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Drug Profile Comparison Between Pitolisant

Pitolisant, Armodafinil, and Modafinil are psychostimulant drugs approved to treat excessive daytime sleepiness. Pitolisant is a histamine receptor antagonist, while Armodafinil and Modafinil are indirect dopamine receptor agonists. They have similar dosages and indications to improve wakefulness in adult patients with excessive sleepiness associated with conditions like narcolepsy or sleep apnea. Common adverse effects include headache, nausea, and insomnia. While their mechanisms are not fully understood, they are thought to act on histamine, norepinephrine, serotonin, dopamine and orexin systems in the brain.

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115 views3 pages

Drug Profile Comparison Between Pitolisant

Pitolisant, Armodafinil, and Modafinil are psychostimulant drugs approved to treat excessive daytime sleepiness. Pitolisant is a histamine receptor antagonist, while Armodafinil and Modafinil are indirect dopamine receptor agonists. They have similar dosages and indications to improve wakefulness in adult patients with excessive sleepiness associated with conditions like narcolepsy or sleep apnea. Common adverse effects include headache, nausea, and insomnia. While their mechanisms are not fully understood, they are thought to act on histamine, norepinephrine, serotonin, dopamine and orexin systems in the brain.

Uploaded by

akshay dahiwele
Copyright
© © All Rights Reserved
We take content rights seriously. If you suspect this is your content, claim it here.
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Download as DOCX, PDF, TXT or read online on Scribd
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Drug profile comparison between Pitolisant, Armodafinil and

Modafinil
Comparative Parameters Pitolisant Armodafinil Modafinil

Class Histamine receptor antagoni Psychostimulant Psychostimulant


st/ inverse agonists
Approval status in USA, USA, Europe USA, Europe, India (2010) USA, Europe, India(2003)
Europe and India
Indication  Indicated for the Indicated to improve Indicated to improve
excessive daytime wakefulness in adult wakefulness in adult patients
sleepiness in narcolepsy patients with excessive with
 Cataplexy sleepiness associated with Excessive sleepiness
obstructive sleep apnea associated with narcolepsy,
(OSA), narcolepsy, or shift obstructive sleep apnea
work disorder (SWD)
Dosage and administration  Recommended dosage  OSA or Narcolepsy: 150  Narcolepsy or OSA: 200 mg
range is 17.8 mg to 35.6 mg to 250 mg once a once a day in the morning.
mg daily day in the morning.  SWD: 200 mg once a day,
 Dose titration:  SWD: 150 mg once a taken approximately one
 Week 1: Initiate with day, taken hour prior to start of the work
8.9 mg once daily approximately one hour shift.
 Week 2: Increase prior to start of the work
dosage to 17.8 mg shift.
once daily
 Week 3: May
increase to the
maximum
recommended
dosage of
 35.6 mg once daily
Mode of action Mechanism is unclear, Mechanism is unclear, Mechanism is unclear, however,
however it acts as a however, armodafinil have Most research on modafinil’s
antagonist/inverse agonist wake-promoting actions wake-promoting mechanism has
at histamine-3 (H3) similar to sympathomimetic focused on monoaminergic
receptors agents including effects showing modafinil
amphetamine and stimulates histamine (HA),
methylphenidate, although norepinephrine (NE), serotonin
their pharmacologic profile (5-HT), dopamine (DA), and
is not identical. orexin systems in the brain
Pharmacodynamics Pitolisant binds to H3 Armodafinil is an indirect Modafinil is not a direct-or
receptors with a high affinity dopamine receptor agonist; indirect-acting dopamine
and has no appreciable armodafinil bind in vitro to receptor agonist. However, in
binding to other the dopamine transporter vitro, modafinil binds to the
histamine receptors (H1, and inhibit dopamine dopamine transporter and
H2, or H4 receptors). reuptake. inhibits dopamine reuptake.
Pharmacokinetics Absorption: oral absorption Absorption: Readily Absorption: readily absorbed
– 90%, Tmax of Pitolisant is absorbed after oral after oral administration
3.5 hours. administration. Distribution: Vd is approximately
Distribution: Vd - 5-10L/kg Tmax – 2 hrs in fasting stage 0.9 L/kg, plasma protein binding
Protein binding: 91-96% Distribution: Vd – 42 L, - 60%
Elimination: T1/2 – 20hrs Terminal t1/2 – 15hrs Metabolism is primarily by the
Metabolism: by CYP2D6 Metabolism: cytochrome liver, with subsequent renal
and CYP3A4 P450 (CYP) 3A4/5 elimination of the metabolites
Excretion: Majority by renal Elimination: mostly by liver
and to some extent by to some extent by renal
feces.
Adverse drug reaction The most common adverse Most common adverse Most common adverse reactions
reactions were insomnia, reactions (>5%): headache, (≥5%): headache, nausea,
nausea, and anxiety nausea, dizziness, and nervousness
insomnia. rhinitis, diarrhea, back pain,
anxiety, insomnia, dizziness,
and dyspepsia.

References
1. https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=23da56b8-7552-4362-a1ab-e794c131194c
2. https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=e16c26ad-7bc2-d155-3a5d-da83ad6492c8
3. Gerrard P, Malcolm R. Mechanisms of modafinil: A review of current research. Neuropsychiatr Dis Treat. 2007;3(3):349-364.
4. https://www.accessdata.fda.gov/drugsatfda_docs/label/2019/211150s000lbl.pdf

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