Амиклав®

General characteristics. Structure:

Active agents: amoxicillin (in the form of trihydrate amoxicillin) 125 mg 250 mg, clavulanic acid (in the form of clavulanate potassium) 31,25 mg 62,5 mg.

Excipients: Natrium benzoicum, sodium citrate, anhydrous citric acid, sodium alginate, silicon dioxide colloid, fragrance dry orange, cellulose microcrystallic, sodium of a karmelloz, sugar.

Pharmacological properties:

Pharmacokinetics. In general pharmacokinetic parameters of clavulanic acid and amoxicillin are similar at the combined use therefore they have no mutual influence on pharmacokinetic properties of each separately taken substance.

After intake amoxicillin and clavulanic acid are quickly absorbed from digestive tract. Reception of Amiklava® during food does not exert impact on absorption. The maximum concentration is reached in blood in 1 h after reception. High concentration of active agents are found in plasma, a phlegm, a bronchial secret, pleural liquid, lung tissue, a prostate, fatty tissue. Active agents do not get through a blood-brain barrier at an uninflammed meninx, get through a placental barrier. Clavulanic acid and amoxicillin also contact proteins of a blood plasma, respectively, for 22–30% and 17–20%.

The elimination half-life makes 1-1,5 h. The main way of removal from an organism – with urine, some part is removed with a stake or with expired air.

Pharmacodynamics. Амиклав® - the antibiotic of a broad spectrum of activity, contains semi-synthetic penicillin amoxicillin and inhibitor beta лактамаз clavulanic acid. Clavulanic acid inhibits the majority clinically significant beta лактамаз (types 2, 3, 4 and 5 – on classification of Richmond of Sykes), the produced Staphylococcus spp., Escherichia coli, Proteus mirabilis, Haemophilus influenzae, Moraxella catarrhalis, Bacteroides spp.

This combination provides high bactericidal activity of Amiklava®, including concerning strains of microorganisms, resistant to amoxicillin. Clavulanic acid, having higher affinity to a beta - a laktamaza, than amoxicillin, forms the stable deactivated complex with enzyme, interfering with enzymatic degradation of amoxicillin under action a beta – лактамаз.

Амиклав® affects bakteritsidno a wide range of gram-positive and gram-negative bacteria (including strains which gained resistance to a beta laktamnym to antibiotics owing to products beta лактамаз).

Амиклав® it is active concerning aerobic gram-positive bacteria: Streptococcus spp. groups A, B, C, G, Enterococcus faecium, Staphylococcus aureus (except metitsillinrezistentny strains), Staphylococcus epidermidis (except metitsillinrezistentny strains), Corynebacterium spp., Listeria monocytogenes, Nocardia asteroides; aerobic gram-negative bacteria: Aeromonas spp., Bordetella pertussis, Brucella spp., Campylobacter jejuni, Campylobacter coli, Citrobacter spp., Escherichia coli, Gardnerella vaginalis, Haemophilus ducreyi, Haemophilus influenzae, Helicobacter pylori, Klebsiella spp., Legionella pneumophila, Moraxella catarrhalis, Morganella spp., Neisseria gonorrhoeae, Neisseria meningitidis, Proteus mirabilis, Salmonella spp., Shigella spp., Vibrio cholerae, anaerobic bacteria: Actinomyces israelii, Bacteroides spp., Clostridium spp., Peptostreptococcus spp., Treponema pallidum.

Indications to use:

- acute and chronic sinusitis, tonsillitis, pharyngitis;

- chronic bronchitis, pneumonia, pleura empyema;

- acute and chronic otitis;

- cystitis, urethritis, pyelonephritis;

- salpingitis, salpingo-oophoritis, endometritis, pelviperitonitis;

- infections of skin and soft tissues (including phlegmon, wound fever);

- infections of bones and joints (including chronic osteomyelitis);

- cholecystitis, cholangitis.

Route of administration and doses:

The mode of dosing is set individually depending on age, body weight, function of kidneys, and also from severity of an infection. Амиклав® it is recommended to accept at the beginning of food. It is not necessary to continue treatment more than 10 days without repeated assessment of a condition of the patient.

To children aged from 3 months till 1 year – on ½ teaspoons (2,5ml) time suspensions 156,25mg/5ml 3 in days; from 1 year to 7 years – on 1 teaspoon (5 ml) of time suspension 156,25mg/5ml 3 a day or on ½ teaspoons (2,5ml) time suspensions 312,5mg/5ml 3 in days; from 7 to 14 years – on the 2nd teaspoons (10 ml) of time suspension 156,25mg/5ml 3 in days (each 8 hours) or on 1 teaspoon (5 ml) of time suspension 312,5mg/5ml 3 a day (each 8 hours). The dose for intake makes 20-40 mg/kg/days (counting on amoxicillin), depending on weight of an infection (divided into 3 receptions). Duration of treatment is 7-10 days.

Patients with a renal failure. At insufficiency of functions of kidneys with the level of clearance of creatinine of 10 ml/min. and less dosage of Amiklava® is adjusted or increase an interval between administration of drug. At an anury the interval between reception can make 48 hours.

At clearance of creatinine of 80 ml/min. and more interval between reception of Amiklava® makes 8 hours, at clearance of 80-50 ml/min. – 8 hours, at clearance of 50-10 ml/min. – 12 hours, at clearance of 10 ml/min. and less than 0th 24 hours.

Way of preparation of suspension. To fill in a bottle with powder with water half and to shake up carefully. Then to add water to a mark of 100 ml and again to shake up before receiving suspension. To use the prepared suspension within 7 days at storage in the refrigerator.

To shake up contents of a bottle before each use.

Features of use:

Амиклав® with care appoint to the patients inclined to allergic reactions to cephalosporins and others beta лактамные antibiotics (risk of development of cross sensitivity).

Care is necessary at appointment for patients with heavy abnormal liver functions and kidneys (adequate dose adjustment or increase in intervals between reception is required).

Pregnancy and lactation. This dosage form is intended for children. 

This dosage form is intended for children.

Side effects:

- nausea, vomiting, dyspepsia, diarrhea.

Seldom:

- pseudomembranous colitis;

- itch, skin rashes, urticaria, Quincke's disease, bronchospasm, acute anaphylaxis;

- development of superinfection (stomatitis, mycotic vulvovaginitis);

- agitation, alarm, headache, dizziness, inadequate behavior, sleeplessness, spasms, confusion of consciousness, hyperactivity;

- thrombocytopenia, anemia (including cases of hemolitic anemia), a leukopenia, an eosinophilia, an agranulocytosis.

Extremely seldom:

- tranzitorny increase in activity of hepatic transaminases, cholestatic jaundice, hepatitis, abnormal liver functions;

- meteorism, anorexia, gastritis, glossitis, coloenteritis, stomatitis or discoloration of language;

- multiformny erythema, exfoliative dermatitis, Stephens's syndrome;

- Johnson, toxic epidermal necrolysis;

- hamaturia and intersticial nephrite.

Interaction with other medicines:

Clavulanic acid does not influence amoxicillin absorption.

At simultaneous use of Amiklava® and indirect anticoagulants there is strengthening of action of the last.

Simultaneous use of Amiklava® with Disulfiramum, Allopyrinolum, a methotrexate increases risk of development of their side effects. Efficiency of Amiklava® is weakened by a combination with bacteriostatic antibiotics (macroleads, tetracyclines), the combination with rifampicin – is antagonistic.

It is incompatible with aminoglycosides.

Probenetsid reduces amoxicillin removal, increasing its serumal concentration.

Contraindications:

- hypersensitivity to drug components;

- liver failure;

- the cholestatic jaundice or hepatitis caused by reception of antibiotics of group of penicillin in the anamnesis;

- infectious mononucleosis, lymphoid leukosis.

Overdose:

Symptoms: in most cases nausea, diarrhea, vomiting, are possible – excitement, sleeplessness, dizziness, in certain cases – convulsive attacks.

Treatment: symptomatic, in case of recent reception (less than 4 h) to remove drug from digestive tract (a gastric lavage, reception of absorbent carbon for absorption reduction). The hemodialysis is effective.

Storage conditions:

To store in the dry, protected from light place, at a temperature not above 25 °C.

To use the prepared suspension within 7 days at storage in the refrigerator.

To store in the place, unavailable to children!

Issue conditions:

According to the recipe

Packaging:

Powder for preparation of peroral suspension on 25 g in the bottles of 100 ml corked by the screwed metal caps.

On 1 bottle place in a pack from a cardboard, put the approved instructions on a medical use of drug in the state and Russian languages and dosing spoons.