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

auxiliary substances - magnesium stearate - 4.60 mg, microcrystalline cellulose PH 102 - 13.50 mg; capsule number 2: gelatin - up to 61.00 mg; capsule cover: titanium dioxide [E 171] 0.19520 mg, quinoline yellow [E 104] 0.06608 mg, indigocarmine [E 132] -0.05673 mg; Capsule body: titanium dioxide [E 171] -0.72468 mg, quinoline yellow color [E 104] -0,00055 mg.

1 capsule 500 mg contains: active ingredient - amoxicillin 500.00 mg (in the form of amoxicillin trihydrate 573.9 mg);

auxiliary substances - magnesium stearate 9,20 mg, microcrystalline cellulose PH 102 - 26.90 mg; capsule No. 0: gelatin up to 96 mg; capsule cover: titanium dioxide [E 171] - 0,49920 mg, dye sunset yellow [EO] - 0.13774 mg, dye azorubin [E 122] - 0.13336 mg; Capsule body: titanium dioxide [E 171] -0.57600 mg, iron dye oxide yellow [E 172] -0.26899 mg.

Description:

Contents of the capsule: granular powder from white to light yellow color. It is possible to have a pressed cylinder of powder, which when pressed with a glass rod turns into a free-flowing powder.

for 250 mg: fElatin capsules # 2: the lid is dark green, the body is white with a yellowish tinge.

for 500 mg: fElatin capsules # 0: the lid is red, the body is yellow.

Pharmacotherapeutic group:Antibiotic, penicillin semisynthetic.

ATX: & nbsp

J.01.C.A.04 Amoxicillin

Pharmacodynamics:

Semisynthetic aminopenicillin, a bactericidal acid-resistant broad-spectrum agent, belongs to the group of beta-lactam antibiotics. 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. (with the exception of 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 gonorrhoea, Neisseria meningitides, 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 microorganisms producing beta-lactamases (penicillinase, etc.) do not enter the spectrum of its antibacterial activity.

Pharmacokinetics:

Absorption is rapid, 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 250 mg, the maximum concentration in the blood plasma (C_m_Oh) is achieved in 1-2 hours (TCmah) and is 3.5-5 μg / ml. The half-life (T1 / 2) -1-1,5 h.

The connection with plasma proteins is about 17%. Intensively distributed to organs and tissues, is found in biological fluids and pathologically separated; overcomes the histohematological barriers, except for the unchanged blood-brain. In high concentrations it is found in blood plasma, pulmonary, bone and fat tissues, intestinal mucosa, female genital organs, prostate gland, gall bladder (with normal liver function), fetal tissues, pleural and peritoneal fluid, skin blisters, sputum, bronchial secretion (to a lesser extent in purulent discharge), in exudate with inflammation of the middle ear. Concentration in the bile exceeds the concentration in the blood plasma by 2-4 times. AT amniotic fluid and umbilical cord blood, the concentration of amoxicillin is 25-30% of the value in the plasma of a pregnant woman. With inflammation of the meninges amoxicillin overcomes the blood-brain barrier, its concentration in the cerebrospinal fluid, reaches 20% of that in the blood plasma. In a small amount penetrates into breast milk.With increasing dose, the concentration of amoxicillin in organs and tissues increases proportionally.

Partially metabolized to inactive penicillic acid. Excreted mainly by the kidneys - 50-70% in unchanged form by tubular secretion (80%) and glomerular filtration (20%), through the intestine -10 - 20%.

If the renal function is impaired (creatinine clearance less than or equal to 15 ml / min), the elimination half-life increases to 8.5 h.

Indications:

Infectious-inflammatory diseases caused by microorganisms sensitive to amoxicillin:

- respiratory tract infections - acute bronchitis and exacerbation of chronic bronchitis, lobar pneumonia and bronchopneumonia;

- infection of the ENT organs - sinusitis, pharyngitis, tonsillitis, acute otitis media;

- infections of the skin and soft tissues, erysipelas, impetigo, secondarily infected dermatoses;

- infection of the genitourinary system - pyelonephritis, cystitis, urethritis, uncomplicated gonorrhea;

- gynecological infections - endometritis, cervicitis;

- abdominal infections - cholangitis, cholecystitis, enterocolitis, peritonitis;

- intestinal infections - typhoid fever, paratyphoid, salmonella, salmonellosis, shigellosis;

- stomach ulcer and duodenal ulcer (as part of combination therapy);

- endocarditis (prophylaxis for small surgical interventions, including dental surgery);

- other (leptospirosis, listeriosis, Lyme disease (borreliosis)), meningococcal infection.

Contraindications:

Hypersensitivity (including to other penicillins, cephalosporins, carbapenems), atopic dermatitis, bronchial asthma, pollinosis, infectious, mononucleosis, lymphocytic leukemia, liver failure, gastrointestinal diseases in the anamnesis (especially colitis associated with the use of antibiotics), lactation period, children under 5 years (for this dosage form).

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.

Use with caution amoxicillin during lactation (breastfeeding).

Dosing and Administration:

Inside, regardless of food intake, 1 capsule 3 times a day, strictly observing the interval between doses of 8 hours. At high doses, you can take 2 times a day, the interval between doses -12 hours. Capsule to wash down 0,5-1, a glass of water.

Adults

Standard dosing regimen: 1 capsule of 250 mg every 8 hours.

In severe cases: 1 capsule of 500 mg every 8 hours.

A course of treatment 5-12 days; is set individually. As with the use of other antibiotics, treatment is recommended to continue at least 48-72 hours after the normalization of body temperature or after a significant eradication of the pathogen.

The maximum daily dose is 6 g.

Infections of the upper respiratory tract, ENT organs, skin and soft tissues, genitourinary system (with the exception of gonorrhea), gynecological infections (without fever), abdominal infections: PThe standard dosing regimen is used.

Lower respiratory tract infections: Pabout 1 capsule of 500 mg every 8 hours.

Acute uncomplicated urinary tract infections: short-term high-dosage therapy is recommended: 2 doses of 3 g amoxicillin with an interval of 10 -12 hours.

Gonorrhea (acute uncomplicated): 3 g - once (in combination with probenecid).Women are recommended to take this dose again, because it is possible the multiple nature of the lesion (cervix, urethra, rectum) and an upward inflammatory process with the transition to pelvic organs.

Intestinal infection (except salmonella), gynecological infections. accompanied by fever: 1,5 - 2 g 3 times a day or 1 -1,5 g 4 times a day.

Salmonella: on 1,5 - 2 g 3 times a day for 2-4 weeks.

Peptic ulcer of stomach and duodenum (as a part of combined therapy): 750 mg - 1000 g 2 times a day.

Endocarditis (prophylaxis for small surgical interventions, including dental): once, 3 g for 1 h before the intervention. In surgical interventions performed under general anesthesia - once, 3 g for 4 hours before surgery. If necessary - re-reception after 6 hours.

Leptospirosis: 500-750 mg 4 times a day in for 6-12 days.

Elderly patients: with a safe output kidney function correction of the dosing regimen is not required.

Patients with impaired renal function: In severe disorders, the dose should be reduced or the intervals between doses should be increased.

WhenCreatinine clearance (CK) more than 30 ml / min dosage regimen is not required; with CC 10 - 30 ml / min - the maximum daily dose is 1000 mg of amoxycillin (500 mg, 2 times a day); with QC less than 10 ml / min and for patients, on a peritoneal dialysis - 500 mg (250 mg twice a day).

Children older than 5years

The dosage regimen of antibacterial drugs is prescribed by the attending physician, in accordance with the localization and severity of the infection, the sensitivity of the pathogen; the dose is calculated per kilogram of the child's weight. Amoxicillin in a dosage form - Capsules (250 mg and 500 mg) in pediatric practice applicable if use of the drug is shown in a daily dose of not less than 500 mg (in 250 mg 2 times a day).

Standard dosing regimen:

With a body weight of less than 20 kg, the daily dose is 25 mg / kg / day; divided into 3 doses, in severe cases - 50 mg / kg / day as well as in 3 doses.

Body weight over 20 and up to 40 kg the daily dose of amoxicillin is 40 - 90 mg / kg / day, divided into 3 (at low doses) or two doses (at high doses).

With a body weight of more than 40 kg, the adult dosing regimen is applied.

The maximum daily dose is 2 g.

Special recommendations are designed for:

Tonsillitis: 50 mg / kg / day, divided into 3 doses.

Acute otitis media: with severe course and relapses as an alternative therapy scheme can be applied 750 mg 2 times a day, only 2 days.

Prophylaxis of endocarditis: once, 1.5 g for 1 h before intervention. In surgical interventions performed under general anesthesia - once 1.5 g for 4 hours before surgery. If necessary - re-reception after 6 hours.

Children with impaired renal function:

When creatinine clearance (CK) is more than 30 ml / min, dosage regimen correction is not required; with KK 10 - 30 ml / min - increase the interval between doses to 12 h (corresponding to 2/3 of the usual dose); when the SC is less than 10 ml / min, the interval between doses is increased to 24 h (corresponding to the reception of 1/3 of the usual dose).

Important! If you missed taking the drug, you should take the capsule as soon as possible, not waiting for the next appointment. Further, to observe equal time intervals between doses - 8 hours (with the reception mode 3 times a day) or 12 hours (with the reception mode 2 times a day).

Side effects:

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

From the digestive system: dysbacteriosis, eating disorders, dry mouth, nausea, vomiting, diarrhea, stomatitis, glossitis, "black hairy" tongue, moderate increase in the activity of "liver" transaminases, cholestasis, cholestaticsjaundice, acute hepatitis, pseudomembranous hemorrhagic colitis.

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

From the hematopoiesis: leukopenia, neutropenia, thrombocytopenic purpura, anemia, agranulocytosis.

From the urinary system: interstitial nephritis, crystalluria.

Other: shortness of breath, tachycardia, cutaneous candidiasis and mucosal candidiasis, superinfection (especially in patients with chronic diseases or decreased resistance of the organism), increased coagulation time, blood and prothrombin time, staining (yellow, brown or gray plaque) of the teeth, more often in children (removed hygienic means)

Adverse reactions with combined therapy

With triple therapy of peptic ulcer - amoxicillin / clarithromycin / lansoprazole: diarrhea, headache, eating disorders.

When double therapy of peptic ulcer - amoxicillin / lansoprazole: diarrhea, headache.

When combined therapy is recommended to follow the instructions for the drugs that are part of the combination therapy.

Overdose:

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

Treatment: gastric lavage, Activated carbon, salt laxatives, medicines for the normalization of the water-electrolyte balance.

Amoxicillin is removed during hemodialysis.

Interaction:

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

Ethanol reduces the absorption rate of amoxicillin.

Amoxicillin improves the absorption of digoxin.

Probenecid, competing for the elimination route, slows down the elimination of amoxicillin, which leads to an increase in the concentration of amoxicillin in the blood plasma. Similarly amoxicillin interacts with diuretics, non-steroidal anti-inflammatory drugs (oxyphenbutazone, phenylbutazone, acetylsalicylic acid, indomethacin). Amoxicillin promotes a decrease in the clearance of methotrexate, which can lead to the development of toxic effects of the latter.

With the simultaneous administration of allopurinol, the risk of developing skin allergic reactions increases.

Amoxicillin, suppressing the intestinal microflora, reduces the synthesis of vitamin K and the prothrombin index, which increases the effectiveness of indirect anticoagulants and drugs, in the process of metabolism of which paraaminobenzoic acid is formed, which ultimately increases the risk of bleeding "breakthrough".

Amoxicillin reduces the effectiveness of oral contraceptives, since under conditions of altered intestinal biocenosis, reabsorption of estrogens decreases.

With the combined use of amoxicillin with bactericidal antibiotics (aminoglycosides, cephalosporins, cycloserine, vancomycin, rifampicin) there is synergy of antibacterial action. Bacteriostatic preparations (macrolides, chloramphenicol, lincosamides, tetracyclines, sulfonamides), on the contrary, weaken the bactericidal effect of amoxicillin.

Metronidazole increases the antibacterial activity of amoxicillin.

Special instructions:

Before the appointment of amoxicillin, like all penicillins, it is necessary to carefully collect anamnesis for allergic reactions to penicillins, cephalosporins and other beta-lactam antibiotics, taking into account possible cross reactions.

In order to prevent allergic reactions, preventive prescription of antihistamines is allowed.

With the simultaneous use of estrogen-containing oral contraceptives and amoxicillin, additional methods of contraception are recommended. With simultaneous admission with anticoagulants, an increase in prothrombin time is noted. Appropriate monitoring and, possibly, correction (reduction) of the dose of anticoagulant should be carried out.

To prevent the development of crystalluria, the drug should be washed down with a relatively large amount of water (0.5-1, a glass).Compliance with this recommendation is especially important for patients with the original oliguria.

The use of antibiotics is ineffective in the treatment of acute respiratory viral infections.

It is not recommended to apply amoxicillin with infectious mononucleosis and with suspicion of it, since the drug can cause an erythematous skin rash, which exacerbates the symptoms of the disease / complicates the diagnosis.

It is not recommended to apply amoxicillin orally (orally) with diseases of the gastrointestinal tract, accompanied by constant diarrhea or vomiting. Possible development superinfection due to the growth of microflora insensitive to amoxicillin, which requires a corresponding change in antibacterial therapy.

With the development of mild diarrhea against amoxicillin, anti-diarrheal drugs that inhibit intestinal peristalsis should be avoided, kaolin- or attapulgite-containing antidiarrhoeic agents may be used.

Severe diarrhea (a liquid, watery, greenish stool with a sharp, putrefactive odor, with an admixture of blood) in combination with fever and cramping pain in the abdomen is a symptom of a rare but potentially dangerous complication of antibiotic therapy - clostridiotic pseudomembranous colitis, and requires intensive treatment, which is why when these complaints appear, you should immediately consult a doctor.

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 side effects from the nervous system, such as dizziness, agitation, behavioral disorders

Form release / dosage:

Capsules of 250 mg and 500 mg.

Packaging:For 8 capsules in a blister of PVC film and aluminum foil. 2 blisters together with instructions for use in a pack of cardboard.

Storage conditions:Store in a dry, protected from light place at a temperature of 15 to 25 ° C. 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 / 01

Date of registration:30.11.2011

The owner of the registration certificate:Hemofarm ADHemofarm AD Serbia

Manufacturer: & nbsp

HEMOFARM, A.D. Serbia

Representation: & nbspHEMOFARM A.D. HEMOFARM A.D. Serbia

Information update date: & nbsp23.05.2013

Illustrated instructions

Instructions

Amoxicillin (Amoxicillin)