Levoketoconazole Side Effects

Medically reviewed by Drugs.com. Last updated on Feb 4, 2025.

Applies to levoketoconazole: oral tablet.

Precautions

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.

Serious side effects of levoketoconazole

Along with its needed effects, levoketoconazole 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 while taking levoketoconazole:

Other side effects of levoketoconazole

Some side effects of levoketoconazole 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:

For healthcare professionals

Applies to levoketoconazole: oral tablet.

General adverse events

The most significant adverse reactions were hepatotoxicity, QT prolongation, and hypocortisolism.^[Ref]

Hepatic

Percentage of patients with elevations in AST or ALT:

AST or ALT greater than the upper limit of normal (ULN): 45%

AST or ALT greater than 3 times ULN (3 x ULN): 11%

AST or ALT greater than 5 x ULN: 5%

AST or ALT greater than 10 x ULN: 3%^[Ref]

• Very common (10% or more): Liver enzyme elevation (included elevated AST, elevated ALT, elevated alkaline phosphatase, elevated GGT; 20%)
• Common (1% to 10%): Hepatic pain, drug-induced liver injury, liver disorders
• Uncommon (0.1% to 1%): Hepatic steatosis

Ketoconazole:

• Postmarketing reports: Serious hepatotoxicity including hepatitis cholestatic, biopsy-confirmed hepatic necrosis, cirrhosis, hepatic failure including cases resulting in transplantation or death^[Ref]

Level 2

Up to 27% of the patients had at least 1 liver-related adverse reaction.

Cardiovascular

• Very common (10% or more): Hypertension (up to 24%), arrythmia (included ECG QT prolonged, ECG T wave abnormal, palpitations, sinus tachycardia, paroxysmal tachycardia, ventricular extrasystoles, bradycardia, carotid pulse increased, defect conduction intraventricular, heart rate increased, sinus bradycardia; up to 24%)
• Frequency not reported: QTc interval prolongation^[Ref]

Level 2

In general, 2.4% of the patients experienced QTcF greater than 500 msec, while 14.7% of patients experienced change-from-baseline QTcF greater than 60 msec.^[Ref]

Endocrine

• Very common (10% or more): Adrenal insufficiency (10%)
• Common (1% to 10%): Hypocortisolism, gynecomastia, hypogonadism

Ketoconazole:

• Postmarketing reports: Adrenocortical insufficiency^[Ref]

Dermatologic

• Very common (10% or more): Erythema (included flushing; 43%), rash (17%), pruritus (15%), dry skin (up to 12%), alopecia (up to 11%)

Ketoconazole:

• Postmarketing reports: Acute generalized exanthematous pustulosis, photosensitivity^[Ref]

Other

• Very common (10% or more): Fatigue (up to 39%), peripheral edema (20%)^[Ref]

Nervous system

• Very common (10% or more): Headache (up to 38%), presyncope/syncope (18%) dizziness (15%), disturbance in attention (14%)

Ketoconazole:

• Postmarketing reports: Reversible intracranial pressure increased (e.g., papilledema, fontanelle bulging in infants)^[Ref]

Gastrointestinal

• Very common (10% or more): Nausea/vomiting (up to 37%), abdominal pain/dyspepsia (included abdominal pain, abdominal distension, dyspepsia, gastric disorder, abdominal discomfort, gastritis, other related terms; up to 33%), diarrhea (up to 19%), dry mouth (11%)
• Common (1% to 10%): Gastrointestinal infection^[Ref]

Metabolic

• Very common (10% or more): Hypokalemia (up to 29%), decreased appetite (13%)^[Ref]

Musculoskeletal

• Very common (10% or more): Arthritis (28%), myalgia (26%), back pain (22%)^[Ref]

Genitourinary

• Very common (10% or more): Abnormal uterine bleeding (up to 24%), urinary tract infection (up to 16%)

Ketoconazole:

• Postmarketing reports: Erectile dysfunction, azoospermia^[Ref]

Level 2

Azoospermia was reported with dosages higher than 200 or 400 mg daily.^[Ref]

Psychiatric

• Very common (10% or more): Insomnia/sleep disturbances (22%), irritability (14%), depression (12%)
• Common (1% to 10%): Decreased libido^[Ref]

Respiratory

• Very common (10% or more): Upper respiratory infection (up to 28%)

Hypersensitivity

• Uncommon (0.1% to 1%): Hypersensitivity

Ketoconazole:

• Postmarketing reports: Allergic conditions including anaphylactic shock, anaphylactic reaction, angioneurotic edema^[Ref]

Hematologic

• Very common (10% or more): Hemorrhage/contusion (included blood urine present, epistaxis, eye hemorrhage, gingival bleeding, hematoma, hematuria, hemorrhoidal hemorrhage, melena, scleral hemorrhage, conjunctival hemorrhage, ecchymosis, hyphema, RBCs urine; up to 40%),

Ketoconazole:

• Postmarketing reports: Thrombocytopenia^[Ref]

See also:

Further information

Levoketoconazole side effects can vary depending on the individual. Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.

Note: Medication side effects may be underreported. If you are experiencing side effects that are not listed, submit a report to the FDA by following this guide.

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