Modafinil
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| 2-((diphenylmethyl)sulfinyl)-acetamide | |
| CAS number 68693-11-8 | ATC code N06BA07 |
| Chemical formula | C15H15NO2S |
| Molecular weight | 273.351 |
| Bioavailability | ? |
| Metabolism | ? |
| Elimination half-life | ? |
| Excretion | ? |
| Pregnancy category | ? |
| Legal status | Schedule IV (USA) |
| Routes of administration | Oral |
Modafinil (Provigil®; Vigicer®; Alertec®) is a stimulant drug produced by the pharmaceutical company Cephalon. It is marketed as a 'wakefulness promoting agent' and is one of the stimulants used in the treatment of narcolepsy. It has also been linked to increased vigilance.
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Indications
The manufacturer claims that modafinil allows people who suffer from unusual fatigue to remain awake without side effects or impairment of job performance. However it does not live up to this in all cases, occasionally producing rashes and intestinal problems. The usual prescription is for a single dose to be taken shortly after waking; its effects last for most of the day without preventing normal sleep at night.
Dosage varies and the drug is more effective on patients who are using modafil for the first time. The half-life in the human body is about 15 hours. Of the many side effects documented in double blind studies only headache was statistically significant at an increase of 5%, however a number of other side effects were about 1% higher than the placebo.
Modafinil is not indicated for complaints of lack of energy or fatigue; but it appears to be very helpful for some patients. Also, it has been used in the treatment of hypersomnia, a disorder in which patients lack the capacity for meaningful sleep and may require ten or more hours per day.
In January of 2005, researchers at the University of Pennsylvania published the results of a small study, which found that modafinil may help recovering cocaine addicts fight their addiction.
Pharmacology
The exact mechanism of action is unclear, although in vitro studies have shown it to inhibit the reuptake of dopamine, while co-administration of a dopamine antagonist eliminated the stimulant effect of the drug. Modafinil activates glutamatergic circuits while inhibiting GABA. Modafinil is thought to have less potential for abuse than other stimulants due to the absence of any significant euphoric or pleasurable effects.
The central stimulating effect of modafinil shows dose and time-related features. The effect tends to be enhanced by chlorination but reduced by methylation. Modafinil blocks the reuptake of noradrenaline by the noradrenergic terminals on sleep-promoting neurons from the ventrolateral preoptic nucleus (VLPO). Such a mechanism could be at least partially responsible for the wake-promoting effect of modafinil.
History
Modafinil originated with the late 1970s invention of adrafinil by scientists working with the French pharmaceutical company Group Lafon. That drug was first offered as an experimental treatment for narcolepsy in France in 1986. Modafinil is the levorotatory isomer of adrafinil, and around 1986 Lafon scientists developed modafinil as a stand-alone drug, among other reasons because modafinil has less in the way of side effects than adrafinil. A U.S. patent (No. 4,927,855) was granted to Lafon over modaifil in 1990. The FDA granted modafinil orphan drug status in 1993, which is good until late 2005. Cephalon filed for U.S. Patent 5,618,845, covering pharmaceutical compositions of modafinil, in 1994. That patent, granted in 1997, was reissued in 2002 as RE37,516, which provides Cephalon with patent protection for the drug in the United States until 2014. Provigil gained FDA approval in 1998.
Military
The French government indicated that the Foreign Legion used modafinil during certain covert operations. Modafinil has reportedly been investigated by the United States military for use by its soldiers.
Legality
On August 3, 2004 ten days before the 2004 Summer Olympics, Modafinil was added onto the list of prohibited substances by the World Anti-Doping Agency.
Modafinil is currently classified as a Schedule IV controlled substance under United States federal law.
External links
- http://www.provigil.com
- http://www.modafinil.com
- http://www.nootropics.com
- Modafinil synthesis (http://www.rhodium.ws/chemistry/adrafinil.modafinil.html)
- http://www.cephalon.com
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