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Armodafinil

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Collated from PsychonautWiki, TripSit, Pharmacology, DrugCentral, DailyMed. Where sources differ (e.g. dosing), Compare shows them side by side.

Sections
StimulantEugeroicBenzhydrylNootropicHabit-formingPW

Also known as Armodafinil, Nuvigil, Waklert, Artvigil, R-Modawake, NeoresotylPW

The more potent of the two modafinil isomers, said to have a longer duration and lesser side effects. Sometimes prescribed for ADHD and daytime sleepiness.TS

Addiction potentialPW
mildly addictive with a low potential for abuse
ToxicityPW
The median lethal dose at which 50% of participants die (LD50) from either armodafinil or modafinil for human beings has never been reached
TolerancePW
full tolerance develops with prolonged and repeated use; half after 3 - 7 days; baseline after 1 - 2 weeks
Cross-tolerancePW
benzhydryl, nootropic

Oral

Route dataPsychonautWiki

Dose
WeakerStronger
ThresholdLightCommonStrongHeavy
20 mg40–100 mg100–200 mg200–300 mg300 mg+
0375 mg
LightCommonStrongHeavy
Duration
ShorterLonger
Onset20–60 minutes
Come-up1–2.5 hours
Peak4–7 hours
Offset2–5 hours
Total8–15 hours
After-effects2–12 hours
OnsetCome-upPeakOffset

Unsafe interactionsPW

DXMMDMAStimulants

Caution / uncertainPW

AlcoholMXEDissociatives

🧬 Receptor activityPHDC

TargetActionAffinitySource
Sodium-dependent dopamine transporter—Ki 647 nMCHEMBL
Unchecked—Ki 8920 nMCHEMBL
D(3) dopamine receptor—Ki 39000 nMCHEMBL
D(2) dopamine receptor—Ki 100000 nMCHEMBL
D(4) dopamine receptor—Ki 100000 nMCHEMBL
Sigma non-opioid intracellular receptor 1—Ki 100000 nMCHEMBL
Sodium-dependent dopamine transporter (SLC6A3)Inhibitor5.497 IC50DRUGCENTRAL
Alpha-1B adrenergic receptor (ADRA1B)——DRUGCENTRAL
Cytochrome P450 1A2 (CYP1A2)——DRUGCENTRAL
Cytochrome P450 2C19 (CYP2C19)——DRUGCENTRAL
D(2) dopamine receptor (DRD2)—6.921 EC50DRUGCENTRAL
D(3) dopamine receptor (DRD3)—4.41 KiDRUGCENTRAL
Sodium-dependent dopamine transporter (Slc6a3)—5.49 KiDRUGCENTRAL
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Mechanism of actionPHDM

Nuvigil (armodafinil) is a single-isomer of modafini. The exact mechanism of action is unknown. Armodafinil belongs to a class of drugs known as eugeroics, which are stimulants that provide long-lasting mental arousal. Pharmacologically, armodafinil does not bind to or inhibit several receptors and enzymes potentially relevant for sleep/wake regulation. Armodafinil is not a direct- or indirect-acting dopamine receptor agonist. However, in vitro, both armodafinil and modafinil bind to the dopamine transporter and inhibit dopamine reuptake. [Medilexicon]

Pharmacokinetics

Half-lifePH

Terminal half-life is approximately 15 hours.

AbsorptionPHDM

Tmax is 2 hours when fasted and can be delayed approximately 2-4 hours by food, potentially affecting the onset of action.
Apparent volume of distribution: 42L.
The oral clearance of armodafinil is approximately 33 mL/min.

MetabolismPH

In vitro and in vivo data show that armodafinil undergoes hydrolytic deamidation, S-oxidation, and aromatic ring hydroxylation, with subsequent glucuronide conjugation of the hydroxylated products. Amide hydrolysis is the single most prominent metabolic pathway, with sulfone formation by cytochrome P450 (CYP) 3A4/5 being next in importance. The other oxidative products are formed too slowly in vitro to enable identification of the enzyme(s) responsible. Only two metabolites reach appreciable concentrations in plasma (i.e., R-modafinil acid and modafinil sulfone). Data specific to armodafinil disposition are not available.

Protein bindingPH

Specific data unavailable. Similar to modafinil: approximately 60%, primarily to albumin.

Plan when to take Armodafinil — see where onset, peak and comedown land on the clock

Fact-sheets from PsychonautWiki. Harm-reduction reference only — not medical advice.