Drug Index

Modafinil

Mechanism :

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 found that modafinil may help recovering cocaine addicts fight their addiction.


Indication :

  • Excessive sleep disorders caused by sleep apnea.
  • Narcolepsy
  • Shift work sleep disorder.

Contraindications :

Hypersensitivity; Caution in mania, psychosis, hepatic impairment, MI, Left ventricular hypertrophy, mitral valve disease


Dosing :

Obstructive sleep apnoea, Narcolepsy:
>16 years: 200 mg orally, in the morning. Max: 400 mg.

Adverse Effect :

Serious Reactions: Anaphylaxis, angioedema, hypersensitivity reaction, Stevens-Johnson syndrome, toxic epidermal necrolysis, drug rash with eosinophilia, syncope, hypertension, arrhythmias, mania, psychosis, suicidal ideation, dependency, abuse.

Common Reactions: Headache, rhinitis, decreased appetite, nausea, abdominal pain, nervousness, dyspepsia, anorexia, xerostomia, chest pain, tachycardia, palpitations, vasodilation, elevated ALT/AST, paresthesia, depression, constipation, somnolence.


Interaction :

Carisoprodol: Strong CYP2C19 inhibitors such as modafinil may decrease the metabolism of CYP2C19 substrates such as carisoprodol. Consider an alternative for one of the interacting drugs in order to avoid toxicity of the substrate. Some combinations are specifically contraindicated by manufacturers. Suggested dosage adjustments are also offered by some manufacturers. Please review applicable package inserts. Monitor for increased effects of the CYP substrate if a CYP inhibitor is initiated/dose increased, and decreased effects if a CYP inhibitor is discontinued/dose decreased.
Clozapine: Modafinil increases the effect and toxicity of clozapine.
Cyclosporine: Modafinil decreases the effect of cyclosporine.
Ethinyl Estradiol: Modafinil may decrease the contraceptive effect of ethinyl estradiol. Hormonal contraception should not be solely relied on during concomitant therapy with modafinil.
Mestranol: Modafinil decreases the effect of the contraceptive.
Roflumilast: Affects CYP1A2 metabolism; decreases level or effect of roflumilast.
Telithromycin: Telithromycin may reduce clearance of Modafinil. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Modafinil if Telithromycin is initiated, discontinued or dose changed.
Triazolam: Modafinil decreases the effect of triazolam.
Trimipramine: The strong CYP2C19 inhibitor, Modafinil, may decrease the metabolism and clearance of Trimipramine, a CYP2D6 substrate. Consider alternate therapy or monitor for changes in therapeutic and adverse effects of Trimipramine if Modafinil is initiated, discontinued or dose changed.
Voriconazole: Voriconazole, a strong CYP3A4 inhibitor, may increase the serum concentration of modafinil by decreasing its metabolism. Monitor for changes in the therapeutic and adverse effects of modafinil if voriconazole is initiated, discontinued or dose changed.



Renal Dose :

Dose in Renal Impairment GFR (mL/min)
20-50Dose as in normal renal function
10-20Dose as in normal renal function
<10Start at 50% normal dose and increase according to response

Dose in Patients undergoing Renal Replacement Therapies
CAPDUnknown dialysability. Dose as in GFR<10 mL/min
HDUnknown dialysability. Dose as in GFR<10 mL/min
HDF/High fluxUnknown dialysability. Dose as in GFR<10 mL/min
CAV/VVHDUnknown dialysability. Dose as in normal renal function

Hepatic Dose :

Moderate to severe hepatic impairment: Reduce dose by 50% in patients.
08/26/2024 22:50:11 Modafinil
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