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[Sustained release cephalexin (S-6436) and genitourinary tract infection (author's transl)].

1) Forty (40) patients with comparatively simply urinary tract infections were orally administered 1 g/day of sustained release cephalexin (S-6436) in two divided doses (after breakfast and dinner) for 7 approximately 14 days, and 20 patients complicated with chronic urinary tract infections or epididymitis were orally given 2 g/day of the drug in two divided doses (after breakfast and dinner) for 7 approximately 28 days. Thirty six (90%) patients of the 40 receiving 1 g/day and seventeen (85%) of the 20 with 2 g/day satisfactorily responded to the drug. 2) Disappearance of organisms was observed in 43 patients (75.4%) of the 57 with urinary tract infections on whom bacteriological examination was conducted. Three (7.0%) of the 43, however, recurred within 7 days after the treatment. In six patients (10.5%) of the 57, the organisms were replaced. 3) Side effects such as gastrointestinal disturbance, allergic reactions, abnormality of blood picture, and impairments of renal and hepatic functions were examined and no such side effects were found except uriticaria in whole body was observed in only one patient with 1 g/day, which disappeared after discontinuation of the administration of the drug.

Adolescent↗

[Clinical efficacy of S-6436 in urinary tract infection (author's transl)].

S-6436 was orally given to the patients mainly with uncomplicated acute cystitis at two divided doses for 7 days with the following results: 1) One or 2g/day of S-6436 were administered to the patients with 93.7% of effectiveness. There is almost no difference in effectiveness between 1 g and 2g dosages. 2) Bacteria in urine disappeared in 74% of the patients treated and superinfection occurred in 22%. The disappearance of the bacteria was observed in 83.3% of the patients with E. coli and 60% with Staph. epidermidis. The superinfection however was observed in 16.5% with E. coli and 33.3% with Staph. epidermidis. The disappearance of bacteria was observed in each one case with Klebsiella, Staph. aureus and Ps. aeruginosa. The superinfection was observed in 2 cases with Proteus. 3) Sensitivity tests on the organisms indicated that 94.4% of E. coli, 40% of Staph. epidermidis, Klebsiella and Staph. aureus were susceptible to the drug but Proteus and Ps. aeruginosa were not susceptible. 4) No remarkable side effects were observed, though digestive was used in several patients. From the above results, S-6436 is considered to be a useful drug which is expected to have as much effectiveness as regular cephalexin at two divided doses after breakfast and dinner.

Adolescent↗

[Clinical experience with sustained release cephalexin (X-6437) (author's transl)].

Oral sustained release cephalexin (S-6437) was administered to 24 pediatric patients. Daily dose used was 18 approximately 60 mg/kg, which was divided into two doses and given after breakfast and dinner. The following are the results of the study. Out of 24 patients, 6 showed very good response, 10 good response, 6 fair, 1 poor and 1 unknown, Ratio of effectiveness was 69.6%. Two patients were reluctant to receive the drug and, therefore, they took other drugs. The other 22 patients, however, were easily given. No remarkable side effects due to S-6437 were found. From the above results, it was recognized that S-6437 has good effectiveness and safety, and it is convenient to give to children because the frequency of the drug administration is only twice a day.

Administration, Oral↗

[Clinical experience with sustained release cefalexin (S-6436) in surgery (author's transl)].

Sustained release cephalexin (S-6436) was studied in 23 outpatients (20 males, 3 females) who visited surgery of our hospital. The summary of the study is as follows: 1) The drug was administered for 2 approximately 8 days and the average was 3.5 days. Clinical effectiveness was 87.0% with the following breakdown: excellent 4, good 16, and poor 3. 2) Causative organisms isolated from the patients showing excellent effectiveness were all staphylococci. 3) No side effects were observed in any patients receiving the drug. From the above results, it is expected that S-6436 has good effectiveness and can be used as a first choice drug to outpatients with mild infections such as superficial infections who want to go to the office or school over their receiving the treatment.

Adolescent↗

[Clinical study of sustained release cephalexin (S-6436, S-6437) in dermatology (author's transl)].

S-6436 or S-6437 was orally administered to 30 patients with bacterial infections including some patients with secondary infections. The following results were obtained: 21 patients had excellent effect, good 5, fair 2 and poor 2. The effectiveness was 86.7%. One gram (potency)/day of sustained release cephalexin was given to most of the patients divided into 2 doses after breakfast and dinner. This b.i.d. regimen was popular among outpatients as well. Staph. aureus isolated from 73.3% of the patients disappeared. Overall bacteriological effectiveness was 72.2%. In only 2 patients, side effects were observed. One had a mild pain in stomach and the other had aggravation of itching in complication of eczema. No abnormalities in laboratory studies which were conducted in some patients were found.

Adult↗

[Dangers of ocusert therapy (author's transl)].

According to many publications, patients who wear Ocusert often loosed their medicamental pocket. We observed a case, who developed an acute angle-block-glaucoma. This was a reason for us, to represent the dangers of Ocusert-therapy. A glaucoma with narrow angle of the anterior chamber should be regarded as a contraindication.

Aged↗

Quinidine syncope: torsade de pointes with low quinidine plasma concentrations.

In 2 patients without clinically significant ischemic heart diseases, oral quinidine was used to control supraventricular arrhythmias. In both patients, syncopal attacks occurred, caused by a particular type of ventricular tachyarrhythmia called torsades de pointes. Quinidine plasma concentrations were low (2.6 and 1.2 mg/1, respectively); QRS duration was normal, but the Q-T interval was markedly prolonged.

Aged↗

[Zollinger-Ellison syndrome treated medically by an inhibitor of H2 histamine receptors].

Metiamide an histamine H2-receptors antagonist has been used to treat a case of Zollinger-Ellison syndrome characterized by a long standing diarrhea, an important gastric hypersecretion and a moderatly elevated plasma gastrin but without digestive ulceration. At the dose of 600 mg per day, Metiamide induced a complete suppression of acid secretion, an effect which lasted for 15 days after stopping the drug. Accordingly and since the only finding at time of laparotomy was a small lymph node enlarged with endocrine metastatic tissue, the stomach was left intact and Metiamide pursued. During the first 4 months of chronic administration of Metiamide, acid secretion was maintained at levels below 25 p.cent of initial values. Ulteriorly however, although dosages of Metiamide were increased, acid hypersecretion resumed and a duodenal ulcer developed. Total gastrectomy was then performed 11 months after the beginning of Metiamide. In spite of the failure of Metiamide treatment, the long term follow up of this case of Zollinger-Ellison Syndrome, allowed us to get theoretical and practical informations.

Adult↗

[Drug-drug interactions (author's transl)].

This short outline of drug-drug interactions does not claim to cover the entire field. The task of this paper is to illustrate the most important principles of drug-drug interactions by paradigms taken from the experience of the practitioner. One consequence of drug-drug interactions is the change in pharmacolinetic parameters important for the therapeutical effect of drugs in the organism. Very often the elucidation of the mechanisms of drug-drug interactions in man is impossible; therefore, for clinical pharmacologists experiments on animals remain the tool in order to gain more knowledge in this field.

Age Factors↗

[Galenical possibilities and problems in protraction of drug effects (author's transl)].

In recent years, dosage forms with sustained release have obtained a significant importance. The technological possibilities for manufacturing are described as coating, embedding and matrix procedures. The range of auxiliary substances, which are responsible for the retardation of drug activity, reaches from lipophilic compounds as lipoids, fatty alcohols and compounds which are forming hydrogels as cellulose derivatives and natural polysaccharides to synthetic polymers derived from acrylic acid. The formulation of the dosage forms requires particular care in respect to the amount of initial and maintenance doses. On account of technological processes, for example during manufacturing of tablets, under certain circumstances the liberation rate is altered. In vitro test methods allow comparisons only then when the results can be counter-checked by in vitro experiments. The release of drug follows different mechanisms, which are described, entirely or in part, to be reactions following the time law of zero or first order. In special cases, a linear correlation is observed as a function of square root of time. The calculation of given special equations for events within the dosage form is feasible from blood-level values.

Biological Availability↗

[The influence of neuroleptic drugs on urinary excretion of non-protein nitrogen (author's transl)].

During treatment with thioxanthenes or phenothiazines of schizophrenic patients non-protein nitrogen in urine was measured. The values were calculated in relation to the excretion of creatinine. a) Flupentixol or fluphenazine applied in optimal dosage, increased the excretion of urea and the amino acids asp, glu + gln, and gly. b) Moreover, if the drug induced a parkinsonoid (thioridazine) the excretion of ser and thr was increased, too. The usual desalting procedure by ion-exchanging resins before chromatography increases the contents of several amino acids, e.g. asp, asn, ala, gly, cys, ser, thr, indicating a breakdown of some instable products.

Amino Acids↗