Ampicillin - instructions for use, dose, side effects, contraindications

Ampicillin is a broad-spectrum antibiotic from the group of semisynthetic penicillins. It acts bactericidal by suppressing the synthesis of the bacterial cell wall. Inhibits the peptidoglycan polymerase and transpeptidase, prevents the formation of peptide bonds and disrupts the late stages of the synthesis of the cell wall of the fissile microorganism, which leads to a decrease in the osmotic resistance of the bacterial cell and causes its lysis.

Active with respect to:

- Gram-positive aerobic bacteria: Staphylococcus spp. (strains that do not produce penicillinase and other beta-lactamases, Streptococcus spp. (including alpha and beta-hemolytic streptococci, Streptococcus pneumoniae), Bacillus anthracis, Listeria spp.

Moderately active against most enterococci Enterococcus spp. (incl. Enterococcus faecalis).

- Gram-negative aerobic bacteria (strains that do not produce beta-lactamase): Haemophilus influenzae, Bordetella pertussis, Neisseria meningitidis, Proteus mirabilis, Yersinia multocida (formerly Pasteurella), many species Salmonella spp., Shigella spp., Escherichia coli;

- Anaerobes: Clostridium spp.

Inactive against penicillinase-producing strains Staphylococcus spp., all strains Pseudomonas aeruginosa, Proteus vulgaris, most strains Klebsiella spp.H Enterobacter spp., some strains Escherichia coli, mycoplasma, chlamydia, rickettsia.

Pharmacokinetics:

Connection with plasma proteins - 20%. At parenteral introduction (in / in, in / m) the concentration in blood exceeds created at intake. It is evenly distributed in the organs and tissues of the body, it is found in therapeutic concentrations in pleural, peritoneal, amniotic and synovial fluids, cerebrospinal fluid, contents of blisters, urine (high concentrations), intestinal mucosa, bones, gall bladder, lungs, female genital tract, bile , in a bronchial secretion (in the purulent bronchial secretion, the accumulation is weak), paranasal sinuses, middle ear fluid, saliva, fetal tissues. Poor penetrates the blood-brain barrier, but its permeability increases with inflammation of the meninges.

Half-life of the drug (T_1/2) - 1-2 hours.

It is excreted mainly by the kidneys (70-80%), very high concentrations of unchanged antibiotic are created in the urine; partially excreted with bile, in nursing mothers - with milk. Do not cumulate. Removed during hemodialysis.

Indications:

Infectious and inflammatory diseases:

- lower respiratory tract (bronchitis, pneumonia, lung abscess);

- ENT organs (sinusitis, tonsillitis, otitis media);

- infection of the kidneys and urinary tract (pyelonephritis, pyelitis, cystitis, urethritis);

- infection of the biliary system (cholangitis, cholecystitis);

- infections of the skin and soft tissues (erysipelas, impetigo, secondarily infected dermatoses);

- infections of the musculoskeletal system;

- infections of the gastrointestinal tract (typhoid and paratyphoid, dysentery, salmonellosis, salmonella carcinoma);

- abdominal infections (peritonitis);

- endocarditis (prevention and treatment);

- meningitis;

- pasteurellosis;

- listeriosis,

- Gonorrhea (including gonorrheal urethritis, gonorrheal cervicitis);

- sepsis.

Contraindications:

Hypersensitivity (including other penicillins, cephalosporins, carbapenems), infectious mononucleosis, lymphocytic leukemia, liver failure, a history of gastrointestinal disease (especially colitis associated with the use of antibiotics), lactation.

Carefully:

Bronchial asthma, pollinosis and other allergic diseases, renal failure, history of bleeding, pregnancy, children under 1 month.

Dosing and Administration:

Intravenous (intravenously) (struino and drip), intramuscularly (IM)

Doses and duration of treatment are set individually, depending on the severity of the course, localization and sensitivity of the causative agent of the infection.

For infections of a moderate course, adults and children with a body weight of more than 20 kg should be injected / m or IV / - 250-500 mg every 6 hours; in severe cases, 1000-2000 mg every 3-4 hours.

Listeriosis - 50 mg / kg every 6 hours.

Typhoid fever - 25 mg / kg every 6 hours.

With gonococcal urethritis - 3.5 g once.

The maximum daily dose of 14 g / day.

Children (with meningitis): newborns with a body weight of up to 2 kg - in / m or in / in 25-50 mg / kg every 12 hours in the first week of life, then 50 mg / kg every 8 g; newborns with a body weight of 2 kg and above - 50 mg / kg every 8 hours in the first week of life, then 50 mg / kg every 6 hours. For other indications in / m or / in children with a body weight of up to 20 kg - 12, 5-25 mg / kg every 6 hours.

The duration of treatment depends on the severity of the disease (from 5-10 days to 2-3 weeks, and in chronic processes - for several months).

Solution for intramuscular injection is prepared by adding to the contents of the bottle water for injection in the amount of: 2 ml per 500 mg bottle; 4 ml - per bottle 1000 mg and 6 ml - per bottle 2 g.

For intravenous fluid administration, a single dose of the drug (not more than 2 g) is dissolved in 5-10 ml of water for injection or 0.9 % solution of sodium chloride and injected slowly for 3-5 minutes. With a single dose exceeding 2 g, the drug is administered only intravenously drip.

For intravenous drip single dose (2-4 g) was dissolved in a small volume of water for injections (7,5-15 ml respectively), then the resulting antibiotic solution is added to 125-250 ml of 0.9% sodium chloride solution or 5 10% dextrose solution and injected at a rate of 60-80 drops per minute.

In the case of drip administration, a 5-10% dextrose solution (30-50 ml, depending on the age) is used as a solvent for children.

The solutions are used immediately after preparation.

Before the appointment of ampicillin should determine the sensitivity of the causative agent of the disease to the drug.

Side effects:

Allergic reactions: Flaky skin, itching, hives, rhinitis, conjunctivitis, angioedema, rare - fever, arthralgia, eosinophilia, erythematous and maculopapular rash, exfoliative dermatitis,multiforme exudative erythema, Stevens-Johnson syndrome, reactions similar to serum sickness, in single cases - anaphylactic shock.

From the digestive system: dysbacteriosis, gastritis, dry mouth, taste change, abdominal pain, vomiting, nausea, diarrhea, stomatitis, glossitis, moderate increase in the level of "liver" transaminases, pseudomembranous enterocolitis.

From the central nervous system: agitation or aggressiveness, anxiety, confusion, behavior change, depression, headache, tremor, convulsions (with high-dose therapy).

Laboratory indicators: leukopenia, neutropenia, thrombocytopenia, agranulocytosis, anemia.

Local Reactions: pain at the injection site, infiltrates with the / m introduction, phlebitis with IV injection in large doses.

Other: interstitial nephritis, nephropathy, superinfection (especially in patients with chronic diseases or reduced resistance of the body), vaginal candidiasis.

Overdose:

Symptoms: the manifestation of toxic effects on the central nervous system (especially in patients with renal insufficiency); nausea, vomiting, diarrhea,violation of water electrolyte balance (as a consequence of vomiting and diarrhea).

Treatment is symptomatic. It is excreted by hemodialysis.

Interaction:

Pharmaceutically incompatible with aminoglycosides.

Bactericidal antibiotics (including aminoglycosides, cephalosporins, cycloserine, vancomycin, rifampicin) - have a synergistic effect; bacteriostatic medicinal products (macrolides, chloramphenicol, lincosamides, tetracyclines, sulfonamides) - antagonistic.

Increases the effectiveness of indirect anticoagulants (suppressing the intestinal microflora, reduces the synthesis of vitamin K and prothrombin index); reduces the effectiveness of estrogen-containing oral contraceptives (it is necessary to use additional methods of contraception), drugs that metabolize parahaminobenzoic acid, ethinyl estradiol (in the latter case, the risk of bleeding "breakthrough" increases).

Diuretics, allopurinol, oxyphenbutazone, phenylbutazone, non-steroidal anti-inflammatory drugs and other drugs that block tubular secretion,increase the concentration of ampicillin in the plasma (due to a decrease in tubular secretion).

Allopurinol increases the risk of skin rash.

Reduces clearance and increases the toxicity of methotrexate.

Synergism of antibacterial action is observed with simultaneous administration with aminoglycoside antibiotics (but not mixing in one syringe!).

Special instructions:

At course treatment it is necessary to monitor the status of the functions of the organs of hematopoiesis, liver and kidneys.

It is possible to develop superinfection by increasing the microflora insensitive to the drug, which requires an appropriate change in antibacterial therapy.

With the appointment of patients with sepsis, the development of a bacteriolysis reaction (the Yarisch-Gerxheimer reaction) is possible.

In patients who have increased sensitivity to penicillins, there may be cross-allergic reactions with other beta-lactam antibiotics.

In the treatment of mild diarrhea, which occurs against the background of course treatment, anti-diarrheal drugs should be avoided, reducing intestinal motility; You can use kaolin- or attapulgite-containing antidiarrhoeal drugs, the withdrawal of the drug is indicated.With severe diarrhea, you should see a doctor.

Treatment should necessarily continue for another 48-72 hours after the disappearance of clinical signs of the disease.

With a mild infection in children, it is preferable to prescribe the drug in the form of a suspension.

Form release / dosage:Powder for solution for intravenous and intramuscular injection 500 mg, 1000 mg, 2 g.

Packaging:

In bottles with a capacity of 10 ml, 20 ml.

1, 5, 10 bottles with instructions for use in packs of cardboard.

50 bottles in boxes of cardboard with 10-15 instructions for use for delivery to hospitals.

Storage conditions:

List B. In a dry, the dark place at a temperature of no higher than 20 ° C.

Keep out of the reach of children.

Shelf life:2 years. Do not use after expiration of the expiration date stated on the package.

Terms of leave from pharmacies:On prescription

Registration number:P N000068 / 04

Date of registration:25.05.2009

Expiration Date:Unlimited

The owner of the registration certificate:SYNTHESIS, OJSC SYNTHESIS, OJSC Russia

Manufacturer: & nbsp

SYNTHESIS, OJSC Russia

Information update date: & nbsp22.08.2017

Illustrated instructions

Instructions

Ampicillin (Ampicillin)