Henry's Law constant = 2.49X10-21 atm-cu m/mol at 25 °C (est)
稳定性/保质期：
Following reconstitution, amoxicillin oral suspensions should preferably be refrigerated at 2-8 °C, but refrigeration is not necessary and the suspension are stable for 14 days at room temp or 2-8 °C
旋光度：
Specific optical rotation: +248 deg to +268 deg
Caco2细胞的药物渗透性：
-6.1
解离常数：
2.6
碰撞截面：
187.4 Ų [M+H]+ [CCS Type: TW, Method: calibrated with polyalanine and drug standards]
Incubation with human liver microsomes has lead to the detection of 7 metabolites. The M1 metabolite has undergone hydroxylation, M2 has undergone oxidative deamination, M3 to M5 have undergone oxidation of the aliphatic chain, M6 has undergone decarboxylation, and M7 has undergone glucuronidation.
IDENTIFICATION AND USE: Amoxicillin is a semi-synthetic antibiotic related to penicillin. HUMAN EXPOSURE AND TOXICITY: Serious and occasionally fatal hypersensitivity (anaphylactic) reactions have been reported in patients on penicillin therapy including amoxicillin. Although anaphylaxis is more frequent following parenteral therapy, it has occurred in patients on oral penicillins. These reactions are more likely to occur in individuals with a history of penicillin hypersensitivity and/or a history of sensitivity to multiple allergens. There have been reports of individuals with a history of penicillin hypersensitivity who have experienced severe reactions when treated with cephalosporins. Before initiating therapy with amoxicillin, careful inquiry should be made regarding previous hypersensitivity reactions to penicillins, cephalosporins, or other allergens. If an allergic reaction occurs, amoxicillin should be discontinued and appropriate therapy instituted. There was no evidence of any association between use of these drugs and the incidence or type of congenital malformation. There was no association with use of these drugs and intrauterine growth retardation or perinatal death, but there was a significant difference in the rate of prematurity in the users (8.9%) compared with nonusers (6.5%). ANIMAL STUDIES: Reproduction studies have been performed in mice and rats at doses up to 2000 mg/kg. There was no evidence of harm to the fetus due to amoxicillin. However, 100 ug/mL amoxicillin altered rat renal development in vitro. Prolonged use of amoxicillin might have a negative effect on bone formation around implants. Studies to detect mutagenic potential of amoxicillin alone have not been conducted; however, the following information is available from tests on a 4:1 mixture of amoxicillin and potassium clavulanate. Amoxicillin and potassium clavulanate was non-mutagenic in the Ames bacterial mutation assay, and the yeast gene conversion assay. Amoxicillin and potassium clavulanate was weakly positive in the mouse lymphoma assay. Amoxicillin and potassium clavulanate was negative in the mouse micronucleus test and in the dominant lethal assay in mice.
Rare instances of idiosyncratic liver injury have been reported in persons receiving the aminopenicillins including amoxicillin. Cases are characterized by a short latency period of a few days to as long as two weeks. The onset of liver injury can occur after the antibiotic is stopped. The serum enzyme pattern associated with aminopenicillin liver injury has included a hepatocellular pattern with marked elevations in ALT and AST, and minimal elevations in alkaline phosphatase and rapid recovery after withdrawal. In addition, cholestatic forms of hepatic injury with marked alkaline phosphatase elevations (as also seen with penicillin-induced liver injury) have also been described, some of which have been associated with prolonged cholestasis (Case 1). The onset of hepatic injury may be accompanied by signs or symptoms of hypersensitivity such as eosinophilia, rash and arthralgias, and in some cases is accompanied by toxic epidermal necrolysis or Stevens Johnson syndrome.
Much more common than liver injury from amoxicillin alone is the typically cholestatic hepatitis that occurs after treatment with the combination of amoxicillin and clavulanate. Indeed, this combination is currently the most common cause of idiosyncratic acute liver injury in the United States, Europe and Australia. The injury, however, is usually attributed to the clavulanate rather than amoxicillin. The clinical features are similar but perhaps not completely the same. In cases of liver injury seeming due to amoxicillin, an extra effort should be made to make sure that it was not amoxicillin-clavulanate [Augmentin] that was taken.
Likelihood score: B (highly likely but rare cause of clinically apparent liver injury).
Amoxicillin is approximately 60% bioavailable. A 250mg dose of oral amoxicillin reaches a Cmax 3.93±1.13mg/L with a Tmax 1.31±0.33h and an AUC of 27.29±4.72mg\*h/L. A 875mg dose of oral amoxicillin reaches a Cmax 11.21±3.42mg/L with a Tmax 1.52±0.40h and an AUC of 55.04±12.68mg\*h/L.
... A 48 year-old woman was admitted because of pneumococcal meningitis. After 4 days on high-dose amoxicillin (320 mg/kg/day), she developed acute oliguric renal failure and amoxicillin crystallization was documented by infrared spectrometry. The outcome was favorable after amoxicillin dosage tapering, together with one single hemodialysis session and further hydratation. Amoxicillin is mainly excreted in the urine in its unchanged form.
