Amoxicillin Dispertab, 500 mg 20 pcs

Pharmacotherapeutic group: Antibiotic, semisynthetic penicillin

Pharmacological action

Antibiotic of the group of semisynthetic penicillins of broad spectrum. It is 4-hydroxyl analogue of ampicillin. It has bactericidal action. It is active against aerobic gram-positive bacteria: Staphylococcus spp. (except for penicillinase-producing strains), Streptococcus spp.; aerobic gram-negative bacteria: Neisseria gonorrhoeae, Neisseria meningitidis, Escherichia coli, Shigella spp., Salmonella spp., Klebsiella spp.

Amoxicillin is resistant to microorganisms producing penicillinase.

In combination with metronidazole it shows activity against Helicobacter pylori. Amoxicillin is believed to inhibit the development of resistance of Helicobacter pylori to metronidazole.

Cross-resistance exists between amoxicillin and ampicillin.

The spectrum of antibacterial activity is broadened with the simultaneous use of amoxicillin and the beta-lactamase inhibitor clavulanic acid. In this combination amoxicillin activity 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

In oral administration amoxicillin is quickly and completely absorbed from the gastrointestinal tract, it is not destroyed in the acidic environment of the stomach. C_max of amoxicillin in blood plasma is reached after 1-2 hours. If the dose is increased by 2 times, the concentration also increases by 2 times. In the presence of food in the stomach it does not reduce total absorption. Similar concentrations of amoxicillin are achieved in the blood when administered intravenously, intramuscularly and by oral administration.

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

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

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

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

In cases of renal failure, T_1/2 may be 7-20 h.

In small amounts amoxicillin penetrates through the HEB in inflammation of the soft medulla.

Amoxicillin is eliminated by hemodialysis.

Indications

Infections caused by microorganisms sensitive to the drug, including:

Active ingredient

Composition

Composition per tablet:

The active ingredient:

Amoxicillin trihydrate – 574,000 mg (in terms of amoxicillin) – 50,000 mg

Excipients:

Hyprolose – 49,000 mg,

Crospovidone XL-10 – 33,600 mg,

Sodium stearyl fumarate – 10,500 mg,

How to take, the dosage

Individual. For oral administration a single dose for adults and children over 10 years old (with body weight over 40 kg) is 250-500 mg, in severe course 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 with body weight less than 40 kg a daily dose, depending on indications and clinical situation, may be 20-100 mg/kg in 2-3 doses.

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

In parenteral use in adults 1 g 2 times per day in m/v, 2-12 g/day in iv (with normal renal function). In children intravenously – 50 mg/kg/day, single dose – 500 mg, frequency of administration – 2 times/day; intravenously – 100-200 mg/kg/day. In patients with impaired renal function, the dose and interval between injections should be adjusted according to the CK values.

Interaction

Probenecid

The simultaneous use of amoxicillin and probenecid is not recommended. Probenecid reduces the secretion of amoxicillin in the renal tubules. Concomitant use of probenecid may lead to increased concentration of amoxicillin in the blood.

Allopurinol

The concomitant use of allopurinol during treatment with amoxicillin increases the possibility of allergic skin reactions.

Tetracyclines

Tetracyclines and other bacteriostatic antibiotics may affect the bactericidal effect of amoxicillin.

Peroral anticoagulants

Peroral anticoagulants and penicillin-based antibiotics are often used together in practice, with no reports of interaction. However, the literature describes cases of increased international normalized ratio in patients treated with acenocoumarol or warfarin against the background of a prescribed course of amoxicillin. If concomitant administration of drugs is necessary, prothrombin time or international normalized ratio should be carefully monitored at the beginning of treatment and after discontinuation of amoxicillin treatment. In addition, it may be necessary to adjust the dose of oral anticoagulants.

Methotrexate

Penicillin antibiotics may decrease methotrexate excretion, which may be accompanied by increased toxicity.

Special Instructions

Hypersensitivity reactions

Before starting treatment with amoxicillin, attention should be paid to the presence of hypersensitivity reactions to penicillins, cephalosporins or other beta-lactam antibiotics in the anamnesis (see sections “Contraindications, side effects”. Contraindications and side effects).

Serious and sometimes fatal hypersensitivity reactions (including anaphylactic reactions and severe skin reactions) have been reported in patients treated with penicillin. The development of these reactions is more likely in people with a history of hypersensitivity to penicillins and in individuals with atopy. In case of allergic reactions the treatment with amoxicillin should be discontinued and an appropriate alternative treatment should be prescribed.

Acute coronary syndrome associated with hypersensitivity (Coneys syndrome)

In rare cases, hypersensitivity reactions (acute coronary syndrome associated with hypersensitivity) have been reported during treatment with amoxicillin. If this reaction occurs, amoxicillin should be discontinued and appropriate treatment should be prescribed.

Nonsensitive microorganisms

In some types of infections before prescribing amoxicillin it is necessary to previously identify the causative agent and its sensitivity to the drug, or to make sure that it is likely that the pathogen is treatable with amoxicillin. This includes patients with urinary tract infections and severe infections of the ear, nose, and throat.

Convulsions

Convulsions may occur in patients with renal failure, in patients receiving high doses of the drug, as well as in patients with predisposing factors – the presence of seizures in the history, treatment of epilepsy or meningitis, etc.

Convulsions may occur in patients with renal insufficiency, in patients receiving high doses of the drug and in patients with predisposing factors – the presence of seizures in the anamnesis, treatment of epilepsy or meningitis, etc. (see section “Side effects”).

Renal failure

In patients with renal failure, the dose should be adjusted according to the degree of renal failure (see section on Dosage and administration).

Skin reactions

The occurrence of generalized erythema with fever accompanied by pustules in the initial phase of treatment may be a symptom of OGEP (see section “Side effects”). In this case, the use of amoxicillin should be discontinued, and its subsequent use will be contraindicated in all situations.

The use of amoxicillin by patients with suspected infectious mononucleosis should be avoided, since a rash (exanthema) associated with the use of amoxicillin in this disease may occur.

Jarisch-Herxheimer reaction

Jarisch-Herxheimer reaction has been observed after using amoxicillin in patients with Lyme disease. This reaction is associated with the bactericidal effect of amoxicillin on Lyme disease pathogens, spirochaetes Borrelia burgdorferi. Patients should be explained that this reaction is a common side effect of Lyme disease treatment with antibiotics and usually goes away on its own.

Excessive growth of insensitive microorganisms

Long-term use of the drug can sometimes lead to excessive growth of microorganisms insensitive to amoxicillin (superinfection).

With almost all antibiotic drugs, it is possible to develop colitis associated with antibiotic use. Its severity can range from mild to severe (life-threatening). Therefore, it is important to consider the possibility of this diagnosis in patients who develop diarrhea during or after the use of antibiotics. If diarrhea develops, the patient should immediately stop taking amoxicillin, consult a physician and begin appropriate treatment. Drugs that inhibit peristalsis are contraindicated in this situation.

Duration of treatment

In long-term therapy, periodic monitoring of hematopoietic, renal and hepatic function should be performed. Increased activity of “hepatic” enzymes and changes in the number of blood cells have been reported.

Anticoagulants

In patients receiving amoxicillin rare cases of increase in prothrombin time were reported. When concomitant administration of the drug with anticoagulants the appropriate monitoring should be conducted, and the dose of oral anticoagulants may need to be adjusted to maintain the desired level of clotting (see sections “Interaction with other medicinal products” and “Side effects”).

Crystalluria

Crystalluria was very rarely observed in patients with decreased diuresis, mainly during parenteral therapy. When using high doses of amoxicillin, it is recommended to maintain adequate fluid intake and diuresis to reduce the likelihood of crystalluria associated with the use of amoxicillin. In patients with catheterized bladder, the patency of the catheter should be regularly checked.

Influence on diagnostic studies

The increased levels of amoxicillin in serum and urine may affect some laboratory studies. Because of high concentrations of amoxicillin in the urine, chemical methods often give false-positive results.

The use of enzymatic glucose oxidase tests is recommended when determining glucose in the urine during treatment with amoxicillin.

The use of amoxicillin may affect the results of quantitative determination of estradiol in the urine in pregnant women.

Influence on the ability to drive vehicles, mechanisms

The studies of the effect of amoxicillin on the ability to drive vehicles or operate other mechanisms have not been conducted. However, side effects may occur (e.g., allergic reactions, dizziness, seizures) that affect the ability to drive vehicles or operate other mechanisms.

Synopsis

Contraindications

Hypersensitivity to amoxicillin, other penicillins or any other component of the drug.

A history of severe immediate-type hypersensitivity reactions (e.g., anaphylaxis) to another beta-lactam antibiotic (e.g., cephalosporin, carbapenem or monobactam).

Cautions:

Allergic reactions (including bronchial asthma, polliposis, hypersensitivity to acetylsalicylic acid) in the history, gastrointestinal diseases in the history (especially colitis associated with the use of antibiotics), renal failure, infectious mononucleosis, lympholeukosis, pregnancy, breastfeeding period, prematurity, advanced age.

Side effects

Allergic reactions: urticaria, erythema, Quincke’s edema, rhinitis, conjunctivitis; rarely – fever, joint pain, eosinophilia; in single cases – anaphylactic shock.

Effects associated with chemotherapeutic action: superinfections may develop (especially in patients with chronic diseases or low resistance of the body).

In long-term use in high doses: dizziness, ataxia, confusion, depression, peripheral neuropathies, seizures.

Predominantly when used in combination with metronidazole: nausea, vomiting, anorexia, diarrhea, constipation, epigastric pain, glossitis, stomatitis; rarely – hepatitis, pseudomembranous colitis, allergic reactions (urticaria, angioedema), interstitial nephritis, hematopoiesis disorders.

Predominantly when used in combination with clavulanic acid: cholestatic jaundice, hepatitis; rarely erythema multiforme, toxic epidermal necrolysis, exfoliative dermatitis.

Overdose

Symptoms: gastrointestinal dysfunction – nausea, vomiting, diarrhea; consequence of vomiting and diarrhea may be a violation of water-electrolyte balance.
Amoxicillin-associated crystalluria has been observed, which in some cases may lead to renal failure. In patients with impaired renal function or in patients receiving high doses of the drug, seizures may occur.

Treatment: induce vomiting or gastric lavage followed by oral administration of activated charcoal and osmotic laxatives (sodium sulfate); measures to restore water-electrolyte balance, hemodialysis are used.

Pregnancy use

Pregnancy

The results of animal studies have shown no direct or indirect harmful effects with respect to reproductive toxicity. Limited data on the use of amoxicillin during pregnancy in humans indicate no increased risk of congenital malformations. Amoxicillin may be used during pregnancy if the potential benefit to the mother exceeds the potential risk to the fetus.

Breastfeeding period

Amoxicillin is excreted into the breast milk in small amounts, if necessary, it is possible to use the drug during breastfeeding. A child who is being breastfed may develop diarrhea, sensitization and fungal infection of the mucous membranes and therefore discontinuation of breastfeeding may be required. Amoxicillin should be used during breastfeeding only after evaluation by the treating physician of the benefit/risk ratio.

Similarities