Aprid 375

General characteristics. Structure:

Active ingredient: 507 mg of a sultamitsillin of tosylate of a dihydrate equivalent 375 mg of a sultamitsillin respectively.

Excipients: sodium of starch glikolit, magnesium stearate, cellulose microcrystallic,

Structure of a cover: gidroksipropilmetiltsellyuloz (gipromeloz), titanium dioxide (E171), polyethyleneglycol.

Pharmacological properties:

Pharmacodynamics. Aprid - a bactericidal antibiotic of a broad spectrum of activity, кислотоустойчив. Blocks synthesis of a peptidoglikan of a cell wall of microorganisms. An effective agent is ampicillin - the semi-synthetic penicillinic antibiotic of a broad spectrum of activity collapsing beta lactamelements. The second component - to sulbakta, without having antibacterial activity, inhibits beta lactamelements and in this regard ampicillin gains ability to work on steady (the producing beta lactamelements) strains.

Sultamitsillin is pro-medicine of ampicillin and inhibitor beta lactamelements of a sulbaktam. It consists of two connections connected chemically as double ester.

Aprid is effective concerning a wide range of gram-positive and gram-negative aerobic and anaerobic bacteria.

Gram-positive bacteria: Staphylococcus aureus, Staphylococcus epidermidis, Staphylococcus saprophyticus (which are producing and not producing beta lactamelements), Streptococcus pneumoniae, Streptococcus (Enterococcus) faecalis, Streptococcus pyogenes, Streptococcus viridans.

Gram-negative bacteria: Haemophilus influenzae (which are producing and not producing beta lactamelements), Moraxella catarrhalis (which are producing and not producing beta lactamelements), Escherichia coli (which are producing and not producing beta lactamelements), Klebsiella spp. (all known versions produce beta lactamelements), Proteus mirabilis (which are producing and not producing beta lactamelements), Proteus vulgaris, Providencia stuartii, Providencia rettgeri, Morganella morganii and Neisseria gonorrhoeae (which are producing and not producing beta lactamelements).

Anaerobe bacterias: Clostridium spp., Peptococcus spp., Peptostreptococcus spp., Bacteroides fragilis and sibling species.

It is inefficient concerning penitsillinazoprodutsiruyushchy strains of stafilokokk, all strains of a pyocyanic stick and the majority of strains of enterobakteriya.

Pharmacokinetics. After intake сультамициллин it is hydrolyzed with formation of a sulbaktam and ampicillin in a molar ratio 1:1 in system circulation. Bioavailability of a peroral dose makes 80% of the equal dose of a sulbaktam and ampicillin entered intravenously. Food does not influence system bioavailability of a sultamitsillin. The maximum concentration of ampicillin in blood serum after reception of a sultamitsillin exceeds the level reached after reception of an equal dose of ampicillin approximately twice. Ampicillin approximately for 28% reversibly contacts serum proteins, and to sulbakta - approximately for 38%. Elimination half-lives make about 0,75 and 1 hour for a sulbaktam and ampicillin respectively. 50 - 75% of each component are allocated with urine in not changed look. Elderly patients and patients with an impaired renal function have processes of removal of ampicillin and a sulbaktam are changed and elimination half-lives are increased.

Indications to use:

The bacterial infections of various localization caused by sensitive microflora:

- infections of ENT organs (including sinusitis, tonsillitis, average otitis);

- infections of a respiratory organs (including pneumonia, abscess of lungs, chronic bronchitis, pleura empyema);

- infections of urinary tract and generative organs (pyelonephritis, pyelitis, cystitis, urethritis, prostatitis, endometritis, gonorrhea);

- infections of biliary tract (cholecystitis, cholangitis);

- infections of skin and soft tissues (the ugly face, impetigo for the second time infected dermatitis);

- GIT infections (dysentery, salmonellosis, salmonellonositelstvo);

- infections of bones and joints;

- septic endocarditis, meningitis, sepsis, peritonitis;

- prevention of postoperative complications.

Route of administration and doses:

The recommended Aprid's dose for adults (including elderly patients) makes 375 - 750 mg in 2 times a day.

To children 6 years with the body weight of 30 kg and more, the recommended doses as for adults are more senior.

Duration of a course of therapy makes 5 - 10 days, however at heavy infections this period can last.

At uncomplicated gonorrhea the single dose in 2:25 g of a sultamitsillin is appointed (6 tablets Aprid 375 mg or 3 tablets Aprid 750).

After normalization of body temperature and disappearance of pathological symptoms treatment is continued during 48 h.

In case of gonorrhea with suspicion on existence of syphilis carrying out a research in a dark field before purpose of a sultamitsillin and monthly serological tests within 4 months is necessary.

Performing, at least, 10-day treatment of the infections caused by hemolitic streptococci for prevention of acute rheumatic fever and a glomerulonephritis is recommended.

At a heavy renal failure (clearance of creatinine <30 ml/min.) the pharmacokinetics of ampicillin and a sulbaktam changes equally therefore their ratio in plasma remains to constants. Reduction of a dose or increase in an interval between receptions is necessary. At dialysis purpose of an additional dose after the procedure is necessary.

Features of use:

Before appointment it is necessary to ask in detail the patient concerning the postponed reactions of hypersensitivity to penicillin, cephalosporins and other allergens. At the patients having hypersensitivity to penicillin cross allergic reactions with tsefalosporinovy antibiotics are possible. In case of development of allergic reaction it is necessary to cancel drug and to appoint the corresponding        treatment.

Serious anaphylactic reactions demand the emergency treatment by adrenaline. If necessary appoint oxygen, glucocorticoids intravenously and the measures directed to improvement of passability of respiratory tracts including an intubation.

At course treatment it is necessary to carry out control of a condition of function of bodies of a hemopoiesis, a liver and kidneys.

Development of superinfection due to growth of microflora, insensitive to it, is possible that demands corresponding change of antibacterial therapy.

As the infectious mononucleosis is a viral infection, Aprid it is not necessary to appoint for his treatment.

At treatment of patients with sepsis development of reaction of a bacteriolysis (Yarisha-Gerksgeymer's reaction) is possible.
With care appoint at a liver and/or renal failure.

Ampicillin and to sulbakta have no cancerogenic, mutagen effect and do not influence fertility.

Use in pediatrics. To children up to 6 years do not recommend to appoint the tableted dosage forms therefore it is necessary to appoint Aprid in the form of suspension.

Pregnancy and period of a lactation. At pregnancy apply in cases when the estimated advantage for mother exceeds potential risk for a fruit.

Features of influence of medicine on ability to manage the vehicle or potentially dangerous mechanisms

Considering side effects of medicine it is necessary to be careful at control of motor transport or potentially dangerous mechanisms.

Side effects:

- nausea, vomiting, a loss of appetite, pains in epigastric area, diarrhea;

- drowsiness, indisposition, headache;

- rash, itch, urticaria, dermahemia, Quincke's disease, rhinitis, conjunctivitis, fever, arthralgias, eosinophilia, acute anaphylaxis;

- the superinfection caused by microorganisms, steady against drug, (candidiasis) in need of prolonged treatment.

Seldom:

- increase in activity of "hepatic" transaminases;

- anemia, leukopenia, thrombocytopenia;

- azotemia, increase in concentration of urea, giperkreatininemiya.

Very seldom:

- pseudomembranous coloenteritis.

Interaction with other medicines:

At simultaneous use:

- with probenetsidy, diuretics, phenylbutazone, non-steroidal anti-inflammatory drugs renal canalicular secretion of ampicillin and a sulbaktam decrease. Simultaneous use of these drugs with Aprid can lead to increase in levels of ampicillin and a sulbaktam in blood

- with bactericidal antibiotics (aminoglycosides, cephalosporins, Cycloserinum, Vancomycinum, rifampicin) a synergism is shown

- with bacteriostatic antibiotics (macroleads, chloramphenicol, linkozamida, tetracyclines, streptocides) - antagonism

- with indirect anticoagulants, ampicillin strengthens effect of indirect anticoagulants, suppressing intestinal microflora, reduces synthesis of vitamin K and a prothrombin ratio

- with antacids, a glycosamine, purgatives, aminoglycosides ampicillin absorption is slowed down and decreases

- with ascorbic acid, ampicillin absorption increases

- with peroral estrogensoderzhashchy drugs, efficiency of contraceptives decreases

- ampicillin reduces effect of medicines in the course of   which metabolism PABK is formed

- with Allopyrinolum, the probability of emergence of rash increases.

Contraindications:

- hypersensitivity to ampicillin and other components of drug;

- infectious mononucleosis;

- lymphoid leukosis;

- lactation period;

- children's age up to 6 years.

Overdose:

Symptoms: diarrhea, itch, rash, spasms.

Treatment: symptomatic therapy. Concentration of ampicillin and a sulbaktam in blood serum can be reduced by means of a hemodialysis.

Storage conditions:

To store at a temperature from 15 °C to 30 °C in the dry, protected from light place. To store in the place, unavailable to children! Period of storage 2 years. Not to apply after a period of storage

Issue conditions:

According to the recipe

Packaging:

On 10 and 20 tablets, film coated place in bottles from dark glass with the screwing-up plastic cover with control of the first opening. On a bottle paste the self-adhesive label.

The bottle together with the instruction on a medical use in the state and Russian languages is placed in a pack from a cardboard with the hologram of firm - producer.