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

Antibiotic of a group of semisynthetic penicillins of a wide spectrum of action. Has a bactericidal effect. 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. Active against aerobic Gram-positive bacteria (Staphylococcus spp. (with the exception of strains producing penicillinase), Streptococcus spp.), aerobic Gram-negative bacteria (Neisseria gonorrhoeae, Neisseria meningitides, Escherichia coli, Shigella spp., Salmonella spp., Klebsiella spp.). The microorganisms producing penicillinase are resistant to the action of amoxicillin.

Pharmacokinetics:

Ingestion amoxicillin quickly and almost completely (93%) is absorbed from the gastrointestinal tract, does not break down in the acidic environment of the stomach,eating does not affect absorption. The maximum concentration (C_m_Oh) when administered orally at a dose of 125 mg and 250 mg is 1.5-3 μg / ml and 3.5-5 μg / ml, respectively. Time to reach the maximum concentration (TC_m_Oh) -1-2 hours.

Has a large volume of distribution - high concentrations are found in plasma, sputum, bronchial secretion (in the purulent bronchial secretion is weak), pleural and peritoneal fluid, urine, skin blisters, lung tissue, intestinal mucosa, female genital organs, prostate gland, fluid middle ear, bones, adipose tissue, gallbladder (with normal liver function), fetal tissues. When the dose is doubled, the concentration also doubles. 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. Badly penetrates the blood-brain barrier, with inflammation of the meninges (meningitis), the concentration in the cerebrospinal fluid is about 20% of the plasma level. The connection with plasma proteins is 17%.

Partially metabolized with the formation of inactive metabolites.

It is excreted by 50-70% by kidneys in the unchanged form (by tubular excretion - 80% and glomerular filtration - 20%), liver - 10-20%. In small amounts excreted in breast milk. Half-life (T_1/2) - 1-1.5 hours.

If the renal function is impaired (creatinine clearance less than or equal to 15 ml / min), the elimination half-life (T_1/2) increases to 8.5 h.

Indications:

Infectious-inflammatory diseases caused by sensitive microflora: respiratory tract infections (bronchitis, pneumonia) and ENT organs (sinusitis, pharyngitis, tonsillitis, acute otitis media), urogenital system (pyelonephritis, pyelitis, cystitis, urethritis, gonorrhea, endometritis, cervicitis) (enterocolitis, typhoid fever, cholangitis, cholecystitis), skin and soft tissue infections (rye, impetigo, secondarily infected dermatoses), leptospirosis, listeriosis, Lyme disease (borreliosis), dysentery, salmonellosis, salmonella (prevention).

Contraindications:

Hypersensitivity (including to other penicillins, cephalosporins, carbapenems), children's age to 3 years.

Carefully:

Allergic diseases (including in the anamnesis), infectious mononucleosis and lymphatic leukemia, diseases of the gastrointestinal tract in the anamnesis (especially colitis associated with the use of antibiotics), renal failure.

Pregnancy and lactation:

Possible applications for pregnancy and lactation, if the expected effect of therapy exceeds the potential risk to the fetus and the baby.

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 500 mg (2 tablets) 3 times a day; in severe infection - 750-1000 mg (3-4 tablets) 3 times a day.

Children aged 5-10 years - 250 mg (1 tablet) 3 times a day; 3-5 years - on 125 mg (on 1/2 tablets) 3 times a day.

The course of treatment is 5-12 days.

In acute uncomplicated gonorrhea appoint 3000 mg (12 tablets) 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 - 1500-2000 mg (6-8 tablets) 3 times a day or 1000-1500 mg (4-6 tablets ) 4 times a day.

When leptospirosis adults - 500 -750 mg (2-3 tablets) 4 times a day for 6 to 12 days.

In case of salmonella-bearing adults - 1500-2000 mg (6-8 tablets) 3 times a day for 2-4 weeks.

For the prevention of endocarditis in small surgical interventions for adults - 3000-4000 mg (12-16 tablets) for 1 hour 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; when creatinine clearance is less than 10 ml / min, the dose is reduced by 15-50%; with anuria - the maximum dose of 2.0 g / day.

Side effects:

Allergic reactions: possible hives, hyperemia of the skin, erythema, angioedema, rhinitis, conjunctivitis; rarely - fever, pain in the joints, eosinophilia, exfoliative dermatitis, polymeric exudative erythema (incl. 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, moderate increase in the activity of "liver" transaminases, rarely - pseudomembranous enterocolitis.

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

Changes in 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: nausea, vomiting, diarrhea, violation of water-electrolyte balance (as a consequence 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 the absorption of amoxicillin; ascorbic acid increases the absorption of amoxicillin.

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

Amoxicillin improves 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 which produces paraaminobenzoic acid and ethinyl estradiol, which increases the risk of bleeding "breakthrough".

Diuretics, allopurinol, oxyphenbutazone, phenylbutazone, non-steroidal anti-inflammatory drugs, drugs that block tubular secretion, increase the concentration of amoxicillin in the blood.

With the combined use of amoxicillin and allopurinol, the risk of developing skin rashes increases.

Amoxicillin reduces clearance and increases the toxicity of methotrexate.

Amoxicillin enhances 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.

Perhaps the development of superinfection due to the growth of microflora insensitive to amoxicillin,which requires an appropriate change in antibacterial therapy.

When treating patients with bacteremia, the development of a bacteriolysis reaction (the Yarisch-Gerxheimer reaction) is possible (rarely).

In patients who have increased sensitivity to penicillins, allergic reactions with other beta-lactam antibiotics (penicillins, cephalosporins, carbapenems) are possible.

When treating mild diarrhea against the background of course treatment with amoxicillin, antidiarrheal drugs should be avoided, which reduce intestinal peristalsis; can use kaolin- or attapulgite-containing antidiarrhoeic agents. With severe diarrhea, you should see a doctor.

Treatment with amoxicillin must necessarily continue for another 48-72 hours after the disappearance of clinical signs of the disease.

When using estrogen-containing oral contraceptives and amoxicillin concomitantly, other or additional methods of contraception should be used whenever possible.

Form release / dosage:

Tablets of 250 mg.

Packaging:

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

1 or 2 contour squares, together with instructions for use, are placed in a pack of cardboard for consumer containers.

Storage conditions:

List B. In dry the 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 time specified on the package.

Terms of leave from pharmacies:On prescription

Registration number:LS-000176

Date of registration:18.07.2008

Expiration Date:Unlimited

The owner of the registration certificate:VALENTA PHARM, PAO VALENTA PHARM, PAO Russia

Manufacturer: & nbsp

VALENTA PHARMACEUTICS, JSC Russia

Information update date: & nbsp19.08.2017

Illustrated instructions

Instructions

Amoxicillin (Amoxicillin)