Modafinil - Wikipedia. Modafinil(R)- (−)- modafinil (armodafinil; top). S)- (+)- modafinil (bottom)Clinical data. Trade names. Provigil, others (see below)Synonyms. CRL- 4. 04. 76; Diphenylmethylsulfinylacetamide.

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AU: B3. US: C (Risk not ruled out)Dependenceliability. Psychological: Very low[1]Physical: Negligible[1]Addictionliability. Very low to low[2]Routes ofadministration. Oral (tablets)ATC code. Legal status. Legal status.

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Pharmacokinetic data. Bioavailability. Not determined due to the aqueous insolubility.

Protein binding. 62%Metabolism. Hepatic (primarily via amide hydrolysis; [3]CYP1.

A2, CYP2. B6, CYP2. C9, CYP2. C1. 9, CYP3. A4, CYP3. A5 involved [4]Biological half- life.

R- enantiomer),4 hours (S- enantiomer)[5]Excretion. Urine (8. 0%)Identifiers. CAS Number. Pub. Chem. CIDIUPHAR/BPSDrug. Bank. Chem. Spider.

UNIIKEGGCh. EBICh. EMBLECHA Info. Card. Chemical and physical data. Formula. C1. 5H1. NO2. SMolar mass. D model (JSmol)O=S(C(c.

CC(=O)NIn. Ch. I=1. S/C1. 5H1. 5NO2. S/c. H,1. 1H2,(H2,1. 6,1. YKey: YFGHCGITMMYXAQ- UHFFFAOYSA- N Y  (verify)Modafinil is a wakefulness- promoting drug used for treatment of disorders such as narcolepsy, shift work sleep disorder, and excessive daytime sleepiness associated with obstructive sleep apnea.[6] It has also seen widespread off- label use as a purported cognitive enhancer.

In English- speaking countries it is sold under the brand names Alertec, Modavigil, and Provigil. In the United States modafinil is classified as a schedule IV controlled substance and restricted in availability and usage, due to concerns about possible addiction potential. In most other countries it is a prescription drug but not otherwise legally restricted. Modafinil acts as an atypical, selective, and weak dopamine reuptake inhibitor which indirectly activates the release of orexinneuropeptides and histamine from the lateral hypothalamus and tuberomammillary nucleus, respectively, by unknown mechanisms, all of which contribute to heightened arousal.[7][8][9]. Modafinil tablets - Modalert 2.

Medical[edit]Modafinil is a eugeroic used for treatment of narcolepsy, shift work sleep disorder, and excessive daytime sleepiness associated with obstructive sleep apnea.[6][1. Because of the risk for development of skin or hypersensitivity reactions and serious adverse psychiatric reactions, the European Medicines Agency has recommended that new patient prescriptions should only be to treat sleepiness associated with narcolepsy.[1. Off- label use for fatigue[edit]Modafinil has also found off- label use with the neurological fatigue reported by some with multiple sclerosis.[1.

In 2. 00. 0, Cephalon conducted a study to evaluate modafinil as a potential treatment for MS- related fatigue. A group of 7. 2 people with MS of varying degrees of severity tested two different doses of modafinil and an inactive placebo over nine weeks. Fatigue levels were self- evaluated on standardized scales. Participants taking a lower dose of modafinil reported feeling less fatigued and there was a statistically significant difference in fatigue scores for the lower dose versus the placebo.

The higher dose of modafinil was not reported to be significantly more effective.[1. Modafinil is also used off- label to treat sedation and fatigue in many conditions, including depression,[1. Parkinson's disease.[2. Modafinil has been shown to improve excessive daytime somnolence and fatigue in primary biliary cirrhosis.[2. Occupational use[edit]Armed forces of several countries are known to have expressed interest in modafinil as an alternative to amphetamine—the drug traditionally employed in combat situations or lengthy missions where troops face sleep deprivation. The French government indicated that the Foreign Legion used modafinil during certain covert operations.[citation needed] The United Kingdom's Ministry of Defence commissioned research into modafinil[2. Qineti. Q and spent £3.

In 2. 01. 1, the Indian Air Force announced that modafinil was included in contingency plans.[2. In the United States military, modafinil has been approved for use on certain Air Force missions, and it is being investigated for other uses.[2. As of November 2. Air Force as a "go pill" for fatigue management.[2. The use of dextroamphetamine is no longer approved.[2.

The Canadian Medical Association Journal also reports that modafinil is used by astronauts on long- term missions aboard the International Space Station. Modafinil is "available to crew to optimize performance while fatigued" and helps with the disruptions in circadian rhythms and with the reduced quality of sleep astronauts experience.[2. Contraindications[edit]Allergy and hypersensitivity are the only contraindications of the drug,[3. Cephalon advises that it is important to consult a physician before using it, as problems may arise for people who are sensitive to constituents of the tablets, people with cirrhosis (which may impair the metabolism of the drug), and people with various cardiovascular problems.[citation needed]Adverse effects[edit]According to documentation distributed by Teva Pharmaceuticals, one- third of participants in clinical trials reported experiencing headaches; 1.

Rare occurrences have been reported of more serious adverse effects, including severe skin rashes and other symptoms that are probably allergy- related. From the date of initial marketing, December 1. January 3. 0, 2. 00.

US Food and Drug Administration received six cases of severe cutaneous adverse reactions associated with modafinil, including erythema multiforme (EM), Stevens–Johnson syndrome (SJS), toxic epidermal necrolysis (TEN), and DRESS syndrome, involving adult and pediatric patients. The FDA issued a relevant alert. In the same alert, the FDA also noted that angioedema and multi- organ hypersensitivity reactions have also been reported in postmarketing experiences.[3. In 2. 00. 7, the FDA ordered Cephalon to modify the Provigil leaflet in bold- face print of several serious and potentially fatal conditions attributed to modafinil use, including TEN, DRESS syndrome, and SJS. The long term safety and effectiveness of modafinil have not been determined.[3.

Modafinil may have an adverse effect on hormonal contraceptives for up to a month after discontinuation.[3. Addiction and dependence potential[edit]The addiction and dependence liabilities of modafinil are very low.[1][2][3. It shares biochemical mechanisms with addictive stimulant drugs, and some studies have reported it to have similar mood- elevating properties, although to a lesser degree.[3. Monkeys will self- administer modafinil if they have previously been trained to self- administer cocaine.[3. Although modafinil does not produce reinforcing effects in mice at doses that are equivalent to those used therapeutically in humans, it does do so at higher doses.[3. In accordance, although very rare, case reports of modafinil abuse exist.[3. As such, modafinil is classified by the United States FDA as a schedule IV controlled substance, a category for drugs with valid medical uses and low but significant addiction potential.[2][4.

Psychological dependence upon modafinil has only been noted in case reports involving daily overdoses on modafinil for an extended period of time.[1] Reported withdrawal symptoms include anhedonia, lethargy, anxiety, and insomnia.[1]Tolerance[edit]Large- scale clinical studies have found no evidence of tolerance with modafinil at therapeutic dosages even with prolonged use (for 4. Watch Strike A Pose Download Full. Overdose[edit]In mice and rats, the median lethal dose (LD5.

Oral LD5. 0 values reported for rats range from 1. Intravenous LD5. 0 for dogs is 3.

Clinical trials on humans involving taking up to 1.