Амиклав
Producer: JSC Himfarm Republic of Kazakhstan
Code of automatic telephone exchange: J01CR02
Release form: Firm dosage forms. Powder for suspension preparation.
General characteristics. Structure:
Powder for preparation of 100 ml of peroral suspension, 156,25 mg / 5 ml and 312,5 mg / 5мл, 25 g.
Active agents:
mix of amoxicillin of 3597.0 mg 7194.0 mg
Pharmacological properties:
Pharmacokinetics. Amoxicillin and clavulanic acid are well dissolved in aqueous solutions with physiological value рН, quickly and completely soaked up from digestive tract after oral administration. Absorption of amoxicillin and clavulanic acid increases in case of administration of drug at the beginning of food. After administration of drug in its bioavailability makes 70%. Therapeutic concentration of amoxicillin and clavulanic acid are reached in lungs, abdominal organs, fatty, bone and muscular fabrics, pleural, synovial and peritoneal liquids, skin, bile, urine, purulent separated, a phlegm. Linkng of amoxicillin and clavulanic acid with proteins of plasma low also makes 25% of total quantity of clavulanic acid and 18% of amoxicillin. Amoxicillin, and also trace amounts of clavulanic acid get into breast milk. Amoxicillin and clavulanic acid get through a placental barrier.
Amoxicillin is removed, mainly, by kidneys whereas clavulanic acid - by means of both renal, and extrarenal mechanisms. Amoxicillin is partially emitted with urine in the form of inactive penicillic acid in the quantity equivalent to 10-25% of the accepted dose. Clavulanic acid in an organism is exposed to intensive metabolism to 2,5-digidro-4-(2 hydroxyethyl) - 5-oxo-1H-pyrrol-3-carboxylic acid and 1 - amino - 4 - hydroxy - butane - 2 - it also is allocated with urine and a stake, and also in the form of carbon dioxide through expired air.
Pharmacodynamics. Амиклав® is the combined antibiotic containing amoxicillin and clavulanic acid with a wide range of bactericidal action, steady against a beta laktamaze. Amoxicillin is a semi-synthetic antibiotic of a broad spectrum of activity, active concerning many gram-positive and gram-negative microorganisms. Amoxicillin collapses under the influence of a beta laktamaz and does not affect microorganisms which produce this enzyme. The mechanism of effect of amoxicillin consists in inhibition of biosynthesis of peptidoglikan of a cell wall of a bacterium. Clavulanic acid is beta лактамат, on chemical structure close to penicillin which has ability to inactivate enzymes beta лактамаз, that preventing an amoxicillin inactivation. Beta лактамазы are produced by many gram-positive and gram-negative bacteria. Action beta лактамаз can lead to destruction of some antibacterial drugs even prior to their impact on pathogens. Clavulanic acid blocks effect of enzymes, recovering sensitivity of bacteria to amoxicillin. In particular, it has high activity concerning plasmid beta лактамаз with which medicinal resistance is often connected, but is less effective concerning chromosomal beta лактамаз 1 type.
Presence of clavulanic acid at structure of Amiklava® protects amoxicillin from the destroying action beta лактамаз and expands its range of antibacterial activity with inclusion in it of microorganisms, usually resistant to other penicillin and cephalosporins. Clavulanic acid in the form of monodrug does not render clinically significant antibacterial effect. Амиклав® has bactericidal effect on the following microorganisms: gram-positive aerobes: Enterococcus faecalis, Gardnerella vaginalis, Staphylococcus aureus (sensitive to Methicillinum), a coagualase - negative stafilakokk (sensitive to Methicillinum), Streptococcus agalactiae, Streptococcus pneumoniae1, Streptococcus pyogenes and other beta and hemolitic streptococci, the group Streptococcus viridans, Enterococcus faecium *; gram-negative aerobes: Capnocytophaga species, Eikenella corrodens, Haemophilus influenzae, Moraxella catarrhalis (Branhamella catarrhalis), Pasteurella multocida, Escherichia coli *, Klebsiella oxytoca *, Klebsiella pneumoniae *, Proteus mirabilis *, Proteus vulgaris *; anaerobe bacterias: Bacteroides fragilis, Fusobacterium nucleatum, Prevotella species.
Microorganisms with natural resistance: gram-negative aerobes: Acinetobacter species, Citrobacter freundii, Enterobacter species, Legionella pneumophila, Morganella morganii, Providencia species, Pseudomonas species, Serratia species, Stenotrophomonas maltophilia; others: Chlamydophila pneumoniae, Chlamydophila psittaci, Coxiella burnetti, Mycoplasma pneumoniae.
* Some strains of these species of bacteria can be insensitive to monotherapy amoxicillin.
1 – an exception of strains of Streptococcus pneumoniae which resistance is not connected with development beta лактамаз.
Indications to use:
- infections of ENT organs (bacterial sinusitis, tonsillitis, acute average otitis);
- respiratory infections (acute, chronic bronchitis, community-acquired pneumonia);
- infections of a gall bladder and biliary tract (cholecystitis, cholangitis);
- infections of urinary tract (cystitis, pyelonephritis);
- gynecologic infections;
- infections of skin and soft tissues (in particular, cellulitis, stings of animals, acute abscesses and phlegmons of maxillofacial area);
- infections of bones and joints (in particular, osteomyelitis).
Route of administration and doses:
The mode of dosing is set individually depending on age, body weight, and also from severity of an infection. Амиклав® it is recommended to accept at the beginning of food.
Daily dosages of suspension of 228,5 mg / 5мл and 457 mg / 5мл (for simplification of the correct dosing the measured (dosing) spoon with a capacity of 5 ml invests in each packaging of suspensions).
|
Age patient / Recommended dose |
228,5 mg / 5мл |
457 mg/ml |
|
Children from 3 months to 1 year |
¼ measured spoons (1,25 ml) 4 times a day |
|
|
Children from 1 year to 2 years |
on ½ measured spoons (2,5 ml) 3 times a day |
¼ measured spoons (1,25 ml) 2 times a day |
|
Children from 2 to 7 years
|
on 1 measured spoon (5 ml) 2 times a day |
on ½ measured spoons (2,5 ml) 2 times a day |
|
Children from 7 to 14 years
|
on 2 measured spoons (10 ml) 2 times a day |
on 1 measured spoon (5 ml) 2 times a day |
The maximum daily dose of amoxicillin makes 45 mg/kg of body weight for children. The maximum daily dose of clavulanic acid (in the form of potassium salt) makes 10 mg/kg of body weight for children. The course of treatment makes 5-10 days. It is not necessary to continue treatment more than 10 days without repeated assessment of a condition of the patient. Administration of drug is not recommended to children aged 3 months are younger.
Features of use:
Before an initiation of treatment of Amiklavom® it is necessary to collect the detailed anamnesis concerning the previous reactions of hypersensitivity to penicillin, cephalosporins or others beta лактамные antibiotics.
Also fatal reactions of hypersensitivity (acute anaphylaxis) on penicillin are described serious, and sometimes. In case of allergic reaction it is necessary to stop treatment of Amiklavom® and to begin alternative therapy.
Амиклав® it is not necessary to appoint at suspicion to an infectious mononucleosis as with this disease amoxicillin can cause skin rash in patients that complicates diagnosis of a disease.
Prolonged treatment of Amiklavom® can be followed by growth of resistant microorganisms.
Antibiotiko-assotsiirovanny pseudomembranous colitis can develop at reception of any antibiotics and vary on severity from easy to life-threatening. Thus, it is necessary to consider this diagnosis at patients who have a diarrhea in time or after reception of antibiotics. At emergence of the antibiotiko-associated colitis of Amiklav® it is necessary to cancel and begin the corresponding treatment immediately.
In general, Amiklav® is transferred well and possesses a hypotoxicity inherent to all penicillin. At treatment of Amiklavom® more than 7 days it is recommended to estimate functions of kidneys, a liver, bodies of a hemopoiesis.
At the patients receiving Amiklav® increase in a prothrombin time therefore at simultaneous use of Amiklava® and anticoagulants it is necessary to carry out the corresponding monitoring is occasionally observed.
With care it is necessary to apply Amiklav® at patients with an abnormal liver function.
Patients with a reduced diuresis in rare instances can have a crystalluria. During introduction of high doses of amoxicillin it is recommended to accept enough liquid and to support an adequate diuresis for reduction of probability of formation of crystals of amoxicillin.
Presence of clavulanic acid at Amiklave® can be the cause of nonspecific binding of IgG and albumine with a membrane of erythrocytes that leads to the false positive test of Koombs.
Purpose of drug at pregnancy is possible when the estimated advantage for mother exceeds potential risk for a fruit.
Considering side effects which can take place at administration of drug (dizziness) it is necessary to be careful when driving or potentially dangerous mechanisms.
Side effects:
Often (≥1/100, <1/10):
- candidiasis;
Infrequently (≥1/1000, <1/100):
- dyspepsia;
- moderate increase in level of liver enzymes;
- skin rash, itch, small tortoiseshell.
Seldom (≥1/10000, <1/1000):
- a reversible leukopenia (including a neutropenia), thrombocytopenia;
- multiformny erythema.
It is unknown:
- reversible agranulocytosis and hemolitic anemia, increase in a bleeding time and index of a prothrombin time;
- Quincke's disease, anaphylaxis; syndrome similar to a serum disease, allergic vasculitis;
- reversible superactivity and spasms;
- pseudomembranous or hemorrhagic colitis;
- change of coloring of a blanket of an adamantine substance of tooth;
- hepatitis, cholestatic jaundice;
- Stephens-Johnson's syndrome, toxic epidermal necrolysis, violent exfoliative dermatitis, acute generalized exanthematous пустулёз;
- intersticial nephrite, crystalluria.
Interaction with other medicines:
Clavulanic acid does not influence amoxicillin absorption.
It is not recommended to apply Amiklav® along with probenitsidy. Probenitsid reduces canalicular secretion of amoxicillin that can lead to increase in amoxicillin level blood.
At simultaneous use of Amiklava® and indirect peroral anticoagulants strengthening of action of the last is possible. In need of joint appointment control of a prothrombin time and dose adjustment of anticoagulants is recommended.
Simultaneous use of Allopyrinolum and Amiklava® can increase risk of emergence of allergic reactions.
Amoxicillin at joint appointment with a methotrexate can reduce its removal from an organism and increase toxicity.
Contraindications:
- hypersensitivity to penicillin or to any component of drug;
- the known hypersensitivity to others beta лактамным to antibiotics (cephalosporins, karbapenema, monobaktama);
- the jaundice or an abnormal liver function which developed against the background of use of Amiklava® or beta лактамных antibiotics;
- infectious mononucleosis, lymphoid leukosis;
- lactation period.
Overdose:
Symptoms: nausea, diarrhea, vomiting, disturbances of water and electrolytic balance.
Treatment: drug withdrawal, gastric lavage, reception of absorbent carbon, symptomatic therapy, correction of water and electrolytic balance. Амиклав® it is brought out of blood by means of a hemodialysis.
Storage conditions:
To store in the dry, protected from light place, at a temperature not above 25 °C.
After dilution by water to store suspension in the refrigerator within 7 days.
To store in the place, unavailable to children!
Issue conditions:
According to the recipe
Packaging:
On 25 g of drug for preparation of 100 ml of peroral suspension in the bottles with a mark of 100 ml corked by the screwed metal caps with a control ring.
On each bottle paste the label from paper label or writing.
On 1 bottle place in a pack from a cardboard for a retail container. Put the approved instructions on a medical use of drug in packs in the state and Russian languages and a dosing spoon.
