Amoxicillin, 250mg/5ml suspension, 100ml vials

Composition

2 g of granules (5 ml of the finished suspension) contain

Active ingredient-amoxicillin 250 mg (in the form of amoxicillin trihydrate);

Auxiliary substances

Sodium Saccharinate dihydrate 3,250 mg

Simethicone S 184 — 7,750 mg

Guar gum 21,000 mg

Sodium Benzoate 25,000 mg

Sodium Citrate Dihydrate 27,000 mg

Sucrose 1642,500 mg

Passionflower Edible Flavor 1,750 mg

Raspberry flavor 5,000 mg

Strawberry flavor 16,750 mg

Pharmacological action

Amoxicillin is a broad-spectrum antibacterial acid-resistant bactericidal agent from the group of semi-synthetic penicillins.

It inhibits transpeptidase, disrupts the synthesis of peptidoglycan (a cell wall support protein) during division and growth, and causes bacterial lysis.

Due to the wide spectrum of action, the drug is active against both gram-positive and gram-negative microorganisms.

Clinically significant gram-negative microorganisms sensitive to amoxicillin include Escherichia coli, Proteus mirabilis, Salmonella, Shigella, CamPylobacter, Haemophilus influenzae, Bordetella pertussis, Leptospira, Chlamydia.

In addition, amoxicillin is active against all microorganisms sensitive to penicillin G, for example, Streptococcus groups A, B, C, G, H, I, M, Streptococcus pneumoniae, staphylococci and Neisseria spp. not

producing penicillinase, Erysipelothrix rhysiopathiae, Corynebacterium, Bacillus anthracis, Actinomycetes, Streptobacilli, Spirillium minus, Pastereulla multocida, Listeria, Spirochaeta (Leptospira, Treponema, Borrelia) and others, as

well as various anaerobic microorganisms (including peptococci, Peptostreptococcus, Clostridium, and fuzobakterii).

Pharmacokinetics

Absorption – fast, high (93%), food intake does not affect absorption, does not break down in the acidic environment of the stomach.

When taken orally at a dose of 125 and 250 mg, the maximum concentration is 1.5-3 mcg / ml and 3.5-5 mcg/ml, respectively.

The action develops in 15-30 minutes after application and lasts 8 hours. The time to reach the maximum concentration after oral use is 1-2 hours.

Has a large volume of high concentrations found in plasma, sputum, bronchial secretions (in purulent bronchial secretion distribution weak), pleural and peritoneal fluid, urine,

content, skin blisters, lung tissue, intestinal mucosa, female genitals, and the prostate gland, middle ear fluid, bone, fat tissue, gall bladder (normal liver), fetal tissues.

When the dose is increased by 2 times, the concentration also increases by 2 times.

The concentration in bile exceeds the concentration in plasma by 2-4 times.

In the amniotic fluid and vessels of the umbilical cord, the concentration of amoxicillin is 25-30% of the level in the plasma of a pregnant woman.

Poorly penetrates the blood-brain barrier, with inflammation of the meninges (meningitis), the concentration in the cerebrospinal fluid is about 20%. Binding to plasma proteins is 17%.

Partially metabolized to form inactive metabolites. The elimination half-life is 1-1.5 hours.

It is excreted by 50-70% by the kidneys in unchanged form by tubular excretion (80%) and glomerular filtration (20%), by the liver – 10-20%.

It is excreted in small amounts in breast milk. If renal function is impaired (creatinine clearance is less than or equal to 15 ml / min), the elimination half-life increases to 8.5 hours.

Amoxicillin is removed during hemodialysis.

Indications

Infectious and inflammatory diseases caused by microorganisms sensitive to amoxicillin:  

infection of the respiratory tract and ENT organs (sinusitis, pharyngitis, tonsillitis, acute otitis media, bronchitis, pneumonia), urogenital system (pyelonephritis, pyelitis, cystitis, urethritis, gonorrhea, endometritis, cervicitis),

gastrointestinal tract (enterocolitis, shigellosis, typhoid fever, salmonellosis, salmonellosis), cholangitis, cholecystitis, peptic ulcer and duodenal ulcer (in combination therapy),

infections of skin and soft tissues (erysipelas, impetigo, secondarily infected dermatoses), leptospirosis, listeriosis, Lyme disease (Lyme disease), meningitis, endocarditis (prevention), sepsis, peritonitis.

Use during pregnancy and lactation

It is possible to use amoxicillin during pregnancy if the benefit to the mother exceeds the potential risk to the fetus.

Amoxicillin is excreted in breast milk in low concentrations.

If it is necessary to use the drug during lactation, the question of stopping breastfeeding should be decided.

Contraindications

• Hypersensitivity to product components (including other penicillins, cephalosporins, carbapenems),
• allergic diseases (including in history),
• bronchial asthma,
• hay fever,
• infectious mononucleosis,
• lymphatic leukemia,
• liver failure,
• colitis associated with antibiotic use, including history,
• lactation,
• children’s age up to 10 years with body weight less than 40 kg.

With caution – pregnancy, allergic reactions (including in the anamnesis), diseases of the gastrointestinal tract in the anamnesis, renal failure, as well as if there is a history of bleeding.

Side effects

Allergic reactions: urticaria, skin hyperemia, erythema, angioedema, rhinitis, conjunctivitis, fever, joint pain, eosinophilia, exfoliative dermatitis, erythema

multiforme, Stevens-Johnson syndrome, acute generalized exanthematous pustulosis; reactions similar to serum sickness, allergic vasculitis, anaphylactic shock.

From the digestive system:  

dysbiosis, taste changes, vomiting, nausea, diarrhea, stomatitis, glossitis, ” black hairy “tongue, discoloration of the surface layer of tooth enamel, moderate increase in the activity of” liver ” transaminases, hepatitis, cholestatic jaundice, pseudomembranous colitis.

Nervous system disorders:  

agitation, anxiety, insomnia, ataxia, confusion, behavior changes, depression, peripheral neuropathy, headache, dizziness, convulsive reactions.

Laboratory parameters:  

leukopenia, neutropenia, thrombocytopenic purpura, anemia.

Other services:  

shortness of breath, tachycardia, hemolytic anemia, agranulocytosis, interstitial nephritis, crystalluria, vaginal candidiasis, superinfection (especially in patients with chronic diseases or reduced body resistance).

Interaction

Pharmacologically incompatible with aminoglycosides (to avoid mutual inactivation, do not mix).

Antacids, glucosamine, laxatives, food, aminoglycosides-slow down and reduce absorption; ascorbic acid increases absorption.

Bactericidal antibiotics (including aminoglycosides, cephalosporins, cycloserine, vancomycin, rifampicin) have a synergistic effect; bacteriostatic drugs (macrolides, chloramphenicol, lincosamides, tetracyclines, sulfonamides) have an antagonistic effect.

Increases the effectiveness of indirect anticoagulants (suppressing the intestinal microflora, reduces the synthesis of vitamin K and the prothrombin index); reduces the effectiveness of estrogen-containing oral contraceptives,

drugs that produce paroaminobenzoic acid in the process of metabolism, ethinyl estradiol – the risk of breakthrough bleeding.

Diuretics, allopurinol, oxifenbutazone, phenylbutazone, nonsteroidal anti-inflammatory drugs; drugs that block tubular secretion-reducing tubular secretion, increase the concentration.

Allopurinol increases the risk of developing a skin rash.

Reduces the clearance and increases the toxicity of methotrexate.

Increases digoxin absorption.

How to take, course of use and dosage

Inside, before or after a meal.

Adults and children over 10 years of age (with a body weight of more than 40 kg)

Standard dosage regimen: 500 mg (10 ml) 3 times a day; in severe cases of infection — 750 mg -1 g (15-20 ml) 3 times a day.

Children aged 5-10 years are prescribed 250 mg (5 ml of suspension) 3 times a day; children 2-5 years-125 mg (2.5 ml of suspension) 3 times a day; younger than 2 years — 20 mg/kg of body weight per day, divided into 3 doses.

The maximum daily dose for children under 3 months of age is 30 mg / kg / day, divided into 2 doses (every 12%^%h).

In preterm infants and newborns, the dose is reduced and / or the interval between doses is increased.

The course of treatment is 5-12 days.

Preparation of the suspension: add water to the bottle until ready and shake well. The prepared suspension should be stored in the refrigerator (at a temperature of 2-8 °C) and used for 14 days.

Before each use, the suspension must be shaken. 5 ml of the prepared suspension (1 scoop) contains 250 mg of amoxicillin. If there are no specific recommendations, the standard dosage regimen is applied. Special recommendations for the dosage regimen

In acute uncomplicated gonorrhea,3 g (60 ml) is prescribed once; in the treatment of women, repeated use of the indicated dose is recommended.

For acute infectious diseases of the gastrointestinal tract (paratyphoid, typhoid fever) and biliary tract, for gynecological infections, adults — 1.5-2 g (30 — 40 ml) 3 times a day or 1-1.5 g 4 times a day.

For gastric and duodenal ulcers (as part of combination therapy): 750-1000 mg 2 times a day.

For leptospirosis adults — 0.5-0.75 g (10 — 15 ml) 4 times a day for 6-12 days. In case of Salmonella transmission to adults-1.5-2 g (30 — 40 ml) 3 times a day for 2-4 weeks.

For the prevention of endocarditis with minor surgical interventions, adults — 3-4 g (60-70 ml) 1 hour before the procedure. If necessary, a second dose is prescribed after 8-9 hours. In children, the dose is reduced by 2 times.

In patients with impaired renal function with a creatinine clearance of 15-40 ml / min, the interval between doses is increased to 12 hours; with a creatinine clearance below 10 ml/min, the dose is reduced by 15-50%; with anuria, the maximum dose is 2 g / day.

Overdose

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

Treatment: gastric lavage, activated charcoal, saline laxatives, medications to maintain water and electrolyte balance; hemodialysis.

Description

Granular powder from white to white with a yellowish tinge of color. When water is added, a yellowish suspension with a characteristic fruity smell is formed.

Special instructions

During the course of treatment, it is necessary to monitor the state of function of the hematopoietic organs, liver and kidneys.

It is possible to develop superinfection due to the growth of microflora that is insensitive to it, which requires a corresponding change in antibacterial therapy.

When prescribed to patients with bacteremia, a bacteriolysis reaction (Yarish-Gerksheimer reaction) may develop.

Patients who are hypersensitive to penicillins may have cross-allergic reactions with other beta-lactam antibiotics.

In the treatment of mild diarrhea during the course of treatment, antidiarrheal drugs that reduce intestinal motility should be avoided; kaolin-or attapulgite-containing antidiarrheal agents can be used.

If you have severe diarrhea, you should consult a doctor.

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

When using estrogen-containing oral contraceptives and amoxicillin at the same time, other or additional methods of contraception should be used if possible.

Patients with diabetes should take into account that 5 ml of suspension (2 g of granules) contains 1.65 g of sucrose (or 0.14 bread units, XE), respectively, the maximum daily dose of amoxicillin contains 3.3 XE.

Form of production

Granulate for preparation of oral suspension

Storage conditions

At temperatures up to 25 °C in the original packaging, in a dry place protected from light. Keep out of reach of children.

Shelf

life is 3 years. Do not use after the expiration date indicated on the package.

Active ingredient

Amoxicillin

Conditions of release from pharmacies

By prescription

Dosage form

suspension for oral use

Purpose

Pregnant women as prescribed by a doctor, Children as prescribed by a doctor, Adults as prescribed by a doctor

Indications

Bronchitis, Pharyngitis, Urinary Tract Infections, Skin Infections, Otitis Media, Respiratory Tract Infections, Intestinal Infections, Sore Throat