Sulbactam kinetics and excretion into breast milk in postpartum women

Foulds, George; Rd, Miller; Ak, Knirsch; Ld, Thrupp

doi:10.1038/clpt.1985.247

Cited by 17 publications

(3 citation statements)

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“…Significant penetration of sui bact am + ampicillin into prostate tissue (Dorflinger & Madsen 1985), pus (Foulds 1986), middle-ear fluid (Reilly et al 1983) and across the placental barrier (Dubois et al 1983) has been described. Peak concentrations below 3 mg/L are found in human breast milk (Foulds et al 1985b). …”

Section: Distributionmentioning

confidence: 98%

Clinical Pharmacokinetics of Enzyme Inhibitors in Antimicrobial Chemotherapy

Watson

Stewart

Platt

1988

Clinical Pharmacokinetics

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The effectiveness of some antimicrobial agents can be enhanced by using them in combination; such combinations are termed synergistic. Where one compound potentiates the effect of a second drug they may be coformulated. Inhibition of the bacterial degradation of an active antimicrobial is the basis of clavulanate and sulbactam-potentiated penicillin combinations, and inhibition of degradative pathways in the host is the rationale behind imipenem/cilastatin therapy. Trimethoprim/sulphonamide combinations depend on the maintenance of an effective ratio for synergistic action. In order to achieve potentiation the coformulated drugs should have similar pharmacokinetics. Trimethoprim was originally matched with sulphamethoxazole, since these two drugs have similar elimination half-lives, but the significantly poorer penetration of sulphonamides, their greater non-renal clearance, the emergence of resistance, and the adverse reactions attributable to them argue against the rationale that underlies their coformulation. Time-dependent inhibition of bacterial beta-lactamases by clavulanic acid and sulbactam has extended the use of penicillins which are highly susceptible to beta-lactamase inactivation. The beta-lactamase inhibitors must penetrate to the same extent as the penicillin used with them, and be present long enough to effect inhibition; thus, rapid penetration, similar or slower elimination and equivalent volume of distribution are necessary. These requirements are met for amoxycillin/clavulanic acid, ticarcillin/clavulanic acid and ampicillin/sulbactam combinations. Clavulanic acid is absorbed orally and is given with amoxycillin. However, since sulbactam is labile by this route, the combination of sulbactam with ampicillin to form the prodrug sultamicillin has been necessary to enable an oral form to be developed. Imipenem is metabolised by renal brush-border dehydropeptidases, and may cause proximal tubular necrosis. Cilastatin was designed to inhibit this metabolism, which it effectively does, thereby both potentiating the effect of imipenem and avoiding toxicity. Appropriate matching of the kinetics of coformulated drugs is intended to maximise potentiation and minimise the risk of emergent resistance. The kinetics of the above combinations are discussed in the light of these requirements and the effects of age and disease.

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Section: Distributionmentioning

confidence: 98%

Clinical Pharmacokinetics of Enzyme Inhibitors in Antimicrobial Chemotherapy

Watson

Stewart

Platt

1988

Clinical Pharmacokinetics

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“…In total, 66 studies were assessed using the checklist based on FDA and ILCA guidelines (Table ). For five antibiotic groups, only one study was included and for three antibiotic groups, two studies were included. The results of the quality determination of the different parameters (Table ) of six antibiotic groups with at least five studies are shown in Figure A‐D.…”

Section: Outcomementioning

confidence: 99%

Antibiotics and lactation: An overview of relative infant doses and a systematic assessment of clinical studies

Wattum

Leferink

Wilffert

et al. 2018

Basic Clin Pharma Tox

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Breastfeeding is important for the development of the child. Many antibiotics are considered safe during breastfeeding. The aim of the study was to assess the quality of lactation studies with antibiotics using the FDA and International Lactation Consultant Association quality guidelines for lactation studies. The secondary goal was to determine the exposure of the breastfed infant to antibiotics in relation to bacterial resistance and the developing microbiome. A literature search was performed and the included studies were scored on methodology, parameters concerning maternal exposure to antibiotics, maternal plasma and milk sampling. The infant exposure has been calculated and expressed as a percentage of a normal infant therapeutic dose. Sixty-six studies were included in five antibiotic groups (broad-spectrum penicillin, cephalosporins, macrolides and lincosamides, quinolones and sulphonamides). Cephalosporins were the most studied group of antibiotics (n = 21). Fifteen studies met all the criteria of "mother exposure to antibiotic". Six studies met every criterion related to "plasma sampling". Only one case report met all listed criteria for lactation studies. The correct calculation of infant exposure to antibiotics via the milk:plasma ratio (AUC) varies between 13% for macrolides and 38% for broad-spectrum penicillin. The highest assessed exposure as a percentage of infant therapeutic dose was for metronidazole (11%). The studies meet to a limited extent with the quality standards for lactation research. The breastfed infants are exposed to a subtherapeutic concentration of antibiotics.

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“…With sulbactam, the relative daily dose transmitted was a maximum of 1% (Foulds 1985). With aztreonam, a 0.2% relative dose was reported for the baby at the next breastfeeding after the mother had taken a single dose (Ito 1990).…”

Section: Penicillins Cephalosporins and Other β-Lactam Antibioticsmentioning

confidence: 99%

Anti-infectives

Padberg¹

2015

Drugs During Pregnancy and Lactation

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Sulbactam kinetics and excretion into breast milk in postpartum women

Cited by 17 publications

References 0 publications

Clinical Pharmacokinetics of Enzyme Inhibitors in Antimicrobial Chemotherapy

Clinical Pharmacokinetics of Enzyme Inhibitors in Antimicrobial Chemotherapy

Antibiotics and lactation: An overview of relative infant doses and a systematic assessment of clinical studies

Anti-infectives

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