Pharmacological properties

Pharmacodynamics

Amoxicillin — a bactericidal antibiotic of a broad spectrum of activity of group of semi-synthetic penicillin. suppresses synthesis of a cell wall of bacteria. amoxicillin is inactive concerning microorganisms which make beta lactamelements. level of resistance of sensitive microorganisms can vary depending on the region.

To drug: gram-positive aerobes: Enterococcus faecalis, Listeria monocytogenes, beta and hemolytic streptococci (groups A, B, C, G) — Streptococcus agalactiae, Streptococcus bovis, Streptococcus pyogenes; gram-negative aerobes: Helicobacter pylori; anaerobe bacterias: Peptostreptococci; others: Borrelia.

(the acquired resistance can become a problem): Enterococcus faecium, Streptococcus pneumoniae, Streptococcus viridans, Escherichia coli, Haemophilus influenzae, Haemophilus parainfluenzae, Moraxella catarrhalis, Proteus mirabilis, Salmonella spp., Prevotella, Clostridium spp., Fusobacterium spp.

: Staphylococcus aureus, Acinetobacter, Citrobacter, Enterobacter, Klebsiella, Legionella, Morganella morganii, Proteus vulgaris, Providencia, Pseudomonas, Serratia, Bacteroides fragilis, Chlamydia, Mycoplasma, Rickettsia.

Pharmacokinetics

Absorption. The bioavailability of amoxicillin depends on a dose and is in limits of 75-90%. In doses of 250-1000 mg bioavailability (the max AUC and C _parameters ) it is linearly proportional to a dose. At higher doses the extent of absorption decreases. Meal practically does not influence medicine absorption. After reception of a single dose of 500 mg the concentration of amoxicillin in blood plasma makes 6–11 mg/l. The C _max in blood plasma is reached in 1–2 h

Distribution. About 17% of amoxicillin contact proteins of blood plasma. Therapeutic concentration is quickly reached in blood plasma, lungs, bronchial secretion, liquid of a middle ear, bile and urine. Concentration of medicine in bile exceeds its concentration in blood by 2–4 times. Amoxicillin badly gets into SMZh; however at inflammation of a meninx (for example at meningitis) concentration in SMZh makes about 20% of concentration in blood plasma.

Metabolism. Amoxicillin is partially metabolized, the majority of its metabolites are inactive.

Removal. Amoxicillin is emitted mainly with kidneys. About 60-80% of the accepted dose eliminirut in 6 h in not changed look. The t _½ medicine makes 1-1.5 h. In a renal failure of T _½ medicine increases and reaches 8.5 h at an anury.

T _½ medicine does not change at an abnormal liver function.

Indication

for treatment of such infections:

• sharp bacterial sinusitis;
• sharp otitis of a middle ear;
• sharp streptococcal tonsillitis and pharyngitis;
• exacerbation of chronic bronchitis;
• not hospital pneumonia;
• sharp cystitis;
• an asymptomatic bacteriuria during pregnancy;
• sharp pyelonephritis;
• tifoidny and paratifoidny fever;
• dental abscesses with widespread cellulitis;
• an infection of the fitted a prosthesis joints;
• Helicobacter pylori eradikation (as a part of combination therapy);
• Lyme's disease.

Drug is used for treatment and prevention of an endocarditis.

Dose of amoxicillin the doctor depending on age establishes to

, body weights and conditions of kidneys of the patient and also from sensitivity of microorganisms and localization of infectious process.

Adults and children with the body weight of ≥40 kg

Indication *	Dose *
Acute bacterial sinusitis	250-500 mg each 8 h or 750 mg – up to 1 g each 12 h
Asymptomatic bacteriuria during pregnancy
Acute pyelonephritis	in case of heavy infections: 750 mg – up to 1 g each 8 h In sharp cystitis it is possible to appoint 3 g 2 times a day for 1 day
Dental abscess with extensive cellulitis
Acute cystitis
Acute average otitis	500 mg each 8 h or 750 mg – to 1 g each 12 h in case of heavy infections — 750 mg-1 of each 8 h during 10 days
Acute streptococcal tonsillitis and pharyngitis
Exacerbation of chronic bronchitis
Not hospital pneumonia	500 mg – to 1 g each 8 h
Tifoidnaya and paratifoidny fever	500 mg – to 2 g each 8 h
Infection of the fitted a prosthesis joints	500 mg – to 1 g each 8 h
Prevention of an endocarditis	2 g in once in 30–60 min. to holding a procedure
Eradikation Helicobacter pylori as a part of combination therapy	750 mg-1 of 2 times in day in a combination with inhibitor of a proton pomp (for example omeprazolum, lansoprazoly) and other antibiotic (for example klaritromitsiny, metronidazole) during 7 days
Lyme's Disease	Initial stage — 500 mg-1 of each 8 h, the maximum dose — 4 g/days in stages during 14 days (the course of treatment can last from 10 to 21 days). A late stage (systemic lesions) — 500 mg-2 of each 8 h, the maximum dose — 6 g/days in stages within 10–30 days

* Should consider the official guides to appropriate treatment to each indication.

Children with the body weight of 40 kg

Indication *	Dose *
Acute bacterial sinusitis	From 20 to 90 mg/kg/days in stages ** (not to exceed a dose of 3 g/days). Usually to children at the age of 1–3 years appoint 250 mg 2 times a day or 125 mg 3 times a day. To children at the age of 3–12 years on 250 mg 3 times a day. Attention! Exact daily doses are calculated according to the body weight of the child, but not his age
Acute average otitis
Not hospital pneumonia
Acute sinusitis
Acute pyelonephritis
Dental abscess with extensive cellulitis
Acute streptococcal tonsillitis and pharyngitis	From 40 to 90 mg/kg/days in stages ** (not to exceed a dose of 3 g/days)
Tifoidnaya and paratifoidny fever	100 mg/kg/days in 3 receptions
Prevention of an endocarditis	50 mg/kg of body weight inside once in 30–60 min. prior to holding a procedure
Lyme's Disease	Initial stage — 25–50 mg/kg/days in 3 receptions within 10–21 days Late stage (systemic lesions) — 100 mg/kg/days in 3 receptions within 10–30 days

* Should consider the official guides to appropriate treatment for each indication.

** the Daily dose of medicine is recommended to be distributed on 2 receptions if it approaches the maximum recommended.

application Duration. In case of infections of easy and average degree to take the medicament within 5–7 days. However if infections are caused by a streptococcus, duration of treatment has to be not less than 10 days.

in case of chronic diseases, local infectious defeats, infections of a heavy current duration of treatment is defined on klinich