4- Modafinil

The mode of action of modafinil, a new arousal-promoting compound used in the treatment of sleepiness associated with narcolepsy, is not fully understood. 

It has been suggested that modafinil increases wakefulness by activating ai noradrenergic receptors or hypothalamic cells that contain the peptide hypocre-tin [3], or that it may act by modulating the GABAergic tone that might lead to an increased dopamine release in the nucleus accumbens. On the other hand, modafinil does not have any effect in DAT knockout mice. 

Modafinil 400 mg is prescribed. The drug is available in 200-mg tablets. The nurse administers. ... 

C 3H,20 91-01-0) see Adrafinil Modafinil benzhydroximic acid chloride (C7H C1N0 698-16-8) see Imolamine Oxacillin benzhydryl bromide... 

C2H3CIO2 79-11-8) see Acediasulfone Acefylline Adrafinil Adrenalone Carbocisteine Diodone Mefexamide Methoxsalen Modafinil Nitrofurantoin Pifoxime Praziquantel Propyliodone... 

Amantidine, bromocriptine, mazindol, pergolide, cabergoline, L-dopa/carbidopa, pramipexole, ABT-431, catecholamine metabolism inhibitors (disulfiram, phenelzine, selegiline), amineptine Methylphenidate, /-amphetamine, tropanes, GBR-12909 (partial agonist that may also act as antagonist), modafinil, coca tea... 

Amantadine 100 mg orally every morning and early afternoon Modafinil 200 mg orally daily Second-line therapies ... 

Administer the ESS at each visit to monitor progress with modafinil or stimulant therapy. Unfortunately, EDS in narcolepsy patients rarely is fully reversed. 

Modafinil Increase metabolism of COCs Decrease efficacy of COCs alternative method of contraception is recommended... 

Ferraro, L., Antonelh, T., TanganeUr, S. et al. (1999). The vigilance promoting drug modafinil increases extracellular glutamate levels in the medial preoptic area and the posterior hypothalamus of the conscious rat prevention by local GABAA receptor blockade. Neuropsychopharmacology 20, 346-56. 

Wesensten, N. J., Killgore, W. D. Balkin, T. J. (2005). Performance and alertness effects of caffeine, dextroamphetamine, and modafinil during sleep deprivation./. Sleep Res. 14 (3), 255-66. 

Scammell, T. E., Estabrooke, 1. V., McCarthy, M. T. et al. (2000). Hypothalamic arousal regions are activated during modafinil-induced wakefulness. /. Neurosci. 20,... 

Willie, J. T., Renthal, W., Chemelli, R. M. et al. (2005). Modafinil more effectively induces wakefulness in orexin-null mice than in wild-type littermates. Neuroscience, 130, 983-995. 

Some CNS stimulants have an effect on the same systems that are involved in wakefulness, including glutamate-, NE-, DA-, 5-HT-, histamine-, hypocretin- and ACh-containing neurons. This group includes molecules such as cocaine, amphetamine, and nicotine. The sleep-promoting systems are concentrated in the medial part of the brainstem, dorsal reticular substance of the medulla, anterior hypothalamus, and basal forebrain (Jones 2005). Other stimulants, such as caffeine and theophylline, block some sleep-inducing mechanisms. Modafinil is also a CNS stimulant with an unknown mechanism of action. 

Akaoka H., Roussel B., Lin J. S., Chouvet G., Jouvet M. (1991). Effect of modafinil and amphetamine on the rat catecholaminergic neuron activity. Neurosci Lett. 123, 20-2. 

Engber T. M., Koury E. J., Dennis S. A. et al. (1998). Differential patterns of regional c-Fos induction in the rat brain by amphetamine and the novel wakefulness-promoting agent modafinil. Neurosci. Lett. 241, 95-8. 

Lin J. S., Hou Y., Jouvet M. (1996). Potential brain neuronal targets for amphetamine-, methylphenidate-, and modafinil-induced wakefulness, evidenced by c-fos immunocytochemistry in the cat. Proc. Natl. Acad. Sci. USA 93, 14128-33. 

Mignot E., Nishino S., Guilleminault C., Dement W. C. (1994). Modafinil binds to the dopamine uptake carrier site with low affinity. Sleep 17, 436-7. 

A derived crystal packing model proved to be useful in resolving the crystal structure of a metastable polymorph of racemic modafinil, where details of the solved crystal structure of one polymorph was used as a basis for developing the structure of the other [12]. It was found that the calculated XRPD pattern matched well with the experimental data, indicating the correctness of the analysis. The powder diffraction of two polymorphs of chlorothalonil were solved to obtain... 

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