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Pharmacological properties

amoxil dt is a broad-spectrum antibiotic of the group of semisynthetic penicillins. acts bactericidal.

The following table illustrates the in vitro sensitivity of amoxicillin to some clinically relevant microorganisms.

Activity in vitro The average minimum inhibitory concentration (MIC)
0.01–0.1 μg / ml 0.1–1 mcg / ml 1-10 mcg / ml
Gram-positive microorganisms Streptococci (B)

Streptococci

S. pneumonie,

C. welchii

C. tetani

S. aureus

(negative for ß-lactamase)

B. anthracis

L. subtilis

L. monocytogenes

S. faecalis
Gram-negative microorganisms N. gonorrhoeae

N. meningitidis

H. influenzae

B. pertussis

E. coli

P. mirabilis

S. typhi

S. sonnei

V. cholerae

Amoxicillin is inactive against microorganisms producing β-lactamase, for example, such as Pseudomonas and Enterobacter strains. The level of resistance of amoxicillin-sensitive microorganisms can be variable in different territories.

Pharmacokinetics

Suction. After oral administration of the drug, amoxicillin is rapidly and almost completely absorbed (85–90%), the drug is acid-resistant. Eating practically does not affect the absorption of the drug. Cmax the active substance in the blood plasma is reached in 1-2 hours. After oral administration of 375 mg of amoxicillin Cmax the active substance in blood plasma is 6 μg / L. When doubling (or reducing by 2 times) the dose of the drug Cmax in blood plasma also varies (increases or decreases) by 2 times.

Distribution. About 20% of amoxicillin binds to plasma proteins. Amoxicillin penetrates the mucous membranes, bone tissue, intraocular fluid, sputum in therapeutically effective concentrations. The concentration of amoxicillin in bile exceeds its concentration in the blood by 2–4 times. In amniotic fluid and umbilical vessels, the concentration of amoxicillin is 25-30% of its level in the blood plasma of a pregnant woman. Amoxicillin diffuses poorly in the CSF, however, with inflammation of the meninges (for example, with meningitis), the concentration in the CSF is about 20% of the concentration in the blood plasma.

Metabolism. Amoxicillin is partially metabolized, most of its metabolites are inactive against microorganisms.

Amoxicillin is eliminated mainly by the kidneys, about 80% - by tubular excretion, 20% - by glomerular extraction. About 90% of amoxicillin eliminates after 8 hours, 60–70% is excreted unchanged by the kidneys. In the absence of impaired renal function T½ amoxicillin is 1–1.5 hours. In premature, newborns and infants under the age of 6 months T½ amoxicillin is 3-4 hours.

In case of impaired renal function (creatinine clearance ≤15 ml / min) T½ amoxicillin increases and reaches 8.5 hours with anuria

T½ amoxicillin does not change with impaired liver function.

Indications

Infections caused by drug-sensitive microorganisms:

  • respiratory organs

Tags: Amoxicillin