Theophylline was first extracted from tea leaves and chemically identified around 1888 by the German biologist Albrecht Kossel. Theophylline is a bronchodilator. It works by relaxing muscles in the lungs and chest, and makes the lungs less sensitive to allergens and other causes of bronchospasm. Theophylline is used to treat the symptoms of asthma, bronchitis and emphysema.
Abstract
Theophylline is a bronchodilator. It works by relaxing muscles in the lungs and chest, and makes the lungs less sensitive to allergens and other causes of bronchospasm. Theophylline is used to treat the symptoms of asthma, bronchitis and emphysema.
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Brand Names
Theo-Dur
Theo-24
Uniphyl
Slo-Bid
Gyrocaps
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History
Theophylline was first extracted from tea leaves and chemically identified around 1888 by the German biologist Albrecht Kossel.Just seven years after its discovery, a chemical synthesis starting with 1,3-dimethyluric acid was described by Emil Fischer and Lorenz Ach. The Traube synthesis, an alternative method to synthesize theophylline, was introduced in 1900 by another German scientist, Wilhelm Traube. Theophylline's first clinical use came in 1902 as diuretic.It took an additional 20 years until its first description in asthma treatment.
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Pharmacology
Chemical formula: C7H8N4O2
Theophylline is a naturally occurring alkaloid found in tea and is a methylxanthine similar to caffeine. It is available as a number of different salts, the most common of which are aminophylline (the ethylenediamine) and choline theophyllinate. All 3 behave similarly and will be considered together. Theophylline works as a bronchodilator by the relaxation of bronchial smooth muscle. Several mechanisms have been proposed which include the inhibition of phosphodiesterase to increase intracellular cAMP levels. However, the concentrations of theophylline required to produce measurable increases in cAMP are far outside the levels at which there is a clinical effect. Theophylline is an antagonist of adenosine at pharmacological doses, but a theophylline analogue, enprofylline, does not antagonise adenosine yet still retains potent bronchodilator activity.
Theophylline is a central nervous system stimulant and can increase minute ventilation in man by stimulation of the medullary respiratory centres. This is thought to be mediated by augmentation of hypoxic ventilatory drive and could account for its effectiveness in reducing apnoeic episodes in premature infants and reducing Cheyne-Stokes respiration. Other effects of theophylline include peripheral and coronary vasodilation, but in the central nervous system, cerebrovascular vasoconstriction and reduced cerebral blood flow.
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Uses
Theophylline is the most effective nonsteroidal prophylactic used for chronic asthma. Theophylline has the potential for serious toxicity at excessive serum concentrations. Nonetheless, its major justification for use today, when so many other asthma medications have become available, is because of the high degree of efficacy that can be attained with appropriate use. The optimal likelihood of maximal safe effect is attained with maintenance of serum concentrations within the 10 to 20 micrograms/ml therapeutic range.
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Scheduling
In the US, it is an unscheduled drug.
Psychological and physical addiction liability
Like any other Xanthines, theophylline is an addictive compound. Withdrawal symptoms include headaches, fatigue and drowsiness.
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Withdrawal Effects
Withdrawal effects are not nearly as severe, but include Nausea vomiting, headaches, insomnia.
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Long term effects
Excessive intake of theophylline can cause sleeplessness, tremors, restlessness, anxiety, as well as contribute to increased production of urin, darkening of stool.
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Physical effects
The possible side effects of theophylline are nausea, vomiting, headaches and in some cases insomnia
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Psychological treatment options
Hypnotherapy and Neuro-linguistic programming (NLP)
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Medical Treatment options
There are no medications currently available recommended by the FDA for Xanthines addiction. As this area remains largely unexplored, just breaking the schedule from the intake of sources of xanthines is best recommended. Hypnotherapy and Neuro-linguistic programming (NLP) are the available psychological treatment options. The use hypnotherapy and NLP to help a patient break out of this loop. NLP helps in changing patterns in a conscious way while hypnotherapy helps in communicating with a patient's unconscious pattern.
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Related drugs
Drugs related to Theophylline are:
Xanthines
Theobromine
Caffeine
Theophylline Theophylline
Aminophylline
Adenosine
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References
[1] http://www.drugbank.ca/drugs/DB00277
[2] http://www.drugs.com/mtm/theophylline.html
[3] http://onlinelibrary.wiley.com/doi/10.1111/j.1365-2222.1982.tb01641.x/abstract
[4] http://priory.com/cmol/theo.htm
[5] http://www.ncbi.nlm.nih.gov/pubmed/2862172
[6] http://toxipedia.org/display/toxipedia/Theophylline
[7] http://copd.emedtv.com/theophylline/theophylline-p3.html
[8] http://www.webmd.com/asthma/theophylline-for-long-term-control-of-asthma
[9] http://www.who.int/substance_abuse/terminology/who_lexicon/en/
