DDInter915 DDInter1480
Indacaterol is a novel, ultra-long-acting, rapid onset β(2)-adrenoceptor agonist developed for Novartis for the once-daily management of asthma and chronic obstructive pulmonary disease. It was approved by the European Medicines Agency (EMA) on 30 November 2009 and by the FDA on 1 July 2011. It is marketed in Europe as Onbrez and in America as Arcapta Neohaler. Indacaterol is provided as its maleate salt form. Indacaterol is also a chiral molecule but only the pure R-enantiomer is dispensed.
Pitolisant is a selective antagonist or inverse agonist of the histamine H3 receptor used to treat type 1 or 2 narcolepsy. Narcolepsy is a chronic neurological disorder that affects 1 in 2,000 individuals and is characterized by excessive daytime sleepiness, abnormal REM sleep manifestations, sleep paralysis and hypnagogic hallucinations. About 60-70% of patients with narcolepsy experience cataplexy, which is a sudden loss of muscle tone triggered by positive or negative emotions. Histaminergic neuron signalling in the brain plays a role in maintaining wakefulness; by blocking histamine autoreceptors, pitolisant enhances the activity of histaminergic neurons, as well as increasing the signalling of other neurotransmitters in the brain. In a European clinical trial of adult patients with narcolepsy, there was a reduction in the Epworth Sleepiness Scale (ESS) score from pitolisant therapy compared to placebo. The therapeutic effectiveness of pitolisant was comparable to that of [modafinil]. Pitolisant therapy was also effective in treating refractory sleepiness in adolescent patients with narcolepsy, where it decreased ESS score and increased the mean sleep onset latency. Adolescent patients with cataplexy also experienced a slight improvement in the frequency and severity of symptoms ; however, the safety of use in adolescent or paediatric patients have not been established with pitolisant. Commonly marketed under the trade name Wakix, oral pitolisant was approved by the EMA in 2016 for the treatment of narcolepsy with or without cataplexy. FDA approved the use of pitolisant in 2019 for excessive daytime sleepiness (EDS) associated with narcolepsy in adults.
Indacaterol {u} (Compound) treats {v} (Disease) asthma
asthma {u} (Disease) is treated by {v} (Compound) Hydrocortisone
Hydrocortisone {u} may cause a moderate interaction that could exacerbate diseases when taken with {v} Pitolisant
Indacaterol {u} (Compound) binds {v} (Gene) ADRB1
ADRB1 {u} (Gene) is bound by {v} (Compound) Formoterol
Formoterol {u} may cause a moderate interaction that could exacerbate diseases when taken with {v} Pitolisant
Indacaterol {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} Pitolisant
Indacaterol {u} (Compound) is included by {v} (Pharmacologic Class) Adrenergic beta2-Agonists
Adrenergic beta2-Agonists {u} (Pharmacologic Class) includes {v} (Compound) Salbutamol
Salbutamol {u} may cause a moderate interaction that could exacerbate diseases when taken with {v} Pitolisant
Indacaterol {u} (Compound) causes {v} (Side Effect) Cardiac disorder
Cardiac disorder {u} (Side Effect) is caused by {v} (Compound) Diclofenac
Diclofenac {u} may cause a moderate interaction that could exacerbate diseases when taken with {v} Pitolisant
Indacaterol {u} (Compound) binds {v} (Gene) ADRB2
ADRB2 {u} (Gene) is downregulated by {v} (Compound) Dasatinib
Dasatinib {u} may cause a moderate interaction that could exacerbate diseases when taken with {v} Pitolisant
Indacaterol {u} (Compound) causes {v} (Side Effect) Cardiac disorder
Cardiac disorder {u} (Side Effect) is caused by {v} (Compound) Metronidazole
Metronidazole {u} may cause a minor interaction that can limit clinical effects when taken with {v} Pitolisant
Indacaterol {u} (Compound) binds {v} (Gene) ADRB2
ADRB2 {u} (Gene) is upregulated by {v} (Compound) Irinotecan
Irinotecan {u} may cause a moderate interaction that could exacerbate diseases when taken with {v} Pitolisant
Indacaterol {u} (Compound) binds {v} (Gene) ADRB2
ADRB2 {u} (Gene) is upregulated by {v} (Compound) Terbinafine
Terbinafine {u} may lead to a major life threatening interaction when taken with {v} Pitolisant
Indacaterol {u} (Compound) causes {v} (Side Effect) Unspecified disorder of skin and subcutaneous tissue
Unspecified disorder of skin and subcutaneous tissue {u} (Side Effect) is caused by {v} (Compound) Toremifene
Toremifene {u} may lead to a major life threatening interaction when taken with {v} Pitolisant
Indacaterol (Compound) treats asthma (Disease) and asthma (Disease) is treated by Hydrocortisone (Compound) and Hydrocortisone may cause a moderate interaction that could exacerbate diseases when taken with Pitolisant
Indacaterol (Compound) binds ADRB1 (Gene) and ADRB1 (Gene) is bound by Formoterol (Compound) and Formoterol may cause a moderate interaction that could exacerbate diseases when taken with Pitolisant
Indacaterol (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 Pitolisant
Indacaterol (Compound) is included by Adrenergic beta2-Agonists (Pharmacologic Class) and Adrenergic beta2-Agonists (Pharmacologic Class) includes Salbutamol (Compound) and Salbutamol may cause a moderate interaction that could exacerbate diseases when taken with Pitolisant
Indacaterol (Compound) causes Cardiac disorder (Side Effect) and Cardiac disorder (Side Effect) is caused by Diclofenac (Compound) and Diclofenac may cause a moderate interaction that could exacerbate diseases when taken with Pitolisant
Indacaterol (Compound) binds ADRB2 (Gene) and ADRB2 (Gene) is downregulated by Dasatinib (Compound) and Dasatinib may cause a moderate interaction that could exacerbate diseases when taken with Pitolisant
Indacaterol (Compound) causes Cardiac disorder (Side Effect) and Cardiac disorder (Side Effect) is caused by Metronidazole (Compound) and Metronidazole may cause a minor interaction that can limit clinical effects when taken with Pitolisant
Indacaterol (Compound) binds ADRB2 (Gene) and ADRB2 (Gene) is upregulated by Irinotecan (Compound) and Irinotecan may cause a moderate interaction that could exacerbate diseases when taken with Pitolisant
Indacaterol (Compound) binds ADRB2 (Gene) and ADRB2 (Gene) is upregulated by Terbinafine (Compound) and Terbinafine may lead to a major life threatening interaction when taken with Pitolisant
Indacaterol (Compound) causes Unspecified disorder of skin and subcutaneous tissue (Side Effect) and Unspecified disorder of skin and subcutaneous tissue (Side Effect) is caused by Toremifene (Compound) and Toremifene may lead to a major life threatening interaction when taken with Pitolisant