Modafinil (CAS No. 68693-11-8) is a medicine which stimulates central nervous system and is used commonly in conditions which lead to excessive daytime sleepiness. These conditions may include shift work sleep disorder usually encountered in shift workers working outside the normal schedule, narcolepsy related fatigue experienced during daytime and obstructive sleep apnea in combination with continuous positive airway pressure (CPAP).
The primary mechanism of action of modafinil is not very clear but it is known to be inhibiting the dopamine reuptake, hence increasing its concentration in blood which is a stimulant itself and well known as ‘happy hormone’. It has also been observed that it increases the concentrations of nor-epinephrine and serotonin in the prefrontal cortex and hypothalamus which can be due to indirect effect of increased dopamine. All these hormones and neurotransmitters are considered as stimulant, thereby making modafinil as wakefulness promoting agent.
Modafinil is readily absorbed orally, and it is available as 100mg and 200mg oral tablets. For adults, it is recommended to take 200mg orally once a day in the morning for the treatment of narcolepsy or obstructive sleep apnea and one hour before the start of the work shift for treatment of shift work disorder. Modafinil is not approved to be used in pediatric population because its efficacy and safety in this age group has not been established yet.
Modafinil is generally well-tolerated medicine with extremely rare serious adverse events. Commonly experienced adverse events are very mild including headache, nausea and decreased appetite which have been observed in less than 10% of the users. Few other adverse effects may include anxiety, insomnia, dizziness, diarrhea, and rhinitis. Although it is a safe drug but if any patient experiences any rare serious rash including Stevens-Johnson syndrome, it should be discontinued at the same time.
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Flmodafinil (CAS No. 90280-13-0) also known as bisfluoromodafinil, lauflumide, CRL-40,940, N-deshydroxyl Fladrafinil and bis-(p)-fluoromodafinil is a new medicine which promises advantages over Modafinil. Its structure is almost identical to Modafinil with addition of just two fluoride atoms. This small change in structure has led to increased effectiveness by almost four times, longer duration of action as well as minimal adverse effects as compared to Modafinil. Similar to Modafinil, it is also used as wakefulness-enhancing agent in conditions leading to excessive daytime sleepiness. Since it is fairly a new drug, so, it is being studied in clinical trials for its use in narcolepsy and other sleep disorders. There are some potential benefits observed with Flmodafinil like increasing attentiveness in subjects with fatigue and counteracting harmful effects related to sleep deprivation, may also improve learning skills and recall in healthy as well as patients dealing with depression. Some evidence from the animal studies have shown that Flomodafinil can be used as mood booster and can help in increasing concentration in heathy or sleep deprived subjects.
Being bisfluoro analogue of modafinil, its mechanism of action is similar to modafinil and acts by inhibiting the reuptake of dopamine leading to increased concentration of dopamine. It should be started at fairly low dose of 12.5mg to 25mg in beginners and around 100mg for not more than 2-3 times in a week in subjects who have already taken Modafinil in the past. Dose of 150mg or more is generally nor recommended as it may lead to side effect of insomnia but some users use it to stay awake all night.
Because of the fact that it is relatively a new medicine and still undergoing several clinical trials, its spectrum of adverse events is not well known, but it has been claimed that this medicine will have fewer and milder adverse events as compared to Modafinil. This notion has been backed up by anecdotal reports obtained from subjects who took both Modafinil and Flomodafinil as part of the research. Also, keeping in structure similarity of Flomodafinil and Modafinil, their range of side effects would be quite similar like headache, anxiety, gastrointestinal issues.
Bromantane or NP-160 (CAS No. 87913-26-6) comes under the class of actoprotector which increases not only mental but physical work capacity without any increase in oxygen consumption or production of heat. It also has antiasthenic properties which contribute to increase in working capacity which is often inhibited by hypoxia and hyperthermia. In addition, it is found to have both stimulative as well as anxiolytic effects, thus increasing physical ability in addition to the intellectual working capacity. It improves the learning process, coordination of movements and exhibits neuropsychoactivation effect because of which Bromantane is also referred as psychomotor stimulant. There is another use of Bromantane in increasing the immunity even with a single dose by exerting its antiradical and membrane protective properties and increasing the B cells and immune complexes in the blood. Bromantane is useful for people who want to increase their cognitive performance, energy levels, and physical endurance. It has also been useful to enhance libido.
The mechanism of action of bromantane is obtained through increasing the activity of the lower centers of the central nervous system through dopaminergic system and increasing the circulating concentration of dopamine without any action on noradrenergic mediators. Bromantane may also act through strengthening of GABA-ergic mediation by supervising the synthesis of GABA-transporters. It is well absorbed orally and very quickly in women as compared to men and stays in the body for a considerable period of time because of its slow elimination. It is available in capsule as well as powder form and should be started from low dose of 25mg. The starting dose is higher (50mg) for women as it is metabolized quickly in females.
As far as its safety is concerned, almost no side effects are observed with therapeutic doses of Bromantane. It does not have nay addictive potential. Higher doses of Bromantane have shown toxic reactions in animal experiments and few subjects have reported brain fog and fatigue with higher doses.
Sunifiram or DM-235 (CAS No. 314728-85-3) is an experimental medicine which is a piperazine alkaloid derived from Piracetam that can potentially boost memory retention, speed up the learning process, and enhance recall. It is also observed from anecdotal evidence from subjects that it potentiates the process of learning, focus, cognitive ability and understanding. It has been proved in animal experiments that Sunifiram can reverse the amnesia which is produced by certain chemicals. Therefore, it is suitable for treatment of amnesia in humans including neurological conditions like Alzheimer’s and Parkinson’s disease.
The mechanism of action of Sunifiram is not fully understood but it may act by stimulating the release of acetylcholine as it has been observed in experiment that it opposed the effects of scopolamine which blocks acetylcholine release. It may also act by promoting the release of glutamate which is an excitatory neurotransmitter, that furthers increased the functioning of NMDA receptors to which glutamate binds to enhance the synaptic plasticity.
The official information regarding the dose of Sunifiram is unavailable but according to the information obtained from subjects who have been taking this medicine, dose of 5-10mg is considered as appropriate. It can also be taken sublingually for quick onset of action as it is directed absorbed into the bloodstream. It is recommended to start with the lower dose and then titrate according to the required level of effects.
Sunifiram is considered as a safe drug which is well tolerated with no serious side effects reported with this medicine. Few of the mild side effects observed by some users are headache, insomnia, increase in body temperature, perspiration and salivation, blocked nose and mental sluggishness. These side effects are dose related and observed when dose is increased. It has been seen that taking Sunifiram later in the day decreases the incidence of insomnia and headaches can be avoided by concomitant use of choline along with Sunifiram.
Noopept or N-Phenylacetyl-l-prolylglycine ethyl ester or GVS- 111 (CAS No. 157115-85-0) belongs to racetam family of nootropic compounds and is similar in action to Piracetam but is almost 1000 times more potent than Piracetam. This medicine is used as a neuroprotective which improves memory, cognition and overall brain health. It also exerts anxiolytic effect boosting mood and lowering anxiety. The subjects who have used Noopept have reported that they found it useful as a study aid, increase focus, improve mood and to potentiate long term memory. It has been observed that Noopept increases the ability to both form and retain memory.
This new medicine modulates the functioning of neuroreceptors by keeping glutamate and acetylcholine levels, hence, protecting the neurons from damage by glutamate. This leads to enhancement in cognition, mood, learning, memory, recall and relieve anxiety. It also modulates AMPA and NMDA receptors boosting the level of cycloprolylglycine in the brain. Noopept helps in neuroplasticity by increasing Nerve Growth factor (NGF), mRNA and Brain-derived Neurotrophic factor (BDNF). This mechanism is particularly helpful in patients with neurodegenerative diseases like Parkinson’s or Alzheimer’s disease. In animal experiments, it was depicted that Noopept stimulated learning with just single administration.
Noopept is available in tablet, capsule and powder form. The recommended dose of Noopept is around 10-30 mg/ day. It has good bioavailability and can easily cross blood brain barrier to reach the brain. It can be taken sublingually to have quick onset of action.
Noopept is well tolerated and considered as safe drug within the recommended dosage. Adverse effects are very rare and usually seen with increase dosage of Noopept. These may include fatigue, headaches, insomnia or gastrointestinal discomfort. To decrease the incidence of headache, the subject can combine Noopept with choline supplement as headaches usually arise from deficiency of choline.
Mebicar or Temgicoluril or Adaptol or tetramethylglycouril (CAS No. 10095-06-4) is a non-benzodiazepine transquilizer which is used as an anxiolytic medication. It is primarily used in prevention as well as treatment of anxiety, emotional stress, irritability and excitement. It also potentials the effect of transquilizers and helps in normalization of the sleep disturbances but it doesn’t have its own direct hypnotic effect. It is also found to be effective in the treatment of alcohol withdrawal and smoking cessation. There is evidence that it can help in cardialgias which are not associated with cardiovascular disorders. It can also be useful for prophylaxis of stressful conditions.
Due to similarity in structure of Mebicar with the metabolites in human body, it doesn’t interact with oxidising or reducing agents, acids or alkali. It exerts its action on all four major neurotransmitters including acetylcholine, serotonin, adrenaline and nor-adrenaline as well as γ aminobutyric acid (GABA). Mebicar exerts its major action on limbic-reticular complex and particularly hypothalamus. It also improves blood flow to brain and increases both physical and mental ability to work. Mebicar is well absorbed orally and adult dosage is 300-500 mg 2-3 times per day. The total dose should not be more than 10 gm per day and the highest single dose should not exceed 3 gm. To help the patient get rid of smoking, the dose should be 600-1000mg per day for 5-6 weeks. Dosage adjustment is not required in the elderly as well as patients with liver disease. Mebicar is not well studied in pediatric population, hence is contraindicated in children and adolescents below 18 years of age.
Side effects with Mebicar are usually rare and seen with higher doses only. Common side effects reported are dizziness, decrease in blood pressure, weakness, low body temperature, gastrointestinal disorders and allergic reactions. If the subject experience any allergic reaction with the use of Mebicar, then it should be discontinued.
L-dopa or levodopa or l-3,4-dihydroxyphenylalanine (CAS No. 59-92-7) is a medicine which is in the market for decades for its use in Parkinson disease. Levodopa is actually a precursor to dopamine and because of the deficiency of dopamine in Parkinson’s disease, it is used as replacement therapy. It is the most common and most effective medication which is used to improve the quality of life in such patients especially the one with idiopathic cause. It also most effectively deals with the bradykinetic symptoms. It is not used as a first line agent in Parkinson disease but it becomes rather important to prescribe this medication once the symptoms are not controlled by other anti-Parkinson medications. Recent studies have shown that the progression of Parkinson’s disease can be slowed down by L-dopa and benefits are observed even after the cessation of this drug. L-dopa is also used in off-label indications of restless leg syndrome and periodic limb movement in sleep.
In Parkinson’s disease, there is disruption of nigrostriatal pathway which eventually leads to decrease in dopamine levels. Levodopa coverts to dopamine in the body in both central nervous system and periphery. It if often prescribed along with peripheral decarboxylase inhibitors like carbidopa to prevent its conversion to dopamine in the periphery, which leads to more levodopa crossing the blood brain barrier and exerting its effect on postsynaptic dopaminergic receptors. L-dopa should be initiated at the dose of 25 mg to 100 mg orally thrice a day immediately after meals. It is recommended to increase the dose by 50-125 mg every day until the optimum dosage for that patient is reached. Usually, the maintenance dose is 250-500 mg thrice daily to be taken immediately after meals.
Common side effects observed with L-dopa are dizziness, headache, nausea and somnolence. The dose of carbidopa should be increased to get relief from nausea and even after that, if nausea persists, then domperidone can be given to the patient. Central nervous side effects are mostly encountered in elderly patients taking levodopa which includes hallucinations, delusions, agitation, confusion and psychosis. The dose reduction or abrupt withdrawal of L-dopa can increase the risk of neuroleptic malignant syndrome. If it occurs, L-dopa should be started at the previous doses with supportive care in hospital settings.
