化合物详情

CAS25953-19-9
分子式C14H14N8O4S3
分子量454.51 g/mol g/mol
危化品

Cefazolin is a first-generation cephalosporin compound having [(5-methyl-1,3,4-thiadiazol-2-yl)sulfanyl]methyl and (1H-tetrazol-1-ylacetyl)amino side-groups at positions 3 and 7 respectively. It has a role as an antibacterial drug. It is a cephalosporin, a member of tetrazoles, a member of thiadiazoles and a beta-lactam antibiotic allergen. It is a conjugate acid of a cefazolin(1-).

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化合物详情

Toxicity

Toxicity
14
Fate Summary
ATMOSPHERIC FATE: According to a model of gas/particle partitioning of semivolatile organic compounds in the atmosphere(1), cefazolin, which has an estimated vapor pressure of 1.5X10-18 mm Hg at 25 °C(SRC), determined from a fragment constant method(2), is expected to exist solely in the particulate phase in the ambient atmosphere. Particulate-phase cefazolin may be removed from the air by wet or dry deposition(SRC). Cefazolin absorbs light at wavelengths >290 nm (UV max = 272 nm with a possible shoulder above 290 nm)(3) and therefore may be susceptible to direct photolysis by sunlight(4).
Soil Adsorption / Mobility
The Koc of cefazolin is estimated as 12(SRC), using a log Kow of -0.58(1) and a regression-derived equation(2). According to a classification scheme(3), this estimated Koc value suggests that cefazolin is expected to have very high mobility in soil. An estimated pKa of 3.6(SRC), calculated using a method based on linear free energy relationships and perturbed molecular orbital theory(4), indicates that this compound will exist primarily as an anion in the environment and anions generally have higher mobility in soils than their neutral counterparts(5).
Environmental Bioconcentration
An estimated BCF of 0.2 was calculated for cefazolin(SRC), using a log Kow of -0.58(1) and a regression-derived equation(2). According to a classification scheme(3), this BCF suggests the potential for bioconcentration in aquatic organisms is low(SRC).
Volatilization from Water / Soil
The estimated pKa of cefazolin is 3.6 (carboxylic acid), calculated using a method based on linear free energy relationships and perturbed molecular orbital theory(1). Based on this pKa value, cefazolin is expected to exist primarily as an anion in the environment(SRC). Volatilization of cefazolin from moist soil or water surfaces is not expected to be an important fate process(SRC) because anions do not volatilize. Cefazolin is not expected to volatilize from dry soil surfaces(SRC) based upon an estimated vapor pressure of 1.5X10-18 mm Hg(SRC), determined from a fragment constant method(2).
Environmental Abiotic Degradation
Cefazolin is not expected to undergo hydrolysis in the environment due to the lack of functional groups that hydrolyze under environmental conditions(1). Cefazolin absorbs light at wavelengths >290 nm (UV max = 272 nm with a possible shoulder above 290 nm)(2) and therefore may be susceptible to direct photolysis by sunlight(1).
Milk Concentrations
EXPERIMENTAL MILK: In depletion studies carried out in lactating cows it was shown that after the recommended treatment with the commercial formulation intended for lactating cows (two treatments of all four quarters at two successive milkings), residues in composite milk samples were below 50 ug/L at the 7th milking and below 25 ug/L at the 8th milking after the last treatment.
Artificial Pollution Sources
Cefazolin's production and use as an actibacterial drug for both humans and animals(1-3) may result in its release to the environment through various waste streams(SRC).
Probable Routes of Human Exposure
NIOSH (NOES Survey 1981-1983) has statistically estimated that 16,111 workers (13,596 of these are female) are potentially exposed to cefazolin in the US(1). Occupational exposure to cefazolin may occur through dermal contact with this compound at workplaces where cefazolin is produced or used(SRC). Exposure to cefazolin among the general population may be limited to those administered this substance as a drug and to those who administer cefazolin to animals(SRC).
Environmental Fate / Exposure Summary
Cefazolin's production and use as an actibacterial drug for both humans and animals may result in its release to the environment through various waste streams. If released to air, an estimated vapor pressure of 1.5X10-18 mm Hg at 25 °C indicates cefazolin will exist solely in the particulate phase in the atmosphere. Cefazolin absorbs light at wavelengths >290 nm (UV max = 272 nm with a possible shoulder above 290 nm) and therefore may be susceptible to direct photolysis by sunlight. If released to soil, cefazolin is expected to have very high mobility based upon an estimated Koc of 12. The pKa of cefazolin is 3.6 (carboxylic acid), indicating that this compound will exist primarily as an anion in the environment and anions generally have higher mobility in soil than their neutral counte...
Drug Induced Liver Injury
References: DOI:10.1016/j.drudis.2019.09.022
Non-Human Toxicity Values
LD50 Rat oral (acute) >11000 mg/kg bw
Populations at Special Risk
Serious bleeding related either to ... thrombocytopenia, and/or platelet dysfunction has been reported with several beta-lactam antibiotics. This appears to be a particular problem with certain patients (elderly, poorly nourished, or those with renal insufficiency) who are receiving moxalactam. /Cephalosporins/
Antidote and Emergency Treatment
/SRP:/ Advanced treatment: Consider orotracheal or nasotracheal intubation for airway control in the patient who is unconscious, has severe pulmonary edema, or is in severe respiratory distress. Positive-pressure ventilation techniques with a bag valve mask device may be beneficial. Consider drug therapy for pulmonary edema ... . Consider administering a beta agonist such as albuterol for severe bronchospasm ... . Monitor cardiac rhythm and treat arrhythmias as necessary ... . Start IV administration of D5W /SRP: "To keep open", minimal flow rate/. Use 0.9% saline (NS) or lactated Ringer's if signs of hypovolemia are present. For hypotension with signs of hypovolemia, administer fluid cautiously. Watch for signs of fluid overload ... . Treat seizures with diazepam or lorazepam ... . Use...
Effects During Pregnancy and Lactation
◉ Effects on Lactation and Breastmilk
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