- March 15, 2022
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Brand Name :
Recorlev
Synonyms :
levoketoconazole
Class :
Cortisol synthesis Inhibitors
Dosage forms and strengths
tablet
(150mg)
Initial dose: orally 150 mg 2 times daily
Maintenance dose: Titrate the daily dosage by 150 mg, at regular intervals of no more then 2-3 weeks taking into the 24-hour urine free levels of cortisol and the patient's tolerance, until a satisfactory response is attained
Maximum dose: daily dosage is 1200 mg, divided into two equal doses of 600 mg each, Administered two times daily
Safety and efficacy are not established
Refer adult dosing
levoketoconazole: they may diminish the absorption of antacids
levoketoconazole: they may diminish the absorption of antacids
levoketoconazole: they may diminish the absorption of antacids
levoketoconazole: they may diminish the absorption of antacids
levoketoconazole: they may diminish the absorption of antacids
Sucralfate may diminish the serum concentration of levoketoconazole
it may decrease the absorption of Levoketoconazole
it may decrease the absorption of Levoketoconazole
it may decrease the absorption of Levoketoconazole
it may decrease the absorption of Levoketoconazole
it may decrease the absorption of Levoketoconazole
may have an increased QTc-prolonging effect when combined with levoketoconazole
may have an increased QTc-prolonging effect when combined with levoketoconazole
may have an increased QTc-prolonging effect when combined with levoketoconazole
may have an increased QTc-prolonging effect when combined with levoketoconazole
may have an increased QTc-prolonging effect when combined with levoketoconazole
may have an increased QTc-prolonging effect when combined with levoketoconazole
may have an increased QTc-prolonging effect when combined with levoketoconazole
may have an increased QTc-prolonging effect when combined with levoketoconazole
It may enhance the effect when combined with dyphylline by CYP3A4 metabolism
may have an increased QTc-prolonging effect when combined with levoketoconazole
may have an increased QTc-prolonging effect when combined with levoketoconazole
levoketoconazole: they may increase the QTc-prolonging effect of QTc-prolonging Agents
levoketoconazole: they may increase the QTc-prolonging effect of QTc-prolonging Agents
levoketoconazole: they may increase the QTc-prolonging effect of QTc-prolonging Agents
levoketoconazole: they may increase the QTc-prolonging effect of QTc-prolonging Agents
when both drugs are combined, there may be a decreased metabolism of vinblastine
when both drugs are combined, there may be a decreased metabolism of alpelisib
when both drugs are combined, there may be a reduced metabolism of abemaciclib
when both drugs are combined, there may be a reduced metabolism of erlotinib
the effect of levoketoconazole is increased by lorlatinib, by altering intestinal or hepatic CYP3A4 enzyme metabolism
levoketoconazole increases the effect of lapatinib by altering the intestinal or hepatic CYP3A4 enzyme metabolism
CYP3A strong enhancers of the small intestine may reduce the bioavailability of levoketoconazole
it will increase the impact or level of regorafenib by altering the intestinal or hepatic CYP3A4 enzyme metabolism
it increases the effect or level of ruxolitinib by altering the intestinal or hepatic CYP3A4 enzyme metabolism
it increases the QTc-prolongation effect of sunitinib
QT-prolonging CYP3A4 substrates increase the QTc prolonging effect of ketoconazole
QT-prolongers increase the QTc prolongation of levoketoconazole
may increase the QTc-prolonging effect of QT-prolonging Agents
it may enhance the QTc-prolonging effect of levoketoconazole
it may enhance the QTc-prolonging effect of levoketoconazole
it may enhance the QTc-prolonging effect of levoketoconazole
it may enhance the QTc-prolonging effect of levoketoconazole
it may enhance the QTc-prolonging effect of levoketoconazole
QTc-prolongers increase the effect of levoketoconazole
QTc-prolongers increase the effect of levoketoconazole
QTc-prolongers increase the effect of levoketoconazole
QTc-prolongers increase the effect of levoketoconazole
QTc-prolongers increase the effect of levoketoconazole
It may enhance the effect when combined with oxiconazole by affecting CYP3A4 metabolism
levoketoconazole: they may diminish the absorption of antacids
increase the therapeutic effects of busulfan by inhibiting metabolism
when both drugs are combined, there may be a decreased metabolism of paclitaxel
has a synergistic effect over brentuximab vedotin by showing altered intestinal/hepatic CYP3A4 enzyme metabolism.
increase the therapeutic effect of daunorubicin by P-glycoprotein efflux transporter
increase serum levels by increasing p-glycoprotein efflux transporter
increase serum levels by increasing p-glycoprotein efflux transporter
increase the therapeutic effect of idarubicin by P-glycoprotein efflux transporter
QT-prolongers increase the QTc extending effect of levoketoconazole
cyclophosphamide effect of action increased by affecting enzyme CYP3A4 metabolism.
it increases the effect or level of osimertinib by altering the intestinal or hepatic CYP3A4 enzyme metabolism
it increases the efficacy of sorafenib by altering the hepatic CYP3A4 enzyme metabolism
it increases by affecting the hepatic enzyme CYP3A4 metabolism
Actions and Spectrum
Action: The drug involves the suppression of ergosterol synthesis .an essential component of fungal cell membranes. Ergosterol is responsible for maintaining the integrity and function of fungal cells. The drug disrupts the fungal cell membrane by inhibiting its synthesis, leading to cell death and ultimately eliminating the fungal infection.
Spectrum: drug has a broad spectrum of activity against various fungal pathogens. It is effective against both yeasts and molds. It can cure infections by Candida species (such as oral and vaginal thrush) and dermatophytes (which cause skin, hair, and nail infections like athlete’s foot and ringworm). drug is also effective against certain endemic fungi, such as Histoplasma and Blastomyces species, which cause systemic fungal infections.
Frequency defined
>10%
Abnormal uterine bleeding (20-24%)
Abdominal pain/dyspepsia (15-33%)
Upper respiratory infection (18-28%)
Hemorrhage/contusion (23-40%)
Nausea/vomiting (30-37%)
Headache (21-38%)
Myalgia (26%)
Hypokalemia (15-29%)
Arthritis (28%)
Fatigue (18-39%)
Hypertension (20-24%)
Erythema (43%)
Hepatoxicity
≥1 liver related adverse reaction (27%)
AST/ALT >ULN (45%)
AST/ALT >3x ULN (11%)
Liver enzyme elevation (20%)
1-10%
Hypersensitivity (1%)
Hypogonadism (2-4%)
Decreased libido (5%)
Hypocortisolism (7%)
Gastrointestinal infection (5-6%)
QTcF >500 msec (2.4%)
Gynecomastia (3%)
Adrenal insufficiency (3-10%)
Hepatoxicity
Hepatic steatosis (1%)
Drug-induced liver injury (2%)
AST/ALT >10x ULN (3%)
AST/ALT >5x ULN (5%)
Liver disorders (2%)
Hepatic pain (4%)
Black Box Warning:
None
Contraindication/Caution:
Hypersensitivity: Individuals who have a confirmed hypersensitivity or allergic reaction to the medication or any of its constituents should avoid using the drug.
Liver Disease: The liver metabolizes the drug, so caution is advised in individuals with severe liver impairment. In such cases, it may require dose adjustments or close monitoring of liver function.
Certain Medications: drug can interact with other medications, potentially leading to adverse effects or reduced efficacy.
QT Prolongation: drug may prolong the QT interval on an electrocardiogram (ECG), which can increase the risk of serious cardiac arrhythmias.
Pregnancy and Breastfeeding: The safety of drug during pregnancy and breastfeeding has not been established. It should be avoided unless the potential benefits outweigh the potential risks. Ask a healthcare advisor if you are pregnant, planning to become pregnant, or breastfeeding.
Pediatric Use: The safety and efficacy of levoketoconazole is not established in children and adolescents. A pediatric specialist should carefully evaluate its use in this population.
Pregnancy warnings:
Pregnancy category: N/A
Lactation: Excreted into human milk is known (ketoconazole)
Pregnancy Categories:
Category A: Studies that were well-controlled and met expectations revealed no risk to the fetus in either the first or second trimester.
Category B: There were a lack of studies on pregnant women and no evidence of risk to the fetus in animal experiments.
Category C: there was evidence of risk of adverse effects in animal reproduction studies, and no adequate evidence in human studies must take care of potential risks in pregnant women.
Category D: adequate data with sufficient evidence of human fetal risk from various platforms, but despite the potential risk, and used only in emergency cases for potential benefits.
Category X: Drugs listed in this category outweigh the risks over benefits. Hence these categories of drugs need to be avoided by pregnant women.
Category N: There is no data available for the drug under this category
Pharmacology:
Drug is an antifungal medication that belongs to azole antifungals drug class; levoketoconazole, specifically the (S)-enantiomer of ketoconazole.
Pharmacodynamics:
The pharmacodynamics of drug involve its interactions with fungal enzymes called cytochrome P450 (CYP) enzymes. The drug effectively hinders the function of certain enzymes, including CYP3A4, that play a crucial role in producing ergosterol—a vital element found in fungal cell membranes. Through the inhibition of ergosterol synthesis, this medication causes a disturbance in the integrity and functionality of the fungal cell membrane, ultimately resulting in the demise of the fungal organism.
Pharmacokinetics:
Absorption
drug is administered orally, and its absorption occurs primarily in the gastrointestinal tract certain factors include food or other medications, may affect drug absorption.
Distribution
drug distribution occurs in the whole body, via the bloodstream. It can bind to plasma proteins, including albumin. The drug has the potential to penetrate various tissues, including the skin, nails, and organs.
Metabolism
drug undergoes extensive metabolism in the liver through several metabolic pathways, including oxidation and glucuronidation. The enzymes involved in its metabolism are cytochrome P450 (CYP) enzymes, particularly CYP3A4.
Excretion and Elimination
The metabolites of drug and a small amount of unchanged drug are excreted primarily in the feces and, to a lesser extent, in the urine. The elimination half-life of drug can vary, but it is generally within several hours.
Administration:
Administration of the medication can be done with or without food.
Patient information leaflet
Generic Name: levoketoconazole
Why do we use levoketoconazole?
Cushing’s syndrome: drug is approved for the treatment of endogenous Cushing’s syndrome, a hormonal disorder characterized by excessive cortisol levels in the body. It works by inhibiting the enzymes in cortisol synthesis, thus reducing cortisol production.
Fungal infections: levoketoconazole, like its parent compound ketoconazole, is effective against various fungal infections. It can treat conditions such as candidiasis (yeast infections), dermatophytosis (ringworm), and certain systemic fungal infections.
Off-label uses: The drug is also being investigated for potential use in other conditions. Some studies have explored its role in treating prostate cancer, as cortisol can stimulate the growth of prostate cancer cells. Additionally, drug may have applications in other hormone-related disorders, such as congenital adrenal hyperplasia and primary aldosteronism.
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