ABSTRACT
Groups of 5 fasting male and female patients aged 32-83 years were each given 3 gm of the cholecystographic contrast medium iosumetic acid in micronized form (particle size less than 20 mum); Group I with 150 ml tea (standard administration); Group II with 500 ml tea; Group III with 150 ml tea plus 10 mg metoclopramide (Paspertin) 5 min p. admin. i.v.; and Group IV with 150 ml tea and 3 gm sodium bicarbonate. Blood samples were taken in the period up to 6 hours after administration in order to determine the iodine concentration according to the method of Juegst and Stauch. In Groups I and II maximum blood levels were reached 2.1 +/- 0.4 or 2.0 +/- 0.4 h p. admin. respectively, in Group III 1.6 +/- 0.2 h p. admin (in comparison to Group I: p less than 0.05) and in Group IV the maximum level was reached after only 0.9 +/- 0.2 h p. admin. The difference between Group IV and the other three groups is statistically significant (p less than 0.01). A half-life of 0.3 +/- 0.1 h was calculated for absorption in Group IV.
Subject(s)
Cholecystography , Contrast Media/metabolism , Intestinal Absorption , Iodobenzenes/metabolism , Administration, Oral , Adult , Aged , Bicarbonates , Female , Gastric Juice/metabolism , Humans , Male , Metoclopramide , Middle Aged , TeaABSTRACT
Meglumin-Iodrinat has been synthesized as the contrasting part of Myelografin by Schering AG. and tested for lumbar Myelography in animal experiments. The excellent neural and general compatibility justified a first clinical trial. 200 patients were examined, 100 each with following upright or lying down positions. There were no local symptoms, no signs of spinal or cerebral irritation. This is seen to be the main advantage compared with drugs used so far. Intensity of contrast corresponded with that of Conray 60 and Dimer X. The most common complaints like headache and nausea were interpreted as CSF hypotension and can be clearly reduced by lying down. Also the concentration of the contrastmedium diminishes more rapidly with the patient lying down.
Subject(s)
Contrast Media/adverse effects , Lumbar Vertebrae/diagnostic imaging , Posture , Animals , Dogs , Drug Tolerance , Haplorhini , Humans , Myelography/methods , Papio , Rabbits , SolubilityABSTRACT
The oral antidiabetic agent 1-(hexahydro-1-H-azepin-1-yl)-3-(p-[2-(5-methyl-isoxazol-3-carboxamido)-ethyl]-phenylsulfonyl)-urea (glisoxepide, BS 4231, Pro-Diaban¿) was studied in a multi-centre open clinical trial comprising 4337 patients and was found to be an effective therapeutic agent for maturity-onset diabetics. About 66% of the patients had been pre-treated with oral antidiabetics. 54.7% of those 3572 patients treated with Pro-Diaban for at least 3 months achieved stabilization, which was classified according to strict criteria as "good", 73.4% achieved at least "satisfactory" stabilization. 12.5% of the cases dropped out after having received at least 12 mg/day because of inadequate efficacy of Pro-Diaban; 51.9% of these patients dropped out in the first 3 months (early failures 6.9% of the total case number). 61.9% received their daily dose in one portion, 29% in two and 10% in three portions. 98% received maximally 16 mg, 70% maximally 8 mg, and 42% 4 mg per day. Hypoglycaemic episodes led in 0.9% to a termination of the trial. In 1.22% of the cases the trial was terminated because of side effects, in 0.18% of cases they consisted of allergic or suspected allergic complaints and in 0.69% they consisted mainly of gastro-intestinal symptoms. Of the side-effects which did not lead to a termination of the trial, dizziness, headache and nausea were the relatively more frequent symptoms. An analysis of the laboratory data under consideration of pathological and normal initial and subsequent values showed that under the influence of Pro-Diaban pathological data reverted to normal more frequently than initially normal values changed to pathological ones. The analysis of laboratory and blood pressure data from 4 subgroups of patients, e.g. patients with diseases of the liver or the kidneys and hyperlipaemic or hypertensive patients, revealed that those data of special interest in each subgroup had mostly improved or remained unchanged under Pro-Diaban.
Subject(s)
Diabetes Mellitus/drug therapy , Sulfonylurea Compounds/therapeutic use , Aged , Blood Glucose/metabolism , Body Weight/drug effects , Clinical Trials as Topic , Diabetes Complications , Diabetic Angiopathies/blood , Diabetic Nephropathies/blood , Drug Administration Schedule , Drug Hypersensitivity , Female , Humans , Hyperlipidemias/blood , Hypertension/blood , Liver Diseases/blood , Male , Middle Aged , Sulfonylurea Compounds/administration & dosage , Sulfonylurea Compounds/adverse effectsABSTRACT
The time course of 1-butylbiguanide concentration in plasma and the urinary and fecal elimination of the substance were measured in six female elimination of the substance were measured in six female diabetic patients after oral administration of 100 mg of 14C-1-butylibiguanide hydrochloride as Sindiatil. The mean maximum plasma concentration was 37 mug/100 ml and was reached after about 2 1/2 h. At least semi-maximum plasma concentrations (greater than or equal 18 mug/100 ml) were maintained between the 1st and 8th h after administration. Within 24 h 64% of the administered dose were eliminated (36% via the kidneys, 28% with the faeces). After 3 days a total of 80% had been eliminated, one-half each in urine and faeces, respectively. The average time taken for 50% of maximum renal elimination, and thus of the absorbed quantity, to be excreted was 7.2 h.
Subject(s)
Biguanides/blood , Buformin/blood , Diabetes Mellitus/blood , Aged , Buformin/administration & dosage , Delayed-Action Preparations , Female , Humans , Kinetics , Middle AgedABSTRACT
A double blind comparison between Ioglycamid (Bilivistan) and the new I-V cholegraphic medium Iotroxamid (proposed trade name Chologram) is reported. Chologram produces better pictures and it is better tolerated. Pharmaco-kinetic data are published for the first time.
Subject(s)
Biliary Tract/diagnostic imaging , Iodobenzoates , Ioglycamic Acid , Triiodobenzoic Acids , Chemical Phenomena , Chemistry , Cholangiography , Cholecystography , Humans , Ioglycamic Acid/adverse effects , Triiodobenzoic Acids/adverse effects , Triiodobenzoic Acids/analogs & derivatives , Triiodobenzoic Acids/metabolismABSTRACT
Gliflumide is an optically active sulfonylaminopyrimidine. In rats, the drug exhibited a long-lasting hypoglycemic effect following oral as well as intravenous administration. This effect resembled the action of glibenclamide, but was brought about by doses 5-10 times lower. In healthy volunteers, oral administration (0.0125 mg/kg) or intravenous injection (0.01mg/kg) of gliflumide resulted in a 30-40 per cent decrease of blood glucose characterized by slow onset and long duration. The stimulation of insulin secretion was studied after intravenous injection of gliflumide (0.01 mg/kg) and compared to the action of glibenclamide (0.01 mg/kg) and tolbutamide (10 mg/kg). Although the effect of these doses, measured by the area above the initial level, was similar, a different time course of action was found. Gliflumide and glibenclamide, compared with tolbutamide, produced a delayed and prolonged response. These characteristics were more pronounced with gliflumide. Maximal serum insulin levels were found after 3, 23, and 90 minutes for tolbutamide, glibenclamide, and gliflumide, respectively. In maturity-onset diabetics requiring glibenclamide or glibenclamide + biguanide, gliflumide was shown to have about the same efficacy as glibenclamide, the corresponding doses being 1.5-5 (generally 3) times lower.
