Severe psychotic exacerbation during combined treatment with aripiprazole/haloperidol after prior treatment with risperidone.

Objective: Aripiprazole is a new generation antipsychotic drug that shows a partial agonistic activity at D(2) and 5-HT(1A) receptors. This might lead in some cases to an exacerbation of psychotic symptoms due to dopamine agonism.

Methods: We report the case of a 39-year-old woman with an ICD-10 defined schizoaffective disorder.

Hyponatraemia during psychopharmacological treatment: results of a drug surveillance programme.

Hyponatraemia (HN) can be a life-threatening medical condition which may lead to severe neurological and psychiatric symptoms. The AMSP (Arzneimittelsicherheit in der Psychiatrie) is a multicentre drug surveillance programme that assesses severe or new adverse drug reactions during psychopharmacological treatment in psychiatric inpatients. We report on a total of 263 864 psychiatric inpatients monitored from 1993 to 2007 in 80 psychiatric hospitals in Germany, Switzerland and Austria.

[Celecoxib in the symptomatic treatment of active osteo- or rheumatoid arthritis. Results of a post-marketing surveillance].

Background And Objective: The introduction of cyclooxygenase (COX)-2 selective drugs now offers physicians the possibility of a adequate analgesic and anti-inflammatory therapy. Drug induced side effects typically associated with NSAIDs are reduced. Using a post-marketing surveillance study (PSS) efficacy and tolerability of the COX-2-selective drug Celecoxib was evaluated.

Relative bioavailability and bioequivalence study of theophylline sustained release formulations.

The objective of this study was to determine the bioequivalence of two theophylline (CAS 58-55-9) sustained release formulations containing 400 mg (Theophyllin 400 retard Heumann, formulation A) and 375 mg (formulation C) theophylline, respectively. In addition, the relative bioavailability of the sustained release formulations in comparison to an oral solution (formulation B) was investigated. Twenty-four healthy male volunteers participated in the open randomized three-way crossover study.

Nonsteroidal antiinflammatory drugs and a selective cyclooxygenase 2 inhibitor uncouple mitochondria in intact cells.

Objective: Uncoupling of isolated mitochondria by nonsteroidal antiinflammatory drugs (NSAIDs) has been considered relevant to the development of gastrointestinal (GI) side effects. We investigated the occurrence of NSAID-induced uncoupling of mitochondria in intact cells (rat thymocytes) compared with the effects of a selective cyclooxygenase 2 (COX-2) inhibitor.

Methods: Oxygen consumption and mitochondrial membrane potential were simultaneously measured amperometrically and by distribution of radioactive tracer molecules, respectively, in the presence and absence of pharmacologically relevant concentrations of the NSAIDs indomethacin and diclofenac and the selective COX-2 inhibitor SC-236.

Analysis of formulation and food effect on the absorption of metoclopramide.

Objectives: Assessment of the relative and absolute bioavailability of immediate release and sustained release formulations of metoclopramide. Assessment of the effect of a high-fat meal on the pharmacokinetics of sustained release metoclopramide.

Material And Methods: In a balanced 4-way crossover study in 16 healthy male volunteers, a sustained release (SR) formulation of metoclopramide was compared with a solution for injection (A) and an immediate release tablet (B).

The effect of tasuldine, a bronchosecretolytic agent, on mucus rheology and clearability and the interaction with acetylcholine in ferrets.

Tasuldine (Ts) is an orally active bronchosecretolytic agent shown to be clinically effective in human studies. Tasuldine decreases the sialomucin content of the mucus and, in animal studies, this modulation of the glycopeptide correlates with decreased mucus viscosity. The aim of this study was to evaluate the effect of tasuldine on mucus viscoelasticity and correlate the rheological changes to mucociliary and cough clearability.

Sensitive high-performance liquid chromatographic determination of arbidol, a new antiviral compound, in human plasma.

A highly sensitive and selective HPLC method was developed and validated for the determination of arbidol in human plasma. The method involves the liquid-liquid extraction of drug and internal standard from plasma with tert.-butyl methyl ether followed by evaporation and reconstitution in mobile phase.

Investigation on the bioequivalence of 2 oral preparations containing spironolactone and furosemide.

The bioequivalence of 2 formulations containing spironolactone and furosemide was determined. The test preparation was Spironolacton 50 plus Heumann tablets, a new generic spironolactone preparation, developed by Heumann Pharma GmbH, the reference preparation was Osyrol 50-Lasix capsules, Hoechst AG. The study was designed as a randomized 2-period, 2-sequence, crossover study.

Analysis of metabolites--a new approach to bioequivalence studies of spironolactone formulations.

The aldosterone antagonist spironolactone undergoes extensive and complex biotransformation. For investigation of bioequivalence of 2 oral spironolactone formulations, Spironolacton 50 Heumann and Aldactone 50, the pharmacokinetics and bioequivalence of the parent drug and 2 predominant active metabolites, canrenone and 7 alpha-thiomethylspirolactone, were determined in a 2-way crossover study in 24 young healthy male volunteers after multiple oral dosing of 100 mg once daily. Plasma samples were measured by a newly developed HPLC assay and individual pharmacokinetic parameters of the 3 compounds were calculated by use of noncompartmental techniques.

Improved high-performance liquid chromatographic determination of amoxicillin in human plasma by means of column switching.

A highly sensitive and selective HPLC method was developed for the determination of amoxicillin in human plasma. After addition of buffer and internal standard, the sample was ultrafiltered and injected on to a precolumn to remove polar plasma interferences. Detection was effected with a UV detector set at 230 nm.

Sensitive determination of nitrofurantoin in human plasma and urine by high-performance liquid chromatography.

A highly sensitive and selective HPLC method was developed and validated for the determination of nitrofurantoin in human plasma and urine. The method involves the liquid-liquid extraction of drug and internal standard from plasma with ethyl acetate followed by evaporation and reconstitution in mobile phase. Urine samples were simply diluted with purified water.

Improved determination of sulfadiazine in human plasma and urine by high-performance liquid chromatography.

A high-performance liquid chromatographic method for the determination of sulfadiazine in human plasma and human urine was developed and validated. The method involves the acid extraction of drug and internal standard from plasma with ethyl acetate followed by evaporation and reconstitution in mobile phase. Urine samples were simply diluted with purified water.

Pharmacokinetics and bioavailability of different formulations of aciclovir.

The pharmacokinetics and bioavailability of aciclovir (CAS 59277-89-3) were examined after administration of newly developed 200 mg and 400 mg tablets. Two studies, each with 24 subjects of either sex, were performed. In the three-way study I, two different tablets containing 200 mg of aciclovir (test and reference products) and a short infusion of 250 mg aciclovir were compared.

New, high-sensitivity high-performance liquid chromatographic method for the determination of acyclovir in human plasma, using fluorometric detection.

A high-performance liquid chromatographic method for the determination of acyclovir in human plasma has been developed. It is the first published chromatographic method capable of determining acyclovir in plasma with sufficient sensitivity and for sufficiently long periods of time following oral administration of a standard dose of acyclovir during pharmacokinetic investigations. Following precipitations of the proteins with perchloric acid, the sample is chromatographed with a strongly acidic mobile phase on a reversed-phase column, and is then subjected to fluorometric detection (excitation 260 nm, emission 375 nm).

Putative mechanisms of cytoprotective effect of certain antacids and sucralfate.

An investigation of cytoprotective activity of certain antacids and inert particles was carried out by treating ethanol-induced gastric mucosal damage in rats in order to clarify possible mechanisms by which aluminum-containing antacids act. Al(OH)3 inhibited gastric mucosal damage in a dose-related and time-dependent manner. Neither aluminum ions themselves nor the particle size of the Al(OH)3 complex were responsible for the observed cytoprotection, since neither AlCl3, chemically inert Al2O3*C, nor sea sand showed protective effects.

Effects of sodium salicylate on elimination kinetics of indomethacin and bile production in dogs.

We investigated the effects of sodium salicylate on the elimination kinetics of indomethacin in bile duct-cannulated beagles. Indomethacin and metabolites were quantified by HPLC in plasma, bile, and urine. Indomethacin was administered as iv bolus injection and iv infusion to yield a steady-state plasma concentration of approximately 1 microgram/ml.

Bioavailability and pharmacokinetics of rectally administered metoclopramide.

The absolute and relative bioavailability of metoclopramide following the administration of a single suppository--test (Gastrosil) and reference preparations--containing 20 mg of the pure drug or after i.v. injection of 17.

Suitability of long-acting metoclopramide for prophylaxis of chemotherapy-induced delayed nausea and vomiting.

Delayed nausea and emesis are common after cancer chemotherapy, especially cisplatin-containing regimens. Often no, or inadequate, prophylactic antiemetic cover is prescribed in these usually ambulant patients. Metoclopramide is a very effective drug in preventing the acute emetic and nauseating effects of cisplatin.

Oral bioavailability of atenolol.

The bioavailability of two formulations of atenolol was compared in an open, randomized crossover study. Each film-coated tablet contained 100 mg of active drug. The plasma concentrations of atenolol were determined using a newly developed and specific high-performance liquid chromatography procedure.

Effect of an aluminium-hydroxide containing antacid on the oral bioavailability of pirenzepine.

The effect of an antacid containing aluminium-hydroxide, magnesium-hydroxide and calcium carbonate (Trigastril) on the bioavailability of orally administered pirenzepine (Gastricur) was evaluated in 10 subjects in a double-blind single dose cross-over study. Pirenzepine was assayed in plasma by a highly sensitive high-performance liquid chromatographic method. A 2-compartment model was taken as a basis for the calculation of the plasma concentration curves and the pharmacokinetic parameters.

Gastric prostaglandin E2 release induced by aluminium hydroxide and aluminium hydroxide-containing antacids in rats. Effect of low doses and citric acid.

Suspensions of aluminium hydroxide or a commercial antacid containing aluminium hydroxide (Trigastril) was instilled intragastrically in rats in doses comparable to high and low human therapeutic doses (aluminium hydroxide, 125 mg and 12.5 mg/kg, respectively). Corresponding experiments were carried out with 0.