Amoxicillin pills 1g №12

pharmachologic effect

Amoxicillin is an aminobenzyl penicillin, which has a bactericidal effect as a result of inhibiting the synthesis of bacterial cell walls.

MIC thresholds vary for different sensitive organisms.

Enterobacteriaceae are considered sensitive when inhibited by amoxicillin at a concentration of ≤ 8 μg / ml of amoxicillin and resistant at a concentration of ≥ 32 μg / ml.

In accordance with the recommendations of the NCCLS and when using the NCCLS-specified methodsM. catarrhalis(β-lactamase negative) andN. influenzae(β-lactamase negative) are regarded as sensitive at concentrations of ≤ 1 μg / ml and resistant at ≥ 4 μg / ml;Str.pneumoniaeare considered sensitive when MIC ≤ 2 mcg / ml and resistant when ≥ 8 mcg / ml.

The prevalence of resistant strains varies geographically, so it is desirable to focus on local information on resistance, especially in the treatment of severe infections. At this level of prevalence of resistant strains, at which the feasibility of using the drug becomes questionable, at least in the treatment of certain infections, it is better to seek help from a specialist.

Sensitive:

^a)% of the production of p-lactamase.

^b)penicillin resistance (including intermediate resistance).

# To date, there are no reports of the appearance of r-lactamase-producing strains.

^§ Non-constant sensitivity, it is impossible to predict sensitivity without testing for sensitivity.

^* Clinical efficacy has been shown for sensitive strains when used as indicated.

Bacteria can be resistant to amoxicillin (and, consequently, ampicillin) as a result of production of beta-lactamase, hydrolyzing aminopenicillins, changes in penicillin-binding proteins, impaired permeability to the drug or due to the functioning of special pump pumps that pump the drug out of the cell. In one microorganism, several mechanisms of resistance can be simultaneously present, which explains the existence of variable and unpredictable cross-resistance to other beta-lactams and antibacterial drugs from other groups.

Pharmacokinetics

Suction:

The absolute bioavailability of amoxicillin depends on the dose and mode of administration and is in the range from 75 to 90%. In doses of 250 mg to 750 mg, bioavailability (parameters: AUC and / or urinary excretion) is linearly proportional to the dose. At higher doses, absorbability is lower. Intake is not affected by food intake. Amoxicillin is acid resistant. In the case of an oral single dose of 500 mg, the concentration of amoxicillin in the blood is 6-11 mg / l. After a single dose of 3 g of amoxicillin, the concentration in the blood reaches 27 mg / l. C_maxin plasma observed 1 to 2 hours after taking the drug.

Distribution:

About 17% of amoxicillin is in a state bound to plasma proteins. Therapeutic drug concentration is quickly reached in plasma, lungs, bronchial secretions, middle ear fluid, bile and urine. Amoxicillin can penetrate the inflamed meninges into the cerebrospinal fluid. Amoxicillin passes through the placenta and is found in small amounts in breast milk.

Biotransformation and elimination:

The main place of removal of amoxicillin are the kidneys. About 60-80% of the oral dose of amoxicillin is excreted within 6 hours after administration in the unchanged active form via the kidneys and a small fraction is excreted into the bile. Approximately 7–25% of the dose is metabolized to inactive penicilloic acid. The half-life of plasma in patients with unchanged kidney function is 1-1.5 hours.In patients with severe renal failure, the half-life varies from 5 to 20 hours. The substance is susceptible to hemodialysis.

Indications

It is indicated for oral therapy of the following bacterial infections caused by amoxicillin-sensitive gram-positive and gram-negative pathogens:

- infections of the upper respiratory tract, including infections of the ear, nose and throat: acute otitis media, acute sinusitis and pharyngitis.

- lower respiratory tract infections: exacerbation of chronic bronchitis, community-acquired pneumonia.

- infections of the lower urinary tract: cystitis.

- infections of the gastrointestinal tract: bacterial enteritis. Combination therapy may be required for infections caused by anaerobic microorganisms.

- endocarditis: prevention of endocarditis in patients at risk for the development of endocarditis - for example, during dental procedures.

Dosing regimen

Inside

Infection Therapy:

As a rule, therapy is recommended to continue for 2-3 days after the symptoms disappear. In the case of infections caused by β-hemolytic streptococcus, complete eradication of the pathogen requires therapy for at least 10 days.

Parenteral therapy is indicated when oral inability is impossible and in the treatment of severe infections.

Adult dosages (including elderly patients):

Standard dose:

The usual dose ranges from 750 mg to 3 g of amoxicillin per day in divided doses.In some cases, it is recommended to limit the dose of 1500 mg per day in several doses.

Short course of therapy:

Uncomplicated urinary tract infections: double administration of the drug in 3 g for each injection with an interval between doses of 10 to 12 hours.

Children's dosages (up to 12 years)

The daily dose for children is 25–50 mg / kg / day in several doses (maximum 60 mg / kg / day) depending on the indication and the severity of the disease.

Children weighing more than 40 kg should receive an adult dosage.

Dosing for renal failure:

In patients with severe renal insufficiency, the dose should be reduced. With renal clearance of less than 30 ml / min, an increase in the interval between doses or a decrease in subsequent doses is recommended. In case of renal insufficiency, short courses of therapy are contraindicated. 3

Adults (including elderly patients):