Adrafinil is an awakeness enhancer that was originally designed as a prescription medicine for narcoleptics. It became replaced by modafinil. Both adrafinil and modafinil are excellent for alertness and vigilance, but also have several side benefits. Adrafinil, by the way, metabolizes into modafinil through liver-pass metabolism. Modafinil was developed by French manufacturers of pharmaceuticals Cephalon. When it was found modafinil was the active metabolism in adrafinil modafinil swiftly replaced adrafinil in prescription usage.
Modafinil has some benefits over adrafinil. Since it doesn’t have to be metabolized it poses much less of a risk to the liver. Certain unwanted peripheral effects have also been noted in modafinil and since there’s some loss in metabolism the dosage on adrafinil is of necessity greater. Both modafinil and adrafinil are classed as eugregorics or “good energizers.” They earn this title through the fact that they enhance alertness and awakeness without the stimulation experienced when you use traditional stimulants like coffee.
Coffee’s “wakefulness” effect is due to the fact that the caffeine molecule is very similarly shaped to that of the neurotransmitter adenosine. Adenosine is released when work has been exerted and is a sign to the body and brain that we’re tired. When caffeine is introduced to the system it takes up the spot for adenosine, blocking it and its effects. Traditional stimulants like methylphenidate (Ritalin) or amphetamines like Adderall are both psychostimulants as well as CNS (central nervous system) stimulants and can be taxing for the heart, negatively affect blood pressure and have other notable failings like “the crash.”
OFF LABEL USE OF ADRAFINIL
A military study of helicopter pilots revealed modafinil to work as well as 20mg of dextroamphetamine as far as improving alertness and “countering the debilitating mood and cognitive effects of sleep loss during sustained operations[.]” Research into “off-label” uses for modafinil extend beyond merely improving helicopter pilots endurance. Since the 90’s a number of clinical studies have been published. Therapeutic applications of modafinil beyond that of narcolepsy include discussion of fatigue, ADHD, clinical depression, Parkinson’s and related illness, medication related fatigue, chronic fatigue, negative or “flattened” affect in schizophrenia, obesity and even cerebral palsy and cocaine addiction.
Modafinil has a similar cognitive enhancing potential to caffeine, methylphenidate and amphetamines, and are considered focusing agents. A randomized double-blind clinical trial comparing methylphenidate and modafinil “was found to improve attention for a well-rested individual, while maintaining wakefulness, memory and executive functions to a significantly higher degree in sleep deprived individuals than did a placebo. “
Executive function is just one aspect of focus and cognition. Executive function is involved in difficult or complex tasks. A study regarding “sustaining executive function” modafinil was tested against caffeine and dextroamphetamine. The results of the study suggested different stimulants had a tendency to improve different aspects and areas of focus and cognition. Modafinil, caffeine and dextroamphetamine had different areas they improved. Depending on “the cognitive demands of the task” different interventions proved more useful and effective. According to the study, “the modafinil group demonstrated greater deliberation before making a move” in comparison with the other stimulants utilized in the study.
The test found that “the modafinil group demonstrated greater deliberation before making move” in comparison with the other stimulants in the study. According to multiple studies, modafinil (and by extension, its parent compound adrafinil) would be an excellent adjunctive (or perhaps even primary) intervention in certain cases of treatment resistant conditions ranging from bipolar and clinical depression to schizophrenia.
The body of evidence presented at least tentatively suggests that modafinil would present, in some cases, an excellent adjunctive or even primary medical intervention, especially in some otherwise treatment resistant existing conditions. From bipolar, to depression, and even treatment resistant schizophrenia.
Lethargy, fatigue (from multiple sources ranging from medication to depression) are especially well treated by modafinil and adrafinil. There are multiple possible roots to serious, pathological fatigue. In addition to this fatigue can have a complex interplay with other conditions, either exacerbating, being exacerbated by or both. Energy level is tied to mood, physical performance and even pain perception. The full mechanics behind this is still something of a mystery for now. Lethargy and lack of energy can be caused by depression or vice versa. Depression and lethargy exacerbate fatigue as well. Depression itself has been shown to amplify pain perception. In certain cases, it’s a tricky riddle of the chicken and the egg. Patients living with chronic pain may be especially sensitive to the effects of lethargy and depression.
Sleep and wakefulness are inextricably bound to mood and in just as mysterious a manner. Modafinil increases monoaminergic neurotransmitters and histamine. Histamine can be involved not only with allergic reactions but with energy levels and wakefulness. This is why most OTC and other drugs that operate on the histaminic pathways are either sedating or energizing. SSRI’s (selective serotonin reuptake inhibitors) are a commonly prescribed anti-depressant that is effective for a large portion of depression sufferers. For this reason, the “serotonin hypothesis” of depression has become somewhat accepted. Certain “resistant” forms of clinical depression may be related to deficiency of other neurotransmitters such as norepinephrine (NE) and dopamine(DA). Histamine itself is closely related to norepinephrine, adrenaline and certain endorphins. “Brain circuits determine destiny in depression: a novel approach to the psychopharmacology of wakefulness, fatigue and executive dysfunction in major depressive disorder” was a study published in the Journal of Clinical Psychiatry. It put forth the findings that “fatigue in obstructive sleep apnea may be driven by depressive symptoms rather than by apnea severity, so the actions of modafinil in relieving fatigue in both obstructive sleep apnea and depression may be due to a common action on a common neurotransmitter in a common pathway. ” Equally interesting, as far as modafinil and adrafinil’s anti-depressant potential goes are the researchers findings that “neuropharmacological profile is distinct from that of antidepressants and that of stimulants and predicts potential actions in relieving not only sleepiness but also fatigue and executive dysfunction in MDD without substantial abuse potential.”
And there’s the rub, “without addiction potential.” Unlike traditional ADHD drugs, modafinil and adrafinil are far less likely to lead to tolerance, withdrawal, and addiction or abuse. That being said, it’s always best to consult with your doctor before undergoing any new diet, fitness or supplementation regimen, especially if you’re currently taking any over the counter or prescription medications for an existing condition. Modafinil is a prescription drug in many countries, so check with the laws of this and other compounds before attempting to purchase them. If modafinil is not available, adrafinil may be a good substitute, but remember not to co-ingest with alcohol and steer clear if you have any liver related conditions.