Modafinil
Modafinil (Provigil, Alertec, Modavigil) is a wakefulness promoting agent (eugeroic) with nootropic effects used to enhance cognition, reduce fatigue, and increase alertness. It is approved by the United States' Food and Drug Administration for the treatment of obstructive sleep apnea, shift work sleep disorder, and narcolepsy. [1] However, studies have shown that Modafinil may also be useful off-label for alleviating the symptoms of Depression, [2], Bipolar Disorder, [3] Parkinson's Disease, [4] Seasonal Depressive Disorder, [5] ADHD, [6]and various other diseases which cause fatigue as a symptom.
Modafinil | |||||||||||||||||||||||||||||||||
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Chemical Nomenclature | |||||||||||||||||||||||||||||||||
Common names | Modafinil, Alertec, Modavigil, Modiodal, Provigil, Modalert | ||||||||||||||||||||||||||||||||
Substitutive name | Modafinil | ||||||||||||||||||||||||||||||||
Systematic name | 2-[(Diphenylmethyl)sulfinyl]acetamide | ||||||||||||||||||||||||||||||||
Class Membership | |||||||||||||||||||||||||||||||||
Psychoactive class | Stimulant / Eugeroic | ||||||||||||||||||||||||||||||||
Chemical class | Benzhydryl | ||||||||||||||||||||||||||||||||
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Hormonal Birth Control | |||||||||||||||||||||||||||||||||
CYP2C19-substrates |
The substance has also been used as a doping agent by various athletes due to its effects on physical stimulation. It has recently gained popularity for its use as a smart drug to improve memory and increase productivity.
Chemistry
Modafinil can be classed as a benzhydryl compound. This is where two benzene rings are both attached to a single carbon molecule.
Modafinil is classified as a sulphinyl benzhydryl molecule due to the sulphinyl, a sulphur molecule double-bonded to an oxygen molecule, attached to the carbon of the benzhydryl group. At the end of the chain is an amino acid group (an amine group attached to a carbonyl group). An amine is a nitrogen attached to hydrogen atoms, while a carbonyl is a carbon double-bonded to an oxygen.
Pharmacology
Research suggests that Modafinil increases hypothalamic histamine levels in the brains of rats, which may contribute to its locomotor effects. [7] Modafinil has recently been shown to act as an uptake inhibitor for the neurotransmitter dopamine, evidently leading to increased extraceullular concentrations of dopamine and dopaminergic neurotransmission. [8] This essentially allows dopamine to accumulate and be reused, causing physically stimulating and motivating effects.
Subjective effects
The effects listed below are based upon the subjective effects index and personal experiences of PsychonautWiki contributors. The listed effects will rarely (if ever) occur all at once, but heavier dosages will increase the chances and are more likely to induce a full range of effects.
Physical effects
The physical effects of Modafinil can be broken down into several components. These are described below and generally include:
- Stimulation - In terms of its effects on the user's physical energy levels, Modafinil is commonly considered to be stimulating and energetic, but can be considered as much less stimulating when compared to amphetamine. This stimulation encourages physical movement and activities such as running, playing sports, socializing, and/or exercising. The particular style of stimulation which Modafinil presents can result in jaw clenching, teeth grinding, or other involuntary movements comparable to that of traditional stimulants at high dosages, but are manifested much less consistently and intensely when compared to amphetamine or cocaine.
- Dehydration - Dehydration and dry mouth commonly occur due to an increase in motivation to engage in physical activities as well as an increased sense of focus which causes one to forget to drink water.
- Headaches - In terms of physical discomfort, Modafinil can cause headaches, especially if dehydrated, if you have not eaten food, or if you have been sitting in an awkward position for an extended period of time focused intensely on a task.
- Photophobia - Although uncommon, Modafinil can cause a temporary visual intolerance to light.
- Appetite suppression - The above components are also accompanied by a suppression of appetite which is usually much less intense in strength in comparison to the appetite suppression experienced with amphetamine.
- Diarrhea - Modafinil has the tendency to increase the frequency of bowel movements in certain individuals.
- Wakefulness
- Increased heart rate
- Dizziness
- Nausea
Cognitive effects
The cognitive effects of Modafinil can be broken down into several components. These are described below and generally include:
Toxicity and harm potential
Lethal dosage
The median lethal dose at which 50% of participants die (LD50) from Modafinil for human beings has never been reached. No life-threatening effects have taken place in clinical trials involving the administration of 1000mg to 1600mg of Modafinil per day for 7 to 21 consecutive days. Intentional acute overdoses of 4500mg and 4000mg in two adult subjects and an accidental injestion of 800mg by a three-year-old child did not result in any life-threatening effects or death. [9] After overdosing on 5000mg of Modafinil in a suicide attempt, a fifteen-year-old female reported a severe headache, nausea, and tachycardia, but did not appear to have any lethal or long-term effects. [10]
Tolerance and addiction potential
Although it is often used on a daily basis for extended periods of time, the long-term safety and effectiveness of modafinil have not been determined.[11] This substance does seem to have a tolerance and has been used by people for many months in a row with no noticeable side effects. Despite this, however, it does not seem to be addictive either.
Legal issues
Modafinil is legally approved for medical purposes worldwide. However, it is illegal to sell and possess in most countries without a prescription.
- United States: In the United States, Modafinil is a Schedule IV controlled substance. It is illegal to buy, sell, or possess the drug without a prescription or DEA license. [12]
- Canada: Modafinil is listed as a Schedule F prescription drug in Canada and it can be prescribed for human and veterinary use. [13]
See also
References
- ↑ Provigal (Manufacturer's Website) | http://www.provigil.com/
- ↑ Modafinil augmentation of selective serotonin reuptake inhibitor therapy in MDD partial responders with persistent fatigue and sleepiness | http://www.ncbi.nlm.nih.gov/pubmed/17729016
- ↑ A placebo-controlled evaluation of adjunctive modafinil in the treatment of bipolar depression | http://www.ncbi.nlm.nih.gov/pubmed/17671288
- ↑ Neuroprotective effects of modafinil in a marmoset Parkinson model: behavioral and neurochemical aspects | http://www.ncbi.nlm.nih.gov/pubmed/16940766
- ↑ PubMed - Modafinil treatment in patients with seasonal affective disorder/winter depression: an open-label pilot study | http://www.ncbi.nlm.nih.gov/pubmed/15306145
- ↑ Modafinil improves symptoms of attention-deficit/hyperactivity disorder across subtypes in children and adolescents | http://www.ncbi.nlm.nih.gov/pubmed/18280848
- ↑ European Journal of Pharmacology - Involvement of central histaminergic systems in modafinil-induced but not methylphenidate-induced increases in locomotor activity in rats | http://www.sciencedirect.com/science/article/pii/S001429990701031X
- ↑ The Journal of Pharmacology and Experimental Therapeutics - Evidence for the Involvement of Dopamine Transporters in Behavioral Stimulant Effects of Modafinil | http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2672878
- ↑ The National Library of Medicine - PROVIGIL | http://dailymed.nlm.nih.gov/dailymed/lookup.cfm?setid=fd75a8a7-a8ab-4141-9af9-989a220b9c19
- ↑ Journal of Clinical Sleep Medicine - Unsuccessful Suicide Attempt of a 15 Year Old Adolescent with Ingestion of 5000 mg Modafinilhttp://www.ncbi.nlm.nih.gov/pmc/articles/PMC2725258
- ↑ Pharmacotherapy for excessive daytime sleepiness | http://www.smrv-journal.com/article/S1087-0792(04)00024-3/abstract
- ↑ Placement of Modafinil Into Schedule IV - U.S. Department of Justice | http://www.deadiversion.usdoj.gov/fed_regs/rules/1999/fr0127.htm
- ↑ National Association of Pharmacy Regulatory Authorities - Regulations Amending the Food and Drug Regulations (1184 — Modafinil) | http://napra.ca/Content_Files/Files/FDR-Project1184-Modafinil-Oct122006.pdf