Amoxicillin - instructions for use, dose, side effects, contraindications

active substance - amoxicillin 250 mg (in the form of amoxicillin trihydrate);
Excipients - 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, passion-edible flavors - 1,750 mg, raspberry flavor 5,000 mg, strawberry flavor 16,750 mg.

Description:

Granular powder from white to white with a yellowish hue of color.

When water is added, a yellowish suspension with a characteristic fruity smell is formed.

Pharmacotherapeutic group:Antibiotic - penicillin semisynthetic

ATX: & nbsp

J.01.C.A.04 Amoxicillin

Pharmacodynamics:

Antibacterial bactericidal acid-resistant broad spectrum agent from the group of semisynthetic penicillins. It inhibits transpeptidase, breaks the synthesis of peptidoglycan (the supporting protein of the cell wall) in the period of division and growth, causes bacterial lysis.

It is active against aerobic gram-positive bacteria: Bacillus anthracis, Corynebacterium spp., Enterococcus faecalis, Listeria monocytogenes, Staphylococcus spp. (behind excluding strains producing penicillinase); Streptococcus spp., in t.ch. Streptococcus pneumoniae;

aerobic gram-negative bacteria: Bordetella pertussis, Brucella spp., Escherichia coli, Haemophilus influenzae, Klebsiella spp., Neisseria gonorrhoeae, Neisseria meningitidis Shigella spp., Salmonella spp., Pasteurella septica, Proteus mirabilis, Vibrio cholerae;

other microorganisms: Clostridium spp, Leptospira spp., and Helicobacter pylori, Borrelia burgdorferi.

Amoxicillin undergoes destruction by beta-lactamases, therefore the microorganisms producing beta-lactamases (penicillinase, etc.) do not enter the spectrum of its antibacterial activity.

Pharmacokinetics:

Absorption - fast, high (about-93%), food intake does not affect absorption, amoxicillin does not degrade in the acidic environment of the stomach. When administered orally at a dose of 125 mg and 250 mg, the maximum concentration in the blood plasma is achieved after 1-2 hours and is 1.5-3 μg / ml and 3.5-5 μg / ml, respectively.

Has a large volume of distribution: in high concentrations found in plasma, sputum, bronchial secretion (in the purulent bronchial secretion is weak), pleural and peritoneal fluid, urine; the contents of skin blisters, lung tissue, intestinal mucosa, female genital organs, prostate gland, middle ear fluid; bone, adipose tissue, gallbladder (with normal liver function), tissues of the fetus. When the dose is increased, the concentration also doubles.Concentration in bile exceeds the concentration in plasma by 2-4 times. In amniotic fluid and vessels of the umbilical cord, the concentration of amoxicillin is 25-30% of the value 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%. The connection with plasma proteins is about 17%.

Partially metabolized with the formation of inactive metabolites. The half-life is -1-1.5 hours. It is excreted by 50 -70% kidneys in unchanged form by tubular secretion (80%) and glomerular filtration (20%), liver - 10-20%. In small amounts excreted in breast milk. Half-life in preterm, newborns and children up to 6 months is 3-4 hours. If renal function is impaired (creatinine clearance less than or equal to 15 ml / min), the elimination half-life increases to 8.5 hours. Amoxicillin is removed during hemodialysis.

Indications:

Infectious-inflammatory diseases caused by microorganisms sensitive to amoxicillin: respiratory tract infections and ENT organs (sinusitis, pharyngitis, tonsillitis, acute otitis media, bronchitis, pneumonia), urogenital system (pyelonephritis, pyelitis, cystitis, urethritis, gonorrhea, endometritis, cervicitis ), the gastrointestinal tract (enterocolitis, shigellosis, typhoid fever, salmonellosis, salmonellosis), cholangitis, cholecystitis, gastric and duodenal ulcer (as part of combination therapy), skin and soft tissue infections (erysipelas, impetigo, secondarily infected dermatoses), leptospirosis, listeriosis, Lyme disease (borreliosis), meningitis, endocarditis (prophylaxis ), sepsis, peritonitis.

Contraindications:

Hypersensitivity to amoxicillin and / or accessory components of the drug, hypersensitivity to beta-lactam antibiotics (including to others. penicillins, cephalosporins, carbapenems and Pp.)) atopic dermatitis,bronchial asthma, pollinosis, infectious mononucleosis, lymphocytic leukemia, liver failure, gastrointestinal diseases in history (especially colitis associated with use of antibiotics), lactation period, sugarase / isomaltase deficiency, fructose intolerance, glucose-galactose malabsorption.

Carefully:Pregnancy, renal insufficiency, bleeding in the history, allergic reactions (including in the anamnesis).

Pregnancy and lactation:

Amoxicillin penetrates the placental barrier in small amounts, excreted in breast milk.

If you need to use amoxicillin during pregnancy, you should carefully weigh the expected benefit of therapy for the mother and the potential risk to the fetus.

During lactation (breastfeeding) amoxicillin use with caution.

Dosing and Administration:

Inside, before or after eating.

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

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

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

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

In preterm 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: in the vial add water to the risks and shake well. The prepared suspension should be stored in a refrigerator (at a temperature of 2-8 ° C) and used within 14 days.

Before each use, the suspension must be shaken.

5 ml of the prepared suspension (1 measuring spoon) contain 250 mg of amoxicillin.

If there are no special recommendations, the standard dosing regimen is applied.

Special recommendations on the dosing regimen

In acute uncomplicated gonorrhea appoint 3 g (60 ml) once; in the treatment of women, repeated intake of this dose is recommended.

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

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

When leptospirosis adults - 0,5-0,75 g (10-15 ml) 4 times a day for 6-12 days.

In case of salmonella carrying to adults -1.5-2 g (30-40 ml) 3 times a day for 2-4 weeks.

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

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

Side effects:

Allergic reactions: urticaria, skin hyperemia, erythema, angioedema,rhinitis, conjunctivitis, fever, joint pain, eosinophilia, exfoliative dermatitis, multiforme exudative erythema, Stevens-Johnson syndrome, acute generalized exanthematous pustulosis; reactions similar to serum sickness, allergic vasculitis, anaphylactic shock.

From the digestive system: dysbacteriosis, taste change, 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.

From the nervous side system: agitation, anxiety, insomnia, ataxia, confusion, behavior change, depression, peripheral neuropathy, headache, dizziness, convulsive reactions.

Laboratory indicators: leukopenia,neutropenia, thrombocytopenic purpura, anemia.

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

Overdose:

Symptoms: nausea, vomiting, diarrhea, impairment, water-electrolyte balance (as a consequence of vomiting and diarrhea).

Treatment: gastric lavage, Activated carbon, salt laxatives, medicines to maintain the water-electrolyte balance; hemodialysis.

Interaction:

Pharmaceutically incompatible with aminoglycosides (to avoid mutual inactivation it is impossible to mix).

Antacids, glucosamine, laxatives, food, aminoglycosides - slow down and reduce absorption; ascorbic acid increases absorption. Bactericidal antibiotics (including: aminoglycosides, cephalosporins, cycloserine, vancomycin, rifampicin) - synergistic effect; bacteriostatic drugs - (macrolides, chloramphenicol, lincosamides, tetracyclines, sulfonamides) - antagonistic.

Increases the effectiveness of indirect anticoagulants (suppressing the shoulder microflora, reduces the synthesis of vitamin K and prothrombin index); reduces the effectiveness of estrogen-containing oral contraceptives (including ethinylestradiol), medicines, in the process of metabolism of which the para-aminobenzoic acid - the risk of bleeding "breakthrough".

Diuretics, allopurinol, oxyphenbutazone, phenylbutazone, non-steroidal anti-inflammatory drugs; drugs that block tubular secretion - reducing tubular secretion, increase concentration.

Allopurinol increases the risk of skin rash.

Reduces clearance and increases the toxicity of methotrexate.

Increases the absorption of digoxin.

Unchanged amoxicillin is excreted in the urine. High concentrations of amoxicillin give a false positive reaction to urine glucose when using a Benedict reagent or Felling solution. It is recommended to use enzymatic reactions with glucose oxidase.

Special instructions:

In course treatment it is necessary to monitor the status of the functions of the organs of hematopoiesis, liver and kidneys.

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

With the appointment of patients and bacteremia, the development of a bacteriolysis reaction (the Yarisch-Gerxheimer reaction) is possible.

In patients who have increased sensitivity to penicillins, there may be cross-allergic reactions with other beta-lactam antibiotics.

In the treatment of mild diarrhea against the background of course treatment, antidiarrheal drugs should be avoided, which reduce intestinal peristalsis; it is possible to use kaolin- or attapulgite-containing antidiarrhoeic agents. When severe diarrhea should be referred to a doctor.

Treatment necessarily continues for another 48-72 hours after the disappearance of clinical signs of the disease.

With the simultaneous use of estrogen-containing oral contraceptives and amoxicillin, whenever possible, use other or additional methodscontraception.

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.

Effect on the ability to drive transp. cf. and fur:

During the use of the drug, patients should be very careful to drive and engage in other potentially hazardous activities, due to possible adverse reactions from the nervous system,such as dizziness, agitation, behavioral disorders.

Form release / dosage:

Granules for the preparation of a suspension for oral administration 250 mg / 5 ml.

Packaging:40 grams of granules for the preparation of 100 ml of suspension in a vial of dark glass with a risk, sealed with a plastic or metal cover screwed with a first opening control. On the top side of the plastic cover is a scheme for opening the bottle. 1 bottle with a measuring spoon (volume 5 ml, with a risk for volume of 2.5 ml) and instructions for use in a pack of cardboard.

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

Shelf life:

4 years.

Do not use after the expiry date printed on the package.

Terms of leave from pharmacies:On prescription

Registration number:П N011641 / 02

Date of registration:29.08.2011 / 29.01.2016

Expiration Date:Unlimited

The owner of the registration certificate:Hemofarm ADHemofarm AD Serbia

Manufacturer: & nbsp

HEMOFARM, A.D. Serbia

Representation: & nbspNizhpharm, JSCNizhpharm, JSCRussia

Information update date: & nbsp19.08.2017

Illustrated instructions

Instructions

Amoxicillin (Amoxicillin)