Composition, form of production and packaging
Tablets are white or almost white in color, capsular, with a risk.
1 tab.
amoxicillin (in the form of trihydrate) 250 mg
Auxiliary substances: lactulose - 300 mg, povidone low molecular weight - 5 mg, crospovidone (collidon CL-M) - 25 mg, croscarmellose sodium 35 mg, talcum - 14 mg, magnesium stearate 7 mg, potato starch - up to 700 mg.
5 pieces. - packings cellular planimetric (2) - packs cardboard.
5 pieces. - packings cellular planimetric (4) - packs cardboard.
10 pieces. - packings of cellular contour (1) - packs cardboard.
10 pieces. - packings cellular planimetric (2) - packs cardboard.
20 pcs. - plastic bottles (1) - packs of cardboard.
20 pcs. - polymer cans (1) - packs of cardboard.
Tablets are white or almost white in color, capsular, with a risk.
1 tab.
amoxicillin (in the form of trihydrate) 500 mg
Auxiliary substances: lactulose - 600 mg, povidone low molecular weight - 10 mg, crospovidone (collidon CL-M) - 50 mg, croscarmellose sodium - 70 mg, talc - 28 mg, magnesium stearate - 14 mg, potato starch - up to 1400 mg.
5 pieces. - packings cellular planimetric (2) - packs cardboard.
5 pieces. - packings cellular planimetric (4) - packs cardboard.
10 pieces. - packings of cellular contour (1) - packs cardboard.
10 pieces. - packings cellular planimetric (2) - packs cardboard.
20 pcs. - plastic bottles (1) - packs of cardboard.
20 pcs. - polymer cans (1) - packs of cardboard.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2016.
PHARMACHOLOGIC EFFECT
Antibacterial bactericidal acid-fast preparation of a wide spectrum of action 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 microorganisms : Staphylococcus spp. (with the exception of strains producing penicillinase), Streptococcus spp; and aerobic Gram-negative bacteria : Neisseria gonorrhoeae, Neisseria meningitidis, Escherichia coli, Shigella spp., Salmonella spp., Klebsiella spp. The microorganisms producing penicillinase are resistant to the action of amoxicillin.
PHARMACOKINETICS
Suction
Absorption - fast, high (93%), food intake does not affect absorption; Amoxicillin does not degrade in the acidic environment of the stomach. When administered orally in the form of a suspension (or tablets) at a dose of 125 and 250 mg C max is 1.5-3 Ојg / ml and 3.5-5 Ојg / ml, respectively. The time to reach C max after oral administration is 1-2 hours. When the dose is doubled, the concentration also doubles.
Distribution
Has a large V d - high concentrations are found in plasma, sputum, bronchial secretion (in the purulent bronchial secretion the distribution is weak), pleural and peritoneal fluid, urine, skin blisters, lung tissue, intestinal mucosa, female genital organs, prostate gland, fluid middle ear, bone, adipose tissue, gall bladder (with normal liver function), fetal tissues. 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 concentration, determined in the plasma of a pregnant woman. In small amounts excreted in breast milk. Poor penetration through the BBB, with inflammation of the meninges (meningitis), the concentration in the cerebrospinal fluid is about 20% of the concentration in the plasma. Binding to plasma proteins - 17%.
Metabolism
Partially metabolized with the formation of inactive metabolites.
Excretion
The 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%), by the liver - by 10-20%.
Pharmacokinetics in special clinical cases
If the renal function is impaired (CC is less than or equal to 15 ml / min), T 1/2 increases to 8.5 hours. Amoxicillin is removed during hemodialysis.
INDICATIONS
Bacterial infections caused by sensitive microflora:
- respiratory tract infections and ENT organs (sinusitis, pharyngitis, tonsillitis, acute otitis media, bronchitis, pneumonia);
- infections of the genitourinary system (pyelonephritis, pyelitis, cystitis, urethritis, gonorrhea, endometritis, cervicitis);
- Gastrointestinal infections (enterocolitis, typhoid fever, cholangitis, cholecystitis);
- infections of the skin and soft tissues (erysipelas, impetigo, secondarily infected dermatoses);
- Leptospirosis;
- listeriosis;
- Lyme disease (borreliosis);
- dysentery;
- salmonellosis, salmonella;
endocarditis (prophylaxis).
DOSING MODE
The drug is taken orally, before or after a meal.
Adults and children over 10 years of age (with a body weight of more than 40 kg) are prescribed 0.5 g 3 times / day; in severe infection - 0.75-1.0 g 3 times / day.
Children aged 5-10 years are prescribed 0.25 g 3 times / day; children aged 3-5 years - 0.125 g 3 times / day; at a severe course of infection - 60 mg / kg / day in 3 doses (maximum daily dose).
The course of treatment is 5-12 days.
In acute uncomplicated gonorrhea appoint 3 g once; in the treatment of women, repeated intake of this dose is recommended.
In acute infectious diseases of the digestive tract (paratyphoid, typhoid) and biliary tract , with gynecological infectious diseases adults are prescribed 1.5-2 g 3 times / day or 1-1.5 g 4 times / day.
With leptospirosis, adults are prescribed 0.5-0.75 g 4 times / day for 6-12 days.
With salmonella, adults are prescribed 1.5-2 g 3 times / day for 2-4 weeks.
To prevent endocarditis with small surgical interventions, adults are prescribed 3-4 g for 1 h 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 QC 15-40 ml / min, the interval between doses is increased to 12 h; at CC below 10 ml / min the dose is reduced by 15-50%; with anuria the maximum dose is 2 g / day.
SIDE EFFECT
Allergic reactions: hives are possible, skin hyperemia, erythema, angioedema, rhinitis, conjunctivitis; rarely - fever, joint pain, eosinophilia, exfoliative dermatitis, erythema multiforme exudative, Stevens-Johnson syndrome, reactions similar to serum sickness; in isolated cases - anaphylactic shock.
On the part of the digestive system: dysbacteriosis, taste change, vomiting, nausea, diarrhea, stomatitis, glossitis, impaired liver function, moderate increase in hepatic transaminase activity, pseudomembranous enterocolitis.
From the nervous system: agitation, anxiety, insomnia, ataxia, confusion, behavior change, depression, peripheral neuropathy, headache, dizziness, convulsive reactions.
From 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).
CONTRAINDICATIONS
- hypersensitivity (including to other penicillins, cephalosporins, carbapenems);
- Children's age under 3 years (for this dosage form).
With caution should prescribe the drug for allergic diseases (including history), gastrointestinal diseases in history (especially colitis associated with the use of antibiotics), kidney failure, severe violations of liver function, pregnancy, lactation, infectious mononucleosis, lymphocytic leukemia .
PREGNANCY AND LACTATION
The use of the drug during pregnancy is possible only if the intended benefit for the mother exceeds the potential risk to the fetus.
If it is necessary to prescribe the drug during lactation, breastfeeding should be stopped.
APPLICATION FOR FUNCTIONS OF THE LIVER
The drug with caution is prescribed to patients with renal insufficiency.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
The drug with caution is prescribed for severe violations of the liver.
APPLICATION FOR CHILDREN
Contraindicated in the use of this dosage form in childhood up to 3 years.
SPECIAL INSTRUCTIONS
At 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 resistant to amoxicillin, which requires an appropriate change in antibacterial therapy.
In the treatment of patients with bacteremia, the development of an endotoxic shock reaction (the Yarisch-Gerxheimer reaction) is possible.
In patients who have increased sensitivity to penicillins, there may be cross-allergic reactions to antibiotics of the cephalosporin group.
In the treatment of mild diarrhea against the background of course treatment should avoid antidiarrhoeal drugs that reduce peristalsis of the intestine. With severe diarrhea, a specialist consultation is necessary. Be sure to continue treatment 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.
OVERDOSE
Symptoms: nausea, vomiting, diarrhea, disturbance of water-electrolyte balance (as a consequence of vomiting and diarrhea).
Treatment: gastric lavage, the appointment of activated charcoal, saline laxatives, correction of water-electrolyte balance; hemodialysis.
DRUG INTERACTION
Antacids, glucosamine, laxatives, food, aminoglycosides slow down and decrease absorption; ascorbic acid increases absorption.
Bactericidal antibiotics (including aminoglycosides, cephalosporins, vancomycin, rifampicin) have a synergistic effect; bacteriostatic drugs (macrolides, chloramphenicol, lincosamides, tetracyclines, sulfonamides) - antagonistic.
The drug 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 para-aminobenzoic acid, as well as ethinyl estradiol (risk of development of breakthrough bleeding).
Diuretics, allopurinol, oxyphenbutazone, phenylbutazone, NSAIDs, drugs that block tubular secretion (reducing tubular secretion) increase the concentration of amoxicillin.
With simultaneous application with allopurinol, the risk of developing skin rashes increases.
Amoxicillin reduces clearance and increases the toxicity of methotrexate; increases absorption of digoxin.
TERMS OF RELEASE FROM PHARMACY
The drug is released by prescription.
TERMS AND CONDITIONS OF STORAGE
The drug should be stored in a dry, protected from light, out of reach of children at a temperature of no higher than 25 В° C. Shelf life - 2 years. Do not use the drug after the expiration date.
