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Theophylline, also known as 1,3-dimethylxanthine, is a drug that inhibits phosphodiesterase and blocks adenosine receptors. It is used to treat chronic obstructive pulmonary disease (COPD) and asthma. Its pharmacology is similar to other methylxanthine drugs. Trace amounts of theophylline are naturally present in tea, coffee, chocolate, yerba maté, guarana, and kola nut.
A bronchodilator or broncholytic is a substance that dilates the bronchi and bronchioles, decreasing resistance in the respiratory airway and increasing airflow to the lungs. Bronchodilators may be originating naturally within the body, or they may be medications administered for the treatment of breathing difficulties, usually in the form of inhalers. They are most useful in obstructive lung diseases, of which asthma and chronic obstructive pulmonary disease are the most common conditions. Although this remains somewhat controversial, they might be useful in bronchiolitis and bronchiectasis. They are often prescribed but of unproven significance in restrictive lung diseases.
Pseudoephedrine, sold under the brand name Sudafed among others, is a sympathomimetic medication which is used as a decongestant to treat nasal congestion. It has also been used off-label for certain other indications, like treatment of low blood pressure. At higher doses, it may produce various additional effects, including psychostimulant, appetite suppressant, and performance-enhancing effects. In relation to this, non-medical use of pseudoephedrine has been encountered. The medication is taken by mouth.
Ephedrine is a central nervous system (CNS) stimulant and sympathomimetic agent that is often used to prevent low blood pressure during anesthesia. It has also been used for asthma, narcolepsy, and obesity but is not the preferred treatment. It is of unclear benefit in nasal congestion. It can be taken by mouth or by injection into a muscle, vein, or just under the skin. Onset with intravenous use is fast, while injection into a muscle can take 20 minutes, and by mouth can take an hour for effect. When given by injection, it lasts about an hour, and when taken by mouth, it can last up to four hours.
Ephedra is a medicinal preparation from the plant Ephedra sinica. Several additional species belonging to the genus Ephedra have traditionally been used for a variety of medicinal purposes, and are a possible candidate for the soma plant of Indo-Iranian religion. It has been used in traditional Chinese medicine, in which it is referred to as Ma Huang, for more than 2,000 years. Native Americans and Mormon pioneers drank a tea brewed from other Ephedra species, called "Mormon tea" and "Indian tea".
Pantoprazole, sold under the brand name Protonix, among others, is a medication used for the treatment of stomach ulcers, short-term treatment of erosive esophagitis due to gastroesophageal reflux disease (GERD), maintenance of healing of erosive esophagitis, and pathological hypersecretory conditions including Zollinger–Ellison syndrome. It may also be used along with other medications to eliminate Helicobacter pylori. Pantoprazole is a proton-pump inhibitor (PPI) and its effectiveness is similar to that of other PPIs. It is available by mouth and by injection into a vein.
Hydroxyzine, sold under the brand names Atarax and Vistaril among others, is an antihistamine medication. It is used in the treatment of itchiness, anxiety, insomnia, and nausea. It is used either by mouth or injection into a muscle.
Cetirizine is a second-generation antihistamine used to treat allergic rhinitis, dermatitis, and urticaria (hives). It is taken by mouth. Effects generally begin within thirty minutes and last for about a day. The degree of benefit is similar to other antihistamines such as diphenhydramine, which is a first-generation antihistamine.
Zileuton (trade name Zyflo) is an orally active inhibitor of 5-lipoxygenase, and thus inhibits leukotrienes (LTB4, LTC4, LTD4, and LTE4) formation, used for the maintenance treatment of asthma. Zileuton was introduced in 1996 by Abbott Laboratories and is now marketed in two formulations by Cornerstone Therapeutics Inc. under the brand names Zyflo and Zyflo CR. The original immediate-release formulation, Zyflo, is taken four times per day. The extended-release formulation, Zyflo CR, is taken twice daily.
The ECA stack is a drug combination used in weight loss and as a stimulant. ECA is an initialism for ephedrine, caffeine, and aspirin, with variants of it including the EC stack, which removes the aspirin for those who can not tolerate it. Dietary supplements based on or including elements of ECA were popular through the 1990s and early 2000s, but the marketing of ephedra- or ephedrine-containing stimulant combinations for weight loss and bodybuilding is now restricted or illegal in the United States and the Netherlands due to reports of heart attack, stroke, and death associated with these supplements.
Ephedra is a genus of gymnosperm shrubs. The various species of Ephedra are widespread in many arid regions of the world, ranging across southwestern North America, southern Europe, northern Africa, southwest and central Asia, northern China and western South America. It is the only extant genus in its family, Ephedraceae, and order, Ephedrales, and one of the three living members of the division Gnetophyta alongside Gnetum and Welwitschia.
Enoxacin is an oral broad-spectrum fluoroquinolone antibacterial agent used in the treatment of urinary tract infections and gonorrhea. Insomnia is a common adverse effect. It is no longer available in the United States.
Fenethylline or fenetylline (INN) 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
Secobarbital/brallobarbital/hydroxyzine was a combination tablet containing 50 mg brallobarbital, 150 mg secobarbital and 50 mg hydroxyzine that was used as a sedative. It was sold under the brand name Vesparax. This drug has been withdrawn from the market in most countries.
Brallobarbital was a barbiturate developed in the 1920s. It has sedative and hypnotic properties, and was used for the treatment of insomnia. Brallobarbital was primarily sold as part of a combination product called Vesparax, composed of 150 mg secobarbital, 50 mg brallobarbital and 50 mg hydroxyzine. The long half-life of this combination of drugs tended to cause a hangover effect the next day, and Vesparax fell into disuse once newer drugs with lesser side effects had been developed. Vesparax reportedly was the drug that musician Jimi Hendrix supposedly overdosed on and led to his untimely death. It is no longer made.
Theodrenaline, also known as noradrenalinoethyltheophylline or as noradrenaline theophylline, is a chemical linkage of norepinephrine (noradrenaline) and theophylline used as a cardiac stimulant. It is sometimes combined with cafedrine.
Doxofylline is a phosphodiesterase inhibiting bronchodilator used in the treatment of chronic respiratory diseases such as asthma and COPD. Like theophylline, it is a xanthine derivative.
4-Methoxyphencyclidine is a dissociative anesthetic drug that has been sold online as a research chemical. The synthesis of 4-MeO-PCP was first reported in 1965 by the Parke-Davis medicinal chemist Victor Maddox. A 1999 review published by a chemist using the pseudonym John Q. Beagle suggested the potency of 4-MeO-PCP in man was reduced relative to PCP, two years later Beagle published a detailed description of the synthesis and qualitative effects of 4-MeO-PCP, which he said possessed 70% the potency of PCP. 4-MeO-PCP was the first arylcyclohexylamine research chemical to be sold online, it was introduced in late 2008 by a company trading under the name CBAY and was followed by several related compounds such as 3-MeO-PCP and methoxetamine. 4-MeO-PCP has lower affinity for the NMDA receptor than PCP, but higher affinity than ketamine, it is orally active in a dosage range similar to ketamine, with some users requiring doses in excess of 100 mg for desired effects. Users have reported substantial differences in active dose, these discrepancies can be partially explained by the presence of unreacted PCC and other impurities in samples sold on the grey market. 4-MeO-PCP has Ki values of 404 nM for the NMDA receptor, 713 nM for the norepinephrine transporter, 844 nM for the serotonin transporter, 296 nM for the σ1 receptor and 143 nM for the σ2 receptor.
A codrug consists of two drug moieties, generally "active against the same disease", that are joined through one or more covalent chemical bonds to create a single new chemical entity; they can also be described as a mutual prodrug, recognising that a catabolic biosynthetic step is most often required to liberate the two drugs. While acting against the same disease, the two moities may operate via different mechanisms of action, and so display differing specific therapeutic effects. The recognised advantages of a codrug approach to small molecule drug design include the possibilities of (i) combined efficacies of the two drugs that are therapeutically synergistic, (ii)) altered properties that improve the pharmacokinetics of the codrug over its indivially administered components (iii) improved modes of drug delivery, and (iv) masking of reactive functional groups of each component drug, possibly improving shelf life.
Theophylline ephedrine, or theophylline/ephedrine, sold under the brand name Franol among others, is a fixed-dose combination formulation of theophylline, an adenosine receptor antagonist, and ephedrine, a norepinephrine releasing agent and indirectly acting sympathomimetic agent, which has been used as a bronchodilator in the treatment of asthma and as a nasal decongestant. It was first studied and used to treat asthma in the 1930s or 1940s and combinations of the two drugs subsequently became widely used. A ratio of 5:1 theophylline to ephedrine is usually used in combinations of the drugs. Later research found that the combination was no more effective for asthma than theophylline alone but produced more side effects however.
References
- ↑ Hunt TM (2011). Drug Games: The International Olympic Committee and the Politics of Doping, 1960–2008. University of Texas Press. p. 45. ISBN 978-0-292-73957-4 . Retrieved 20 July 2018.
- ↑ Marax Micromedex Detailed Consumer Information . Accessed 23 April 2021.
- ↑ Fixley M, Shen DD, Azarnoff DL (June 1977). "Theophylline bioavailability: a comparison of the oral absorption of a theophylline elixir and two combination theophylline tablets to intravenous aminophylline". The American Review of Respiratory Disease. 115 (6): 955–62. doi:10.1164/arrd.1977.115.6.955 (inactive 1 November 2024). PMID 262107.
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