Modafinil

Modafinil
ATC Code N06BA07
Formula C15H15NO2S
Molar Mass (g·mol−1) 273,35
Physical State solid
Density (g·cm−3) 1,342
Melting Point (°C) 164–166
CAS Number 68693-11-8
PUB Number 4236
Drugbank ID DB00745
Solubility insoluble in water

Basics

Modafinil is a drug used to treat sleepiness due to narcolepsy, sleep disturbances due to shift work, or obstructive sleep apnea. It is also used off-label for the alleged improvement of cognitive abilities. However, its efficacy for this application has not been confirmed. It is taken by mouth.

Pharmacology

Pharmacodynamics

The exact mechanism of action is not fully understood. Modafinil is thought to inhibit the reuptake of dopamine by binding to the dopamine reuptake pump, leading to an increase in extracellular dopamine. Modafinil also activates glutamate receptors while inhibiting GABA channels. Modafinil has less abuse potential than other stimulants (Adderall, Ritalin) because it does not induce significant euphoric effects.

Pharmacokinetics

Modafinil is rapidly absorbed in the gastrointestinal tract. Plasma protein binding is approximately 60%. Modafinil is metabolized in the liver and 90% is excreted in the urine. The half-life is between 23 and 215 hours.

Drug Interactions

Concomitant administration of Modafinil with opioids such as hydrocodone, oxycodone, and fentanyl, as well as various other drugs, may result in a decrease in plasma concentrations.

Toxicity

Side effects

Common side effects include headache, anxiety, sleep disturbances, and nausea.

Severe side effects may include allergic reactions such as anaphylaxis, Stevens-Johnson syndrome, and hallucinations. The dose may need to be adjusted in people with kidney or liver problems.

It is not recommended in cardiac arrhythmias, significant hypertension, or left ventricular hypertrophy.

There are no data on the safety of modafinil during pregnancy and lactation, so the drug should not be taken during this time.

Toxicological Data

LD50 (mouse, i.v.): > 800 mg-kg-1

Sources

  • Drugbank
  • PubChem
  • Aktories, Förstermann, Hofmann, Starke: Allgemeine und spezielle Pharmakologie und Toxikologie, Elsvier, 2017
Markus Falkenstätter

Markus Falkenstätter
Author

Markus Falkenstätter ist Autor zu pharmazeutischen Themen in der Medizin-Redaktion von Medikamio. Er befindet sich im letzten Semester seines Pharmaziestudiums an der Universität Wien und liebt das wissenschaftliche Arbeiten im Bereich der Naturwissenschaften.

Mag. pharm Stefanie Lehenauer

Mag. pharm Stefanie Lehenauer
Lector

Stefanie Lehenauer ist seit 2020 freie Autorin bei Medikamio und studierte Pharmazie an der Universität Wien. Sie arbeitet als Apothekerin in Wien und ihre Leidenschaft sind pflanzliche Arzneimittel und deren Wirkung.

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