Ampicillin sodium salt

General characteristics. Structure:

Powder for preparation of solution for injections, 0,5 g or 1,0 g.

Active agent - ampicillin sodium salt (in terms of ampicillin) 0,5 g or 1,0 g.

Pharmacological properties:

Pharmacokinetics. At an intramuscular injection the maximum level of drug in a blood plasma is reached in 30-60 minutes. About 17-20% of ampicillin get into plasma proteins. Distribution volume – about 15 l.

Ampicillin well gets into fabrics, passes through a placental barrier and is emitted with maternal milk. At the unimpaired meninx drug level in liquor reaches only 5% of level in plasma. However concentration in liquor increases to 50% of concentration in plasma if the meninx is inflamed.

Ampicillin is removed, generally in not changed form with urine and bile. After parenteral use about 73 + 10% of the entered dose are allocated with urine in not changed form within 12 hours. To 10% of one dose it is allocated as metabolism products. The elimination half-life makes 50-60 minutes. In the conditions of an oliguria the elimination half-life can increase till 8-20 o'clock. The elimination half-life increases also at newborn children (2-4 hours). The renal clearance of ampicillin after intravenous use makes about 194 ml/min.

At a renal failure removal of ampicillin is slowed down. The semi-elimination period at patients with the clearance of creatinine (CC) more than 30 ml/min. makes 1 hour, at KK of 15-29 ml/min. it is equal to 5 hours and at KK of 5-14 ml/min. – 9 hours. At the patients who are on a hemodialysis, the period of semi-elimination of ampicillin makes 4,0-5,1 h.

At persons 60 years are more senior elimination of ampicillin is slowed down. The period of semi-elimination makes at children of the 1st month of life of 1,7-6,2 h, elderly persons have 4,9-6,7 h.

Pharmacodynamics. Ampicillin - a semi-synthetic antibiotic of group of aminopenicillin of a broad spectrum of activity. Works bakteritsidno, oppressing synthesis of a cell wall of microorganisms.

The mechanism of action is connected with inhibition of activity of membrane-bound transpeptidases of bacteria and disturbance, thus, of a cross stitching of peptidoglikan in murein molecules which provide durability and rigidity of a cell wall of bacteria. Ampicillin is unstable in the relation both plasmid, and genomic лактамаз which produce bacteria. Collapses all beta lactamelements of the I-V classes on classification of Richmond, Sykes & Mattew.

Shows the greatest activity concerning gram-positive aerobic bacteria: Staphylococcus spp. (except the beta lactamazoproducing strains), Staphylococcus aureus (except the beta lactamazoproducing strains), Streptococcus pyogenes, Streptococcus viridans, Streptococcus agalactiae, Streptococcus pneumoniae, Listeria monocytogenes, Corynebacterium diphtheriae, Corynebacterium xerose, Bacillus anthracis, Enterococcus spp.; gram-negative aerobic bacteria: Neisseria gonorrhoeae, Neisseria meningitides, Haemophilus influenzae, is moderately active concerning gram-negative Escherichia coli, Proteus mirabilis, Shigella spp., Salmonella spp., Leptospira spp., Borrelia spp., Treponema pallidum, Vibrio cholerae; gram-negative anaerobic cocci: Peptostreptococcus spp., Clostridium spp., Propionibacterium acnes, Fusobacterium spp.

The beta lactamazoproducing Staphylococcus spp strains are steady against ampicillin. and other gram-negative bacteria, Pseudomonas aeruginosa, an indole - positive strains of Proteus spp., Bacteroides spp., Enterobacter aerogenes, Klebsiella pneumoniae, Rickettsia spp., Mycoplasma spp., Chlamydia spp., H. pylori, Mycobacterium tuberculosis. Now the majority of hospital strains of Escherichia coli and Proteus mirabilis are steady against drug (level of stability of 20-30%).

Indications to use:

The infectious and inflammatory diseases caused by microorganisms, sensitive to drug:

- bronchitis, pneumonia, lung abscess;

- quinsy, tonsillitis;

- sinusitis, pharyngitis, average otitis;

- cholangitis, cholecystitis;

- pyelonephritis, pyelitis, cystitis, urethritis;

- gonorrhea;

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

- typhoid, paratyphoid, dysentery, salmonellosis;

- peritonitis;

- meningitis;

- endocarditis;

- sepsis.

Route of administration and doses:

Ampicillin is entered intramusculary or intravenously (struyno or kapelno).

Intravenously: the single dose of drug for adults makes 0,5 - 1,0, each 4-6 hours, daily – 1-3 g. At heavy infections the daily dose can be increased to 10 g and more. The maximum daily dose - 14 g. The newborn drug each 12 h the first week of life, then 50 mg of kg each 8 h, newborn weighing 2 kg and above - 50 mg of kg each 8 h in the first week of life, then 50 mg of kg each 6 h appoint in a daily dose 25-50 mg/kg. At the heavy course of an infection the specified doses can be doubled. The daily dose is entered into 4-6 receptions with an interval of 4-6 hours.

Solution for intravenous jet administration is prepared by ex tempore, the single dose of drug (no more than 2 g) is dissolved in 5-10 ml of sterile water for injections or isotonic solution of sodium of chloride and enter slowly, within 3-5 minutes.

At the single dose exceeding 2 g, the drug is administered intravenously kapelno. The adult for intravenous drop administration the single dose of drug (2-4 g) is dissolved in the small volume of water for injections (respectively in 7,5-15,0 ml), then the received solution of an antibiotic is added to 125,0-250,0 ml of isotonic solution of sodium of chloride or 5% of solution of glucose and entered with a speed of 60-80 thaws a minute.

At drop introduction to children as solvent use 5-10% glucose solution (30-50 ml depending on age). Solutions enter right after preparation.

The daily dose is distributed on 3-4 introductions. Duration of treatment makes 5-7 days with the subsequent (if necessary) transition to intramuscular introduction.

Intramusculary: the single dose of drug for adults makes 0,5-1,0 g, each 4-6 hours, daily - 2-4 g. At heavy infections the daily dose can be increased to 10 g and more. The maximum daily dose - 14 g. The newborn drug appoint in a daily dose 100 mg/kg, to children of other age groups - 50 mg/kg. At the heavy course of an infection the specified doses can be doubled. The daily dose is entered into 4-6 receptions with an interval of 4-6 hours. Solution for intramuscular introduction is prepared by ex tempore, adding to bottle contents 2 ml (0,5 g) or 4 ml (1,0 g) of sterile water for injections.

Duration of treatment depends on localization of an infection, disease severity and makes of 5-10 days.

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. At appointment as the patient with sepsis development of reaction of a bacteriolysis (Yarisha-Gerksgeymer's reaction) is possible. At the patients having hypersensitivity to penicillin cross allergic reactions with others beta лактамными antibiotics are possible.

At treatment of slight diarrhea against the background of course treatment it is necessary to avoid the antidiarrheal medicines reducing an intestines peristaltics; use a kaolin is possible - or attapulgitsoderzhashchy antidiarrheal drugs, drug withdrawal is shown. At heavy diarrhea it is necessary to see a doctor. Treatment has to continue surely for 48-72 more h after disappearance of clinical signs of a disease.

With care it is necessary to apply at children's age up to 1 month, at pregnant women, and also at children if in the anamnesis of mother there is an instruction on her hypersensitivity to penicillin. At bronchial asthma, hay fever and other allergic diseases drug is used along with the desensibilizing means.

It is inadmissible to mix in one syringe Ampicillin with other medicines.

At prolonged treatment by drug at the weakened patients development of the superinfection caused by microorganisms, steady against drug, is possible. It is reasonable to such patient to appoint nystatin or levorinum at the same time.

Drug can be used during pregnancy if the expected advantage of therapy for mother exceeds potential risk for a fruit. In the first trimester of pregnancy it should be applied only according to vital indications.

During treatment it is necessary to be careful when driving or potentially dangerous mechanisms.

Side effects:

- skin rash, small tortoiseshell, Quincke's edema, rhinitis, conjunctivitis, fever;

- toxic action on the central nervous system (at use of high doses for patients with a renal failure);

- dryness in a mouth, nausea, vomiting, an abdominal pain, diarrhea, moderate increase in activity of "hepatic" transaminases, dysbacteriosis, stomatitis, a glossitis, gastritis, a pseudomembranous coloenteritis.

Seldom:

- joint pain, eosinophilia;

- acute anaphylaxis;

- leukopenia, thrombocytopenia, agranulocytosis, anemia;

- intersticial nephrite, nephropathy.

Local reactions:

- pain together introductions;

- infiltrates at intramuscular introduction;

- phlebitis at intravenous administration in high doses.

Interaction with other medicines:

Ampicillin increases effect of anticoagulants, antibiotics of an aminoglikozidny row, reduces – oral contraceptives. Probenetsid reduces canalicular secretion of ampicillin therefore the risk of development of its toxic action increases. Allopyrinolum increases probability of emergence of skin rash. Diuretics, Allopyrinolum, oxyphenbutazolum, NPVP blocking canalicular secretion increase concentration of ampicillin in plasma.

Contraindications:

- hypersensitivity to penicillin, cephalosporins, karbapenema;

- heavy disturbances of functions of a liver and kidneys;

- infectious mononucleosis;

- leukemia;

- HIV infection;

- bronchial asthma, hay fever;

- lymphoid leukosis;

- lactation period.

Overdose:

Symptoms: toxic impact on the central nervous system (hallucinations, spasms, agitation), and also the dispeptic phenomena (nausea, vomiting, a liquid chair), allergic reactions in the form of skin rashes.

Treatment: gastric lavage, absorbent carbon, salt laxatives, maintenance of water and electrolytic balance, symptomatic therapy. It is removed by means of a hemodialysis.

Storage conditions:

To store in the dry, protected from light place, at a temperature not above 30 °C.

To store in the place, unavailable to children!

Issue conditions:

According to the recipe

Packaging:

Powder for preparation of solution for injections on 0,5 g in a bottle together with the instruction on a medical use in the state and Russian languages or on 1.0 g of active agent in the bottles hermetically corked by rubber bungs, which are pressed out by caps aluminum and import plastic covers of "FLIPP OFF".

On 100 bottles pack into a film polyethylene with thermoshrinkable with a tray from a cardboard or into boxes from a cardboard bandbox with partitions from the same cardboard. Put the approved instructions on a medical use in packaging in the state and Russian languages.