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A Cephalon-founded study in which patients were administered modafinil, methylphenidate, and a placebo found that modafinil produces "psychoactive and euphoric effects and feelings consistent with [methylphenidate]." [12] Like modafinil, armodafinil is an inhibitor and/or inducer of certain cytochrome P450 enzymes.
Chemical structure of modafinil. This page lists chemical compounds similar to modafinil, known as modafinil analogues and derivatives. These are structural analogues and derivatives of modafinil, a drug that affects dopamine levels in the brain in an unusual way (atypical dopamine reuptake inhibitor or DRI).
Modafinil is generally well-tolerated but can have potential risks and side effects. Common adverse effects of modafinil, experienced by less than 10% of users, include headaches, nausea, and reduced appetite. [93] [94] [20] Anxiety, insomnia, dizziness, diarrhea, and rhinitis are also reported in 5% to 10% of users. [20]
The drug has been found to block the dopamine transporter (DAT) by 83%, to a greater extent than methylphenidate without unfavorable concomitant adrenergic effects. [8] The drug is an atypical DRI similarly to modafinil. [11] [1] [9] The affinities for the DAT of flmodafinil's enantiomers and modafinil have also been studied.
Both enantiomers of modafinil preferentially bind to the DAT in an inward facing conformation that is associated with atypical dopamine reuptake inhibitor (DRI) profiles. [ 5 ] [ 6 ] Esmodafinil and armodafinil are said to have equipotent pharmacological effects but differing pharmacokinetics (see below).
Adrafinil acts as a prodrug of modafinil and hence shares its mechanism of action. [13] Certain other drugs acting as atypical DRIs with known or potential wakefulness-promoting effects include solriamfetol (also a norepinephrine reuptake inhibitor), [14] [15] vanoxerine, [16] phenylpiracetam, [17] [18] [19] and mesocarb.
Modafinil and its analogues are known to act as dopamine reuptake inhibitors and this is thought to be involved in their wakefulness-promoting effects. [1] Chemically, fladrafinil is a derivative of adrafinil (N-hydroxymodafinil) and is also known as bisfluoroadrafinil (it is the bis(4-fluoro) phenyl ring-substituted derivative of adrafinil). [1]
Interactions with other drugs, food and drink, and other factors may increase or decrease the effect of certain analgesics and alter their half-life. Because some listed analgesics are prodrugs or have active metabolites , individual variation in liver enzymes (e.g., CYP2D6 enzyme) may result in significantly altered effects.
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