What’s interesting is that there are some good things that stimulants do without having the overstimulation.ĭebra Stultz, MD: Right. All these are good for different things on a theme, different variations of a theme. Modafinil is a dopamine reuptake inhibitor. Remember, I told you that bupropion is a norepinephrine reuptake inhibitor. Stephen Stahl, MD, PhD: It’s like a stimulant in a certain sense because stimulants are norepinephrine and dopamine reuptake inhibitors. Stephen Stahl, MD, PhD: It’s like bupropion, isn’t it? I’m sure you will think from a neurotransmitter. Stephen Stahl, MD, PhD: But most of what you want to do is make sure you’re stopping the medicines that cause the activation to be blocked, and you want to start medications that boost activating neurotransmitters.ĭebra Stultz, MD: Right. Stephen Stahl, MD, PhD: For people who have sodium, it can be a problem.ĭebra Stultz, MD: But the new formulation has 92% less sodium and the same effectiveness, and it’s also been approved for sleepiness and cataplexy Stephen Stahl, MD, PhD: It’s a heck of a sodium load, isn’t it? Now they have the new form with less sodium. The access problems can be somewhat problematic or a hassle, but the good news is that it works so well that people are coming up with once-a-day formulations.ĭebra Stultz, MD: Patients get used to it after a while. It’s so short acting that it’s a pain to take sometimes. Stephen Stahl, MD, PhD: The main problem is that it causes you to have to take it twice. There have also been some studies on it helping the sleep paralysis and hypnagogic hallucinations. It’s FDA approved for excessive daytime sleepiness and cataplexy. It helps with the disrupted nocturnal sleep. It’s probably the most powerful drug to make you have slow-wave sleep.ĭebra Stultz, MD: That’s a really good point. Stephen Stahl, MD, PhD: It’s got a checkered history, but boy does it work to make narcolepsy better. That medicine changed the face of narcolepsy for sure. Let’s talk for just a minute about sodium oxybate. Sometimes we have to add a sprinkle of it to some other medicines. Because stimulants, unless you give the controlled release, must all be given more than once a day.ĭebra Stultz, MD: Stimulants certainly have their place, and they add on, but they have more of an abuse potential and more cardiac effects. Sometimes you have to give them twice a day, sometimes just once a day. They tend to happen, but it’s much easier to do that with modafinil and armodafinil because they don’t have the overstimulating effects, and they don’t have the rapid onset and the big peaks. It’s hard to get a dose-response curve with stimulants that have the right amount of efficacy without the adverse effects. They often must be taken more than once a day, although there are some new ones that don’t. They go up too high a dose they overstimulate. Stephen Stahl, MD, PhD: The stimulants work sometimes too well because they work rapidly. One of the only things we had for several years for that was stimulants. They do not have the same significant adverse effects on heart rate, blood pressure, and abuse potential that the stimulants have. These medications, I believe, have helped change the medicines when they came out-a new way to treat the success of daytime sleepiness. By doing that, they wake you up.ĭebra Stultz, MD: Yes. In so doing, they have a mild stimulant effect and boost the arousal neurotransmitter dopamine. But modafinil and its active enantiomer or armodafinil boost dopamine, but not norepinephrine transporters it doesn’t look like it. In treating people with modafinil, 1 of the first things you want to do is to say, “Am I blocking dopamine or any of these other neurotransmitters,” and stop those drugs if you can. It turns out that you can be in trouble if you block any of the arousal neurotransmitters. These are the more arousal neurotransmitters. You remember the old reticular activating system-dopamine, norepinephrine, not so much serotonin, but histamine, acetylcholine. If you don’t have orexins to boost arousal, you have to have medicines to boost arousal. Almost all the medicines are dedicated to boosting arousal. They’re weak stimulants in the sense that they probably don’t rapidly block the transporter and don’t completely block the transporter. Stephen Stahl, MD, PhD: Those are agents that would probably be best characterized as dopamine reuptake blockers. Do you want to start with modafinil and armodafinil? Debra Stultz, MD: Let’s talk about some medicines that we’ve used for narcolepsy.
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