DDInter1166 DDInter1008
Methadone is a potent synthetic analgesic that works as a full µ-opioid receptor (MOR) agonist and N-methyl-d-aspartate (NMDA) receptor antagonist. As a full MOR agonist, methadone mimics the natural effects of the body's opioids, endorphins, and enkephalins through the release of neurotransmitters involved in pain transmission. It also has a number of unique characteristics that have led to its increased use in the last two decades; in particular, methadone has a lower risk of neuropsychiatric toxicity compared to other opioids (due to a lack of active metabolites), minimal accumulation in renal failure, good bioavailability, low cost, and a long duration of action.[F4685,F4688,F4691,A185885,A185900,A185903] Due to its unique mechanism of action, methadone is particularly useful for the management of hard to treat pain syndromes
Ketoconazole is an imidazole antifungal agent used in the prevention and treatment of a variety of fungal infections.[FDA Label] It functions by preventing the synthesis of ergosterol, the fungal equivalent of cholesterol, thereby increasing membrane fluidity and preventing growth of the fungus.[A181802,T116] Ketoconazole was first approved in an oral formulation for systemic use by the FDA in 1981. At this time it was considered a significant improvement over previous antifungals, [miconazole] and [clotrimazole], due to its broad spectrum and good absorption. However, it was discovered that ketoconazole produces frequent gastrointestinal side effects and dose-related hepatitis.[A188054,A188057] These effects combined with waning efficacy led to its eventual replacement by triazole agents, [fluconazole], [itraconazole], [voriconazole], and [posaconazole]. Ketoconazole and its predecessor [clotrimazole] continue to be used in topical formulations.
Methadone {u} (Compound) binds {v} (Gene) CYP3A4
CYP3A4 {u} (Gene) is bound by {v} (Compound) Ketoconazole
Methadone {u} (Compound) causes {v} (Side Effect) Hypersensitivity
Hypersensitivity {u} (Side Effect) is caused by {v} (Compound) Ketoconazole
Methadone {u} (Compound) binds {v} (Gene) CYP3A4
CYP3A4 {u} (Gene) is bound by {v} (Compound) Itraconazole
Itraconazole {u} (Compound) resembles {v} (Compound) Ketoconazole
Methadone {u} (Compound) causes {v} (Side Effect) Hypersensitivity
Hypersensitivity {u} (Side Effect) is caused by {v} (Compound) Itraconazole
Itraconazole {u} (Compound) resembles {v} (Compound) Ketoconazole
Methadone {u} (Compound) causes {v} (Side Effect) Electrocardiogram QT prolonged
Electrocardiogram QT prolonged {u} (Side Effect) is caused by {v} (Compound) Posaconazole
Posaconazole {u} (Compound) resembles {v} (Compound) Ketoconazole
Methadone {u} (Compound) binds {v} (Gene) ABCB1
ABCB1 {u} (Gene) is bound by {v} (Compound) Posaconazole
Posaconazole {u} (Compound) resembles {v} (Compound) Ketoconazole
Methadone {u} (Compound) binds {v} (Gene) ABCB1
ABCB1 {u} (Gene) regulates {v} (Gene) ALDOC
ALDOC {u} (Gene) is upregulated by {v} (Compound) Ketoconazole
Methadone {u} may cause a moderate interaction that could exacerbate diseases when taken with {v} Miconazole
Miconazole {u} (Compound) resembles {v} (Compound) Econazole
Econazole {u} (Compound) resembles {v} (Compound) Ketoconazole
Methadone {u} may cause a moderate interaction that could exacerbate diseases when taken with {v} Miconazole
Miconazole {u} (Compound) binds {v} (Gene) CYP3A4
CYP3A4 {u} (Gene) is bound by {v} (Compound) Ketoconazole
Methadone {u} may cause a moderate interaction that could exacerbate diseases when taken with {v} Miconazole
Miconazole {u} (Compound) is included by {v} (Pharmacologic Class) Azoles
Azoles {u} (Pharmacologic Class) includes {v} (Compound) Ketoconazole
Methadone (Compound) binds CYP3A4 (Gene) and CYP3A4 (Gene) is bound by Ketoconazole (Compound)
Methadone (Compound) causes Hypersensitivity (Side Effect) and Hypersensitivity (Side Effect) is caused by Ketoconazole (Compound)
Methadone (Compound) binds CYP3A4 (Gene) and CYP3A4 (Gene) is bound by Itraconazole (Compound) and Itraconazole (Compound) resembles Ketoconazole (Compound)
Methadone (Compound) causes Hypersensitivity (Side Effect) and Hypersensitivity (Side Effect) is caused by Itraconazole (Compound) and Itraconazole (Compound) resembles Ketoconazole (Compound)
Methadone (Compound) causes Electrocardiogram QT prolonged (Side Effect) and Electrocardiogram QT prolonged (Side Effect) is caused by Posaconazole (Compound) and Posaconazole (Compound) resembles Ketoconazole (Compound)
Methadone (Compound) binds ABCB1 (Gene) and ABCB1 (Gene) is bound by Posaconazole (Compound) and Posaconazole (Compound) resembles Ketoconazole (Compound)
Methadone (Compound) binds ABCB1 (Gene) and ABCB1 (Gene) regulates ALDOC (Gene) and ALDOC (Gene) is upregulated by Ketoconazole (Compound)
Methadone may cause a moderate interaction that could exacerbate diseases when taken with Miconazole and Miconazole (Compound) resembles Econazole (Compound) and Econazole (Compound) resembles Ketoconazole (Compound)
Methadone may cause a moderate interaction that could exacerbate diseases when taken with Miconazole and Miconazole (Compound) binds CYP3A4 (Gene) and CYP3A4 (Gene) is bound by Ketoconazole (Compound)
Methadone may cause a moderate interaction that could exacerbate diseases when taken with Miconazole and Miconazole (Compound) is included by Azoles (Pharmacologic Class) and Azoles (Pharmacologic Class) includes Ketoconazole (Compound)