Theophylline

Authors: Prof. Dr. med. Peter Altmeyer, Prof. Dr. med. Martina Bacharach-Buhles

Last updated on: 29.10.2020

Synonym(s)

1,3-dimethylxanthine. CAS No: 58-55-9; Theocin; Theophyllins; Theophyllinum anhydricum; Theophyllinum Ph.Eur.8

Definition
This section has been translated automatically.

Methylxanthine derivative which is used medicinally mainly as a bronchodilator. Theophylline occurs naturally in tea leaves, cocoa beans and coffee beans.

Half-life
This section has been translated automatically.

3,6–12,8 h

You might also be interested in

Phytotherapy

Structural formula of various naturally occurring pyrethrins (see also there).

Pyrethroids

Synthetic structural relatives of naturally occurring pyrethrins. For example Allethrin I (allyl homologue ...

Advertisment

Pharmacodynamics (Effect)
This section has been translated automatically.

Relaxation of bronchial muscle culture, increase of mucociliary clearance, inhibition of mediator release, increase of respiratory muscle contractility, decrease of pulmonary artery pressure, anti-allergic effect.

Indication
This section has been translated automatically.

Bronchial asthma, chronic bronchitis, chronic obstructive bronchitis, emphysema.

Cosmetics: Under the INCI designation "Theophylline" the alkaloid is offered in cellulite products.

Limited indication
This section has been translated automatically.

Pregnancy, alcohol addiction, severe heart disease or hypertension, liver disease, kidney disease, porphyria, newborns, epilepsy.

Dosage and method of use
This section has been translated automatically.

Intraindividual dosage, initial 5 mg/kg bw/day p.o. or i.v. as short infusion, dose adjustment depending on the theophylline level, maintenance dose approx. 10 mg/kg bw, if necessary dosage depending on the theophylline level in serum.

Notice!

Smokers have an increased theophylline clearance and require a correspondingly higher dosage (approx. 16 mg/kg bw). Acute viral infections, cardiac insufficiency, cor pulmonale and liver cirrhosis reduce the theophylline clearance so that the dosage must be reduced (approx. 5 mg/kg bw)!

Undesirable effects
This section has been translated automatically.

Bronchospasm, leukocytosis, lymphadenopathy, gastrointestinal disturbances, increase in transaminases, albuminuria, proteinuria, allergic reactions, hyperhidrosis, cardiac arrhythmia, tachycardia, depression, headaches, seizures, tremors, dizziness, hyperglycemia, hypercalcemia, muscle twitching.

Interactions
This section has been translated automatically.

See Table 2.

Contraindication
This section has been translated automatically.

Lactation, fresh myocardial infarction, tachyarrhythmia, hypersensitivity to the active substance or xanthine derivatives.

Preparations
This section has been translated automatically.

Solosine, Euphylong

Note(s)
This section has been translated automatically.

Standard value: The standard value is between 10 and 20 mg/l in serum

Tables
This section has been translated automatically.

Dosage of theophylline depending on the theophylline level

Theophylline serum concentration	Recommended dose
Therapeutic range: 8-20 mg/l	Maintain dose; check serum concentration every 3 months
20-25 mg/l	Reduce daily dose by 10%.
25-30 mg/l	Skip next single dose and reduce the total dose by 25%.
> 30 mg/l	Skip next 2 single doses, reduce total dose by 50%.
7,5-10 mg/l	Increase dose by 25%.
5-7.5 mg/l	Increase dose by 25%.

Essential interactions of theophylline

Barbiturates	Theophylline levels ↓
Carbamazepine	reciprocal mirrors ↓
Cimetidine	Theophylline levels ↑
Disulfiram	Theophylline levels ↑
Ephedrine	Mutual toxicity ↑
INFα 2α	Theophylline levels ↑
Ketoconazole	theophylline levels by up to 50% ↓
Lithium salt	Lithium effect ↓
Macrolide antibiotics	Theophylline levels ↑
Phenytoin	reciprocal mirrors ↓
β -receptor blockers	Theophylline excretion ↓
Rifampicin	Theophylline levels ↓
Sulfinpyrazone	Theophylline levels ↓
β -Sympathomimetics	cardiac arrhythmia, tachycardia
Tiabendazole	Theophylline levels ↑
Smoking cigarettes	Theophylline HWZ ↓, possibly 50-100% dose increase required