at least 3 months until
resolved
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Considerations for Special
Populations
Pregnancy: No data on exposure to itraconazole during pregnancy for approved indications
Nursing mothers: Consider benefits of breastfeeding with potential adverse effect on infant
Pediatric: Not established Elderly: Insufficient number studied;
reversible or permanent hearing loss reported Hepatic or renal impairment: Monitor
carefully
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Contraindications
Concomitant methadone, disopyramide,
dofetilide, dronedarone, quinidine,
isavuconazole, ergots, irinotecan, lurasidone,
oral midazolam, pimozide, triazolam,
felodipine, nisoldipine, ivabradine, ranolazine,
eplerenone, naloxegol, lomitapide, lovastatin,
simvastatin, avanafil, ticagrelor
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Contraindications
Concomitant colchicine, fesoterodine, or
solifenacin in renal/hepatic impairment
Concomitant eliglustat in poor or intermediate
CYP2D6 metabolizers or those taking strong
or moderate CYP2D6 inhibitors
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Boxed Warning
Congestive heart failure (CHF)
Drug interactions
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Warnings/Precautions
CHF risk (eg, ischemic/valvular disease,
COPD, renal failure, edema); monitor and
reassess treatment if occurs
Monitor for signs/symptoms of liver
dysfunction; discontinue and perform LFTs if
develop
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Warnings/Precautions
Discontinue if neuropathy, hearing loss or
hypersensitivity occurs
Elevated liver enzymes, active liver
disease, previous hepatotoxicity: not
recommended unless serious or life-
threatening situation
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Interactions
See Contraindications
Serious cardiac effects with pimozide, methadone,
quinidine, others
Concomitant alfuzosin, silodosin, tamsulosin,
fentanyl, apixaban, rivaroxaban, vorapaxar,
antineoplastics (see full labeling), simeprevir,
aliskiren, riociguat, sildenafil or tadalafil (for PAH),
everolimus, sirolimus, IV temsirolimus, salmeterol,
darifenacin, vardenafil, colchicine, conivaptan,
tolvaptan, regorafenib, saccharomyces boulardii:
not recommended during and 2 weeks after
itraconazole
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Interactions
Avoid itraconazole for more than 2 weeks
during bedaquiline therapy
Rifabutin, carbamazepine,
lumacaftor/ivacaftor: avoid 2 weeks before,
during, and 2 weeks after itraconazole
Avoid isoniazid, rifampicin, phenobarbital,
phenytoin, efavirenz, nevirapine 2 weeks
before and during itraconazole therapy
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Interactions
Potentiates alfentanil, buprenorphine, oxycodone,
sufentanil, digoxin, clarithromycin, trimetrexate, cilostazol,
dabigatran, warfarin, repaglinide, saxagliptin, praziquantel,
eletriptan, certain antineoplastics, antipsychotics, anxiolytics,
hypnotics, zopiclone, daclatasvir, indinavir, maraviroc,
nadolol, diltiazem, other dihydropyridines, verapamil,
bosentan, guanfacine, aprepitant, loperamide, budesonide,
ciclesonide, dexamethasone, fluticasone,
methylprednisolone, cyclosporine, tacrolimus, atorvastatin,
venlafaxine, fesoterodine, solifenacin, dutasteride,
oxybutynin, sildenafil, tadalafil, tolterodine, eliglustat, oral
alitretinoin, cabergoline, cannabinoids, cinacalcet, ivacaftor;
monitor, may need to reduce dose of these
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Interactions
Potentiated by ciprofloxacin, erythromycin,
clarithromycin, idelalisib, cobicistat, protease
inhibitors, diltiazem, gastric acid
suppressants (eg, antacids, H2 blockers,
PPIs), other CYP3A4 inhibitors; monitor, may
need to reduce itraconazole dose
Tinnitus or hearing impairment with quinidine
Increased risk of CHF with concomitant CCBs
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Interactions
Concomitant artemether-lumefantrine,
quinine, cobicistat, elvitegravir (ritonavir-
boosted), ritonavir, saquinavir (unboosted),
tenofovir disoproxil fumarate, dienogest,
ulipristal, netupitant; monitor for adverse
events
Antagonizes meloxicam; increase dose if
necessary
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Adverse Reactions
Nausea
Rash
Vomiting
Edema
Headache
Diarrhea
Fatigue
Fever
Pruritus
Hypertension
Abnormal hepatic function
Abdominal pain
Dizziness
Hypokalemia
Anorexia
Malaise
Decreased libido
Somnolence
Albuminuria
Impotence
Hepatotoxicity
CHF
Neuropathy
Hearing loss
Hypersensitivity
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Mechanism of Action
Itraconazole inhibits the CYP450-
dependent 14C-demethylation of ergosterol,
a vital component of fungal cell membranes
Tolsura utilizes a proprietary technology
that improves the bioavailability of poorly
soluble drugs
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Clinical Studies
The approval of Tolsura was supported by
data from clinical studies in invasive mycoses
conducted with itraconazole 100mg capsules
Dosage for Tolsura is different from that of
other itraconazole formulations
Tolsura is not interchangeable or
substitutable with other itraconazole
products
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New Product Monograph
For more information view the product
monograph available at:
https://www.empr.com/drug/tolsura/