Amoksil-K
Producer: Arterium (Arterium) Ukraine
Code of automatic telephone exchange: J01CR02
Release form: Liquid dosage forms. Powder for preparation of solution for injections.
General characteristics. Structure:
Active ingredients: amoxicillin, clavulanic acid;
1 bottle contains sterile mix (5:1) amoxicillin of sodium salt and clavulanate of potassium salt, in recalculation on amoxicillin of 1,0 g and clavulanic acid of 0,2 g.
Pharmacological properties:
Pharmacodynamics. Amoxicillin - a semi-synthetic antibiotic with a wide range of antibacterial activity against many gram-positive and gram-negative microorganisms. Amoxicillin is sensitive to a beta laktamaze and breaks up under its influence therefore the range of activity of amoxicillin does not include microorganisms which synthesize this enzyme. Clavulanic acid has beta лактамную structure, like structure of penicillin. Besides, it is capable to inactivate beta лактамазные enzymes which are a part of microorganisms, resistant to penicillin and cephalosporins. Clavulanic acid is active rather important, from the clinical point of view, plasmid beta лактамаз which often are responsible for emergence of cross resistance to antibiotics. Presence of clavulanic acid as a part of Amoksila-K protects amoxicillin from disintegration under the influence of enzymes beta лактамаз and expands a range of antibacterial effect of amoxicillin, including those microorganisms which in general rezistentna to amoxicillin and other penicillin and cephalosporins.
Thus, Amoksil-K shows properties of an antibiotic of a broad spectrum of activity and inhibitor beta лактамаз. Medicine renders bactericidal action of rather wide range of microorganisms, including:
gram-positive aerobes: Bacillus anthracis *, types of Corynebacterium, Enterococcus faecalis *, Enterococcus faecium *, Listeria monocytogenes, Nocardia asteroides, Staphylococcus aureus *, koagulazootritsatelny staphylococcus (including Staphylococcus epidermidis), Streptococcus agalactiae, Streptococcus pneumoniae, Streptococcus pyogenes, types of Streptococcus, viridans;
gram-positive anaeroby:vida of Clostridium, types of Peptococcus, types of Peptostreptococcus;
gram-negative aerobes: Bordetella pertussis, types of Brucella, Escherichia coli *, Gardnerella vaginalis, Haemophilus influenzae *, Helicobacter pylori, types of Klebsiella *, types of Legionella, Moraxella catarrhalis * (Branhamella catarrhalis), Neisseria gonorrhoeae *, Neisseria meningitidis *, Pasteurella multocida, Proteus mirabilis *, Proteus vulgaris *, types of Salmonella *, types of Shidella *, Vibrio cholerae, Yersinia enterocolitica *;
gram-negative anaeroby:vida of Bacteroides (including Bacteroides fragilis), types of Fusobacterium;
others mikroorganizmy:borrelia burgdorferi, types of Chlamydia, Leptospira icterohaemorrhagiae, Treponema pallidum.
The note * Some representatives of these species of bacteria produce beta lactamazu that does them insensitive to motor-therapy by amoxicillin.
Pharmacokinetics.
Average pharmacokinetic parameters for Amoksila-K of 1,2 g.
Amoxicillin.
Average pharmacokinetic parameters
Amoxicillin Dose Average peak T of ½ h, (period of AUC of h/mg/l ( Vyvedeniye Square
amoxicillin concentration of semi-removal) under a curve with urine
in plasma, mkg/ml "concentration/time") 0-6 h, %
Amoksil-K
1,2 g 1 g 105,4 0,9 76,3 77,4
Clavulanic acid.
Average pharmacokinetic parameters
Klavulanovy Dose klavulanovy Average peak T of ½ h AUC Removal with
acid acid concentration in plasma, mkg/ml of h/mg/l urine of 0-6 h, %
Amoksil-K
1,2 g 200 mg 28,5 0,9 27,9 63,8
Distribution. After introduction therapeutic concentration of amoxicillin and clavulanic acid are observed in fabrics and intersticial liquid. Therapeutic concentration of both substances are found in a gall bladder, tissues of an abdominal cavity, skin, fatty and muscular fabrics; and also in synovial and peritoneal liquids, bile and pus. Amoxicillin and clavulanic acid poorly contact proteins; in researches it is established that indicators of linkng with proteins make 25% for clavulanic acid and 18% for amoxicillin of their general concentration in plasma.
Removal. As well as other penicillin, the main way of removal of amoxicillin is renal excretion whereas a conclusion of clavulanate is carried out also by kidneys, and by extrarenal mechanisms. About 60-70% of amoxicillin and 40-65% of clavulanic acid are allocated with urine in a neizmenyony look for the first 6 hours. Amoxicillin is also partially removed with urine in the form of inactive penicillic acid in the quantities equivalent to 10-25% of the applied dose. Clavulanic acid is considerably metabolized in a human body to 2,5-digidro-4-(2 hydroxyethyl) - 5-oxo-1H-pirol-3-carboxyl acid and 1-amino-4 – hydroxy - butane - 2 - it also is allocated with urine and excrements, and also in the form of carbon dioxide with expired air.
Pharmaceutical characteristics.
Main physical and chemical properties: powder of white or almost white color, hydroscopic.
Incompatibility.
Amoksil-K it is not necessary to mix with blood products, other liquids which supporting squirrels, in particular with hydrolyzates of proteins, and with emulsions of fats for intravenous use.
If Amoksil-K apply along with aminoglycoside, antibiotics should not be mixed in one syringe, capacity for intravenous solution or in other tanks as activity of aminoglycoside is lost.
Indications to use:
Short treatment of the bacterial infections caused by microorganisms, sensitive to Amoksilu-K.
Infections of ENT organs, including recurrent tonsillitis, sinusitis, average otitises.
Lower respiratory tract infections, including exacerbation of chronic bronchitis, lobar and bronchial pneumonia.
Infections of an urinary system, including cystitis, uretrita, pyelonephritises, infections of female generative organs and gonorrhea.
Infections of skin and soft tissues.
Bone and joint infections, including osteomyelites.
Other infections, including intraabdominal sepsis.
Prevention of infectious complications at surgical interventions, in most cases at operative measures on digestive tract, pelvic bodies, the head and a neck, heart, kidneys, when replacing joints and surgery of bilious channels.
The infections caused by amoksitsillinchuvstvitelny microorganisms effectively are treated by Amoksil - To, considering content of amoxicillin in it. Multi-infections which are caused by amoksitsillinnechuvstvitelny microorganisms in combination with amoksitsillinchuvstvitelny microorganisms - producers beta lactamelements - can be treated by Amoksil - To.
Route of administration and doses:
Doses depend on age, weight and function of kidneys at patients, and also on severity of an infection. Doses are specified in units amoxicillin/clavulanate everywhere. Amoksil-To enter intravenously (struyno, slowly, for 3-4 minutes) or kapelno (the infusion period - 30-40 minutes). This Amoksila-form K is not applied to intramuscular injections. Treatment cannot last more than 14 days without assessment of results of use and a clinical picture.
Dosing for adults.
Standard dose: To 1000/200 mg there are each 8 hours.
Heavy infections: To 1000/200 mg there are each 4-6 hours.
Prevention of complications at surgical interventions.
Operation duration <1 h: one dose of 1000/200 mg of drug is entered to anesthesia. Operation duration> 1 h: as it is stated above, and to 4 doses of 1000/200 mg of drug it is entered according to the instruction for 24 hours.
The purpose of use of Amoksil - To at surgical interventions is a protection of the patient for risk of a postoperative infectious complication.
During operation it is necessary to conduct a full course of intravenous or oral administration of Amoksil of a case of emergence of clinical signs of an infection - To later operation.
Renal failure. Correction of dosing is based on the maximum recommended amoxicillin doses.
Clearance of creatinine> 30 ml/min.: amendments of dosing are not necessary.
Clearance of creatinine of 10-30 ml/min.: 1000/200 mg, then 500/100 mg 2 times a day.
The clearance of creatinine <10 ml/min:1000/200 to mg, then 500/100 mg is each 24 hours.
Hemodialysis. Amendments of dosing are based on the maximum recommended amoxicillin doses. The first dose makes 1000/200 mg, then to 500/100 mg there are each 24 hours. Considering need of maintenance of effective concentration, one more dose should be entered after the termination of a hemodialysis.
Abnormal liver function. It is necessary to be careful when dosing, to carry out continuous monitoring of function of a liver with regular intervals. The available recommendations made insufficiently for formation concerning dosing.
Patients of advanced age. Correction is not necessary. If necessary, doses for adults adjust depending on function of kidneys.
Dosing for children.
Dosing for children with body weight to 40 kg depends on weight; the minimum interval of dosing - 4 hours.
Children aged up to 3 months:
The body weight of the child is less than 4 kg: To 25/5 mg/kg there are each 12 hours.
The body weight of the child is more than 4 kg: to 25/5 mg/kg each 8 hours, depending on disease.
Children aged from 3 months up to 12 years:
25/5 mg/kg each 6 - 8 hours, depending on the course of a disease.
Renal failure. Correction of dosing is based on the maximum recommended amoxicillin doses.
Clearance of creatinine> 30 ml/min.: amendments of dosing are not necessary.
Clearance of creatinine of 10-30 ml/min.: 25/5 mg/kg 2 times a day.
Clearance of creatinine <10 ml/min.: 25/5 mg/kg once a day.
Hemodialysis. Amendments of dosing are based on the maximum recommended amoxicillin doses. 25/5 mg/kg once a day. Considering need of recovery of effective system of concentration, one more dose should be entered after the termination of a hemodialysis (25/5 mg/kg/day).
Abnormal liver function. It is necessary to show care when dosing; it is necessary to carry out continuous monitoring of function of a liver with regular intervals. The available data are not enough for recommendations concerning dosing.
Preparation of solution and feature of introduction.
Amoksil - To enter by intravenous injections (struyno) or in the form of periodic infusions (kapelno). Amoksil-To it is impossible to enter intramusculary.
Bottle of 1,2 g: to dissolve contents in 20 ml of water for injections (the final volume of-20,9 ml).
At dissolution there can be a temporary pink coloring which disappears. Amoksila-K solutions usually colourless or have pale straw color.
Intravenous injection. Stability of Amoksila-K solution has concentration dependence therefore medicinal средстро it is necessary to apply right after dissolution and to enter slowly for 3-4 minutes. Amoksil-K it is possible to enter directly into a vein or through a catheter, kapelno.
Intravenous infusion. Amoksil-K it is possible to enter intravenously in the form of infusion in water for injections or into 0,9% chloride sodium solution for injections. To add 1,2 g of solution to 100 ml of liquid for infusion (it is better to apply a mini-container or the burette). To carry out infusion of 30-40 minutes during no more than 4 hours after dissolution. The entered solutions have to be brought to full volume, directly after powder dissolution. The remained solution of an antibiotic cannot be applied.
Stability of the prepared solution. Intravenous infusions of Amoksila-K can be made by means of different intravenous solutions. Satisfactory concentration of an antibiotic remains at 5 °C and at the room temperature (25 °C) in the recommended volumes of the infusion solutions provided below. At dissolution of drug and its stay at the room temperature of infusion have to be made throughout time provided below.
Solution for intravenous (in/in) introductions the stability Period at 25 °C (hours)
Water for injections 4
0,9% chloride 4 sodium solution
Solution of sodium of a lactate 4
The combined solution
chloride sodium (Ringer's solution) 3
The combined sodium lactate solution
(Hartman's solution) 3
Solution of potassium of chloride and sodium of chloride 3
Stability of Amoksila-K solutions depends on concentration. If solution prepares bigger concentration, the period of stability of solution in proportion increases. At storage at a temperature of 5 °C solution 1000/200 of mg can be added to previously cooled solution for infusion (in a plastic sterile container), the received drug can be stored at the specified temperature till 8 o'clock.
Solution for intravenous infusions the stability Period at 5 °C (hours)
Water for injections 8
0,9% chloride 8 sodium solution
When heating to room temperature solution should be used immediately. Amoksil-K is less stable in solutions of glucose, a dextran and bicarbonate. Solutions on the specified basis need to be used for 3-4 minutes after dissolution.
Any unused solution should be destroyed.
Amoksil-K it is not expected the multidose mode of use.
Features of use:
Before therapy of Amoksilom-K it is necessary to define carefully existence in the anamnesis of reaction of hypersensitivity to penicillin, cephalosporins or other allergens. Serious, and from time to time even fatal cases of hypersensitivity (anaphylactic reactions) are observed at patients during therapy by penicillin. These reactions it is more probable at persons with similar reactions to penicillin in the past. In case of allergic reactions it is necessary to stop therapy of Amoksilom-K and to begin the corresponding alternative therapy. Serious anaphylactic reactions demand immediate treatment using adrenaline. Also perhaps as necessary use of an oxygenotherapy, intravenous administration of steroids and the managed breath, including an intubation. Amoksil-K it is necessary to cancel at suspicion on an infectious mononucleosis as emergence at this disease of root-shaped rash can be connected with amoxicillin reception. Long administration of drug can also sometimes serve as the reason of activation insensitive to Amoksilu-K of microflora.
Occasionally at patients who accept Amoksil-K and peroral anticoagulants lengthening a lot of prothrombin time (increase in level of the international normalized ratio (INR)) can be observed. At a concomitant use of anticoagulants the corresponding monitoring is necessary. Dose adjustment of peroral anticoagulants can be necessary for maintenance of necessary level of anti-coagulation.
Amoksil-K patients should appoint with care with liver dysfunction. Correction of dosing according to extent of these disturbances is necessary for patients with renal failures.
Presence of clavulanic acid in Amoksile-K can cause not specific binding of IgG and albumine on membranes of erythrocytes and as a result false positive reaction of Koombs.
In need of parenteral administration of high doses of drug it is necessary to pay attention to the content of sodium in solutions at treatment of patients who are on a natriykontroliruyemy diet.
Patients with an oligouriya very seldom can have a crystalluria, mainly at parenteral administration of drug. Therefore at use of high doses of amoxicillin adequate reception of liquid and control of an otkhozhdeniye of urine for the purpose of reduction of possibility of a crystalluria of amoxicillin is recommended.
Ability to influence speed of response at control of motor transport or work with other mechanisms. Negative influence on ability to manage motor transport or to work with other mechanisms was not observed.
Side effects:
Side effects were classified by the frequency of their emergence - from very frequent to very rare. Frequency of other side effects (for example, with a frequency <1 on 10 000) displays the frequency of receipt of data on side effect, than frequency of their emergence more.
Such classification of frequency of emergence of side effects is applied:
very often (≥ 1/10),
often (≥ 1/100 and <1/10),
infrequently (≥ 1/1000 and <1/100),
seldom (≥ 1/10 000 and <1/1000),
very seldom (<1/10).
Infections and invasions.
Often - candidiasis of skin and mucous membranes.
Circulatory and lymphatic systems.
Seldom - the return leukopenia (including a neutropenia) and thrombocytopenia.
Very seldom - the return agranulocytosis and hemolitic anemia. Increase in a bleeding time and prothrombin ratio.
Immune system.
Very seldom – a Quincke's disease, an anaphylaxis, the syndrome similar to a serum disease, an allergic vasculitis.
Nervous system.
Infrequently - dizziness, a headache.
Very seldom - spasms. Spasms can arise at patients with an impaired renal function or at those who receive high doses of drug.
Vascular disorders.
Seldom – thrombophlebitis in a drug injection site.
Gastrointestinal reactions.
Often - diarrhea.
Infrequently - nausea, vomiting, digestion disturbance.
Very seldom – antibiotikoassotsiirovanny colitis (including pseudomembranous colitis and hemorrhagic colitis) which probability of emergence is much lower at parenteral administration of drug.
Gepatobilliarny reactions.
Infrequently - moderate increase in level of nuclear heating plant and/or ALT is noted at patients who are treated beta лактамными by antibiotics.
Very seldom - hepatitises and cholestatic jaundice. These phenomena arise at use of other penicillin and cephalosporins.
Hepatitises arise, mainly, at men and patients of advanced age, their emergence can be connected with long treatment by drug. Signs and symptoms of a disease arise in time or right after treatment, but in certain cases can arise in several weeks after the end of treatment. These phenomena usually have the return character. Very seldom lethal cases which always happen at patients to a serious basic disease or at patients who are at the same time treated by the drugs which are negatively influencing a liver take place.
Skin and hypodermic fabrics.
Infrequently – skin rash, an itch, a small tortoiseshell.
Seldom - a polymorphic erythema.
Very seldom – Stephens-Johnson's syndrome, a toxic epidermal necrolysis, bubbly exfoliative dermatitis, acute generalized exanthematous пустулёз.
In case of any allergic dermatitis treatment should be stopped.
Kidneys and urinary system.
Very seldom – intersticial nephrite, a crystalluria.
Interaction with other medicines:
Simultaneous use with probenetsidy is not recommended. Probenetsid reduces renal canalicular secretion of amoxicillin. Simultaneous use of Amoksila-K can lead to increase in level in amoxicillin blood, is long, but not clavulanic acid.
The concomitant use of Allopyrinolum during treatment by amoxicillin can increase probability of allergic reactions from skin. There are no data about simultaneous use of Amoksila-K and Allopyrinolum.
As well as other antibiotics, Amoksil-K influences intestines flora that leads to reduction of a reabsorption of estrogen and reduction of efficiency of the combined peroral contraceptive means.
There are separate messages on increase in the INR level at patients who are treated atsenokumaroly or warfarin and accept amoxicillin. In need of such use it is necessary to control carefully a prothrombin time or the INR level with addition or cancellation of Amoksila-K.
Contraindications:
Hypersensitivity to beta lactams, including to penicillin and cephalosporins. Existence in the anamnesis of jaundice/dysfunction of a liver which are connected using Amoksil - To.
Overdose:
The overdose can be followed by symptoms from digestive tract and disturbances of water and electrolytic balance. The specified symptoms treat symptomatic, with special attention to correction of water and electrolytic balance.
The amoxicillin crystalluria can be observed that in certain cases can lead to a renal failure. There are messages on amoxicillin precipitation in an uric catheter at intravenous administration of Amoksila-K in high doses. It is necessary to check its passability regularly.
Amoksil-K it can be brought out of a blood-groove by a hemodialysis method.
Use during pregnancy or feeding by a breast.
It is necessary to avoid use of Amoksila-K during pregnancy, except for situations when the advantage of use of drug for mother prevails over potential risk for a fruit.
Amoksil-K it can be applied during feeding by a breast. Excepting the risk of development of hypersensitivity connected with allocation of trace quantities in breast milk any harmful effects for the child who is on breastfeeding no.
Children. Apply at children as it is described in the section "Route of Administration and Doses".
Storage conditions:
Period of validity 1 year. To store in original packaging, at a temperature not over 25 ºС. To store in the place, unavailable to children.
Issue conditions:
According to the recipe
Packaging:
On 1,2 g in bottles. 1 or 10 bottles in a pack.
