Antibacterial acid-antibacterial broad spectrum of action of the group of semisynthetic penicillins. Inhibits transpeptidase, violates the synthesis of peptidoglycan (the reference protein of the cell wall) during the division and growth, causes lysis of the bacteria. It is active against aerobic Gram-positive microorganisms: Staphylococcus spp, (except for strains producing penicillinase), Streptococcus spp; aerobic and gram-negative bacteria: Neisseria gonorrhoeae, Neisseria meningitidis, Escherichia coli, Shigella spp, Salmonella spp, Klebsiella spp… Microorganisms producing penicillinase, are resistant to the action of proviron libido. Pharmacokinetics. Absorption – a fast, high (93%), food intake has no effect on the absorption is not destroyed in the acid environment of the stomach. When administered as a suspension (or tablets) in a dose of 125 and 250 mg, the maximum concentration – 1.5-3 mcg / ml and 3.5-5 ug / ml, respectively. Time to maximum concentration after receiving peroralnogo 1-2 hours. It has a large volume of distribution – the high concentrations found in plasma, sputum, bronchial secretions (in suppurative bronchial secretions distribution weak), pleural and peritoneal fluid, urine contents skin blisters, lung tissue, intestinal mucosa, female genital organs, prostate gland, liquid middle ear bones, adipose tissue, gallbladder (normal liver), fetal tissues. With increasing doses of 2-fold concentration is also increased by 2 times. The concentration in the bile exceeding the plasma concentration of 2-4 fold. The amniotic fluid and umbilical cord vessels proviron libido concentration – 25-30% of the level determined in the plasma of pregnant women. Poorly penetrates the blood brain barrier, inflammation of the meninges (meningitis) concentrations in the cerebrospinal fluid of about 20% of the level in blood plasma. Connection with the plasma protein-17%. The partially metabolized to inactive metabolites. The half-life of 1-1.5 hours. Displayed 50-70% kidneys unchanged by tubular secretion (80%) and glomerular filtration rate (20%), liver – 10-20%. The small amount is excreted in breast milk. If the kidney function (creatinine clearance less than or equal to 15 ml / min) half-life is increased to 8.5 hours. Amoksitsiyalin removed by hemodialysis.
Indications for use:
Bacterial infections caused by sensitive microflora: respiratory tract infections and LOP-bodies (sinusitis, pharyngitis, tonsillitis, acute otitis media, bronchitis, pneumonia), urogenital system (pyelonephritis, pyelitis, cystitis, urethritis, gonorrhea, endometritis, cervicitis), gastrointestinal intestinal tract (enterocolitis, typhoid fever, cholangitis, cholecystitis), infection of the skin and soft tissues (erysipelas, impetigo, secondarily infected dermatoses), leptospirosis, listeriosis, Lyme disease (borreliosis), dysentery, salmonellosis, salmonellonositelstvo, endocarditis (prophylaxis).
Hypersensitivity (including to other penicillins, cephalosporins, carbapenems), children under 3 years (for a given dosage form). Be wary – allergic diseases (including history), gastrointestinal disease in history (especially colitis associated with the use of antibiotics), kidney failure, severe liver dysfunction, pregnancy, lactation, infectious mononucleosis, lymphatic leukemia.
Pregnancy and lactation
Use of the drug during pregnancy is possible only when the intended benefits to the mother outweighs the potential risk to the fetus. If necessary, the appointment during lactation should stop breastfeeding.
Dosage and administration:
. Inside, before or after meals
for adults and children over 10 years (with a body weight over 40 kg) administered 0.5 g 3 times a day; . in severe infections 0.75-1.0 g 3 times a day
Children aged 5-10 years appoint 0.25 g; 3-5 years 0,125 g 3 times a day; in severe infections 60 mg / kg / day in 3 divided doses (maximum daily dose). . The course of treatment 5-12 days
in acute uncomplicated gonorrhea appoint 3 g single dose; Repeated reception of this dose is recommended in the treatment of women.
In acute infectious diseases of the gastrointestinal tract (paratyphoid fever, typhoid fever), and biliary tract, gynecological infectious diseases of adult 1.5-2 g 3 times a day or 1-1.5 g 4 twice a day.
when grown leptospirosis 0.5-0.75 g 4 times a day for 6-12 days.
in adults salmonellonositelstve 1.5-2 g 3 times daily for 2-4 weeks.
to prevent endocarditis in small surgical interventions for adults 3-4 g for 1 hour before the procedure. If necessary, repeat the dose administered 8-9 hours. In children, the dose is reduced by half.
In patients with impaired renal function at creatinine clearance 15-40 ml / min, the interval between doses increased to 12 hours; with creatinine clearance below 10 ml / min the dose is reduced by 15-50%;when anuria maximum dose of 2 g / day.
Side effects: Allergic reactions: possible urticaria, flushing of the skin, erythema, angioedema, rhinitis, conjunctivitis; rarely – fever, joint pain, eosinophilia, exfoliative dermatitis, erythema poliformnaya, Stivenea-Dzhoneona syndrome; reactions similar to serum sickness; in rare cases – anaphylactic shock. On the part of the gastrointestinal tract: goiter, change in taste, nausea, vomiting, diarrhea, stomatitis, glossitis, hepatic impairment, a moderate increase in activity of “liver” transaminases, pseudomembranous enterocolitis. From the nervous system: excitation , anxiety, insomnia, ataxia, confusion, behavioral changes, depression, peripheral neuropathy, headache, dizziness, convulsive reaction. Laboratory findings: leukopenia, neutropenia, thrombocytopenic purpura, anemia. Other:shortness of breath, tachycardia, interstitial nephritis, vaginal candidiasis , superinfection (especially in patients with chronic diseases or low resistance of the body).
Symptoms include nausea, vomiting, diarrhea, disruption of water and electrolyte balance (as a result of vomiting and diarrhea).
Treatment: gastric lavage, the appointment of activated carbon, saline laxatives, correction fluid and electrolyte balance; hemodialysis.
Interaction with other drugs:
Antacids, glucosamine, laxatives, food, aminoglycosides – slow down and reduce absorption; ascorbic acid increases absorption.
The bactericidal antibiotics (including aminoglycosides, cephalosporins, vancomycin, rifampicin) – a synergistic effect; . bacteriostatic drugs (macrolides, chloramphenicol, lincosamides, tetracyclines, sulfonamides) – antagonistic
Improves the effectiveness of indirect anticoagulants (suppressing the intestinal microflora, reduces the synthesis of vitamin K and prothrombin index); estrogensoderzhaschih reduces the effectiveness of oral contraceptives, medicines, in the process of metabolism that produce para-aminobenzoic acid, ethinyl estradiol – the risk of bleeding “breakthrough”.
Diuretics, allopurinol, oxyphenbutazone, phenylbutazone, nonsteroidal anti-inflammatory drugs, drugs that block tubular secretion – reducing the tubular secretion, increase the concentration .
Allopurinol increases the risk of skin rash.
reduces clearance and increases the toxicity of methotrexate.
enhances the absorption of digoxin.
In exchange treatment is necessary to monitor the state functions of blood, liver and kidneys.
Perhaps the development of superinfection due to growth resistant to proviron libido microflora, which requires a corresponding change in antibiotic therapy.
In the treatment of patients with bacteremia may develop endotoxin shock reaction (Jarisch-Herxheimer) .
in patients with hypersensitivity to penicillin, may be cross-allergic reactions to cephalosporin antibiotics.
in the treatment of mild diarrhea on the background of a course of treatment should be avoided antidiarrhoeal drugs that reduce intestinal motility. In severe diarrhea should consult a specialist.
Treatment continues for sure 48-72 hours after the disappearance of clinical signs of the disease.
In an application estrogensoderjath oral contraceptives and proviron libido should be possible to use other or additional contraceptive methods.
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