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Wakix
pitolisant
Adult Dosing .
Dosage forms: TAB: 4.45 mg, 17.8 mg
narcolepsy
- [17.8-35.6 mg PO qam]
- Start: 8.9 mg PO qam x1wk, then 17.8 mg PO qam x1wk, then may incr. to 35.6 mg PO qam; Max: 35.6 mg/day; Info: for patients with cataplexy or excessive daytime sleepiness; max 17.8 mg/day in CYP2D6 poor metabolizers
renal dosing
- [see below]
- eGFR 60-89: not defined, caution advised; eGFR 15-59: start 8.9 mg qd x7 days, then incr. to max 17.8 mg/day; eGFR <15: avoid use
- HD/PD: not defined
hepatic dosing
- [see below]
- Child-Pugh Class B: start 8.9 mg qd x14 days, then incr. to max 17.8 mg/day; Child-Pugh Class C: contraindicated
Peds Dosing .
- Dosage forms: TAB: 4.45 mg, 17.8 mg
narcolepsy
- [6 yo and older, <40 kg]
- Dose: 17.8 mg PO qam; Start: 4.45 mg PO qam x1wk, then 8.9 mg PO qam x1wk, then 17.8 mg PO qam; Max: 17.8 mg/day; Info: for patients with cataplexy or excessive daytime sleepiness; max 8.9 mg/day in CYP2D6 poor metabolizers
- [6 yo and older, >40 kg]
- Dose: 17.8-35.6 mg PO qam; Start: 4.45 mg PO qam x1wk, then 8.9 mg PO qam x1wk, then 17.8 mg PO qam x1wk, then may incr. to 35.6 mg PO qam; Max: 35.6 mg/day; Info: for patients with cataplexy or excessive daytime sleepiness; max 17.8 mg/day in CYP2D6 poor metabolizers
renal dosing
- [<40 kg]
- eGFR 60-89: not defined, caution advised; eGFR 15-59: start 4.45 mg qd x7 days, then incr. to max 8.9 mg/day; eGFR <15: avoid use
- HD/PD: not defined
- [>40 kg]
- eGFR 60-89: not defined, caution advised; eGFR 15-59: start 4.45 mg qd x7 days, then 8.9 mg qd x7 days, then may incr. to max 17.8 mg/day; eGFR <15: avoid use
- HD/PD: not defined
hepatic dosing
- [<40 kg]
- Child-Pugh Class B: start 4.45 mg qd x14 days, then incr. to max 8.9 mg/day; Child-Pugh Class C: contraindicated
- [>40 kg]
- Child-Pugh Class B: start 4.45 mg qd x14 days, then 8.9 mg qd x14 days, then may incr. to max 17.8 mg/day; Child-Pugh Class C: contraindicated
Contraindications / Cautions .
- hypersensitivity to drug or ingredient
- hepatic impairment, Child-Pugh Class C
- eGFR <15
- electrolyte abnormalities, uncorrected
- long QT syndrome, congenital
- QT prolongation
- QT prolongation family history
- torsades de pointes history
- arrhythmia history
- bradycardia
- MI, recent
- CHF
- caution: hepatic impairment, Child-Pugh Class A-B
- caution: eGFR 15-89
- caution: CYP2D6 poor metabolizers
Drug Interactions .
Overview
pitolisant
H3 antagonist/inverse agonist
- CYP2D6 substrate
- CYP3A4 substrate
- CYP3A4 inducer, weak
- increases central histamine effects
- prolongs QT interval (conditional)
Contraindicated
- paroxetine
- pimozide
- quinidine (CYP2D6 inhibitor)
- thioridazine
Avoid/Use Alternative
- adagrasib
- amiodarone
- amitriptyline
- amoxapine
- anagrelide
- apalutamide
- apomorphine
- aripiprazole bimonthly injection
- aripiprazole lauroxil
- aripiprazole monthly injection
- aripiprazole oral
- arsenic trioxide
- artemether/lumefantrine
- asenapine
- azithromycin
- bedaquiline
- brexpiprazole
- brompheniramine
- cabozantinib
- carbinoxamine
- cariprazine
- ceritinib
- cetirizine
- chlophedianol
- chlorcyclizine
- chloroquine
- chlorpheniramine
- chlorpromazine
- cisapride
- citalopram
- clarithromycin
- clemastine
- clofazimine
- clomipramine
- clozapine
- crizotinib
- cyproheptadine
- degarelix
- desflurane
- desipramine
- desogestrel (contraceptive)
- dexbrompheniramine
- dexchlorpheniramine
- dexmedetomidine injection
- dienogest (contraceptive)
- dimenhydrinate
- diphenhydramine
- disopyramide
- dofetilide
- domperidone
- donepezil
- dordaviprone
- doxepin
- doxepin topical
- doxylamine
- dronedarone
- droperidol
- drospirenone (contraceptive)
- encorafenib
- ephedra
- epirubicin
- eribulin
- erythromycin
- estradiol (contraceptive)
- ethinyl estradiol (contraceptive)
- ethynodiol (contraceptive)
- etonogestrel (contraceptive)
- fexinidazole
- flecainide
- fluorouracil
- fluphenazine
- fosfomycin injection
- gilteritinib
- glasdegib
- goserelin
- haloperidol
- hydroxychloroquine
- hydroxyzine
- ibutilide
- iloperidone
- imipramine
- inotuzumab ozogamicin
- isoflurane
- ivosidenib
- lefamulin
- leuprolide
- levofloxacin
- levoketoconazole
- levonorgestrel (contraceptive)
- levonorgestrel (post-coital contraceptive)
- lofexidine
- lonafarnib
- loxapine
- macimorelin
- meclizine
- medroxyprogesterone (contraceptive)
- methadone
- milsaperidone
- mirtazapine
- mobocertinib
- moxifloxacin
- nefazodone
- nilotinib
- norelgestromin (contraceptive)
- norethindrone (contraceptive)
- norgestimate (contraceptive)
- norgestrel (contraceptive)
- nortriptyline
- olanzapine
- oliceridine
- ondansetron
- osimertinib
- pacritinib
- paliperidone
- palonosetron
- pasireotide
- pentamidine
- perphenazine
- pheniramine
- procainamide
- prochlorperazine
- promethazine
- propafenone
- protriptyline
- pyrilamine
- quetiapine
- quinidine (antiarrhythmic)
- quinine
- quizartinib
- revumenib
- ribociclib
- risperidone
- rolapitant
- romidepsin
- rucaparib
- segesterone (contraceptive)
- selpercatinib
- sevoflurane
- sotalol
- taletrectinib
- telavancin
- tetrabenazine
- thiothixene
- toremifene
- tramadol
- trazodone
- triclabendazole
- trifluoperazine
- trifluridine
- trimipramine
- triprolidine
- triptorelin
- ulipristal (post-coital contraceptive)
- vandetanib
- vemurafenib
- ziftomenib
- ziprasidone
Monitor/Modify Tx
- abiraterone acetate
- berotralstat
- bupropion
- butalbital
- capivasertib
- carbamazepine
- cinacalcet
- dacomitinib
- dexmedetomidine
- duloxetine
- eliglustat
- enzalutamide
- fedratinib
- fluoxetine
- fosphenytoin
- givosiran
- histrelin
- lumacaftor/ivacaftor
- mavorixafor
- mirabegron
- mitotane
- pentobarbital
- phenobarbital
- phenytoin
- primidone
- rifabutin
- rifampin
- St. John's wort
- terbinafine
- tipranavir
Caution Advised
- bosentan
- cenobamate
- dabrafenib
- efavirenz
- etravirine
- levonorgestrel intrauterine device (contraceptive)
- lopinavir/ritonavir
- lorlatinib
- mavacamten
- mitapivat
- modafinil
- nafcillin
- pexidartinib
- repotrectinib
- rifapentine
- sotorasib
Adverse Reactions .
Serious Reactions
- QT prolongation
- anaphylaxis
Common Reactions
- headache
- insomnia
- nausea
- anxiety
- URI
- musculoskeletal pain
- HR incr.
- hallucinations
- appetite decr.
- abdominal pain
- irritability
- sleep disturbance
- cataplexy
- xerostomia
- rash
Safety/Monitoring .
Monitoring Parameters
eGFR at baseline; QTc if eGFR 15-89 or Child-Pugh Class A or B hepatic impairment
Pregnancy/Lactation .
Pregnancy
Clinical Summary
weigh risk/benefit during pregnancy; inadequate human data available; possible risk of delayed skeletal development based on animal data at 2 and 4x MRHD and risk of embryo-fetal toxicity and death at 8x MRHD
Pregnancy Registry
encourage patients to enroll in Wakix Pregnancy Registry at 1-800-833-7460
Lactation
Clinical Summary
weigh risk/benefit while breastfeeding; no human data available to assess risk of infant harm, though drug excreted into milk; no human data available to assess effects on milk production
Pharmacology .
Metabolism: for pitolisant: liver extensively; CYP450: 2D6 (primary), 3A4 substrate
Excretion: for pitolisant: urine 90% (<2% unchanged), feces 2.3%; Half-life: 7.5-24.2h
Subclass: Narcolepsy/Somnolence
Mechanism of Action
for pitolisant: exact mechanism of action unknown; binds to histamine-3 receptors as an antagonist and inverse agonist
Formulary .
No Formulary Selected
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