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Thread: 4-AP ---> DEBBIE

  1. #1

    4-AP ---> DEBBIE

    How is it working, any improvements???????

    Me.

  2. #2

    4-AP

    Polette,

    So far my spasms are more controllable, and I can feel when my bladder is full. My PT says she can feel more muscles in my hips and legs and for a longer period of time. Now, given I am only 14 months post, I don't know if it is the 4-AP or my own healing. My plan is to take it one more month then wean myself off and see if the improvements stay or go away.

    Deb

  3. #3
    Senior Member
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    how did you get the AP-4

    how did you get the AP-4. I am 20 months post and I would like to try some. I have an appointment with my doctor in May and I would like to ask for some...

    EM

  4. #4

    College Pharmacy

    EM,

    You can call Pete Hueseman, R.Ph., P.D. College Pharmacy 1-800-888-9358 Ext.116.

    Please read what Dr. Young wrote about 4-AP and the ramping up procedure.

    "Please, DO NOT TAKE 4-aminopyridine without the supervision of an experienced doctor. Let me say it again... you should not be taking 4-AP without working with a doctor who is familiar with the drug and its effects on people, and who can take care of complications. When I say a doctor, I don't mean me or this bulletin board. You should not be doing this without a doctor's guidance. If you don't understand what follows, you have no business taking 4-AP.

    Let me comment first on the side-effects of 4-AP, the formulations of 4-AP from compounding pharmacies, the dose of 4-aminopyridine, and then an example of a ramping approach that some people have used.

    1. Side-effects of 4-AP. Please, 4-AP is not an innocuous drug. It blocks voltage-sensitive potassium channels in the heart, nerves, brain, and spinal cord. These potassium channels play an important role in limiting the duration of action potentials. Action potentials are the excitatory signals of these cells. The drug can greatly increase the excitability of the brain, heart, peripheral nerves, and other excitable tissues of the body. When you take too much (and the definition of too much varies from person to person), 4-AP can cause epileptic seizures, high blood pressure, and abnormal and even life-threatening cardiac arrhythmia. In moderate doses, it can cause nervousness, insomnia, numbness and tingling particularly around the lips, increased bowel frequency. In low doses, particularly when taken for the first time, 4-AP can cause excitement, sympathetic overactivity (heart pounding), parasympathetic overactivity (dry mouth), etc.

    2. Formulation of 4-AP. There are two formulations of 4-AP. You better know what formulation you are using because it makes a big difference. One formulation is called "immediate release" and this is just the drug mixed with filler material in gelcaps. The second formulation is what some compounding pharmacies call "time-release". The immediate release formulation is rapidly absorbed by the body and produces high peak levels within 30 minutes after taking the pill and is usually cleared within 3-4 hours.

    The time-release formulation of 4-AP is usually mixed with some material that keeps the 4-AP from being released right away and this may carry the drug lower into the gut where some of the 4-AP may be lost or not absorbed. Time-release formulations generally result in more prolonged drug effects that may last 8-12 hours. It may be less effective that the immediate release formulation because not all of it may be absorbed.

    Please note that the formulation of 4-AP that is currently in clinical trial by Acorda Therapeutics is different from the time-release formulation provided by compounding pharmacies. The Acorda formulation is called fampridine SR (sustained release). It was developed by Elan Pharmaceuticals and was carefully tested to produce sustained plasma levels of drug when the drug is taken twice a day. The time-release formulations made by compounding pharmacies are not the same. Also, the formulations vary from pharmacy to pharmacy.

    3. Dose of 4-AP. I strongly recommend against anybody taking more than four 10 mg of immediate release 4-aminopyridine per day, usually 4-6 hours apart. Please note that the drug effect from the immediate release formulation wears off after 4-6 hours. I was absolutely shocked one day to find somebody posting on the Cando forums a year or two ago, saying that he took four capsules of 10 mg of 4-AP all at one time, thinking that this was the way to take 40 mg per day. Can you imagine how nervous that made me. How much you take at a time is what determines your blood levels of the drug. Taking 20 mg at one time can cause seizures in some people.

    There is little data concerning the time-release formulations from compounding pharmacies. It is unclear how much of the 4-AP actually gets into the body (bioavailability) of the drug. Some pharmacies mix their immediate release formulation with dextrose or other sugars that reduce the shelf-life of the drug. I have heard that the drug potency declines significantly over several months. Therefore, people should not be ordering large supplies of the drug and keeping them for months.

    4. Ramping up. When people start taking 4-AP for the first time, they generally have more side-effects at the beginning. There is some evidence that ramping up the dose slowly over several weeks will reduce the side effects of the 4-AP. There is no specifically recommended approach although I know some people who have done the following. Your doctor should prescribe some 5-mg capsules for the ramping up. Some doctors start with one 5-mg capsule and progressively increase the number of daily capsules over several days. For example, on day one, take one 5 mg capsule. Day 2, take a 5 mg capsule in the morning and another one in the afternoon (6 hours later) . Day 3, take 5 mg capsule in the morning, afternoon, and evening (six hours apart). Day 4, take a 5-mg capsule in the morning and then a capsule every four hours apart. At any time, if you are getting side-effects, don't keep ramping up.

    If you have no side-effects from the above over several days, you can start substituting a 10-mg capsule for the morning 5-mg capsule. Next day, substitute a 10-mg capsule for the second. If you are tolerating the drug well, you can keep going until you are taking 10-mg capsules four times day. Again, please do not continue ramping up if you are getting side effects. If you are taking the immediate release formulation, do not exceed 10-mg capsules taken 4 hours apart without close supervision from your doctor.

    Don't stop the drug suddenly. If you want to get off the drug, ramp down the dose over a two week period. If you suddenly stop the drug, you may get increased spasticity.

    Finally, a comment about dose relative to body size. The distribution of the immediate release 4-AP in the body is still not completely understood. Because the drug crosses the blood brain barrier and distributes in certain tissues preferentially, it is not clear that it is appropriate to take more drug if you are a bigger person. There is no data concerning the distribution of the drug in women versus men. There may be differences of absorption of the drug in different people, as well as a difference in the sensitivity of people to the drug. The presence of certain drugs, such as baclofen, alcohol, antidepressants, etc. may also influence the effects of the drug.

    What should you do if you take too much 4-AP? First, your doctor should understand that the drug clears from the body in a few hours and, if the side-effects are minor, they should subside. However, if you get a seizure, people around you have to be aware how to handle a seizure and to get you to an emergency room immediately to stop the seizure as quickly as possible. Prolonged seizures damage the brain.

    If the above is scaring you, it is meant to. By the way, did I mention that you should not be taking the drug unless under the supervision of an experienced doctor? Please, I cannot overemphasize this enough. The fact that you say that you are going to take 80 mg per day is scaring the living daylights out of me. Is it a time-release formulation? Is 80 mg per day what the compounding pharmacy is recommending to you?

    Wise."

  5. #5
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    Some additional 4-AP input

    I just returned from a 2 week motorhome trip of southern California and found this posting on 4-AP

    I thought you might be interested in my experience with 4-AP.

    I am a T5/T6 complete para almost 3 years post injury. (I might add I am a young 68 year old).

    I have been following the 4-AP and Acorda story now for quite some time. Two months ago, I decided to give it a try and I contacted Pete at the College Pharmacy and had quite a long talk with him regarding 4-AP. He described both the immediate and the time-release formulas and I decided to try the immediate formula. According to Pete, the immediate formula would result in my experiencing any changes sooner. I followed his recommendations for ramping up and I didn't experince any side effects. The ramping procedure I followed was:

    Day 1 thru day 5, 5 Mg. 3 times/day = 15 Mg.
    Day 6 thru day 10, 5 Mg. 4 times/day = 20 Mg.
    Day 11 thru day 15, 10 Mg. 3 times/day = 30 Mg.
    Day 16 thru day 20, 10 Mg. 4 times/day = 40 Mg.
    Day 21 thru day 25, 15 Mg., 10, 10, 10 = 45 Mg.
    Day 26 thru day 30, 15 Mg., 10, 15, 10 = 50 Mg.
    Day 31 thru day 35, 15 Mg., 15, 15, 10 = 55 Mg.
    Day 36 thru day 40, 20 Mg., 20, 20 = 60 Mg.

    All these values were dispursed thoughout the day (24 hrs.) as evenly as possible.

    I have now been on the 60 Mg. per day thoughtout the remainder of the two months I've been taking the drug.

    I was hoping to find some improvement in the bladder or bowel functions. However, no such luck.
    I have, however, noticed that my level of paralysis has lowered to the point that I have increased muscular control of the abdominal muscles. Along with this, I've also noticed that although I still can't feel pin pricks on the surface of the skin, I can feel internal sensations in my groin and legs. If I concentrate and try to move my legs, I can feel the sensation that the muscles are actually trying to move. (Can't really understand this.)

    In summary, I am going to continue taking the 60 Mgs. throughout the remander of the three months that Pete recommended. If by then I don't experience any additional improvements, I'll evaluate if the increased muscular actions are worth the cost of continuing the use of 4-AP.

    I hope this information helps in evaluating the drug.

    Don..

  6. #6
    Super Moderator Sue Pendleton's Avatar
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    "If I concentrate and try to move my legs, I can feel the sensation that the muscles are actually trying to move. (Can't really understand this.)"

    Squaw, you would not be the first to be categorized complete soon after injury and gradually, after swelling and some possible "normal" regeneration, become an incomplete in some ways. The new standard of incomplete says that you have feeling and/or movement in the last sacral segment (the anal reflex thing). But if you feel muscles trying to move, keep up what you are doing. I'd also check back with a physiatrist or neurologist and see if you can get some electrical stimulation and PT to go with what you are feeling.

    If you take any anti-spasmotics also you might want to discuss their continued use with your doctor in relation to what the 4-AP is doing. Um, doctor not Pete.

  7. #7
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    4-AP and additional drugs.

    Sue, in answer to your question of additional drugs, the only drug I take is 16 Mgs. of Neurotin. I was taking 32 Mgs. but wasn't sure if it was helping. I stopped taking Neurotin and noticed additional discomfort so starting taking it again. When the discomfort went away I was on 16 Mgs. so decided to remain at that level.

    Don

  8. #8
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    "Oops"

    I meant to say 1600 Mg. and 3200 Mg...

    Don

  9. #9
    Super Moderator Sue Pendleton's Avatar
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    LOL I sort of figured there were some zeros missing or I know some severely over medicated people. Sounds good then. I'd talk yourself back into PT for awhile or at least get a FES unit and have a PT teach you how to use it at home. The more muscle you have the fewer health problems you'll have.

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