Brand Name: Azstarys
Generic Name: dextro-methylphenidate 70% ser-dex-methylphenidate 30% dex-methylphenidate
Advantages: Like Focalin, this medication contains only the active stereoisomer dextro- methylphenidate. By eliminating
the inactive levo-methylphenidate, side effects may be reduced. This medication is a pro-drug (which cannot enter the brain if it is snorted or injected) therefore it cannot be abused. However, abuse of methylphenidate by children with ADHD is rare.
Disadvantages: T his medication was only very recently approved by the FDA (March 2021), so little is known about this medication
in clinical use. Difficult to switch from another medication to Jornay because of the dosage preparations.
Expensive and are not often covered by insurance.
Summary: Azstarys was approved by the FDA for the treatment of ADHD in March 2021. Because it was so recently approved, few physicians have had experience in prescribing this medication.18
Azstarys is another extended-release form of methylphenidate. Azstarys is different from the other methylphenidate medications listed above in two ways. First, the active ingredient is dextro-methylphe- nidate only. Dextro-methylphenidate is the right-handed version ofmethylphenidate, which is the only ingredient in Focalin (to understand what dextro-methylphenidate is, please see the section on mirror-image molecules in Chapter 7). Dextro-methylphenidate is responsible for most or all of the benefit in all of the methylphenidate medications listed above, while its mirror-image (levo-methylphenidate) is virtually useless. As stated above in the discussion on Focalin, a medication based on dextro-methylphenidate alone might have fewer side effects, because you are eliminating the half of the molecules that contribute to the side effects without benefiting the patient.
More Details: Second, Azstarys is unique in that it is a prodrug. A prodrug is created when the active ingredient (in this case, dextro-methylphe- nidate) is combined with another chemical entity (in this case, the amino acid serine) so that the new combined medication, ser-dextro- methylphenidate, is not active and cannot even get into the brain. Once the pill is swallowed, the body metabolizes the medication so that the serine amino acid is removed, leaving the active ingredient to do its work.
This new methylphenidate prodrug has two main advantages. Because the prodrug must be metabolized by the body before it can be absorbed into the brain to do its business, the onset is usually a little delayed, but in the end the drug will last longer. The pharmaceutical company that makes Azstarys claims that its studies indicate that this medication lasts up to thirteen hours. Unfortunately, I cannot comment on the clinical use of this medication. Because of its recent release, we do not have any clinical experience with it yet, and studies by scientists independent of the pharmaceutical company that makes the medication have not been performed.
Another advantage of the combined chemical entity is that if some- one wanted to abuse the drug by crushing the pill and snorting it, that person would not get high because the methylphenidate, combined with serine, cannot pass into the brain. This virtually eliminates the possibility of abuse.
However, much of this is beside the point. Methylphenidate is not often abused because it produces only a minimal high in people without ADHD. Children with ADHD treated with methylphenidate do not feel a high at all, because medication simply allows the brain chemistry to function the same way it does in all other children without ADHD.
If a prodrug is being prescribed for an eight-year-old, it is unlikely that an eight-year-old will consider snorting the medication. So, then, why use the expensive brand-name drug when a medication such as Concerta costs much less and will do exactly the same thing as the pro-drug? The pro-drug concept is a good idea, but in reality, prodrugs are another example of evergreening. Prodrugs have benefits (they prevent abuse and they usually last a little longer, but at the expense of taking longer to take effect in the morning). At the same time, prodrugs are also used by pharmaceutical companies to claim that they have a new drug that the FDA will approve as a brand-name drug for which they can charge much more.
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