DDInter154 DDInter1329
Azelastine is a phthalazine compound having an oxo substituent at the 1-position, a 1-methylazepan-4-yl group at the 2-position and a 4-chlorobenzyl substituent at the 4-position. It has a role as a H1-receptor antagonist, an anti-allergic agent, an anti-asthmatic drug, a bronchodilator agent, a platelet aggregation inhibitor and an EC 1.13.11.34 (arachidonate 5-lipoxygenase) inhibitor. It is a member of phthalazines, a tertiary amino compound and a member of monochlorobenzenes.
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™.
Azelastine {u} (Compound) resembles {v} (Compound) Clemastine
Clemastine {u} may cause a moderate interaction that could exacerbate diseases when taken with {v} Oliceridine
Azelastine {u} (Compound) resembles {v} (Compound) Loxapine
Loxapine {u} may cause a moderate interaction that could exacerbate diseases when taken with {v} Clidinium
Clidinium {u} may cause a moderate interaction that could exacerbate diseases when taken with {v} Oliceridine
Azelastine {u} (Compound) resembles {v} (Compound) Prazepam
Prazepam {u} (Compound) resembles {v} (Compound) Methdilazine
Methdilazine {u} may cause a moderate interaction that could exacerbate diseases when taken with {v} Oliceridine
Azelastine {u} (Compound) resembles {v} (Compound) Meclizine
Meclizine {u} (Compound) resembles {v} (Compound) Cetirizine
Cetirizine {u} may cause a moderate interaction that could exacerbate diseases when taken with {v} Oliceridine
Azelastine {u} (Compound) resembles {v} (Compound) Buclizine
Buclizine {u} (Compound) resembles {v} (Compound) Imatinib
Imatinib {u} may lead to a major life threatening interaction when taken with {v} Oliceridine
Azelastine {u} (Compound) resembles {v} (Compound) Clozapine
Clozapine {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
Azelastine {u} (Compound) binds {v} (Gene) CYP1A2
CYP1A2 {u} (Gene) is bound by {v} (Compound) Daunorubicin
Daunorubicin {u} may cause a moderate interaction that could exacerbate diseases when taken with {v} Oliceridine
Azelastine {u} (Compound) resembles {v} (Compound) Clozapine
Clozapine {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
Azelastine {u} (Compound) binds {v} (Gene) CYP2C19
CYP2C19 {u} (Gene) is bound by {v} (Compound) Dexamethasone
Dexamethasone {u} may lead to a major life threatening interaction when taken with {v} Oliceridine
Azelastine {u} (Compound) resembles {v} (Compound) Clozapine
Clozapine {u} may lead to a major life threatening interaction when taken with {v} Abarelix
Abarelix {u} may cause a moderate interaction that could exacerbate diseases when taken with {v} Oliceridine
Azelastine (Compound) resembles Clemastine (Compound) and Clemastine may cause a moderate interaction that could exacerbate diseases when taken with Oliceridine
Azelastine (Compound) resembles Loxapine (Compound) and Loxapine may cause a moderate interaction that could exacerbate diseases when taken with Clidinium and Clidinium may cause a moderate interaction that could exacerbate diseases when taken with Oliceridine
Azelastine (Compound) resembles Prazepam (Compound) and Prazepam (Compound) resembles Methdilazine (Compound) and Methdilazine may cause a moderate interaction that could exacerbate diseases when taken with Oliceridine
Azelastine (Compound) resembles Meclizine (Compound) and Meclizine (Compound) resembles Cetirizine (Compound) and Cetirizine may cause a moderate interaction that could exacerbate diseases when taken with Oliceridine
Azelastine (Compound) resembles Buclizine (Compound) and Buclizine (Compound) resembles Imatinib (Compound) and Imatinib may lead to a major life threatening interaction when taken with Oliceridine
Azelastine (Compound) resembles Clozapine (Compound) and Clozapine 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
Azelastine (Compound) binds CYP1A2 (Gene) and CYP1A2 (Gene) is bound by Daunorubicin (Compound) and Daunorubicin may cause a moderate interaction that could exacerbate diseases when taken with Oliceridine
Azelastine (Compound) resembles Clozapine (Compound) and Clozapine 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
Azelastine (Compound) binds CYP2C19 (Gene) and CYP2C19 (Gene) is bound by Dexamethasone (Compound) and Dexamethasone may lead to a major life threatening interaction when taken with Oliceridine
Azelastine (Compound) resembles Clozapine (Compound) and Clozapine may lead to a major life threatening interaction when taken with Abarelix and Abarelix may cause a moderate interaction that could exacerbate diseases when taken with Oliceridine