2010/09/21

Arlet

Composition, structure and packing

Tablets, film-coated white or almost white, oblong.

1 tab. amoxicillin (in the form of trihydrate) 250 mg Clavulanic acid (in the form of potassium salt) 125 mg.

Excipients: povidone (polyvinylpyrrolidone), talc, starch 1500, calcium stearate, colloidal silicon dioxide (aerosil), microcrystalline cellulose.

The composition of the shell: gipromelloza (oksipropilmetiltsellyuloza), propylene glycol, titanium dioxide, macrogol 4000 (polyethylene 4000).

Tablets, film-coated white or almost white, oblong.

1 tab. amoxicillin (in the form of trihydrate) 500 mg Clavulanic acid (in the form of potassium salt) 125 mg.

Excipients: povidone (polyvinylpyrrolidone), talc, starch 1500, calcium stearate, colloidal silicon dioxide (aerosil), microcrystalline cellulose. The composition of the shell: gipromelloza (oksipropilmetiltsellyuloza), propylene glycol, titanium dioxide, macrogol 4000 (polyethylene 4000).

Tablets, film-coated white or almost white, oblong.

1 tab. amoxicillin (in the form of trihydrate) 875 mg Clavulanic acid (in the form of potassium salt) 125 mg.

Excipients: povidone (polyvinylpyrrolidone), talc, starch 1500, calcium stearate, colloidal silicon dioxide (aerosil), microcrystalline cellulose. The composition of the shell: gipromelloza (oksipropilmetiltsellyuloza), propylene glycol, titanium dioxide, macrogol 4000 (polyethylene 4000).

Clinico-pharmacological group: Antibiotic penicillin group broad-spectrum beta-lactamase inhibitor.

Pharmacological action

Broad-spectrum antibiotic, contains a semisynthetic penicillin, amoxicillin and irreversible inhibitor of β-lactamases clavulanic acid. Clavulanic acid provides a stable inactivated complex with these enzymes and provides stability to the effects of amoxicillin β-lactamase produced by microorganisms. Clavulanic acid, similar to the structure of β-lactam antibiotics, has its own weak antibacterial activity.

The drug has broad spectrum antibacterial action. Active against susceptible to amoxicillin strains, including strains producing β-lactamases: aerobic Gram-positive bacteria - Streptococcus pneumoniae, Streptococcus pyogenes, Streptococcus viridans, Streptococcus bovis, Staphylococcus aureus (except methicillin-resistant strains), Staphylococcus epidermidis (except methicillin-resistant strains ), Staphylococcus saprophyticus, Listeria spp., Enterococcus spp.; aerobic gram-negative bacteria - Bordetella pertussis, Brucella spp., Campylobacter jejuni, Escherichia coli, Gardnerella vaginalis, Haemophilus influenzae, Haemophilus ducreyi, Klebsiella spp., Moraxella catarrhalis, Neisseria gonorrhoeae, Neisseria meningitidis, Pasteurella multocida, Proteus spp., Salmonella spp., Shigella spp., Vibrio cholerae, Yersinia enterocolitica, Helicobacter pylori, Eikenella corrodens; anaerobic Gram-positive bacteria - Peptococcus spp., Peptostreptococcus spp., Clostridium spp., Actinomyces israelii, Fusobacterium spp ., Prevotella spp.; anaerobic Gram-negative bacteria - Bacteroides spp.

Pharmacokinetics

The main pharmacokinetic parameters of amoxicillin and clavulanic acid are similar.

Absorption

After taking the drug inside the two components are well absorbed from the gastrointestinal tract, food intake does not affect the degree of suction. Cmax in plasma obtained 1 h after drug administration and is (depending on dose) for amoxicillin 3-12 ug / ml for clavulanic acid - about 2 ug / ml.

Distribution

Both components are characterized by good volume distribution in body fluids and tissues (including lungs, middle ear, pleural and peritoneal fluid, uterus, ovaries). Amoxycillin penetrates well into synovial fluid, liver, prostate gland, palatine tonsils, muscle, gall bladder, the secret of the paranasal sinuses, saliva, bronchial secretion. Amoxicillin and Clavulanic acid does not penetrate the BBB under nevospalennyh mater.

The active substances penetrate the placenta and in trace concentrations excreted with breast milk. The degree of binding to plasma proteins is low. Metabolism Amoxicillin partially metabolized Clavulanic acid is exposed, apparently, metabolic rate.

Withdrawal

Amoxicillin is displayed by the kidneys virtually unchanged by tubular secretion and glomerular filtration. Clavulanic acid is obtained by glomerular filtration and partly in the form of metabolites. Smaller quantities can be displayed through the intestines and lungs. T1 / 2 of amoxicillin and clavulanic acid - 1-1.5 hours

Pharmacokinetics in special clinical situations

In severe renal insufficiency T1 / 2 increases to 7.5 h for amoxicillin and up to 4.5 h for clavulanic acid. Both components are removed by hemodialysis and small amounts - peritoneal dialysis.

Statement

Treatment of infectious-inflammatory diseases caused by microorganisms sensitive to the drug:
infections of the upper respiratory tract and ENT-organs (including acute and chronic sinusitis, acute and chronic otitis media, retropharyngeal abscess, tonsillitis, pharyngitis);
Infection of lower respiratory tract (including acute bronchitis with bacterial superinfection, chronic bronchitis, pneumonia);
urinary tract infections;
gynecological infections;
infections of skin and soft tissues;
infection of bone and connective tissue;
biliary tract infections (cholecystitis, cholangitis);
odontogenic infection.

Dosage regimen

Adults and children over 12 years (or c-weight 40 kg) with mild to moderate infections or appoint 1 tab. 250/125 mg every 8 hours or 1 tab. 500/125 mg every 12 hours, in severe cases, infection and respiratory infections - 1 pi. 500/125 mg every 8 hours or 1 tab. 875/125 mg every 12 hours

Children under 12 years old with body weight below 40 kg dose was selected individually on the basis of the recommended dosing schemes (for amoxicillin) - 45 mg / kg / day in 2 divided doses or 40 mg / kg / day in 3 divided doses. Optimum dosage forms of the drug for children from 6 to 12 years are tablets 500/125 mg in the appointment of two times a day. The maximum daily dose of clavulanic acid (in the form of potassium salt) is for adults - 600 mg for children - 10 mg / kg body weight. The maximum daily dose of amoxicillin for adults - 6 g, for children - 45 mg / kg body weight. The course of treatment is 5-14 days. The duration of treatment is determined by your doctor.

Treatment should not last more than 14 days without re-medical examination. In odontogenic infections appoint 1 tab. 250/125 mg every 8 h or 1 tab. 500/125 mg every 12 h for 5 days. In renal insufficiency, moderate (CC 10-30 ml / min) appoint 1 tab. 500/125 mg every 12 hours for adults and 15/3.75 mg / kg body weight 2 times / day for children under 12 years. In renal insufficiency, severe (CC <10 ml / min) - 1 tab. 500/125 mg every 24 hours for adults, children under 12 years - 15/3.75 mg / kg of body weight one time per day. When anuria interval between administration of a single dose should be increased to 48 hours or more.

Adults who are on hemodialysis, should appoint a drug in a dose of 1 tablet. 500/125 mg or 2 tab. 250/125 mg every 24 hours to compensate for the reduction of the concentration of amoxicillin and clavulanic acid in the blood serum during dialysis should be added to a dose of the drug during the dialysis session and another dose at the end of the session. Children who are on hemodialysis, should appoint a drug in a dose of 15/3.75 mg / kg of body weight one time per day. To compensate for the reduction of the concentration of amoxicillin and clavulanic acid in the blood during dialysis should additionally take a dose before the dialysis session and another dose after the dialysis session.

Side effect
On the part of the digestive system: loss of appetite, nausea, vomiting, diarrhea, rarely - liver problems, increased activity of ALT and AST, and in rare cases - cholestatic jaundice, hepatitis, pseudomembranous colitis.
From the side of the central nervous system: dizziness, headache, reversible hyperactivity, and convulsions.
On the part of the hemopoietic system: a reversible increase in prothrombin time, leukopenia, reversible agranulocytosis and hemolytic anemia.
On the part of the genitourinary system: interstitial nephritis, crystalluria. Allergic reactions: itching, rash, erythematous rash, rarely - exudative erythema multiforme, angioedema, anaphylactic shock, in rare cases - exfoliative dermatitis, Stevens-Johnson syndrome. Other: the development of superinfection (including candidiasis).

Contraindications
infectious mononucleosis (also in the appearance of korepodobnoy rash);
Children under 3 years;
increased sensitivity to antibiotics of penicillin, cephalosporins;
hypersensitivity to amoxicillin or clavulanic acid.

Be wary prescribers for patients with liver failure severe, gastrointestinal diseases (including colitis associated with antibiotic penicillin group in history), chronic renal insufficiency.

Pregnancy and lactation

The drug prescribed with caution during pregnancy and lactation (breastfeeding). Arlette can be used during pregnancy if the expected benefit to the mother outweighs the potential risk to the fetus. Amoxicillin and Clavulanic acid in small amounts are excreted with breast milk, so if you need to appoint during lactation must decide whether termination of breastfeeding.

Application for violations of liver function

The drug should be considered in patients with otsrozhnostyu with hepatic insufficiency.

Application for violations of renal function

Prapart should be cautious to use in violation of the kidney. In renal insufficiency, moderate (CC 10-30 ml / min) appoint 1 tab. 500/125 mg every 12 hours for adults and 15/3.75 mg / kg body weight 2 times / sutdetyam to 12 years, with renal failure, severe (CC <10 ml / min) - 1 tab. 500/125 mg every 24 hours for adults, children under 12 years - 15/3.75 mg / kg of body weight one time per day. When anuria Interval doses should be increased to 48 hours or more.

Adults located at gemodialeze should appoint a drug in a dose of 1 tablet. 500/125 mg or 2 tab. 250/125 mg every 24 hours to compensate for the reduction of the concentration of amoxicillin and klavuronovoy acid in the blood serum during dialysis should be further understood one dose of the drug during the dialysis session and another dose at the end of the session.

Children under 12 years located on gemodialeze should appoint a drug in a dose of 15/3.75 mg / kg of body weight one time per day. To compensate for the reduction of the concentration of amoxicillin and klavuronovoy acid in the blood serum during dialysis should be further understood one dose prior to dialysis session and another dose after the dialysis session.

Cautions

With careful use the drug in patients with impaired liver function during treatment regularly monitor liver function.

In exchange therapy should be monitored blood function, liver and kidneys. In patients with severely impaired renal function requires adequate correction of dosing regimen or increased intervals between doses of the drug. To reduce the risk of adverse reactions from the gastrointestinal tract should take the drug with food.

Because the tablets of the drug combination 250 mg/125 mg and 500 mg/125 mg contain the same amount of clavulanic acid (125 mg), then 2 tablets of 250 mg/125 mg are not equivalent to 1 tablet 500 mg/125 mg.

High concentrations of amoxicillin give false-positive reaction in the determination of glucose in urine using Benedict's reagent or solution Felling (recommend the use of enzymatic reaction with glycosidase).

Effects on ability to drive vehicles and management mechanisms

The drug at recommended doses does not affect the ability to drive transport and management of complex mechanisms.

Overdose

Symptoms: abdominal pain, diarrhea, vomiting, possibly as agitation, insomnia, dizziness, and in some cases - seizures.

Treatment: In the case of the recent treatment (less than 4 hours) is necessary to gastric lavage and activated charcoal to appoint to reduce the absorption of the drug, the patient must remain under medical supervision, if necessary, carry out palliative care. Effective hemodialysis.

Drug Interactions

With simultaneous application of Arlette enhances the toxicity of methotrexate. With simultaneous application of Arleta with allopurinol increases the risk of exanthema. With simultaneous application of Arleta with antacids, glucosamine, laxatives, aminoglycoside absorption slows down, with ascorbic acid - increases.

With simultaneous application of Arleta with bactericidal antibiotics (including aminoglycosides, tsefalosproriny, cycloserine, vancomycin, rifampicin) shows synergistic effects; with antibiotics with bacteriostatic mechanism of action (including macrolides, chloramphenicol, Lincosamides, tetracyclines, sulfonamides) - antagonism.

With simultaneous application of Arlette increases the efficiency of the indirect anticoagulants due to suppression of intestinal microflora, reducing the synthesis of vitamin K and a decrease in prothrombin index. In the appointment of this combination should be dynamic control of blood tests.

With simultaneous application of Arlette reduces the effectiveness of oral contraceptives.

In case of simultaneous appointment of Arleta with drugs in the process of metabolism which is formed of para-aminobenzoic acid, ethinylestradiol increased the risk of breakthrough bleeding. Diuretics, allopurinol, fenilbutazon, NSAIDs and other drugs that block tubular secretion, increase the concentration of amoxicillin (Clavulanic acid is derived mainly by glomerular filtration).

Terms and Conditions of storage

The drug should be stored in a dry place protected from light, away from children at or above 25 ° C. Shelf life - 2 years. The drug should not be used after the expiration date.