Drug/Small Molecule:
modafinil

2D structure

Overview

Generic Names: modafinil
Trade Names: Dea No. 1680; Modafinil [Usan:Inn]; Modafinilo [Spanish]; Modafinilum [Latin]; Moderateafinil; Modiodal; Provigil; Sparlon
PharmGKB Accession Id: PA450530

Description

Modafinil is a stimulant drug marketed as a 'wakefulness promoting agent' and is one of the stimulants used in the treatment of narcolepsy. Narcolepsy is caused by dysfunction of a family of wakefulness-promoting and sleep-suppressing peptides, the orexins, whose neurons are activated by modafinil. The prexin neuron activation is associated with psychoactivation and euphoria. The exact mechanism of action is unclear, although in vitro studies have shown it to inhibit the reuptake of dopamine by binding to the dopamine reuptake pump, and lead to an increase in extracellular dopamine. Modafinil activates glutamatergic circuits while inhibiting GABA. (source: Drug Bank)

Indication

To improve wakefulness in patients with excessive daytime sleepiness (EDS) associated with narcolepsy. (source: Drug Bank)

ATC Therapeutic Category

  • N06BA:Centrally acting sympathomimetics

Pharmacology, Interactions, and Contraindications

Mechanism Of Action

The exact mechanism of action is unclear, although <i>in vitro</i> studies have shown it to inhibit the reuptake of dopamine by binding to the dopamine reuptake pump, and lead to an increase in extracellular dopamine. Modafinil activates glutamatergic circuits while inhibiting GABA. Modafinil is thought to have less potential for abuse than other stimulants due to the absence of any significant euphoric or pleasurable effects. It is possible that modafinil acts by a synergistic combination of mechanisms including direct inhibition of dopamine reuptake, indirect inhibition of noradrenalin reuptake in the VLPO and orexin activation. Modafinil has partial alpha 1B-adrenergic agonist effects by directly stimulating the receptors. (source: Drug Bank)

Pharmacology

Modafinil is a stimulant drug marketed as a 'wakefulness promoting agent' and is one of the stimulants used in the treatment of narcolepsy. Narcolepsy is caused by dysfunction of a family of wakefulness-promoting and sleep-suppressing peptides, the orexins, whose neurons are activated by modafinil. The prexin neuron activation is associated with psychoactivation and euphoria. Modafinil is not indicated for complaints of lack of energy or fatigue; but it appears to be very helpful for some patients. Also, it has been used in the treatment of hypersomnia, a disorder in which patients lack the capacity for meaningful sleep and may require ten or more hours per day. Recent studies have have found that modafinil may help recovering cocaine addicts fight their addiction. (source: Drug Bank)

Food Interactions

Take without regard to meals. (source: Drug Bank)

Absorption, Distribution, Metabolism, Elimination & Toxicity

Biotransformation

Hepatic (source: Drug Bank)

Protein Binding

60% (source: Drug Bank)

Absorption

Rapid following oral administration. (source: Drug Bank)

Isomeric SMILES Code:

C1=CC=C(C=C1)C(C2=CC=CC=C2)[S@](=O)CC(=O)N (source: Drug Bank)

The following genes are in curated knowledge about this drug.

  Gene Relationship Evidence
Phenotype data available Genotype Data Available Literature annotations available Has annotations
COMT
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  • PD
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Publications
No phenotype data Genotype Data Available Literature annotations available Not annotated
CYP1A2
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  • PK
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Publications
Phenotype data available Genotype Data Available Literature annotations available Has annotations
CYP2C19
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  • PK
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Publications
Phenotype data available Genotype Data Available Literature annotations available Not annotated
CYP3A
  •   
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  • PK
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Publications
Phenotype data available Genotype Data Available Literature annotations available Has annotations
CYP3A4
  •   
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  • PK
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Publications
Phenotype data available Genotype Data Available Literature annotations available Has annotations
CYP3A5
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  • PK
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Publications

A list of non-curated publications that mention this drug along with other genes is available.

Drug Targets

Gene Description
ADRA1B Uncurated Annotation (source: Drug Bank)
SLC6A3 Uncurated Annotation (source: Drug Bank)

The following drugs are in curated knowledge about this drug.

  Drug Relationship Evidence
No phenotype data No genotype data Literature annotations available Not annotated
ethinyl estradiol
  •   
  •   
  • PK
  •   
  •   
Publications
No phenotype data No genotype data Literature annotations available Not annotated
triazolam
  •   
  •   
  • PK
  •   
  •   
Publications

A list of non-curated publications that mention this drug along with other drugs is available.

Drug Interactions

Drug Description
clozapine Uncurated Annotation Modafinil increases the effect and toxicity of clozapine (source: Drug Bank)
cyclosporine Uncurated Annotation Modafinil decreases the effect of cyclosporine (source: Drug Bank)
ethinyl estradiol Uncurated Annotation Modafinil decreases the effect of the contraceptive (source: Drug Bank)
mestranol Uncurated Annotation Modafinil decreases the effect of the contraceptive (source: Drug Bank)
triazolam Uncurated Annotation Modafinil decreases the effect of triazolam (source: Drug Bank)

Curated Information

The following diseases are in curated knowledge about this drug.

  Disease Relationship Evidence
No phenotype data No genotype data Literature annotations available Not annotated
Narcolepsy
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  • PD
  •   
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  •   
Publications

Non-Curated Information

A list of non-curated publications that mention this drug along with other diseases is available.

Additional Datasets

These datasets are minimally curated and are sorted alphabetically by title.

  1. Genetic Variants in ADHD Stimulant associated Adverse Events

LinkOuts

Web Resource:
Wikipedia
DrugBank:
DB00745
KEGG Drug ID:
D01832
PubChem Compound ID:
4236
PubChem Substance ID:
188735

Common Searches

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Non-Curated Publications

A list of non-curated publications that mention this drug is available.

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