Amoxicillin

General characteristics. Structure:

Active ingredient: 250 mg of amoxicillin in 1 capsule.

Excipients: magnesium stearate, talc.

Structure of a gelatin capsule: diamond blue E133, E122 carmoisin, orange yellow E110, titanium dioxide, iron oxide yellow, gelatin.

Antibiotic of a broad spectrum of activity.

Pharmacological properties:

Pharmacodynamics. Amoxicillin — derivative β-aminopenicillanic acid. Has antibacterial, bactericidal effect. Inhibits transpeptidase, breaks synthesis of a peptidoglikan during division and growth, causes a lysis of microorganisms.

It is active concerning gram-positive and gram-negative cocci, some gram-negative sticks. Collapses β-lactamelements therefore microorganisms — producers β-лактамаз rezistentna to effect of amoxicillin.

Pharmacokinetics. At intake it is soaked up quickly and almost completely (93%). The maximum concentration in a blood plasma (3,5 — 5 mkg/ml) is created in 1 — 2 hour after intake of 250 mg of amoxicillin. It is stable in acid medium, meal does not influence absorption. Gets into various fabrics and bodies, easily passes gistogematichesky barriers (except for not changed blood-brain barrier). The elimination half-life makes 1 — 1,5 hours, at a renal failure the elimination half-life is extended till 4 — 12,6 o'clock. It is partially metabolized with formation of inactive metabolites. It is removed by kidneys in not changed look (50 — 70%), 10 — 20% of an antibiotic are excreted with bile. In a small amount it is allocated with breast milk.

Indications to use:

Respiratory infection and ENT organs (bronchitis, pneumonia, quinsy, acute average otitis, pharyngitis, sinusitis), urinogenital system (urethritis, cystitis, pyelonephritis, endometritis, uncomplicated gonorrhea), skin and soft tissues, digestive tract (peritonitis, enteritis, cholecystitis, cholangitis, typhoid); leptospirosis, listeriosis, meningitis, disease Laima (borreliosis), prevention of an endocarditis and surgical infection; a combination therapy of a peptic ulcer of a stomach (in combination with metronidazole), sepsis (together with aminoglycosides).

Route of administration and doses:

Drug is appointed inside. The single dose for adults and teenagers is more senior than 10 years makes 0,5 g 3 times a day. At a severe disease the dose is increased to 1,0 g by 3 times a day. The maximum daily dose — 6 g. To children aged from 5 up to 10 years appoint 0,25 g 3 times a day; from 2 to 5 years — on 0,125 g 3 times a day; up to 2 years — at the rate of 0,02 g/kg of body weight, the calculated daily dose is divided into 3 receptions. The course of treatment makes 5 — 12 days (at streptococcal infections — not less than 10 days).

To patients with clearance of creatinine lower than 10 ml/min. reduce a dose by 15 — 50%, at an anury the dose should not exceed 2 g a day.

For treatment of uncomplicated gonorrhea appoint 3,0 g of drug to one reception; along with amoxicillin it is desirable to appoint 1,0 g of a probenetsid.

Features of use:

Treatment is continued surely within 48 — 72 hours after disappearance of clinical signs of a disease.

At pregnancy apply according to vital indications taking into account the expected effect to mother and potential risk to a fruit.

Precautionary measures. At heavy renal failures (the clearance of creatinine is lower than 10 ml/min.) it is necessary to increase an interval between introductions to 12 — 24 h. With care apply at urticaria and hay fever. It is necessary to control periodically function of a liver, kidneys and a hemogenesis in the course of long therapy.

Side effects:

Nausea, vomiting, diarrhea, pains in the field of an anus, stomatitis, a glossitis, excitement, concern, sleeplessness, confusion of consciousness, a headache, dizziness, convulsive reactions, the complicated breath, tachycardia, joint pains, intersticial nephrite, dysbacteriosis, superinfection, candidiasis of an oral cavity or vagina, pseudomembranous or hemorrhagic colitis, moderate increase in level of transaminases in blood, tranzitorny anemia, a Werlhof's disease, an eosinophilia, a leukopenia, a neutropenia, an agranulocytosis, allergic reactions (exfoliative dermatitis, a mnogoformny exudative erythema, Stephens-Johnson's syndrome, an acute anaphylaxis, makulopapulezny rash, an itch, a small tortoiseshell, a Quincke's edema).

Interaction with other medicines:

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

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

Contraindications:

Hypersensitivity to penicillin, cephalosporins, karbapenema, allergic diathesis, bronchial asthma, hay fever, an infectious mononucleosis, a lymphoid leukosis, digestive tract diseases in the anamnesis (especially the colitis connected using antibiotics), a lactation (it is necessary to stop breastfeeding for treatment).

Overdose:

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

Treatment: gastric lavage, purpose of absorbent carbon, salt laxatives, correction of water and electrolytic balance, hemodialysis.

Storage conditions:

To store in the dry, protected from light place at a temperature not above 25 °C. A period of validity - 3 years.

Issue conditions:

According to the recipe

Packaging:

Capsules of 250 mg in packaging No. 20, No. 30 (No. 10х2, No. 10х3 in blister strip packagings).