Pitolisant

Category: pharmacological

Aliases: Wakix

Pharmacological Mechanism

Histamine H3 receptor antagonist / inverse agonist; raises central histamine to promote wakefulness (narcolepsy). CYP2D6 + CYP3A4 metabolism.

Half-Life (t½)

PO: 20h

Dosing Guidelines

• PO: Typical 17.8 mg (Range: 17.8–35.6 mg)

Target Organ Systems

• nervous

Notes

PK from FDA prescribing information (DailyMed setid 8daa5562-824e-476c-9652-26ceef3d4b0e): oral absorption ~90% (F 0.9), Vd 5–10 L/kg (~700 L), terminal t½ ~20 h, Tmax 3.5 h, CYP2D6/3A4. ka_hr 1.0 derived from Tmax 3.5 h (ke from t½ 20 h).

Chemical Identifiers

• PubChem CID: 9948102
• Formula: C17H26ClNO
• Molecular weight: 295.8 g/mol
• InChIKey: NNACHAUCXXVJSP-UHFFFAOYSA-N
• SMILES: C1CCN(CC1)CCCOCCCC2=CC=C(C=C2)Cl

References

• PMID 26084539