Amoxycillin and Co-Trimoxazole in Acute Purulent Exacerbations of Chronic Bronchitis

Pines, A.; Nandi, Alolika; Raafat, H.; Rahman, Mizanur

doi:10.1159/000221972

Cited by 18 publications

(4 citation statements)

References 4 publications

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“…Our study has established that the combination of rifampicin with trimetho prim reduces the selection of rifampicin-re sistant strains to an acceptable rate, compa rable with the one found in studies with oth er antimicrobial agents, such as streptomy cin [Finland et al, 1946], nalidixic acid [Ronald et al, 1966], sulfonamides [Wil liams et al, 1965], cephaloridine [Stewart and Holt, 1964] carbenicillin [Jones and Lowbury, 1967] and cotrimoxazole [Pines et al, 1977],…”

Section: Discussionsupporting

confidence: 72%

Double-Blind Multicenter Trial of a Rifampicin–Trimethoprim Combination and Rifampicin Alone in Urinary Tract Infections

Palminteri¹,

Sassella²

1979

Chemotherapy

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A double-blind multicenter trial was carried out in 146 patients with urinary tract infections in order to compare the combination of rifampicin and trimethoprim (450 mg plus 120 mg twice daily) with rifampicin alone (450 mg twice daily). The success rate on the day after a 10-day course of treatment was significantly higher after the combination than after rifampicin alone (72% of 60 cases vs. 45% of 55 cases). The difference was still significant, and of the same order of magnitude, 1 week after the end of the treatment (53% of 51 vs. 24% of 45 cases). The subgroups of patients with organisms sensitive to both rifampicin and trimethoprim before treatment were considered separately in each treatment group: rifampicin-resistant strains were isolated after treatment in 27% of 26 patients treated with rifampicin alone, and in 7% of 27 patients in the other group. The tolerances of the two treatments were superimposable. The combination rifampicin-trimethoprim appears to overcome the problem of selection of rifampicin-resistant strains, with the concomitant therapeutic failures, in urinary tract infections.

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Section: Discussionsupporting

confidence: 72%

Double-Blind Multicenter Trial of a Rifampicin–Trimethoprim Combination and Rifampicin Alone in Urinary Tract Infections

Palminteri¹,

Sassella²

1979

Chemotherapy

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“…This difference was statistically significant. 70 Chodosh, 52 analyzing long-term follow-up data on a series of trials in AECB, has shown that the mean time from the end of therapy of one exacerbation to the onset of the next may allow more reliable assessment of comparative efficacy. Thus, if the time to relapse after ampicillin therapy (about 200 days) is taken as the index value, ratios for the same periods applicable to other agents can be calculated.…”

Section: New Approaches To 0utco~e Assessmentmentioning

confidence: 99%

Epidemiology and Treatment of Chronic Bronchitis and Its Exacerbations

Ball¹

1995

Chest

214

123

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“…The presence of salivary amoxicihlin in chronic bronchitis patients could be due to penetration of amoxicillin into sputum through inflamed lung tissue, high intrabronchial concentrations (13) and contamination of saliva by sputum, or even by the dosing and saliva collection techniques. A similar relationship was observed between ampicilhin and its methoxymethyl ester (BL-P1761).…”

Section: Methodsmentioning

confidence: 99%

Human pharmacokinetics and disposition of sarmoxicillin, a lipophilic amoxicillin prodrug

Smyth¹,

Pfeffer²,

Harken³

et al. 1981

Antimicrob Agents Chemother

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Sarmoxicillin, an amoxicillin prodrug, is the methoxymethyl ester of hetamoxicillin. Esterification converted amoxicillin from an amphoteric to a cationic compound and resulted in a 30-to 600-fold increase in lipid partitioning. Oral absorption studies in normal subjects demonstrated that sarmoxicillin was only partially hydrolyzed by nonenzymatic and gut or hepatic first-pass metabolism and that ificant quantities of intact ester appeared in the systemic circulation. Sarmoxicillin was converted to amoxicillin in plasma by hydrolysis of the acetone penicinate and the methoxymethyl ester bonds. Significant amoxicillin levels were demonstrated in saliva after administration of sarmoxicillin, but not amoxicillin, over a 250-to 1,000-mg dose range. Differences in the absorption, distribution, or metabolism of amoxicillin were also evident in the lower plasma amoxicillin maximum concentration and area under the curve and longer half-life after sarmoxicillin administration. Differences in the distribution of this lipophilic ester could result in a significant increase in tissue penetration and subsequent therapeutic efficacy of amoxicillin when administered as sannoxicillin.Sarmoxicillin, the methoxymethyl ester of hetamoxicillin ( Fig. 1), has the same in vitro antimicrobial spectrum as amoxicillin (Bristol Laboratories, unpublished data). However, esterification of the carboxyl group results in a significant change in the physiochemical and tissue distribution characteristics of amoxicillin. Esterification converts amoxicillin from an amphoteric (18) (pKI, 2.4, 7.4, 9.6) to a cationic (pK., 7.4, 9.6) compound with increased lipophilicity at physiological pH. Increased cerebrospinal and prostatic fluid concentrations of antibiotic activity have been demonstrated in dogs with the methoxymethyl ester of hetacillin as compared with ampicillin (9, 10). Ampicillin ester prodrugs have also been prepared to improve bioavailability. Although the pivaloyloxyethyl (pivampicillin) (2), phthalidyl (talampicillin) (7), and ethoxycarbonyloxyethyl (bacampicillin) (6) esters have at least twofold-greater oral bioavailability than ampicillin, these esters are almost completely hydrolyzed in the gastrointestinal mucosa and appear in the portal circulation as ampicillin. The methoxymethyl ester of ampicillin is only partially hydrolyzed by gut and hepatic first-pass metabolism and appears in the systemic circulation and tissues as intad ester (11).The purpose of the present studies was to characterize the physiochemical properties, absorption, distribution in saliva, metabolism, and elimination of sarnoxicillin and amoxicillin in man. MATERIALS AND METHODSFormulations were as follows: formulation A, sarmoxicillin tablet, 250 mg of anhydrous amoxicillinequivalent activity per tablet; formulation B, amoxicillin capsules, 250 mg of anhydrous amoxicillin-equivalent activity per capsule; formulation C, capsule containing ground sarmoxiciflin tablet, 125 mg of anhydrous amoxicilin-equivalent activity sealed at capsule interface and polished ...

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Amoxycillin and Co-Trimoxazole in Acute Purulent Exacerbations of Chronic Bronchitis

Cited by 18 publications

References 4 publications

Double-Blind Multicenter Trial of a Rifampicin–Trimethoprim Combination and Rifampicin Alone in Urinary Tract Infections

Double-Blind Multicenter Trial of a Rifampicin–Trimethoprim Combination and Rifampicin Alone in Urinary Tract Infections

Epidemiology and Treatment of Chronic Bronchitis and Its Exacerbations

Human pharmacokinetics and disposition of sarmoxicillin, a lipophilic amoxicillin prodrug

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