Amoksitsillin-FT

General characteristics. Structure:

Active ingredient: 125 mg, 250 mg, 500 mg. 750 mg and 1000 mg of amoxicillin (in the form of trihydrate amoxicillin).

Excipients: povidone, sodium stearate, cellulose microcrystallic krakhmalglikolit (type A), magnesium.

Antibiotic of group of semi-synthetic penicillin of a broad spectrum of activity.

Pharmacological properties:

Pharmacodynamics. Amoxicillin is an antibiotic of group of semi-synthetic penicillin of a broad spectrum of activity. Represents a 4-hydroxylic analog of ampicillin. Pharmacodynamics. Possesses bactericidal action as a result of inhibition of synthesis of a bacterial cell wall. It is active concerning aerobic gram-positive bacteria: Staphylococcus spp. (except for the strains producing a penicillinase), Streptococcus spp; aerobic gram-negative bacteria: Neisseria gonorrhoeae, Neisseria meningitidis, Escherichia coli, Shigella spp. Salmonella spp., Klebsiella spp.

Threshold MIC values for various sensitive organisms vary. Enterobacteriaceae is considered to be sensitive at their inhibition amoxicillin in concentration <8 mkg/ml of amoxicillin and resistant at concentration> 32 mkg/ml.

According to recommendations of NCCLS and when using NCCLS-of the specified catarrhalis methods M. (beta лактамаза negative) and N. influenzae (beta лактамаза negative) are regarded as sensitive at concentration <1 mkg/ml and resistant at> 4 mkg/ml; Str. pneumoniae are considered sensitive at MIC <2 mkg/ml and resistant at> 8 mkg/ml.

Bacteria can have resistance to amoxicillin as a result of products beta лактамаз, hydrolyzing aminopenicillin, changes penicillin - the connecting proteins, disturbance of permeability for drug or thanks to functioning of the special pompovy pumps extorting drug from a cell. At one microorganism there can be at the same time several mechanisms of resistance that explains existence of variable and unpredictable cross resistance to other beta lactams and antibacterial drugs from other groups.

Pharmacokinetics. Absorption: Absolute bioavailability of amoxicillin depends on a dose and the mode of introduction and is ranging from 75 to 90%. In doses from 250 mg to 750 mg bioavailability (parameters: AUC and/or allocation with urine) is proportional (linearly) to a dose. In higher doses absorbability lower. At intake amoxicillin is quickly and completely absorbed from a GIT, does not collapse in acid medium of a stomach. At increase in a dose of reception twice concentration in blood also increases twice. At an oral single dose of 500 mg concentration of amoxicillin in blood makes 6-11 mg/l. After a single dose of 3 g of amoxicillin concentration in blood reaches 27 mg/l. Amoxicillin Cmax in a blood plasma is reached in 1-2 h. Presence of food at a stomach does not reduce the general absorption. Irrespective of a way of introduction (in/in, in oil or intake) in blood similar concentration of amoxicillin are reached.

Distribution: Linkng of amoxicillin with proteins of plasma makes about 20%. It is widely distributed in fabrics and liquids of an organism. It is reported about high concentration of amoxicillin in a liver. Therapeutic concentration of drug is quickly reached in plasma, lungs, a bronchial secret. to liquid of a middle ear, bile and urine. Amoxicillin can get through the inflamed meninx into cerebrospinal liquid. Amoxicillin passes through a placenta and in a small amount it is found in breast milk.

Biotransformation and elimination: As the main place of removal of amoxicillin serve kidneys. About 60 - 80% of a peroral dose of amoxicillin are allocated within 6 hours after reception in not changed active form through kidneys. At a dose of 250 mg concentration of amoxicillin in urine makes more than 300 mkg/ml. The small fraction of amoxicillin is excreted with bile. Some of its quantity is defined in Calais. About 7-25% of a dose are metabolized to inactive penitsillovy acid. Plasma elimination half-life (T1/2) at patients with not changed function of kidneys makes 1-1,5 hours. At newborns and elderly people of T1/2 can be longer. At patients with a heavy renal failure the elimination half-life varies from 5 to 20 hours.

Amoxicillin from a blood plasma is removed by a hemodialysis.

Indications to use:

- infectious diseases of upper parts of respiratory tracts and ENT organs;
- infectious diseases of lower parts of respiratory tracts (acute and chronic bronchitis, pneumonia, lung abscesses, initial stages or incubation interval of whooping cough);
- infectious diseases of bodies of urinogenital system (acute and chronic pyelonephritises, pyelites, prostatitis, an epididymite, cystitis, an urethritis, an asymptomatic bacteriuria during pregnancy);
- gonorrhea;
- gynecologic infections (septic abortion, adnexitis, endometritis);
- a typhoid and a paratyphoid, including complicated by a septicaemia (in a combination with aminoglycosides);
- salmonellonositelstvo;
- shigellosis;
- infectious diseases of bilious ways (a cholangitis, cholecystitis) in case of lack of a cholestasia;
- infectious diseases of skin and soft tissues;
- hay fever;
- acute and latent listeriosis.

Medicine is also applied for short-term (24-48 h) prevention of infectious complications during small surgical interventions.

Medicine is used also at treatment of an infectious endocarditis (in combination with aminoglycosides), meningitis, a septicaemia in case parenteral antimicrobic therapy is not required.

Route of administration and doses:

AMOKSITSILLIN-FT is appointed inside irrespective of meal. The single dose at adults and children is more senior than 10 years (with body weight more than 40 kg) makes on 0.5 g 3 times a day; at the heavy course of an infection on 0.75-1 g 3 times a day. To children aged from 5 up to 10 years appoint 0:25 g 3 times a day; from 3 to 5 years on 0.125 g 3 times a day. At children 3 years are younger use of drug in the form of tablets is complicated. The daily dose for adults (including patients of advanced age) fluctuates from 750 mg to 3 g (at most 6 g) of amoxicillin in stages. At children 3 years a daily dose are more senior makes 25 - 60 mg/kg/days in stages (at most 100 mg/kg/days) depending on the indication and disease severity. Higher doses are recommended to patients at the combined infection, chronic diseases, a recurrence and infections of a heavy current. For adults and children the interval between receptions makes 8 hours, but can increase till 12 o'clock.

Children with body weight over 40 kg have to receive an adult dose. The course of treatment averages 5-12 days. Treatment should be continued within 2-3 days after disappearance of clinical displays of a disease. The streptococcal infections caused β - a hemolitic streptococcus, for a full eradikation of a pathogenic microorganism it is necessary to treat not less than 10 days for the prevention of complications (WHO recommendation).

At uncomplicated infections of lower parts of urinary tract the short course of therapy with double administration of drug on 3 g is appointed to each introduction with an interval between doses of 10-12 hours. At a renal failure such short courses of therapy (3 g) are contraindicated. At treatment of acute uncomplicated gonorrhea in a combination with probenetsidy appoint AMOKSITSILLIN-FT once in a dose of 3 g; at treatment of women repeated reception of the specified dose in 10-12 hours is recommended. At GIT acute infectious diseases (paratyphus, a typhoid, etc.) and bilious ways with high temperature, at gynecologic infectious diseases the adult appoint 1.5-2 g 3 times a day or on 1-1.5 g 4 times a day, at a hay fever - on 0.5-0.75 g 4 times a day within 6-12 days, at a salmonellonositelstvo - on 1.5-2 g 3 times a day during 2-4 weeks. For prevention of an endocarditis at small surgical interventions adult appoint 3-4 g for 1 h before holding a procedure and if necessary appoint a repeated dose in 8-9 hours. For N.'s eradikation of pylori it is recommended to adults on 1 g twice (in 12 hours, "triple" to therapy) or three times a day (in 8 hours, "double" to therapy) for 14 days. At children up to 10 years in all listed above cases the dose has to be twice less.

Patients with a renal failure need to adjust a dose and an interval between introductions according to the CC (clearance of creatinine) values. At KK of 10-40 ml/min. the interval between receptions should be increased till 12 o'clock, at KK less than 10 ml/min. the interval between receptions has to make 24 h. At an anury — the maximum dose of 2 g/days. Change of a dose at infections of uric ways is not required.

Features of use:

With care apply at the patients inclined to allergic reactions. Use of AMOKSITSILLIN-FT (as well as other antibiotics) is inefficient at treatment of acute respiratory viral infections.

Against the background of a combination therapy with metronidazole it is not recommended to take alcohol

In the presence of heavy frustration from digestive tract with diarrhea and vomiting it is not necessary to apply AMOKSITSILLIN-FT as these states can reduce its absorbability. Purpose of a parenteral form of amoxicillin is recommended to such patients.

When determining availability of glucose in urine against the background of therapy amoxicillin recommends to use enzymatic glyukozoksidantny methods. When using chemical methods high concentration of amoxicillin in urine can be the cause of frequent false positive results of a research.

Management of transport and mechanisms. Special researches concerning influence of amoxicillin on ability to manage motor transport and mechanisms were not conducted.

Pregnancy and lactation. Amoxicillin gets through a placental barrier, and in small amounts is emitted with breast milk. In need of use of amoxicillin at pregnancy it is necessary to weigh carefully expected advantage of therapy for mother and potential risk for a fruit. With care to apply amoxicillin in the period of a lactation (breastfeeding). In need of purpose of drug in the period of a lactation it is necessary to stop breastfeeding.

Side effects:

Allergic reactions: small tortoiseshell, erythema, Quincke's edema, rhinitis, conjunctivitis; seldom - fever, joint pains, an eosinophilia; in isolated cases - an acute anaphylaxis. The effects connected with chemotherapeutic action: development of superinfections is possible (especially at patients with chronic diseases or the lowered resistance of an organism).

At prolonged use in high doses: dizziness, ataxy, confusion of consciousness, depression, peripheral neuropathies, spasms.

Preferential at use in a combination with metronidazole: nausea, vomiting, anorexia, diarrhea, a lock, pains in epigastriums, a glossitis, stomatitis; seldom – hepatitis, pseudomembranous colitis, allergic reactions (a small tortoiseshell, a Quincke's disease), intersticial nephrite, disturbances of a hemogenesis.

Preferential at use in a combination with clavulanic acid: cholestatic jaundice, hepatitis; seldom - a mnogoformny erythema, a toxic epidermal necrolysis, exfoliative dermatitis.

Interaction with other medicines:

Use of amoxicillin can lead to tranzitorny reduction of concentration of estrogen and progesterone in blood and to reduce efficiency of the contraceptives accepted inside. In this regard it is recommended for the period of treatment by amoxicillin in addition to use other non-hormonal methods of contraception.

At simultaneous use of amoxicillin with bactericidal antibiotics (including aminoglycosides, cephalosporins. Cycloserinum, Vancomycinum, rifampicin) show a synergism; with bacteriostatic antibiotka (including macroleads, chloramphenicol, linkozamida, tetracyclines, streptocides) - antagonism. Amoxicillin strengthens effect of indirect anticoagulants, suppressing intestinal microflora, reduces synthesis of vitamin K and a prothrombin ratio. At purpose of anticoagulants together with amoxicillin monitoring of homeostatic indicators is required.

Amoxicillin reduces effect of medicines in the course of which metabolism PABK is formed.

Probenetsid, diuretics, Allopyrinolum, phenylbutazone, NPVS reduce canalicular secretion of amoxicillin that can be followed by increase in its concentration in a blood plasma.

Antacids, glycosamine, purgatives, aminoglycosides slow down and reduce, and ascorbic acid increases amoxicillin absorption.

At the combined use of amoxicillin and clavulanic acid the pharmacokinetics of both components does not change.

Allopyrinolum: Combined use with Allopyrinolum can lead to development of allergic skin reactions.

Digoxin: Increase in absorbability of digoxin against the background of therapy by amoxicillin is possible

Methotrexate: Combined use with amoxicillin can increase degree of toxicity of a methotrexate, perhaps, as a result of competitive inhibition amoxicillin of tubular renal secretion of a methotrexate.

Contraindications:

The known hypersensitivity to amoxicillin or other component of a ready dosage form.

Infectious mononucleosis. the lymphoid leukosis, heavy infections of a GIT which are followed by diarrhea or vomiting (to apply parenterally), allergic diathesis, bronchial asthma, hay fever, hypersensitivity to penicillin and/or cephalosporins.

For use in a combination with metronidazole: the age is younger than 18 years; diseases of a nervous system; hemopoiesis disturbances, lymphoid leukosis, infectious mononucleosis; hypersensitivity to nitroimidazole derivatives.

Contraindication for use of tablets is the age up to 3 years in view of difficulty of their proglatyvaniye by small children. At this age it is necessary to appoint parenteral or suspension forms of medicines.

For tablets a dosage of 1 and 0,75 g - age up to 6 years.
For tablets a dosage of 1 g - age up to 10 years.

Overdose:

Symptoms. Amoxicillin usually does not cause acute toxic effects, even at accidental reception of high doses. The overdose can be shown by symptoms of gastrointestinal frustration, disturbance of water and electrolytic balance. At patients with a heavy renal failure the overdose by high doses of amoxicillin can be followed by signs of nephrotoxicity and a crystalluria.

Therapy. The specific antidote of amoxicillin does not exist. Therapy includes administration of absorbent carbon (there are no indications for a gastric lavage, as a rule) or symptomatic measures. Special attention should be paid to vodnoyoelektrolitny balance. Use of a hemodialysis is possible.

Storage conditions:

To store in the place protected from light at a temperature not above +25 °C. To store in the place, unavailable to children. Period of storage 2 years.

Issue conditions:

According to the recipe

Packaging:

Coated tablets on 125 mg in a blister strip packaging No. 10x1, No. 10x2 and in banks No. 20; 250 mg in a blister strip packaging No. 12x1, No. 12x2 and in banks No. 20; 500 mg in a blister strip packaging No. 12x1, No. 12x2 and in banks No. 10; 750 mg, 1000 mg in a blister strip packaging No. 6x1, No. 6x2 and in banks No. 10 in packaging No. 1. Together with a leaf insert one or two blister strip packagings, or bank are located in a pack from a cardboard.