Pitolisant Brand Name– WAKIX
What is Pitolisant
Pitolisant is an oral histamine-3 (H3) receptor antagonist/inverse agonist, the first in its class.
Pitolisant is indicated for the treatment of excessive daytime sleepiness (EDS) in adult patients with narcolepsy.
The efficacy of pitolisant for the treatment of EDS was established in 2 placebo-controlled, active control trials of 8 weeks duration.
In both trials, pitolisant significantly improved EDS measured according to the least-squares mean final Epworth Sleepiness Scale (ESS) used by patients to rate their perceived likelihood of falling asleep during usual daily life activities, with lower scores indicating less severe disease.
Final mean ESS scores at week 8 were 12.4 (1.01 SE) and 15.5 (1.03) for pitolisant- and placebo-treated patients, respectively, with a significant subtracted difference of -3.1 (95% CI -5.73; -0.46) for study 1.
Final mean ESS scores at week 8 were 13.3 (1.19) and 15.5 (1.32) for pitolisant- and placebo-treated patients, respectively, with a significant subtracted difference of -2.2 (95% CI -4.17; -0.22) for study 2.
The drug may cause QT prolongation and it is contraindicated in patients with severe hepatic impairment.
Pitolisant was FDA-approved in August 2019.
Indications
- narcolepsy
For the treatment of excessive daytime sleepiness in patients with narcolepsy
Side Effects
- abdominal pain
- abnormal dreams
- anxiety
- arthralgia
- atopic dermatitis
- back pain
- carpal tunnel syndrome
- cataplexy
- depression
- fatigue
- hallucinations
- headache
- infection
- insomnia
- irritability
- migraine
- musculoskeletal pain
- myalgia
- nausea
- nightmares
- pharyngitis
- pruritus
- QT prolongation
- rash
- rhinitis
- seizures
- sinus tachycardia
- sinusitis
- sleep paralysis
- suicidal ideation
- urticaria
- weight gain
- xerostomia
Monitoring Parameters
- LFTs
- serum bilirubin
- serum creatinine/BUN
Contraindications
- apheresis
- AV block
- bradycardia
- breast-feeding
- cardiac arrhythmias
- cardiomyopathy
- celiac disease
- children
- contraception requirements
- females
- fever
- geriatric
- heart failure
- hepatic disease
- human immunodeficiency virus (HIV) infection
- hyperparathyroidism
- hypocalcemia
- hypokalemia
- hypomagnesemia
- hypothermia
- hypothyroidism
- infants
- long QT syndrome
- myocardial infarction
- pheochromocytoma
- poor metabolizers
- pregnancy
- QT prolongation
- renal failure
- renal impairment
- rheumatoid arthritis
- sickle cell disease
- sleep deprivation
- stroke
- systemic lupus erythematosus (SLE)
Interactions
- Acetaminophen; Caffeine; Magnesium Salicylate; Phenyltoloxamine
- Acetaminophen; Caffeine; Phenyltoloxamine; Salicylamide
- Acetaminophen; Chlorpheniramine; Dextromethorphan; Phenylephrine
- Acetaminophen; Chlorpheniramine; Dextromethorphan; Pseudoephedrine
- Acetaminophen; Chlorpheniramine; Phenylephrine; Phenyltoloxamine
- Acetaminophen; Dextromethorphan; Doxylamine
- Acetaminophen; Diphenhydramine
- Aclidinium; Formoterol
- Acrivastine; Pseudoephedrine
- Albuterol
- Albuterol; Ipratropium
- Alfuzosin
- Amiodarone
- Amitriptyline
- Amitriptyline; Chlordiazepoxide
- Amoxicillin; Clarithromycin; Lansoprazole
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- Anagrelide
- Apalutamide
- Apomorphine
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- Bedaquiline
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- Brompheniramine
- Brompheniramine; Carbetapentane; Phenylephrine
- Brompheniramine; Dextromethorphan; Guaifenesin
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- Chlorpheniramine; Guaifenesin; Hydrocodone; Pseudoephedrine
- Chlorpheniramine; Hydrocodone
- Chlorpheniramine; Hydrocodone; Phenylephrine
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