Composition, form of production and packaging
The tablets covered with a cover from white up to almost white color, oval.
1 tab.
amoxicillin (in the form of trihydrate) 250 mg
clavulanic acid (in the form of a potassium salt) 125 mg
[PRING] silicon colloidal dioxide, microcrystalline cellulose, croscarmellose sodium, magnesium stearate, hypromellose, dibutyl phthalate, talc purified, titanium dioxide, isopropanol, methylene chloride.
3 pcs. - blisters (5) - packs of cardboard.
3 pcs. - blisters (7) - packs of cardboard.
3 pcs. - Strips (7) - packs of cardboard.
3 pcs. - Strips (5) - packs of cardboard.
21 pcs. - bottles of dark glass (1) - packs of cardboard.
The tablets covered with a cover from white up to almost white color, oval.
1 tab.
amoxicillin (in the form of trihydrate) 500 mg
clavulanic acid (in the form of a potassium salt) 125 mg
[PRING] silicon colloidal dioxide, microcrystalline cellulose, croscarmellose sodium, magnesium stearate, hypromellose, dibutyl phthalate, talc purified, titanium dioxide, isopropanol, methylene chloride.
3 pcs. - blisters (5) - packs of cardboard.
3 pcs. - blisters (7) - packs of cardboard.
3 pcs. - Strips (5) - packs of cardboard.
3 pcs. - Strips (7) - packs of cardboard.
21 pcs. - bottles of dark glass (1) - packs of cardboard.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the print edition of 2007.
PHARMACHOLOGIC EFFECT
Antibacterial preparation is a combination of amoxicillin-semisynthetic penicillin with a broad spectrum of antibacterial activity and clavulanic acid, an irreversible inhibitor of О±-lactamases (II, III, IV, V type, in respect of type I inactive). Clavulanic acid forms a stable inactivated complex with these enzymes and prevents the loss of antibacterial activity of amoxicillin caused by the production of ОІ-lactamases as the main pathogens and co-pathogens and opportunistic microorganisms. This combination provides a high bactericidal activity Rapiklava.
The drug has a broad spectrum of antibacterial action. Active against amoxicillin-sensitive and ОІ-lactamase-producing strains, gram-positive aerobes: Streptococcus pneumoniae, Streptococcus pyogenes, Streptococcus viridans, Streptococcus bovis, Staphylococcus aureus (except methicillin-resistant strains), Staphylococcus epidermidis (except methicillin-resistant strains), Listeria spp. , Enteroccocus spp .; Gram-negative aerobes: Bordetella pertussis, Brucella spp., Campylobacter jejuni, Escherichia coli, Gardnerella vaginalis, Haemophilus influenzae, Haemophilus ducreyi, Klebsiella spp., Moraxella catarrhalis, Neisseria gonorrhoeae, Neisseria meningitidis, Pasteurela multocida, Proteus spp., Salmonella spp., Shigella spp., Vibriocholerae, Yersenia enterocolitica; anaerobes: Peptococcus spp., Peptostreptococcus spp., Clostridium spp., Bacteroides spp., Actinimyces israelli.
PHARMACOKINETICS
The main pharmacokinetic parameters of amoxicillin and clavulanic acid are similar.
Suction
Both components are well absorbed from the digestive tract after ingestion, the intake of food does not affect the degree of absorption. C max active substances in the plasma are determined approximately 1 hour after ingestion.
Distribution
Both components are characterized by a good V d and are distributed in the body fluids and tissues (including the lungs, middle ear, pleural and peritoneal fluids, uterus, ovaries). Amoxicillin also penetrates into the synovial fluid, the liver, the prostate, palatine tonsils, muscle tissue, gall bladder, the secret of the paranasal sinuses, saliva and bronchial secretions.
Amoxicillin and clavulanic acid do not penetrate the BBB in uninflated cerebral membranes, but penetrate the placental barrier and are excreted in breast milk in trace concentrations.
The binding to plasma proteins in amoxicillin and clavulanic acid is low.
Metabolism
Amoxicillin is metabolized in part, clavulanic acid is apparently subjected to intense metabolism.
Excretion
Amoxicillin is excreted by the kidneys practically unchanged through tubular secretion and glomerular filtration. Clavulanic acid is excreted by glomerular filtration, partly in the form of metabolites. Small amounts can be excreted through the intestines and lungs. T 1/2 of amoxicillin and clavulanic acid is 1-1.5 h.
Pharmacokinetics in special clinical situations
In patients with severe renal failure, T 1/2 increases to 7.5 h for amoxicillin and up to 4.5 h for clavulanic acid.
Both substances are removed during hemodialysis, with peritoneal dialysis - slightly.
INDICATIONS
Treatment of infectious-inflammatory diseases caused by pathogens that are sensitive to the combination:
- infection of ENT organs (acute and chronic sinusitis, acute and chronic otitis media, tonsillitis, pharyngitis);
- infections of the respiratory system (acute and chronic bronchitis and pneumonia, empyema of the pleura);
- urinary tract infections (including cystitis, urethritis, pyelonephritis);
- gynecological infections (including salpingitis, salpingo-oophoritis, endometritis, septic abortion, pelvioperitonitis);
- infections of bones and joints (including chronic osteomyelitis);
- infections of the skin and soft tissues (including phlegmon, wound infection);
- biliary tract infections (cholecystitis, cholangitis);
- Sexually transmitted diseases (gonorrhea, chancroid);
odontogenic infections.
DOSING MODE
Tablets should be taken orally while eating, without chewing, with a small amount of water.
Adults and children over 12 years of age (or with a body weight of more than 40 kg), the average dose for the treatment of infections of mild to moderate severity is 1 tab. 250 mg / 125 mg 3 times / day.
In severe infections , 2 tablets are prescribed. 250 mg / 125 mg 3 times / day or 1 tab. 500 mg / 125 mg 3 times / day.
The maximum daily dose of clavulanic acid (in the form of potassium salt) is 600 mg for adults and 10 mg / kg for children.
The maximum daily dose of amoxicillin is 6 g for adults and 45 mg / kg for children.
The course of treatment is 5-14 days and is set individually, depending on the clinical situation. The drug should not be taken for more than 14 days without a second medical examination.
With odontogenic infections, the drug is prescribed 1 tablet. 500 mg / 125 mg every 12 hours for 5 days.
With renal failure and KK 10-30 ml / min, the drug is prescribed 1 tablet. 500 mg / 125 mg every 12 hours, with CC less than 10 ml / min - 1 tab. 500 mg / 125 mg every 24 hours.
With anuria, the interval between taking the drug should be increased to 48 hours or more.
SIDE EFFECT
On the part of the digestive system: nausea, vomiting, diarrhea, impaired liver function, increased activity of hepatic transaminases; in isolated cases - cholestatic jaundice, hepatitis, pseudomembranous colitis.
Allergic reactions: urticaria, erythematous rashes; rarely - erythema multiforme, anaphylactic shock, Quincke's edema, Stevens-Johnson syndrome; extremely rare - exfoliative dermatitis.
Local reactions: in some cases - phlebitis in the place of intravenous administration.
Other: candidiasis, development of superinfection, reversible increase in prothrombin time.
CONTRAINDICATIONS
- infectious mononucleosis (including with carpal-like rash);
- Hypersensitivity to the components of the drug, to cephalosporins and other beta-lactam antibiotics.
With caution appoint the drug to patients with severe hepatic insufficiency, gastrointestinal diseases (including when referring to a history of colitis associated with the use of penicillins), with chronic renal failure.
PREGNANCY AND LACTATION
With caution appoint the drug during pregnancy and lactation (breastfeeding).
APPLICATION FOR FUNCTIONS OF THE LIVER
With caution appoint the drug to patients with chronic renal failure.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
With caution appoint the drug to patients with severe hepatic insufficiency.
APPLICATION FOR CHILDREN
Children older than 12 years (or with a body weight of more than 40 kg), the average dose for the treatment of infections of mild to moderate severity is 1 tab. 250 mg / 125 mg 3 times / day.
SPECIAL INSTRUCTIONS
In course treatment it is necessary to monitor the indicators of the state of the hematopoiesis system, the functions of the liver and kidneys.
To reduce the risk of side effects from the GIT, the drug should be taken with food.
It is possible to develop superinfection by increasing the microflora insensitive to the drug, which requires an appropriate change in antibacterial therapy.
When the drug is prescribed for patients with sepsis, the development of a bacteriolysis reaction (the Yarisch-Geyxheimer reaction) is possible.
In patients who are hypersensitive to penicillins, there may be cross-allergic reactions with cephalosporin antibiotics.
Receiving Rapiklava leads to the appearance of amoxicillin in the urine. High concentrations of amoxicillin give a false positive response to urine glucose when using a Benedict reagent or Felling solution. It is recommended to carry out enzymatic reactions with glucose oxidase.
OVERDOSE
Symptoms: a violation of the function of the gastrointestinal tract and water-electrolyte balance.
Treatment: if necessary, conduct symptomatic therapy. Hemodialysis is effective.
DRUG INTERACTION
At simultaneous reception with Rapiklav antacids, glucosamine, laxatives, aminoglycosides slow down and reduce the absorption of active substances; ascorbic acid increases their absorption.
When combined, bactericidal antibiotics (including aminoglycosides, cephalosporins, cycloserine, vancomycin, rifampicin) exert a synergistic effect with Rapiclav;bacteriostatic drugs (macrolides, chloramphenicol, lincosamides, tetracyclines, sulfonamides) - antagonistic.
With simultaneous application Rapiklav increases the effectiveness of indirect antigoagulants (suppressing the intestinal microflora, reduces the synthesis of vitamin K and prothrombin index). The use of such a combination requires the control of blood coagulability.
With simultaneous application Rapiklav reduces the effectiveness of oral contraceptives, ethinyl estradiol, drugs, in the process of metabolism of which forms paraminobenzoic acid.
With the simultaneous use of diuretics, allopurinol, phenylbutazone, NSAIDs and other drugs that block the tubular secretion, increase the concentration of amoxicillin (clavulanic acid is excreted mainly by glomerular filtration).
With simultaneous application with Rapiklav, allopurinol increases the risk of developing skin rashes.
TERMS OF RELEASE FROM PHARMACY
The drug is released by prescription.
TERMS AND CONDITIONS OF STORAGE
List B. The drug should be stored in a dry, protected from light, out of reach of children at a temperature of no higher than 25 В° C. Shelf life - 1.5 years.
