Instructions for Amoxil tablets 250 mg No. 20
Composition
active ingredient: amoxicillin;
1 tablet contains amoxicillin trihydrate, equivalent to amoxicillin – 250 mg or 500 mg;
Excipients: sodium starch glycolate (type A), povidone, calcium stearate.
Dosage form
Pills.
Main physicochemical properties: white tablets with a yellowish tinge, flat-cylindrical with a bevel and a score.
Pharmacotherapeutic group
Antibacterials for systemic use. Beta-lactam antibiotics, penicillins. ATX code J01C A04.
Pharmacological properties
Pharmacodynamics.
Amoxicillin is a semi-synthetic aminopenicillin antibiotic of broad spectrum of action for oral use. It inhibits the synthesis of the bacterial cell wall. It has a broad spectrum of antimicrobial action.
The following types of microorganisms are sensitive to the drug:
gram-positive aerobes: Corinebacterium diphteriae, Enterococcus faecalis, Listeria monocytogenes, Streptococcus agalactiae, Streptococcus bovis, Streptococcus pyogenes;
Gram-negative aerobes: Helicobacter pylori;
anaerobes: Peptostreptococci;
others: Borrelia.
Intermittently sensitive (acquired resistance may complicate treatment): Corinebacterium spp., Enterococcus faecium, Streptococcus pneumoniae, Streptococcus viridans, Escherichia coli, Haemophilus influenzae, Haemophilus parainfluenzae, Moraxella catarrhalis, Proteus mirabilis, Prevotella, Fusobacterium spp.
Resistant species such as: Staphylococcus aureus, Acinetobacter, Citrobacter, Enterobacter, Klebsiella, Legionella, Morganella morganii, Proteus vulgaris, Providencia, Pseudomonas, Serratia, Bacteroides fragilis, Chlamidia, Mycoplasma, Rickettsia.
Pharmacokinetics.
Absorption.
After oral administration, amoxicillin is absorbed in the small intestine quickly and almost completely (85-90%). Food intake has almost no effect on the absorption of the drug. After taking a single dose of 500 mg, the concentration of amoxicillin in the blood plasma was 6-11 mg/l. The maximum concentration of the active substance in the blood plasma is reached after 1-2 hours.
Distribution.
About 20% of amoxicillin binds to plasma proteins. Amoxicillin penetrates the mucous membranes, bone tissue and intraocular fluid, sputum in therapeutically effective concentrations. The concentration of amoxicillin in bile exceeds its concentration in the blood by 2-4 times. Amoxicillin diffuses poorly into the cerebrospinal fluid; however, in inflammation of the meninges (for example, in meningitis), the concentration in the cerebrospinal fluid is approximately 20% of the concentration in the blood plasma.
Metabolism.
Amoxicillin is partially metabolized, most of its metabolites are inactive.
Breeding.
Amoxicillin is excreted mainly by the kidneys. Approximately 60-80% of the dose is eliminated unchanged within 6 hours. The half-life of amoxicillin is 1-1.5 hours. In case of impaired renal function, the half-life of amoxicillin increases and reaches 8.5 hours in anuria.
The half-life of amoxicillin is not altered by impaired liver function.
Indication
Infections of the respiratory system, genitourinary system, digestive tract (including in combination with metronidazole or clarithromycin used to treat diseases associated with Helicobacter pylori), skin and soft tissues caused by microorganisms sensitive to the drug.
Contraindication
Hypersensitivity to any component of the drug and/or to any antibacterial agents of the penicillin group.
History of severe hypersensitivity reactions (including anaphylaxis) associated with the use of other beta-lactam agents (including cephalosporins, carbapenems or monobactams).
Infectious mononucleosis and leukemoid reactions of the lymphatic type.
Interaction with other medicinal products and other types of interactions
Probenecid, phenylbutazone, oxyphenbutazone, and to a lesser extent, acetylsalicylic acid and sulfinpyrazone inhibit the tubular secretion of penicillin drugs, which leads to an increase in the half-life and concentration of amoxicillin in blood plasma.
Drugs with bacteriostatic action (tetracycline antibiotics, macrolides, chloramphenicol) can neutralize the bactericidal effect of amoxicillin. Parallel use of aminoglycosides is possible (synergistic effect).
Not recommended combinations
Allopurinol. Simultaneous use with amoxicillin contributes to the occurrence of allergic skin reactions.
Digoxin. The absorption of digoxin increases, therefore its dose adjustment is necessary.
Disulfiram. Concomitant use with amoxicillin is contraindicated.
Anticoagulants. Concomitant use of amoxicillin and coumarin anticoagulants may prolong bleeding time. Dose adjustment of anticoagulants may be necessary. There have been reports of increased activity of oral anticoagulants in patients receiving amoxicillin.
Methotrexate. The use of amoxicillin with methotrexate leads to an increase in the toxic effect of the latter. Amoxicillin reduces the renal clearance of methotrexate, therefore its serum concentration should be monitored.
Probenecid
Concomitant use of probenecid is not recommended. Probenecid reduces renal tubular secretion of amoxicillin. Concomitant use of probenecid may result in prolonged elevation of amoxicillin blood levels.
Amoxicillin should be used with caution in combination with oral hormonal contraceptives - plasma levels of estrogen and progesterone may temporarily decrease, which may reduce the effectiveness of hormonal contraceptives. Therefore, it is recommended to use additional non-hormonal contraceptives.
Simultaneous administration with antacids reduces the absorption of amoxicillin.
Other types of interactions.
Forced diuresis leads to a decrease in the concentration of amoxicillin in the blood by increasing its elimination.
The occurrence of diarrhea may lead to a decrease in the absorption of other drugs and adversely affect their effectiveness.
Impact on diagnostic laboratory test results: When testing for glucose in urine, the enzymatic glucose oxidase method is recommended. False-positive results are commonly observed when chemical methods are used.
Amoxicillin may reduce the amount of estriol in the urine of pregnant women.
At high concentrations, amoxicillin may reduce serum glycemia. Amoxicillin may interfere with colorimetric protein determination.
Application features
Hypersensitivity reactions. Before initiating therapy with amoxicillin, careful inquiry should be made regarding the patient's history of hypersensitivity reactions to penicillins, cephalosporins, or other allergens. Cross-hypersensitivity and cross-resistance (10-15%) between penicillins and cephalosporins may exist.
Serious and sometimes fatal cases of hypersensitivity (anaphylactoid reactions and severe cutaneous adverse reactions) have been observed in patients receiving penicillin therapy. Hypersensitivity reactions may also progress to Kunis syndrome, a serious allergic reaction that may lead to myocardial infarction (see section 4.8). Such reactions occur more frequently in patients with a known history of severe allergic reactions. Treatment with the drug should be discontinued and appropriate alternative therapy should be instituted. Treatment of symptoms of anaphylactic reactions may be necessary, e.g. immediate administration of adrenaline, steroids (intravenously) and emergency treatment for respiratory failure.
Acute coronary syndrome associated with hypersensitivity reaction (Kounis syndrome). Hypersensitivity reactions have been reported rarely with amoxicillin treatment (acute coronary syndrome associated with hypersensitivity reaction, see section 4.8); appropriate treatment should be given if such reactions occur.
Renal impairment: In patients with renal impairment, the elimination of amoxicillin may be reduced depending on the degree of renal impairment. In severe renal impairment, treatment with amoxicillin should either be discontinued or the dose of amoxicillin should be reduced.
Convulsions: Convulsions may occur in patients with impaired renal function, as well as in those taking high doses of the drug or in those with predisposing factors (e.g., history of epilepsy, tendency to seizures, concomitant treatment for epilepsy, meningitis, or CNS diseases) (see section "Adverse Reactions").
Jarisch-Herxheimer reaction. It should be noted that the Jarisch-Herxheimer reaction (see section 4.8) may occur during treatment of Lyme disease with amoxicillin, which is due to the bactericidal effect of amoxicillin on the spirochete Borrelia burgdorferi, the causative agent of Lyme disease. Patients should be advised that this is a common side effect of antibiotic treatment of Lyme disease; symptoms usually resolve upon recovery.
Crystalluria: Crystalluria (including acute kidney injury) has been reported very rarely in patients with reduced urine output, mainly with parenteral therapy. When using high doses of the drug, sufficient fluid intake is necessary to prevent crystalluria, which may be caused by amoxicillin. The presence of high concentrations of amoxicillin in the urine may cause precipitation in the urinary catheter, so it should be visually inspected at regular intervals (see sections "Adverse Reactions" and "Overdose").
Non-susceptible organisms: Since amoxicillin is not indicated for the treatment of certain types of infections, the drug should only be used when the pathogenic microorganism is identified or when there is reason to believe that the infectious agent is likely to be susceptible to amoxicillin (see section 5.1). This applies in particular to the treatment of patients with urinary tract infections and serious ear, nose and throat infections.
Pseudomembranous colitis. Antibiotic-associated colitis, ranging in severity from mild to life-threatening, has been reported with virtually all antibacterial agents, including amoxicillin. If severe diarrhea consistent with pseudomembranous colitis (mostly caused by Clostridium difficile) occurs, discontinuation of the drug and appropriate supportive measures should be considered. Medicinal products that inhibit peristalsis are contraindicated in this setting.
Necessary measures should also be taken in the event of hemorrhagic colitis or hypersensitivity reactions.
Patients with severe gastrointestinal disorders accompanied by diarrhea and vomiting should not use oral forms of amoxicillin due to the risk of reduced absorption.
Drug-induced enterocolitis syndrome (DIES) has been reported, mainly in children receiving amoxicillin (see section 4.8). Drug-induced enterocolitis syndrome is an allergic reaction characterized by prolonged vomiting (1–4 hours after drug administration) in the absence of allergic skin or respiratory symptoms. Additional symptoms may include abdominal pain, diarrhea, hypotension, or leukocytosis with neutrophilia. Severe cases have been reported, including progression to shock.
In children, amoxicillin can discolor tooth enamel, so the patient must strictly adhere to oral hygiene.
Infectious mononucleosis: Exanthema, not due to hypersensitivity to penicillins, has been frequently reported in patients with infectious mononucleosis or leukemoid reactions of the lymphatic type. Therefore, the drug should not be used in patients with mononucleosis.
Amoxicillin is not recommended for the treatment of patients with acute lymphoblastic leukemia or infectious mononucleosis due to an increased risk of erythematous skin rashes.
During high-dose therapy, blood counts should be monitored regularly.
Skin reactions: The occurrence of generalized erythema with fever and pustules at the beginning of treatment may indicate the development of acute generalized eczematous pustulosis, which requires discontinuation of amoxicillin therapy. Further use of amoxicillin is contraindicated.
Amoxicillin can cause severe skin reactions such as toxic epidermal necrolysis, Stevens-Johnson syndrome and drug reaction with eosinophilia and systemic symptoms (DRESS). If severe skin reactions occur, amoxicillin should be discontinued and appropriate treatment and/or measures should be taken.
During long-term treatment, it is recommended to periodically assess the function of body systems, including the kidneys, liver, and hematopoietic system.
During high-dose therapy, blood counts should be monitored regularly. Elevated liver enzymes and changes in blood cell counts have been reported (see section 4.8).
Anticoagulants
Prolongation of prothrombin time has been reported rarely in patients receiving amoxicillin.
Appropriate monitoring is necessary when anticoagulants are used concurrently.
To maintain the desired level of blood clotting, dose adjustment of oral anticoagulants may be necessary (see sections “Interaction with other medicinal products and other types of interactions” and “Adverse reactions”).
When using amoxicillin as part of combination therapy for the eradication of Helicobacter pylori, the instructions for medical use of other medicines for combination therapy should be consulted.
The drug Amoxil®, tablets, contains sodium (in a 250 mg tablet, the sodium content is from 3.311 mg/tab to 4.967 mg/tab; in a 500 mg tablet - from 6.622 mg/tab to 9.933 mg/tab), which should be taken into account when treating patients who are on a sodium-controlled diet.
Use during pregnancy or breastfeeding
Amoxicillin crosses the placental barrier; its concentration in the fetal plasma is approximately 25-30% of the concentration in the maternal plasma. No teratogenic effect of amoxicillin has been identified.
Limited data on the use of amoxicillin during pregnancy indicate no adverse effects on the fetus/newborn. If it is necessary to prescribe amoxicillin during pregnancy, a careful assessment of the potential risk to the fetus and the expected benefit to the woman should be made.
Amoxicillin is excreted in small amounts in breast milk, so the risk of hypersensitivity in the child during breastfeeding cannot be excluded. The use of the drug during this period is possible only if the expected benefit to the woman outweighs the potential risk to the child. Breastfeeding should be discontinued if the newborn develops gastrointestinal disorders (diarrhea, candidiasis) or skin rashes.
Fertility: There are no data on the effect of amoxicillin on fertility in humans. In animal reproductive toxicity studies, no effect on fertility was observed.
The ability to influence the reaction speed when driving or working with other mechanisms
Until the individual reaction to the drug is determined (dizziness, convulsions may occur), it is recommended to exercise caution when driving or working with complex mechanisms.
Method of administration and doses
The dosage range for Amoxil® is very wide. The doctor sets the dose, frequency of administration and duration of treatment individually.
Adults and children weighing more than 40 kg should take 250 mg to 500 mg of Amoxil® three times a day or 500 mg to 1000 mg twice a day. For sinusitis, pneumonia and other severe infections, 500 mg to 1000 mg should be taken three times a day. The daily dose can be increased to a maximum of 6 g.
Children weighing less than 40 kg should generally receive 40-90 mg/kg/day of Amoxil® daily in three divided doses or 25 mg to 45 mg/kg/day in two divided doses. The maximum daily dose for children is 100 mg/kg of body weight.
In case of mild to moderate infections, the drug should be taken for 5-7 days. However, in case of infections caused by streptococcus, the duration of treatment should be at least 10 days.
When treating chronic diseases, local infectious lesions, and severe infections, the dosage of the drug should be determined taking into account the clinical picture of the disease.
The drug should be continued for 48 hours after the symptoms of the disease disappear.
Amoxil® can be used in patients with renal insufficiency. In severe renal insufficiency (creatinine clearance < 10 ml/min, i.e. 0.16 ml/s), the dosing intervals of the drug should be 12-24 hours, and the dose of the drug should be reduced by 15-50%.
In case of impaired liver function, dosage adjustment is not required.
Amoxil® can be taken regardless of meals. The tablet should be swallowed with liquid. During treatment with Amoxil®, the patient is advised to drink more fluids than usual.
Children
Children under 5 years of age are prescribed other dosage forms of amoxicillin.
Overdose
Symptoms: digestive tract dysfunction – nausea, vomiting, diarrhea, which may result in a violation of water and electrolyte balance.
Cases of crystalluria, sometimes leading to renal failure, have been reported. Convulsions may occur in patients with impaired renal function or in patients receiving high doses of the drug.
Treatment: induce vomiting or perform gastric lavage, followed by administration of activated charcoal and an osmotic laxative. Maintain fluid and electrolyte balance. Amoxicillin can be removed from the bloodstream by hemodialysis. No specific antidote is known.
Side effects
The most commonly reported adverse reactions were diarrhea, nausea, and vomiting.
Adverse reactions obtained during clinical trials and post-marketing surveillance of amoxicillin are presented below according to the MEdDRA classification.
Adverse reactions are classified according to their frequency of occurrence:
× very common (≥1/10),
× common (≥1/100 and <1/10),
× uncommon (≥1/1000 and <1/100),
× rare (≥1/10,000 and <1/1,000),
× very rare (<1/10,000),
× frequency unknown (cannot be estimated from the available data).
Infections and infestations: very rare - prolonged or repeated use of the drug may lead to the development of superinfections and overgrowth of non-susceptible microorganisms or yeasts, causing candidiasis of the skin and mucous membranes.
From the blood and lymphatic system: very rarely - eosinophilia, hemolytic anemia, leukopenia (including severe neutropenia and agranulocytosis), reversible thrombocytopenia, pancytopenia, myelosuppression, granulocytopenia, increased bleeding time and prothrombin index. These manifestations are reversible upon discontinuation of treatment (see section "Special instructions").
On the part of the immune system: as for all antibiotics - very rarely: severe allergic reactions, including anaphylaxis, angioedema, laryngeal edema, serum sickness, allergic vasculitis, anaphylactic shock, enanthema, hyperemia, fever; frequency unknown - Jarisch-Herxheimer reaction (see section "Special instructions"). If an anaphylactic reaction develops, appropriate therapy should be initiated immediately.
Nervous system: very rarely - insomnia, loss of consciousness, headache, hyperkinesia, confusion, hyperactivity, dizziness, convulsions (in patients with epilepsy and meningitis, in case of impaired renal function, when using high doses of amoxicillin); frequency unknown - aseptic meningitis. These effects occur more often in patients using very high doses.
Cardiac disorders: frequency unknown – Kunis syndrome (acute coronary syndrome associated with a hypersensitivity reaction).
On the part of the hepatobiliary system: very rarely - hepatitis, cholestatic jaundice, moderate and short-term increase in liver enzymes (AST, ALT).
Skin and subcutaneous tissue disorders: *often - skin rash; *uncommon - urticaria, pruritus; very rarely - erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis, bullous and exfoliative dermatitis and drug reaction with eosinophilia and systemic symptoms (DRESS syndrome), acute generalized exanthematous pustulosis. Sudden onset of urticaria indicates an allergic reaction to amoxicillin and requires immediate discontinuation of therapy. Linear immunoglobulin A (IgA) disease - frequency unknown.
Renal and urinary system: acute interstitial nephritis, crystalluria (including acute kidney injury) (see sections "Special warnings and precautions for use" and "Overdose"). In case of severe side effects, the drug should be discontinued.
Others: general weakness.
* the frequency of these adverse reactions was obtained from an evaluation of clinical trial data involving a total of approximately 6,000 adults and children taking amoxicillin.
# children have superficial tooth discoloration. Proper dental care can help prevent tooth discoloration, as plaque is usually removed by brushing your teeth.
Expiration date
4 years.
Storage conditions
Store in original packaging, at a temperature not exceeding 25 ° C. Keep out of the reach of children.
Packaging
10 tablets in a blister, 2 blisters in a pack.
Vacation category
According to the recipe.
Producer
PJSC "Kyivmedpreparat".
Address
Ukraine, 01032, Kyiv, Saksaganskoho St., 139.
