Amoxicillin

General characteristics. Structure:

Active agent: amoxicillin (in the form of trihydrate) 250 mg

Excipients: magnesium stearate, cellulose microcrystallic PH 102.

Structure of a cover of the capsule: titanium dioxide (E171), dye quinolinic yellow (E104), dye azoruby (E122), dye blue patent V (E131), dye black brilliant (E151), gelatin.

 
Active agent: amoxicillin (in the form of trihydrate) 500 mg

Excipients: magnesium stearate, cellulose microcrystallic.

Structure of a cover of the capsule: titanium dioxide (E171), dye quinolinic yellow (E104), dye azoruby (E122), dye crimson (Ponso 4R) (E124), dye ferrous oxide yellow (E172), gelatin.

Pharmacological properties:

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., Salmonella spp., Klebsiella spp. The microorganisms producing a penicillinase, rezistentna to effect of amoxicillin.

Pharmacokinetics. Absorption - bystry, high (about 93%), meal does not exert impact on absorption, does not collapse in acid medium of a stomach. At intake in a dose of 125 mg and 250 mg of Cmax in a blood plasma it is reached in 1-2 h and makes 1.5-3 mkg/ml and 3.5-5 mkg/ml, respectively. Has big Vd: in high concentration it is 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 about 17%.

It is partially metabolized with formation of inactive metabolites. T1/2 is 1-1.5 h. It is brought to 50-70% by kidneys in not changed look by canalicular secretion (80%) and glomerular filtering (20%), to cookies - 10-20%. In a small amount it is allocated with breast milk. T1/2 at premature, newborns and children up to 6 months - 3-4 h. At a renal failure (the clearance of creatinine less or is equal to 15 ml/min.) T1/2 increases to 8.5 h. Amoxicillin is removed at a hemodialysis.

Indications to use:

The bacterial infections caused by sensitive microflora:
— respiratory infection and ENT organs (sinusitis, pharyngitis, tonsillitis, acute average otitis; bronchitis, pneumonia);
— infections of urinogenital system (pyelonephritis, pyelitis, cystitis, urethritis, gonorrhea, endometritis, cervicitis);
— GIT infections (peritonitis, coloenteritis, typhoid, cholangitis, cholecystitis);
— infections of skin and soft tissues (the ugly face, impetigo for the second time infected a dermatosis); hay fever;
— listeriosis;
— disease Laima (borreliosis);
— dysentery;
— salmonellosis;
— salmonellonositelstvo;
— meningitis;
— endocarditis (prevention);
— sepsis.

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 500 mg of 3 times/days; at the heavy course of an infection - on 0.75-1 g 3 times/days.

To children appoint in the form of suspension: at the age of 5-10 years - on 250 mg (5 ml of suspension) of 3 times/days; 2-5 years - on 125 mg (2.5 ml of suspension) of 3 times/days; 2 years - 20 mg/kg of body weight the day divided into 3 receptions are younger.

At premature and newborn the dose is reduced and/or increase an interval between receptions. A course of treatment - 5-12 days.

Suspension preparation: to add water to risks to a bottle and it is good to shake up. The prepared suspension is stable at the room temperature within 14 days. Before each use suspension needs to be shaken up. 5 ml of the prepared suspension (1 measured spoon) contain 250 mg of amoxicillin.

At acute uncomplicated gonorrhea appoint 3 times / сут.г once; at treatment of women repeated reception of the specified dose is recommended.

At GIT acute infectious diseases (paratyphus, a typhoid) and bilious ways, at gynecologic infectious diseases adult - 1.5-2 g 3 or on 1-1.5 g 4 times/days.

At a hay fever adult - 0.5-0.75 g 4 times / сут.в a current of 6-12 days.

At a salmonellonositelstvo adult - 1.5-2 g 3 times / сут.в a current of 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 appointment as the patient 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 it is necessary to use whenever possible other or additional methods of contraception.

Side effects:

Allergic reactions: the small tortoiseshell, a dermahemia, an erythema, a Quincke's disease, rhinitis, conjunctivitis are possible; seldom - fever, joint pains, an eosinophilia, exfoliative dermatitis, a poliformny exudative erythema, Stephens-Johnson's syndrome; reactions similar to a serum disease; in isolated cases - an acute anaphylaxis.
From the alimentary system: dysbacteriosis, taste change, vomiting, nausea, diarrhea, stomatitis, glossitis, moderate increase in activity of hepatic transaminases, pseudomembranous coloenteritis.
From a nervous system: excitement, uneasiness, sleeplessness, ataxy, confusion of consciousness, change of behavior, depression, peripheral neuropathy, headache, dizziness, convulsive reactions.
Laboratory indicators: leukopenia, neutropenia, Werlhof's disease, anemia.
Others: the complicated breath, tachycardia, intersticial nephrite, vagina candidiasis, superinfection (especially at patients with chronic diseases or the lowered resistance of an organism).

Interaction with other medicines:

Pharmaceutical it is incompatible with aminoglycosides (in order to avoid a mutual inactivation it is impossible to mix).
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 paroaminobenzoyny acid, ethinylestradiol - risk of development of bleedings of break is formed.
Diuretics, Allopyrinolum, оксифенбутазон, the phenylbutazone, NPVP, drugs blocking canalicular secretion reduce canalicular secretion, increase concentration.
Allopyrinolum increases risk of development of skin rash.
Reduces clearance and increases toxicity of a methotrexate.
Strengthens digoxin absorption.

Contraindications:

— allergic diathesis;
— bronchial asthma;
— pollinosis;
— infectious mononucleosis;
— lymphoid leukosis;
— liver failure;
— gastrointestinal diseases in the anamnesis (especially the colitis connected using antibiotics);
— lactation period;
— hypersensitivity (including to other penicillin, cephalosporins, karbapenema).

With care - pregnancy, a renal failure, bleedings in the anamnesis.

Use of the drug AMOXICILLIN at pregnancy and feeding by a breast
With care use drug at pregnancy. It is contraindicated in the period of a lactation.

Use at abnormal liver functions
It is contraindicated at a liver failure.

Use at renal failures
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.

Use for children
To children appoint in the form of suspension: at the age of 5-10 years - on 250 mg (5 ml of suspension) of 3 times/days; 2-5 years - on 125 mg (2.5 ml of suspension) of 3 times/days; 2 years - 20 mg/kg of body weight the day divided into 3 receptions are younger.
At premature and newborn the dose is reduced and/or increase an interval between receptions. A course of treatment - 5-12 days.

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, medicines for maintenance of water and electrolytic balance; hemodialysis.

Storage conditions:

List B. To store in the unavailable to children, dry, protected from light place at a temperature from 15 °C to 25 °C.

Issue conditions:

According to the recipe

Packaging:

Capsules on 250 or 500 mg in the blister of 8 pieces; in a box 2 blisters.