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PubMed1983

[Effects of 3 varieties of antisickling substances measured by ektacytometry as a function of oxygen pressure].

The ektacytometer measures with precision the deformability of erythrocytes during a continuous change in oxygen tension. Automation of the instrument renders easily feasible the evaluation of proposed antisickling compounds. Drugs representative of the three modes of action presently recognized have been selected: those which increase oxygen affinity (potassium cyanate); those which inhibit hemoglobin polymerization (butylurea); membrane-active compounds. An anionic phenothiazine (metiazinic acid) had an interesting activity on deformability.

Antisickling Agents↗

PubMed1990

Development and validation of an automated enzyme assay for paracetamol (acetaminophen).

A rapid, enzymatic assay for serum or plasma paracetamol has been developed with the potential for adaptation to a wide range of clinical analysers. The method involves the action of an amidase enzyme to produce 4-aminophenol from paracetamol, which in turn reacts with 8-hydroxyquinoline in the presence of manganese ions to form a blue dye. Two stable reagents are used and excellent precision is achieved over the drug concentration range 0-2.5 mmol/l. The method, which is complete within 6 min, has been validated using a Monarch centrifugal analyser and shows no significant interference from endogenous serum compounds, drugs or paracetamol metabolites.

Acetaminophen↗

PubMed2004

National survey of the impact of drug shortages in acute care hospitals.

PURPOSE: The impact of drug shortages on patient care, the resources used to manage drug shortages, and the cost associated with drug shortages were studied. METHODS: A national online survey was conducted to quantify the effects of drug shortages on patient care and pharmacy expenses. Directors of pharmacy in acute care institutions in the ASHP member database were asked to estimate the impact of drug shortages on acquisition costs, pharmacist and nonpharmacist staff time dedicated to specific functions related to drug shortages, and drug-compounding expenses. RESULTS: Usable responses were received from 370 (24.7%) of 1496 pharmacy directors. Nearly all pharmacy directors surveyed believed that shortages had changed practice, and a majority felt that drug shortages had compromised patient care. Hospital pharmacy personnel devoted a significant amount of time to managing drug shortages. The results suggest that shortages increase the acquisition cost of pharmaceuticals in the United States by over dollar 99 million annually. CONCLUSION: A national survey indicated that drug shortages are having a significant impact on patient care activities and finances in hospitals.

Data Collection↗

PubMed2005

Mutations in the Pneumocystis jirovecii DHPS gene confer cross-resistance to sulfa drugs.

Pneumocystis jirovecii is a major opportunistic pathogen that causes Pneumocystis pneumonia (PCP) and results in a high degree of mortality in immunocompromised individuals. The drug of choice for PCP is typically sulfamethoxazole (SMX) or dapsone in conjunction with trimethoprim. Drug treatment failure and sulfa drug resistance have been implicated epidemiologically with point mutations in dihydropteroate synthase (DHPS) of P. jirovecii. P. jirovecii cannot be cultured in vitro; however, heterologous complementation of the P. jirovecii trifunctional folic acid synthesis (PjFAS) genes with an E. coli DHPS-disrupted strain was recently achieved. This enabled the evaluation of SMX resistance conferred by DHPS mutations. In this study, we sought to determine whether DHPS mutations conferred sulfa drug cross-resistance to 15 commonly available sulfa drugs. It was established that the presence of amino acid substitutions (T(517)A or P(519)S) in the DHPS domain of PjFAS led to cross-resistance against most sulfa drugs evaluated. The presence of both mutations led to increased sulfa drug resistance, suggesting cooperativity and the incremental evolution of sulfa drug resistance. Two sulfa drugs (sulfachloropyridazine [SCP] and sulfamethoxypyridazine [SMP]) that had a higher inhibitory potential than SMX were identified. In addition, SCP, SMP, and sulfadiazine (SDZ) were found to be capable of inhibiting the clinically observed drug-resistant mutants. We propose that SCP, SMP, and SDZ should be considered for clinical evaluation against PCP or for future development of novel sulfa drug compounds.

Amino Acid Substitution↗

PubMedDate not supplied

[The character of development of the immune response to sheep erythrocytes and parallel responses to exo- and endobiotics].

The immune response to sheep erythrocytes (SE) is usually used as the indicator system in screening of immunotropic compounds. We had shown earlier that a rapid immune reaction develops in response to a chemical compound (drug). It is characterized by an increase in the number of antigen-recognizing and antigen-producing lymphocytes and their blast forms, titers of antibodies specific of the introduced compound and endobiotics mobilized under its effect.

Animals↗

PubMed2003

Efflux transporters of the human placenta.

The use of pharmaceuticals during pregnancy is often a necessity for the health of the mother. Until recently, the placenta was viewed as a passive organ through which molecules are passed indiscriminately between mother and fetus. In reality, the placenta contains a plethora of transporters, some of which appear to be specifically dedicated to removal of xenobiotics and toxic endogenous compounds. Drug efflux transporters such as P-glycoprotein (P-gp), several multidrug resistant associated proteins (MRPs) and breast cancer resistant protein (BCRP) may provide mechanisms that protect the developing fetus. Bile acid transporters may also play a role in exporting compounds back into the maternal compartment. Steroid hormones directly influence the level of expression and function in some of these transporters. Investigating the link between the hormones of pregnancy and these drug efflux transporters is one possible key in developing strategies to deliver drugs to the mother with minimal fetal risk.

ATP Binding Cassette Transporter, Subfamily B, Mem↗

PubMedDate not supplied

Some pharmacological properties of new analogs of MP 3022, the 5-HT1A receptor antagonist.

Two new analogs of full 5-HT1A receptor antagonist 4-[3-(1-benzotriazolyl)propyl]-1-(2-methoxyphenyl)piperazine (MP 3022; 1) containing di- (5) or tetramethylene- (6) spacer were synthesized. In the radioligand binding studies, compounds 5 and 6 showed high 5-HT1A (Ki = 14.7 nM and 11.8 nM, respectively) and low 5-HT2 receptor affinity (Ki = 2,696 nM and 389.2 nM, respectively). In behavioral studies both compounds behaved like postsynaptic 5-HT1A receptor antagonists as they reduced lower lip retraction and behavioral syndrome induced by 8-OH-DPAT (5-HT1A receptor agonist) in rats, but 6 was more effective in these tests. Derivative 5 did not affect body temperature in mice, whereas 6 decreased it. Furthermore, 5 did not change hypothermia induced by 8-OH-DPAT, and 6-induced lowering of body temperature in mice was not antagonized by (S)-WAY 100135 (5-HT1A antagonist), so in that model 5 and 6 did not behave as antagonist or agonist, respectively, at presynaptic 5-HT1A receptors. Compound 6 was studied in behavioral tests used to predict a potential anxiolytic (conflict drinking test in rats) and antidepressant (forced swimming test in rats) activity. Diazepam and imipramine were used as reference drugs. Compound 6 significantly increased the number of shocks accepted in water-deprived rats in conflict drinking test and shortened the immobility time in forced swimming test in rats. The above findings indicate that new 5-HT1A postsynaptic antagonist 6 behaves like anxiolytic and antidepressant, but mechanisms of these properties of 6 remain unknown.

8-Hydroxy-2-(di-n-propylamino)tetralin↗

PubMed2006

Incorporation of a monolithic column into sequential injection system for drug-protein binding studies.

A sequential injection analysis (SIA) manifold was incorporated with a monolithic strong anion-exchanger disk for on-line drug-protein interaction studies. The antibiotic ciprofloxacin (CF) was selected as a model drug compound. The separation principle was based on the strong retention of bovine serum albumin (BSA) on the monolithic strong anion-exchanger and the liberation/release of the free form of the drug. Elution of the retained BSA was easily achieved by delivering a different mobile phase via the SIA manifold. The type of functional group of the monolithic support, the breakthrough volume and the injected volumes of CF and BSA were studied and optimized. The influence of the variation of incubation time was studied in on-line binding assays. Scatchard plot was employed to obtain the number of binding sites and the equilibrium binding constants. For the off-line study of the CF-BSA binding, two binding classes were determined with constants of (3.16+/-0.21)x10(6)M(-1) and (1.27+/-0.48)x10(4)M(-1) and 6.1+/-1.3 and 17.8+/-3.9 binding sites per class, respectively. In non-equilibrium binding experiments the binding rate constant was k(1)=785 M(-1)min(-1). All measurements were monitored with fluorescence (lambda(ext)=300 nm, lambda(em)=460 nm) and spectrophotometric detection (lambda=280 nm). To evaluate the accuracy of the developed method the obtained results were compared versus ultrafiltration experiments and were found in good agreement.

Anion Exchange Resins↗

PubMed1999

Substituted amylose as a matrix for sustained drug release.

PURPOSE: Amylose derivatives form an important group of polymers, and many of them can be used as drug sustained-release systems. METHODS: Substituted amylose can be prepared in a 1-step reaction with substituent(s) in a basic medium. The substituents can be represented as (A-R), where (A) serves an epoxy, halide or suitable organic or inorganic function reacting with hydroxyl groups located on the amylose chain, and (R) is an organic radical. RESULTS: The present work shows the synthesis of different polymers and the effect of different (A) and/or (R) and their different degrees of substitution (n) on the sustained drug release from matrix tablets prepared by direct compression. CONCLUSIONS: SA polymers are interesting excipients for the preparation of controlled drug release tablets.

Acetaminophen↗

PubMed1996

Bioavailability and stability of microencapsulated ferrous sulfate in fluid milk: studies in mice.

Iron deficiency is the most important nutritional problem all over the world. Fluid milk is an attractive vehicle for iron fortification, since it is a food with a high nutritional value, accessible to the whole population and easy to be given to children. Fortification of this food with iron has the disadvantage of the interaction of the iron with the constitutive elements of milk, diminishing its bioavailability and changing its sensorial properties, making it unacceptable. Nowadays, this problem can be overcome by the implementation of a new technological procedure, which consists in the microencapsulation of the ferrous sulfate with lecithin, thus avoiding the interaction of iron with the food. The absorption obtained in mice for milk-ferrous sulfate was 7.9 +/- 3.2%, while for microencapsulated ferrous sulfate-milk the result was 11.6 +/- 4.5%. Comparing these data with those obtained with the ferrous ascorbate in water 13.1 +/- 4.9% and ferrous sulfate in water 13.2 +/- 4.3%, both of them considered as reference standards, no statistically significant difference between them and the microencapsulated ferrous sulfate in milk can be observed. However, this difference becomes significant (p < 0.01) when these products are compared to the non-encapsulated ferrous sulfate in milk. On the other hand, we demonstrated that this product is stable to heat-processing (100 degrees C, 30 min) and storage at a room temperature up to 6 months that lacteous products are usually submitted to.

Absorption↗

PubMed1991

A need to intensify drug surveillance in Germany.

Despite all its limitations, the spontaneous reporting system still forms the basis for drug safety assessments in the Federal Republic of Germany. Although there have been some promising attempts to standardise the methodology of detecting, analysing and evaluating adverse drug events (ADEs) in certain clinico-pharmacological institutes and psychiatric departments, the approaches have not been integrated and are used only locally. The only exception is the Freiburg Documentation Centre for Severe Skin Diseases, which is attempting comprehensive, country-wide documentation of toxic epidermal necrolysis (Lyell's syndrome) and Stevens-Johnson syndrome. We show that surveillance of 40% of all hospital beds would allow the acquisition of reliable data even on rare and serious AEs which could then be extrapolated in a statistically meaningful way. The medical societies in Germany have traditionally taken a leading role in establishing standards for the preclinical and clinical investigation of new drug compounds. We suggest that they also make it their task to define the framework for an intensified adverse events monitoring system, since it is the patient who ultimately benefits from a quantification of drug therapy risks.

Bed Occupancy↗

PubMed1998

Peroral sustained-release film-coated pellets as a means to overcome physicochemical and biological drug-related problems. I. In vitro development and evaluation.

In vitro preformulation testing has shown that the solubility and dissolution rate of the model drug compound ucb 11056 are highly pH dependent. Considering this, different sustained-release (SR) oral dosage forms of ucb 11056 were developed aiming to obtain the most constant and complete release of the drug during transit in the gastrointestinal (GI) tract. Classical approaches based on the use of SR formulations such as hydrophilic matrix tablets or pellets coated with one film-forming polymer (Eudragit NE30D or L30D-55) did not fulfill all expectations on the basis of their in vitro evaluation, i.e., the drug release and pattern remained highly dependent on the pH of the dissolution medium. Therefore, taking advantage of the flexibility of release adjustment obtainable from coating of pellets with different kinds of pH-sensitive film layers, a quite satisfactory pH independence of the release characteristics was obtained using formulation blends of neutral and anionic acrylic polymers. For the selected SR pellets batch 15 coated with NE30D/L30D-55 (7:3), the tridimensional topographic representation of the drug release versus time and pH showed that, notwithstanding the pH-dependent aqueous solubility of the drug, the release profiles were relatively homogeneous for any pH value ranging between 1 and 7.

Acrylic Resins↗

PubMed1990

A possible case of drug-induced familial pemphigus.

Two sisters developed pemphigus vulgaris and pemphigus erythematosus within 3 years. The diagnosis was confirmed by clinical, histologic and immunofluorescent antibody studies. One of the sisters experienced a common cold before the pemphigus developed and displayed a positive macrophage migration inhibition (MIF) test to a combination drug compounded of paracetamol, caffeine, chlorpheniramine maleate and phenylephrine HCl, which she had received 2 weeks prior to the appearance of the cutaneous lesions. It is suggested that her pemphigus was triggered by the drug. Although the patient had a strong genetic and familial predisposition to pemphigus, her clinical symptoms did not become evident until they were activated through an exogenous factor, namely, the causative drug. This case offers an example of a possible interaction between endogenous, genetic factors, and exogenous, triggering factors in the development of full-blown disease.

Acetaminophen↗

PubMed1990

The challenge of health care developments for hospital pharmacy.

The traditional role of hospital pharmacists in drug analysis and drug compounding broadened to a patient-oriented approach during the sixties and seventies. The clinical pharmacy concept was adopted. This practice includes daily-prepared total parenteral nutrition and chemotherapy, sophisticated analgesic systems, individualized drug distribution and specific information. The hospital pharmacy provides aseptic procedures as well as specialized logistics. Clinical pharmacy practice concentrates on tailor-made pharmaceutical care. As home health care usually deals with therapeutic modalities, this approach offers great possibilities for highly skilled out-patient care. Financial and legal interferences and the traditional gap between in-patient care and out-patient care must be removed. Home health care challenges the hospital pharmacists to place his knowledge and abilities at the disposal of this new type of patient care.

Delivery of Health Care↗

PubMed1986

Pharmacokinetics of estulic [corrected] in humans.

Estulic [corrected] given orally without food after overnight fast produces a blood concentration curve with a pronounced second peak that does not appear when the drug is taken with food. A two-compartment open model involving two different time lags is used to study the pharmacokinetics of estulic [corrected] in humans after oral administration. The drug accumulates in a tissue or organ that is well perfused in the first pass transfer. The accumulation appears to occur by a competitive process. The second peak apparently is the result of a rapid release of drug and bioreversible drug compounds from the hepatic-biliary system with subsequent reabsorption. This release may occur spontaneously, but appears to be triggered by food intake. We use an optimization method to characterize the pharmacokinetic profiles of drug for this model. This technique which provides the global minimum of the deviation delta, from the given observations, leads to the optimization of a single variable function. The results are compared with those obtained from the generalized least squares method.

Absorption↗

PubMed2002

Applications of affinity chromatography to the study of drug-melanin binding interactions.

This short review reports on progresses in the study of drug-melanin interactions using the technique of affinity chromatography. Melanins are natural or synthetic pigments derived from the oxidation and polymerization of various precursors including L-dopa, tyrosine and cystein. Accumulation of toxic compounds, drugs, and metal ions in pigmented tissues through reversible binding to melanin has been linked to chronic toxicity. Affinity chromatography using chromatographic stationary phases based on physically adsorbed or chemically bonded melanin provides a useful tool for studying the interactions of small molecules and metal ions with melanin

Chromatography, Affinity↗

PubMed2006

Novel approach to DPI carrier lactose with mechanofusion process with additives and evaluation by IGC.

The effect of lactose carrier surface property on the inhalation profile of dry powder inhaler (DPI) was evaluated using a micronized drug (Compound A) by inverse gas chromatography (IGC). Mechanofusion with magnesium stearate (Mg-St) or sucrose stearate increased the fine particle fraction (FPF), considered to be due to decrease in the interaction between Compound A and the lactose carrier. The effect of Compound A concentration on FPF was smaller in mechanofusion-processed lactose compared to intact lactose, especially when processed with Mg-St. The relationship between the IGC parameters of the lactose and FPF was also investigated. FPF increased as both the dispersive component of the surface energy and acidity similarity between the lactose carriers and Compound A increased. Although further investigation is necessary, it could be suggested that acidity similarity decreases the interaction between Compound A and lactose, thus contributing to the increase in the FPF. In conclusion, (1) mechanofusion with Mg-St or sucrose stearate could be an effective method to improve FPF of a DPI drug formulation; (2) IGC would be a valuable method to investigate the interaction between a drug and the DPI carrier; and (3) a relationship between surface acidity and inhalation profile was suggested.

Chromatography, Gas↗

PubMed2003

Distribution of acidic and neutral drugs in surface waters near sewage treatment plants in the lower Great Lakes, Canada.

Prescription and nonprescription drugs have been detected in rivers and streams in Europe and the United States. Sewage treatment plants (STPs) are an important source of these contaminants, but few data exist on the spatial distribution of drugs in surface waters near STPs. Samples of surface water were collected in the summer and fall of 2000 at open-water sites in the lower Great Lakes (Lake Ontario and Lake Erie), at sites near the two STPs for the city of Windsor (ON, Canada), and at sites in Hamilton Harbour (ON, Canada), an embayment of western Lake Ontario that receives discharges from several STPs. In a follow-up study in the summer of 2002, samples of surface water and final effluent from adjacent STPs were collected from sites in Hamilton Harbour and Windsor. In addition, surface water and STP effluent samples were collected in Peterborough (ON, Canada). All samples of surface water and STP effluents were analyzed for selected acidic and neutral drugs. In the survey of Hamilton Harbour and Windsor conducted in 2000, acidic drugs and the antiepileptic drug carbamazepine were detected at ng/L concentrations at sites that were up to 500 m away from the STP, but the hydrological conditions of the receiving waters strongly influenced the spatial distribution of these compounds. Drugs were not detected at open-water locations in western Lake Erie or in the Niagara River near the municipality of Niagara-on-the-Lake (ON, Canada). However, clofibric acid, ketoprofen, fenoprofen, and carbamazepine were detected in samples collected in the summer of 2000 at sites in Lake Ontario and at a site in the Niagara River (Fort Erie, ON, Canada) that were relatively remote from STP discharges. Follow-up studies in the summer of 2002 indicated that concentrations of acidic and neutral drugs in surface waters near the point of sewage discharge into the Little River (ON, Canada) STP were approximately equal to the concentrations in the final effluent from the STP. Caffeine and cotinine, a metabolite of nicotine, were generally present in STP effluents and surface waters contaminated by drugs. The antidepressant fluoxetine and the antibiotic trimethoprom were also detected in most STP effluents and some surface water samples. For the first time, the lipid regulating drug atorvastatin was detected in samples of STP effluent and surface water.

Acids↗