Amoxicillin

General characteristics. Structure:

Active ingredient: 0,25 g or 0,5 g of amoxicillin of trihydrate (in terms of amoxicillin).

Excipients: potato starch, talc, twin-80 (polysorbate-80) magnesium stearate.

Antibacterial bactericidal acid resisting broad-spectrum agent from group of semi-synthetic penicillin.

Pharmacological properties:

Pharmacodynamics. Inhibits transpeptidase, breaks synthesis of a peptidoglikan (basic protein of a cell wall) during division and growth, causes a lysis of bacteria. Thanks to action spectrum width, drug is active in the relation of 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.

Besides, amoxicillin is active concerning all microorganisms sensitive to penicillin G, for example, streptococci of the group A,B,C,G,H,I,M, Streptococcus pneumoniae, staphylococcus and Neisseria spp., not producing penicillinases, Erysipelothrix rhysiopathiae, Corynebacterium, Bacillus anthracis, Actinomycetes, Streptobacilli, Spirillium minus, Pastereulla multocida, Listeria, Spirochaeta (Leptospira, Treponema, Borrelia) and others, and also various anaerobic microorganisms (including peptokokk, peptostreptokokk, clostridiums and fuzobakteriya).

Pharmacokinetics. Absorption - bystry, high (93%), meal does not exert impact on absorption, does not collapse in acid medium of a stomach. At intake in a dose of 125 and 250 mg, the maximum concentration - 1.5-3 mkg/ml and 3.5-5 mkg/ml, respectively. Action develops in 15-30 min. after use and lasts 8 h. Time of achievement of the maximum concentration after oral administration - 1-2 h.

Has the large volume of distribution - high concentration are found in plasma, a phlegm, a bronchial secret (in a purulent bronchial secret distribution weak), pleural and peritoneal liquid, urine, contents of skin blisters, lung tissue, a mucous membrane of intestines, female generative organs, a prostate, liquid of a middle ear, a bone, fatty tissue, a gall bladder (at normal function of a liver), fruit fabrics. At increase in a dose twice concentration also increases twice.

Concentration in bile exceeds concentration in plasma by 2-4 times. In amniotic liquid and vessels of an umbilical cord concentration of amoxicillin - 25-30% of level in plasma of the pregnant woman. Badly gets through a blood-brain barrier, at an inflammation of a meninx (meningitis) concentration in cerebrospinal fluid - about 20%. Communication with proteins of plasma - 17%. It is partially metabolized with formation of inactive metabolites. An elimination half-life - 1-1.5 h.

It is brought to 50-70% by kidneys in not changed look by canalicular excretion (80%) and glomerular filtering (20%), to cookies - 10-20%. In a small amount it is allocated with breast milk. At a renal failure (the clearance of creatinine less or is equal to 15 ml/min.) the elimination half-life, increases to 8.5 h. Amoxicillin is removed at a hemodialysis.

Indications to use:

The bacterial infections caused by microorganisms, sensitive to amoxicillin: respiratory infection and ENT organs (sinusitis, pharyngitis, tonsillitis, acute average otitis; bronchitis, pneumonia), urinogenital system (pyelonephritis, a pyelitis, cystitis, an urethritis, gonorrhea, an endometritis, a cervicitis), digestive tract (peritonitis, a coloenteritis, a typhoid, a cholangitis, cholecystitis), infections of skin and soft tissues (the ugly face, impetigo for the second time infected a dermatosis), leptospirosis, acute and latent listeriosis, a disease Laima (borreliosis), dysentery, salmonellosis, a salmonellonositelstvo, bacterial meningitis (depending on results of definition of sensitivity. Especially at children), an infectious endocarditis, for example, enterokokkovy (separately or in a combination with aminoglycosides), the septicaemia caused by the microorganisms sensitive to amoxicillin.

Route of administration and doses:

Inside, to or after meal. To adults and children 10 years are more senior (with body weight more than 40 kg) appoint 0.5 g 3 times a day; at the heavy course of an infection - 0.75-1 g 3 times a day.

At acute uncomplicated gonorrhea appoint 3 g once; at treatment of women repeated reception of the specified dose is recommended. At digestive tract acute infectious diseases (paratyphus, a typhoid) and bilious ways, at gynecologic infectious diseases adult - 1.5-2 g 3 times a day or on 1-1.5 g 4 times a day.

At heavy infections (meningitis, a septicaemia) the adult – to 6 g a day in 3-4 receptions. To children – 250-500 mg 3 times a day. Duration of treatment depends on indications and a clinical picture and makes usually 5-7 days.

At otitis and similar to it infections at children two times reception of Amoxicillin is sufficient. In cases of chronic diseases, recurrent infections, infections of a heavy current of the adult appoint 750 mg - 1 g 3 times a day, to children to 60 mg/kg the day divided into 3 receptions.

At a hay fever adult - 0.5-0.75 g 4 times a day within 6-12 days.

At listeriosis adult – 0.5 g 3 times a day within 6-12 days. At a salmonellonositelstvo adult - 1.5-2 g 3 times a day during 2-4 weeks.

For prevention of an endocarditis at small surgical interventions adult - 3-4 g for 1 h before holding a procedure. If necessary appoint a repeated dose in 8-9 h. At children the dose is reduced twice.

At patients with a renal failure at clearance of creatinine of 15-40 ml/min. the interval between receptions is increased to 12 h; at clearance of creatinine lower than 10 ml/min. reduce a dose by 15-50%; at an anury - the maximum dose of 2 g/days.

Features of use:

At course treatment it is necessary to carry out control of a condition of function of bodies of a hemopoiesis, a liver and kidneys. Development of superinfection due to growth of microflora, insensitive to it, is possible that demands corresponding change of antibacterial therapy. At treatment of patients with bacteremia development of reaction of a bacteriolysis (Yarisha-Gerksgeymer's reaction) is possible.

At the patients having hypersensitivity to penicillin cross allergic reactions with tsefalosporinovy antibiotics are possible.

At treatment of slight diarrhea against the background of course treatment it is necessary to avoid the antidiarrheal drugs reducing an intestines peristaltics; it is possible to use a kaolin or attapulgitsoderzhashchy antidiarrheal means. At heavy diarrhea it is necessary to see a doctor. Treatment surely continues 48-72 more h after disappearance of clinical signs of a disease.

At simultaneous use of estrogensoderzhashchy oral contraceptives and amoxicillin, follows whenever possible other or additional methods of contraception. 

Features of influence of medicine on ability to manage the vehicle and other mechanisms. Data on negative influence of drug in the recommended doses on ability to driving or work with mechanisms are absent.

Use at pregnancy and during breastfeeding. Use of amoxicillin at pregnancy in that case when the advantage for mother exceeds potential risk for a fruit is possible. Amoxicillin is emitted with breast milk in low concentration. In need of use of drug in the period of a lactation it is necessary to resolve an issue of the breastfeeding termination.

Side effects:

Allergic reactions: skin rash, hyperemia, itch, small tortoiseshell, erythema, Quincke's disease, rhinitis, conjunctivitis; fever, joint pains, an eosinophilia, exfoliative dermatitis, a poliformny exudative erythema, Stephens's syndrome - Johnson; reactions similar to a serum disease, toxic epidermal necrolysis, generalized exanthematous пустуллез, allergic vasculitis, acute anaphylaxis.

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

From a nervous system: excitement, uneasiness, sleeplessness, ataxy, confusion of consciousness, change of behavior, depression, peripheral neuropathy, headache, dizziness, spasms.

Laboratory indicators: leukopenia, neutropenia, Werlhof's disease, anemia.

Others: the complicated breath, tachycardia, intersticial nephrite, a crystalluria, an eosinophilia, an agranulocytosis, vagina candidiasis, superinfection (especially at patients with chronic diseases or the lowered resistance of an organism).

Interaction with other medicines:

Antacids, glycosamine, purgatives, food, aminoglycosides - slow down and reduce absorption; ascorbic acid increases absorption.

Bactericidal antibiotics (including aminoglycosides, cephalosporins, Cycloserinum, Vancomycinum, rifampicin) - sinergidny action; bacteriostatic drugs (macroleads, chloramphenicol, linkozamida, tetracyclines, streptocides) - antagonistic.

Increases efficiency of indirect anticoagulants (suppressing intestinal microflora, reduces synthesis of vitamin K and a prothrombin ratio); reduces efficiency of estrogensoderzhashchy oral contraceptives, medicines in the course of which metabolism paraaminobenzoic acid, ethinylestradiol – risk of development of bleedings of "break" is formed.

Diuretics, Allopyrinolum, оксифенбутазон, phenylbutazone,  non-steroidal anti-inflammatory drugs;  the drugs blocking  canalicular  secretion  - reducing canalicular secretion, increase concentration.

Allopyrinolum increases risk of development of skin rash.

Reduces clearance and increases toxicity of a methotrexate. Strengthens digoxin absorption.

Contraindications:

Hypersensitivity to drug components (including to other penicillin, cephalosporins, karbapenema), allergic diseases (including in the anamnesis), bronchial asthma, a pollinosis, an infectious mononucleosis, a lymphoid leukosis, a liver failure, the colitis connected using antibiotics including in the anamnesis, the lactation period, children's age up to 10 years with body weight less than 40 kg.

With care: pregnancy, allergic reactions (including in the anamnesis), digestive tract diseases in the anamnesis, a renal failure, and also at instructions in the anamnesis on bleedings.

Overdose:

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

Treatment: a gastric lavage, absorbent carbon, salt laxatives, drugs for maintenance of water and electrolytic balance; hemodialysis.

Storage conditions:

In the dry, protected from light place at a temperature not above 25 °C. In the place, unavailable to children. Period of validity 2 years. Not to use after the expiry date specified on packaging

Issue conditions:

According to the recipe

Packaging:

Tablets on 250 mg, 500 mg. On 10 tablets in a blister strip packaging. 2 planimetric packagings together with the application instruction place in a pack from a cardboard.