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: Staphilococcus spp., (with the exception of strains producing penicillinase), Streptococcus spp., Listeria monocytogenes, Enterococcus faecalis and aerobic Gram-negative bacteria: Neisseria gonorrhoeae, Neisseria meningitidis, Haemophilus influenza, Escherichia coli, Shigella spp., Salmonella spp., Helicobacter pilori. The microorganisms that produce β-lactamase are resistant to the action of amoxicillin.

Pharmacokinetics:

After oral administration Amoxicillin absorbed quickly and almost completely (up to 93%), eating ns has an effect on absorption, does not break down in the acidic environment of the stomach.When administered orally at a dose of 250 mg and 500 mg, the maximum concentration of 5 μg / ml and 10 μg / ml, respectively. The time to reach the maximum concentration after oral administration is 1 to 2 hours. Amoxicillin It is widely distributed in tissues and body fluids: high concentrations found in plasma, bronchial secretions (in suppurative bronchial secretions distribution weak), liver, lymph nodes, uterus, ovaries, paranasal sinuses, pleural and peritoneal fluid, saliva and tear fluid, urine contents skin blisters, lung tissue, intestinal mucosa, middle ear fluid, and paranasal sinuses, bone, adipose tissue, the gall bladder (the concentration in the bile exceeding the concentration of plasma in 10 times - with Normal of the permeability of the bile ducts), the tissues of the fetus. When the dose is doubled, the concentration also doubles. In amniotic fluid and vessels of the umbilical cord, the concentration of amoxicillin is about 50% of the level in the plasma of a pregnant woman. Poorly penetrates the blood-brain barrier, inflammation of the meninges (meningitis) concentrations in the cerebrospinal fluid - is increased to 20% of plasma levels.Connection with plasma proteins - 1 5-25%.

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

Indications:

Bacterial infections caused by microorganisms sensitive to amoxicillin:

- infections of the upper respiratory tract (sinusitis, tonsillopharyngitis, acute otitis media);

- infection of the lower respiratory tract (acute bacterial bronchitis, exacerbation of chronic bronchitis, pneumonia);

- infection of the genitourinary system (pyelonephritis, pyelitis, cystitis, urethritis, endometritis, cervicitis);

- infections of the digestive system (peritonitis, enterocolitis, typhoid fever, cholangitis, cholecystitis, shigellosis, salmonellosis, salmonella)

- infections of the skin and soft tissues (erysipelas, impetigo, secondarily infected dermatoses);

- leptospirosis, listeriosis, Lyme disease (borreliosis), meningitis, endocarditis (prophylaxis), sepsis.

Contraindications:

Hypersensitivity (including to others.penicillins, cephalosporins, carbapenems), atopic dermatitis, bronchial asthma, pollinosis, infectious mononucleosis, lymphocytic leukemia, hepatic insufficiency, history of the gastrointestinal tract (especially colitis associated with the use of antibiotics), lactation period, children under 5 years.

Pregnancy and lactation:

The use of amoxicillin during pregnancy is possible only if the intended benefit to the mother exceeds the potential risk to the fetus and the baby. The drug is contraindicated in breastfeeding, as it is excreted in breast milk and can lead to the development of diarrhea and / or fungal colonization of the mucosa in newborns. It is also important to consider the possibility of sensitization of the newborn to beta-lactam antibiotics.

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) prescribe 250 mg 3 times a day or 500 mg 2 times a day; with sinusitis, community-acquired pneumonia and other serious infections it is recommended to prescribe 500 mg - 1000 mg 3 times a day. The maximum daily dose is 6000 mg.

Children aged 5-10 years (with a body weight of less than 40 kg) prescribe 20 mg - 40 mg / kg / day, divided into 3 doses or 25 mg - 45 mg / kg / day, divided into 2 doses. In cases where the probability of infection caused by a resistant Streptococcus pneumonia, higher doses are recommended at the rate of 80 mg / kg / day, divided into 3 doses or 90 mg / kg / day, divided into 2 doses. The maximum daily dose for children is 100 mg / kg / day.

In acute infectious diseases of the digestive system and bile ducts, with infections of the genitourinary system adults - 1500-2000 mg 3 times a day or 1000-1500 mg 4 times a day.

With Lyme disease (borreliosis)

Adults and children with a body weight above 40 kg are prescribed 500 mg - 1000 mg 3 times a day.

Children with body weight less than 40 kg - 50 mg / kg / day, divided into 3 doses.

With leptospirosis adults - 500 - 750 mg 4 times a day for 6-12 days. With salmonella carrying adults 1500-2000 mg 3 times a day for 2-4 weeks.

For the prevention of endocarditis with small surgical interventions for adults - 3000-4000 mg for 1 hour before the procedure. If necessary, appoint a second dose after 8-9 hours. In children, the dose is reduced by half.

Prophylaxis of endocarditis

Adults are recommended 3000 mg for 1 hour before surgery and 1500 mg - 6 hours after the procedure.

Children are recommended; 50 mg / kg / day before the procedure and 25 mg / kg / day - after the procedure.

Carefully

With renal insufficiency

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 - up to 24 hours with anuria - the maximum dose of 2000 mg / day.

Side effects:

Side effects are classified according to the gradation of frequency according to WHO classification as follows:

Often:> 1/100 and <1/10 infrequently:> 1/1000 and <1/100 Rarely:> 1/10000 and <1/1000 Very rarely, including isolated cases: <1/10000

Allergic reactions:

Often: hives, skin flushing, erythematous rashes are possible.

Rarely: angioedema (Quincke's edema), rhinitis, conjunctivitis, multiforme exudative erythema, exfoliative dermatitis, fever, joint pain, eosinophilia, Stevens-Johnson syndrome, reactions similar to serum sickness.

Rarely - anaphylactic shock.

From the digestive system:

Often: nausea, vomiting, diarrhea, dysbacteriosis, taste change, stomatitis, glossitis,

Disturbance of the liver and bile ducts:

Often: a violation of liver function, a moderate increase in the activity of "hepatic" transaminase.

Rarely: pseudomembranous colitis.

From the nervous system:

Rarely: agitation, anxiety, insomnia, ataxia, confusion, behavior change, depression, peripheral neuropathy, headache, dizziness, convulsive reactions.

Violations of the blood and lymphatic system:

Rarely: eosinophilia, hemolytic anemia.

Rarely: leukopenia, neutropenia, thrombocytopenic purpura, anemia.

Other:

Rarely: shortness of breath, tachycardia, interstitial nephritis.

Infrequently: superinfection (especially in patients with chronic diseases or reduced resistance of the body), candidiasis of the vagina.

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 forms para-aminobenzoic 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.

Perhaps the development of superinfection due to the growth of microflora insensitive to amoxicillin, 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 avoid antidiarrhoeal drugs that reduce intestinal peristalsis; it is possible to use kaolin - or attapulgite-containing prohydricaria. 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 or additional methods of contraception should be used whenever possible.

Effect on the ability to drive transp. cf. and fur:

Amoxicillin can affect the ability to drive vehicles and to engage in other potentially hazardous activities,requiring increased concentration of attention and speed of psychomotor reactions, since the drug is capable of causing dizziness and convulsions.

Form release / dosage:

Tablets 250 mg, 500 mg.

Packaging:

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

For 1, 2 contour mesh packages together with the instruction for use are placed in a pack of cardboard.

Storage conditions:

In a dry, protected from light place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

3 years. Do not use after expiry date.

Terms of leave from pharmacies:On prescription

Registration number:LP-000736

Date of registration:29.09.2011

Manufacturer: & nbsp

AVVA RUS, OJSC Russia

Information update date: & nbsp05.05.2014

Illustrated instructions

Instructions

Amoxicillin (Amoxicillin)