Amoxicillin - instructions for use, dose, side effects, contraindications

Antibacterial bactericidal acid-fast spectrum of action from the group of semisynthetic penicillins. Inhibits transpeptidase, disrupts the synthesis of peptidoglycan (supporting cell protein walls) during the period of division and growth, causes bacterial lysis. Clinically significant gram-negative microorganisms sensitive to amoxicillin include Escherichia coli, Proteus mirabilis, Salmonella, Shigella, Campilobacter, Haemophilus influenzae, Leptospira, Chlamydia (in vitro), Neisseria gonorrhoeae, Neisseria meningitidis, Klebsiella spp.

It is active against aerobic Gram-positive microorganisms: Staphylococcus spp. (with the exception of strains producing penicillinase), Streptococcus spp. including Streprococcus faecalis, Streprococcus pneumoniae.

Amoxicillin is also active against Helicobacter pylori.

Does not affect indole-positive strains of proteas (P.vulgaris, R. Rettgeri); Serratia spp., Enterobacter spp, Morganella morganii, Pseudomonas spp). ' Rickettsia, mycoplasmas, and viruses are resistant to its action. The microorganisms producing penicillinase are resistant to the action of amoxicillin. The action develops 15-30 minutes after administration and lasts 8 hours.

Pharmacokinetics:

Absorption - fast, high (93%), food intake does not affect absorption, does not break down in the acidic environment of the stomach. After 1-2 hours after oral administration of a dose of 250 mg, a maximum plasma concentration of 3.5-5 μg / ml is achieved. The connection with plasma proteins is 17%. Passes histohematological barriers, except for unchanged blood-brain; has a large volume of distribution - 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 exudate of the middle ear in inflammation, bone and fatty tissues, gall bladder (with normal liver function), fetal tissues. With increasing dose, the concentration in organs and tissues increases proportionally.Concentration in the bile is 2-4 times higher than the concentration in the blood plasma. AT amniotic fluid and umbilical cord blood concentration of amoxicillin is 25-30% of the level in the plasma of a pregnant woman. Poor penetration of the blood-brain barrier, with inflammation of the meninges (meningitis), the concentration of amoxicillin in the cerebrospinal fluid is about 20% of the level in the blood plasma.

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

Indications:

Infectious-inflammatory diseases caused by microorganisms sensitive to Amoxicillin:

- infections of the upper respiratory tract and ENT organs (sinusitis, pharyngitis, tonsillitis, acute otitis media);

- Infections of the lower respiratory tract (acute and chronic bronchitis, pneumonia);

- infection of the genitourinary system (acute and chronic pyelonephritis, pyelitis, cystitis, urethritis, gonorrhea); gynecological infections (endometritis, cervicitis);

- infections of the gastrointestinal tract (enterocolitis, typhoid, salmonellosis, carriage of salmonella, shigellosis); gastric ulcer and duodenal ulcer, chronic gastritis associated with Helicobacter pylori in combination therapy;

- biliary tract infections (cholangitis, cholecystitis); infections of the skin and soft tissues (erysipelas, impetigo, secondarily infected dermatoses); leptospirosis; acute and latent listeriosis;

- Lyme disease (borreliosis);

- infective endocarditis, for example, enterococcus.

Contraindications:

Hypersensitivity to amoxicillin and other ingredients (including to other. Penicillins, cephalosporins, carbapenems), atopic dermatitis, bronchial asthma, hay fever, infectious mononucleosis, lymphocytic leukemia, hepatic failure, diseases of the gastrointestinal tract in history (especially colitis, associated with the use of antibiotics), lactation.

Children under 5 years of age and / or body weight less than 40 kg (for this dosage form).

Carefully:

Renal failure, bleeding in the history, allergic reactions (including in the anamnesis).

Pregnancy and lactation:

When pregnancy is possible, if the benefit to the mother exceeds the potential risk for the fetus (adequate and strictly controlled studies in pregnant women are not conducted).

If necessary, the appointment in the lactation period should stop breastfeeding.

Dosing and Administration:

Inside, before or after eating. Adults and children over 10 years of age (with a body weight of more than 40 kg) are prescribed 250 mg 3 times a day; when the infection is severe - 500 mg 3 times a day. Children under 10 years of age are prescribed as a suspension, since at this age the dosage of the drug in capsules is difficult. The interval between each intake of 8 hours should be strictly observed. The maximum daily dose should not exceed 6 g. The course of treatment is 5-12 days. Treatment is recommended to continue for 48-72 hours after the normalization of body temperature or after a reliable destruction of the pathogen.

Infections of the upper respiratory tract and ENT organs (sinusitis, pharyngitis, tonsillitis, acute otitis media): 250 mg every 8 hours.

Infections of the lower respiratory tract (acute and chronic bronchitis, pneumonia): 500 mg every 8 hours.

Acute uncomplicated infections of the genitourinary system: therapy with high doses is recommended: 2 doses of 3 g at intervals of 10-12 hours.

In acute uncomplicated gonorrhea, men are prescribed 3 g once; when treating women, it is recommended to take this dose twice, at intervals of 10-12 hours, in connection with the possible multiple nature of the lesion and the ascending inflammatory process with the transition to pelvic organs.

Gynecological infections without fever: 250 mg every 8 hours.

Gynecological infections accompanied by fever: 1,5-2 g 3 times a day or 1-1,5 g 4 times a day.

Infections of the gastrointestinal tract (enterocolitis, typhoid fever, shigellosis): 1,5 - 2 g 3 times a day or 1-1,5 g 4 times a day.

Salmonellae: 1,5 - 2 g 3 times a day for 2-4 weeks.

Peptic ulcer of stomach and duodenum, chronic gastritis associated with Helicobacter pylori in combination therapy: 1 g 2 times a day.

Infections of the biliary tract (cholangitis, cholecystitis): 1.5-2 g 3 times a day or 1-1.5 g 4 times a day.

Infections of the skin and soft tissues (erysipelas, impetigo, secondarily infected dermatoses): 250 mg every 8 hours.

Leptospirosis: 500 mg - 750 mg 4 times a day for 6-12 days.

Lyme disease (borreliosis): at the I stage of the disease 500 mg 3 times a day. Infective endocarditis, for example, enterococcus: for the prevention of endocarditis with small surgical interventions for adults - 3-4 g for 1 h before the procedure. If necessary, appoint a second dose after 8-9 hours.

Patients with severe impairment of kidney function should reduce the dose or increase the intervals between doses of amoxicillin.

When creatinine clearance is less than 10 ml / min and for patients on peritoneal dialysis the maximum daily dose is 500 mg (250 mg twice a day); with a creatinine clearance of 10-30 ml / min, the maximum daily dose is 1000 mg (500 mg twice a day); when the creatinine clearance is more than 30 ml / min, the dosage regimen should not be adjusted; with anuria - the maximum dose should not exceed 2 g / day.

For children aged 5-10 years, the dose is calculated per kilogram of the child's weight. In children's practice Amoxicillin in the form of capsules is applicable if the daily dose of at least 500 mg with a double intake (250 mg twice a day).

At a body weight of the child less than 20 kg, the daily dose is 25 mg / kg / day,divided into 3 receptions; at a severe course of the disease - 50 mg / kg / day, divided into 3 doses.

At a body weight of the child in the range of 20-40 kg amoxicillin is prescribed in a dose of 40-90 mg / kg / day in 3 divided doses at low doses and in 2 doses at high doses.

Children with a body weight above 40 kg of the drug is prescribed, based on the dosing regimen for adults. Tonsillitis: 50 mg / kg / day in 3 divided doses.

Acute otitis media: with severe course and relapses, an alternative therapy regimen can be applied 750 mg twice a day for 2 days.

Prophylaxis of endocarditis: 1.5 g for 1 hour before surgery once. In surgical interventions performed under general anesthesia, -1.5 g for 4 hours before surgery once. If necessary, re-reception after 6 hours.

Children with impaired renal function with creatinine clearance less than 10 ml / min should increase the interval between doses to 24 hours, which corresponds to the reception of 1/3 of the usual dose; with a creatinine clearance in the range of 10-30 ml / min, the interval between doses is increased to 12 hours, which corresponds to the reception of 2/3 of the usual dose; when the creatinine clearance is more than 30 ml / min, the dosage regimen is not required.

If you miss a dose, you should as soon as possible to take a capsule, without waiting for the next meal, and then observe regular intervals between doses.

Side effects:

Allergic reactions: Urticaria, skin redness, erythema, angioedema, rhinitis, conjunctivitis, fever, joint pain, eosinophilia, exfoliative dermatitis, erythema poliformnaya, Stevens-Johnson syndrome, reactions similar to serum sickness, anaphylactic shock.

From the digestive system: Goiter, change in taste, nausea, vomiting, diarrhea, stomatitis, glossitis, hepatic dysfunction, a moderate increase in activity of "liver" transaminases, pseudomembranous colitis, itching in the anal area.

From the nervous system: agitation or psychomotor agitation, anxiety, insomnia, ataxia, confusion; changes in behavior, depression, peripheral neuropathy, headache, dizziness, convulsions, aseptic meningitis.

From the urinary system: crystalluria and acute interstitial nephritis.

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

Other: shortness of breath, tachycardia, candidiasis of the oral and vaginal mucosa, superinfection (especially in patients with chronic diseases or reduced resistance of the body). Brown, yellow or gray teeth, especially in children.

Overdose:

Symptoms of an overdose: nausea, vomiting, diarrhea, violation of water-electrolyte balance (as a consequence of vomiting and diarrhea).

Measures to help with overdose: gastric lavage, activated charcoal, salt laxatives, preparations to maintain the water-electrolyte balance; hemodialysis.

Interaction:

Antacids, glucosamine, laxatives, aminoglycosides, food - slow down and reduce absorption; ascorbic acid increases absorption. Bactericidal antibiotics (including aminoglycosides, cephalosporins, vancomycin, rifampicin) - synergistic effect; bacteriostatic drugs (macrolides, chloramphenicol, lincosamides, tetracyclines, sulfonamides) - antagonistic.

When treating the drug Amoxicillin In combination with metronidazole, nausea, vomiting, anorexia, diarrhea, constipation, epigastric pain, digestive disorders, rarely jaundice, interstitial nephritis, hematopoietic disorders are observed.

Amoxicillin 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 of which forms para-aminobenzoic acid and ethinyl estradiol, contributing to the risk of bleeding "breakthrough".

Diuretics, allopurinol, oxyphenbutazone, phenylbutazone, non-steroidal anti-inflammatory drugs, drugs that block tubular secretion - reducing tubular secretion, increase the concentration of amoxicillin in the blood.

Simultaneous use of amoxicillin and allopurinol increases the risk of skin rash.

Amoxicillin reduces clearance and increases the toxicity of methotrexate. Increases the absorption of digoxin.

Special instructions:

In course treatment it is necessary to monitor the status of the functions of the organs of hematopoiesis, liver and kidneys.

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

In the treatment of patients with bacteremia, the development of a bacteriolysis reaction (the Yarisch-Gerxheimer reaction) is possible.

In patients who are hypersensitive to penicillins, there may be cross-allergic reactions with cephalosporin antibiotics.

In the treatment of mild diarrhea against the background of course treatment, antidiarrheal drugs should be avoided, which reduce intestinal peristalsis; it is possible to use kaolin- or attapulgite-containing agents. If severe diarrhea is necessary, 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 used whenever possible.

In case of allergic reactions, it is necessary to cancel the drug and prescribe the usual treatment with norepinephrine, antihistamines and glucocorticosteroids.With the advent of maculopapular rash, treatment can be continued only in the case of life-threatening conditions under the strict supervision of a physician.

When carrying out therapy, adequate fluid intake and maintaining sufficient diuresis are extremely important. Patients with cholangitis or cholecystitis antibiotics can be prescribed only with mild degrees of disease and in the absence of cholestasis.

With persistent severe diarrhea, pseudomembranous colitis due to antibiotics, which may pose a threat, for the life of the patient (watery feces with an admixture of blood and mucus, blunt or colonic pain in the abdomen, fever, sometimes, tenesmus) should be suspected. In such cases Amoxicillin it is necessary to immediately cancel and prescribe a specific treatment for the causative agent, for example, Edicyin (vancomycin). Means that reduce peristalsis of the gastrointestinal tract are contraindicated.

Before starting treatment for gonorrhea in patients with suspected primary syphilitic lesions, it is necessary to conduct a study in a dark field. All other patients with suspected concomitant syphilis should be serologically testeddynamics for at least 4 months.

Effect on the ability to drive transp. cf. and fur:

When using Amoxicillin, caution should be exercised when driving vehicles and engaging in other potentially hazardous activities requiring increased concentration of attention and speed of psychomotor reactions, the drug may cause dizziness and other side effects that may affect these abilities.

Form release / dosage:

Capsules of 250 mg.

Packaging:

10 capsules per contour cell packaging made of polyvinylchloride film and aluminum foil.

For 1 or 2 contour mesh packages along with the instruction for use are placed in a pack of cardboard.

Storage conditions:

In a dry, protected from light place at a temperature of no higher than 25 ° C.

Keep out of the reach of children.

Shelf life:

2 years. Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LS-000409

Date of registration:25.06.2010 / 27.09.2012

Expiration Date:Unlimited

The owner of the registration certificate:AVVA RUS, OJSC AVVA RUS, OJSC Russia

Manufacturer: & nbsp

AVVA RUS, OJSC Russia

Information update date: & nbsp19.08.2017

Illustrated instructions

Instructions

Amoxicillin (Amoxicillin)