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Biomedical subjects

J L Schelling

Publications and source records attributed to J L Schelling.

At least 19 recordsLinked to original sources
PubMed1991

Absence of metabolic effects of the topical carbonic anhydrase inhibitors MK-927 and sezolamide during two-week ocular administration to normal subjects.

Potential systemic effects of the racemic carbonic anhydrase inhibitor MK-927 and its S-enantiomer, sezolamide hydrochloride, after topical ocular administration were investigated in a double-masked, randomized, placebo-controlled study in 16 healthy volunteers. A controlled diet was started 4 days before initiation of treatment and continued throughout the study. For 14 days six volunteers received bilaterally one drop of 2% MK-927 (1.2 mg) q.i.d., six received one drop of 1.8% sezolamide (1.1 mg) q.i.d., and four received the common vehicle q.i.d. Blood and urine electrolytes and acid-base profiles were measured before and on days 1, 7, and 14 of treatment, and 24-hour urine samples were collected daily. All values were compared with those on the pretreatment day. Taking the circadian variations of the parameters into account, no significant treatment effect was observed in either the daily profiles or the 14-day cumulative sodium, potassium, and citrate excretions. Because the usual variability of the measured biologic parameters has been reduced markedly by the stringent requirements of this study, it can be concluded that the induction of clinically significant metabolic changes by topically administered MK-927 or sezolamide is unlikely.

Administration, Topical↗
PubMed1989

Influence of food and antacid administration on fluoride bioavailability from enteric-coated sodium fluoride tablets.

The relative bioavailability of enteric-coated sodium fluoride (NaF) tablets (10 mg F-) has been assessed following administration with a standard calcium-rich breakfast or calcium-poor lunch, and 2 h before or simultaneously with antacid administration (2.4 g aluminum-magnesium hydroxide), versus intake on an empty stomach. Twelve volunteers were studied 3 times according to an open, three-way crossover design over a 24 h period at weekly intervals. Meals were found to decrease the peak serum concentration of NaF from 122 micrograms/L during fasting (after baseline subtraction) to 71 and 88 micrograms/L with breakfast and lunch respectively, and to slow its absorption rate with Tmax increasing from 3.3 to 7.3 and 11.2 hours, without altering its bioavailability. Antacid impaired the bioavailability of NaF by 80% when administered simultaneously, with AUC decreasing from 987 to 155 micrograms.h/L, but had no significant effect when taken 2 h before NaF. In conclusion, the enteric-coated NaF tablets used in this study can be administered with food or after a 2-hour delay following antacid administration, but should not be taken simultaneously with antacid.

Adult↗
PubMed1988

[Dose-response curve and preliminary clinical study of a laxative, lactilol].

15 women complaining of chronic constipation were included in a prospective open trial to determine the laxative action and minimal effective dose of lactitol. Through the administration of increasing doses, an ED50 of 0.25 g/kg/day, was established. During a 15-day treatment period at the minimal effective dose, all patients had reduced symptoms of constipation as compared with a previous 15-day control period. Side effects of minor intensity were frequently recorded (flatulence, rumblings, wind, and, less frequently, abdominal cramps or nausea). Thus, the use of lactitol for symptomatic treatment of constipation deserves further clinical studies to determine better its indications and benefit.

Adult↗
PubMed1988

Tolerability and pharmacokinetics of L-648,051. A leukotriene D4-receptor antagonist, in healthy volunteers.

Two formulations of L-648,051 (L) were studied [intravenous (i.v.) and aerosol (A)] in two separate trials. Study I (i.v.) involved 4 normal male subjects in a single blind dose ranging study where good systemic tolerability and safety was shown. However, dose dependent local irritation at the injection site was observed at all dose levels (35, 52.5 and 70 mg/5 min infusion). L has a high systemic clearance rate (1.2 1/min), a small volume of distribution (4.41) and a short plasma half-life (2.4 min). Study II (A) involved 16 normal male volunteers who received incremental aerosolized doses of L from 0.1 to 1.6 mg in a double-blind, placebo controlled, dose ranging study. Complaints of mild local irritation or discomfort in the upper respiratory tract were the only significant findings. No dose relationship of these complaints could be shown. In conclusion, L is a safe and well tolerated drug when administered by aerosol. It causes dose related local, but not systemic, adverse experiences when administered i.v. In view of this tolerability and of its demonstrated activity against LTD4-challenge in animals, clinical efficacy studies with the aerosol formulation are warranted.

Adult↗
PubMed1985

[Psychotropic agents in elderly persons].

The response to narcotics, sedatives, hypnotics, antidepressants and antipsychotic drugs is modified in elderly patients. The effects of these drugs are enhanced, and dosage reduction is required. This phenomenon is gradual and occurs before any sign of senile dementia. The choice of a drug within a therapeutic class may depend on the severity of adverse reactions, some of which are particularly disturbing in elderly patients.

Aged↗
PubMed1985

Does renal failure induce a decrease in cyclosporine blood concentrations?

Blood Cys concentrations were monitored twice weekly by RIA in nine patients undergoing renal transplantation. The Cys dose was adapted to obtain blood values between 100-400ng/ml. A negative correlation was found between plasma creatinine and blood Cys, even in those patients in whom the oral dosage was not changed (r = 0.65, n = 23, p less than 0.001). In vitro studies showed no effect of uraemic blood on Cys measurement. It seems probable that uraemia induces changes in distribution volume and/or gastrointestinal absorption of the drug. Careful monitoring of Cys during uraemia is therefore warranted.

Adult↗
PubMed1979

Judgments of trained observers on adverse drug reactions.

Patients (672) admitted to a department of medicine during five consecutive months were followed by an investigator who identified 110 clinical manifestations which could have been considered adverse drug reactions. From these, 42 were excluded because they did not correspond to the definition of adverse reaction or they were inadequately documented. The remaining 68 cases were submitted to three independent observers who had to reply to a series of questions; from these replies five degrees of probability for the reaction itself were deduced. Reactions (54; 49% of the manifestations reported) were considered as certain or probable by at least two observers, but only 27 rections of these (25%) were attributed to the same drug by all three observers. There was a low level of agreement between any two observers (paired agreement ratio: 0.6 to 0.7) and little difference of agreement between any one observer and each of the others (personal agreement ratio: 0.6 to 0.7).

Drug-Related Side Effects and Adverse Reactions↗
PubMed1978

[Frequency of drug prescriptions and their adverse effects in a medical department].

The enquiries carried out in our unit since 1971, in some 1600 patients who received in all more than 13000 drug prescriptions and who were observed during 3 periods whose total duration was 12 months, prompt the following conclusions. The number of adverse reactions in which the relationship of cause and effect with one or several drugs was either definite or probable amounted to 217, 2--3% among patients at admission and 5--11% of patients during their hospital stay. The average number of prescriptions per patient remained stable and the average number of drug reactions per 100 prescriptions varied from 0.6 to 1.6. Severe drug reactions occurred in 1.1% of patients at admission and 1.1% of patients during their hospital stay.

Drug Prescriptions↗
PubMed1978

[Serum and joint levels of cefacetrile during its administration for septic arthritis].

Six patients, five of whom had normal and one impaired renal function, and all suffering from purulent arthritis caused by cephalosporin-sensitive germs, were given a seven-day course of 8 g cephacetrile daily. On the first day, 6 g were administered by continuous intravenous infusion at the rate of 500 mg/h, followed by 2 g over a further 45 min. On days 2 to 7, the patients received 2 short infusions of 4 g each at an interval of 12 h. In four patients with normal renal function, serum half-life ranged from 0.8 to 1.4 h, serum levels during continuous infusion from 19 to 31 microgram/ml, and total clearances from 265 to 434 ml/min. In one patients, these values were 1.6 h, 70 microgram/ml and 131 ml/min respectively (small volume of distribution). The concentrations in the synovial fluid varied from 2 to 29 mcirogram/ml; they were generally lower than the serum levels, but clearly exceeded the minimum inhibitory concentrations for germs commonly present in purulent arthritis. In five patients, the synovial fluid became germ-free and the arthritis was clinically cured. In the case presenting with renal insufficiency, the serum half-life was 5.8 h. During continuous administration, a steady state was not attained; peak serum levels amo9nted to 75 microgram/ml and the total clearance to 61 ml/min. The cephacetrile concentrations in the synovial fluid were very high (26 and 67 microgram/ml). In this case, in which the renal insufficiency associated with mycosis fungoides was present before the treatment, renal function deteriorated futher during treatment while the arthritis improved.

Adolescent↗