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Theophylline. Theophylline, also known as 1,3-dimethylxanthine, is a drug that inhibits phosphodiesterase and blocks adenosine receptors. [1] It is used to treat chronic obstructive pulmonary disease (COPD) and asthma. [2] Its pharmacology is similar to other methylxanthine drugs (e.g., theobromine and caffeine). [1]
Because one of the active ingredients in Tedral is theophylline, Tedral is contraindicated if the patient has: [3] [6] Hypersensitivity to xanthine derivatives; Coronary artery disease (cardiac stimulating effects of Theophylline may prove harmful) Peptic ulcer; Concomitant use with ephedrine in children.
A combination of theophylline, ephedrine, and hydroxyzine has been marketed under the brand name Marax among others as well. [16] [17] [18] Combinations of theophylline, ephedrine, and a barbiturate were later phased out in favor of combinations of theophylline and ephedrine alone (e.g., brand name Franol).
Fenethylline (BAN, USAN) or fenetylline is a codrug of amphetamine and theophylline and so a mutual prodrug of both. It is also spelled phenethylline; other names for it are amphetamin oethyl theophylline and amfetyline. The drug was marketed for use as a psychostimulant under the brand names Captagon, Biocapton, and Fitton.
Aminophylline is a compound of the bronchodilator theophylline with ethylenediamine in 2:1 ratio. The ethylenediamine improves solubility, and the aminophylline is usually found as a dihydrate. [2] Aminophylline is less potent and shorter-acting than theophylline. Its most common use is in the treatment of airway obstruction from asthma or COPD ...
8-Chlorotheophylline, also known as 1,3-dimethyl-8-chloroxanthine, is a stimulant drug of the xanthine chemical class, with physiological effects similar to caffeine. [1] Its main use is in combination (salt) with diphenhydramine in the antiemetic dimenhydrinate (Dramamine). Diphenhydramine reduces nausea but causes drowsiness, and the ...
Dimenhydrinate. Dimenhydrinate, sold under the brand name Dramamine, among others, is an over-the-counter medication used to treat motion sickness and nausea. Dimenhydrinate is a theoclate salt composed of diphenhydramine (an ethanolamine derivative) and 8-chlorotheophylline (a chlorinated theophylline derivative) in a 1:1 ratio.
Recognition that the knowledge about PDE could be used to develop drugs that were PDE inhibitors led to extensive research. Most studies used analogues of the nucleotide substrates or derivatives of natural product inhibitors such as xanthine (e.g. theophylline) and papaverine.