Oral administration of terbutaline in asthmatic patients. 1984

E Ripe, and Y Hörnblad, and K Tegnér

The absorption and excretion profiles of orally administered terbutaline were investigated in 10 asthmatic patients who received a solution containing 5 mg of [3H]terbutaline sulphate. Bronchodilating effect and side-effects were followed. The mean serum concentration curve reached its maximum of 3.0 +/- 0.3 (SEM) ng/mL at 60-90 min. Renal clearance data indicated that terbutaline was excreted only via glomerular filtration. Approximately 30% of the dose was excreted in the urine in 12 h and 40% in 72 h. Three compounds appeared in the urine: unchanged terbutaline, a sulphate conjugate, and a glucuronide, the main metabolite being the sulphate conjugate. The maximum mean increase in volume of air expelled in the first second of forced expiration (FEV1) was 35%, attained 90-120 min after intake of terbutaline. There was a correlation (r = 0.74) between the serum level and the bronchodilator effect. No significant effects on heart rate or blood pressure were found. Tremor, as objectively measured with the aid of an accelerometer, was experienced by the patients when it increased to twice its basal level. The observed tremor did not appear to parallel either the serum level or the bronchodilating effect. A comparative study in 3 of the patients showed that [3H]terbutaline formulated as a tablet had similar bioavailability.

UI MeSH Term Description Entries
D008657 Metabolic Clearance Rate Volume of biological fluid completely cleared of drug metabolites as measured in unit time. Elimination occurs as a result of metabolic processes in the kidney, liver, saliva, sweat, intestine, heart, brain, or other site. Total Body Clearance Rate,Clearance Rate, Metabolic,Clearance Rates, Metabolic,Metabolic Clearance Rates,Rate, Metabolic Clearance,Rates, Metabolic Clearance
D001794 Blood Pressure PRESSURE of the BLOOD on the ARTERIES and other BLOOD VESSELS. Systolic Pressure,Diastolic Pressure,Pulse Pressure,Pressure, Blood,Pressure, Diastolic,Pressure, Pulse,Pressure, Systolic,Pressures, Systolic
D005541 Forced Expiratory Volume Measure of the maximum amount of air that can be expelled in a given number of seconds during a FORCED VITAL CAPACITY determination . It is usually given as FEV followed by a subscript indicating the number of seconds over which the measurement is made, although it is sometimes given as a percentage of forced vital capacity. Forced Vital Capacity, Timed,Timed Vital Capacity,Vital Capacity, Timed,FEVt,Capacities, Timed Vital,Capacity, Timed Vital,Expiratory Volume, Forced,Expiratory Volumes, Forced,Forced Expiratory Volumes,Timed Vital Capacities,Vital Capacities, Timed,Volume, Forced Expiratory,Volumes, Forced Expiratory
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
D006339 Heart Rate The number of times the HEART VENTRICLES contract per unit of time, usually per minute. Cardiac Rate,Chronotropism, Cardiac,Heart Rate Control,Heartbeat,Pulse Rate,Cardiac Chronotropy,Cardiac Chronotropism,Cardiac Rates,Chronotropy, Cardiac,Control, Heart Rate,Heart Rates,Heartbeats,Pulse Rates,Rate Control, Heart,Rate, Cardiac,Rate, Heart,Rate, Pulse
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D000284 Administration, Oral The giving of drugs, chemicals, or other substances by mouth. Drug Administration, Oral,Administration, Oral Drug,Oral Administration,Oral Drug Administration,Administrations, Oral,Administrations, Oral Drug,Drug Administrations, Oral,Oral Administrations,Oral Drug Administrations
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
D001711 Biotransformation The chemical alteration of an exogenous substance by or in a biological system. The alteration may inactivate the compound or it may result in the production of an active metabolite of an inactive parent compound. The alterations may be divided into METABOLIC DETOXICATION, PHASE I and METABOLIC DETOXICATION, PHASE II.
D013726 Terbutaline A selective beta-2 adrenergic agonist used as a bronchodilator and tocolytic. Arubendol,Asthmoprotect,Brethaire,Brethine,Bricanyl,Bricanyl SA,Butaliret,Butalitab,Contimit,KWD-2019,Monovent,Taziken,Tedipulmo,Terbasmin,Terbul,Terbutalin AL,Terbutalin Stada,Terbutalin-ratiopharm,Terbutaline Sulfate,Terbuturmant,terbutalin von ct,KWD 2019,KWD2019,Terbutalin ratiopharm

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