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Biomedical subjects

A Filippelli

Publications and source records attributed to A Filippelli.

At least 73 records · Page 4Linked to original sources

Aminoethers of (+)-1,3,3-trimethyl-2-oxabicyclo[2.2.2]-octan-6-hydroxyimine with hypotensive activity. II.

The synthesis of a series of N-substituted 3-amino-2-hydroxypropyl ethers (III a-1) starting from (+)-1,3,3-trimethyl-2-oxabicyclo [2.2.2]-octan-6-hydroxyimine is described. Some of these compounds showed a remarkable hypotensive and a weak bradycardic activity in rats, as well as a moderate local anesthetic activity in mice. All compounds were found to be devoid of antiarrhythmic activity in rats and of beta-blocking activity in dogs.

Adrenergic beta-Antagonists↗

Derivatives of 1,2,3,3-tetramethyl-2-azabicyclo-[2.2.2]octan-5-trans-ol with antiarrhythmic and other activities. VI.

The synthesis of a series of alkyl and aryl amides (IV) starting from 5-trans-(3-aminopropoxy)-N-benzyl-1,2,3,3-tetramethyl-2-azabicyclo [2.2.2] octane is described. Some of compounds (IV) showed a moderate hypotensive activity in rats and infiltration anesthesia in mice. Effects on heart rate in rats and antiarrhythmic activity in mice were practically absent.

Anesthetics, Local↗

Pharmacological properties of a new non-steroidal anti-inflammatory drug: flunoxaprofen.

The anti-inflammatory, analgesic and antipyretic activities of S-(+)-2(4-fluorophenyl)-alpha-methyl-5 benzoxazole acetic acid (flunoxaprofen: Flu), a new non-steroidal anti-inflammatory drug, were compared with those of indomethacin and other non-steroidal anti-inflammatory drugs (NSAIDs) in experimental animals. Flu showed strong inhibitory activity on acute and subacute inflammation tests in rats, such as carrageenin hind paw oedema (oral: 6-25 mg/kg; rectal: 50-100 mg/kg); pellet-induced granuloma formation (5-20 mg/kg/day) and adjuvant-induced arthritis (10 mg/kg/day). Its potency was comparable with that of indomethacin (I) and higher than that of acetyl salicylic acid (ASA), ibuprofen (IBU) or phenylbutazone (P). The analgesic activity of Flu, evaluated by the hot plate method and tail pinching in mice, was slightly lower than that of I but higher than that of ASA and IBU. In pyretic rabbits Flu showed an antipyretic activity higher than that of ASA and IBU. The ability of Flu to affect platelet aggregation, mucopolysaccharide synthesis by fibroblasts and the proteolytic action of trypsin was also investigated.

Animals↗

Cardiovascular and respiratory effects of spermidine and spermine: an experimental study.

Spermidine (SPD) and spermine (SPM) produced in anaesthetized dogs significant cardiovascular changes at higher doses than other transmitters, i.e. l-noradrenaline, l-adrenaline, histamine, acetylcholine, which produce cardiovascular effects at doses of 0.01-0.05 micrograms/kg given intravenously. SPD was shown to be more active than SPM. The hypotensive response observed after i.v. injection is due to histamine release. The hypotensive and bradycardic effects observed after microinjection of SPD into III cerebral ventricle or into the vertebral artery and of SPM into the vertebral artery are due to an increase in parasympathetic output. Spermidine increased and spermine decreased the baroreceptor reactivity. SPD and SPM did not change the vascular beta- and alpha-adrenergic, cholinergic and histaminergic receptor reactivity.

Animals↗

Cardiovascular effects of 15(S) 15 methyl-PGF2 alpha.

The effects of 15(S) 15-methyl-PGF2 alpha were studied on the cardiovascular system of dogs. Intravenous and intravertebral artery administration of 15(S)-methyl-PGF 2 alpha induced arterial hypertensive and respiratory effects more intense and longer lasting than those observed for PGF2 alpha. Intravenous administration of 15(S) 15-methyl-PGF2 alpha induced a decrease of vascular reactivity to 1-norepinephrine and 1-epinephrine and to carotidal occlusion. Infiltration of the carotid sinus walls with 15(S) 15-methyl-PGF2 alpha decreased the baroreceptor reactivity.

Animals↗

Fructose-1,6-diphosphate (FDP), hemodynamics and heart metabolism: preliminary experimental studies.

Fructose-1,6-diphosphate (FDP) has been reported to exert beneficial effects on several cardiac functions. We studied the effects of FDP on the biochemical and dynamic functions of the heart in anesthetized dogs. Significant effects of FDP were noted mostly as related to pyruvate and lactate metabolism. The results seem to indicate that FDP may improve heart metabolism, and coronary function in restricted animals.

Animals↗

Aging and in vitro vascular responses to endothelin-1 in several rat strains.

The endothelins are a recently discovered family of potent contractile peptides produced by endothelial cells. These peptides have been suggested to play an important role in the pathogenesis of hypertension, myocardial infarction, cardiogenic shock, and so on. The aim of our study was to compare the responses to endothelin-1 (ET-1) with those to L-noradrenaline (NA) in aortic rings from rats of different strains and ages. Thoracic aorta rings from spontaneously hypertensive (SHR), Wistar Kyoto (WKY), Brown Norway (BN) and spontaneously hyperlipemic (Yoshida, YOS) rats 2-4 (young), 6-8 (adult) and 20-25 (old) months old were used. There were no changes in the pD2 values for ET-1 and NA between WKY and SHR rats at the ages studied. The ET-1 and NA Emax in adult SHR rats was significantly lower than in the age-matched WKY animals. Old age reduced the ET-1 and NA Emax in both SHR and WKY rats abolishing the difference observed at 6-8 months in the same groups. The reactivity to ET-1 and NA of BN and YOS rats was modified only in young rats. In YOS strain aging did not modify the ET-1 and NA responses as the pD2 and Emax values remained unchanged. Our findings demonstrate that ET-1 is a more potent vasoconstrictor than NA and that this potency remains unchanged throughout the ages and the pathologies studied. In contrast, the pD2 of NA decreases with old age in SHR and WKY rats. We conclude that rat strain but not hypertension or hyperlipemia can modify the response to ET-1 or NA in old age. We suppose that this functional change may involve alterations in the responsiveness of vascular smooth muscle.

Aging↗

Management of hypertension by general practitioners: an Italian observational study.

Data on patients receiving antihypertensive therapy were collected from 20 general practitioners (GPs) in Campania, Italy, to determine the prescription of different antihypertensive classes and their use with other drugs for concomitant diseases, to investigate the main factors influencing antihypertensive choice, to document treatment outcome, and to assess adverse drug reactions (ADRs). Each GP completed a data card for each consultation that produced an antihypertensive prescription; 1900 cards were collected. The most frequently used antihypertensives were angiotensin-converting enzyme inhibitors (49.6%), calcium antagonists (24.8%), beta blockers (11.7%), angiotensin II-receptor blockers (5.5%), and alpha blockers (0.9%). In 82% of patients, blood pressure was reduced but did not reach normotensive levels. The choice of antihypertensive treatment was influenced by international guidelines (56%), clinical diagnosis (25%), concomitant diseases (8%), cost (4%), compliance (3%), and other factors (5%). ADRs--most often cough (35.7%), edema (22.7%), headache (13.3%), and tachycardia (7.8%)--occurred in 11.8% of patients.

Antihypertensive Agents↗

Self-prescribed laxative use: a drug-utilization review.

This study was conducted to determine the reasons for the choice of self-prescribed laxatives and to acquire information on how they were used and tolerated. From November 1999 to February 2000, 70 pharmacies, uniformly located throughout the Campania region of southern Italy, distributed a questionnaire to purchasers of over-the-counter laxatives. The average age of the (mostly female) respondents was 45.9 years; 23.8% were elderly. Among the 7324 individuals who completed the survey, 77.6% selected an oral product; 22.4% preferred rectal administration. A physician influenced the choice of a laxative in 37.7% of the cases, a pharmacist in 20.5%; other suggestions came from relatives (14%), acquaintances (12.1%), advertisements (11.7%), and miscellaneous sources (4%). Only 59.8% of respondents used these drugs correctly, and 58.2% consulted a physician or pharmacist because of constipation. Adverse effects, mainly gastrointestinal symptoms, occurred in 6.1% of those surveyed. The long-term use or abuse of laxatives can cause serious medical consequences, as well as mask diseases, delaying diagnosis and appropriate treatment. Physicians, pharmacists, and other health-care personnel should counsel patients on the proper use of these easily available, ubiquitous drugs.

Adolescent↗

Over-the-counter oral nonsteroidal anti-inflammatory drugs: a pharmacoepidemiologic study in southern Italy.

The Pharmacoepidemiologic Service of the Second University of Naples analyzed the use and tolerability of over-the-counter (OTC) oral nonsteroidal anti-inflammatory drugs (NSAIDs) purchased in Campania, a region of southern Italy. Forty private pharmacies uniformly distributed throughout the region were recruited. The study was conducted by means of a questionnaire completed by purchasers and lasted from December 1, 1999 to March 31, 2000; 2,053 questionnaires were collected. The age of respondents averaged 45.3 +/- 3.49 years (range, 17-85 years). The NSAIDs analyzed were acetylsalicylic acid, paracetamol, ibuprofen, ketoprofen, diclofenac, and piroxicam. Adverse effects, mainly gastrointestinal symptoms, were reported by 5.5% of the users and occurred primarily with diclofenac, piroxicam, ibuprofen, and ketoprofen. Because the use and availability of OTC NSAIDs are increasing, further studies of the tolerability of this important drug class are warranted.

Adolescent↗