DDInter1008 DDInter1329
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
Severe acute pain occurs through nociceptive signalling involving both ascending and descending spinal pathways, in which nerve conductance is mediated in part by the action of opioid receptors.[A218041, A218046] Opioid receptors are seven-transmembrane G-protein-coupled receptors (GPCRs), of which the μ-opioid receptor subtype is predominantly targeted by and is responsible for the effects of opioid agonists.[A218031, A218046] However, due to the ability of some opioid agonists to bind to other targets, as well as activation of additional downstream pathways from opioid receptors such as those involving β-arrestin, the beneficial analgesic effects of opioids are coupled with severe adverse effects such as constipation and respiratory depression.[A218026, A218031, A218036, A218041, A218046] Oliceridine (formerly known as TRV130) is a "biased agonist" at the μ-opioid receptor by preferentially activating the G-protein pathway with minimal receptor phosphorylation and recruitment of β-arrestin.[A218026, A218031] By acting as a biased agonist, oliceridine provides comparable analgesia compared with traditional opioids such as [morphine] at a comparable or decreased risk of opioid-related adverse effects such as constipation and respiratory depression.[A218026, A218031, A218051, A218056, A218061, A218066, A218071, L15516] Oliceridine was first reported in 2013,[A218026, A218086] but was initially not approved by the FDA due to concerns raised by the Anesthetic and Analgesic Drug Products Advisory Committee. Oliceridine gained FDA approval on August 7, 2020, and is currently marketed by Trevena Inc as OLINVYK™.
Ketoconazole {u} (Compound) resembles {v} (Compound) Econazole
Econazole {u} (Compound) resembles {v} (Compound) Miconazole
Miconazole {u} may cause a moderate interaction that could exacerbate diseases when taken with {v} Oliceridine
Ketoconazole {u} (Compound) resembles {v} (Compound) Posaconazole
Posaconazole {u} may cause a minor interaction that can limit clinical effects when taken with {v} Metronidazole
Metronidazole {u} may cause a minor interaction that can limit clinical effects when taken with {v} Oliceridine
Ketoconazole {u} (Compound) binds {v} (Gene) CYP3A4
CYP3A4 {u} (Gene) is bound by {v} (Compound) Dextromethorphan
Dextromethorphan {u} may cause a moderate interaction that could exacerbate diseases when taken with {v} Oliceridine
Ketoconazole {u} (Compound) resembles {v} (Compound) Posaconazole
Posaconazole {u} may cause a moderate interaction that could exacerbate diseases when taken with {v} Promethazine
Promethazine {u} may cause a moderate interaction that could exacerbate diseases when taken with {v} Oliceridine
Ketoconazole {u} (Compound) binds {v} (Gene) CYP3A4
CYP3A4 {u} (Gene) is bound by {v} (Compound) Metronidazole
Metronidazole {u} may cause a minor interaction that can limit clinical effects when taken with {v} Oliceridine
Ketoconazole {u} (Compound) resembles {v} (Compound) Posaconazole
Posaconazole {u} may lead to a major life threatening interaction when taken with {v} Glasdegib
Glasdegib {u} may cause a moderate interaction that could exacerbate diseases when taken with {v} Oliceridine
Ketoconazole {u} (Compound) binds {v} (Gene) ABCB11
ABCB11 {u} (Gene) is bound by {v} (Compound) Dexamethasone
Dexamethasone {u} may lead to a major life threatening interaction when taken with {v} Oliceridine
Ketoconazole {u} (Compound) resembles {v} (Compound) Posaconazole
Posaconazole {u} may cause a moderate interaction that could exacerbate diseases when taken with {v} Eribulin
Eribulin {u} may cause a moderate interaction that could exacerbate diseases when taken with {v} Oliceridine
Ketoconazole {u} (Compound) binds {v} (Gene) CYP1A1
CYP1A1 {u} (Gene) is upregulated by {v} (Compound) Bisacodyl
Bisacodyl {u} may cause a moderate interaction that could exacerbate diseases when taken with {v} Oliceridine
Ketoconazole {u} (Compound) resembles {v} (Compound) Posaconazole
Posaconazole {u} may lead to a major life threatening interaction when taken with {v} Lapatinib
Lapatinib {u} may cause a moderate interaction that could exacerbate diseases when taken with {v} Oliceridine
Ketoconazole (Compound) resembles Econazole (Compound) and Econazole (Compound) resembles Miconazole (Compound) and Miconazole may cause a moderate interaction that could exacerbate diseases when taken with Oliceridine
Ketoconazole (Compound) resembles Posaconazole (Compound) and Posaconazole may cause a minor interaction that can limit clinical effects when taken with Metronidazole and Metronidazole may cause a minor interaction that can limit clinical effects when taken with Oliceridine
Ketoconazole (Compound) binds CYP3A4 (Gene) and CYP3A4 (Gene) is bound by Dextromethorphan (Compound) and Dextromethorphan may cause a moderate interaction that could exacerbate diseases when taken with Oliceridine
Ketoconazole (Compound) resembles Posaconazole (Compound) and Posaconazole may cause a moderate interaction that could exacerbate diseases when taken with Promethazine and Promethazine may cause a moderate interaction that could exacerbate diseases when taken with Oliceridine
Ketoconazole (Compound) binds CYP3A4 (Gene) and CYP3A4 (Gene) is bound by Metronidazole (Compound) and Metronidazole may cause a minor interaction that can limit clinical effects when taken with Oliceridine
Ketoconazole (Compound) resembles Posaconazole (Compound) and Posaconazole may lead to a major life threatening interaction when taken with Glasdegib and Glasdegib may cause a moderate interaction that could exacerbate diseases when taken with Oliceridine
Ketoconazole (Compound) binds ABCB11 (Gene) and ABCB11 (Gene) is bound by Dexamethasone (Compound) and Dexamethasone may lead to a major life threatening interaction when taken with Oliceridine
Ketoconazole (Compound) resembles Posaconazole (Compound) and Posaconazole may cause a moderate interaction that could exacerbate diseases when taken with Eribulin and Eribulin may cause a moderate interaction that could exacerbate diseases when taken with Oliceridine
Ketoconazole (Compound) binds CYP1A1 (Gene) and CYP1A1 (Gene) is upregulated by Bisacodyl (Compound) and Bisacodyl may cause a moderate interaction that could exacerbate diseases when taken with Oliceridine
Ketoconazole (Compound) resembles Posaconazole (Compound) and Posaconazole may lead to a major life threatening interaction when taken with Lapatinib and Lapatinib may cause a moderate interaction that could exacerbate diseases when taken with Oliceridine