Amoxicillin - instructions for use, dose, side effects, contraindications

Antibacterial bactericidal acid-resistant broad spectrum agent from the group of semisynthetic penicillins. It inhibits transpeptidase, breaks the synthesis of peptidoglycan (the supporting protein of the cell wall) in the period of division and growth, causes bacterial lysis. It is active against aerobic gram-positive bacteria: Staphylococcus spp. (with the exception of strains producing penicillinase), Streptococcus spp; and aerobic Gram-negative bacteria: Neisseria gonorrhoeae, Neisseria meningitidis, Escherichia coli, Shigella spp., Salmonella spp., Klebsiella spp. The microorganisms producing penicillinase are resistant to the action of amoxicillin. The action develops 15-30 minutes after administration and lasts 8 hours.

Pharmacokinetics:

Absorption - fast, high (93%), food intake does not affect absorption, does not break down in the acidic environment of the stomach.When administered orally at a dose of 125 and 250 mg, the maximum concentration is 1.5-3 μg / ml and 3.5-5 μg / ml, respectively. The time to reach the maximum concentration after oral administration is 1-2 hours. It has a large volume of distribution - high concentrations are found in plasma, sputum, bronchial secretion (in the purulent bronchial secretion the distribution is weak), pleural and peritoneal fluid, urine, skin blisters, lung tissue , intestinal mucosa, female genital organs, prostate gland, middle ear fluid, bone, adipose tissue, gall bladder (with normal liver function), fetal tissues. When the dose is doubled, the concentration is also increases by 2 times. Concentration in bile exceeds the concentration in plasma by 2-4 times. In amniotic fluid and vessels of the umbilical cord, the concentration of amoxicillin is 25-30% of the level in the plasma of a pregnant woman. Poor penetration through the blood-brain barrier, with inflammation of the meninges (meningitis) concentration in spinal fluid - about 20%. The connection with plasma proteins is 17%.

Partially metabolized with the formation of inactive metabolites. The half-life is 1-1.5 hours.It is excreted by 50-70% kidneys unchanged through tubular excretion (80%) and glomerular filtration (20%), the liver - 10-20%. In small amounts excreted in breast milk. If the kidney function is impaired (creatinine clearance less than or equal to 15 ml / min), the elimination half-life increases to 8.5 hours. Amoxicillin is removed during hemodialysis.

Indications:

Bacterial infections caused by sensitive microflora: infections of the respiratory tract and ENT organs (sinusitis, pharyngitis, tonsillitis, acute otitis media, bronchitis, pneumonia), urogenital system (pyelonephritis, pyelitis, cystitis, urethritis, gonorrhea, endometritis, cervicitis) intestinal tract (peritonitis, enterocolitis, typhoid fever, cholangitis, cholecystitis), skin and soft tissue infections (rye, impetigo, secondarily infected dermatoses), leptospirosis, listeriosis, Lyme disease (borreliosis), dysentery, salmonellosis, salmonella, meningi t, endocarditis (prophylaxis), sepsis.

Contraindications:

Hypersensitivity (including to other penicillins, cephalosporins, carbapenems), allergic diathesis, bronchial asthma, pollinosis, infectious mononucleosis, lymphocytic leukemia, hepatic insufficiency,diseases of the gastrointestinal tract in the anamnesis (especially colitis, associated with the use of antibiotics), lactation period.

Children under 10 years old (for this dosage form).

Carefully:

Pregnancy, renal insufficiency, bleeding in the anamnesis.

Dosing and Administration:

Inside, before or after eating.

Adults and children over 10 years of age (with a body weight of more than 40 kg) are prescribed 0.5 g 3 times a day; in severe infection - 0.75-1 g 3 times a day.

In acute uncomplicated gonorrhea appoint 3 g once; in the treatment of women, repeated intake of this dose is recommended.

In acute infectious diseases of the gastrointestinal tract (paratyphoid, typhoid) and biliary tract, with gynecological infectious diseases adults - 1.5-2 g 3 times a day or 1-1.5 g 4 times a day.

When leptospirosis adults - 0.5-0.75 g 4 times a day for 6-12 days.

With salmonella carrying adults - 1.5-2 g 3 times a day for 2-4 ned.

For the prevention of endocarditis with small surgical interventions for adults - 3-4 g for 1 h before the procedure. If necessary, appoint a second dose after 8-9 hours. In children, the dose is reduced by half.

In patients with impaired renal function with creatinine clearance of 15-40 ml / min, the interval between doses is increased to 12 h; with clearance of creatinine below 10 ml / min the dose is reduced by 15-50%; with anuria - the maximum dose of 2 g / day.

Side effects:

Allergic reactions: hives, skin flushing, erythema, angioedema, rhinitis, conjunctivitis; rarely - fever, joint pain, eosinophilia, exfoliative dermatitis, polymeric exudative erythema, Stevens-Johnson syndrome; reactions similar to serum sickness; in isolated cases - anaphylactic shock.

From the digestive system: dysbacteriosis, taste change, vomiting, nausea, diarrhea, stomatitis, glossitis, impaired liver function, moderate increase in the activity of "liver" transaminases, pseudomembranous enterocolitis,

From the nervous system: agitation, anxiety, insomnia, ataxia, confusion, behavior change, depression, peripheral neuropathy, headache, dizziness, convulsive reactions.

Laboratory indicators: leukopenia, neutropenia, thrombocytopenic purpura, anemia.

Other: shortness of breath, tachycardia, interstitial nephritis, vaginal candidiasis, superinfection (especially in patients with chronic diseases or reduced resistance of the body).

Overdose:

Symptoms include nausea, vomiting, diarrhea, disruption of water and electrolyte balance (as a result of vomiting and diarrhea). Treatment: gastric lavage, Activated carbon, salt laxatives, preparations for maintaining the water-electrolyte balance; hemodialysis.

Interaction:

Antacids, glucosamine, laxatives, food, aminoglycosides - slow down and reduce absorption; ascorbic acid increases absorption.

Bactericidal antibiotics (including aminoglycosides, cephalosporins, cycloserine, vancomycin, rifampicin) - synergistic effect; bacteriostatic drugs (macrolides, chloramphenicol, lincosamides, tetracyclines, sulfonamides) - antagonistic.

Increases the effectiveness of indirect anticoagulants (suppressing the intestinal microflora, reduces the synthesis of vitamin K and prothrombin index); reduces the effectiveness of estrogen-containing oral contraceptives, drugs,in the process of metabolism of which is formed paraminobenzoic acid, ethinyl estradiol - the risk of bleeding "breakthrough".

Diuretics, allopurinol, oxyphenbutazone, phenylbutazone, non-steroidal anti-inflammatory drugs; drugs that block tubular secretion - reducing tubular secretion, increase concentration.

Allopurinol increases the risk of skin rash.

Reduces clearance and increases the toxicity of methotrexate.

Increases the absorption of digoxin.

Special instructions:

In course treatment it is necessary to monitor the status of the functions of the organs of hematopoiesis, liver and kidneys.

It is possible to develop superinfection due to the growth of insensitive microflora, which requires a corresponding change in antibacterial therapy.

In the treatment of patients with bacteremia, the development of a bacteriolysis reaction (the Yarisch-Gerxheimer reaction) is possible.

In patients who are hypersensitive to penicillins, there may be cross-allergic reactions with cephalosporin antibiotics.

In the treatment of mild diarrhea against the background of course treatment should be avoided antidiarrheal drugs,reducing peristalsis of the intestine; it is possible to use kaolin- or attapulgite-containing antidiarrhoeic agents. With severe diarrhea, you should see a doctor.

Treatment necessarily continues for another 48-72 hours after the disappearance of clinical signs of the disease.

With the simultaneous use of estrogen-containing oral contraceptives and amoxicillin, other possible or additional contraceptive methods should be used whenever possible.

Form release / dosage:Tablets of 250 mg.

Packaging:

For 10 tablets in a contour mesh box made of polyvinylchloride film and aluminum foil printed lacquered.

2, 3, 4 or 5 contour mesh packages together with the instruction for use are placed in a pack of cardboard.

Storage conditions:

List B.

In dry, dark place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:2 years. Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LSR-003896/07

Date of registration:19.11.2007 / 29.12.2011

Expiration Date:Unlimited

The owner of the registration certificate:DALHIMFARM, OJSC DALHIMFARM, OJSC Russia

Manufacturer: & nbsp

DALHIMFARM, OJSC Russia

Information update date: & nbsp19.08.2017

Illustrated instructions

Instructions

Amoxicillin (Amoxycillin)