Since its discovery as component of the tea leaf by Albert Kossel in 1888, the history of theophylline (CAS 58-55-9) has been a long and successful one. At the turn of the century, theophylline became less expensive due to chemical synthesis and was primarily used as diuretic in subsequent years. It was Samuel Hirsch who discovered the bronchospasmolytic effect of theophylline in 1992, however, despite this pioneering discovery theophylline continued to be used primarily as diuretic and cardiac remedy. The molecular mechanism of bronchodilatation is inhibition of phosphodiesterase(PDE)3 and PDE4, but the anti-inflammatory effect may be due to histone deacetylase (HDAC) activation, resulting in switching off of activated inflammatory genes. Theophylline is indicated for the treatment of acute exacerbations of the symptoms and reversible airflow obstruction associated with asthma and other chronic lung diseases, e.g., emphysema and chronic bronchitis.

Caffeine is a methylxanthine alkaloid found in the seeds, nuts, or leaves of a number of plants native to South America and East Asia that is structurally related to adenosine and acts primarily as an adenosine receptor antagonist with psychotropic and anti-inflammatory activities. Upon ingestion, caffeine binds to adenosine receptors in the central nervous system (CNS), which inhibits adenosine binding. This inhibits the adenosine-mediated downregulation of CNS activity; thus, stimulating the activity of the medullary, vagal, vasomotor, and respiratory centers in the brain. The anti-inflammatory effects of caffeine are due the nonselective competitive inhibition of phosphodiesterases. Caffeine is used by mouth or rectally in combination with painkillers (such as aspirin and acetaminophen) and a chemical called ergotamine for treating migraineheadaches. It is also used with painkillers for simple headaches and preventing and treating headaches after epidural anesthesia. Caffeine creams are applied to the skin to reduce redness and itching in dermatitis. Healthcare providers sometimes give caffeine intravenously (by IV) for headache after epidural anesthesia, breathing problems in newborns, and to increase urine flow. In foods, caffeine is used as an ingredient in soft drinks, energy drinks, and other beverages.

FLUFYLLINE, a theophylline derivative, has a long-lasting blood pressure lowering activity as well as remarkable serotonin- and histamine antagonism and broncholytic activity.

Theophylline ephedrine is a pharmacologically active salt useful for the treatment of obstructive ventilatory disorders. Theophylline / Ephedrine is used for Wheezing, Shortness of breath, Chest tightness, Interruption of breathing in newborns, Mild and chronic bronchial asthma, Low blood pressure and other conditions.

Guaithylline (or Guaifylline), a xanthine derivative that was studied as a bronchodilator and expectorant, however, has never been marketed.

Dimethazan is a caffeine derivative. Dimethazan differs from caffeine by the replacement of the third methyl group. Dimethazan possesses antidepressant and diuretic properties. Dimethazan, administered intravenously to geriatric patients, produced respiratory and cerebral stimulation in the majority of cases. The clinical utilization of the respiratory stimulatory effect was confirmed in a patient markedly depressed with chlorpromazine. Oral administration to patients hospitalized for treatment of mental and physical depression indicated a dual effect: central nervous system stimulation and sedation. It is safe and well tolerated with none of the shortcomings of other caffeine preparations.

Tameridone is a neurotransmitter antagonist was developed as a psychotropic agent for use in veterinary. Information about the current use of this drug is not available.

Nestifylline [ABC 99] is a methylxanthine derivative that was at the preclinical stage of development with ABC for the treatment of asthma. ABC 99 has been studied in the animal to evaluate its pharmacological activity. This compound was found to have antibronchospastic activity in vitro and in vivo markedly greater than aminophylline. The new compound also had moderate antitussic properties and was an active mucoregulator. ABC 99 acts as an intestinal muscle relaxant, but it has no cardiovascular, urinary, or CNS side effects. The mechanism of ABC 99 could be explained by its inhibition of guinea-pig lung phosphodiesterases and affinity for adenosine receptors, particularly A2 receptors. ABC 99 was observed to have marked anti-inflammatory activity in a series of experimental trials involving the principal mediators of inflammation (PAF, histamine, serotonin, LTC4-like substances, etc). ABC 99 is of particular interest in the treatment of respiratory disorders involving obstructive inflammation and bronchial hypersensitivity.

Pimefylline is an N-methylated xanthine derivative. It is a coronary vasodilator and muscle relaxant.