In 1976 my pediatrician started prescribing liquid theophylline Sustaire to control my asthma. I remember my mom feeding me that stuff with a teaspoon, and it tasted nasty. For the next 30 years I would end up chronically dependent on this stuff.
In the 1860s Dr. Henry Hyde Salter wrote a book, "On Asthma," where he recommended strong coffee and tea to help control hardluck asthma. In fact, this was occasionally tried by a young asthmatic Teddy Roosevelt.
Salter may have known coffee was a member of the xanthine family, but he probably didn't know the xanthines are mild bronchodilators (they dilate the air passages in your lungs). This wasn't proven until 1921, and by 1922 theophylline suppositories were used to treat asthma.
Amimophylline is the IV version of theophylline, and was first used in 1937. If you were admitted to a hospital with asthma between 1950 and 1990, chances are you had this running in your IV at some point. I know from my medical records I did.
The bronchodilator effects from caffeine are very suttle compared to Theophylline, which was first extracted from tea leaves in 1888 by a german scientist. It wasn't until 1950, however, that it was approved for use as a bronchodilator. For the next 4 decades it was a top line therapy for treating asthma and COPD.
The problem with theophylline was that it had a very narrow therapeutic level. Too low and it didn't do anything, yet if your theophylline level was too high (as in greater than 20) there were toxic effects, such as vomiting and even death. So you had to have your blood level checked frequently.
Another problem with this drug is it only lasted in your system 4 hours, so I had to take it every 8 hours or my levels dipped in the middle of the day causing asthma symptoms. Once as a kid I had a 24 hour theophylline study done, and had to have my blood drawn every few hours. It wasn't so bad, though, because they put a line in my hand to draw from.
My doctor told me in 1995 that the normal dose he prescribes is 300mg twice a day. I required 600mg twice a day, and somehow that still kept me under the toxic level. (I wonder how many cups of coffe that's equivelent to.)
In the early 1980s theophylline was determined to be "less efficacious" than anticholinergic medicines like Atropine when it comes to dilating bronchioles, yet it wasn't until the 21st century that it faded away as a top line asthma drug.
Many doctors were staunch defenders of this medicine because it worked so well for them for so many years. I was a staunch defender of it because my body became dependent on it to the point that when I forgot to take a pill I would have the worse asthma attacks ever.
Perhaps some of my fellow asthmatics will empathise with me. A good example of this was when I forgot to take my theophylline for three days when I was busy in college in 1988. Absent this bronchodilator my lungs freaked out. My chin became itchy, my chest burned, and my mucus production increased almost to the point I felt I might choke.
My room mate Frank walked in on me and I must have been a sorry sight all frogged up on the edge of my chair, grunting with each expiration, tears in my eyes, misting nebulizer clipped between my teeth.
"Do I need to take you to the ER," he said.
"NO! I'll be fine," I grunted.
"You look like you're gonna die."
"NO!" I insisted. I had just popped a Theo-Dur pill dry. I knew from past experience it would take about 20 minutes before my breath started coming back.
The Albuterol treatment was useless during one of these attacks, however I always took one. When I was really little and this happened I'd go to the ER, but at some point in my asthmatic life I learned the difference between a regular asthma attack and one induced by a low theophylin level.
"Give me ten more minutes," I grunted, "If I still look like I'm going to die, drag me to the ER." Feeling helpless I'm sure, he stood by and watched as I suffered.
Then, right on cue, I felt the mucus letting up; the chest tickling feeling letting go, and my breath coming back. First came a quarter breath, then a half a breath five minutes later, and finally... "Ahhhhh, man it feels good to breathe."
That's why I was such a staunch defendent of this medicine, and was vexed to learn Theodur was no longer made, and I had to swallow generic theophylline horse pills instead.
The problem with theohylin is it's a systemic drug with some undesirable systemic side effects. The thinking used to be if you need it for a chronic lung condition you need it, because some minor side effects are far better than suffering or dying from asthma.
Most side effects, though, are generally mild. Some are similar to when you take caffeine, such as irritibility, insomnia, nervousness and jitters. Since Xanthines are also mild diuretics, it might cause you to pee more. It can also irritate the lining of your stomach.
To some extent, I've experienced all of these side effects. However, the one that bothered me the most was an irritated stomach that I attributed to this medicine, and why I wanted to get off it.
I approached my doctor about getting off theophylin, and he said, "It's neat you bring this up, because when I started as a doctor nearly every one of my asthma patients were on theophylin, and now you're one of only two."
In the past Theophylin was a top line bronchodilator usually used in conjunction with corticosteroids. New long term bronchodilators with fewer side effects have replaced theophylin, they are called Serevent & Formoterol, and are usually given in conjuction with the inhaled corticosteroids Flovent and Pulmicort respectively in the popular medicines Advair and Symbicort.
My doctor said, "You've been on theophylin so long, and it seems to work so well for you, I'd hate to tinker with it."
"One attempt, doc" I said. "I just want to make one last attempt at getting off it. If it doesn't work, it doesn't work."
We decided on a very, very slow wean. In fact, the wean took a full year to complete. And it worked. On January 31, 2007, I took that last pill. And, just in case (as if in tribute to an old friend), I left an unopened prescription bottle of theophylin in the medicine cabinet just in case. It's still there to this day, a daily reminder of what used to be.
So while Teddy Roosevelt guzzled cups of coffee praying it would help him catch his breath, scientists gave asthmatics theophylin in the 1950s. Now, with even greater advancements in asthma medicine, theophylin is little needed today.
(For a doctor's perspective on theophylin click here).