Levoketoconazole (Oral route)

Pronunciation:

lee-voe-kee-toe-KON-a-zole

Brand Names:

Recorlev

Dosage Forms:

Tablet

Warnings:

Oral route(Tablet)

HepatotoxicityCases of hepatotoxicity with a fatal outcome or requiring liver transplantation have been reported with the use of oral ketoconazole. Some patients had no obvious risk factors for liver disease. Serious hepatotoxicity has been reported in patients receiving levoketoconazole.Levoketoconazole is contraindicated in patients with cirrhosis, acute liver disease or poorly controlled chronic liver disease, recurrent symptomatic cholelithiasis, a prior history of drug induced liver injury to ketoconazole or any azole antifungal therapy that required discontinuation of treatment, or extensive metastatic liver disease.Evaluate liver enzymes prior to and during treatment. Interrupt levoketoconazole treatment immediately if signs of hepatotoxicity occur.QT ProlongationLevoketoconazole is associated with dose-related QT interval prolongation. QT interval prolongation may lead to life-threatening ventricular dysrhythmias such as torsades de pointes.Coadministration of levoketoconazole with other drugs that prolong the QT interval associated with ventricular arrhythmias, including torsades de pointes, and use in patients with a prolonged QTcF interval of greater than 470 msec at baseline, history of torsades de pointes, ventricular tachycardia, ventricular fibrillation, or long QT syndrome (including first-degree family history) are contraindicated.Perform an ECG and correct hypokalemia and hypomagnesemia prior to and during treatment. Temporarily discontinue levoketoconazole if QTcF interval exceeds 500 msec .

Classifications:

Therapeutic—

Steroid Synthesis Inhibitor

Chemical—

Imidazole

Uses of This Medicine:

Levoketoconazole is used to treat endogenous hypercortisolemia (high cortisol levels) in patients with Cushing's syndrome who cannot have surgery or who had surgery that did not work well.

This medicine is available only with your doctor's prescription.

Before Using This Medicine:

In deciding to use a medicine, the risks of taking the medicine must be weighed against the good it will do. This is a decision you and your doctor will make. For this medicine, the following should be considered:

Allergies—

Tell your doctor if you have ever had any unusual or allergic reaction to this medicine or any other medicines. Also tell your health care professional if you have any other types of allergies, such as to foods, dyes, preservatives, or animals. For non-prescription products, read the label or package ingredients carefully.

Children—

Appropriate studies have not been performed on the relationship of age to the effects of levoketoconazole in the pediatric population. Safety and efficacy have not been established.

Older adults—

Appropriate studies performed to date have not demonstrated geriatric-specific problems that would limit the usefulness of levoketoconazole in the elderly.

Breast-feeding—

There are no adequate studies in women for determining infant risk when using this medication during breastfeeding. Weigh the potential benefits against the potential risks before taking this medication while breastfeeding.

Other medicines—

Although certain medicines should not be used together at all, in other cases two different medicines may be used together even if an interaction might occur. In these cases, your doctor may want to change the dose, or other precautions may be necessary. When you are taking this medicine, it is especially important that your healthcare professional know if you are taking any of the medicines listed below. The following interactions have been selected on the basis of their potential significance and are not necessarily all-inclusive.

Using this medicine with any of the following medicines is not recommended. Your doctor may decide not to treat you with this medication or change some of the other medicines you take.

Abemaciclib
Acalabrutinib
Adagrasib
Alfentanil
Alfuzosin
Amiodarone
Amisulpride
Amitriptyline
Anagrelide
Apixaban
Apomorphine
Aprepitant
Aripiprazole
Aripiprazole Lauroxil
Arsenic Trioxide
Asenapine
Astemizole
Atazanavir
Avanafil
Avapritinib
Azithromycin
Bedaquiline
Bepridil
Bosutinib
Brotizolam
Budesonide
Buprenorphine
Buserelin
Buspirone
Ceritinib
Chloroquine
Chlorpromazine
Ciprofloxacin
Cisapride
Citalopram
Clarithromycin
Clofazimine
Clomipramine
Clozapine
Cobimetinib
Colchicine
Conivaptan
Crizotinib
Cyclobenzaprine
Cyclosporine
Dabigatran Etexilate
Dabrafenib
Daridorexant
Darifenacin
Darolutamide
Darunavir
Dasatinib
Degarelix
Delamanid
Desipramine
Deslorelin
Deutetrabenazine
Digoxin
Dihydroergotamine
Disopyramide
Dofetilide
Dolasetron
Domperidone
Donepezil
Doxepin
Dronedarone
Droperidol
Ebastine
Efavirenz
Elagolix
Eletriptan
Eliglustat
Elvitegravir
Encorafenib
Entrectinib
Eplerenone
Ergotamine
Eribulin
Erythromycin
Escitalopram
Everolimus
Famotidine
Felbamate
Felodipine
Fentanyl
Fexinidazole
Fexofenadine
Finerenone
Fingolimod
Flecainide
Flibanserin
Fluconazole
Fluoxetine
Fluticasone
Formoterol
Fosaprepitant
Foscarnet
Fosphenytoin
Galantamine
Gatifloxacin
Gemifloxacin
Gilteritinib
Glasdegib
Gonadorelin
Goserelin
Granisetron
Halofantrine
Haloperidol
Histrelin
Hydroquinidine
Hydroxychloroquine
Hydroxyzine
Ibrexafungerp
Ibrutinib
Ibutilide
Iloperidone
Imipramine
Indinavir
Inotuzumab Ozogamicin
Isavuconazole
Itraconazole
Ivabradine
Ivacaftor
Ketoconazole
Lapatinib
Lefamulin
Lenvatinib
Leuprolide
Levofloxacin
Lofexidine
Lomitapide
Lopinavir
Lovastatin
Lumefantrine
Lurasidone
Macimorelin
Maraviroc
Mefloquine
Mesoridazine
Methadone
Methotrimeprazine
Metronidazole
Midazolam
Midostaurin
Mifepristone
Mizolastine
Mobocertinib
Moricizine
Moxifloxacin
Nafarelin
Naldemedine
Naloxegol
Nelfinavir
Nicardipine
Nilotinib
Nintedanib
Nisoldipine
Norfloxacin
Octreotide
Ofloxacin
Olanzapine
Ondansetron
Osilodrostat
Osimertinib
Oxaliplatin
Oxycodone
Paliperidone
Panobinostat
Papaverine
Paritaprevir
Paroxetine
Pasireotide
Pazopanib
Pentamidine
Perphenazine
Pimavanserin
Pimozide
Pipamperone
Piperaquine
Pitolisant
Ponesimod
Posaconazole
Probucol
Procainamide
Prochlorperazine
Promethazine
Propafenone
Protriptyline
Quetiapine
Quinidine
Quinine
Ranolazine
Ribociclib
Rimegepant
Risperidone
Ritonavir
Rivaroxaban
Saquinavir
Selpercatinib
Sertindole
Sertraline
Sevoflurane
Sildenafil
Simvastatin
Siponimod
Sirolimus
Sodium Phosphate
Sodium Phosphate, Dibasic
Sodium Phosphate, Monobasic
Solifenacin
Sorafenib
Sotalol
Sparfloxacin
Sulpiride
Sultopride
Sunitinib
Tamoxifen
Telaprevir
Telavancin
Telithromycin
Temsirolimus
Terfenadine
Tetrabenazine
Thioridazine
Ticagrelor
Tilidine
Tipranavir
Tolterodine
Tolvaptan
Toremifene
Trazodone
Triazolam
Triclabendazole
Trimipramine
Triptorelin
Ubrogepant
Ulipristal
Vandetanib
Vardenafil
Velpatasvir
Vemurafenib
Venetoclax
Venlafaxine
Vilanterol
Vinflunine
Voclosporin
Voriconazole
Vorinostat
Voxilaprevir
Ziprasidone
Zotepine
Zuclopenthixol

Using this medicine with any of the following medicines is usually not recommended, but may be required in some cases. If both medicines are prescribed together, your doctor may change the dose or how often you use one or both of the medicines.

Abacavir
Acarbose
Acetazolamide
Adalimumab
Albendazole
Allopurinol
Alprazolam
Ambrisentan
Anidulafungin
Apalutamide
Atomoxetine
Atorvastatin
Atovaquone
Azacitidine
Balsalazide
Bexarotene
Bicalutamide
Boceprevir
Bortezomib
Bosentan
Busulfan
Captopril
Carbamazepine
Caspofungin
Cefadroxil
Cefdinir
Chenodiol
Chlorzoxazone
Cimetidine
Clofarabine
Clopidogrel
Cobicistat
Cyproheptadine
Dactinomycin
Danazol
Dantrolene
Deferasirox
Dexlansoprazole
Dexmethylphenidate
Diclofenac
Diflunisal
Disulfiram
Divalproex Sodium
Duloxetine
Ebrotidine
Enalapril
Enalaprilat
Entecavir
Enzalutamide
Epoprostenol
Erlotinib
Esomeprazole
Ethambutol
Etodolac
Etravirine
Febuxostat
Fenoprofen
Flutamide
Fosamprenavir
Fulvestrant
Ganciclovir
Gemcitabine
Gemtuzumab Ozogamicin
Glimepiride
Golimumab
Griseofulvin
Hydroxyurea
Idelalisib
Imatinib
Indomethacin
Infliximab
Interferon Beta-1a
Interferon Beta-1b
Isoniazid
Ixabepilone
Josamycin
Labetalol
Lamotrigine
Lansoprazole
Leflunomide
Levetiracetam
Lonafarnib
Lumacaftor
Mefenamic Acid
Memantine
Mercaptopurine
Mesalamine
Metformin
Methazolamide
Methimazole
Mibefradil
Micafungin
Milnacipran
Minocycline
Mitotane
Nevirapine
Niacin
Nilutamide
Nitisinone
Nitrofurantoin
Nizatidine
Nortriptyline
Olsalazine
Omeprazole
Orlistat
Oxandrolone
Pantoprazole
Peginterferon Alfa-2a
Phenytoin
Propylthiouracil
Rabeprazole
Raltegravir
Ramipril
Ranitidine
Ranitidine Bismuth Citrate
Ribavirin
Rifabutin
Rifampin
Rifapentine
Rifaximin
Riluzole
Roxatidine
St John's Wort
Sucralfate
Sulindac
Terbinafine
Testosterone
Tigecycline
Tizanidine
Tolcapone
Tramadol
Troleandomycin
Tucatinib
Valproic Acid
Vincristine
Zafirlukast
Zidovudine
Zolpidem

Other interactions—

Certain medicines should not be used at or around the time of eating food or eating certain types of food since interactions may occur. Using alcohol or tobacco with certain medicines may also cause interactions to occur. The following interactions have been selected on the basis of their potential significance and are not necessarily all-inclusive.

Using this medicine with any of the following is usually not recommended, but may be unavoidable in some cases. If used together, your doctor may change the dose or how often you use this medicine, or give you special instructions about the use of food, alcohol, or tobacco.

Ethanol

Other medical problems—

The presence of other medical problems may affect the use of this medicine. Make sure you tell your doctor if you have any other medical problems, especially:

Cholelithiasis (gallbladder stones), recurrent or
Heart rhythm problems (eg, long QT syndrome, torsades de pointes, ventricular fibrillation, ventricular tachycardia), history of or
Liver disease (eg, cirrhosis), active or poorly controlled or
Liver injury caused by medicines (eg, ketoconazole), history of—Should not be used in patients with these conditions.

Hypokalemia (low levels of potassium), history of or
Hypomagnesemia (low levels of magnesium), history of—Use with caution. May make these conditions worse.

Proper Use of This Medicine:

Take this medicine exactly as directed by your doctor. Do not take more of it, do not take it more often, and do not take it for a longer time than your doctor ordered. To do so may increase the chance for unwanted effects.

This medicine should come with a patient information leaflet. Read and follow these instructions carefully. Ask your doctor if you have any questions.

You may take this medicine with or without food.

Do not take carbamazepine, efavirenz, isoniazid, mifepristone, mitotane, nevirapine, phenytoin, rifabutin, rifampicin, ritonavir, ritonavir-boosted darunavir, and ritonavir-boosted fosamprenavir 2 weeks before and during treatment with levoketoconazole.

Take antacids (eg, aluminum hydroxide) at least 2 hours after you take this medicine.

Do not drink alcohol while you are using this medicine.

Dosing—

The dose of this medicine will be different for different patients. Follow your doctor's orders or the directions on the label. The following information includes only the average doses of this medicine. If your dose is different, do not change it unless your doctor tells you to do so.

The amount of medicine that you take depends on the strength of the medicine. Also, the number of doses you take each day, the time allowed between doses, and the length of time you take the medicine depend on the medical problem for which you are using the medicine.

For oral dosage form (tablets):
- For hypercortisolemia:
  - Adults—At first, 150 milligrams (mg) 2 times a day. Your doctor may adjust your dose as needed and tolerated. However, the dose is usually not more than 1200 mg per day (600 mg 2 times a day).
  - Children—Use and dose must be determined by your doctor.

Missed dose—

If you miss a dose of this medicine, skip the missed dose and go back to your regular dosing schedule. Do not double doses.

Storage—

Store the medicine in a closed container at room temperature, away from heat, moisture, and direct light. Keep from freezing.

Keep out of the reach of children.

Do not keep outdated medicine or medicine no longer needed.

Ask your healthcare professional how you should dispose of any medicine you do not use.

Precautions While Using This Medicine:

It is very important that your doctor check your progress at regular visits to make sure that this medicine is working properly. Blood and urine tests may be needed to check for unwanted effects.

Using this medicine while you are pregnant can harm your unborn baby. Use an effective form of birth control to keep from getting pregnant during treatment with this medicine. If you think you have become pregnant while using this medicine, tell your doctor right away.

You should not use this medicine together with alfentanil (Alfenta®), avanafil (Stendra®), bosutinib (Bosulif®), buspirone (Buspar®), cisapride (Prepulsid®), clarithromycin (Biaxin®), cobimetinib (Cotellic™), conivaptan (Vaprisol®), crizotinib (Xalkori®), dabigatran (Pradaxa®), darifenacin (Enablex®), darunavir (Prezista®), digoxin (Lanoxin®), disopyramide (Norpace®), dofetilide (Tikosyn®), dronedarone (Multaq®), ebastine (Ebast®), eliglustat (Cerdelga®), everolimus (Afinitor®), fexofenadine (Allegra®), ibrutinib (Imburvica™), ivabradine (Corlanor®), lomitapide (Juxtapid®), lovastatin (Mevacor®), lurasidone (Latuda®), methadone (Methadose®), midazolam (Versed®), midostaurin (Rydapt®), naloxegol (Alfenta®), nicardipine (Cardene®), nisoldipine (Alfenta®), pimozide (Alfenta®), quinidine (Alfenta®), ranolazine (Movantik®), saquinavir (Invirase®), simvastatin (Zocor®), sirolimus (Rapamune®), tacrolimus (Astagraf XL®), tipranavir (Aptivus®), triazolam (Halcion®), or vardenafil (Levitra®).

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

This medicine may cause heart rhythm problems (eg, QT prolongation). Check with your doctor right away if you have chest pain or discomfort, fainting, irregular or slow heart rate, or trouble breathing.

Check with your doctor right away if you have darkening of the skin, diarrhea, dizziness, fainting, loss of appetite, mental depression, nausea, skin rash, unusual tiredness or weakness, or vomiting. These may be symptoms of adrenal gland problems (eg, low cortisol levels).

This medicine may cause serious allergic reactions, which can be life-threatening and require immediate medical attention. Check with your doctor right away if you have chest tightness, cough, difficulty swallowing, dizziness, fast heartbeat, hives, itching, skin rash, puffiness or swelling of the eyelids or around the eyes, face, lips, or tongue, or unusual tiredness or weakness.

This medicine may decrease testosterone levels in men and women. Check with your doctor right away if you have decreased interest in sexual intercourse, inability to have or keep an erection, loss in sexual ability, desire, drive, or performance, mood changes swelling of the breasts or breast soreness.

Some men and women who use this medicine have become infertile (unable to have children). Talk with your doctor before using this medicine if you plan to have children.

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.

Side Effects of This Medicine:

Along with its needed effects, a medicine may cause some unwanted effects. Although not all of these side effects may occur, if they do occur they may need medical attention.

Check with your doctor immediately if any of the following side effects occur:

More common: Bleeding gums; bloating or swelling of the face, arms, hands, lower legs, or feet; blurred vision; body aches or pain; chills; cough; coughing up blood; darkening of the skin; decreased interest in sexual intercourse; decreased urine; diarrhea; difficulty in swallowing; dizziness; dry mouth; ear congestion; fainting; fever; headache; inability to have or keep an erection; increased menstrual flow or vaginal bleeding; increased thirst; loss in sexual ability, desire, drive, or performance; loss of appetite; loss of voice; mental depression; mood changes; muscle pain or cramps; nausea or vomiting; nervousness; nosebleeds; numbness or tingling in the hands, feet, or lips; paralysis; prolonged bleeding from cuts; pounding in the ears; rapid weight gain; red or black, tarry stools; red or dark brown urine; seizures; slow or fast heartbeat; sneezing; sore throat; stuffy or runny nose; trouble breathing; unusual tiredness or weakness; unusual weight gain or loss

Less common: Swelling of the breasts or breast soreness in both females and males

Incidence not known: Bulging soft spot on head of an infant; change in ability to see colors, especially blue or yellow; chest tightness; dark urine; large, hive-like swelling on the face, eyelids, lips, tongue, throat, hands, legs, feet, or sex organs; pinpoint red spots on skin; puffiness or swelling of the eyelids or around the eyes, face, lips, or tongue; stomach pain, severe; trouble sleeping; unusual bleeding or bruising; yellow eyes or skin

Some side effects may occur that usually do not need medical attention. These side effects may go away during treatment as your body adjusts to the medicine. Also, your health care professional may be able to tell you about ways to prevent or reduce some of these side effects. Check with your health care professional if any of the following side effects continue or are bothersome or if you have any questions about them:

More common: Acid or sour stomach; back pain; belching; difficulty in moving; heartburn; indigestion; loss or thinning of the hair; muscle aches or stiffness; pain, swelling, or redness in the joints; stomach discomfort or upset

Incidence not known: Increased sensitivity of the skin to sunlight; redness or other discoloration of the skin; severe sunburn

Other side effects not listed may also occur in some patients. If you notice any other effects, check with your healthcare professional.

Call your doctor for medical advice about side effects. You may report side effects to the FDA at 1-800-FDA-1088.

Last Updated: 4/24/2024

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