AMOKSIKLAV (Powder for solution)

Active material: Amoksiцillin, Clavulanic acid
When ATH: J01CR02
CCF: Antibiotics penicillin with a broad-spectrum beta-lactamase inhibitor
ICD-10 codes (testimony): A46, A54, A57, H66, J00, J01, J02, J03, J04, J15, J20, J31, J32, J35.0, J37, J42, J47, J85, J86, J90, K81.0, K81.1, K83.0, L01, L02, L03, L08.0, L30.3, M00, M86, N10, N11, N15.1, N30, N34, N41, N70, N71, N72, N73.0, O08.0, O85, T14.0, T79.3, Z29.2
When CSF: 06.01.02.04.02
Manufacturer: LEK d.d. (Slovenia)

Pharmaceutical form, composition and packaging

Powder for solution for i / v administration white to yellowish-white.

Bottles (5) – packs cardboard.

Powder for solution for i / v administration white to yellowish-white.

Bottles (5) – packs cardboard.

Pharmacological action

Broad-spectrum antibiotic; It contains a semisynthetic penicillin, amoxicillin and the β-lactamase inhibitor clavulanic acid. Clavulanic acid forms a stable inactivated complex with β-lactamases and provides stability of amoxicillin to their effects.

Clavulanic acid, structurally similar β-lactam antibiotics, It has its own weak antibacterial activity.

Thus, Amoksiklav^® bactericidal effect on a wide spectrum of Gram-positive and Gram-negative bacteria (incl. on strains, which have acquired resistance to beta-lactam antibiotics due product β-lactamase).

Amoksiklav^® active against aerobic Gram-positive bacteria: Streptococcus spp. (incl. Streptococcus pneumoniae, Streptococcus viridans, Streptococcus pyogenes, Streptococcus bovis), Enterococcus spp., Staphylococcus aureus (except methicillin-resistant strains of), Staphylococcus epidermidis (except methicillin-resistant strains of), 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., Providencia spp., Salmonella spp., Shigella spp., Vibrio cholerae, Yersinia enterocolitica, Eikenella corrodens; anaerobic gram-positive bacteria: Peptococcus spp., Actinomyces israelii, Prevotella spp., Clostridium spp., Peptostreptococcus spp., Fusobacterium spp.; anaerobic gram-negative bacteria: Bacteroides spp.

Pharmacokinetics

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

Distribution

C_max After bolus injection Amoksiklava^® 1.2 g of amoxicillin 105.4 mg / l of clavulanic acid and – 28.5 mg / l. Both components are characterized by good volume distribution in body fluids and tissues (lungs, middle ear, plevralynaya and peritonealynaya zhidkosti, uterus, ovary). Amoxicillin penetrates well into the synovial fluid, liver, prostate, tonsils, muscle, gallbladder, the secret of the paranasal sinuses, spittle, bronchial secretion.

Amoxicillin and Clavulanic acid does not penetrate the BBB in the non-inflamed meninges.

C_max in body fluids there through 1 hours after reaching C_max plasma.

Active substances penetrate the placenta and in trace concentrations excreted with breast milk. Amoxicillin and clavulanic acid have a low binding to plasma proteins.

Metabolism

Amoxicillin partially metabolized, Clavulanic acid is exposed, apparently, intensive metabolism.

Deduction

Amoxicillin appears kidneys virtually unchanged by tubular secretion and glomerular filtration rate. Clavulanic acid is eliminated by glomerular filtration, partly as metabolites. Small quantities can be derived through the intestines and lungs. T_1/2 amoxicillin and clavulanic acid is 1-1.5 no.

Both components are removed in hemodialysis and peritoneal dialysis minor amounts.

Pharmacokinetics in special clinical situations

In severe renal insufficiency T_1/2 increases to 7.5 h dlya amoksitsillina and 4.5 h for clavulanic acid.

Testimony

Treatment of infectious and inflammatory diseases, caused by sensitive microorganisms:

- Infections of the upper respiratory tract and ENT (incl. acute and chronic sinusitis, acute and chronic otitis media, retropharyngeal abscess, tonsillitis, pharyngitis);

- Infections of the lower respiratory tract (incl. acute bronchitis with bacterial superinfection, chronic bronchitis, pneumonia);

- Urinary tract infections;

- Gynecological infections;

- Infections of the skin and soft tissues, including human and animal bites;

- Bone and joint infections;

- Infections of the abdominal cavity, incl. biliary tract (cholecystitis, kholangit);

- Odontogenic infections;

- Infections, sexually transmitted (gonorrhea, şankroid);

- Prevention of infections after surgery.

Dosage regimen

The drug is introduced into / in.

Adults and children over 12 years (body weight >40 kg) the drug is prescribed in a dose 1.2 g (1000 mg plus 200 mg) intervals 8 no, when severe infection – intervals 6 no.

Children aged 3 Months before 12 years the drug is prescribed in a dose 30 mg / kg body weight (based on the total Amoxiclav^®) intervals 8 no, when severe infection – intervals 6 no.

Children under 3 Months: prematurity and perinatal – dose 30 mg / kg body weight (based on the total Amoxiclav^®) every 12 no; in postperinatalnom period – dose 30 mg / kg body weight (based on the total Amoxiclav^®) every 8 no.

Every 30 mg formulation Amoksiklav^® contains 25 mg amoxycillin and 5 mg clavulanic acid.

Preventive dose surgery is 1.2 g at ​​induction of anesthesia (at least the duration of the operation 2 no); with longer operations – by 1.2 g to 4 time / day.

To patients with renal insufficiency the dose and / or the dosage interval should be adjusted according to creatinine clearance.

Since 85% Amoksiklava^® removed by hemodialysis, administration of the preparation is carried out at the end of hemodialysis. In peritoneal dialysis, does not require correction dosing regimen.

Course of treatment 5-14 days. The duration of treatment is determined individually. By reducing the severity of symptoms to continue therapy to switch to oral forms of the drug Amoxiclav^®.

Terms of preparation and administration solutions for I / injection

It should dissolve the contents of the vial 600 mg (500 mg plus 100 mg) in 10 ml water for injection or 1.2 g (1000 mg plus 200 mg) – in 20 ml water for injection.

B / administered slowly (during 3-4 min.)

Terms of preparation and administration solutions for in / infusion

For infusion administration Amoksiklava^® need for further breeding: made solutions, containing 600 mg (500 mg plus 100 mg) or 1.2 g (1000 mg plus 200 mg) product, must be diluted 50 ml or 100 ml infusion solution, respectively. The duration of infusion 30-40 m.

When using the following infusion solutions in the recommended amounts are stored in the appropriate concentration of the antibiotic.

As the solvent for I / infusions can be used following infusion solutions.

Amoksiklav^® less stable in infusion solutions, dextrose (glucose), dextran or bicarbonate.

Amoksiklav^® be administered during 20 minutes after the preparation of solutions for the on / in the. Use only clear solutions. Prepared solutions do not freeze.

Side effect

From the digestive system: loss of appetite, nausea, vomiting, diarrhea; rarely – abnormal liver function, increased ALT and AST; in a few cases – cholestatic jaundice, hepatitis, psevdomembranoznыy colitis.

Allergic reactions: itch, hives, erythematous rash; rarely – erythema multiforme exudative, angioedema, anaphylactic shock; in a few cases – exfoliative dermatitis, Stevens-Johnson syndrome.

Other: reversible increase in prothrombin time (when combined with anticoagulants); rarely – candidiasis and other forms of superinfection.

Contraindications

- An indication of a history of cholestatic jaundice or liver dysfunction, caused by the intake of amoxicillin / clavulanic acid;

- Increased sensitivity to antibiotics of penicillin;

- Hypersensitivity to amoxicillin or clavulanic acid or other ingredients.

FROM caution prescribe the drug to patients with known hypersensitivity to cephalosporin antibiotics, pseudomembranous colitis in history, hepatic failure, severe renal impairment.

Pregnancy and lactation

The appointment of the drug during pregnancy is possible only when there are clear indications. Amoxicillin and Clavulanic acid in small amounts are excreted in breast milk.

Cautions

In exchange application of the drug necessary to carry out monitoring of the functions of blood, liver, kidney.

Patients with severely impaired renal function requires adequate dosage adjustment Amoksiklava^® or increasing the intervals between use of the drug.

Because, that a large number of patients with infectious mononucleosis and lymphocytic leukemia, poluchavshih ampitsillin, erythematous rash was observed appearance, antibiotic ampicillin group in these patients is not recommended.

The preparation contains potassium.

Patients, a diet with restriction of sodium content, should be considered, in each vial 600 mg (500 mg plus 100 mg) contains 29.7 mg of sodium, Each vial 1.2 g (1000 mg plus 200 mg) contains 59.3 mg of sodium. The amount of sodium in the maximum daily dose exceeds 200 mg.

In primenenii Amoksiklava^® in high doses can be false positive reaction in determining the level of glucose in the urine using Benedict's reagent or solution Felling (recommend the use of enzymatic reactions with glucose oxidase).

Effects on ability to drive vehicles and management mechanisms

Information about the negative impact Amoksiklava^® at recommended doses on the ability to drive vehicles and management mechanisms are absent.

Overdose

There is no reports of deaths or life-threatening occurrence of side effects due to drug overdose.

Symptoms: abdominal pain, diarrhea, vomiting; it is also possible agitation, insomnia, dizziness; in some cases – convulsions.

Treatment: symptomatic therapy, necessary medical supervision. Effective hemodialysis.

Drug Interactions

In an application Amoksiklava^® anticoagulants, and there is an increase in prothrombin time. Therefore, this combination is assigned with caution.

In an application Amoksiklava^® with allopurinol increases the risk of side effects such as rash.

In an application Amoxiclav^® increases the toxicity of methotrexate.

In an application with Amoksiklava^® Diuretic, allopurinol, phenylbutazone, NSAIDs and other drugs, block tubular secretion, increase the concentration of amoxicillin (Clavulanic acid is derived mainly by glomerular filtration).

Antibiotics reduce the effectiveness of oral contraceptives.

Avoid concurrent use with disulfiram.

Amoksiklav^® should not be mixed in a syringe or infusion bottles with other drugs.

Avoid mixing Amoksiklava^® with glucose solution, dextran, bicarbonate and solutions, containing blood, proteins, lipids.

Pharmaceutical interaction

Amoksiklav^® and aminoglycoside antibiotics are physically and chemically compatible.

Avoid mixing Amoksiklava^® with dextrose solutions (Glucose), dextran, bicarbonate (tk. in their formulation is less stable), as well as with solutions of, containing blood, proteins and lipids.

Amoksiklav^® not mixed in the same syringe or infusion bottles with other drugs.

Conditions of supply of pharmacies

The drug is released under the prescription.

Conditions and terms

The drug should be stored out of reach of children, dark place at a temperature no higher than 25 ° C. Shelf life – 2 year.