Modafinil, an effective drug, is used for the treatment of narcolepsy and cataplexy. Narcolepsy is a condition which causes excessive daytime sleepiness or shift work sleep disorders. Shift work sleep disorder means feeling sleepy during normal waking hours and difficulty in falling asleep during regular sleeping hours. It mostly occurs in people who work at night or on rotating shifts. Cataplexy is a condition in which there is abrupt control over muscles in the body. It is a wake-promoting agent. Due to wake-promoting properties of modafinil, it is categorized as a psychostimulant. There are many pieces of evidence showing that it is useful for the treatment of several sleep disorders.
Earlier Modafinil was developed by Cephalon, Inc, a biopharmaceutical company which came into existence in 1987. This drug is sold under the brand name as either Provigil or Alertec. FDA approved this medication in 1998 after many years of clinical studies. Modafinil changes the levels of the natural substances which are present in the brain. These substances control sleep and wakefulness. It works with the release of a substance called monoamine, and at the same time, it increases the level of hypothalamic histamine. This makes modafinil a CNS (central nervous system) stimulant and a drug helping to remain awake with concentration and focus. Amphetamines previously were used for the treatment of sleeping disorders. Modafinil is an updated form of this drug. It is having lesser adverse effects than the earlier and also useful for the treatment of most problems related to sleepiness. There are many neurotransmitters on which modafinil works. These are as follows:
Orexin is a neuropeptide and neurons that respond to orexin found in the hypothalamus. It helps in the sleep-wake cycle. There are increased levels of dopamine and norepinephrine in the hypothalamus with the activation of these neurons, and also there is an increase in histamine levels. There are many studies which show that a defect in orexin systems leads to narcolepsy disorder.
Another mechanism on which modafinil works is the increase in the amount of dopamine. It works with the blockage of the dopamine transporters which are present in the brain as these are the molecules which act to remove dopamine from the synaptonemal complex. Thus modafinil increases the amount of dopamine and also its availability for its action to work upon. Modafinil work like caffeine as it makes the brain highly focused and also increases the levels of Dopamine D2 receptors.
Histamine is a chemical which works as a neurotransmitter. It plays an important role in the regulation of sleep-wake cycle. Neurons of Histamine are found in the hypothalamus in the brain. Other than this, these are present in tuberomammillary nuclei which are also a part of the hypothalamus. It elevates the level of histamine.
It promotes vigilance and alertness. Besides this, it accelerates the heart rate. Norepinephrine is similar to adrenaline.
For balancing and regulation of mood swings, Serotonin plays an important role. Studies on serotonin show that Modafinil is having the quality of improving the mood of the people.
6 GABA (Gamma Amino Butyric Acid)
Modafinil reduces the amount of gamma-aminobutyric acid which leads to increase in histamine. GABA promotes sleep and also induces relaxation. So it also accounts for the vigilance effects of Modafinil (Ferraro et al 1999).
Glutamate is the main excitatory neurotransmitter. It is involved in cognitive functioning (attention and memory) of the brain. The levels of glutamate rise while using with modafinil. (Ferraro et al 2005).
Doses between 100mg/day and 200mg/day are effective in a dose-dependent manner. The doses of Modafinil can be taken either with food or without food. For treating narcolepsy, it should be administered in the morning and for shift work disorders one hour prior to work.
Side-effects related to this medicine are nausea, headache, anxiety, and insomnia. Besides, this drug is having side-effects when taken with other drugs like cyclosporine, theophylline, Micronor, ortho novum. There are other drugs which when taken with modafinil shows increased effects or toxicity wiz, warfarin, diazepam, propranolol, phenytoin, etc. Other than these medicines rifampin, phenobarbital, carbamazepine also increases the toxicity of modafinil.
Alternatives to modafinil are : adrafinil, racetams, Modalert and sulbutiamine. Adrafinil is the pro-drug to modafinil. It means that when it is consumed it gets converted into modafinil. This drug is discovered earlier to modafinil, and it is less potent. Both racetams and adrafinil are unscheduled and unregulated compounds in the USA. It is legal to buy modafinil and use them, but their sales are limited due to FDA laws. Sulbutiamine is good to enhance the mood at the same time. It is an engineered form of vitamin B1. As these drugs enhance focus and mood, they cannot be used for the treatment of narcolepsy. For this purpose, modafinil is useful.
Purchasing of this drug is legal if a doctor prescribed it. But there are many medical stores and online websites that can provide it without any prescription. As this drug has many side-effects, it cannot be consumed without the prescription of a doctor. Too prolonged use of this drug is also harmful. Modafinil becomes a smart choice for students who want to stay awake for a long time and to work hard but it is not prescribed for this, and they often obtain it illegally. Students who use it for quick learning shared experiences, saying that this drug gives them the ability to work longer and harder, improves their focus towards study, increased their working time to 5-6 hours continuously. Although severe side-effects of modafinil cannot be reported till date, it is safe to use when doctors prescribe it. Many countries have adopted the use of this medicine for military purpose, example: French, United Kingdom and the United States of America.