Armodafinil
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🧬 Receptor activity
| Target | Action | Affinity | Source | |
|---|---|---|---|---|
| Sodium-dependent dopamine transporter | — | Ki 647 nM | CHEMBL | TargetSodium-dependent dopamine transporter Action— AffinityKi 647 nM SourceCHEMBL |
| Unchecked | — | Ki 8920 nM | CHEMBL | TargetUnchecked Action— AffinityKi 8920 nM SourceCHEMBL |
| D(3) dopamine receptor | — | Ki 39000 nM | CHEMBL | TargetD(3) dopamine receptor Action— AffinityKi 39000 nM SourceCHEMBL |
| D(2) dopamine receptor | — | Ki 100000 nM | CHEMBL | TargetD(2) dopamine receptor Action— AffinityKi 100000 nM SourceCHEMBL |
| D(4) dopamine receptor | — | Ki 100000 nM | CHEMBL | TargetD(4) dopamine receptor Action— AffinityKi 100000 nM SourceCHEMBL |
| Sigma non-opioid intracellular receptor 1 | — | Ki 100000 nM | CHEMBL | TargetSigma non-opioid intracellular receptor 1 Action— AffinityKi 100000 nM SourceCHEMBL |
Mechanism of action
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-life
Terminal half-life is approximately 15 hours.
Absorption
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.
Metabolism
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 binding
Specific data unavailable. Similar to modafinil: approximately 60%, primarily to albumin.
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