Armodafinil Waklert


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Armodafinil is the enantiopure of the wakefulness-promoting agent modafinil (Provigil), and is indicated to improve wakefulness in adult patients with excessive sleepiness associated with obstructive sleep apnea (OSA), narcolepsy, or shift work disorder (SWD).

Research has shown that armodafinil significantly improves driving simulator performance in patients with SWD. Armodafinil consists of the (−)-R-enantiomer of the racemic modafinil.

Armodafinil is produced by the pharmaceutical company Cephalon Inc. (a wholly owned subsidiary of Teva Pharmaceutical Industries Ltd.) and was approved by the U.S. Food and Drug Administration (FDA) in June 2007.

Investigated for use/treatment in sleep disorders, obstructive sleep apnea, schizophrenia and schizoaffective disorders, depression, and bipolar disorders.

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If you have been diagnosed with moderate to severe chronic Shift Work Sleep Disorder (SWSD) and non-drug therapies have been unsuitable or unsuccessful, Armodafinil may be prescribed to keep you awake during your work shift.

Precisely how Armodafinil works is not known, but it is known that it acts on the central nervous system (the brain). It differs from other stimulant medicines that promote wakefulness. Armodafinil increases wakefulness.

Mechanism of action

Waklert (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]


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.

Absorption: Peak plasma concentrations are attained at approximately 2 hours when fasted, and can be delayed approximately 2-4 hours in a fed state. Since the delay in tmax is also associated with elevated plasma concentrations later in time, food can potentially affect the onset and time course of pharmacologic action for armodafinil.

Half life: Terminal half-life is approximately 15 hours.

Side effects

All medicines may cause side effects, but many people have no, or minor, side effects.Some medical conditions may interact with Armodafinil.

Tell your doctor or pharmacist if you have any medical conditions.

Stop taking Armodafinil and call your doctor right away or get emergency treatment if you have a skin rash, hives, sores in your mouth, or your skin blisters and peels, or if you have any sudden wheeziness, difficulty in breathing, swelling, or itching (especially affecting the whole body). Armodafinil may cause the following side effects in some people. In clinical studies, these side effects also occurred in people who received non-active (sugar) tablets. Tell your doctor if you notice any of these: headache, nausea, diarrhoea, dry mouth, poor appetite, runny nose, sore throat, nervous feeling, dizziness, back pain, feeling anxious, upset stomach, trouble sleeping.

This is not a complete list of all side effects that may occur. If you have questions about side effects, contact your health care provider.


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