Expiration date: 11/2025

Pharmachologic effect:

Broad-spectrum antibiotic group of semisynthetic penicillins. Effective bactericidal. Inhibits transpeptidase, violates the synthesis of peptidoglycan (the reference polymer cell wall) during the division and growth, causes lysis of the bacteria. Is acid.

It is active against aerobic Gram-positive bacteria: Staphycccus spp. (Except for strains producing penicillinase), Streptcccus spp. Aerobic gram-negative bacteria: Neisseria gnrrheae, Neisseria meningitidis, Bacius anthracis, Listeria mncytgenes, Heicbacter pyri, Kebsiea spp.

Microorganisms that produce penicillinase, resistant to the action of amoxicillin.

Action develops within 15-30 min after administration and continuing for 8 hours.

Pharmacokinetics:

Suction

After oral administration, amoxicillin is rapidly and almost completely (93%) absorbed from the gastrointestinal tract. Eating does not affect the absorption of the drug is not degraded in the acidic environment of the stomach. Cmax in plasma of the active substance is observed after 1-2 h. When administered in a dose of 125 mg and 250 mg Cmax in plasma is 1.5-3 mg / mL and 3.5-5 ug / ml, respectively.

Distribution

It has a large volume distribution: in the high concentrations found in plasma, sputum, bronchial secretions (in suppurative bronchial secretions distribution weak), pleural and peritoneal fluid, urine contents skin blisters, lung tissue, intestinal mucosa, female genital organs, prostate gland, middle ear fluid, bone, adipose tissue, gallbladder (normal liver), fetal tissues. With increasing doses of 2-fold concentration is also increased by 2 times. The concentration in the bile exceeding the plasma concentration of 2-4 fold. The amniotic fluid and umbilical cord vessels amoxicillin concentration - 25-30% of the level in the plasma of pregnant women. Poor permeates through GEB, inflammation of the meninges (meningitis), the concentration in the cerebrospinal fluid - about 20%.

Binding to plasma proteins - 17%.

The small amount is excreted in breast milk.

Metabolism

Amoxicillin is partly metabolized to inactive metabolites.

breeding

T1 / 2 of amoxicillin is 1-1.5 hours Amoxicillin output by 50-70% in the urine as unchanged by tubular excretion (80%) and glomerular filtration rate (20%), with bile -. 10-20% .u premature, newborn and children under 6 months - 3-4 hours.

Pharmacokinetics in special clinical situations

In preterm, infants and children under 6 months of T1 / 2 of 3-4 hours.

If the kidney function (creatinine clearance e 15 ml / min) T1 / 2 of amoxicillin increased to 8.5 hours.

Amoxicillin is removed by hemodialysis.

Testimony:

Infectious-inflammatory diseases caused by susceptible to malaria infections:

• Respiratory infections (including bronchitis, pneumonia)
  
• Upper respiratory tract infections (including sinusitis, pharyngitis, tonsillitis, acute otitis media)
  
• Infections of the genitourinary system (including pyelonephritis, pyelitis, cystitis, urethritis, gonorrhea)
  
• Gynecological infections (including endometritis, cervicitis)
  
• Digestive tract infections (including peritonitis, enterocolitis, typhoid fever, cholangitis, cholecystitis)
  
• Infections of skin and soft tissue (including erysipelas, impetigo, secondarily infected dermatoses)
  
• leptospirosis
  
• listeriosis
  
• Lyme disease (borreliosis)
  
• dysentery
  
• Salmonellosis, salmonellonositelstvo
  
• meningitis
  
• Endocarditis (prophylaxis)
  
• Sepsis.
  

Dosage and administration:

The drug is taken orally before or after a meal. The mode set individually, taking into account the severity of the disease, the sensitivity of the pathogen to the drug, the patient's age.

Adults and children over 10 years (with a body weight gt40 kg) administered at 500 mg 3 times / day, in severe disease - at 0.75-1 g 3 times / day.

Children aged 5 to 10 years appoint 250 mg 3 times / day, from 2 to 5 years - 125 mg 3 times / day, at the age of 2 - 20 mg / kg / day in 3 divided doses. The course of treatment - 5-12 days. Children under the age of 5 years, the drug is administered in the form of a suspension.

For the treatment of acute uncomplicated gonorrhea drug prescribed at a dose of 3 g single dose is recommended in the treatment of women receiving this dose repeated.

In acute infectious diseases of the gastrointestinal tract (paratyphoid fever, typhoid fever), and biliary tract, gynecological infectious diseases of adults appoint 1.5-2 g 3 times / day or 1-1.5 g 4 times / day.

When leptospirosis adult prescribe on 500-750 mg 4 times / day for 6-12 days.

When salmonellonositelstve adults - 1.5-2 g 3 times / day for 2-4 weeks.

For the prevention of endocarditis with small surgical interventions for adults is prescribed in a dose of 3-4 g for 1 hour before the procedure. If necessary, repeat the dose administered 8-9 hours. In children, the dose is reduced by half.

In patients with impaired renal function (creatinine clearance 15 to 40 mL / min) interval between doses increased to 12 hours, in the terminal stage of chronic renal failure (KKt10 ml / min), the dose should be reduced by Amosina 15-50% or increase the interval between doses up to 24 hours, with anuria - the maximum dose is 2 g / day.

Terms preparation of the suspension

single-dose package

The clean glass is poured boiled and cooled water in the amount shown in the table, then pour the contents of one packet and stirred until a homogeneous suspension.

The dose of the package required amount of water

2.5 ml of 125 mg

250 mg of 5 ml

10 mg 500 ml

After receiving a glass rinsed with water, dried and stored in a dry, clean place.

Side effects:

Allergic reactions: possible - hives, skin flushing, erythema, angioedema, rhinitis, conjunctivitis rarely - fever, joint pain, eosinophilia, exfoliative dermatitis, erythema multiforme exudative, Stevens-Johnson syndrome, a reaction similar to serum sickness and in rare cases - anaphylactic shock.

From the digestive system: goiter, change in taste, nausea, vomiting, diarrhea, stomatitis, glossitis, hepatic dysfunction, a moderate increase in liver transaminases, rarely - pseudomembranous enterocolitis.

From the central and peripheral nervous system: agitation, anxiety, insomnia, ataxia, confusion, behavioral changes, depression, peripheral neuropathy, headache, dizziness, convulsive reaction.

From the urinary system: rarely - interstitial nephritis.

Hematopoietic system: leukopenia, neutropenia, thrombocytopenic purpura, anemia.

Other: shortness of breath, tachycardia, vaginal candidiasis, superinfection (especially in patients with chronic diseases or low resistance of the body).

Contraindications:

• Allergic diathesis
  
• Asthma, hay fever
  
• Infectious mononucleosis
  
• lymphocytic leukemia
  
• liver failure
  
• Gastrointestinal disease in history (especially colitis, associated with the use of antibiotics)
  
• Lactation (breast-feeding)
  
• Hypersensitivity to the drug
  
• Increased sensitivity to other penicillins, cephalosporins, carbapenems)
  
• Children up to age 3 years (for tablets and capsules).
  

Precautions should be prescribed the drug during pregnancy, renal failure, as well as indications of a history of bleeding.

Pregnancy and lactation:

Use of the drug during pregnancy is possible only when the intended benefits of therapy for the mother outweighs the potential risk to the fetus.

Use during lactation is contraindicated. If necessary, use during lactation should stop breastfeeding.

Special instructions:

During the course of treatment Amosinom need to monitor the state of the functions of blood, liver and kidneys.

Perhaps the development of superinfection due to growth insensitive to amoxicillin microflora, which requires a corresponding change in antibiotic therapy.

When treating patients with bacteremia rarely develops bacteriolysis reaction (Jarisch-Herxheimer).

In patients with increased sensitivity to penicillins, possible allergic cross-reaction with cephalosporin antibiotics.

In the treatment of mild diarrhea during treatment Amosina should be avoided antidiarrhoeal drugs that reduce intestinal motility can use kaolin or attapulgitsoderzhaschie antidiarrheals. If severe diarrhea is necessary to make a differential diagnosis and prescribe appropriate therapy.

Treatment should continue for 48-72 hours after the disappearance of clinical signs of disease.

With simultaneous use of oral contraceptives and estrogensoderjath amoxicillin should, whenever possible, to use additional methods of contraception.

Overdose:

Symptoms include nausea, vomiting, diarrhea, disruption of water and electrolyte balance (as a result of vomiting and diarrhea).

Treatment: gastric lavage, activated charcoal, saline laxative measures to maintain water and electrolyte balance hemodialysis.

Drug Interactions:

Antacids, glucosamine, laxatives, food, aminoglycoside antibiotics, while applying slow down and reduce the absorption of amoxicillin ascorbic acid - increases its absorption.

Bactericidal antibiotics (including aminoglycosides, cephalosporins, cycloserine, vancomycin, rifampicin) exhibit synergism with amoxicillin bacteriostatic drugs (macrolides, chloramphenicol, lincosamides, tetracyclines, sulfonamides) - antagonism.

Amoxicillin, while the application improves efficiency anticoagulants (suppressing the intestinal microflora, reducing the synthesis of vitamin K and prothrombin index) estrogensoderzhaschih reduces the effectiveness of oral contraceptives, ethinyl estradiol (risk of intermenstrual bleeding) and drugs metabolized which is formed of p-aminobenzoic acid.

Diuretics, allopurinol, oxyphenbutazone, phenylbutazone, NSAIDs, and drugs that block tubular secretion, while the use of Amosinom reduce tubular secretion, increase the concentration of amoxicillin.

In an application Amosina with allopurinol increases the risk of skin rash.

Amoxicillin while the application reduces clearance and increases the toxicity of methotrexate.

Amoxicillin while the application increases the absorption of digoxin.

Conditions and terms:

List B. The drug should be stored out of reach of children, dry, dark place. Powder for suspension should be stored at a temperature of 15 ° to 25 ° C. Tablets and capsules should be stored at a temperature not exceeding 25 ° C. Shelf life - 2 years.