Amoxicillin

General characteristics. Structure:

Active agent: amoxicillin of 250 mg; 500 mg.

Pharmacological properties:

Antibiotic of group of semi-synthetic penicillin of a broad spectrum of activity. Represents a 4-hydroxylic analog of ampicillin. Has bactericidal effect. It is active concerning aerobic gram-positive bacteria: Staphylococcus spp. (except for the strains producing a penicillinase), Streptococcus spp; aerobic gram-negative bacteria: Neisseria gonorrhoeae, Neisseria meningitidis, Escherichia coli, Shigella spp., Salmonella spp., Klebsiella spp.
The microorganisms producing a penicillinase are steady against amoxicillin.
In a combination with metronidazole shows activity concerning Helicobacter pylori. Believe that amoxicillin inhibits development of resistance of Helicobacter pylori to metronidazole.
Between amoxicillin and ampicillin there is a cross resistance.
The range of antibacterial action extends at simultaneous use of amoxicillin and inhibitor beta лактамаз clavulanic acid. In this combination activity of amoxicillin concerning Bacteroides spp increases., Legionella spp., Nocardia spp., Pseudomonas (Burkholderia) pseudomallei. However Pseudomonas aeruginosa, Serratia marcescens and a set of other gram-negative bacteria remain resistant.

Pharmacokinetics. At intake amoxicillin is quickly and completely absorbed from a GIT, does not collapse in acid medium of a stomach. Cmax of amoxicillin in a blood plasma is reached in 1-2 h. At increase in a dose twice concentration also increases twice. In the presence of food in a stomach does not reduce the general absorption. At in/in, introduction in oil and intake to blood similar concentration of amoxicillin are reached.
Linkng of amoxicillin with proteins of plasma makes about 20%.
It is widely distributed in fabrics and liquids of an organism. It is reported about high concentration of amoxicillin in a liver.
T1/2 makes 1-1.5 h of plasma. About 60% of the dose accepted inside are removed in not changed view with urine by glomerular filtering and canalicular secretion; at a dose of 250 mg concentration of amoxicillin in urine makes more than 300 mkg/ml. A quantity of amoxicillin is defined in Calais.
At newborns and elderly people of T1/2 can be longer.
At a renal failure of T1/2 can make 7-20 h.
In small amounts amoxicillin gets through GEB at an inflammation of a soft meninx.
Amoxicillin is removed by a hemodialysis.

Indications to use:

For use in the form of monotherapy and in a combination with clavulanic acid: the infectious and inflammatory diseases caused by sensitive microorganisms including bronchitis, pneumonia, quinsy, pyelonephritis, an urethritis, GIT infections, gynecologic infections, infectious diseases of skin and soft tissues, listeriosis, leptospirosis, gonorrhea.

For use in a combination with metronidazole: chronic gastritis in an aggravation phase, a peptic ulcer of a stomach and duodenum in an aggravation phase, associated with Helicobacter pylori.

Route of administration and doses:

Individual. For intake the single dose for adults and children is more senior than 10 years (with body weight more than 40 kg) makes 250-500 mg, at a severe disease - to 1 g. For children at the age of 5-10 years the single dose makes 250 mg; aged from 2 up to 5 years - 125 mg; for children under 2 years the daily dose makes 20 mg/kg. For adults and children an interval between receptions of 8 h. At treatment of acute uncomplicated gonorrhea - 3 g once (in a combination with probenetsidy). At patients with a renal failure at KK of 10-40 ml/min. the interval between receptions should be increased to 12 h; at KK less than 10 ml/min. the interval between receptions has to make 24 h.

Features of use:

With care apply at the patients inclined to allergic reactions.
In a combination with metronidazole 18 years do not recommend to apply amoxicillin at patients more young; it is not necessary to apply at liver diseases.
Against the background of a combination therapy with metronidazole it is not recommended to take alcohol.

Side effects:

Allergic reactions: small tortoiseshell, erythema, Quincke's edema, rhinitis, conjunctivitis; seldom - fever, joint pains, an eosinophilia; in isolated cases - an acute anaphylaxis.
The effects connected with chemotherapeutic action: development of superinfections is possible (especially at patients with chronic diseases or the lowered resistance of an organism).
At prolonged use in high doses: dizziness, ataxy, confusion of consciousness, depression, peripheral neuropathies, spasms.
Preferential at use in a combination with metronidazole: nausea, vomiting, anorexia, diarrhea, a lock, pains in epigastriums, a glossitis, stomatitis; seldom - hepatitis, pseudomembranous colitis, allergic reactions (a small tortoiseshell, a Quincke's disease), intersticial nephrite, disturbances of a hemogenesis.
Preferential at use in a combination with clavulanic acid: cholestatic jaundice, hepatitis; seldom - a mnogoformny erythema, a toxic epidermal necrolysis, exfoliative dermatitis.

Interaction with other medicines:

Amoxicillin can reduce efficiency of contraceptives for intake.

At simultaneous use of amoxicillin with bactericidal antibiotics (including aminoglycosides, cephalosporins, Cycloserinum, Vancomycinum, rifampicin) show a synergism; with bacteriostatic antibiotka (including macroleads, chloramphenicol, linkozamida, tetracyclines, streptocides) - antagonism.

Amoxicillin strengthens effect of indirect anticoagulants suppressing intestinal microflora, reduces synthesis of vitamin K and a prothrombin ratio.

Amoxicillin reduces effect of medicines in the course of which metabolism PABK is formed.

Probenetsid, diuretics, Allopyrinolum, phenylbutazone, NPVS reduce canalicular secretion of amoxicillin that can be followed by increase in its concentration in a blood plasma.

Antacids, glycosamine, purgatives, aminoglycosides slow down and reduce, and ascorbic acid increases amoxicillin absorption.

At the combined use of amoxicillin and clavulanic acid the pharmacokinetics of both components does not change.

Contraindications:

The infectious mononucleosis, lymphoid leukosis, heavy infections of a GIT which are followed by diarrhea or vomiting, respiratory viral infections, allergic diathesis, bronchial asthma, hay fever, hypersensitivity to penicillin and/or cephalosporins.
For use in a combination with metronidazole: diseases of a nervous system; hemopoiesis disturbances, lymphoid leukosis, infectious mononucleosis; hypersensitivity to nitroimidazole derivatives.
For use in a combination with clavulanic acid: instructions in the anamnesis on the abnormal liver functions and jaundice connected with reception of amoxicillin in a combination with clavulanic acid.

Use at pregnancy and feeding by a breast
Amoxicillin gets through a placental barrier, in small amounts is emitted with breast milk.
In need of use of amoxicillin at pregnancy it is necessary to weigh carefully expected advantage of therapy for mother and potential risk for a fruit.
With care to apply amoxicillin in the period of a lactation (breastfeeding).

Use at abnormal liver functions
Amoxicillin in a combination with metronidazole should not be applied at liver diseases.

Use at renal failures
To patients with a renal failure, it is necessary to adjust a dose and an interval between introductions according to KK values.

Use for children
Use for children is possible according to the dosing mode.
In a combination with metronidazole 18 years do not recommend to apply amoxicillin at patients more young.

Overdose:

There are no data.

Storage conditions:

List B. In the dry, cool place.

Issue conditions:

According to the recipe

Packaging:

Tablets of 250 mg: 10 or 20 pieces.