Ampitsillin-Darnitsa, tab. 0,25g No. 20

General characteristics. Structure:

1 tablet contains Ampicillini trihdras – 0,2886 g, in terms of ampicillin – 0,25 g; 

excipients: potato starch, calcium stearate or magnesium stearate, talc.

Pharmacological properties:

Pharmacodynamics. Ampicillini trihdras  – a semi-synthetic antibiotic of group of penicillin. Has bactericidal effect due to blocking of enzymes of transpeptidases in cellular membranes of bacteria. Кислотоустойчив.

It is effective rather gram-positive and gram-negative bacteria which are in a proliferation stage. In particular, its activity extends to  E. coli, Proteus mirabilis, Salmonella spp., Shigella spp., Haemophilus influenzae, Bordetella pertussis, Neisseria gonorrhoeae, Neisseria meningitidis. Ampicillin trihydrate is active as well rather gram-positive anaerobic  bacteria.

Penitsillinazoobrazuyushchiye rezistentna staphylococcus to Ampicillini trihdras.

Pharmacokinetics. It is well soaked up at intake, without collapsing in acid medium of a stomach. Time of achievement of the maximum concentration (Tmax) in a blood plasma about 1-2 hours. Linkng with proteins of a blood plasma within 28%.

It is evenly distributed in bodies and body tissues, it is found in therapeutic concentration in pleural, peritoneal, amniotic and synovial liquids, liquor, contents of blisters, urine (high concentration), a mucous membrane of intestines, bones, a gall bladder, lungs, fabrics of female generative organs, bile, in a bronchial secret (in a purulent bronchial secret accumulation weak), paranasal sinuses, liquid of a middle ear, saliva, fruit fabrics. Badly gets through a blood-brain barrier (permeability increases at an inflammation of a meninx). 

Plasma elimination half-life of blood _(T1/2) makes 1-2 hours. At patients of advanced age and at people with functional insufficiency of kidneys it can be extended. To   30% of the accepted dose it is metabolized in a liver. It is removed preferential by kidneys, and in urine high concentration of not changed antibiotic are created. It is partially excreted with bile.

Indications to use:

The bacterial infections caused  by activators, sensitive to drug: ENT organs and respiratory system (sinusitis, tonsillitis, pharyngitis, average otitis, bronchitis, pneumonia, abscess of lungs); infections of kidneys and urinary tract (pyelonephritis, pyelitis, cystitis, urethritis); gonorrhea; infections of biliary system (cholangitis, cholecystitis); chlamydial infections at pregnant women (at intolerance of erythromycin); cervicitis; infections of skin and soft tissues (the ugly face, impetigo for the second time infected a dermatosis); musculoskeletal system infections; pasteurellosis; listeriosis; digestive tract infections (typhoid and paratyphoid, dysentery, salmonellosis); abdominal infections (peritonitis); endocarditis (prevention and treatment); sepsis.

Route of administration and doses:

Ampitsillin-Darnitsa accept inside irrespective of meal. The single dose for adults makes 0,5 g, daily – 2-3 g. To children up to 4 years drug appoint 100 mg/kg of body weight in a daily dose, 4 years – in a daily dose of 100-150 mg/kg are more senior. The daily dose is divided into 4-6 receptions. Duration of therapy of Ampitsillinom-Darnitsa is established individually depending on weight and a form of a disease, efficiency of treatment and makes  of 7-14 днейдо 2-3 weeks.

Features of use:

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 in connection with growth of microflora, insensitive to drug, is possible that demands corresponding change of antibacterial therapy. At appointment as sick sepsis development of reaction of a bacteriolysis (Yarisha-Gerksgeymer's reaction) is possible. At the patients having hypersensitivity to penicillin cross allergic reactions are possible. At treatment of slight diarrhea against the background of course treatment it is necessary to avoid the antidiarrheal drugs reducing an intestines peristaltics.

Administration of drug has to continue surely for 48-72 more h after disappearance of clinical signs of a disease. 

At bronchial asthma, hay fever, other allergic diseases and states drug is used at co-administration of the desensibilizing means. 

At a hepatic unsufficiency Ampitsillin-Darnitsa apply under control of biochemical indicators of a liver.

During pregnancy drug is used according to vital indications.

Side effects:

At some patients manifestation of side effect of drug is possible.  Namely: 

•  from the alimentary system: дисбиоз, stomatitis, gastritis, dryness in a mouth, taste change, an abdominal pain, vomiting, nausea, diarrhea, stomatitis, a glossitis, moderate increase in level of "hepatic" transaminases, pseudomembranous colitis;
•  from the central nervous system: a headache, a tremor, spasms (at therapy by high doses);
•  from blood: leukopenia, neutropenia, thrombocytopenia, agranulocytosis, anemia;
• allergic reactions:
• are possible – a skin peeling, an itch, a small tortoiseshell, rhinitis, conjunctivitis, a Quincke's edema;
• seldom – fever, an arthralgia, an eosinophilia, erythematic and makulopapulezny rash, exfoliative dermatitis, a multiformny exudative erythema, a malignant exudative erythema (Stephens-Johnson's syndrome), the reactions similar to a serum disease;
• in isolated cases – the acute anaphylaxis, not allergic ampitsillinovy rash can disappear without the termination of administration of drug ;
• other: intersticial nephrite, a nephropathy, superinfection (especially at patients with chronic diseases or reduced resistance of an organism), vagina candidiasis.

 

Interaction with other medicines:

Antacids, glycosamine, purgatives, food and aminoglycosides slow down and reduce absorption of Ampicillini trihdras; ascorbic acid raises an absorbtsiyuampitsillin of trihydrate. Bactericidal antibiotics (including aminoglycosides, cephalosporins, Cycloserinum, Vancomycinum, rifampicin) have  sinergidny effect; bacteriostatic drugs (macroleads, chloramphenicol, linkozamida, tetracyclines, streptocides) – antagonistic. Ampitsillin-Darnitsa increases efficiency of indirect anticoagulants (suppressing intestinal microflora, reduces synthesis of vitamin K and a prothrombin ratio). Drug reduces efficiency of estrogensoderzhashchy oral contraceptives (it is necessary to use other methods of contraception) and medicines  in the course of which metabolism paraaminobenzoic acid is formed, ethinylestradiol (in the latter case the risk of development of bleedings of "break" increases). Diuretics, Allopyrinolum, оксифенбутазон, the phenylbutazone, non-steroidal anti-inflammatory drugs, drugs blocking canalicular secretion increase concentration of Ampicillini trihdras (due to decrease in canalicular secretion). Allopyrinolum increases risk of development of skin rash at its combined use with Ampitsillinom-Darnitsa. Drug reduces clearance and increases toxicity of a methotrexate, and also strengthens digoxin absorption.

Contraindications:

 Ampitsillin-Darnits's use is contraindicated to children up to 3 years (in this dosage form), at hypersensitivity to drugs of group of penicillin, an infectious mononucleosis, a lymphoid leukosis, feeding by a breast.

Overdose:

Symptoms of overdose are nausea, vomiting, diarrhea, disturbance of water and electrolytic balance, a spasm.  

Treatment. Symptomatic. Gastric lavage, reception of salt  laxatives, absorbent  carbon. In hard cases – an artificial diuresis, a hemodialysis.

Storage conditions:

To store in the place, unavailable to children, at a temperature not over 25 With °.

Period of validity – 2 years.

Issue conditions:

According to the recipe

Packaging:

On 10 tablets in a blister strip packaging, on the 2nd blister strip packagings in a pack.