Description of the active substance:
This information is a reference and it is not enough that the drug has been prescribed by a doctor ..
PHARMACHOLOGIC EFFECT
Antibiotic of a group of semisynthetic penicillins of a wide spectrum of action. It is a 4-hydroxyl analogue of ampicillin. Has a bactericidal effect. It is active against aerobic gram-positive bacteria: Staphylococcus spp. (with the exception of strains producing penicillinase), Streptococcus spp .; aerobic Gram-negative bacteria: Neisseria gonorrhoeae, Neisseria meningitidis, Escherichia coli, Shigella spp., Salmonella spp., Klebsiella spp.
Amoxicillin is resistant to microorganisms that produce penicillinase.
In combination with metronidazole, it shows activity against Helicobacter pylori. It is believed that amoxicillin inhibits the development of Helicobacter pylori resistance to metronidazole.
Between amoxicillin and ampicillin there is cross-resistance.
The spectrum of antibacterial action expands with simultaneous use of amoxicillin and clavulanic acid beta-lactamase inhibitor. In this combination, amoxicillin activity increases with respect to Bacteroides spp., Legionella spp., Nocardia spp., Pseudomonas (Burkholderia) pseudomallei. However, Pseudomonas aeruginosa, Serratia marcescens and many other Gram-negative bacteria remain resistant.
PHARMACOKINETICS
When administered orally, amoxicillin is rapidly and completely absorbed from the digestive tract, does not degrade in the acidic environment of the stomach. C maxamoxicillin in blood plasma is achieved after 1-2 hours. When the dose is increased by 2 times, the concentration also doubles. In the presence of food in the stomach does not reduce the total absorption. When IV, in / m administration and ingestion in the blood, similar concentrations of amoxicillin are achieved.
The binding of amoxicillin with plasma proteins is about 20%.
Widely distributed in tissues and body fluids. High concentrations of amoxicillin in the liver are reported.
T 1/2 from the plasma is 1-1.5 hours. About 60% of the dose taken orally is excreted unchanged in the urine by glomerular filtration and tubular secretion; at a dose of 250 mg, the concentration of amoxicillin in urine is more than 300 Ојg / ml. Some amount of amoxicillin is determined in the feces.
In newborns and the elderly, T 1/2 may be longer.
With renal failure, T 1/2 can be 7-20 hours.
In small amounts, amoxicillin penetrates through the BBB during inflammation of the soft dura mater.
Amoxicillin is removed by hemodialysis.
INDICATIONS
For use in the form of monotherapy and in combination with clavulanic acid: infectious and inflammatory diseases caused by sensitive microorganisms, incl.bronchitis, pneumonia, tonsillitis, pyelonephritis, urethritis, gastrointestinal infections, gynecological infections, infectious diseases of the skin and soft tissues, listeriosis, leptospirosis, gonorrhea.
For use in combination with metronidazole: chronic gastritis in the phase of exacerbation, peptic ulcer of the stomach and duodenum in the acute phase associated with Helicobacter pylori.
DOSING MODE
Individual. For oral administration, a single dose for adults and children older than 10 years (with a body weight of more than 40 kg) is 250-500 mg, with a severe course of the disease - up to 1 g. For children aged 5-10 years, a single dose is 250 mg; at the age from 2 to 5 years - 125 mg; for children under 2 years of age, the daily dose is 20 mg / kg. For adults and children, the interval between doses is 8 hours. In the treatment of acute uncomplicated gonorrhea - 3 g once (in combination with probenecid). In patients with impaired renal function with KK 10-40 ml / min, the interval between doses should be increased to 12 h; with QC less than 10 ml / min, the interval between doses should be 24 hours.
For parenteral application to adults, I / m - 1 g 2 times / day, iv / (with normal kidney function) - 2-12 g / day. Children in / m - 50 mg / kg / day, single dose - 500 mg, frequency of administration - 2 times / day; in / in - 100-200 mg / kg / day. Patients with impaired renal function, dose and interval between administrations should be adjusted in accordance with the values ​​of CC.
SIDE EFFECT
Allergic reactions: urticaria, erythema, Quincke's edema, rhinitis, conjunctivitis; rarely - fever, joint pain, eosinophilia; in isolated cases - anaphylactic shock.
Effects associated with chemotherapeutic action: possible development of superinfections (especially in patients with chronic diseases or reduced resistance of the body).
With prolonged use in high doses: dizziness, ataxia, confusion, depression, peripheral neuropathies, convulsions.
Predominantly 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, hematopoietic disorders.
Advantageously when used in combination with clavulanic acid: cholestatic jaundice, hepatitis; rarely - erythema multiforme, toxic epidermal necrolysis, exfoliative dermatitis.
CONTRAINDICATIONS
Infectious mononucleosis, lymphocytic leukemia, severe gastrointestinal infections accompanied by diarrhea or vomiting, respiratory viral infections, allergic diathesis, bronchial asthma, hay fever, hypersensitivity to penicillins and / or cephalosporins.
For use in combination with metronidazole: diseases of the nervous system; disorders of hematopoiesis, lymphocytic leukemia, infectious mononucleosis;hypersensitivity to nitroimidazole derivatives.
For use in combination with clavulanic acid: a history of liver function abnormalities and jaundice associated with amoxicillin plus clavulanic acid.
PREGNANCY AND LACTATION
Amoxicillin penetrates through the placental barrier, in small quantities excreted in breast milk.
If you need to use amoxicillin during pregnancy, you should carefully weigh the expected benefit of therapy for the mother and the potential risk to the fetus.
Be wary of using amoxicillin during lactation (breastfeeding).
APPLICATION FOR FUNCTIONS OF THE LIVER
Patients with impaired renal function, dose and interval between administrations should be adjusted in accordance with the values ​​of CC.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
Amoxicillin in combination with metronidazole should not be used for liver disease.
APPLICATION FOR CHILDREN
Use in children is possible according to the dosing regimen.
Amoxicillin in combination with metronidazole is not recommended for use in patients younger than 18 years.
SPECIAL INSTRUCTIONS
Use with caution in patients prone to allergic reactions.
Amoxicillin in combination with metronidazole is not recommended for use in patients younger than 18 years of age; should not be used for liver disease.
Against the background of combined therapy with metronidazole, it is not recommended to drink alcohol.
DRUG INTERACTION
Amoxicillin can reduce the effectiveness of oral contraceptives.
With the simultaneous use of amoxicillin with bactericidal antibiotics (including aminoglycosides, cephalosporins, cycloserine, vancomycin, rifampicin), synergy appears; with bacteriostatic antibiotics (including macrolides, chloramphenicol, lincosamides, tetracyclines, sulfonamides) - antagonism.
Amoxicillin strengthens the effect of indirect anticoagulants suppressing the intestinal microflora, reduces the synthesis of vitamin K and prothrombin index.
Amoxicillin reduces the effect of drugs, in the process of metabolism which forms PABC.
Probenecid, diuretics, allopurinol, phenylbutazone, NSAIDs reduce the tubular secretion of amoxicillin, which can be accompanied by an increase in its concentration in the blood plasma.
Antacids, glucosamine, laxatives, aminoglycosides slow down and decrease, and ascorbic acid increases the absorption of amoxicillin.
With the combined use of amoxicillin and clavulanic acid, the pharmacokinetics of both components do not change.
