DDInter1088 DDInter1008
Loperamide is an anti-diarrheal agent that is available as various over-the-counter products for treating diarrhea. The drug was first synthesized in 1969 and used medically in 1976. It is a highly lipophilic synthetic phenylpiperidine opioid that is structurally similar to opiate receptor agonists such as [diphenoxylate] and [haloperidol]. Due to pharmacological properties, loperamide has been misused and abused to self-manage opioid withdrawal symptoms and to induce euphoria.[A251610, A251625] However, loperamide is associated with a risk for experiencing a range of adverse effects, often life-threatening, if taking for non-therapeutic reasons or at doses higher than the recommended dose.
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.
Loperamide {u} may lead to a major life threatening interaction when taken with {v} Posaconazole
Posaconazole {u} (Compound) resembles {v} (Compound) Ketoconazole
Loperamide {u} (Compound) binds {v} (Gene) CYP3A4
CYP3A4 {u} (Gene) is bound by {v} (Compound) Ketoconazole
Loperamide {u} (Compound) upregulates {v} (Gene) FDFT1
FDFT1 {u} (Gene) is upregulated by {v} (Compound) Ketoconazole
Loperamide {u} (Compound) causes {v} (Side Effect) Hypersensitivity
Hypersensitivity {u} (Side Effect) is caused by {v} (Compound) Ketoconazole
Loperamide {u} (Compound) upregulates {v} (Gene) CYP51A1
CYP51A1 {u} (Gene) is bound by {v} (Compound) and {u} (Gene) is upregulated by {v} (Compound) Ketoconazole
Loperamide {u} may lead to a major life threatening interaction when taken with {v} Posaconazole
Posaconazole {u} (Compound) resembles {v} (Compound) Itraconazole
Itraconazole {u} (Compound) resembles {v} (Compound) Ketoconazole
Loperamide {u} (Compound) binds {v} (Gene) CYP3A4
CYP3A4 {u} (Gene) is bound by {v} (Compound) Itraconazole
Itraconazole {u} (Compound) resembles {v} (Compound) Ketoconazole
Loperamide {u} (Compound) upregulates {v} (Gene) FDFT1
FDFT1 {u} (Gene) regulates {v} (Gene) SLC2A6
SLC2A6 {u} (Gene) is upregulated by {v} (Compound) Ketoconazole
Loperamide {u} (Compound) upregulates {v} (Gene) SLC2A6
SLC2A6 {u} (Gene) is regulated by {v} (Gene) FDFT1
FDFT1 {u} (Gene) is upregulated by {v} (Compound) Ketoconazole
Loperamide {u} (Compound) upregulates {v} (Gene) INSIG1
INSIG1 {u} (Gene) is upregulated by {v} (Compound) Itraconazole
Itraconazole {u} (Compound) resembles {v} (Compound) Ketoconazole
Loperamide may lead to a major life threatening interaction when taken with Posaconazole and Posaconazole (Compound) resembles Ketoconazole (Compound)
Loperamide (Compound) binds CYP3A4 (Gene) and CYP3A4 (Gene) is bound by Ketoconazole (Compound)
Loperamide (Compound) upregulates FDFT1 (Gene) and FDFT1 (Gene) is upregulated by Ketoconazole (Compound)
Loperamide (Compound) causes Hypersensitivity (Side Effect) and Hypersensitivity (Side Effect) is caused by Ketoconazole (Compound)
Loperamide (Compound) upregulates CYP51A1 (Gene) and CYP51A1 (Gene) is bound by Ketoconazole (Compound) and CYP51A1 (Gene) is upregulated by Ketoconazole (Compound)
Loperamide may lead to a major life threatening interaction when taken with Posaconazole and Posaconazole (Compound) resembles Itraconazole (Compound) and Itraconazole (Compound) resembles Ketoconazole (Compound)
Loperamide (Compound) binds CYP3A4 (Gene) and CYP3A4 (Gene) is bound by Itraconazole (Compound) and Itraconazole (Compound) resembles Ketoconazole (Compound)
Loperamide (Compound) upregulates FDFT1 (Gene) and FDFT1 (Gene) regulates SLC2A6 (Gene) and SLC2A6 (Gene) is upregulated by Ketoconazole (Compound)
Loperamide (Compound) upregulates SLC2A6 (Gene) and SLC2A6 (Gene) is regulated by FDFT1 (Gene) and FDFT1 (Gene) is upregulated by Ketoconazole (Compound)
Loperamide (Compound) upregulates INSIG1 (Gene) and INSIG1 (Gene) is upregulated by Itraconazole (Compound) and Itraconazole (Compound) resembles Ketoconazole (Compound)