Pharmacological group: central stimulant, psychostimulant, nootropic. Pharmacological action: the treatment of narcolepsy, sleep apnea, and other sleep disorders. Effect on receptor alpha-1-adrenoceptor (agonist)
Modafinil or benzhydrylsulfinylacetamide – central stimulant (psychostimulant). Substance approved by the FDA for the treatment of narcolepsy (a disease characterized by sudden and uncontrollable episodes of deep sleep, fatigue or excessive sleepiness), sleep apnea, and sleep disturbances caused by changes in the operating mode. Tests were conducted quality drug, including, as an agent for treating Alzheimer’s disease, depression, and attention deficit disorder. Modafinil belongs to a group of drugs known as evgeroiki (stimulants), promotes mental alertness and attention. One of the known mechanisms of action of these drugs is agonism alpha 1-adrenoceptor, resulting in drugs affect mood, increasing energy by increasing dopamine release in the central nervous system. This also leads to changes in the levels of GABA and glutamate. In studies of modafinil as a stimulant were shown superior efficacy compared with amphetamines. To begin with, that the substance is supposed to have a much lower potential for abuse due to the fact that its effects do not cause the same euphoria. Moreover, the drug has minimal effect on peripheral CNS stimulation (i.e., showing less side effects), has a minimal effect on blood pressure without causing disruption of sleep (hangover or without need to “catch” sleep), and, according to clinical trials, has a more reliable safety profile. It is used even in the United States armed forces as an energy stimulant for pilots and soldiers required to operate for long periods of time without sleep. This is not as strange as it may seem at first glance, as in the past, military pilots and soldiers are widely used Dexedrine (amphetamine) during long periods of lack of sleep. Soldiers applying modafinil often report that the drug helps them to maintain excellent cognitive function for up to 40 hours without sleep, and has fewer side effects than Dexedrine. Modafinil has been tested in recent combat situations, such as Afghanistan and Iraq, and perhaps in the future will receive official recognition as a special preparation for the military. Modafinil recently gained popularity among competitive athletes. They use it not only as a preparation for the “courage”, and as a stimulant, increasing performance and endurance. Such use is likely to be a surprise for the developers of this drug, as it was reported earlier that the “soft” drug increases alertness does not have strong stimulatory effects, and can not improve athletic performance. Recent studies contradict these statements. A study in Canada found that taking modafinil may provide benefits expressed sports. In a double blind study 15 male volunteers had taken the drug at a dose of 4 mg per kg body weight (equivalent to 200 mg for a person weighing 220 pounds) or placebo. Three hours after the meal were performed aerobic exercise on a bicycle ergometer at 85% of maximal aerobic power, until exhaustion. Taking modafinil men could exercise over much longer periods of time (up to 30% longer) and used more oxygen intake during exercise. Also reported a reduction in the perceived tension, resulting in marked increase in performance during training.
Modafinil was developed by Lafon Laboratories in France. In 1998, the drug was approved by the FDA for sale in the United States, where it is sold under the brand name Provigil. Modafinil is also found in the international market for these and certain other trade names, including Modiodal, Vigil, Alertec and Modasomil. Although the drug has a favorable safety profile in the United States for some time, he was considered a drug that can provoke possible abuse. Modafinil is currently included in Schedule IV controlled substances, along with Valium and Xanax. Thus, its use in non-medical purposes is limited by significant legal penalties for possession and importation of the drug. The drug has a fairly wide medical use, including sleep disorders associated with changes in the operating mode. The drug is often prescribed on prescription. In 2000-2004 Modafinil has become popular among competitive athletes before sports regulatory authorities have not begun to show concern about the use of the drug. In 2004, broke the doping scandal involving the company VALCO, when it became known that many of the athletes, which gave a positive result in the use of tetragidrogestrinona also used and Modafinil. After this, the IOC forbids the use of modafinil, and through a series of research methodology has been developed to detect this chemical in the urine. Now this test is part of the standard screening athletes before the Olympic competition. Most other international sporting bodies have followed the example of the IOC ban and testing of modafinil. Since then, the drug has lost its appeal as an “invisible” in tests, although it is still used by many athletes, not passing urine sample testing.
Modafinil often supplied as tablets of 100 mg and 200 mg each.
Structural characteristics of
Modafinil is a central nervous system stimulant, close to adrafinilu. It has the chemical name of 2 [(diphenylmethyl) sulfinyl] acetamide.
Modafinil side effects
Modafinil side effects usually associated with the stimulation of the central nervous system and may include nervousness, insomnia, tremors, euphoria, personality changes and agitation. The drug can also cause gastrointestinal disturbances such as nausea, vomiting, abdominal pain, dry mouth, anorexia, and headache. There may also be high blood pressure, heart palpitations or abnormal heart rhythm. In rare cases, it may manifest allergic rash, increased alkaline phosphatase, or in violation of voluntary movements.
In clinical use for the treatment of excessive daytime sleepiness associated with narcolepsy or obstructive sleep apnea, the recommended dosage usually ranging from 200 to 400 mg per day. Dose may be taken once in the morning or in two divided doses (morning and noon). When used to improve physical performance, typical effective dosage is in the range of 100-400 mg. The drug is often mistaken for 2-3 hours before sporting events. Please note that side effects may depend on the dose. Often advised to start using modafinil at the lowest effective dose, and increase it to 50-100 mg for the reception to establish the optimum level. The scope of the drug are huge and, in fact, include any sports that focus on aerobic exercise and endurance. It is also excellent for athletes performing exercises for strength or speed in short intervals of repetitions (anaerobic exercise), such as shot put, pole vault and long jump. Modafinil is not popular drug of builders, since it does not directly affect the increase in muscle or reducing body fat. Some, however, believe that the drug is an effective stimulant pre-workout, especially during periods of fatigue or loss of physical activity after hard work or because of other reasons.
Modafinil is currently to be found in more than two dozen countries. The drug, however, is not particularly popular on the black market and is not a lucrative target for counterfeiting. Modafinil is sold by prescription.