Thomas A. M. Kramer, MD


Medscape General Medicine. 2003;5(1) 

In This Article

Nonsteady State

There are some examples, however, of medications whose therapeutic effect takes place solely during a rise in their blood level and are considerably less effective at steady state. The euphoric effects of alcohol, probably the most widely used psychotropic compound, only occur when the blood level of alcohol is rising. Unfortunately, the same cannot be said about alcohol-induced impairment. These are some of the reasons alcohol can be addictive and dangerous. Perhaps the best example of this phenomenon in prescribed psychotropics is the use of methylphenidate in attention deficit/hyperactivity disorder (ADHD). While methylphenidate is very effective in the treatment of ADHD, for many years it was somewhat problematic because in order for it to work, the child needed to take multiple doses during the day, requiring visits to the school nurse or other similar arrangements. This is because the therapeutic effect of methylphenidate only takes place when the blood level is increasing. The initial attempts to make a long-acting preparation of methylphenidate were less than satisfactory to both patients and clinicians because they essentially put the child into steady state rather than simulating the process of giving the child multiple doses. The recent success and widespread use of long-acting methylphenidate preparations is because these preparations are made not to slowly release the drug but to release it in a series of boluses so that with a once-a-day administration they can create pharmacokinetics similar to what was achieved with 3-times-a-day dosing.


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