Amoxicillin

General characteristics. Structure:

Active agent - trihydrate amoxicillin (in terms of 100% substance) 250.00 mg.

Excipients: cellulose microcrystallic, calcium stearate, 

structure of gelatin capsules, in milligrams the case: gelatin, titanium dioxide (Е 171); lid: gelatin, titanium dioxide (Е 171), methylparahydroxybenzoate, пропилпарагидроксибензоат.

Pharmacological properties:

Pharmacokinetics. Absorption – bystry, high (93%), meal does not exert impact on absorption, does not collapse in acid medium of a stomach. At intake in 250 mg, the maximum concentration of-3,5-5 mkg/ml. 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 gland, a gall bladder (at normal function of a liver). 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 makes 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%. 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.

In a small amount it is allocated with breast milk.

Pharmacodynamics. Amoxicillin - antibacterial bactericidal acid resisting broad-spectrum agent from group of semi-synthetic penicillin. Inhibits transpeptidase, breaks synthesis of a peptidoglikan (basic protein of a cell wall) during division and growth, causes a lysis of bacteria. It is active concerning aerobic gram-positive bacteria: Staphylococcus spp. (except for the strains producing a penicillinase), Streptococcus spp; and aerobic gram-negative bacteria: Neisseria gonorrhoeae, Neisseria meningitidis, Escherichia coli, Shigella spp., Klebsiella spp. The microorganisms producing a penicillinase, rezistentna to effect of amoxicillin. Action develops in 15-30 min. after introduction and lasts 8 h.

Indications to use:

- sinusitis, pharyngitis, tonsillitis, acute average otitis, bronchitis, pneumonia;

- pyelonephritis, pyelitis, cystitis, urethritis;

- gonorrhea;

- endometritis, cervicitis;

- cholangitis, cholecystitis;

- coloenteritis;

- peritonitis (as a part of a combination therapy);

- typhoid;

- the ugly face, impetigo for the second time infected a dermatosis;

- leptospirosis, listeriosis, disease Laima (borreliosis), dysentery, salmonellosis, salmonellonositelstvo;

- meningitis (as a part of a combination therapy);

- sepsis (as a part of a combination therapy);

- prevention of an endocarditis.

Route of administration and doses:

Inside. To adults and children 10 years are more senior (with body weight more than 40 kg) appoint 500 mg 3 times a day; at the heavy course of an infection - 750 mg – 1 g 3 times a day.

To children aged from 6 up to 10 years appoint 250 mg 3 times a day.

Average course of treatment — 5–7 days, at streptococcal infections — not less than 10 days.

For treatment of uncomplicated gonorrhea appoint 3,0g drug once (in a combination with probenetsidy).

Features of use:

With care it is necessary to appoint at a renal failure, bleeding in the anamnesis.

Changes of laboratory indicators: leukopenia, neutropenia, Werlhof's disease, anemia.

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 purpose of 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, it is necessary to use whenever possible other or additional methods of contraception.

At children up to 6 years other dosage forms of drug are applied.

Amoxicillin gets through a placenta, in small amounts is emitted with breast milk.

In need of use of amoxicillin at pregnancy it is necessary to weigh carefully expected advantage of therapy for mother and potential risk for a fruit. With care to apply amoxicillin during breastfeeding.

Considering side effects of drug it is necessary to be careful when driving or potentially dangerous mechanisms.

Side effects:

- small tortoiseshell, dermahemia, erythema, Quincke's disease, rhinitis, conjunctivitis;

- fever, joint pains, an eosinophilia, exfoliative dermatitis, a polymorphic exudative erythema, Stephens's syndrome – Johnson, the reaction similar to a serum disease;

- taste change, vomiting, nausea, diarrhea;

- stomatitis, glossitis;

- abnormal liver function, moderate increase in "hepatic" transaminases;

- dysbacteriosis;

- pseudomembranous coloenteritis;

- excitement, uneasiness, sleeplessness, ataxy, confusion of consciousness, change of behavior, depression, peripheral neuropathy;

- headache, dizziness, convulsive reactions;

- the complicated breath, tachycardia, intersticial nephrite, vagina candidiasis, superinfection (especially at patients with chronic diseases or the lowered resistance of an organism).

In isolated cases:

- acute anaphylaxis.

Interaction with other medicines:

Amoxicillin reduces effect of estrogensoderzhashchy peroral contraceptive drugs, reduces clearance and increases toxicity of a methotrexate. Amoxicillin strengthens digoxin absorption. Excretion is slowed down probenetsidy, Sulfinpyrazonum, acetylsalicylic acid, indometacin, oksifenbutazony, by phenylbutazone, etc. the drugs suppressing tubular secretion.

Antibacterial activity of amoxicillin decreases bacteriostatic chemotherapeutic means and antacids, increases — aminoglycosides and metronidazole.

Contraindications:

- hypersensitivity (including to other penicillin, cephalosporins, karbapenema);

- allergic diathesis;

- bronchial asthma;

- pollinosis;

- infectious mononucleosis;

- lymphoid leukosis;

- liver failure;

- digestive tract diseases in the anamnesis (especially the colitis connected using antibiotics).

Overdose:

Symptoms: nausea, vomiting, diarrhea, disturbance of water and electrolytic balance.

Treatment: to wash out a stomach, absorbent carbon, salt laxatives, drugs for maintenance of introduction and electrolytic balance, a hemodialysis.

Storage conditions:

To store in the dry, protected from light place, at a temperature not above 30 °C. To store in the place, unavailable to children!

Issue conditions:

According to the recipe

Packaging:

On 10 capsules in a blister strip packaging from a film of polyvinyl chloride and aluminum foil.

Planimetric packagings place in boxes from a cardboard. Put the approved instructions on a medical use in each box in the state and Russian languages.