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Amoxicillin is a semi-synthetic antibiotic of the III generation penicillin group. Possesses bactericidal action, has a wide spectrum of action. Violates the synthesis of peptidoglycan (the reference polymer of cell steaks) during the period of division and growth, causes lysis of bacteria.
Active against aerobic gram-positive microorganisms: Staphylococcusspp. (with the exception of strains producing penicillinase). Streptococcusspp. and aerobic gram-negative microorganisms: Neisseria gonorrhoeae, Neisseria meningitidis, Escherichia coli, Shigella spp. Salmonella spp., Klebsiella spp. Penicillinase producing strains are resistant to Amoxicillin. Pharmacocnietna:
Absorption - fast, high (93%), food intake does not affect absorption, does not collapse in the acidic environment of the stomach. When taken orally, at a dose of 250 mg, the maximum concentration in serum is 3.5-5 m kg / ml. The time to reach the maximum concentration after oral administration is 1-2 hours. It has a large volume of distribution: it is found in high concentrations in plasma, sputum, bronchial secretion (in the purulent bronchial secretion is weak), pleural and peritoneal fluid, urine, skin blister contents, tissue easyintestinal mucosa, the female genital organs, the prostate gland, the middle ear fluid (with inflammation), bone, adipose tissue, gall bladder (with normal liver function), and fetal tissues. With an increase in dose of 2 times the concentration also increases by 2 times. Concentration in bile exceeds concentration in plasma 2-4 times. In the amniotic fluid and umbilical cord vessels, amoxicillin concentration is 25-30% of the plasma level of a pregnant woman. It penetrates poorly through the blood-brain barrier, with inflammation of the meninges, the concentration in the cerebrospinal fluid is about 20% of the plasma level. Communication with plasma proteins - 17%.
Partially metabolized to form inactive metabolites. The elimination half-life is 1-1.5 hours. Excreted at 50-70% by the kidneys unchanged (by canalicular secretion - 80% and glomerular filtration - 20%), by the liver - 10-20%. In small quantities excreted in breast milk. In case of kidney dysfunction (creatinine clearance less than or equal to 15 ml / min), the elimination half-life increases to 8.5 h. Amoxicillin is removed during hemodialysis.
For oral therapy of the following bacterial infections caused by amoxicillin-sensitive gram-positive and gram-negative pathogens:
Upper respiratory tract infections, including infections of the ear, nose, and throat:
Acute otitis media.
Acute sinusitis and bacterial pharyngitis.
Lower respiratory infections:
Exacerbation of chronic bronchitis.
Infections of the lower urinary tract:
Infections of the gastrointestinal tract:
Bacterial enteritis. Combination therapy may be required for infections caused by anaerobic microorganisms.
Endocarditis prophylaxis in patients at risk for endocarditis development - for example, when performing dental procedures.
Hypersensitivity to penicillin.
Simultaneous use with beta-lactam antibiotics, such as cephalosporins, carbopenems (the possibility of cross-allergy).
In children, preterm and newborns.
Acute lymphoblastic leukemia.
Infectious mononucleosis (due to the increased risk of erythematous rash on the skin).
The use of amoxicillin during pregnancy and breastfeeding is possible only if the intended benefit to the mother outweighs the potential risk to the fetus and infant.
The drug is excreted in breast milk and in rare cases it can lead to the development of diarrhea and / or fungal colonization of the mucous membrane in newborns. It is also important to consider the possibility of sensitizing the newborn to beta-lactam antibiotics.
If necessary, the appointment of the drug during lactation should stop breastfeeding.
Inside, before or after meals. Adults and children over 10 years old (weighing more than 40 kg) are prescribed 0.5 g 3 times a day, in case of severe infection, the maximum daily dose may be increased to 6 g. The course of treatment is 5-12 days. In acute uncomplicated gonorrhea, 3 g is administered once. With acute infectious diseases of the gastrointestinal tract and biliary tract, with gynecological infectious diseases - 1.5-2 g 3 times a day or 1-1.5 g 4 times a day. When leptospirosis - 0.5-0.75 g 4 times a day for 6-12 days. When Salmonellostane -1.5-2 g 3 times a day for 2-4 weeks. With borreliosis - 0.5-1 g 3 times a day. For the prevention of endocarditis in small surgical interventions for adults - 3-4 g for 1 hour before the procedure. If necessary, appoint a repeated dose after 8-9 hours. In children, reduce the dose in two. In patients with impaired renal function with creatinine clarence of 15–40 ml / min, the interval between doses is increased to 12 hours, with creatinine clearance below 10 ml / min, the dose is reduced by 15-20%, with anuria - the maximum dose of 2 g / day.
Allergic reactions: possible urticaria, skin flushing, erythematous rash, angioedema, rhinitis, conjunctivitis, rarely - fever, arthralgia, eosinophilia, exfoliative dermatitis, exudative erythema multiforme (including Stevens-Johnson syndrome), reactions similar to serum sickness, in rare cases - anaphylactic shock.
On the part of the digestive system: dysbacteriosis, change in taste, vomiting, nausea, diarrhea, stomatitis, glossitis, moderate increase in the activity of (liver) transaminases, rarely - pseudomembranous enterocolitis.
On the part of the nervous system: agitation, anxiety, insomnia, ataxia, confusion, behavioral changes, deprissia, peripheral neuropathy, headache, dizziness, convulsive reactions.
Laboratory indicators: leukopenia, neutropenia, thrombocytopenic purpura, anemia.
Others: shortness of breath, tachycardia, interstitial nephritis, vaginal candidiasis, superinfection (especially in patients with chronic diseases or low body resistance).
In the course of treatment, it is necessary to monitor the state of the function of the blood-forming organs, liver and kidneys. The development of superinfection is possible due to the growth of microflora insensitive to it, which requires a corresponding change in antibacterial therapy.
When prescribed to patients with sepsis, a bacteriolysis reaction may be possible (the Jarish-Herxheimer reaction) (rarely).
In patients with increased sensitivity to penicillins, allergic cross-reactions with other beta-lactam antibiotics are possible.
In the treatment of mild diarrhea on the background of a course of treatment, antidiarrheal drugs that reduce intestinal motility should be avoided, kaolin or attapulgite-containing antidiarrheal drugs may be used. In severe diarrhea, you should consult a doctor.
The treatment necessarily continues for another 48-72 hours after the disappearance of the clinical signs of the disease.
With the simultaneous use of estrogen-containing oral contraceptives and amoxicillin, if possible, use other or additional methods of contraception.
Combined use is not recommended
Combined use with Allopurinol can lead to the development of allergic skin reactions.
An increase in Digoxin absorption is possible during therapy with Amoxicillin Sandoz.
The combined use of amoxicillin and anticoagulants, such as coumarin, may increase the likelihood of bleeding due to prolonged prothrombin time. When prescribing anticoagulants along with Amoxicillin Sandoz, monitoring of homeostatic indicators is required.
Probenecid inhibits the excretion of amoxicillin through the kidneys, and leads to an increase in the concentration of amoxicillin in the bile and blood.
There is a possibility of antagonism of the action of amoxicillin with the simultaneous administration of bacteriostatic drugs: macrolides, tetracyclines, sulfonamides and chloramphenicol.
The combined use of Methotrexate and amoxicillin may increase the degree of methotrexate toxicity, possibly as a result of competitive inhibition of tubular renal secretion of methotrexate by amoxicillin.
Use with caution
Oral hormonal contraceptives: the use of amoxicillin can lead to a transient decrease in the concentration of estrogen and Progesterone in the blood, and reduce the effectiveness of contraceptives. In this regard, it is recommended to use other non-hormonal methods of contraception at the time of treatment with amoxicillin.
Symptoms: Amoxicillin does not usually cause acute toxic effects, even with the occasional high dose. Overdose can manifest symptoms of gastrointestinal disorders, violation of water and electrolyte balance. In patients with severe renal insufficiency, overdose with large doses of amoxicillin may be accompanied by signs of nephrotoxicity and crystalluria.
Treatment: There is no specific antidote for amoxicillin. Therapy includes the introduction of Activated carbon (indications for gastric lavage, as a rule, no) or symptomatic measures. Special attention should be paid to the water-electrolyte balance. Perhaps the use of hemodialysis.
Store in a dry place protected from light at a temperature not exceeding 30 C. Keep out of the reach of children.