◉ Summary of Use during Lactation:Because of the low levels of erythromycin in breastmilk and safe administration directly to infants, it is acceptable in nursing mothers. The small amounts in milk are unlikely to cause adverse effects in the infant. Monitor the infant for irritability and possible effects on the gastrointestinal flora, such as diarrhea, candidiasis (thrush, diaper rash). One case report and unconfirmed epidemiologic evidence indicates that hypertrophic pyloric stenosis in infants might occur with maternal use of erythromycin during the first two weeks of breastfeeding; however, if it occurs, the frequency is very low and others have questioned this relationship.
Infant side effects are unlikely with topical application for acne, although topical application to the nipple may increase the risk of diarrhea in the infant. Only water-miscible cream or gel products should be applied to the breast because ointments may expose the infant to high levels of mineral paraffins via licking.[1]
◉ Effects in Breastfed Infants:Pyloric stenosis, vomiting, sedation, poor sucking and poor weight gain probably related to erythromycin in breastmilk was reported in a 3-week-old infant.[4]
A cohort study of infants diagnosed with infantile hypertrophic pyloric stenosis found that affected infants were 2.3 to 3 times more likely to have a mother taking a macrolide antibiotic during the 90 days after delivery. Stratification of the infants found the odds ratio to be 10 for female infants and 2 for male infants. All of the mothers of affected infants nursed their infants. Seventy-two percent of the macrolide prescriptions were for erythromycin. However, the authors did not state which macrolide was taken by the mothers of the affected infants.[5]
A study comparing the breastfed infants of mothers taking amoxicillin to those taking a macrolide antibiotic found no instances of pyloric stenosis. However, most of the infants exposed to a macrolide in breastmilk were exposed to roxithromycin. Only 2 of the 55 infants exposed to a macrolide were exposed to erythromycin. Adverse reactions occurred in 12.7% of the infants exposed to macrolides which was similar to the rate in amoxicillin-exposed infants. Reactions included rash, diarrhea, loss of appetite, and somnolence.[6]
A retrospective database study in Denmark of 15 years of data found a 3.5-fold increased risk of infantile hypertrophic pyloric stenosis in the infants of mothers who took a macrolide during the first 13 days postpartum, but not with later exposure. The proportion of infants who were breastfed was not known, but probably high. The proportion of women who took each macrolide was also not reported.[7]
In one telephone follow-up study, mothers reported diarrhea 2 infants and irritability in 2 infants out of 17 infants whose mothers were taking erythromycin during breastfeeding. None of the reactions required medical attention.[8]
Two meta-analyses failed to demonstrate a relationship between maternal macrolide use during breastfeeding and infantile hypertrophic pyloric stenosis.[9][10]
◉ Effects on Lactation and Breastmilk:Relevant published information was not found as of the revision date.
A 77-YR-OLD WOMAN IS REPORTEDLY MAINTAINED ON 7.5 MG OF WARFARIN DAILY IN WHOM THE ADMIN OF ORAL ERYTHROMYCIN STEARATE, 500 MG 4 TIMES A DAY, RESULTED IN A PROTHROMBIN TIME OF 64 SECONDS (CONTROL, 11 SECONDS).
AMONG ALLERGIC REACTIONS ARE FEVER, EOSINOPHILIA, & SKIN ERUPTIONS, WHICH MAY OCCUR ALONE OR IN COMBINATION; EACH DISAPPEARS SHORTLY AFTER THERAPY IS STOPPED. ...OFTEN PRODUCES IRRITATIVE EFFECTS. ORAL ADMIN...FREQUENTLY ACCOMPANIED BY EPIGASTRIC DISTRESS, WHICH MAY BE QUITE SEVERE. /ERYTHROMCYIN/
IM INJECTION OF QUANTITIES LARGER THAN 100 MG PRODUCES EXTREMELY SEVERE PAIN THAT PERSISTS FOR HOURS. IV INFUSION OF 1-G DOSES...ALMOST REGULARLY IS FOLLOWED BY THROMBOPHLEBITIS. /ERYTHROMYCIN/
PEAK CONCN IN PLASMA...0.3-0.5 UG/ML 4 HR AFTER ORAL ADMIN OF 250 MG OF BASE & ARE 0.3-1.9 UG/ML AFTER...500-MG TABLET. VARIOUS ESTERS OF ERYTHROMYCIN HAVE BEEN PREPARED TO...IMPROVE STABILITY & FACILITATE ABSORPTION. ...CONCN OF ERYTHROMYCIN IN PLASMA ARE LITTLE DIFFERENT IF STEARATE IS GIVEN ORALLY.
...DIFFUSES READILY INTO INTRACELLULAR FLUIDS, & ANTIBACTERIAL ACTIVITY... ACHIEVED AT...ALL SITES EXCEPT BRAIN & CSF. ...ONE OF FEW ANTIBIOTICS THAT PENETRATES INTO PROSTATIC FLUID, CONCN ARE APPROX 40% OF...PLASMA. EXTENT OF BINDING...TO PLASMA PROTEINS VARIES...PROBABLY EXCEEDS 70% IN ALL.../FORMS OF DRUG/. /ERYTHROMYCIN/
来源:Hazardous Substances Data Bank (HSDB)
吸收、分配和排泄
红霉素碱从小肠上部被充分吸收；它会被胃液灭活...胃中的食物会延迟其最终吸收。/红霉素/
ERYTHROMYCIN BASE IS ADEQUATELY ABSORBED FROM UPPER PART OF SMALL INTESTINE; IT IS INACTIVATED BY GASTRIC JUICE... FOOD IN STOMACH DELAYS ITS ULTIMATE ABSORPTION. /ERYTHROMYCIN/
来源:Hazardous Substances Data Bank (HSDB)
吸收、分配和排泄
红霉素可穿过胎盘屏障；胎儿血浆中的药物浓度约为母体循环中的5-20%。/红霉素/
ERYTHROMYCIN TRAVERSES PLACENTAL BARRIER; & CONCN OF DRUG IN FETAL PLASMA ARE ABOUT 5-20% OF THOSE IN MATERNAL CIRCULATION. /ERYTHROMYCIN/
SMALL MOLECULE COMPOUNDS SELECTIVE AGAINST GRAM-NEGATIVE BACTERIAL INFECTIONS
申请人：DeBrabander Jef
公开号：US20150329582A1
公开（公告）日：2015-11-19
The described invention provides fully synthetic, biologically active mangrolide A. It describes schemes to chemically synthesize mangrolide A, intermediates and analogs of mangrolide A, and their antibacterial activity.
8-N-substituted-2H-isothiazolo[5,4-b]quinolizine-3,4-diones and related compounds as antiinfective agents
申请人：Bradbury J. Barton
公开号：US20060173026A1
公开（公告）日：2006-08-03
The invention provides compounds and salts of Formula I and Formula II:
which possess antimicrobial activity. The invention also provides novel synthetic intermediates useful in making compounds of Formula I and Formula II. The variables A
1
, A
8
, R
2
, R
3
, R
5
, R
6
, R
7
, and R
9
are defined herein.
Certain compounds of Formula I and Formula II disclosed herein are potent and selective inhibitors of bacterial DNA synthesis and bacterial replication. The invention also provides antimicrobial compositions, including pharmaceutical compositions, containing one or more compounds of Formula I or Formula II and one or more carriers, excipients, or diluents. Such compositions may contain a compound of Formula I or Formula II as the only active agent or may contain a combination of compounds of Formula I and/or Formula II and one or more other active agents. The invention also provides methods for treating microbial and protozoal infections in animals.
[EN] CARBAPENEM ANTIBACTERIALS WITH GRAM-NEGATIVE ACTIVITY AND PROCESSES FOR THEIR PREPARATION<br/>[FR] BACTERICIDES AU CARBAPENEM A ACTIVITE GRAM-NEGATIVE ET PROCEDES D'ELABORATION CORRESPONDANTS
申请人：FOB SYNTHESIS
公开号：WO2005123066A1
公开（公告）日：2005-12-29
The present invention provides β-methyl carbapenem compounds and pharmaceutical compositions useful in the treatment of bacterial infections and methods for treating such infections using such compounds and/or compositions. The invention includes administering an effective amount of a carbapenem compound or salt and/or prodrug thereof to a host in need of such a treatment. The present invention is also in the field of synthetic organic chemistry and is specifically provides an improved method of synthesis of β-methyl carbapenems which are useful as antibacterial agents.
8A,9-dihydro-4aH-isothiazolo[5,4-b]quinoline-3,4-diones and related compounds as anti-infective agents
申请人：Bradbury J. Barton
公开号：US20060100215A1
公开（公告）日：2006-05-11
The invention provides compounds and salts of Formula I and Formula II:
which possess antimicrobial activity. The invention also provides novel synthetic intermediates useful in making compounds of Formula I and Formula II. The variables n, m, p, R
A
, R
B
, A
1
, R
2
, R
3
, R
5
, R
6
, R
7
, A
8
and R
9
are defined herein.
Certain compounds of Formula I and Formula II disclosed herein are potent and/or selective inhibitors of bacterial DNA synthesis and bacterial replication. The invention also provides antimicrobial compositions, including pharmaceutical compositions, containing one or more compounds of Formula I or Formula II and one or more carriers, excipients, or diluents. Such compositions may contain a compound of Formula I or Formula II as the only active agent or may contain a combination of a compound of Formula I or Formula II and one or more other active agents. The invention also provides methods for treating microbial infections in eukaryotes.
[EN] CARBAPENEM COMPOUNDS AND COMPOSITIONS FOR THE TREATMENT OF BACTERIAL INFECTIONS<br/>[FR] COMPOSÉS DE CARBAPENEM ET COMPOSITIONS POUR LE TRAITEMENT D'INFECTIONS BACTÉRIENNES
申请人：FOB SYNTHESIS INC
公开号：WO2018227178A1
公开（公告）日：2018-12-13
The present invention provides carbapenem compounds and pharmaceutical compositions useful in the treatment of bacterial infections, including drug resistant or multiple-drug resistant bacterial infections, and methods for treating such infections using such compounds and/or compositions. The invention includes administering an effective amount of a carbapenem compound or salt and/or prodrug thereof to a host in need of such a treatment.
