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Safe and Effective 4-Aminopyridine is Available.
4-aminopyridine (4AP) has been used for many years, prescribed for people with multiple sclerosis. It is a potassium channel blocker that, when used correctly, improves walking and other motor activities.
There’s a “trick” to using 4AP correctly. Using too much could cause seizures. The compounded 4AP preparation is made in 5mg or 10mg strengths with simple filler. The drug is quickly absorbed and begins working in just a few minutes. The trick is that a user should follow a ramping schedule to establish how the drug will work for them, and the best dose.
A commercial version of 4AP is now available, Ampyra. It is a 10mg, slow release tablet taken every 12 hours. It is expected to release its contents uniformly over a specific number of hours. Real life situations consist of differing diets and health conditions that make it unrealistic to expect that a swallowed dose will dissolve precisely as expected, time after time. While the slow release filler could help ease stomach distress for some medications, it is not likely an effective method for achieving consistent, clinically effective blood levels for drugs with narrow clinical windows.
The commercial tablet cannot be broken or chewed. It is costly and only available from special outlets.
We make this preparation as a safe, regular release capsule. From our experience, we conclude that the new commercial drug is likely to be less efficient and potentially more harmful than the compounded capsule. A single dose every 12 hours may be fine for some people, but the wide variation in the MS population can make it ineffective – and possibly dangerous – for others. For doctors who choose to dose more carefully, we suggest that 5mg capsules are a superior choice.
We provide a written ramp protocol that begins at 5mg per day and increases per a schedule to a level of 30 to 40mg per day - 0.23mg/pound. It is profoundly unwise to use more than that. It typically takes two weeks to achieve the maximum effective, safe dose. Doses are spaced four to five hours apart. Here is one suggested ramping schedule;
- 5mg per day - in the morning - for 2 days
- Then, 5mg BID (twice daily; breakfast and late afternoon) for 3 days.
- Then, 5mg TID (3 times a day; every 5-6 hours while awake) for 4 days = 15 mg/day
- Then, 5mg QID (4 times a day; every 4-5 hours while awake) for 5 days = 20 mg/day
- Then, IF TOLERATED and if needed may go up gradually to 10mg QID (4 times a day; every 4-5 hours while awake) = 40 mg/day maximum
Compounded 4-aminopyridine is available. Depending on strength, the price ranges from $69.00 to $79.00 for a month’s supply.
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