Pharmacokinetics of theophylline in young children with asthma: comparison of rectal enema and suppositories. 1979

P Bolme, and P O Edlund, and M Eriksson, and L Paalzow, and B Winbladh

Six children, aged 2 months - 4 years, received theophylline 5-6 mg/kg intravenously. Its disposition could be described by a two-compartment open model, the mean serum half life (t 1/2 beta) was 3.75 h, i.e., shorter than in adults, but there was a considerable interindividual variation (1.8-7.0 h, in one patient 13.3 h). Thirteen children (2 months - 4 years) received theophylline suppositories in a dose of 3.8-5.0 mg/kg, and ten (6 months - 4 years) in a dose of 8.4-14.5 mg/kg. Absorption was slow (mean half-time 43 min), incomplete and variable (biological availability 8-100%, mean 80%). Only four of the patients given the higher dose and none given the lower dose reached a therapeutic serum concentration (10-20 microgram/ml). Nine children (6 months - 4 years) received rectal enemas of theophylline 4.1-9.2 mg/kg. Absorbtion was rapid (mean half-time 5.5 min) and biological availability averaged 100%. Six patients reached a serum concentration within the therapeutic range. Using the mean values of the calculated pharmacokinetic parameters, rectal enemas providing a dose of theophylline of 6-8 mg/kg t.i.d. were computed to give serum concentrations between 8-20 microgram/ml, without producing too high a level during the absorption phase.

UI MeSH Term Description Entries
D007223 Infant A child between 1 and 23 months of age. Infants
D007275 Injections, Intravenous Injections made into a vein for therapeutic or experimental purposes. Intravenous Injections,Injection, Intravenous,Intravenous Injection
D007700 Kinetics The rate dynamics in chemical or physical systems.
D012007 Rectum The distal segment of the LARGE INTESTINE, between the SIGMOID COLON and the ANAL CANAL. Rectums
D002675 Child, Preschool A child between the ages of 2 and 5. Children, Preschool,Preschool Child,Preschool Children
D004733 Enema Insertion of a solution or compound through the RECTUM with the purpose of cleansing the COLON or for diagnostic procedures. Enemata,Enemas,Enematas
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D000367 Age Factors Age as a constituent element or influence contributing to the production of a result. It may be applicable to the cause or the effect of a circumstance. It is used with human or animal concepts but should be differentiated from AGING, a physiological process, and TIME FACTORS which refers only to the passage of time. Age Reporting,Age Factor,Factor, Age,Factors, Age
D001249 Asthma A form of bronchial disorder with three distinct components: airway hyper-responsiveness (RESPIRATORY HYPERSENSITIVITY), airway INFLAMMATION, and intermittent AIRWAY OBSTRUCTION. It is characterized by spasmodic contraction of airway smooth muscle, WHEEZING, and dyspnea (DYSPNEA, PAROXYSMAL). Asthma, Bronchial,Bronchial Asthma,Asthmas
D013488 Suppositories Medicated dosage forms that are designed to be inserted into the rectal, vaginal, or urethral orifice of the body for absorption. Generally, the active ingredients are packaged in dosage forms containing fatty bases such as cocoa butter, hydrogenated oil, or glycerogelatin that are solid at room temperature but melt or dissolve at body temperature. Rectal Suppositories,Vaginal Suppositories,Vaginal Suppository,Suppositories, Rectal,Suppositories, Vaginal,Suppository, Vaginal

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