Pharmacology of Cinoxacin in Humans

Black, Henry R.; Israel, Karen; Wolen, Robert L.; Brier, G. L.; Obermeyer, Boyd D.; Ziege, Edgar A.; Wolny, J. D.

doi:10.1128/aac.15.2.165

Cited by 28 publications

(7 citation statements)

References 10 publications

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“…The drug half-life in plasma increased from a mean normal value of 1.1 to 2.0 h with acidification and decreased to 0.6 h with alkalinization. The pharmacokinetic values for cinoxacin in control subjects were in good agreement with those reported previously (2,13).…”

Section: Resultssupporting

confidence: 80%

“…However, in view of the high levels of cinoxacin which are obtained in both acidic and basic urine, the impact of urine pH on cinoxacin antibacterial efficacy would be of minor clinical importance. Cinoxacin has been shown to exhibit antibacterial activity against most gram-negative orgnisms commonly encountere in urinary tract infections (4,11). It is well absorbed from onl doses and is rpidly excreted from the body under normal conditions with an eliminaton half-life of 1 to 1.5 h (2,13).…”

mentioning

confidence: 99%

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Influence of Urinary pH on the Pharmacokinetics of Cinoxacin in Humans and on Antibacterial Activity In Vitro

Barbhaiya

Gerber

Craig

et al. 1982

Antimicrob Agents Chemother

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The impact of acidification and alkalinization of the urine on the pharmacokinetics of cinoxacin was examined after single 500-mg oral doses were aministered to nine healthy male volunteers. Acidic and alkaline conditions were achieved by repeated orl doses of ammoum chloride or sodium bicarbonate, respectively. Plasma cinoxacin levels in all subjects were adequately described in terms ofone-compartment-model kinetics with first-order absorption and elimination. Acidification and alkalinizati treatment had no effect on cinoxacin absorption or distribution. The mean eliminaon half-life of cinoxacin in plasma was 1.1, 2.0, and 0.6 h in control subjects and with acidification and aanization Of urine, respectively. Recovery of intact cinoxacin in samples of urine collected 0 to 36 h after cinoxacin administration represented 65% of the dose in control subjects and urine acidification and 80% of the dose with alikainization of urine. The mean renal clearance of cinoxacin was 76, 118, and 278 ml/min with acidificaton, control, and a, respectively, and renal cleaance was highly correlated with urinary pH.

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Section: Resultssupporting

confidence: 80%

mentioning

confidence: 99%

Influence of Urinary pH on the Pharmacokinetics of Cinoxacin in Humans and on Antibacterial Activity In Vitro

Barbhaiya

Gerber

Craig

et al. 1982

Antimicrob Agents Chemother

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“…This is an excellent example of the profound effect that delayed stomach Sennello et al (1978) Neu (1974) Bogentoft et al (1978) Volans (1974 Glynne et al (1978) Harvengt et al (1973; Haginaka et al (1979); Tetzlaff et al (1978). Harvengt et al (1973);Mischler et al (1974) Bodemar et al (1979) Black et al (1979) Willis et al (1981a,b) Sanchez et al (1973; Johnson et al (1978) Kelly et al (1974) Wahiin-Boll et al (1980) Tamassia et al (1977 420 McCracken et al (1978); Melander ei al. (19771) Jaffe et al (1971); Mattock and McGilveray (1973); Heading et al (1973).…”

Section: Aspirinmentioning

confidence: 92%

Interactions Affecting Drug Absorption

Welling¹

1984

Clinical Pharmacokinetics

158

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The influence of drug-drug and drug-food interactions affecting the absorption of orally administered medication is reviewed. Drug-drug interactions can be classified in terms of indirect effects by one drug on gastrointestinal tract physiology influencing the absorption of other drugs, or direct interactions involving altered pH, adsorption, absorption, or chelation. Most, but not all, drug-drug interactions result in reduced or delayed systemic drug availability. Drug-food interactions may result in reduced, delayed, or increased systemic drug availability. The absorption of only a small number of drugs is unaffected by concomitant food intake. The degree of interaction and whether it positively or negatively affects drug absorption depends on a number of factors including the physical and chemical nature of the drug, the formulation, the type of meal, and the time interval between eating and dosing. Mechanisms of drug-food interactions are not well characterised. They clearly involve both direct and indirect factors in a similar fashion to drug-drug interactions, but indirect factors probably predominate. Reduced or delayed drug absorption is generally attributed, at least in part, to delayed stomach-emptying due to food. Increased absorption may also result from delayed stomach-emptying facilitating greater drug dissolution before it passes from the stomach into the small intestine. Increased bioavailability of some drugs, e.g. propranolol, metoprolol and labetalol, may be related to reduced presystemic clearance. The potential clinical implications of drug-drug and drug-food interactions must be taken into account with oral medications in order to minimise variations in systemic drug availability and hence in clinical efficacy.

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“…Cinoxacin concentrates in renal tissue, where levels may exceed serum levels [24]. Approximately 60 % of the parent compound is excreted in the urine along with at least four microbiologically inactive metabolites [25].…”

Section: Mechanism Of Actionmentioning

confidence: 99%