Drilldown: Medicines
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mechanism:
None (1) ·
Positive allosteric modulator of the GABA<sub>A</sub> receptor at the benzodiazepine binding site; increases frequency of Cl<sup>−</sup> channel opening, producing anxiolytic, sedative, hypnotic, anticonvulsant, and skeletal-muscle relaxant effects. (1) ·
Selective dopamine and norepinephrine reuptake inhibitor (DAT and NET inhibition). Unlike amphetamine, does not significantly release monoamines, pure reuptake inhibition. (1)
uses:
Excessive daytime sleepiness in adults with narcolepsy or obstructive sleep apnea (OSA) (1) ·
Excessive daytime sleepiness or cataplexy in adults with narcolepsy (FDA-approved August 2019) (1) ·
No approved medical problem. Encountered as a designer/research benzodiazepine and, increasingly, as an adulterant in illicit opioid supplies. (1)
starting dose:
Narcolepsy: 75 mg PO once daily upon awakening, titrate every 3 days. OSA: 37.5 mg PO once daily, titrate. (1) ·
No medical dose. Active recreational doses reported in the 0.5–1.5 mg range (similar potency to alprazolam). (1) ·
Week 1: 8.9 mg PO once daily in the morning. Week 2: 17.8 mg. Week 3+: 35.6 mg (max). Titrate as needed. (1)
preparations:
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pregnancy:
Avoid. Benzodiazepines are associated with neonatal sedation, floppy-infant syndrome, and withdrawal; teratogenic signal weak but non-zero. Designer benzo with no safety data, assume worst-case. (1) ·
Limited data; pitolisant may reduce hormonal contraceptive efficacy (1) ·
Limited data; pregnancy exposure registry available (1)
Showing below up to 3 results in range #1 to #3.