Buy Theophylline (phosphodiesterase) Cas 58-55-9

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] Trace amounts of theophylline are naturally present in tea, coffee, chocolate, yerba mate, guarana, and kola nut.^[1][3]

The main actions of theophylline involve:^[2]

• relaxing bronchial smooth muscle
• increasing heart muscle contractility and efficiency (positive inotrope)
• increasing heart rate (positive chronotropic)
• increasing blood pressure
• increasing renal blood flow
• anti-inflammatory effects
• central nervous system stimulatory effect, mainly on the medullary respiratory center^[4][5]

The main therapeutic uses of theophylline are for treating:^[2]

• Chronic obstructive pulmonary disease (COPD)^[6]
• Asthma
• Infant apnea^[7]
• Blocks the action of adenosine; an inhibitory neurotransmitter that induces sleep, contracts the smooth muscles and relaxes the cardiac muscle.
• Treatment of post-dural puncture headache.^[8][9]

Theophylline and other methylxanthines are often used for their performance-enhancing effects in sports, as these drugs increase alertness, bronchodilation, and increase the rate and force of heart contraction.^[10] There is conflicting information about the value of theophylline and other methylxanthines as prophylaxis against exercise-induced asthma.^[11]

The use of theophylline is complicated by its interaction with various drugs and by the fact that it has a narrow therapeutic window (<20 mcg/mL).^[2] Its use must be monitored by direct measurement of serum theophylline levels to avoid toxicity. It can also cause nausea, diarrhea, increase in heart rate, abnormal heart rhythms, and CNS excitation (headaches, insomnia, irritability, dizziness, and lightheadedness).^[2][12] Seizures can also occur in severe cases of toxicity, and are considered to be a neurological emergency.^[2]

Its toxicity is increased by erythromycin, cimetidine, and fluoroquinolones, such as ciprofloxacin. Some lipid-based formulations of theophylline can result in toxic theophylline levels when taken with fatty meals, an effect called dose dumping, but this does not occur with most formulations of theophylline.^[13] Theophylline toxicity can be treated with beta blockers. In addition to seizures, tachyarrhythmias are a major concern.^[14] Theophylline should not be used in combination with the SSRI fluvoxamine.^[15][16]

Like other methylated xanthine derivatives, theophylline is a competitive nonselective phosphodiesterase inhibitor which increases intracellular levels of cAMP and cGMP,^[2][17] activates PKA, inhibits TNF-alpha^[18][19] and inhibits leukotriene^[20] synthesis, and reduces inflammation and innate immunity.^[20] Theophylline also acts as a nonselective adenosine receptor antagonist, antagonizing A₁, A₂, and A₃ receptors almost equally, which explains many of its cardiac effects.^[2][21] Theophylline activates histone deacetylases.^[2]