SRI VENKATESWARA COLLEGE

OF PHARMACY
DRUG PROFILE – THEOPHYLLINE
by – R.ROSHNI
16GTIT0016
4TH YEAR PHARM D
DRUG INFORMATION

• NAME : Theophylline
• BRAND NAME : Theo24, Elixophylline, theochron
• GENERIC NAME : Aminophylline
• DRUG CATEGORY :- xanthine derivatives
• MECHANISM OF ACTION :- Theophylline relaxes smooth muscles of respiratory tract and
suppress the response of airway to stimuli.
• USES: relaxes bronchial smooth muscle, increases BP, COPD, Asthma, infant apnea
PHARMACOKINETICS

• Administration – oral , IV
• Absorption - Onset:Variable, Duration:Variable
• Bioavailability 100%
• Protein Binding 40-45%
• Metabolism - Metabolized in liver by CYP1A2 and CYP3A4
• T 1/2 - 8hrs
• Excretion – urine , Clearance: 1.45 mL/min/kg
• ADR :- nausea, diarrhea, increased heart rate, headache, insomnia, dizziness, seizures, abnormal
heart rhythms
• SUSCEPTIBILITY : -hypersensitivity, peptic ulcer
• DRUG INTERACTION
• Erythromycin X theophylline -------> theophylline toxicity
• Cimetidine X theophylline ----------> theophylline toxicity
• PHARMACODYNAMICS :
• it works by opening the airways in the lungs , it does this by relaxing the muscles and
decreasing the response to the substances that has caused the airways to constrict .
• COMBINATIONS :- Theophylline(23gm)+ Etophylline (77mg)
Aminophylline is a drug combinationthat contains theophylline and ethylenediamine in a
2:1 ratio
• PREGNANCY CATEGORY :- C
• LACTATION : mild toxicity may occur , so breastfeeding while taking theophylline is not
suggested
MECHANISM OF ACTION
LATEST FINDINGS

• It was recently found that it suppresses the production of luekotiene B4 by alveolar

macrophages invivo. So theophylline adds to the newer class of anti inflammatory
medication.
• Recent research has proven that theophylline use may cause cognitive and behavioral
side effects in children.
• Preparations containing only theophylline is the best one to administer. Some older
combination with ephedrin and sedatives may cause rapid heart beat and may control
brain's respiratory centre.
• PRECAUTIONS:
• Blood test should be done regulaarly inorder to check the unwanted effects.
• This medicine may add to CNS EFFECTS stimulate like caffuene containing food or
beverages such as tea, coffee, and cola drinks. Avoid these foods while taking the medicine
• Do not take OTC medication of theophylline.
• MONITORING:
• CHF, Hypothyroidism,liver disease, pulmonary edema,, heart rhythm problem,shock, seizures,
stomach ulcers
 FERTILITY :- theophylline is observed to enhance sperm permeation
TOLERABILITY : Not well tolerated
• TERATOGENECITY : the risk of teratogenic & fetal toxicity caused by theophylline is
dependent on its dosage.
• ADDICTION : it may cause addiction but it mostly depends on quantity & quality of
substance taken daily
• CARCINOGENICITY : no carcinogenic activity is observed
• MUTAGENICITY : not a potent mutagen
• REPORT : The drug information of theophylline was collected & submitted.