Frequently Asked Questions About Antinarcoleptic Medications

Narcolepsy is a dysfunction of the brain distinguished by the incorrect sleep-awakening regulation by the brain. People are born with this dysfunction so it cannot be acquired. It is usually diagnosed at an early age. The primary signs are cataplexy and unexpected falling asleep. Cataplexy is an unexpected and quick incident of muscle weakness with full consciousness. It is typically induced by emotions such as laughing, fear, surprise, and others. Individuals with narcolepsy do not necessarily have these episodes but they always have sleepiness attacks throughout the day which doesn’t depend on the night sleep amount. Sleepiness that occurs during these attacks can be is comparable to unbearable episodes of sleepiness in healthy people who had been deprived of sleep for 24-48 hours.

Other manifestations of the disorder include bad night sleep, hallucinations accompanying sleepiness attacks and awakening from them, sometimes short-term paralysis of the body right after awakening is occurring.

The disorder usually is developed in kids and adolescents of the male sex. It is identified in 20-40 persons per 100,000. The nature of the disease isn’t fully studied yet but it’s known that it is a genetically-transmitted dysfunction, and, presumably, it can be also triggered by external factors such as viral infections.

There is a theory that the disorder is based on the insufficiency of orexins (hypocretins), hypothalamic peptides. This is based on the observation that in persons with the dysfunction, in the cerebrospinal fluid, the fluid circulating constantly in the ventricles of the brain, low content of orexins is found. This substance is a biologically active agent that regulates the process of alternating slow-wave sleep phase and rapid eye movement sleep phase (REM).

The therapy methods available today can only make the manifestations of the disorder milder and better the quality of life of persons with the dysfunction but do not cure it.

The formulations used for narcolepsy are divided into three groups:
– Wakefulness-promoting formulations;
– Cataplexy management formulations;
– Night-sleep normalizing formulations.

The most frequently used formulations for the disorder today are wakefulness-promoting pills based on Armodafinil and Modafinil. These are the first-line therapy because they are efficient against daytime sluggishness and do not induce addiction development. Instead of them, amphetamines can be used but they cause dependence and other negative effects on general health.

Besides the first-line sleepiness-battling formulations, such psychostimulants as dextroamphetamine sulfate (Dexedrine, Dextrostat), methamphetamines (Deoxin), methylphenidate (Ritalin), pemoline (Zillert), and mazindol (sanorex) are used.

For cataplexy management, sometimes antidepressants are used. They include Clomipramine, Imipramine, Protriptyline, Venlafaxine, and other formulations that suppress REM sleep. For normal night sleep in its violation sleeping pills are appointed such as Zolpidem and Zopiclone.

– Wakefulness-promoting formulations: this group of medications influences the chemicals in the brain that are active when a person is awake. They “trick” the brain to be awake even if it wants to shut down for sleep. The pills are also effective for individuals deprived of sleep who don’t have narcolepsy.
– Cataplexy management formulations include majorly antidepressants which principle of action is laid in the inhibition/prevention of reuptake of free serotonin and norepinephrine by the presynaptic cleft. The increased level of these substances achieved through prevention of reuptake results in better emotion control and as a result, rarer episodes of cataplexy.
– Night-sleep normalizing formulations are pills that are also appointed for insomnia. They usually have muscle relaxant, anxiolytic, sedative, hypnotic, amnestic, and anticonvulsant effects. The effect of these drugs is based on different mechanisms. The effect of already mentioned medication Zolpidem is based on specific agonism with central omega receptors (benzodiazepine receptors type I and II), macromolecular GABA receptor complexes that cause the opening of neuronal anionic channels for chlorine. It reduces the time of falling asleep and the number of nightly awakenings prolongs the duration of sleep and improves its quality.

The safest antinarcoleptic pills that can be used even by healthy people or individuals with other causes of daytime sleepiness are based on Armodafinil and Modafinil. These medications can be called differently based on their producers. For instance, you can get Waklert by Sun Pharma, Modafinil by Sun Pharma, and so on.

No. Unfortunately, nowadays there is no way to get rid of narcolepsy once and for all. The reason for that is that the cause of the disease isn’t fully understood. Therefore, scientists cannot come up with a solution.

If you are diagnosed with the disorder, most likely you will need to take wakefulness-promoting medicines all your life. Luckily, such medications as Modafinil and Armodafinil are safe to use for extended periods of time, unlike previously used amphetamines. Besides, if you suffer from bad night sleep or cataplexy you may also need to use the drugs for them too. However, antidepressants and sleeping pills are not as safe and you need to consult your physician before you start taking them to find out for how long it is safe to use them without interruptions.

Kids can be given wakefulness-promoting formulations and other medications aimed to cope with cataplexy and bad night sleep but only a medical practitioner who treats narcolepsy in children can appoint appropriate treatment based on the kid’s age.

It is not recommended to take any medications except for vitamins for pregnant women. However, if sleepiness attacks endanger a woman’s life, her doctor can assess the risks and benefits and prescribe appropriate treatment.

The contraindications for wakefulness-promoting medications are:
– Individual intolerance of the pills;
– Heart attack or stroke associated with the use of stimulants;
– Severe heart diseases such as left ventricular hypertrophy or mitral valve prolapse.

Contraindications for antidepressants include:
– Pregnancy and breastfeeding;
– Allergy to the active ingredient;
– Severe cardiovascular diseases;
– Glaucoma;
– Bowel or bladder atony;
– Prostate adenoma;
– Young age (below 18 years).

Sleeping pills contraindications:
– Hypersensitivity;
– Age below 15 years;

Restrictions on the use:
– Sleep apnea, acute and/or severe respiratory failure;
– Myasthenia gravis;
– Depression;
– Alcoholism;
– Drug abuse or drug addiction;
– Severe liver and/or kidney dysfunction
– Age over 65 years.

Wakefulness-promoting medications:
– Backache
– Headache
– Nausea
– Sense of anxiety
– Nasal congestion
– Diarrhea
– Feeling anxious
– Dizziness
– Dyspeptic disorders
– Insomnia

Dangerous side effects include:
– Profuse rash
– Severe allergic reactions involving liver or blood cells
– Urticaria
– Appearance of mouth ulcers
– Blistering or peeling of the skin
– Swelling of the face, eyes, lips, tongue, legs, or throat
– Trouble swallowing and breathing
– Heat
– Shortness of breath
– Yellowing of the skin and whites of the eyes
– Dark urine

Antidepressants:
– Sleepiness
– Dry mouth
– Nausea
– Difficulty achieving orgasm

Sleeping pills:
– Daytime drowsiness
– Dizziness
– Headache.

Your doctor can choose a combined therapy or a single-drug therapy so the dosages of the medications can greatly vary.

Here we are providing the examples of dosages of the most commonly used medications:
– Armodafinil is used by one pill a day in the morning. The dosage per pill is 150 mg.
– Modafinil is used by one pill a day in the morning. The dosage per pill is 200 mg.
– Zolpidem is taken by a single pill before bedtime. The dosage per pill is 10 mg.

Wakefulness-promoting formulations designed for narcolepsy are also called Smart drugs. This name is due to their ability to make even healthy people more energetic and therefore more productive and seemingly more fast-thinking focused, and so on. These medications are based on Armodafinil and Modafinil.

The official uses for wakefulness-promoting formulations are sleep disorder related to night shift work and sleep apnea. However, they are also effective for individuals who do not have sufficient night sleep for different reasons and also suffer from daytime sluggishness. The formulations can be useful for people with low-productivity depression, ADHD, weather sensitivity, people with insomnia, individuals who have trouble memorizing new information, sleep less than 8 hours a day or suffer from any type of hypersomnia (extra need for sleep), and so on.

In general, the mentioned medications besides their main function are cognitive function enhancers. They indeed improve memory, focus, and the speed of thinking and so on.

Off-label uses are the uses that are not yet confirmed by the FDA but which are considered effective and safe. Such uses include coping with sleepiness related to other dysfunctions or lack of sufficient sleep, lowering of cognitive functions (memory, focus, ability to read, write, or think fast, and so on). These uses are called off-label because they are not listed in the official label or package insert that comes with the pills yet the medications are proven to be effective for them and safe.

Yes, it is safe to use Modafinil or Armodafinil off-label as long as you have the symptoms they can help you with and if you tolerate the medications well. However, it is preferable to get a checkup to be sure that you don’t have any underlying conditions that cause the symptoms and you don’t need to treat them. Besides, although these formulations do not cause addiction, it is advised to use them occasionally from time to time and not daily.

The use of the medications for ADHD is in process of approval and testing. However, in many countries, doctors already use Modafinil and Armodafinil for ADHD. But you need to be cautious if you decide to take the pills for this disorder as they can only enhance the hyperactivity symptom and anxiety. It is recommended to consult a specialist and use half of the regular dosage first to see how the medication is tolerated.