2010/09/20

Amoksiklav

Composition, structure and packing

Powder for suspension for oral administration from white to yellowish-white, homogeneous preparation of suspensions, from almost white to yellowish, homogeneous.
5 ml of a suspension prepared. amoxicillin (in the form of trihydrate) 125 mg;
Clavulanic acid (in the form of potassium clavulanate) 31.25 mg.

Excipients: anhydrous citric acid, sodium citrate anhydrous, sodium benzoate, microcrystalline cellulose, sodium karmelloza, Xanthan gum, colloidal silicon dioxide, silicon dioxide, sodium saccharin, mannitol, flavorings (strawberry, wild cherry, lemon).

Powder for suspension for oral administration from white to yellowish-white, homogeneous preparation of suspensions, from almost white to yellowish, homogeneous.
5 ml of a suspension prepared. amoxicillin (in the form of trihydrate) 250 mg;
Clavulanic acid (in the form of potassium clavulanate) 62.5 mg.

Excipients: anhydrous citric acid, sodium citrate anhydrous, sodium benzoate, microcrystalline cellulose, sodium karmelloza, Xanthan gum, colloidal silicon dioxide, silicon dioxide, sodium saccharin, mannitol, flavorings (strawberry, wild cherry, lemon).

Powder for suspension for oral administration from white to yellowish-white, homogeneous preparation of suspensions, from almost white to yellowish, homogeneous.
5 ml of a suspension prepared. amoxicillin (in the form of trihydrate) 400 mg;
Clavulanic acid (in the form of potassium salt) 57 mg.

Excipients: anhydrous citric acid, sodium citrate, anhydrous, microcrystalline cellulose, sodium karmelloza, Xanthan gum, colloidal silicon dioxide, silicon dioxide, sodium saccharin, mannitol, flavorings (strawberry, wild cherry, lemon).

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

Pharmacological action

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

Pharmacokinetics

The main pharmacokinetic parameters of amoxicillin and clavulanic acid are similar. Amoxicillin and Clavulanic acid in combination do not affect each other.

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 plasma levels are reached 1 h after drug administration and up (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 (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. Putting Amoxicillin appears 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 is 1-1.5 h.

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, including human and animal bites;
infection of bone and connective tissue;
biliary tract infections (cholecystitis, cholangitis);
odontogenic infection.

Dosage regimen

Daily dose of suspensions 125 mg + 31.25 mg / 5 ml and 250 mg + 62.5 mg / 5 ml (to facilitate the proper dosage for each package suspension 125 mg + 31.25 mg / 5 ml and 250 mg + 62.5 mg / 5 ml invested scoop size 5 ml).

Babies and children up to 3 months each appoint 30 mg / kg (amoxicillin) per day, divided by 2 divided doses (every 12 hours) for children older than 3 months in moderate infections - 20 mg (amoxicillin) / kg / day, divided into 3 divided doses (every 8 h), in severe infections and respiratory tract infections - 40 mg / kg (amoxicillin) per day, divided into 3 (every 8 h).

Recommended doses of suspensions (125 mg + 31.25 mg / 5 ml and 250 mg + 62.5 mg / 5 ml) determined according to the weight of the child and the severity of infection. Multiplicity reception - 3 times per day. Daily doses of a suspension 400 mg + 75 mg / 5 ml are calculated for 1 kg of body weight, depending on the severity of infection and are 25-45 mg / kg body weight / day (for amoxicillin) divided by 2 divided doses.

To facilitate the proper dosage for each package suspension 400 mg + 75 mg / 5 ml pipette inserted dosage, graded at the same time at 1, 2, 3, 4, 5 ml and 4 equal parts. Recommended doses of suspension 400 mg + 75 mg / 5 ml depending on the weight of the child and the severity of infection. Multiplicity reception - 2 times / day. The exact daily dose calculated on the basis of body weight of the child, not his age. The maximum daily dose of amoxicillin for adults is 6 grams, for children - 45 mg / kg body weight.

The maximum daily dose of clavulanic acid (in the form of potassium salt) for adults is 600 mg for children - 10 mg / kg body weight. In patients with renal failure severe (CC <10 ml / min) dose should be reduced or increased the interval between doses (in anuria of 48 hours or more). 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. Terms preparation of the suspension Powder for suspension 125 mg + 31.25 mg / 5 ml: shake flask, add 86 ml (up to the mark) of water in two portions, each time tossing well to completely dissolve the powder.

Powder for suspension 250 mg + 62.5 mg / 5 ml: shake bottle, add 85 ml (up to the mark) of water in two portions, each time tossing well to completely dissolve the powder.

Powder for suspension 400 mg + 57 mg / 5 ml: shake bottle, add water to the amount indicated on the label and presented in the table (up to the mark) in two portions, each time tossing well to completely dissolve the powder.

Side effect

Side effects in most cases, weakly expressed and transient.

On the part of the digestive system: loss of appetite, nausea, vomiting, diarrhea, rarely - transient increase in liver enzymes (ALT, AST), liver problems, and in rare cases - cholestatic jaundice, hepatitis, pseudomembranous colitis. Allergic reactions: erythematous rash, itching, rash, rarely - exudative erythema multiforme, angioedema, anaphylactic shock, in rare cases - exfoliative dermatitis, Stevens-Johnson syndrome.

Other: rarely - the development of superinfection (including candidiasis), reversible increase of prothrombin time (or combined with anticoagulants).

Contraindications
hypersensitivity to amoxicillin or clavulanic acid;
indication of a history of cholestatic jaundice in or dysfunction of the liver caused by the intake of amoxicillin / clavulanic acid.

Be wary prescribers for patients with known hypersensitivity to cephalosporin antibiotics series, with pseudomembranous colitis in history, with hepatic failure, severe renal dysfunction.

Due to the fact that a large number of patients with infectious mononucleosis and lymphocytic leukemia treated with ampicillin, observed the appearance of erythematous rash, antibiotics of ampicillin for these patients is not recommended.

Pregnancy and lactation

Amoxiclav 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.

Application for violations of liver function

Be wary prescribers for patients with hepatic failure.

Application for violations of renal function

In patients with renal insufficiency (CC 10-30 ml / min) dose should be reduced or increased interval between doses (in anuria of 48 hours or more).

Cautions

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 increasing the intervals between dosing.

To reduce the risk of adverse reactions from the gastrointestinal tract should take the drug during meals.

In applying Amoksiklava in high doses can be false-positive reaction in determining the level of glucose in urine using Benedict's reagent or solution Felling (recommend the use of enzymatic reactions with glucose oxidase). Avoid the simultaneous appointment of disulfiram.

Effects on ability to drive vehicles and management mechanisms

No data.

Overdose

Do not have reports of fatal or life-threatening side effects due to overdosing.

Symptoms: abdominal pain, diarrhea, vomiting, possibly as agitation, insomnia, dizziness and in rare 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 should be under medical supervision, if necessary, carry out palliative care. Effective hemodialysis.

Drug Interactions

With simultaneous application Amoksiklava with antacids, glucosamine, laxatives, aminoglycoside absorption is slowed down, with ascorbic acid - increases. Diuretics, allopurinol, fenilbutazon, NSAIDs and other drugs that block tubular secretion, increase the concentration of amoxicillin (Clavulanic acid is derived mainly by glomerular filtration).

With simultaneous application Amoksiklava and indirect anticoagulants indicate an increase in prothrombin time. Therefore, this combination is assigned with caution.

With simultaneous application Amoxiclav enhances the toxicity of methotrexate.

With simultaneous application Amoksiklava with allopurinol increases the risk of exanthema.

The combination of amoxicillin and rifampicin antagonistic (the mutual weakening of the antibacterial action). Amoxiclav should not be used simultaneously with bacteriostatic antibiotics (macrolides, tetracyclines), sulphonamide due to a possible reduction in effectiveness Amoksiklava.

With simultaneous application Amoxiclav reduces the effectiveness of oral contraceptives. Probenecid reduces the excretion of amoxicillin, increasing its serum concentration.

Terms and Conditions of storage

List B. The drug should be kept dry and away from children at or above 25 ° C.

Shelf life - 2 years. After preparing a suspension for oral administration should be stored at a temperature of 2 ° to 8 ° C in a tightly sealed bottle and use within 7 days.