Рапиклав

General characteristics. Structure:

Active agent: amoxicillin (in the form of trihydrate) 250 mg
clavulanic acid (in the form of potassium salt) 125 mg

Excipients: silicon dioxide colloid, cellulose microcrystallic, sodium of a kroskarmelloz, magnesium stearate, a gipromelloz, the dibutyl phthalate, talc purified titanium dioxide, isopropanol, a methylene chloride.
 
Active agent: amoxicillin (in the form of trihydrate) 500 mg
clavulanic acid (in the form of potassium salt) 125 mg

Excipients: silicon dioxide colloid, cellulose microcrystallic, sodium of a kroskarmelloz, magnesium stearate, a gipromelloz, the dibutyl phthalate, talc purified titanium dioxide, isopropanol, a methylene chloride.

Pharmacological properties:

Antibacterial drug, represents an amoxicillin combination - semi-synthetic penicillin with a wide range of antibacterial activity and clavulanic acid - irreversible inhibitor β-лактамаз (II, III, IV, V types; concerning the I type it is inactive). Clavulanic acid forms the resistant inactivated complex with the specified enzymes and prevents loss of the antibacterial activity of amoxicillin caused by products β-лактамаз as the main activators and to - pathogens, and uslovnopatogenny microorganisms. This combination provides high bactericidal activity Rapiklava.

Drug possesses a wide range of antibacterial action. It is active concerning the sensitive to amoxicillin and producing β-lactamelements strains gram-positive aerobes: Streptococcus pneumoniae, Streptococcus pyogenes, Streptococcus viridans, Streptococcus bovis, Staphylococcus aureus (except Methicillinum - resistant strains), Staphylococcus epidermidis (except Methicillinum - 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; anaerobe bacterias: Peptococcus spp., Peptostreptococcus spp., Clostridium spp., Bacteroides spp., Actinimyces israelli.

Pharmacokinetics. The key pharmacokinetic parameters of amoxicillin and clavulanic acid are similar.

Absorption. Both components are well absorbed from a GIT after administration of drug inside, meal does not influence extent of absorption. Cmax of active agents in plasma are defined approximately by 1 h after intake.

Distribution. Both components are characterized by good Vd and distributed in liquid and body tissue (including in lungs, a middle ear, pleural and peritoneal liquids, a uterus, ovaries). Amoxicillin also gets into synovial fluid, a liver, a prostate, palatine tonsils, muscular tissue, a gall bladder, a secret of adnexal bosoms of a nose, saliva and a bronchial secret.
Amoxicillin and clavulanic acid do not get through GEB at an uninflammed meninx, but get through a placental barrier and are emitted with breast milk in trace concentration.
Linkng with proteins of plasma at amoxicillin and clavulanic acid low.

Metabolism. Amoxicillin is metabolized partially, clavulanic acid is exposed, apparently, to intensive metabolism.

Removal. Amoxicillin is removed by kidneys practically in not changed look by canalicular secretion and glomerular filtering. Clavulanic acid is removed by glomerular filtering, partially in the form of metabolites. Small amounts can be removed through intestines and lungs. T1/2 of amoxicillin and clavulanic acid makes 1-1.5 h.

Pharmacokinetics in special clinical situations. At patients with a heavy renal failure of T1/2 increases to 7.5 h for amoxicillin and to 4.5 h for clavulanic acid.
Both substances are removed at a hemodialysis, at peritoneal dialysis – is insignificant.

Indications to use:

Treatment of the infectious and inflammatory diseases caused sensitive to a combination to drug by activators:
— infections of ENT organs (acute and chronic sinusitis, acute and chronic otitis, tonsillitis, pharyngitis);
— infections of a respiratory organs (acute and chronic bronchitis and pneumonia, pleura empyema);
— infections of urinary tract (including cystitis, uretrita, pyelonephritises);
— gynecologic infections (including salpingitis, salpingo-oophoritis, endometritis, septic abortion, pelviperitonitis);
— infections of bones and joints (including chronic osteomyelitis);
— infections of skin and soft tissues (including phlegmon, wound fever);
— infections of bilious ways (cholecystitis, cholangitis);
— diseases, sexually transmitted (gonorrhea, шанкроид);
— dontogenous infections.

Route of administration and doses:

Pill should be taken inside during food, without chewing, washing down with a small amount of water.

To adults and children 12 years (or with body weight more than 40 kg) an average dose for treatment of infections easy are more senior and moderate severity makes 1 tablets of 250 mg / 125 mg of 3 times/days.
At heavy infections appoint on 2 tablets 250 mg / 125 in mg of 3 times/days or on 1 tablets of 500 mg / 125 in mg of 3 times/days.
The maximum daily dose of clavulanic acid (in the form of potassium salt) makes for adults - 600 mg and for children - 10 mg/kg of body weight.

The maximum daily dose of amoxicillin makes for adults - 6 g and for children - 45 mg/kg of body weight.

The course of treatment makes 5-14 days and is established individually depending on a clinical situation. It is impossible to accept drug more than 14 days without repeated medical examination.
At dontogenous infections drug each 12 h within 5 days appoint on 1 tablets 500 mg / 125 mg.
At a renal failure and KK of 10-30 ml/min. drug each 12 h appoint on 1 tablets 500 mg / 125 mg, at KK less than 10 ml/min. - on 1 tablets of 500 mg / 125 mg each 24 h.
At an anury it is necessary to increase an interval between administration of drug to 48 h and more.

Features of use:

At course treatment it is necessary to carry out control of indicators of a condition of system of a hemopoiesis, function of a liver and kidneys.

For the purpose of decrease in risk of development of side effects from a GIT drug should be accepted during food.

Development of superinfection due to growth of microflora, insensitive to drug, is possible that demands corresponding change of antibacterial therapy.

At purpose of drug to patients with sepsis development of reaction of a bacteriolysis (Yarisha-Geyksgeymer's reaction) is possible.

At the patients having hypersensitivity to penicillin cross allergic reactions with tsefalosporinovy antibiotics are possible.

Rapiklava leads reception to emergence of amoxicillin in urine. High concentration of amoxicillin give false positive reaction to urine glucose when using a reactant of Benedict or solution of Fellinga. It is recommended to carry out enzymatic reactions with glucose oxydas.

Side effects:

From the alimentary system: nausea, vomiting, diarrhea, abnormal liver function, increase in activity of hepatic transaminases; in isolated cases - cholestatic jaundice, hepatitis, pseudomembranous colitis.
Allergic reactions: urticaria, erythematic rashes; seldom – a mnogoformny erythema, an acute anaphylaxis, a Quincke's edema, Stephens-Johnson's syndrome; extremely seldom - exfoliative dermatitis.
Local reactions: in some cases - phlebitis in the place in/in introductions.
Others: candidiasis, development of superinfection, reversible increase in a prothrombin time.

Interaction with other medicines:

At a concomitant use with Rapiklav antacids, a glycosamine, purgatives, aminoglycosides slow down and reduce absorption of active veshchenstvo; ascorbic acid increases their absorption.

At combined use bactericidal antibiotics (including aminoglycosides, cephalosporins, Cycloserinum, Vancomycinum, rifampicin) have sinergidny effect with Rapiklav; bacteriostatic drugs (macroleads, chloramphenicol, linkozamida, tetracyclines, streptocides) - antagonistic.

At simultaneous use of Rapiklav increases efficiency of indirect antigoagulyant (suppressing intestinal microflora, reduces synthesis of vitamin K and a prothrombin ratio). Use of such combination demands control of indicators of coagulability of blood.

At simultaneous use of Rapiklav reduces efficiency of oral contraceptives, ethinylestradiol, medicines in the course of which metabolism paraminobenzoyny acid is formed.

At simultaneous use diuretics, Allopyrinolum, phenylbutazone, NPVS and other drugs blocking kanaltsiyevy secretion increase concentration of amoxicillin (clavulanic acid is removed generally by glomerular filtering).

At simultaneous use with Rapiklav Allopyrinolum increases risk of development of skin rash.

Contraindications:

— an infectious mononucleosis (including at korepodobny rash);
— hypersensitivity to drug komponeta, to cephalosporins and another beta лактамным to antibiotics.
With care appoint drug to patients with a heavy liver failure, gastrointestinal diseases (including at the instruction in the anamnesis to the colitis connected using penicillin), with a chronic renal failure.

Use of drug RAPIKLAV at pregnancy and feeding by a breast
With care appoint drug at pregnancy and in the period of a lactation (breastfeeding).

Use at abnormal liver functions
With care appoint drug to patients with a heavy liver failure.

Use at renal failures
With care appoint drug to patients with a chronic renal failure.

Use for children
To children 12 years (or with body weight more than 40 kg) an average dose for treatment of infections easy are more senior and moderate severity makes 1 tablets of 250 mg / 125 mg of 3 times/days.

Overdose:

Symptoms: dysfunction of a GIT and water and electrolytic balance.
Treatment: if necessary carry out symptomatic therapy. The hemodialysis is effective.

Storage conditions:

List B. Drug should be stored in dry, protected from light, the place, unavailable to children, at a temperature not above 25 °C.

Issue conditions:

According to the recipe

Packaging:

Tablets, покр. cover, 250 mg +125 mg: 15 or 21 pieces. 

Tablets, покр. cover, 500 mg +125 mg: 15 or 21 pieces.