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Antibiotic of group semisynthetic penicillins a wide spectrum of action. It is a 4-hydroxyl analog of ampicillin. It has bactericidal action. amoxicillin is active against aerobic gram-positive bacteria: Staphylococcus spp. (except strains producing penicillinase), Streptococcus spp; aerobic gram-negative bacteria: Neisseria Gonorrhoeae, Neisseria Meningitidis, Escherichia Coli, Shigella spp., Salmonella spp., Klebsiella spp.
Microorganisms producing penicillinase is resistant to amoxicillin.
In combination with metronidazole is active against Helicobacter Pylori. It is believed that inhibits the development of amoxicillin resistance of Helicobacter pylori to metronidazole.
There is a cross-resistance between amoxycillin and ampicillin.
The spectrum of antibacterial action while expanding the application of amoxicillin and beta-lactamase inhibitor clavulanic acid. This combination increased the activity of amoxicillin against Bacteroides spp., Legionella spp., Nocardia spp., Pseudomonas (Burkholderia) Pseudomallei. However, Pseudomonas Aeruginosa, Serratia Marcescens, and many other gram-bacteria are resistant.
When administered orally amoxicillin rapidly and completely absorbed from the gastrointestinal tract and is not destroyed in the acidic environment of the stomach. Cmax of amoxicillin in the blood plasma is reached after 1-2 h. When increasing doses of 2 times the concentration also increased by 2 times. In the presence of food in the stomach does not reduce the overall removals. Similar concentrations of amoxicillin reached in the blood when administered orally, IV and IM.
The binding of amoxicillin to plasma proteins is about 20%.
Widely distributed in tissues and body fluids. Reported high concentrations of amoxicillin in the liver.
T1/2 from the plasma is 1-1.5 h. About 60% of the dose adopted by mouth, is excreted unchanged in the urine by glomerular filtration and tubular secretion, with a dose of 250 mg of amoxicillin concentration in urine exceeds 300 micrograms / ml. A number of amoxicillin is determined in feces.
T1/2 for Newborns and the elderly can be longer.
In renal insufficiency T1/2 may be 7-20 hours.
In small quantities amoxicillin penetrates through BBB in inflammation of the pia mater.
amoxicillin is removed by hemodialysis.
For use as monotherapy and in combination with clavulanic acid: an infectious-inflammatory diseases caused by susceptible microorganisms, including bronchitis, pneumonia, tonsillitis, pyelonephritis, urethritis, infections of the gastrointestinal tract, gynecological infections, infections of the skin and soft tissue, listeria, leptospirosis, gonorrhea.
For use in combination with metronidazole: chronic gastritis in acute, peptic ulcer and duodenal ulcer in acute, associated with Helicobacter Pylori.
Individual. For oral single dose for adults and children over 10 years (body weight over 40 kg) is 250-500 mg, in case of serious illness - up to 1 g. For children aged 5-10 years, a single dose of 250 mg in age from 2 to 5 years - 125 mg for children aged under 2 years of daily dose is 20 mg / kg. For adults and children interval is 8 h. In the treatment of acute uncomplicated gonorrhea - 3 g once (in combination with probenecid). Patients with impaired renal function in creatinine clearance 10-40 ml / min interval between doses should be increased to 12 h and if creatinine clearance is less than 10 ml / min interval between doses should be 24 hours.
When parenteral use in adults IM - 1 g 2 times / day, IV (with normal renal function) - 2.12 g / day. Children IM 50 mg / kg / day, single dose - 500 mg, the frequency of administration - 2 times / day; IV - 100-200 mg / kg / day. Patients with impaired renal function the dose and the interval between the injections need to be adjusted in accordance with the values of creatinine clearance.
Allergic reactions: urticaria, erythema, edema Quincke, rhinitis, conjunctivitis, rarely - fever, joint pain, eosinophilia, in rare cases - anaphylactic shock.
Side effects associated with chemotherapy effect: possible development of super-infection (particularly in patients with chronic diseases or low resistance of the organism).
With prolonged use at high doses: dizziness, ataxia, confusion, depression, peripheral neuropathy, seizures.
Mostly when used in combination with metronidazole: nausea, vomiting, anorexia, diarrhea, constipation, epigastric pain, glossitis, stomatitis; rarely - hepatitis, pseudomembranous colitis, allergic reactions (urticaria, angioedema), interstitial nephritis, a violation of hematopoiesis.
Mostly when used in combination with clavulanic acid: cholestatic jaundice, hepatitis, rarely - erythema multiforme, toxic epidermal necrolysis, exfoliative dermatitis.
Infectious mononucleosis, lymphatic leukemia, severe gastrointestinal infections, accompanied by diarrhea or vomiting, respiratory viral infection, allergic diathesis, bronchial asthma, hay fever, sensitivity to penicillin and / or cephalosporins.
For use in combination with metronidazole: diseases of the nervous system; hemodyscrasia, lymphocytic leukemia, an infectious mononucleosis; Hypersensitivity to nitroimidazole derivatives.
For use in combination with clavulanic acid: a history of instructions for liver problems and jaundice, associated with the reception of amoxicillin in combination with clavulanic acid.
amoxicillin crosses the placenta, in small amounts excreted in breast milk.
If necessary the use of amoxicillin during pregnancy should carefully weigh the potential benefits of therapy for the mother and the potential risk to the fetus.
With careful use amoxicillin during lactation (breastfeeding).
With caution used in patients prone to allergic reactions.
amoxicillin in combination with metronidazole is not recommended to use in patients younger than 18 years should not be used for liver diseases.
In the combined therapy with metronidazole is recommended not to drink alcohol.
Treatment must continue 48-72 hours after the disappearance of clinical signs of disease, with streptococcal infections - 10 days.
During the course treatment is necessary to control the state functions of hematopoiesis, liver and kidneys.
Perhaps the development of superinfection due to growth insensitive to the drug microflora. In the case of superinfection requires removal of amoxicillin and the corresponding change in antibiotic therapy. When treating patients with bacteremia may develop bacteriolysis reaction (reaction of Jarisch-Herxheimer).
Patients who have an increased sensitivity to penicillin, may be cross-allergic reactions to cephalosporin antibiotics.
In the treatment of mild diarrhea at the background of the treatment should be avoided antidiarrhoeal drugs that reduce intestinal motility; can use kaolin or attapulgite containing antidiarrhoeal stuff. Patients with severe diarrhea should consult a doctor.
With simultaneous use of oral contraceptives estrogensoderzhaschih and amoxicillin should if possible to use additional methods of contraception.
amoxicillin may decrease the effectiveness of contraceptives for oral administration.
With the simultaneous use of amoxicillin with bactericidal antibiotics (including aminoglycosides, cephalosporins, cycloserine, vancomycin, rifampicin) appears synergies; with bacteriostatic antibiotic (including macrolides, chloramphenicol, lincosamides, tetracyclines, sulphonamide) - antagonism.
amoxicillin increases the effects of indirect anticoagulants inhibiting intestinal microflora, reduces the synthesis of vitamin K and prothrombin index.
amoxicillin reduces the effect of drugs, in the process of metabolism that produce PABA.
Probenecid, diuretics, allopurinol, phenylbutazone, NSAIDs decrease the tubular secretion of amoxicillin, which can be accompanied by an increase in its concentration in blood plasma.
Antacids, glucosamine, laxatives, aminoglycosides, slow down and reduce, and ascorbic acid increases the absorption of amoxicillin.
With the combined use of amoxicillin and clavulanic acid pharmacokinetics of both components unchanged.
Symptoms: nausea, vomiting, diarrhea, disruption of water and electrolyte balance (as a result of vomiting and diarrhea); for prolonged use at high doses - neurotoxic reactions and thrombocytopenia (these phenomena are reversible and disappear after drug withdrawal).
Treatment: gastric lavage, the prescription of activated charcoal, saline laxatives, correction of water and electrolyte balance; hemodialysis.
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