Amoxicillin pills 500mg №20

Composition

Active substance: Amoxicillin trihydrate (in terms of amoxicillin) - 0.25 g or 0.5 g

Excipients: potato starch, talc, tween-80 (polysorbate-80) Magnesium stearate

Tablets of white or almost white color, flat-cylindrical, with a facet and risky

Pharmacological properties

Pharmacodynamics

Antibacterial, bactericidal, acid-resistant, broad-spectrum agent from the group of semi-synthetic penicillins. Inhibits transpeptidase, violates the synthesis of peptidoglycan (cell wall supporting protein) during the period of division and growth, causes lysis of bacteria. Due to the latitude of the spectrum of action, the drug is active against both gram-positive and gram-negative microorganisms. Clinically significant Gram-negative microorganisms sensitive to amoxicillin include Escherichia coli, Proteus mirabilis, Salmonella, Shigella, Campilobacter, Haemophilus influenzae, Bordetella pertussis, Leptospira, Chlamydia.

In addition, amoxicillin is active against all microorganisms sensitive to penicillin G, for example, streptococci of group A, B, C, G, H, I, M, Streptococcus pneumoniae,staphylococci and Neisseria stif. peptococci, peptostreptokokki, clostridia and fuzobakterii).

Pharmacokinetics

Absorption - fast, high (93%), food intake does not affect absorption, does not collapse in the acidic environment of the stomach. When taken orally at a dose of 125 and 250 mg, the maximum concentration is 1.5-3 mcg / ml and 3.5-5 mcg / ml, respectively. The action develops in 15-30 minutes after application and lasts 8 hours. The time to reach the maximum concentration after oral administration is 1-2 hours. It has a large amount of distribution - high concentrations are found in plasma, sputum, bronchial secretion (in a purulent bronchial secretion is weak), pleural and peritoneal fluid, urine, contents of skin blisters, lung tissue, intestinal mucosa, female genitals, prostate gland, middle ear fluid, bone, adipose tissue, gall bladder ( liver function), fetal tissue. With an increase in dose of 2 times the concentration also increases by 2 times. Concentration in bile exceeds concentration in plasma 2-4 times. In the amniotic fluid and umbilical cord vessels, amoxicillin concentration is 25-30% of the plasma level of a pregnant woman. Poor penetrates the blood-brain barrier, with inflammation of the meninges (meningitis) concentration in the cerebrospinal fluid - about 20%. Communication with plasma proteins - 17%.

Partially metabolized to form inactive metabolites. The elimination half-life is 1-1.5 hours. Excreted at 50-70% by the kidneys unchanged by tubular excretion (80%) and glomerular filtration (20%), by the liver - 10-20%. In small quantities excreted in breast milk. In case of kidney dysfunction (creatinine clearance less than or equal to 15 ml / min), the half-life increases to 8.5 hours. Amoxicillin is removed during hemodialysis. 

Indications and usage

Bacterial infections caused by microorganisms sensitive to amoxicillin: infections of the respiratory tract and ENT organs (sinusitis, pharyngitis, tonsillitis, acute otitis media, bronchitis, pneumonia), urinary system (pyelonephritis, pyelitis, cystitis, urethritis, gonorrhea, endometritis, cervicitis, endometritis, cervitis). gastrointestinal tract (peritonitis, enterocolitis, typhoid fever, cholangitis, cholecystitis), infections of the skin and soft tissues (erysipelas, impetigo, secondarily infected dermatosis), leptospirosis, acute and latent listeriosis, Lyme disease (Borreliosis), dysentery, salm nellez, salmonellonositelstvo, bacterial meningitis (depending on the sensitivity of the determination results. Especially in children), infectious endocarditis, e.g., enterococcal (alone or in combination with aminoglycosides), septicemia caused by microorganisms sensitive to amoxicillin.

Contraindications

Hypersensitivity to the drug components (including to other penicillins, cephalosporins,carbapenems), allergic diseases (including history), bronchial asthma, pollinosis, infectious mononucleosis, lymphocytic leukemia, liver failure, colitis associated with the use of antibiotics, including a history of lactation, children up to 10 years of age with body weight less than 40 kg.

Pregnancy, allergic reactions (including a history), a history of gastrointestinal diseases, renal failure, as well as indications of a history of bleeding.

Pregnancy and Breastfeeding

Perhaps the use of amoxicillin in pregnancy in the case when the benefit to the mother outweighs the potential risk to the fetus.

Amoxicillin is excreted in breast milk in low concentrations. If necessary, the use of the drug during lactation should decide on the termination of breastfeeding.

Dosage and Administration

The drug should be taken orally, before or after meals.

Adults and children over 10 years old (weighing more than 40 kg) are prescribed 0.5 g 3 times a day; with severe infection - 0.75-1 g 3 times a day.

In acute uncomplicated gonorrhea, 3 g is administered once; When treating women, it is recommended to re-take the indicated dose.

With acute infectious diseases of the gastrointestinal tract (paratyphoid fever, typhoid fever) and biliary tract, with gynecological infectious diseases for adults - 1.5-2 g 3 times a day or 1-1.5 g 4 times a day.

With severe infections (meningitis, septicemia) adults - up to 6 g per day in 3-4 doses. Children - 250-500 mg 3 times a day. The duration of treatment depends on the indications and the clinical picture and is usually 5-7 days. With otitis and similar infections in children, it may be sufficient to take Amoxicillin twice a day. In cases of chronic diseases, recurrent infections, severe infections, adults are prescribed 750 mg-1 g 3 times a day, children up to 60 mg / kg per day divided into 3 doses.

For adults with leptospirosis, 0.5–0.75 g 4 times a day for 6–12 days.

In adults with listeriosis - 0.5 g 3 times a day for 6-12 days.

When adults are salmonelloson - 1.5-2 g 3 times a day for 2-4 weeks.

For the prevention of endocarditis in small surgical interventions for adults - 3-4 g for 1 hour before the procedure. If necessary, appoint a repeated dose after 8-9 hours.

In children, the dose is halved.

In patients with impaired renal function with creatinine clearance of 15-40 ml / min, the interval between doses increases to 12 hours; with creatinine clearance below 10 ml / min, the dose is reduced by 15-50%; with anuria - the maximum dose of 2 g / day.

Adverse reactions

Allergic reactions: skin rash, hyperemia, itching, urticaria, erythema, angioedema, rhinitis, conjunctivitis; fever, joint pain, eosinophilia, exfoliative dermatitis, polyformal exudative erythema, Stevens-Johnson syndrome; serum-like reactions, toxic epidermal necrolysis, generalized exantomous pustullosis, allergic vasculitis, anaphylactic shock.

On the part of the digestive system: dysbacteriosis, change in taste, vomiting, nausea, diarrhea, stomatitis, glossitis, abnormal liver function, moderate increase in the activity of "liver" transaminases, cholestatic jaundice, hepatic cholestasis, acute cytolytic hepatitis, pseudomembranous colitis.

Nervous system disorders: agitation, anxiety, insomnia, ataxia, confusion, behavior change, depression, peripheral neuropathy, headache, dizziness, convulsions.

Laboratory indicators: leukopenia, neutropenia, thrombocytopenic purpura, anemia.

Other: shortness of breath, tachycardia, interstitial nephritis, crystalluria, eosinophilia, agranulocytosis, vaginal candidiasis, superinfection (especially in patients with chronic diseases or low body resistance).

Overdose

Symptoms: nausea, vomiting, diarrhea, violation of water and electrolyte balance (as a result of vomiting and diarrhea).

Treatment: gastric lavage, Activated carbon, saline laxatives, drugs to maintain water and electrolyte balance; hemodialysis.

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, linkosamides, tetracyclines, sulfonamides) - antagonistic.

Increases the effectiveness of indirect anticoagulants (suppressing the intestinal microflora, reduces the synthesis of vitamin K and the prothrombin index); reduces the effectiveness of estrogen-containing oral contraceptives, drugs, in the process of metabolism of which para-aminobenzoic acid is formed, ethinyl estradiol - the risk of "breakthrough" bleeding.

Diuretics, Allopurinol, oxyphenbutazone, phenylbutazone, nonsteroidal 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 . Strengthens Digoxin absorption.

In the course of treatment, it is necessary to monitor the state of the function of the blood-forming organs, liver and kidneys.

The development of superinfection is possible due to the growth of microflora insensitive to it, which requires a corresponding change in antibacterial therapy.

When treating patients with bacteremia, the bacteriolysis reaction may be possible (the Jarish-Herxheimer reaction).

In patients with hypersensitivity to penicillins, allergic cross-reactions with cephalosporin antibiotics are possible.

In the treatment of mild diarrhea on the background of a course of treatment, antidiarrheal drugs that reduce intestinal motility should be avoided; kaolin or attapulgite-containing antidiarrheals may be used. In severe diarrhea, you should consult 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 given whenever possible.

Features of the influence of the drug on the ability to drive a vehicle and other mechanisms

There are no data on the negative effect of the drug in recommended doses on the ability to drive a car or work with mechanisms.

In a dry, dark place at a temperature not higher than 25 ° C. In the reach of children