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Biomedical subjects

E Lampa

Publications and source records attributed to E Lampa.

At least 19 recordsLinked to original sources
PubMed2005

Alternative therapy of earth elements increases the chondroprotective effects of chondroitin sulfate in mice.

The administration of mineral sulphur water is an alternative experimental approach for the treatment of rheumatic diseases, such as osteoarthritis (OA), that cause the degeneration of bone and cartilage and sufferance to the patients. Chondroitin sulfate (CS) is a symptomatic slow acting nutropeucital agent currently used in molecular therapy of OA. Therefore, we have studied the role and efficacy of the selective soil paste from the mineral sulphur enriched spring (mud)-therapy alone or in combination with CS in the treatment of OA. The study was performed on 40 C57 Black 6N mice, an experimental model which spontaneously develop an osteoarthritic process. The animals were divided in 4 groups and were treated with the single agents or with the combination. After 30 days of treatment all the mice were sacrificed and right knees and blood were collected. It was found that CS determined a reduction of radiological and histological features of chondrodegeneration and that mud-therapy increased the effects of CS in the animal group treated with the combination. However, the effects of thermal therapy alone were not statistically significant. Since OA is characterized by an increase of the production of nitric oxide (NO) by chondrocytes in extracellular matrix with its consequent elevation in serum and synovial fluid, we have evaluated the effects of the treatments on serum NO levels. CS alone induced a statistically significant reduction of NO serum levels (90+/-13 micromM vs 219+/-60 microM of control group, P<0.05) while mud-therapy alone induced a not statistically significant reduction of serum NO (170+/-62 microM, P>0.05). However, the latter strongly potentiated the decrease of serum NO induced by CS (31+/-1.5 microM) with a high statistical significance if compared to both the control group (P<0.01) and the CS-treated group (P<0.05). In conclusion, this study demonstrates that mud-therapy with sulphur mineral water could represent an important phase of the therapeutic strategy of OA. This experimental strategy could integrate and potentiate the standard pharmacological tools. Moreover, we have set a valid experimental in vivo model for the study of the thermal effects on the development of OA.

Animals↗
PubMed1999

Bioequivalence assessment of two different tablet formulations of diltiazem after single and repeated doses in healthy subjects.

The study was performed on 14 healthy volunteers in order to compare the pharmacokinetics and hence assess the bioequivalence of two different tablet formulations of diltiazem administered orally. The study was carried out after single doses (60 mg) and repeated doses (60 mg three times a day for six days and 60 mg on the seventh day) according to a randomised, cross-over, open design. The pharmacokinetic parameters AUC0-infinity (ng h/ml), Tmax(h) and Cmax (ng/ml) were calculated for the two formulations after a single dose, while AUCt1-t2 (= AUC for a repetitive dose interval or dosing cycle, ng h/ml) and PTF (peak trough fluctuation) were calculated after repeated doses. The bioequivalence assessment was the shortest 90% confidence interval for the ratio (difference) of expected medians in the respective bioequivalence range (0.80-1.20). The results of this study show that, after either a single dose or repeated doses of test or reference formulations of diltiazem, the pharmacokinetics of the two formulations are similar. The ratios of AUC on day 1 (for single-dose treatment) and on day 7 (for repeated-dose treatment), and the corresponding 90% confidence intervals demonstrate bioequivalence between the two formulations of diltiazem within the accepted range of 0.80-1.20 (80-120%).

Adult↗
PubMed1998

Synthesis of 1-methyl-4-(N-aroyl)-piperidinamides with anti-inflammatory and analgesic activities.

Two series of 1-methyl-4-(N-aroyl)-piperidinamides were synthesized and evaluated for their anti-inflammatory and analgesic properties, as well as for their gastrointestinal irritation liability. A non-aromatic derivative, 1-methyl-4-(N-cyclohexanoyl)-piperidinamide, was synthesized and evaluated in order to obtain a more exhaustive knowledge of the structure-activity relationship.

Amides↗
PubMed1998

Bioavailability of timolol and aceclidine after ocular instillation in the rabbit.

The bioavailability of timolol and aceclidine after the ocular instillation of each drug (timolol 0.5% or aceclidine 2%) or both combined (timolol 0.5% + aceclidine 2%) has been evaluated in rabbits. 15 male albino rabbits were treated by the instillation of timolol and aceclidine alone or combined in the conjunctival sac of the right eye. Timolol concentrations in humor aqueous were assayed at 10 min, 30 min, 1 hr, 2 hr, 4 hr and 6 hr after instillation by high-performance liquid chromatography (HPLC). Aceclidine was assayed by a pharmacodynamic method: pupillary diameter at the following time intervals 0 (basal value), 1 min, 5 min, 30 min, 1 hr, 2 hr, 4 hr, 6 hr after treatment. Our results demonstrated that no differences in timolol and aceclidine bioavailability were found between simple-drug preparations and their combination.

Administration, Topical↗
PubMed1997

[Problems associated with the use and monitoring of cyclosporin. Experience at a Clinical Pharmacology Service].

BACKGROUND: A study on cyclosporine A (CyA) monitoring in the January 1992-December 1995 period is reported. The aim of this work was to give epidemiological data on the use of CyA, to verify the progressive increase of CyA determinations and to evaluate the use in other diseases as well as to compare the different technics of CyA assay in blood samples, to stress the timing of blood samples and to underline the CyA monitoring importance. METHODS: The CyA dosage was evaluated by fluorescence polarization immunoassay (FPIA) and high-performance liquid chromatography (HPLC). RESULTS: The study showed that 70% of CyA determinations come from patients undergone to renal, bone marrow and liver transplantations; the remaining 30% was associated to other diseases (psoriasis, uveitis, diabetes, rheumatoid arthritis). CONCLUSIONS: The results obtained showed a progressive and constant increase of CyA determinations. Moreover, the use of drug was increased in autoimmune diseases. It is stressed that CyA monitoring in blood samples is essential to optimize the therapeutic efficacy of drug and minimizing its toxicity.

Autoimmune Diseases↗
PubMed1994

Cobalt blocks L-glutamate-induced apnea and arterial hypotension in the nucleus tractus solitarii of anaesthetized rats.

The local application of cobalt reversibly blocks calcium-channel conductance and therefore synaptic transmission. In this study pretreatment with a solution of cobalt (100 mM) in the nucleus tractus solitarii (NTS) of anaesthetized rats significantly blocked the apnea (P < 0.01) and arterial hypotension induced by L-glutamate (25 mM) and N-methyl-D-aspartate (0.4 mM) microinjected in the NTS. We conclude that cobalt causes these effects by acting at the postsynaptic level.

Anesthesia↗
PubMed1994

Wizards and scientists: the pharmacologic experience in the Middle Ages.

During the Dark ages, Greco-Roman science survived in the eastern Roman Empire and the most important advances in pharmacology and pharmacy were made in Byzantium. As the Arab empires spread in the 7th and 8th centuries, they incorporated earlier learning, and the most important contribution of Arabic medical writers was probably the introduction of formularies to aid in the preparation of medicines. In turn, the later spread of Arabic knowledge to the West introduced little-known plants and fostered an interest in collecting and cultivating them, and also introduced the palatable dose forms preferred by the Arabic doctors. In the West, however, the Christian Church taught a doctrine of unquestioning faith, and despite the centers of learning, e.g. at Salerno, most ordinary people depended on the healing power of faith, religious relics and traditional folk medicine. Hydrology was also well developed in the Middle Ages. The formularia that survive describe many indigenous plants, but with few illustrations. Their gathering and preparation is generally guided by magic ceremonies and ritual, and plants often took their properties from their habitat, e.g. the wayside plantain was thought good for tired or wounded feet. Concepts of therapeutic plants were also influenced by alchemy and were linked to related metals and planets.

Byzantium↗
PubMed1994

Synthesis and pharmacological activities of ethyl 5-cyano-1,6-dihydro-6-oxo-2-(2,3,4-pyridyl)-3-pyridinecarboxylates and derivatives.

The synthesis of ethyl esters of 5-cyano-1,6-dihydro-6-oxo-3-pyridinecarboxylic acids carrying as 2-substituent the 2-,3- or 4-pyridyl group is described. By alkaline hydrolysis followed by acidification, these esters gave the corresponding carboxylic acids, which were decarboxylated to 1,2-dihydro-2-oxo-6-(2,3,4-pyridyl)-3-pyridinecarbonitriles. As milrinone analogues, the above compounds were tested on contractile activity and frequency rate of spontaneously beating atria from reserpine-treated guinea-pigs. Ethyl 5-cyano-1,6-dihydro-6-oxo-2-(2-pyridyl)-3-pyridinecarboxylate showed an appreciable positive inotropic activity, although inferior to that of milrinone; moreover, some other compounds bearing the above 2-substitution pattern showed interesting antiinflammatory, analgesic and hypotensive activity.

Analgesics↗
PubMed1994

Effects of dietary vitamin D deficiency on the cardiovascular system.

Experiments were performed on normotensive rats exposed to vitamin D deficient and control diets from the 22nd to the 180th day of age. In 60-120- and 180-day-old rats. The following parameters were evaluated: a) The vasomotor responses elicited by receptor agonists in the absence and in the presence of the respective antagonists [L-norepinephrine (NE) before and 5 min after prazosin; L-isoprenaline (I) before and 5 min after DL-propranolol; L-dopamine (DA) before and 5 min after L-sulpiride or SCH 23390 or chlorpromazine; acetylcholine (Ach) before and 5 min after atropine; histamine (H) before and after chlorpheniramine; 5-hydroxytryptamine (5-HT) before and 5 min after methysergide or ketanserin]; by carotid-sinus baroreceptor stimulation (CO) before and 5 min after hexamethonium, and by electrical stimulation of the vagus peripheral head (V) before and after atropine; b) Reflex tachycardia elicited by bilateral carotid occlusion (CO) (for 40 sec) and by sodium nitroprusside; c) Catecholamine (norepinephrine, epinephrine) and arginine-vasopressin plasma levels; d) Cholesterol, triglyceride and electrolyte (Na+, K+, Cl-, Ca2+) serum levels. Our results showed that vitamin D deficient diets induced a decrease in pressor responses to NE and CO, and an increase in hypotensive responses to I, DA, Ach, H, 5-HT and V. Changes of arterial blood pressure, heart rate, catecholamine and arginine-vasopressin plasma levels were not observed. Cholesterol, triglyceride and electrolyte (Na+, K+, Cl-) serum levels were not modified, while Ca2+ serum levels decreased. In conclusion, our data suggest that vitamin D depletion can induce changes of pressor and depressor vasomotor responses and suppose a direct role for vitamin D in regulating vasomotor reactivity.

Animals↗
PubMed1993

Clinical pharmacokinetics of theophylline during co-treatment with ticarcillin plus clavulanic acid in patients suffering from acute exacerbation of chronic bronchitis.

The effect of ticarcillin/clavulanic acid, taken for 7 days as vials containing 1000 mg of ticarcillin and 200 mg of clavulanic acid twice daily intramuscularly, on the steady-state pharmacokinetics of theophylline was studied in 12 patients suffering from acute exacerbation of chronic obstructive pulmonary disease. Initially, patients were treated for four days with theophylline as sustained-release formulation in the amount of 600 mg daily; on the last day, blood samples were taken for theophylline determination. Theophylline concentrations were measured serially for 12 hours by the method of polarized immunofluorescence (Abbott TDx system). Subsequently, while theophylline was continued at the same dosage, each patient received in addition ticarcillin/clavulanic acid vials every 12 hours. After seven days of this combined medication, the serial assays of plasma were repeated at the same time intervals as before. No influence of ticarcillin/clavulanic acid was detectable on the steady-state theophylline pharmacokinetics. It is concluded that both drugs can be administered concomitantly without any dosage adjustment of theophylline.

Bronchitis↗
PubMed1993

Ondansetron, an antagonist of 5-HT3 receptors, in the treatment of antineoplastic drug-induced nausea and vomiting in children.

The aim of this study was to evaluate the efficacy and safety of ondansetron, an antagonist of 5-hydroxytryptamine type 3 (serotonin 3) (5-HT3) receptors, in controlling nausea and vomiting induced by antineoplastic therapy in children affected by cancer. Six patients affected by nausea and vomiting due to antineoplastic drugs were treated with ondansetron (4 mg/m2). Urinary samples for the assay of serotonin and 5-hydroxy-indoleacetic acid (5-HIAA) were collected 24 hr before antineoplastic drug treatment, 24 hours after the start of antineoplastic therapy and, 24 hr after the start of ondansetron therapy. All patients were affected by nausea and vomiting within two to four hr after the antineoplastic treatment. Urinary concentrations of serotonin and 5-HIAA were higher and statistically significant (P < 0.01) with respect to basal values. Treatment with ondansetron significantly reduced the number of episodes of nausea and vomiting, as well as the urinary values for serotonin and 5-HIAA.

Antineoplastic Combined Chemotherapy Protocols↗
PubMed1993

N-acyl-4,7,7-trimethyl-N-phenyl-3-(1-piperidinyl or dimethylamino)bicyclo[2.2.1]hept-2-ene-2-carbothioamides with platelet antiaggregating and other activities.

A series of N-acyl-4,7,7-trimethyl-N-phenyl-3-(1-piperidinyl or dimethylamino)bicyclo[2.2.1]hept-2-ene-2-carbothioamides was prepared in excellent yields by reaction of 4,7,7-trimethyl-N-phenyl-3-(1-piperidinyl or dimethylamino)bicyclo[2.2.1]hept-2-ene-2-carbothioamides with a number of aromatic or heterocyclic acyl chlorides in dry pyridine solution and in the presence of sodium hydride. Some of the above compounds showed a platelet antiaggregating activity in vitro superior or comparable to that of acetylsalicylic acid; moreover, some compounds exhibited moderate analgesic, antiinflammatory and hypotensive activities in mice or rats.

Acetylcholine↗
PubMed1993

2H-1-benzopyran derivatives with platelet antiaggregating and other activities.

The synthesis of some N,N-disubstituted 4-amino-5,6,7,8-tetrahydro-3,6- diphenyl-2H-1-benzopyran-2-ones by reaction of phenylchloroketene with a series of N,N-disubstituted 2-aminomethylene-4-phenylcyclohexanones, followed by dehydrochlorination in situ of the primary adducts with DBN, is described. Some compounds showed a platelet antiaggregating activity in vitro superior or comparable to that of acetylsalicylic acid and an appreciable antiarrhythmic activity, as well as weak anti-inflammatory and local anesthetic activities in rats and mice.

Aconitine↗
PubMed1993

Effects of some cephalosporins and teicoplanin on platelet aggregation.

Antibiotics may interfere with platelet (PLT) function, and beta-lactam antibiotics may interact with PLT aggregation, by inhibiting the binding of agonists of this aggregation (such as ADP and collagen) to specific receptor sites. In this study we have evaluated the relative in-vitro antiplatelet effects of some old and new cephalosporins (cefonicid, ceftazidime, ceftriaxone, cefotaxime, cefuroxime and flomoxef) and of teicoplanin, a new glycopeptide antibiotic. All the cephalosporins tested, and also teicoplanin, were found to have the potential to adversely affect human platelet aggregation only at high concentrations which are not achieved in vivo.

Adenosine Diphosphate↗
PubMed1993

Synthesis and pharmacological activity of imidazo[2,1-b]benzothiazole acids.

We have prepared twelve imidazo[2,1-b]benzothiazole carboxylic and acetic acids by reaction of substituted 2-aminobenzothiazoles with ethyl bromopyruvate and 4-chloroacetoacetate, respectively. The acids, obtained from esters by hydrolysis, were tested for their antiinflammatory, analgesic and ulcerogenic activities.

Animals↗
PubMed1992

Participation of arginine vasopressin-mediated and adrenergic system-mediated mechanisms in the hypertension induced by intracerebroventricular administration of NMDA in freely moving rats.

Effects of intracerebroventricular (third ventricle) injection of N-methyl-D-aspartate (NMDA) on arterial blood pressure, on heart rate, on arginine vasopressin (AVP) and levels of catecholamines in plasma and on the behaviour of normotensive freely-moving rats have been evaluated. N-Methyl-D-aspartate significantly (P less than 0.01) increased arterial blood pressure and levels of catecholamines and AVP in plasma. With 0.1-1.0 micrograms/rat all animals presented psychomotor agitation, stereotyped movements, hyperexcitability, exophthalmus, dyspnoea, jumping, rearing and teething. The selective antagonist for NMDA receptors, 2-APV injected in the third ventricle, significantly (P less than 0.01) antagonized the hypertension, the increase in levels of catecholamines and AVP in plasma and behavioural effects. An antagonist of alpha 1 adrenergic receptors, prazosin (i.v.), an agonist of alpha 2 adrenergic receptors, clonidine (i.c.v.) and a relatively selective antagonist of V1 subtype of receptor of AVP, CGP 25838 (i.c.v. and i.v.), 15 min before NMDA, significantly (P less than 0.01) decreased the effects induced by the injections of NMDA. On the contrary, an antagonist of opiate receptors, naloxone (i.v.), 15 min before NMDA, significantly (P less than 0.01) increased the NMDA-induced modifications. Pretreatment with the antagonists at these doses, did not significantly modify the basal values of arterial blood pressure and behaviour. Only 2-APV sometimes induced ataxia, lasting about 5 min. This study points out an increase in the central sympathetic efferent activity and in release of AVP involved in the NMDA-induced cardiovascular and behavioural effects.

2-Amino-5-phosphonovalerate↗