Also known as: Narcolepsy NOS

DrugDrug NameDrug Description
DB00182AmphetamineAmphetamine, a compound discovered over 100 years ago, is one of the more restricted controlled drugs. It was previously used for a large variety of conditions and this changed until this point where its use is highly restricted. Amphetamine, with the chemical formula alpha-methylphenethylamine, was discovered in 1910 and first synthesized by 1927. After being proven to reduce drug-induced anesthesia and produce arousal and insomnia, amphetamine racemic mix was registered by Smith, Kline and French in 1935. Amphetamine structure presents one chiral center and it exists in the form of dextro- and levo-isomers.[A18540] The first product of Smith, Kline and French was approved by the FDA on 1976.[L5194] During World War II, amphetamine was used to promote wakefulness in the soldiers. This use derived into a large overproduction of amphetamine and all the surplus after the war finalized end up in the black market which produced the initiation of the illicit abuse.[A18540]
DB06413ArmodafinilArmodafinil is the enantiopure of the wakefulness-promoting agent modafinil (Provigil), and is indicated to improve wakefulness in adult patients with excessive sleepiness associated with obstructive sleep apnea (OSA), narcolepsy, or shift work disorder (SWD). Research has shown that armodafinil significantly improves driving simulator performance in patients with SWD. Armodafinil consists of the (−)-R-enantiomer of the racemic modafinil. Armodafinil is produced by the pharmaceutical company Cephalon Inc. (a wholly owned subsidiary of Teva Pharmaceutical Industries Ltd.) and was approved by the U.S. Food and Drug Administration (FDA) in June 2007.
DB01576DextroamphetamineDextroamphetamine is the dextrorotary stereoisomer of the amphetamine molecule, which can take two different forms. It is a slightly polar, weak base and is lipophilic.
DB01577MetamfetamineMetamfetamine (methamphetamine) is a psychostimulant and sympathomimetic drug. It is a member of the amphetamine group of sympathomimetic amines. Methamphetamine can induce effects such as euphoria, increased alertness and energy, and enhanced self-esteem. It is a scheduled drug in most countries due to its high potential for addiction and abuse.
DB00422MethylphenidateA central nervous system stimulant used most commonly in the treatment of attention-deficit disorders in children and for narcolepsy. Its mechanisms appear to be similar to those of dextroamphetamine.
DB00745ModafinilModafinil is a stimulant drug marketed as a 'wakefulness promoting agent' and is one of the stimulants used in the treatment of narcolepsy. Narcolepsy is caused by dysfunction of a family of wakefulness-promoting and sleep-suppressing peptides, the orexins, whose neurons are activated by modafinil. The prexin neuron activation is associated with psychoactivation and euphoria. The exact mechanism of action is unclear, although in vitro studies have shown it to inhibit the reuptake of dopamine by binding to the dopamine reuptake pump, and lead to an increase in extracellular dopamine. Modafinil activates glutamatergic circuits while inhibiting GABA.
DB11642PitolisantPitolisant is also known as 1-{3-[3-(4-chlorophenyl)propoxy]propyl}piperidine or BF2.649 [A32025]. It is a selective inverse agonist of the histamine H3 receptor that is used in the treatment of type 1 or 2 narcolepsy with or without cataplexy in adults. Narcolepsy is a chronic neurological disorder that that affects 1 in 2,000 individuals and is characterized by excessive daytime sleepiness, abnormal REM sleep manifestations, sleep paralysis and hypnagogic hallucinations [A32025]. About 60-70% of patients with narcolepsy experience cataplexy, which is a sudden loss of muscle tone triggered by positive or negative emotion [A32022]. As histaminergic signalling in neurons plays a role in maintaining wakefulness, pitolisant works by blocking histamine autoreceptors and enhancing the activity of brain histaminergic neurons [L1471]. In a European clinical trial of adult patients with narcolepsy, a reduction in the Epworth Sleepiness Scale (ESS) score was observed from pitolisant treatment compared to placebo [A32024]. The therapeutic effectiveness of pitolisant was comparable to that of [DB00745] [A32024]. 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 [A32023]. Adolescent patients with cataplexy also experienced a slight improvement in the frequency and severity of symptoms [A32023], however the safety of use in adolescent or paediatric patients have not been established with pitolisant. Pitolisant is marketed by EMA under the trade name Wakix as oral tablets.
DB09072Sodium oxybateSodium oxybate (Xyrem) is a central nervous system depressant used for the treatment of cataplexy and extreme daytime sleepiness (EDS) associated with narcolepsy. It is the sodium salt of gamma hydroxybutyric acid (GHB) which is an endogenous compound and a metabolite of the neurotransmitter GABA. The exact mechanism of action for treating EDS and cataplexy is not known but is is hypothesised that its therapeutic effects are due to GABA(B) effects on noradrenergic, dopaminaergic and thalamocorticol neurons. The drug follows non-linear pharmacokinetics. As it has been associated with misuse/abuse it is strictly controlled and all patients and prescribers must enroll in the sodium oxybate REMs program in order to gain access to the medication.
DrugDrug NameTargetType
DB00182AmphetamineSodium-dependent dopamine transportertarget
DB00182AmphetamineCocaine- and amphetamine-regulated transcript proteintarget
DB00182AmphetamineTrace amine-associated receptor 1target
DB00182AmphetamineCytochrome P450 2D6enzyme
DB00182AmphetamineSolute carrier family 22 member 3transporter
DB00182AmphetamineSolute carrier family 22 member 5transporter
DB00182AmphetamineSynaptic vesicular amine transportertarget
DB00182AmphetamineCytochrome P450 2A6enzyme
DB00182AmphetamineSodium-dependent noradrenaline transportertarget
DB00182AmphetamineAlpha adrenergic receptortarget
DB00182AmphetamineBeta adrenergic receptortarget
DB00182AmphetamineD(2) dopamine receptortarget
DB00182AmphetamineAmine oxidase [flavin-containing] Btarget
DB00182AmphetamineSodium-dependent serotonin transportertarget
DB00182AmphetamineMonoamine oxidasetarget
DB00182Amphetaminevesicular monoamine transporter 2 (VMAT2)target
DB06413ArmodafinilCytochrome P450 2C19enzyme
DB06413ArmodafinilCytochrome P450 3A4enzyme
DB06413ArmodafinilCytochrome P450 1A2enzyme
DB06413ArmodafinilCytochrome P450 2B6enzyme
DB06413ArmodafinilCytochrome P450 3A5enzyme
DB06413ArmodafinilCytochrome P450 2C9enzyme
DB06413ArmodafinilSodium-dependent dopamine transportertarget
DB01576DextroamphetamineAlpha-1A adrenergic receptortarget
DB01576DextroamphetamineAlpha-1B adrenergic receptortarget
DB01576DextroamphetamineSodium-dependent dopamine transportertarget
DB01576DextroamphetamineSodium-dependent noradrenaline transportertarget
DB01576DextroamphetamineSynaptic vesicular amine transportertarget
DB01576DextroamphetamineTrace amine-associated receptor 1target
DB01577MetamfetamineCytochrome P450 2D6enzyme
DB01577MetamfetamineSolute carrier family 22 member 3transporter
DB01577MetamfetamineSolute carrier family 22 member 5transporter
DB01577MetamfetamineSodium-dependent dopamine transportertarget
DB01577MetamfetamineSynaptic vesicular amine transportertarget
DB01577MetamfetamineTrace amine-associated receptor 1target
DB01577MetamfetamineSodium-dependent serotonin transportertarget
DB01577MetamfetamineSodium-dependent noradrenaline transportertarget
DB01577MetamfetamineChromaffin granule amine transportertarget
DB01577MetamfetamineAmine oxidase [flavin-containing] Atarget
DB01577MetamfetamineAmine oxidase [flavin-containing] Btarget
DB01577MetamfetamineAlpha-2A adrenergic receptortarget
DB01577MetamfetamineAlpha-2B adrenergic receptortarget
DB01577MetamfetamineAlpha-2C adrenergic receptortarget
DB00422MethylphenidateSodium-dependent dopamine transportertarget
DB00422MethylphenidateSodium-dependent noradrenaline transportertarget
DB00422MethylphenidateSodium-dependent serotonin transportertarget
DB00745ModafinilSodium-dependent dopamine transportertarget
DB00745ModafinilAlpha-1B adrenergic receptortarget
DB00745ModafinilCytochrome P450 3A4enzyme
DB00745ModafinilCytochrome P450 2C19enzyme
DB00745ModafinilCytochrome P450 1A2enzyme
DB00745ModafinilCytochrome P450 2B6enzyme
DB00745ModafinilCytochrome P450 2C9enzyme
DB00745ModafinilCytochrome P450 3A5enzyme
DB11642PitolisantHistamine H3 receptortarget
DB11642PitolisantCytochrome P450 3A4enzyme
DB11642PitolisantCytochrome P450 2D6enzyme
DB11642PitolisantCytochrome P450 1A2enzyme
DB11642PitolisantCytochrome P450 2B6enzyme
DB11642PitolisantSolute carrier family 22 member 1transporter
DB11642PitolisantPotassium voltage-gated channel subfamily H member 2target
DB09072Sodium oxybateSuccinate-semialdehyde dehydrogenase, mitochondrialenzyme
DB09072Sodium oxybateHydroxyacid-oxoacid transhydrogenase, mitochondrialenzyme
DrugDrug NamePhaseStatusCount
DB09072Sodium oxybate0Recruiting1
DB00201Caffeine1 / 2Recruiting1
DB09311Polycarbophil1 / 2Recruiting1
DB09072Sodium oxybate3Completed3
DB09072Sodium oxybate3Recruiting1
DB06413ArmodafinilNot AvailableRecruiting1
DB00745ModafinilNot AvailableCompleted2
DB00745ModafinilNot AvailableRecruiting1