Flemoxin Solutab^® (Tablets) Instructions for Use

ATC Code

J01CA04 (Amoxicillin)

Active Substance

Amoxicillin (Rec.INN registered by WHO)

Clinical-Pharmacological Group

Broad-spectrum penicillin antibiotic, destroyed by penicillinase

Pharmacotherapeutic Group

Antibiotic, semi-synthetic penicillin

Pharmacological Action

A broad-spectrum antibiotic from the group of semi-synthetic penicillins. It is a 4-hydroxy analogue of ampicillin. It has a bactericidal effect. It is active against aerobic gram-positive bacteria: Staphylococcus spp. (except for strains producing penicillinase), Streptococcus spp.; aerobic gram-negative bacteria: Neisseria gonorrhoeae, Neisseria meningitidis, Escherichia coli, Shigella spp., Salmonella spp., Klebsiella spp.

Microorganisms that produce penicillinase are resistant to amoxicillin.

In combination with metronidazole, it shows activity against Helicobacter pylori. It is believed that Amoxicillin inhibits the development of resistance of Helicobacter pylori to metronidazole.

There is cross-resistance between amoxicillin and ampicillin.

The spectrum of antibacterial action expands with the simultaneous use of amoxicillin and the beta-lactamase inhibitor clavulanic acid. In this combination, the activity of amoxicillin against Bacteroides spp., Legionella spp., Nocardia spp., Pseudomonas (Burkholderia) pseudomallei increases. However, Pseudomonas aeruginosa, Serratia marcescens and many other gram-negative bacteria remain resistant.

Pharmacokinetics

When taken orally, Amoxicillin is rapidly and completely absorbed from the gastrointestinal tract and is not destroyed in the acidic environment of the stomach. The C_max of amoxicillin in blood plasma is reached after 1-2 hours. When the dose is doubled, the concentration also doubles. The presence of food in the stomach does not reduce overall absorption. Similar concentrations of amoxicillin in the blood are achieved with intravenous, intramuscular administration and oral administration.

The binding of amoxicillin to plasma proteins is about 20%.

It is widely distributed in body tissues and fluids. High concentrations of amoxicillin in the liver have been reported.

The T_1/2 from plasma is 1-1.5 hours. About 60% of the orally administered dose is excreted unchanged in the urine by glomerular filtration and tubular secretion; at a dose of 250 mg, the concentration of amoxicillin in the urine is more than 300 µg/ml. Some amount of amoxicillin is found in the feces.

In newborns and the elderly, T_1/2 may be longer.

In renal failure, T_1/2 can be 7-20 hours.

Amoxicillin penetrates the blood-brain barrier in small amounts when the meninges are inflamed.

Amoxicillin is removed by hemodialysis.

Indications

For use as monotherapy and in combination with clavulanic acid: infectious and inflammatory diseases caused by susceptible microorganisms, including bronchitis, pneumonia, tonsillitis, pyelonephritis, urethritis, gastrointestinal infections, gynecological infections, infectious diseases of the skin and soft tissues, listeriosis, leptospirosis, gonorrhea.

For use in combination with metronidazole: chronic gastritis in the acute phase, gastric and duodenal ulcers in the acute phase, associated with Helicobacter pylori.

ICD codes

Dosage Regimen

Tablets

Individual. For oral administration, a single dose for adults and children over 10 years of age (weighing more than 40 kg) is 250-500 mg, in severe cases of the disease – up to 1 g. For children aged 5-10 years, a single dose is 250 mg; for children aged 2 to 5 years – 125 mg. The interval between doses is 8 hours. For children weighing less than 40 kg, the daily dose, depending on the indications and clinical situation, can be 20-100 mg/kg in 2-3 doses.

For the treatment of acute uncomplicated gonorrhea – 3 g once (in combination with probenecid). In patients with impaired renal function with a CC of 10-40 ml/min, the interval between doses should be increased to 12 hours; with a CC of less than 10 ml/min, the interval between doses should be 24 hours.

For parenteral use in adults, intramuscularly – 1 g 2 times/day, intravenously (with normal renal function) – 2-12 g/day. For children, intramuscularly – 50 mg/kg/day, single dose – 500 mg, frequency of administration – 2 times/day; intravenously – 100-200 mg/kg/day. For patients with impaired renal function, the dose and interval between administrations must be adjusted in accordance with CC values.

Adverse Reactions

From the digestive system often – nausea, diarrhea; infrequently – vomiting; rarely – dyspepsia, epigastric pain; very rarely – antibiotic-associated colitis (including pseudomembranous and hemorrhagic colitis), diarrhea with blood, black discoloration of the tongue; frequency unknown – taste change, stomatitis, glossitis.

From the nervous system often – drowsiness, headache; rarely: nervousness, agitation, anxiety, ataxia, behavior change, peripheral neuropathy, restlessness, sleep disorder, depression, paresthesia, tremor, confusion; very rarely – hyperkinesia, dizziness, seizures, hyperesthesia, impairment of vision, smell and tactile sensitivity, hallucinations, aseptic meningitis.

From the cardiovascular system often – tachycardia, phlebitis; rarely – decreased blood pressure; very rarely – QT interval prolongation.

From the liver and biliary tract often – increased serum bilirubin concentration; very rarely – hepatitis, cholestatic jaundice, moderate increase in ALT, AST, ALP, GGT activity, acute liver failure.

From the skin and subcutaneous tissues: often – skin rash; infrequently – urticaria, skin itching; very rarely – photosensitivity, edema of the skin and mucous membranes, toxic epidermal necrolysis (Lyell’s syndrome), Stevens-Johnson syndrome, erythema multiforme, bullous exfoliative dermatitis, acute generalized exanthematous pustulosis and drug rash with eosinophilia and systemic symptoms (DRESS syndrome).

Infectious and parasitic diseases rarely – superinfection (especially in patients with chronic diseases or reduced body resistance); very rarely – candidiasis of the skin and mucous membranes.

From the blood and lymphatic system very rarely – reversible leukopenia (including severe neutropenia and agranulocytosis), reversible thrombocytopenia, hemolytic anemia, increased blood clotting time, increased prothrombin time; frequency unknown – eosinophilia.

From the immune system rarely – serum sickness-like reactions; very rarely – severe allergic reactions, including angioedema, anaphylactic shock, serum sickness and allergic vasculitis; frequency unknown – Jarisch-Herxheimer reaction, allergic acute coronary syndrome (Kounis syndrome).

From the endocrine system rarely – anorexia; very rarely – hypoglycemia, especially in patients with diabetes mellitus.

From the respiratory system rarely – bronchospasm, dyspnea; very rarely – allergic pneumonitis.

From the musculoskeletal system: rarely – arthralgia, myalgia, tendon disorders including tendinitis; very rarely: tendon rupture (may be bilateral and occur 48 hours after starting treatment), muscle weakness, rhabdomyolysis.

From the urinary system rarely – increased serum creatinine concentration; very rarely – interstitial nephritis, crystalluria.

General disorders general weakness; very rarely – increased body temperature.

Contraindications

Infectious mononucleosis, lymphocytic leukemia, severe gastrointestinal infections accompanied by diarrhea or vomiting, respiratory viral infections, allergic diathesis, bronchial asthma, hay fever, hypersensitivity to penicillins and/or cephalosporins.

For use in combination with metronidazole: diseases of the nervous system; hematopoiesis disorders, lymphocytic leukemia, infectious mononucleosis; hypersensitivity to nitroimidazole derivatives.

For use in combination with clavulanic acid: history of liver dysfunction and jaundice associated with the use of amoxicillin in combination with clavulanic acid.

Use in Pregnancy and Lactation

Amoxicillin crosses the placental barrier and is excreted in small amounts in breast milk.

If it is necessary to use amoxicillin during pregnancy, the expected benefit of therapy for the mother and the potential risk to the fetus should be carefully weighed.

Amoxicillin should be used with caution during lactation (breastfeeding).

Use in Hepatic Impairment

Amoxicillin in combination with metronidazole should not be used for liver diseases.

Use in Renal Impairment

In patients with impaired renal function, the dose and interval between administrations must be adjusted in accordance with CC values.

Pediatric Use

Use in children is possible according to the dosage regimen.

Amoxicillin in combination with metronidazole is not recommended for use in patients under 18 years of age.

Special Precautions

Use with caution in patients prone to allergic reactions.

Amoxicillin in combination with metronidazole is not recommended for use in patients under 18 years of age; should not be used for liver diseases.

Against the background of combination therapy with metronidazole, alcohol consumption is not recommended.

Drug Interactions

Amoxicillin may reduce the effectiveness of oral contraceptives.

With the simultaneous use of amoxicillin with bactericidal antibiotics (including aminoglycosides, cephalosporins, cycloserine, vancomycin, rifampicin), synergy is manifested; with bacteriostatic antibiotics (including macrolides, chloramphenicol, lincosamides, tetracyclines, sulfonamides) – antagonism.

Amoxicillin enhances the effect of indirect anticoagulants by suppressing the intestinal microflora, reduces the synthesis of vitamin K and the prothrombin index.

Amoxicillin reduces the effect of drugs in the metabolism of which PABA is formed.

Probenecid, diuretics, allopurinol, phenylbutazone, NSAIDs reduce the tubular secretion of amoxicillin, which may be accompanied by an increase in its concentration in the blood plasma.

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

With the combined use of amoxicillin and clavulanic acid, the pharmacokinetics of both components do not change.

Storage Conditions

Store at 2°C (36°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.