Modafinil is an alertness-promoting agent mainly for the treatment of sleep disorders-namely, narcolepsy, obstructive sleep apnea, and shift work disorder. It is used in off-label prescripÂtion, as a cognitive enhancer, following the popular report of the attainment of increased concentration, alertness, and clarity by the user of the medicine.
Such preparations go by brand names like Provigil. A Schedule IV controlled substance in the United States, since it does have some potential for abuse, though much lower than the levels found with drugs such as amphetamines and methylphenidate.
What Is Modafinil Used For
Modafinil can be used in both humans and animals. Primarily, this drug is prescribed for the minimization of severe sleeping disorders. Besides, this is also utilized to avoid the condition of stopped breathing problems at the time of sleep. Certain students and working individuals take this medication to remain alert during working hours and maintain a regular cycle of sleep. It is also used in the treatment of:
- Obstructive Sleep Apnea: Obstructive sleep apnea patients often experience “sleep fractured” into pieces, leading to excessive daytime somnolence. Modafinil may be prescribed for excessive daytime sleepiness but does not address the root sleep disorder.
- Shift Work Sleep Disorder (SWSD): Irregular shifts, especially night shifts, interfere with the sleep-wake cycle of an individual and cause excessive daytime sleepiness and impaired cognitive functioning. Modafinil may reduce symptoms during the early stages of SWSD, and thus help them to better perform and stay alert during shifts.
Modafinil is also at times prescribed as an off-label medicine for the treatment of ADHD, depression, and some symptoms linked to multiple sclerosis, yet these applications are not approved.
Modafinil Mechanism of Action
The exact mechanism through which the drug modafinil promotes wakefulness and improves cognitive functions remains unclear. Nonetheless, research has given some crucial insight into how it might work within the brain. The primary mechanism through which modafinil acts is by affecting the brain’s neurotransmitter systems, including dopamine, norepinephrine, histamine, and orexin.
- Dopamine: It inhibits DAT- which removes dopamine from the synapse, creating increases in dopamine in the brain, hence causing a light, extended activation of dopamine with special effects found within certain areas of the brain that regulate attention and arousal, such as the prefrontal cortex.
- Orexin (Hypocretin): Orexin is a neuropeptide that plays a very significant role in the regulation of wakefulness and the sleep-wake cycle. It has been commonly believed that the modulation of orexin signaling enhances alertness and then reduces sleepiness.
- Histamine: Another neurotransmitter, histamine, is found to be associated with wakefulness, and the stimulating effect of modafinil is presumed to be because of an increase in the activity level of histamine within the brain.
- Norepinephrine: Modafinil increases endogenous neurochemical norepinephrine, and this is a crucial function in both the response to stress and arousal in the brain. This may account for why modafinil could improve attentional functions.
Modafinil Dosage: Guidelines and Considerations
Modafinil is a prescription medication primarily to promote wakefulness in individuals suffering from sleep disorders like narcolepsy, obstructive sleep apnea (OSA), and shift work sleep disorder (SWSD). The typical dose of modafinil is usually based on the condition being treated, the response of the patient to the medication, and other individual considerations. Some general modafinil dosages and important considerations are described below.
Dosage for Narcolepsy
For the treatment of narcolepsy, the objective would be the control excessive daytime sleepiness so that patients are awake and alert for most of the day.
- Standard Dosage: at Start, The standard initiating dose is 200 mg a day. This dose should be given once daily in the morning.
- Maintenance Dose: If the patient’s response to the drug is satisfactory, then the dose can be further increased to as much as 400 mg per day. Most patients are well taken care of with only 200 mg daily, but some may require more.
- Maximum Dose: 400 mg a day.
Dosage for Obstructive Sleep Apnea (OSA)
The drug is administered for sleep apnea patients with daytime hypersomnia in the setting of persistent and stabilized disease when there is continuous positive airway pressure.
- Standard Dosage: The typical dose is usually started at a dosage of 200 mg/d and may be given once a day in the morning.
- Dosage adjustments: If the first dose is not sufficient to control daytime somnolence, the dose can be raised to 400 mg a day.
- Max Dose: Like the case of narcolepsy, the maximum tolerated dose for the treatment of OSA is 400 mg per day.
Dosage for Shift Work Sleep Disorder (SWSD)
Modafinil will increase alertness among shift workers with sleep disorders when they are at work, especially when these workers often work night shifts or rotating shifts that do not fit the worker’s regular sleep schedule.
- Standard Dose: 200 mg; It should be administered one hour before the start of the work shift. This way, the employee will be able to stay awake and alert during his shift, particularly during periods when he would have been sleeping anyway.
- Dose titration: Most patients respond to 200 mg but, if not so, the dose is escalated to 400 mg. Any higher doses than these are often not suggested for this condition’s treatment.
Dosage for Off-Label Uses
- Some off-label uses include ADHD, depression, and fatigue related to multiple sclerosis, but the dosages for these uses are all over the board and not FDA-approved.
- No standard dosage has been established for cognitive enhancement (for example, in healthy individuals), as modafinil is not officially approved for this use; anecdotal reports cite a range of 100-200 mg/day for common usage. These uses, of course, are lacking in adequate clinical evidence, and long-term safety and efficacy for cognitive enhancement are not established.
Common Side Effects Of Modafinil
Side effects of Modafinil are common in patients. Some side effects affect patients in minor and some get affected with serious side effects. It varies from person to person. So, it is important to follow the doctors’ instructions one by one. Let’s have some knowledge that, of what types of side effects you may face after taking Modafinil.
- Common Side Effects: Headache, sleeplessness, nervousness, dizziness, constipation, diarrhea, gas, dry mouth, strange tastes, etc
- Serious Side Effects: Depression, suicidal tendencies, palpitations, chest pain, allergic reaction, breathing disorder, itching, excessive thirst, eye pain, difficulty, blurred vision, etc
Modafinil Interaction
Modafinil interacts with many drugs, reducing their effect or even increasing the chances of producing side effects.
- CYP450 Enzymes: Modafinil is a CYP3A4 inducer. It lowers the effect of CYP3A4 drugs, such as oral contraceptives, some anticonvulsants like phenytoin and carbamazepine, triazolam antidepressants, simvastatin statins, and other immunosuppressants, including cyclosporine. These require a dose adjustment.
- CYP450 Inhibitors: Patients taking ketoconazole, ritonavir, and clarithromycin, as CYP3A4 inhibitors, may result in increased levels of modafinil in the blood. This can lead to exacerbation of side effects such as insomnia or anxiety.
- Stimulants: Combination of other stimulants like amphetamine or methylphenidate with modafinil may increase cardiovascular side effects and raise heart and blood pressure, or enhance anxiety and nervousness.
- Anticoagulants: Modafinil might interact with other anticoagulants like warfarin and alter their functioning; it is essential to check clotting parameters more often, or INR.
- Antipsychotics/Antidepressants: The following antipsychotics and antidepressants may interact with modafinil by either elevating or lowering their blood levels in a manner that can influence efficacy or cause side effects
High-risk drug interactions Patients should always inform their healthcare providers about the drugs they are taking to avoid these kinds of interactions and ensure the safe use of the drug.
Withdrawal Symptoms
After a long time, it will be quite difficult to stop the medicine. If a patient stops the medicine abruptly then, there are many chances that he/she may suffer from some withdrawal symptoms. You should know this. Read the following to know the withdrawal symptoms of Modafinil.
- Vomiting
- Excess Sweating
- Nausea
- Confusion
- Stomach pain
If all these symptoms take a lot of time, talk to your doctor and ask him/her for solutions.
Warnings & Precautions For Adults, Children & Pregnant
This is very significant to be vigilant and realize warning points. Warnings and precautions can help a patient properly use the drug, and also avert a bad situation with the medicine. Read the points carefully;
- Don’t take medicine at night time. You can’t sleep at night because of your Modafinil dose.
- This drug should not be used for youngsters under 18 years of age.
- Make sure that you are not allergic to Modafinil. You can have a test or can discuss with the pharmacist, or the doctor to know your allergy status.
- Discuss your medical history, if you have any then frankly talk to your doctor about this. For example, if you have kidney, liver, heart disease, or any surgery in the past then you should discuss it. Your doctor can alter the dose or may change the medicine.
- If you have high blood pressure, a genetic disorder, or chest pain, then ensure the medicine first before taking it.
- Take the medicine without any doctor’s prescription or permission.
- Avoid all alcoholic beverages from today itself.
- Doctors will prescribe alternatives for pregnant and breastfeeding women. This drug can cause damage to the fetus and can also be harmful to a newborn baby after delivery. Medications and medicines are found in breast milk. So it is not advisable to avoid feeding a baby if the patient is undergoing Modafinil treatment.
- Do not take the medicine for longer or less duration, or discontinue the medication without consulting a doctor.
Also, continue watching the activities of older patients after the consumption of this drug. The impact of its side effects can affect them seriously.
Storage, Overdose & Missed Dose
Medicine. Store in a dry place. Keep out of the reach of children. If medication has passed the expiration date, dispose of the medication according to the patient’s instruction or consult with the pharmacist for proper disposal process.
If it is going to cause an overdose, then it shouldn’t be by mistake. Do not take an overdose to have the high effect of the medicine. Due to the overdose of Modafinil, severe symptoms may occur, and those may be like having a fast/slow heartbeat, nervousness, restlessness, agitation, nervousness, etc. Therefore, have the emergency number, or contact the doctor right away.
If you happen to miss a dose, then take the missed dose at the earliest. And if the missed dose is almost about to lapse over the next dose then skip the missed dose. However, do not forget your normal Modafinil dosage.
Food & Drug Interactions
Food, drugs, and medicine interactions can alter the work, and effect of the medicine. So, every patient should be aware of this. He/She will describe this before prescribing you the Modafinil. If in case, he/she skipped this important point then ask him/her about the effects of the interactions or read the following;
- Modafinil can interact with birth control drugs and make them less effective. It is also the primary route to expel all drugs in the body.
- Certain drugs increase the risk of side effects due to interaction. Read the following, and remember to avoid taking the medicine along with the following medicines;
- Â Clomipramine
- Cyclosporine
- Ospemifene
- Triazolam
Frequently Asked Questions
Is modafinil a stimulant?
Modafinil is a kind of novel stimulant. It has minimal peripheral side effects, and it only uses a therapeutic dose. So it is not considered a complete stimulant.
Does modafinil make you smarter?
No Modafinil does not make you smarter. It just only makes you active, and awake, as a result, a user can do the work actively, and smartly.
What is the drug Provigil used for?
Provigil is used for controlling excess sleeping issues, and to stay awake for a long time.
Is Adderall and Provigil the same?
No Adderall and Provigil are not the same. Both medicines are different from the others. Adderall is used to control the anxiety disorder, whereas Provigil is used to stay awake and get rid of the excess sleeping issue. But a common point of both medicines is, that they are used to treat narcolepsy.