Trade name: Risalin
Pharmacological Toxicology】: Amoxicillin is a penicillin antibiotic with good antibacterial activity against Streptococcus pneumoniae, Streptococcus haemolyticus and other streptococci, non-penicillinase producing Staphylococcus, Enterococcus faecalis and other aerobic Gram-positive cocci, Escherichia coli, Proteus mirabilis, Salmonella spp, Haemophilus influenzae, Neisseria gonorrhoeae and other aerobic Gram-negative strains of non-β-lactamase producing bacteria and Helicobacter pylori. Amoxicillin exerts its bactericidal effect by inhibiting bacterial cell wall synthesis, which can cause bacteria to rapidly become globular and dissolve and rupture.
【Pharmacokinetics】.
It is rapidly absorbed after oral administration, about 75%-90% can be absorbed from the gastrointestinal tract, the effect of food on drug absorption is not significant. The peak blood concentration (Cmax) after oral administration of 0, 25g, 0, 5g and 1g are 5, 1mg/L, 10, 8mg/L and 20, 6mg/L respectively, and the peak time is 1~2 hours. The product is well distributed in most tissues and body fluids. The mean drug concentrations in sputum 2-3 hours and 6 hours after oral administration of 0,5g of this product in patients with pneumonia or acute exacerbation of chronic bronchitis were 0,52mg/L and 0,53mg/L, respectively, while the blood concentrations were 11mg/L and 3,5mg/L during the same period. 6,2mg/L was found in the middle ear fluid 1-2 hours after oral administration of 1g of this product in children with chronic otitis media. The concentration in cerebrospinal fluid of patients with meningitis is 0.1-1.5mg/L 2 hours after taking 1g of this product orally, which is equivalent to 0.9%-21.1% of the blood concentration in the same period. It can pass through the placenta, and the concentration in the cord blood is ~ of the maternal blood concentration, and it also contains trace amounts in milk, sweat and tears. The protein binding rate of amoxicillin is 17%-20%. The blood elimination half-life (t1/2b) of this product is 1~1,3 hours, and about 24%~33% of the administered amount is metabolized in the liver after taking the drug, and 45%~68% within 6 hours.
Within 6 hours, 45%-68% of the administered amount is excreted in the urine as the prototype drug, and some of the drug is excreted via the biliary tract. The serum half-life can be extended to 7 hours in patients with severe renal insufficiency. Hemodialysis can clear this product, but peritoneal dialysis has no effect on the clearance of this product.
【Indications】.
Amoxicillin is indicated for the following infections caused by sensitive bacteria (non-β-lactamase-producing strains).
1, Streptococcus haemolyticus, Streptococcus pneumoniae, Staphylococcus or Haemophilus influenzae caused by otitis media, sinusitis, pharyngitis, tonsillitis and other upper respiratory tract infections.
2.Urogenital tract infections caused by Escherichia coli, Aspergillus chimaera or Enterococcus faecalis.
3.Streptococcus haemolyticus, Staphylococcus or Escherichia coli-induced skin soft tissue infections.
4.Lower respiratory tract infections such as acute bronchitis and pneumonia caused by Streptococcus haemolyticus, Streptococcus pneumoniae, Staphylococcus or Haemophilus influenzae.
5.Acute simple gonorrhea.
6.It can also be used for the treatment of typhoid fever, typhoid carriers and leptospirosis; amoxicillin can also be used in combination with clarithromycin and lansoprazole to eradicate Helicobacter pylori from the stomach and duodenum and reduce the recurrence rate of peptic ulcers.
【Dosage】.
Take orally. Adults: 0.5g once, once every 6-8 hours, not more than 4g per day; children: 20-40mg/kg per day, once every 8 hours; infants under 3 months: 30mg/kg per day, once every 12 hours.
Patients with severe renal impairment need to adjust the dose, including 0,25-0,5g every 12 hours for patients with endogenous creatinine clearance of 10-30 ml/min; 0,25-0,5g every 24 hours for patients with endogenous creatinine clearance less than 10 ml/min.
【Adverse reactions】.
1, nausea, vomiting, diarrhea and pseudomembranous enteritis and other gastrointestinal reactions.
2, allergic reactions such as rash, drug fever and asthma.
3, anemia, thrombocytopenia, eosinophilia, etc.
4.Serum aminotransferase may be mildly increased.
5.Dual infections caused by Candida or drug-resistant bacteria.
6, Occasionally see excitement, anxiety, insomnia, dizziness and abnormal behavior and other central nervous system symptoms.
Contraindications】：Penicillin allergy and positive penicillin skin test patients are prohibited.
【Caution】.
1, must do penicillin sodium skin test before use, positive reaction is prohibited.
2, patients with infectious mononucleosis are prone to rash, should be avoided.
3.Patients with longer course of treatment should check liver and kidney function and blood routine.
4. Amoxicillin may lead to false positive urine glucose test using Benedict or Fehling’s reagent.
5.It should be used with caution in the following cases.
(1) Those with a history of allergic diseases such as asthma and cushings fever.
(2) Dose adjustment may be required in the elderly and in cases of severe renal impairment.
[For pregnant and lactating women].
Animal reproduction tests have shown that 10 times the human dose of amoxicillin did not impair fertility or fetuses in rats and mice. However, there is a lack of controlled studies in humans, and given that animal reproduction tests are not fully predictive of human response, pregnant women should use this product only when necessary.
Because small amounts of amoxicillin can be secreted in breast milk, administration to lactating mothers may result in infant hypersensitivity.
[Drug Interactions].
1. Propofol competitively reduces the renal tubular secretion of this product, and the simultaneous application of both may cause an increase in amoxicillin blood concentration and prolong the half-life.
2. Chloramphenicol, macrolides, sulfonamides and tetracyclines interfere with the antibacterial effect of amoxicillin in vitro, but their clinical significance is unknown.
[Drug overdose].
In a prospective study involving 51 pediatric patients, it was suggested that amoxicillin administration at doses not exceeding 250 mg/kg did not cause significant clinical symptoms. Renal insufficiency and oliguria due to amoxicillin overdose have been reported in a few patients, but renal impairment is reversible after discontinuation of the drug.
Specification】0.25g*12#/box (dispersible tablets)
【Retail price】：13, 70/box
【Reimbursement Category】：public expense