Composition, form of production and packaging
Tablets covered with a film membrane from white to almost white, oval, biconvex, with a risk on one side; on a break - yellowish color.
amoxicillin (in the form of amoxicillin trihydrate) 875 mg
clavulanic acid (in the form of a mixture of potassium clavulanate and microcrystalline cellulose (1: 1)) 125 mg
Excipients: microcrystalline cellulose - 510.35 mg, sodium carboxymethyl starch (type A) 32.8 mg, magnesium stearate 32 mg, silicon dioxide colloidal anhydrous 24 mg, butyl hydroxy anisole 0.85 mg.
The composition of the film shell: hypromellose - 34.84 mg, titanium dioxide (E171) - 17.42 mg, propylene glycol - 8.17 mg, talc - 3.57 mg.
14 pcs. - banks of dark glass (1) - packs of cardboard.
INSTRUCTION FOR THE SPECIALIST.
Description of the drug approved by the manufacturer for the printed edition of 2014.
Panklava 2X is a combination of amoxicillin - semisynthetic penicillin with a broad spectrum of antibacterial activity - and clavulanic acid - an irreversible inhibitor of О±-lactamase.
Amoxicillin - semisynthetic aminopenicillin, a broad-spectrum antibacterial agent, belongs to the group of beta-lactam antibiotics. It inhibits transpeptidase, breaks the synthesis of peptidoglycan (the supporting protein of the cell wall) in the period of division and growth, causes bacterial lysis.
Clavulanic acid is an inhibitor of ОІ-lactamase enzymes produced by certain bacteria and destroying penicillins and others (3-lactam antibiotics.) The addition of clavulanic acid to amoxicillin, preventing the inactivation of the antibiotic, extends its range of action due to microorganisms whose resistance to amoxicillin is due to production? lactamase, clavulanic acid forms a stable inactive complex with Q-lactamases and protects amoxicillin from the loss of antibacterial activity caused by the production of О±-lactam AMAZ as the main causative agents and co-pathogens and opportunistic microorganisms. Furthermore, clavulanic acid has its own weak antibacterial activity.
Panklava 2X has a broad spectrum of action, is active against amoxicillin-sensitive microorganisms, including strains producing ОІ-lactamases: gram-positive aerobes: Streptococcus pneumoniae, Streptococcus pyogenes, Streptococcus group of viridans, Streptococcus bovis, Staphylococcus aureus (except methicillin-resistant strains), Staphylococcus epidermidis except methicillin-resistant strains), Staphylococcus saprophytics, Listeria monocytogenes, 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, Pasteurella multocida, Proteus spp., Salmonella spp., Shigella spp., Vibrio cholerae, Yersenia enterocolitica, Helicobacter pylori, Eikenella corrodens;
Gram-positive anaerobes: Peptococcus spp., Peptostreptococcus spp., Clostridium spp., Actinomyces israelii, Fusobacterium spp., Prevotella spp .;
Gram-negative anaerobes: Bacteroides spp.
The main pharmacokinetic parameters of amoxicillin and clavulanic acid are similar. Both components are well absorbed after oral administration; the intake of food by the degree of absorption is not affected. Bioavailability is 90% for amoxicillin and 70% for clavulanic acid. The peak of plasma concentrations is achieved approximately 2 to 2.5 hours after administration. The maximum concentration of amoxicillin in the blood (C max ) is about 12 Ојg / ml, clavulanic acid is 3.3 Ојg / ml.The half-life (T 1/2 ) of amoxicillin and clavulanic acid is 1 to 1.5 hours. Connection with plasma proteins: amoxicillin - about 18%, clavulanic acid - 25%. Apparent volume of distribution of amoxicillin is 0.3 - 0.4 l / kg, clavulanic acid - 0.2 l / kg.
Both components are found in many organs and tissues of the body, biological fluids and pathological detachable: amoxicillin - in the lung tissue, bronchial secretion and saliva; in the skin, subcutaneous, muscular and fatty tissues, in the palatine tonsils; in bone tissue and synovial fluid; mucous membrane of the intestine, liver, gall bladder, bile, female genital organs, fetal tissues; pleural and peritoneal fluid, the contents of skin blisters, sputum, bronchial secretion (to a lesser degree in purulent discharge), in exudate with inflammation of the middle ear and accessory sinuses of the nose; clavulanic acid - in the palatine tonsils, organs of the abdominal cavity, bone, muscle and fatty tissues, synovial and peritoneal fluids, bile and purulent discharge. Neither the active components of Panklava 2X nor their metabolites are cumulated in any organs and tissues.
Amoxicillin and clavulanic acid do not penetrate the unchanged blood-brain barrier.
Amoxicillin and clavulanic acid penetrate the placental barrier and into breast milk.
Amoxicillin partially (10-25% of the absorbed dose) is metabolized to inactive penicillic acid; Clavulanic acid is metabolized intensively, its metabolites are excreted through the kidneys, intestines and lungs.
Amoxicillin is excreted mainly by the kidneys through tubular secretion and glomerular filtration. The total clearance of the combination amoxicillin / clavulanic acid is 25 l / h. During the first 6 hours after a single dose of the drug, 60% and 40% of the administered dose of amoxicillin and clavulanic acid are excreted unchanged from the body, respectively.
Both components are removed during hemodialysis, to a lesser extent - with peritoneal dialysis.
Elderly patients: in view of the possible age-related decrease in the excretory function of the kidneys, use with caution is recommended.
In patients with severe renal failure, the elimination half-life increases to 7.5 hours for amoxicillin and up to 4.5 hours for clavulanic acid.
Infectious-inflammatory diseases caused by microorganisms sensitive to amoxicillin / clavulanic acid:
- infections of the upper respiratory tract and ENT organs (including acute and chronic sinusitis, acute and chronic otitis media, peritonsillar abscess, tonsillitis, pharyngitis);
- infections of the lower respiratory tract (acute bronchitis with bacterial superinfection, exacerbation of chronic bronchitis, pneumonia);
- urinary tract infections;
- infection of the pelvic organs;
- skin and soft tissue infections (including after animal and human bites);
- infections of bones and joints (including osteomyelitis);
- bile duct infection (cholecystitis, cholangitis);
infection in dentistry.
Inside, washing down with water; at the beginning of food intake (to reduce the risk of side effects from the gastrointestinal tract), 2 times a day, strictly observing the interval between meals at 12 hours.
Adults and children over 12 years.
Adults and children over 12 years of age (body weight 40 kg and more) - take 1 tablet 2 times a day, every 12 hours.
The maximum daily dose of amoxicillin for adults is 6 g, for children - 45 mg / kg / day.
The maximum daily dose of clavulanic acid for adults (in the form of potassium clavulanate) is 600 mg, for children -10 mg / kg / day.
The course of treatment is 5-14 days; is established individually, taking into account the features of the pathogen, the localization and severity of the infection.
Dosing in renal failure
Tablets 875 mg / 125 mg should be used only in patients with creatinine clearance greater than 30 ml / min, with no dose adjustment required.
Patients on peritoneal dialysis do not need dose adjustment. Patients on hemodialysis may need a dose adjustment.
Important! If the drug is missed, you should take the pill as soon as possible without waiting for the next time. Next, observe equal intervals between meals - for 12 hours. Never take a double dose to compensate for missed medication!
Very often - more than 10%; often - more than 1 and less than 10%; infrequently - more than 0.1 and less than 1%; rarely - more than 0.01 and less than 0.1%; very rarely - less than 0.01%.
From the side of the central nervous system: infrequently - dizziness, headache; very rarely - excitement, anxiety, reversible hyperactivity, insomnia, behavior change, convulsions.
From the gastrointestinal tract: often - loss of appetite, nausea, vomiting, diarrhea; infrequent - dyspepsia, moderate asymptomatic increase in activity of alanine aminotransferase, aspartate aminotransferase, alkaline phosphatase and / or increased bilirubin concentration; rarely - pseudomembranous colitis, discoloration of the teeth (reversible, removed hygienic means); very rarely - "black hairy tongue", hepatitis, cholestatic jaundice, liver failure (usually in the elderly, in men, with prolonged therapy), stomatitis, glossitis.
From the hematopoiesis: rarely - neutropenia, thrombocytopenia / thrombocytosis, hemolytic anemia; very rarely - leukopenia, agranulocytosis, increased prothrombin time and bleeding time, eosinophilia.
From the side of the urinary system: very rarely - interstitial nephritis, crystalluria, hematuria.
Allergic reactions: infrequently - urticaria, rash, itchy skin; rarely erythema multiforme; frequency is not known - angioedema, anaphylaxis, allergic vasculitis, Stevens-Johnson syndrome, toxic epidermal necrolysis (Lyell's syndrome), bullous exfoliative dermatitis, acute generalized exanthematous pustules, a syndrome similar to serum sickness.
Other: often - Candidiasis of the skin and mucous membranes; very rarely - the development of superinfection.
- hypersensitivity to the active and / or accessory components of Panklaw 2X;
- hypersensitivity to beta-lactam antibiotics (penicillins, cephalosporins, carbapenems, etc.);
- a history of cholestatic jaundice and / or liver dysfunction caused by taking a penicillin antibiotic or a combination of amoxicillin / clavulanic acid;
- impaired renal function (creatinine clearance less than 30 ml / min);
- Infectious mononucleosis;
- Breastfeeding (lactation period);
- Children under 12 years of age and / or body weight less than 40 kg (for tablets 875 mg / 125 mg).
Hepatic failure, chronic renal failure (creatinine clearance more than 30 ml / min), pseudomembranous colitis in history, elderly age (over 65, hyperkalemia, pregnancy.
PREGNANCY AND LACTATION
In pregnancy, it can be used when the benefits of using it for the mother greatly exceed the risk to the fetus. If you need to use the drug during lactation, breastfeeding is suspended.
APPLICATION FOR FUNCTIONS OF THE LIVER
Contraindicated in disorders of kidney function (QC less than 30 ml / min); use with caution in chronic renal failure (QC greater than 30 mL / min),
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
Contraindicated in the violation of liver function. Use with caution in liver failure.
APPLICATION FOR CHILDREN
Contraindicated for children under 12 years and children weighing less than 40 kg.
APPLICATION IN ELDERLY PATIENTS
In view of the possible age-related (over 65 years) reduction in the excretory function of the kidneys, use with caution is recommended.
With a long course of treatment, it is necessary to provide control over the status of the function of the organs of hematopoiesis, liver and kidneys.
Patients with severe renal dysfunction require adequate dose adjustment or an increase in intervals between doses of the drug.
To reduce the risk of side effects from the gastrointestinal tract, the drug should be taken at the beginning of food intake.
To prevent the development of crystalluria, the drug should be washed down with a relatively large amount of water (0.5-1 glass).
Unchanged amoxicillin is excreted in the urine. High concentrations of amoxicillin give a false positive reaction to urine glucose when using a Benedict reagent or Felling solution. It is recommended to use enzymatic reactions with glucose oxidase.
Perhaps the development of bacterial or fungal superinfection (Pseudomonas spp., Candida albicans) due to the growth of insensitive to the drug microflora, which requires a corresponding change in antibacterial therapy.
During therapy with the drug as a result of exposure to C. Difficile toxin, the development of pseudomembranous colitis is possible. In case of severe diarrhea, as in the case of diarrhea lasting 2-3 days, you need to see a doctor as soon as possible. With the development of mild diarrhea against the background of Panklava 2X, antidiarrheal drugs should be avoided that inhibit intestinal peristalsis; it is possible to use kaolin or attapulgite-containing antidiarrhoeic agents.
Since Panklav 2X contains potassium, caution should be exercised when prescribing it to patients with initial hyperkalemia.
It is advisable to use caution when administering Panklava 2X to patients with hepatic insufficiency and to provide regular laboratory monitoring of liver function.
When jaundice coloring of the skin, eye whites, darkening of the color of urine and / or clarification of the stool, it is necessary to consult a doctor immediately.
In patients who are hypersensitive to penicillins, there may be cross-allergic reactions with cephalosporin antibiotics. It is not recommended to use Panklav2X for infectious mononucleosis and if it is suspected, as the drug can cause an erythematous skin rash, which aggravates the symptoms of the disease / complicates the diagnosis.
In neonates born to mothers who received preventive therapy with amoxicillin / clavulanic acid for premature rupture of the membranes (premature bladder) with premature pregnancy, there is an increased risk of developing necrotizing enterocolitis.
Impact on the ability to drive vehicles and manage mechanisms
During the period of treatment, it is recommended to use caution when driving vehicles and engaging in other potentially hazardous activities, as vertigo is possible.
Symptoms: nausea, vomiting, abdominal pain, diarrhea, disturbance of water-electrolyte balance; there may be excitement, insomnia; There are isolated cases of seizures and crystalluria in patients with initially impaired renal function. No reports of death or development of life-threatening adverse events in an overdose of the drug.
Treatment: symptomatic; Gastric lavage and intake of absorbent are effective if the drug was taken less than 4 hours ago. Hemodialysis is effective.
Antacids, glucosamine, laxatives, aminoglycosides - slow down and reduce absorption; ascorbic acid increases absorption.
Bactericidal antibiotics (including aminoglycosides, cephalosporins, cycloserine, vancomycin, rifampicin) have a synergistic effect; bacteriostatic drugs (macrolides, chloramphenicol, lincosamides, tetracyclines, sulfonamides) -antagonistic.
Increases the effectiveness of indirect anticoagulants (suppressing the intestinal microflora, reduces the synthesis of vitamin K and prothrombin index). With the simultaneous administration of anticoagulants, it is necessary to monitor blood coagulability.
Reduces the effectiveness of oral contraceptives, drugs, in the process of metabolism which produces paraaminobenzoic acid, ethinyl estradiol - the risk of bleeding "breakthrough".
Diuretics, allopurinol, phenylbutazone, non-steroidal anti-inflammatory drugs and other drugs that block tubular secretion, increase the concentration of amoxicillin (clavulanic acid is excreted mainly by glomerular filtration).
Allopurinol increases the risk of skin rash.
TERMS OF RELEASE FROM PHARMACY
TERMS AND CONDITIONS OF STORAGE
Store at a temperature of no higher than 30 В° C in the original packaging. Keep out of the reach of children. Shelf life - 2 years.