Rapiklav

Rapiklav is an antibacterial drug for systemic use.

Indications of the rapiklava

It is used to eliminate bacterial infectious pathologies provoked by microbes that are sensitive to the drug:

• acute form of bacterial sinusitis;
• acute form of inflammation of the middle ear;
• confirmed exacerbation of chronic bronchitis;
• non-hospital pneumonia;
• pyelonephritis or cystitis;
• infectious processes inside soft tissues and skin (this includes animal bites, cellulitis and severe forms of dental abscesses, followed by cellulite of a common type);
• infection in the joints or bones (among them osteomyelitis).

Release form

The release is carried out in tablets; inside the first blister - 3 tablets. 7 blister plates are placed in a separate pack.

Pharmacodynamics

Rapiklav is a combined drug containing clavulic acid (irreversible inhibitor of β-lactamases), amoxicillin and penicillin with a wide range of antibacterial activity. The drug forms stable complex bonds with enzymes with an enzyme and protects them from the effects of amoxicillin.

Amoxicillin has bactericidal properties - it inhibits the process of binding of the cell wall during the growth of the bacterium (by means of competitive inhibition of transpeptidase activity). Clavulic acid has a slight antibacterial effect, but it is capable of irreversibly synthesizing β-lactamases, preventing the destruction of amoxicillin.

The drug has a wide range of effects, actively affecting the susceptible to amoxicillin-sensitive microbes, and in addition to resistant microorganisms forming β-lactamases, among which:

• Gram-positive aerobic bacteria (anthrax bacillus, corynebacterium, enterococcus fecal, listeria monocytogenes, pneumococcus, streptococcus pyogenes, Streptococcus bovis, Staphylococcus aureus, epidermal staphylococcus and Streptococcus viridans);
• Gram-positive anaerobic microorganisms: clostridia, peptococci and peptostreptococci;
• Gram-negative aerobic microbes: pertussis, brucella, E. Coli, Influenza rod, Moraxella catarrils, Proteus, Klebsiella, Gonococcus, Meningococcus, Pasturella multocida, Proteus mirabilis, vulgar proteus, Salmonella, Shigella and Vibrio cholerae;
• Gram-negative anaerobic microorganisms: bacteroides (among them bacteroidia fraigilis).

Individual representatives of these types of microbes produce β-lactamase, so they become resistant to monotherapy with amoxicillin.

Pharmacokinetics

Clavulic acid and amoxicillin are similar in their pharmacokinetics. They are quickly absorbed when taken orally; food does not affect the degree of absorption. Peak of serum levels they reach after 1-1.25 hours after use.

The half-life of amoxicillin is 78 minutes, and clavulanate is about 60-70 minutes. Both elements are able to penetrate most of the tissues and liquids (in the middle ear, lungs, tonsils and prostate, gall bladder and liver, as well as the ovaries and uterus, in addition to the excreta of the sinuses and maxillary sinuses, peritoneal from the pleural fluid, and in addition allocation of bronchi, sputum and synovia), and along with it through the placenta and BBB (in the latter case - with meningitis).

About 17-20% of amoxicillin, as well as 22-30% of clavulinic acid is synthesized with a plasma protein.

Both components are excreted through the kidneys: most of the amoxicillin is excreted unchanged, but clavulanate is in the form of decay products. Some of the substances can be excreted through the lungs with the intestines, and also get inside the breast milk.

The active ingredient can be removed from the body by a hemodialysis procedure.

Dosing and administration

The drug should be used, given the existing official recommendations for antibiotic therapy, as well as information on local sensitivity to the antibiotic. The tolerability of clavulanate and amoxicillin is different in different terrains and can change over time. If it exists, it is required to study information about local sensitivity and, if necessary, perform a microbiological study and conduct a test for tolerability.

The range of recommended dosages depends on the pathogens observed in the body, as well as their sensitivity to antibacterial drugs. Together with this, the severity of the disease and the location of the infection, and in addition weight, age and kidney function of a person.

Children weighing ≥40 kg and adults are required to take 1750 mg of amoxicillin / 250 mg of clavulanate per day (the dose is 2 tablets). To divide the daily portion should be for 2 uses.

Children weighing <40 kg can take no more than 1000-2800 mg amoxicillin / 143-400 mg clavulanate per day (if the following method is prescribed).

The duration of the course is determined taking into account the clinical response of the patient. For certain infections (such as osteomyelitis), prolonged therapy is necessary.

Children weighing <40 kg: daily dose in the range of 25 \ 3.6-45 \ 6.4 mg / kg. Dose divided into 2 portions.

Dose sizes in the case of functional hepatic impairment.

You should take the drug carefully, regularly monitoring changes in the liver. Information on dosages in this case is not enough.

Dose sizes for functional renal impairment.

Rapiklav in the amount of 875/125 mg can be prescribed only to individuals whose QC index is at least 30 ml / minute. In the case of kidney failure, in which KK - less than 30 ml / minute, this form of medicine can not be used.

The tablet is taken whole, without chewing. If necessary, you can divide it in half, then swallow both halves.

The duration of the course is selected individually. Do not continue therapy for more than 2 weeks without assessing the patient's condition.

The process of treatment can begin with the introduction of the drug parenterally. In the future, a transfer to the reception inside.

[4]

Use of the rapiklava during pregnancy

Reproductive tests of parenteral and oral forms of drugs on animals (dosages used that exceed human ones by a factor of 10) did not reveal a teratogenic effect. In the course of one of the tests involving pregnant women with premature rupture of the membranes, it was found that the use of Rapiklava for prophylaxis may increase the risk of developing a newborn in the NEC. As with other drugs, it is necessary to avoid taking medication during pregnancy (in particular, this applies to the first trimester). The only exceptions are cases where the potential benefit is higher than the risk of violations.

The active substances of the drug are able to penetrate into the breast milk (there is no information on the effects of clavulinic acid on the infants), therefore the infants can develop a fungus in the mucous membrane and diarrhea. As a consequence, it is necessary to cancel feeding for the period of drug use.

In general, lactation is recommended to take Rapiklav only in cases when the doctor evaluates the benefits of using drugs more than the probability of the risk of negative consequences.

Contraindications

Among the contraindications:

• high sensitivity relative to the elements of the drug, and in addition any antibacterial drugs from the category of penicillins;
• presence in the anamnesis of severe manifestations of intolerance (among them anaphylaxis), which are associated with the use of other β-lactam substances (monobactams and carbapenems included here, as well as cephalosporins);
• a history of hepatic dysfunction or jaundice caused by the use of clavulanate or amoxicillin;
• It is forbidden to use in the treatment of children under 12 years of age.

Side effects of the rapiklava

Reception Rapiklava can trigger the development of such side effects:

• infectious and invasive processes: often there is a candidiasis in the field of mucous membranes or skin. Unusually there is an excessive increase in the number of resistant microbes;
• hemopoietic system: occasionally there may be curable leukopenia (also includes neutropenia) or thrombocytopenia. Uniquely appears curable agranulocytosis, and in addition hemolytic form of anemia. Time of PTI and bleeding may also be prolonged;
• manifestations of allergy: single anaphylaxis, Quincke edema, allergic form of vasculitis, and serum sickness;
• reactions of NS: rarely there are headaches or dizziness. Cramps, reversed type hyperactivity and an aseptic form of meningitis can occur sporadically. Seizures usually appear in people with disorders in the work of the kidneys, as well as in people taking drugs in large doses;
• Gastrointestinal tract: adults usually have diarrhea; less often - vomiting or nausea. Children often have vomiting and nausea, and diarrhea (nausea mainly develops due to taking a large dose, the above reactions of the gastrointestinal tract can be reduced by taking drugs before eating). Disorders of digestion occasionally occur. Individually associated with antibiotics, colitis (here go hemorrhagic and pseudomembranous form of the disease) and black villous tongue;
• reactions of the hepatobiliary system: occasionally in persons using antibiotics from the category of β-lactams, there is a moderate increase in ALT or AST. Single intrahepatic cholestasis or hepatitis develops. Similar reactions appear in case of using other penicillins, as well as cephalosporins. For the most part, hepatitis develops in men, as well as in older people, and their appearance can be associated with prolonged therapy. In children, such reactions only occurred occasionally. Symptoms of the disease develop during the treatment or immediately after its termination, but in some cases they developed and a few weeks after the completion of therapy. Such signs are often reversible. Only single cases of death were observed, but they always occurred in people with a severe form of underlying pathology, or in those who simultaneously took medicines that had a negative effect on the liver;
• subcutaneous layers and skin: seldom manifested hives, itching and rashes on the skin. Occasionally, multiform erythema developed. Single Lyell or Stevens-Johnson syndrome, Ritter's disease and acute form of exanthematous pustules (generalized type). If you have an allergic form of dermatitis, you need to finish the treatment;
• system of urination and kidneys: crystaluluria or tubulointerstitial nephritis appeared sporadically.

[1], [2], [3]

Overdose

In case of an overdose, there may be reactions from the digestive tract, as well as a violation of the balance of water and electrolytes. These symptoms should be removed symptomatically, while restoring the balance of electrolytes with water. There is also information about the development of crystalluria, which later on it was transformed into kidney failure at times.

You can remove Rapiklav from the body by applying hemodialysis.

Interactions with other drugs

It is forbidden to combine with probenecid, as it reduces the release of amoxicillin through the renal tubules. When combined with Rapiklave, a prolonged increase in the indices of amoxicillin in the blood is possible, but with probenecid not affecting the indices of clavulanate.

The combination of amoxicillin and allopurinol may increase the risk of allergies. There is no information about the combined reception of Rapiklava with allopurinol.

Like other antibiotics, Rapiklav can affect the intestinal microflora, which is why estrogen reabsorption is reduced, and the effectiveness of combined oral contraception is weakened.

There is some information about the increase in INR values in persons using warfarin or acenocoumarol in combination with amoxicillin. If such a combination is required, it is necessary to carefully monitor the PTV level or the INR score (which also needs to be done for some time after the Rapiklava cancellation).

In people who use mycophenolate for mycophenolate, after starting taking amoxicillin and clavulanate, the pre-dose level of the active decomposition product of mycophenolic acid (approximately 50%) may decrease. This change may not correspond exactly to the changes in AUC of mycophenolic acid.

Penicillins can reduce the excretion of methotrexate, so that the toxic properties of the latter can be enhanced.

[5], [6]

Storage conditions

The medicine should be kept at a temperature of no more than 25 ° C.

[7]

Shelf life

Rapiklav can be used in the period of 2 years from the date of release of the drug.