Hepatic, with 90% conjugated to inactive glucuronide.
Half Life: Half-life in adults with normal hepatic and renal function is 1.5 - 3.5 hours. In patients with impaired renal function half-life is 3 - 4 hours. In patients with severely impaired hepatic function half-life is 4.6 - 11.6 hours. Half-life in children 1 month to 16 years old is 3 - 6.5 hours, while half-life in infants 1 to 2 days old is 24 hours or longer and is highly variable, especially in low birth-weight infants.
Chloramphenicol targets the large 39S subunit of the mitochondrial ribosome thereby deactivation mitochondrial protein synthesis. As a result chloramphenicol is cytotoxic to the most metabolically active cells or tissues including the heart, liver, thymus and bone-marrow. (A7823). The likely target of chloramphenicol is the 16S rRNA molecule in the mitochondrial ribosome, which is analogous to the 23S rRNA in bacterial ribosomes.
The most serious adverse effect associated with chloramphenicol treatment is bone marrow toxicity, which may occur in two distinct forms: 1) bone marrow suppression, which is a direct toxic effect of the drug and is usually reversible, and 2) aplastic anemia, which is idiosyncratic (rare, unpredictable) and generally fatal. Other less serious reactions from chloramphenicol use include fever, rashes, headache, and confusion. Use of intravenous chloramphenicol has also been associated with gray baby syndrome, a phenomenon resulting from newborn infants' inability to metabolize chloramphenicol in the liver via UDP-glucuronyl transferase. Gray baby syndrome is characterized by vomiting, ashen gray color of the skin, limp body tone, hypotension and cyanosis.
◉ Summary of Use during Lactation:Adverse reactions such as vomiting, excessive intestinal gas and falling asleep at the breast have been reported in breastfed infants whose mothers were taking oral chloramphenicol. Milk concentrations are not sufficient to induce "gray baby" syndrome, but since chloramphenicol-induced aplastic anemia is not dose-related, this might occur, but has not been reported. An alternate drug is preferred to chloramphenicol during breastfeeding, especially while nursing a newborn or preterm infant. If the mother must receive chloramphenicol during nursing, monitor the infant for gastrointestinal disturbances and adequacy of nursing. Monitoring of the infant's complete blood count and differential is advisable. In some cases, discontinuation of breastfeeding might be preferred.
◉ Effects in Breastfed Infants:One study reported 50 breastfed infants whose mothers were give oral chloramphenicol beginning 2 to 12 days postpartum in dosages of 1 (n = 20), 2 (n = 20)or 3 grams (n = 10) daily. All of the infants refused to suck, and 50 to 60% fell asleep during nursing. Vomiting occurred after feeding in 10%, 25%, and 90% of infants with daily maternal dosages of 1, 2 and 3 grams, respectively. All infants had excessive intestinal gas and abdominal distention, with severe problems in 0.5%, 20% and 100% of infants with daily maternal dosages of 1, 2 and 3 grams, respectively.
◉ Effects on Lactation and Breastmilk:Relevant published information was not found as of the revision date.
Rapidly and completely absorbed from gastrointestinal tract following oral administration (bioavailability 80%). Well absorbed following intramuscular administration (bioavailability 70%). Intraocular and some systemic absorption also occurs after topical application to the eye.
[EN] ISOTHIAZOLOQUINOLONES AND RELATED COMPOUNDS AS ANTI-INFECTIVE AGENTS<br/>[FR] ANTI-INFECTIEUX A BASE D'ISOTHIAZOLOQUINOLONES ET DE SELS CORRESPONDANTS
申请人：ACHILLION PHARMACEUTICALS INC
公开号：WO2005019228A1
公开（公告）日：2005-03-03
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 A1, R2, R3, R5, R6, R7, A8 and R9 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 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 animals.
COMPOSITIONS AND METHODS FOR REDUCTION OF KETONES, ALDEHYDES AND IMINIUMS, AND PRODUCTS PRODUCED THEREBY
申请人：Adler Marc J.
公开号：US20170362151A1
公开（公告）日：2017-12-21
A method of producing an alcohol, comprises reducing an aldehyde or a ketone with a hydridosilatrane. The reducing is carried out with an activator.
生产醇的方法包括使用氢硅氮烷还原醛或酮。还原过程中需要使用活化剂。
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] MODULATION OF IMMUNE RESPONSES BY ADMINISTRATION OF ROXITHROMYCIN OR ITS DERIVATIVE<br/>[FR] MODULATION DES RÉPONSES IMMUNES PAR ADMINISTRATION DE ROXITHROMYCINE OU DE SES DÉRIVÉS
申请人：Y S THERAPEUTICS CO LTD
公开号：WO2009023196A1
公开（公告）日：2009-02-19
Provided are compounds of formula (III) useful for modulation of immune responses, compositions comprising the compounds, and methods of use of such compositions for treating diseases or disorders involving an immune response. In certain embodiments, the compounds are useful for the treatment of diseases or disorders associated with transendothelial migration of T cells and activated T cells, and proinflammatory cytokine production from T cells and macrophages. Diseases or disorders that can be treated include arthritic and rheumatic disorders, such as rheumatoid arthritis.
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.
