Pharmacokinetics of theophylline and bioavailability of a sustained release theophylline preparation in patients with cystic fibrosis. 1983

S B Valet, and R H Schwartz, and J G Brooks

The elimination of theophylline after intravenous aminophylline bolus and the absorption of a sustained-release oral theophylline preparation (Theo-Dur) were studied in ten patients with cystic fibrosis (C.F.). Each patient received an I.V. bolus of aminophylline equivalent to 4 mg/kg anhydrous theophylline and 10 plasma theophylline levels were obtained over the following eight hours. Elimination half life (T1/2), total body clearance (Cl), volume of distribution (Vd) and area under the concentration curve (AUCiv) were determined. Forty-eight hours later each patient received an oral dose of sustained release theophylline equivalent to 7.47-11.42 mg/kg anhydrous theophylline and 13 plasma theophylline concentrations were measured over 24 hours. Area under the concentration curve (AUCpo) and fractional absorption (F) of the sustained release preparation were determined. Mean values (+/- S.D.) were T1/2 = 4.45 +/- 1.58 hrs, Vd = 505.8 +/- 40.7 ml/kg, Cl = 87.9 +/- 31.6 ml/kg/hr, F = 0.86 +/- 0.26. One patient did not develop detectable plasma theophylline levels until 20 hours after receiving the sustained release product, but rapidly absorbed 96% of orally administered theophylline elixir. While we could demonstrate no consistent abnormality of theophylline distribution or elimination in cystic fibrosis patients, large interindividual differences in elimination may exist. In addition, some C.F. patients may have impaired or delayed absorption of sustained release theophylline preparations.

UI MeSH Term Description Entries
D007700 Kinetics The rate dynamics in chemical or physical systems.
D008099 Liver A large lobed glandular organ in the abdomen of vertebrates that is responsible for detoxification, metabolism, synthesis and storage of various substances. Livers
D008297 Male Males
D008875 Middle Aged An adult aged 45 - 64 years. Middle Age
D002648 Child A person 6 to 12 years of age. An individual 2 to 5 years old is CHILD, PRESCHOOL. Children
D003550 Cystic Fibrosis An autosomal recessive genetic disease of the EXOCRINE GLANDS. It is caused by mutations in the gene encoding the CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR expressed in several organs including the LUNG, the PANCREAS, the BILIARY SYSTEM, and the SWEAT GLANDS. Cystic fibrosis is characterized by epithelial secretory dysfunction associated with ductal obstruction resulting in AIRWAY OBSTRUCTION; chronic RESPIRATORY INFECTIONS; PANCREATIC INSUFFICIENCY; maldigestion; salt depletion; and HEAT PROSTRATION. Mucoviscidosis,Cystic Fibrosis of Pancreas,Fibrocystic Disease of Pancreas,Pancreatic Cystic Fibrosis,Pulmonary Cystic Fibrosis,Cystic Fibrosis, Pancreatic,Cystic Fibrosis, Pulmonary,Fibrosis, Cystic,Pancreas Fibrocystic Disease,Pancreas Fibrocystic Diseases
D003692 Delayed-Action Preparations Dosage forms of a drug that act over a period of time by controlled-release processes or technology. Controlled Release Formulation,Controlled-Release Formulation,Controlled-Release Preparation,Delayed-Action Preparation,Depot Preparation,Depot Preparations,Extended Release Formulation,Extended Release Preparation,Prolonged-Action Preparation,Prolonged-Action Preparations,Sustained Release Formulation,Sustained-Release Preparation,Sustained-Release Preparations,Timed-Release Preparation,Timed-Release Preparations,Controlled-Release Formulations,Controlled-Release Preparations,Extended Release Formulations,Extended Release Preparations,Slow Release Formulation,Sustained Release Formulations,Controlled Release Formulations,Controlled Release Preparation,Controlled Release Preparations,Delayed Action Preparation,Delayed Action Preparations,Formulation, Controlled Release,Formulations, Controlled Release,Prolonged Action Preparation,Release Formulation, Controlled,Release Formulations, Controlled,Sustained Release Preparation,Timed Release Preparation,Timed Release Preparations
D004041 Dietary Fats Fats present in food, especially in animal products such as meat, meat products, butter, ghee. They are present in lower amounts in nuts, seeds, and avocados. Fats, Dietary,Dietary Fat,Fat, Dietary
D005260 Female Females
D006207 Half-Life The time it takes for a substance (drug, radioactive nuclide, or other) to lose half of its pharmacologic, physiologic, or radiologic activity. Halflife,Half Life,Half-Lifes,Halflifes

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