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Theophylline is a methylxanthine bronchodilator (airway-opening medicine) taken by mouth that a pharmacy may compound when a prescriber orders it.
Theophylline (1,3-dimethylxanthine) belongs to the methylxanthine family, the same chemical group as caffeine. It relaxes the smooth muscle of the airways and dampens how strongly the airways react to triggers. Its exact mechanism is not known with certainty; animal studies suggest the airway opening comes from inhibiting phosphodiesterase enzymes. Manufactured products include extended-release tablets and capsules and an oral solution, indicated for the symptoms and reversible airflow obstruction of chronic asthma and other chronic lung diseases such as emphysema and chronic bronchitis. StatPearls notes that US use has shifted mainly to slow heart rate and apnea in premature newborns, which is not an FDA-approved indication of these products. A prescriber might order theophylline compounded in a strength or form that is not manufactured. Compounded preparations are not FDA-approved and require a prescription.
Theophylline labels carry no boxed warning, but the drug has a narrow therapeutic window: levels only slightly too high can cause repeated vomiting, a fast or irregular heartbeat and seizures, which can be fatal. Older age, liver disease, heart failure, a lasting high fever, quitting smoking, and medicines such as cimetidine, ciprofloxacin, erythromycin, fluvoxamine and estrogen birth control pills can raise levels. Smoking, rifampin, carbamazepine and St. John's wort can lower them. Do not use it if you are allergic to theophylline; use extreme caution with active ulcers, seizure disorders or heart rhythm problems. Do not chew or crush extended-release tablets, and limit caffeine. In pregnancy, the label advises use only if the benefit justifies the risk. LactMed finds it acceptable in breastfeeding; watch for infant irritability. Call your prescriber right away about vomiting, a racing heartbeat or a seizure, and talk to your prescriber or pharmacist about side effects.
Theophylline relaxes airway smooth muscle and has non-bronchodilator prophylactic effects; animal data suggest bronchodilation comes from PDE III and, to a lesser extent, PDE IV inhibition, while adverse effects such as tachycardia, headache and emesis involve PDE III inhibition and adenosine receptor antagonism. Oral solution and immediate-release forms are absorbed rapidly and completely without first-pass elimination. About 40% is protein bound. About 90% is metabolized in the liver, mainly by CYP1A2 with contributions from CYP2E1 and CYP3A; about 10% is excreted unchanged in adults versus about 50% in neonates. Elimination is capacity-limited, so small dose changes can produce disproportionate changes in serum concentration. Mean half-life in healthy nonsmoking adult asthmatics is 8.7 hours. Labeled indications: theophylline extended-release tablets, Theo-24 extended-release capsules and oral solution (ANDA) for chronic asthma and other chronic lung diseases. Clearance falls with age over 60, hepatic disease, heart failure, sustained fever, hypothyroidism and smoking cessation, and rises with smoking. Dosing is per prescriber; the label advises starting low and titrating slowly. Monitor serum theophylline concentrations at initiation, before any dose increase, with signs of toxicity, and with new illness or interacting drug changes; measure unbound levels when protein binding is reduced. Theophylline is not a controlled substance.
Compounded at Bayview
Patient guides for the preparations we make most often. Each one is compounded to order and requires a prescription.
For prescribers
Every preparation in our formulary that contains this ingredient. Strength, base and dose form are set by the prescription.
Other salt forms of this molecule, and ingredients commonly compounded alongside it.
This page describes an active pharmaceutical ingredient, not a finished drug product. Bayview Pharmacy compounds preparations containing it only on a prescriber's order for an individual patient.
Compounded preparations are not FDA-approved, and the FDA has not evaluated them for safety, effectiveness, or manufacturing quality. Nothing on this page is a claim that any preparation is effective for any condition.
A valid prescription is required. Availability depends on Bayview's licensure in your state. This page is general information, not medical advice. Discuss your situation with a licensed healthcare provider.
Our pharmacists work with prescribers to build preparations around a patient's dose, form and tolerances. Ask us what is possible with this ingredient.
