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Biomedical subjects

W J Novick

Publications and source records attributed to W J Novick.

32 records · Page 2Linked to original sources
PubMed1978

Fendosal (HP 129): a potent anti-inflammatory and analgesic compound.

Fendosal (HP 129) is one of a series of potent non-steroidal anti-inflammatory agents. Fendosal was compared with aspirin in several anti-inflammatory and analgesic bioassay procedures. Results indicate that fendosal has an anti-inflammatory activity 1.4 times greater than does aspirin in carrageenan-induced rat paw edema. Fendosal is 6.9 to 9.5 times more active than aspirin in the prophylactic and therapeutic adjuvant-induced polyarthritis models of chronic inflammation. The analgesic activity of fendosal is considered to be superior to that of aspirin, with the advantage of a prolonged duration of action. The gastric-irritating properties of fendosal are very low in comparison with those of aspirin. Fendosal has a much wider separation of effective and gastric-irritating doses than does aspirin.

Animals↗
PubMed1978

A comparison of clonidine with morphine for antinociceptive and antiwithdrawal actions.

Clonidine was found to possess dose-dependent analgesic and antiwithdrawal activity. In mice, clonidine prolonged the tail flick latency and inhibited phenylquinone-induced writhing. In rats, it inhibited tail withdrawal from hot water and a pain response to pressure application on an inflamed paw. The effective doses of clonidine were different in the different tests employed, but they were always smaller than those of morphine. Naloxone failed to antagonize the analgesic actions of clonidine but effectively antagonized those of morphine. Phenoxybenzamine also did not alter the inhibition of tail flick-induced by clonidine. Clonidine suppressed morphine withdrawal body shakes in a dose-dependent manner as does morphine. This action of clonidine was not reversed by naloxone. In usual laboratory tests, clonidine appears to be an effective analgesic which antagonizes signs of morphine withdrawal.

Analgesics↗
PubMed1977

Pharmacology of a new non-steroidal, anti-inflammatory agent: 6,11-dihydro-11-oxodibenz [b, e] oxepin-2-acetic acid (HP 549).

HP 549 is an orally effective non-steroidal anti-inflammatory agent with moderate analgesic and antipyretic activity. It is active in adjuvant-induced polyarthritis when given prophylactically or therapeutically. HP 549 also inhibits carrageenan-induced paw edema in the rat, an activity which is not altered by adrenalectomy. The analgesic activity of HP 549 was demonstrated in phenylquinone writhing. However, HP 549 produced variable results in the Randall-Selitto analgesia test. The anti-pyretic activity of HP 549 appears to be weak. HP 549, unlike other pharmacologically active anti-inflammatory drugs, does not produce gastric irritation at effective doses and is 45 times less ulcerogenic than indomethacin. Also the acute therapeutic indices for HP 549 are more favorable than for indomethacin.

Acetates↗
PubMed1976

Absorption, distribution, metabolism, and excretion of furosemide in dogs and monkeys I: analytical methodology, metabolism, and urinary excretion.

35S-Furosemide was administered to beagle dogs and rhesus monkeys in an oral solution on a single and a 20 repeated 5-mg/kg/day dosing regimen. Following the single dose, 25.0% (dogs) and 24.0% (monkeys) of the dose were excreted in the urine in 24 hr. TLC analysis demonstrated that both species had similar excretory patterns; i.e., over 80% of the amount excreted in the urine was present as unchanged durosemide and the remainder was composed of a known metabolite, saluamine, and an as yet unidentified metabolite(s). The repetitive dosing regimen did not appear to alter significantly either the total amount recovered in the 24-hr urine or the excretion pattern. Studies in dogs showed that only 50-60% of furosemide was absorbed from oral solution. A significant biliary secretion elimination pathway for furosemide also was observed.

Animals↗
PubMed1976

Carboxyarylindoles as nonsteroidal antiinflammatory agents.

An extensive series of carboxyarylindoles has been evaluated for antiinflammatory activity in the carrageenin paw edema assay. The requirements for optimal antiinflammatory activity in this series are relatively specific: a central pyrrole nucleus with (a) a 3-carboxy-4-hydroxyphenyl moiety substituted directly on the nitrogen, (b) a 2-phenyl group (R2) with a substituent of low electronegativity, (c) absence of a substituent in the 3 position (R3), and (d) a system fused across the 4,5 positions (X), which is lipophilic, quasiplanar, and does not interact sterically with the N-phenyl group. One derivative, 3-(3-carboxy-4-hydroxyphenyl)-2-phenyl-4,5-dihydro-3H-benz[e]indole (42), has been selected for further study.

Animals↗
PubMedDate not supplied

Effect of blood product medium supplements on the activity of cefotaxime and other cephalosporins against Enterococcus faecalis.

The activities of cefotaxime and other aminothiazoyl oxime cephalosporins against Enterococcus faecalis were enhanced by addition of 5% sheep blood to Mueller-Hinton agar. This effect was not seen with aztreonam (aminothiazoyl oxime monobactam), cefotiam (aminothiazoyl, nonoxime), or other cephalosporins, and it was specific to the syn-configuration of the oxime moiety. Enhancement of cefotaxime activity was demonstrable against approximately 50% of 86 clinical isolates and could only be shown at low bacterial inocula. Human serum, serum alpha 1-, beta- and gamma-globulin fractions and albumin often antagonized or did not affect significantly the antimicrobial activity of cefotaxime, while the alpha 2-globulin fraction usually enhanced drug activity. The in vivo activity of cefotaxime against E. faecalis was examined in a rat peritoneal abscess model. The test organism was resistant to cefotaxime by standard methods (MIC greater than 128 micrograms/ml) but was inhibited by 1.0 microgram/ml when rat serum was presented in the medium. Cefotaxime reduced titers of bacteria within abscesses after 5 days of therapy (5.77 +/- 0.68 log10 CFU/g) in comparison with those in control animals (7.38 +/- 0.28 log10 CFU/g, p less than 0.05). Moxalactam, the in vitro activity of which was not augmented by serum, proved ineffective in the animal model. While these observations do not have direct therapeutic relevance, they offer a possible explanation for the relatively infrequent occurrence of enterococcal superinfection in patients treated with cefotaxime.

Abscess↗
PubMedDate not supplied

Antimicrobial spectrum of cefpirome combined with tazobactam against the Bacteroides fragilis group.

Cefpirome, a so-called fourth-generation cephalosporin, was tested alone and in combination with the sulfone beta-lactamase inhibitor, tazobactam, against 63 members of the Bacteroides fragilis group. The cefpirome MIC50 was only 64 micrograms/ml, but the MIC was reduced eightfold with tazobactam (2:1 ratio). The addition of tazobactam to cefpirome or the use of metronidazole as a codrug appear to be alternative choices to enhance the antianaerobic spectrum. Over 98% of strains had cefpirome-tazobactam MICs of less than or equal to 32 micrograms/ml.

Bacteroides↗
PubMedDate not supplied

Levels of cefotaxime in body fluids and tissues: a review.

Cefotaxime is a third-generation cephalosporin with a broad spectrum of activity. Concentrations of cefotaxime in serum and urine are sufficient for clinical efficacy. This report reviews the available data on the penetration of cefotaxime into other body fluids and tissues. Therapeutic doses of cefotaxime result in significant levels in bile (20 micrograms/ml), in cerebrospinal fluid of patients with meningitis (5-10 micrograms/ml), in pleural fluid (2-7 micrograms/ml), and in otitis media exudate (2-10 micrograms/ml). Lower levels of cefotaxime are obtained in uninflamed aqueous humor (1 microgram/ml), in breast milk (0.1-0.5 microgram/ml), and in cerebrospinal fluid of patients without meningitis (0.2 microgram/ml). Cefotaxime levels in tissues are generally well within the range required for clinical efficacy--i.e., 2-5 micrograms/g, with some higher levels reported in testis, prostate, ureter, skin, and gallbladder wall. Drug levels of less than 2 micrograms/g have been reported in fat, muscle, and uterus. All body fluids and tissues, including bone and skin, are penetrated easily by therapeutic doses of cefotaxime.

Aqueous Humor↗
PubMedDate not supplied

Chronic Pseudomonas aeruginosa endobronchitis in rhesus monkeys: I. Effects of pentoxifylline on neutrophil influx.

Host defense abnormalities in cystic fibrosis (CF) against Pseudomonas aeruginosa (PA) lead to excessive neutrophil influx into the infected lungs, resulting in pulmonary complications. We have developed a rhesus monkey model of chronic PA endobronchitis by intrabronchial instillation of PA-embedded agar beads, utilizing flexible fiberoptic bronchoscopy. Treatment of infected monkeys with pentoxifylline suppressed neutrophil influx and ameliorated pulmonary damage. The results suggest a method by which neutrophil influx and pulmonary damage in CF patients can be managed or prevented.

Animals↗