An effective, widely used drug is ampicillin trihydrate. Medicinal reference book geotar For renal dysfunction

Ampicillin Trihydrate – semisynthetic antibiotic penicillin series wide range actions with bactericidal activity.

Release form and composition

Dosage forms of Ampicillin Trihydrate:

• pills: white, depending on the manufacturer, either round with biconvex surfaces and with a score, or round flat-cylindrical with a chamfer and a score, or a flat-cylindrical shape with a chamfer and a score (10, 20, 24 or 30 pcs. in a strip pack, in a cardboard pack of 1 or 2 packaging; 10 pcs. in a contour-free packaging, in a cardboard pack of 1 or 2 packages, for hospitals - in a cardboard box of 100, 200, 500, 600, 800 or 1000 packages in a glass jar; 10, 20, 30, 40 or 50 pcs. in a polymer jar, 1 jar in a cardboard pack);
• capsules: white (10 pieces in a blister, 1 or 2 blisters in a cardboard box).

1 tablet contains:

• additional components: depending on the manufacturer – potato starch, magnesium/calcium stearate, talc; additionally – povidone (low molecular weight medical polyvinylpyrrolidone with a molecular weight of 12,600 + 2700).

1 capsule contains:

• active substance: ampicillin (in the form of trihydrate) – 250 mg;
• additional components: potato starch, powdered sugar.

Pharmacological properties

Pharmacodynamics

Ampicillin Trihydrate is a semi-synthetic penicillin with a broad spectrum of action, which has a bactericidal effect by inhibiting the synthesis of the bacterial cell wall. The drug is active against the following microorganisms:

• gram-positive: Streptococcus pneumoniae, alpha and beta -hemolytic streptococci, Bacillus anthracis, Staphylococcus spp., Clostridium spp.;
• gram-negative: Neisseria gonorrhoeae, Neisseria meningitidis, Haemophilus influenzae, Yersinia multocida (formerly Pasteurella), Proteus mirabilis, Escherichia coli, many species of Salmonella spp., Shigella spp.;
• aerobic non-spore-forming bacteria.

Ampicillin Trihydrate demonstrates moderate activity against Listeria spp., most Enterococcus spp., including Enterococcus faecalis.

The antibiotic is ineffective against penicillinase-producing strains of Staphylococcus spp., most strains of Klebsiella spp. and Enterobacter spp., all strains of Pseudomonas aeruginosa.

Pharmacokinetics

After oral administration, the active substance is quickly and effectively absorbed, but its bioavailability is 40%. If you take ampicillin at a dose of 500 mg, maximum concentration in the blood (Cmax) can be 3–4 μg/ml, and the time to reach it (TCmax) is 2 hours. The drug binds to proteins by 20%, the half-life (T ½) is 1–2 hours.

Ampicillin trihydrate is characterized by uniform distribution in therapeutic concentrations in the following tissues and organs of the body: synovial, pleural, peritoneal and amniotic fluids, cerebrospinal fluid, urine (in high concentrations), contents of blisters, bile, intestinal mucosa, gall bladder, bones, lungs, tissues of the female genital organs, bronchial secretions (if purulent - slight accumulation), middle ear fluid (if it is inflamed), paranasal sinuses, saliva, fetal tissue.

The active substance does not pass well through the blood-brain barrier (permeability increases with inflammation of the meninges). It is excreted primarily by the kidneys (approximately 70-80%), while high concentrations of unchanged drug are formed in the urine. Partially excreted with bile, when used during lactation - with mother's milk.

Ampicillin trihydrate does not accumulate with repeated doses and is removed during hemodialysis.

Indications for use

According to the instructions, Ampicillin Trihydrate is recommended for the treatment of the following infectious and inflammatory lesions caused by microorganisms sensitive to its action:

• pharyngitis, tonsillitis, sinusitis, otitis media, pneumonia, bronchitis, lung abscess;
• cholecystitis, cholangitis;
• urethritis, cystitis, pyelitis, pyelonephritis;
• cervicitis;
• gonorrhea;
• impetigo, erysipelas, secondary infected dermatoses;
• dysentery, typhoid fever, paratyphoid fever, salmonellosis (including carriage);
• infections of the musculoskeletal system.

Additional indications (depending on manufacturer):

• pasteurellosis, listeriosis;
• chlamydial infections in pregnant women (in case of intolerance to erythromycin).

Contraindications

Absolute:

• history of gastrointestinal diseases (especially colitis caused by taking antibiotics);
• liver failure;
• lymphocytic leukemia;
• infectious mononucleosis;
• age up to 3 years;
• breastfeeding period;
• hypersensitivity to any of the components of Ampicillin Trihydrate, as well as to other penicillins, carbapenems, cephalosporins.

Relative (ampicillin should be used with extreme caution):

• history of bleeding;
• renal failure;
• hay fever, bronchial asthma and others allergic diseases(including history);
• pregnancy.

Instructions for use of Ampicillin Trihydrate: method and dosage

Ampicillin trihydrate is taken orally 30–60 minutes before meals with a small amount of water.

Adults and children over 3 years of age with a body weight of more than 20 kg are recommended to use an antibiotic every 6 hours at a dose of 250–500 mg. The maximum permissible daily dose is 4000 mg.

Children over 3 years old with a body weight of less than 20 kg are recommended to take the drug every 8 hours at 16.7–33.3 mg/kg or every 6 hours at 12.5–25 mg/kg.

When treating gonococcal urethritis, Ampicillin Trihydrate is taken once at a dose of 3500 mg.

The dosage regimen and course of treatment are determined by the attending physician individually, taking into account the sensitivity of the pathogen and the severity of the infection. The duration of drug therapy can vary from 5–10 to 14–20 days, and when chronic processes– reach several months.

Side effects

• digestive system: stomatitis, dry oral mucosa, dysbacteriosis, change in taste, glossitis, nausea, abdominal pain, vomiting, diarrhea, gastritis, moderate increase in the activity of liver transaminases, pseudomembranous colitis;
• allergic reactions: urticaria, itching, peeling of the skin, conjunctivitis, rhinitis, angioedema; rarely - arthralgia, fever, erythematous or maculopapular rash, exudative erythema, including Stevens-Johnson syndrome, exfoliative dermatitis, eosinophilia, reactions similar to serum sickness; isolated cases - anaphylactic shock;
• nervous system: tremor, headache, anxiety, agitation/aggression, depression, behavior changes, confusion, convulsions (when using high doses);
• laboratory parameters: anemia, thrombocytopenia, neutropenia, leukopenia, agranulocytosis;
• other: vaginal candidiasis, nephropathy, interstitial nephritis, superinfection (mainly in the presence of chronic diseases or reduced body resistance), rash (may go away without discontinuing Ampicillin Trihydrate).

Overdose

Symptoms of an overdose of Ampicillin Trihydrate may include nausea, diarrhea, vomiting, water and electrolyte imbalance (caused by vomiting and diarrhea); manifestations of toxic effects on nervous system(mainly in patients with renal failure).

In case of overdose, gastric lavage is prescribed, taking activated carbon, saline laxatives, drugs to maintain water and electrolyte balance, symptomatic medications. The drug is removed by hemodialysis.

Special instructions

Systematic monitoring is required during treatment functional state hematopoietic organs, kidneys and liver.

During therapy with the drug in patients with bacteremia (sepsis), there is a risk of developing a bacteriolysis reaction (Jarisch-Herxheimer reaction).

In the event of an allergy, at its first symptoms, it is necessary to stop using the antibiotic and carry out desensitizing treatment.

Due to the growth of microflora insensitive to Ampicillin Trihydrate, superinfection may occur; in such cases, appropriate adjustment of antibacterial therapy is required.

If there is an existing hypersensitivity to penicillins, the development of cross-allergic reactions with cephalosporin antibiotics may occur.

If mild diarrhea caused by Clostridium difficile occurs during a course of taking the drug, antidiarrheals that reduce intestinal motility should not be used to treat it. The use of kaolin- or attapulgite-containing antidiarrheal drugs is allowed; discontinuation of the antibiotic is possible. For severe diarrhea, consult a doctor.

Treatment with Ampicillin Trihydrate must be continued for another 48–72 hours after withdrawal. clinical symptoms diseases.

Impact on the ability to drive vehicles and complex mechanisms

During therapy, patients driving vehicles or other complex and potentially dangerous equipment should be careful.

Use during pregnancy and lactation

During pregnancy, ampicillin is allowed only if the expected benefit of therapy for the mother far outweighs the possible threat to the health of the fetus.

Since Ampicillin Trihydrate is low concentrations penetrates into mother's milk, if it is necessary to prescribe it during lactation, the issue of stopping breastfeeding should be decided.

Use in childhood

Children under 3 years of age are contraindicated to take antibiotics.

For impaired renal function

In the presence of renal failure, Ampicillin Trihydrate should be used with caution, adjusting the dosage regimen taking into account creatinine clearance.

For liver dysfunction

The drug is contraindicated in patients with liver failure.

Drug interactions

• ascorbic acid: increases the absorption of ampicillin;
• bactericidal antibiotics, including cephalosporins, aminoglycosides, rifampicin, cycloserine, vancomycin: a synergistic effect is noted;
• laxatives, antacids, aminoglycosides, glucosamine: absorption of ampicillin slows down and decreases;
• sulfonamides, lincosamides, macrolides, tetracyclines, chloramphenicol: antagonistic phenomena are observed;
• indirect anticoagulants: the effectiveness of these drugs increases due to the suppression of intestinal microflora, a decrease in the production of vitamin K and the prothrombin index;
• drugs, in the process of metabolic transformation of which is formed para-aminobenzoic acid: the effect of these funds is weakened;
• ethinyl estradiol: its effect is weakened, the threat of breakthrough bleeding worsens;
• estrogen-containing oral contraceptives: their effectiveness decreases (other methods of contraception should be used or additional ones should be used);
• allopurinol: increases the likelihood of developing skin rash;
• non-steroidal anti-inflammatory drugs, phenylbutazone, oxyphenbutazone, allopurinol, diuretics and other drugs that block tubular secretion: the plasma level of ampicillin increases (as a result of a decrease in tubular secretion);
• methotrexate: its clearance decreases and toxicity increases.

Analogs

Analogues of Ampicillin Trihydrate are: Ampicillin, Ampicillin sodium salt-Vial, Ampicillin-AKOS, Ampicillin-Ferein.

Terms and conditions of storage

Store in a place protected from light and moisture, out of reach of children, at a temperature not exceeding 20–25 °C.

The shelf life of tablets is 2 years, capsules are 3 years.

International and chemical names: ampicillin; (2S,5R,6R)-6-[(2R)-2-amino-2-phenylacetyl]amino]-3,3-dimethyl-7-oxo-4-thia-1-azabicycloheptane-2-carboxylic acid ;basic physical and chemical properties: tablets white or white with a yellowish tint, with a flat surface, scored and chamfered;composition: 1 tablet contains ampicillin trihydrate in terms of 100% ampicillin - 250 mg;excipients: potato starch, talc, calcium stearate or magnesium stearate.

Antibiotic of the group of semi-synthetic penicillins of the third generation with a wide spectrum of action.
Pharmacodynamics. Renders bactericidal effect due to suppression of bacterial cell wall synthesis; active against proliferating bacteria. Bactericidal effect due to the ability of ampicillin to bind and inactivate penicillin-binding proteins located on the inner membrane of the bacterial cell wall. As a result, the late stages of cell wall synthesis of a dividing microorganism are disrupted, and osmotic stability is reduced. bacterial cell, which leads to its death (lysis).
Has a wide spectrum of action. Active against gram-positive ά- and β-hemolytic streptococci, Streptococcus pneumoniae, Staphylococcus spp., Bacillus anthracis, Clostridium spp., moderately active against most enterococci, including Enterococcus faecalis), Listeria spp., and gram-negative (Haemophilus influenzae , Neisseria meningitidis, Proteus mirabilis, Yersinia multocida, many species of Salmonella spp., Shigella spp., Escherichia coli, microorganisms, aerobic non-spore-forming bacteria.
Ineffective against penicillinase-producing strains of Staphylococcus spp., all strains of Pseudomonas aeruginosa, most strains of Klebsiella spp. and Enterobacter spp.

Pharmacokinetics. When taken orally, it is quickly absorbed from the gastrointestinal tract without being destroyed in acidic environment stomach. Absorption of ampicillin is reduced when taken simultaneously with food. Bioavailability is 40%. The maximum concentration in blood plasma when taking 500 mg (2 tablets) is reached after 2 hours, amounting to 3-4 mcg/ml, and slowly decreases over 6 hours. It is bound to plasma proteins by 10-30%.
Penetrates well into tissues and biological fluids of the body, is found in therapeutic concentrations in the pleural, peritoneal, amniotic and synovial fluids, liquor, contents of blisters, urine (high concentrations), intestinal mucosa, bones, gallbladder, bile, lungs, tissues of female genital organs, in bronchial secretions (in purulent bronchial secretions the accumulation is weak), paranasal sinuses nose, middle ear fluid (if it is inflamed), saliva, fetal tissue. Penetrates the blood-brain barrier poorly, permeability increases with inflammation meninges.
Practically does not undergo biotransformation - 10-30% of the dose taken is metabolized in the liver. The half-life is 1-1.5 hours. Excreted primarily by the kidneys
(70-80%), and very high concentrations of unchanged drug are created in the urine; partially excreted in bile (20%). May stand out from breast milk(in low concentrations).
Does not accumulate in the body. Removed by hemodialysis.

Infections caused by ampicillin-sensitive microorganisms: respiratory tract and ENT organs (sinusitis, lung), kidney and urinary tract infections (pyelonephritis), biliary system infections (cholangitis), chlamydial infections in pregnant women (with intolerance to erythromycin), skin and soft tissue infections: secondary infected dermatoses; musculoskeletal infections; (typhoid fever and paratyphoid fever, dysentery, salmonella carriage), abdominal infections (peritonitis), (prevention and treatment), .

Administered orally, without chewing, with water. The daily dose is set individually depending on the severity of the disease, the location of the infection and the sensitivity of the pathogen. The daily dose is divided into 4-6 doses.
For adults and children over 14 years old single dose is 250-500 mg (1-2 tablets), daily - 1-3 g (4-12 tablets). The maximum daily dose is 3 g (12 tablets). For severe infections, up to 6 g/day (24 tablets) is prescribed.
For gonorrheal uncomplicated urethritis, cystitis and pyelonephritis, 500 mg (2 tablets) is prescribed, for respiratory tract infections - 250 mg (1 tablet), for infections digestive tract- 500-750 mg (2-3 tablets), for typhoid fever and bacilli carriage - 1-1.5 g (4-6 tablets) every 6 hours.
For gonococcal urethritis, a single dose of 3.5 g of ampicillin (14 tablets) is prescribed in combination with 1 g of probenecid.
Children over 3 years of age are usually prescribed a daily dose of 30-50 mg/kg body weight, which is 125-250 mg 4 times a day. The maximum daily dose is 2 g.
The duration of treatment depends on the severity of the disease (from 5-10 days to 2-3 weeks, for chronic processes - for several months). Treatment must be continued for another 2-3 days after disappearance clinical signs diseases.

During a course of treatment, it is necessary to monitor the state of kidney and liver function (especially with) peripheral blood patterns. Patients with impaired renal function, as well as elderly patients, require adjustment of the dosage regimen in accordance with creatinine clearance values. The use of high doses of the drug in patients with renal failure can lead to toxic effects on the central nervous system. In patients with liver failure, no dose adjustment is required.
Restrictions to medical use the drug are also other allergic diseases; if it is necessary to use ampicillin, desensitizing drugs are prescribed at the same time. If allergic reactions occur, the drug is discontinued and desensitizing therapy is carried out. If signs appear, urgent measures are necessary to remove the patient from this state.
In weakened patients with long-term treatment it is possible to develop superinfection due to the growth of microflora insensitive to it (candidiasis); For such patients, it is advisable to simultaneously prescribe B vitamins and vitamin C, and, if necessary, nystatin or levorin. Antibiotic therapy may need to be adjusted accordingly.
When prescribed to patients with sepsis, the development of a bacteriolysis reaction (Jarisch-Herxheimer reaction) is possible. In patients who are hypersensitive to penicillins, cross-allergic reactions with other β-lactam antibiotics are possible. At treatment of mild in the background course treatment antidiarrheals should be avoided medicines, reducing intestinal motility; you can use kaolin or attapulgite containing antidiarrheal drugs, discontinuation of the drug is indicated. For severe diarrhea, oral antibiotics (metronidazole or vancomycin) are prescribed. Loperamide should not be used. Use during pregnancy is possible only if the expected therapeutic effect exceeds the potential risk to the fetus. During treatment you should stop breastfeeding.

Data on the effect of the drug on the ability to drive vehicles and potentially perform dangerous species There are no activities.

Allergic reactions:, Quincke's edema, itching, exfoliative, exudative erythema multiforme (including Stevens-Johnson syndrome); rarely - anaphylactic shock. From the outside digestive system:, diarrhea (both during treatment and several weeks after its cessation), intestinal dysbiosis, oral candidiasis, vaginal candidiasis (superinfections caused by resistant strains).

Antacids, glucosamine, laxatives, aminoglycosides and food slow down and reduce the absorption of ampicillin; ascorbic acid increases its absorption. Ampicillin increases the effectiveness of anticoagulants and aminoglycoside antibiotics; reduces the effectiveness of estrogen-containing oral contraceptives (additional methods of contraception must be used). Probenecid and other drugs that reduce tubular secretion increase the concentration of ampicillin in plasma. Concomitant use with allopurinol significantly increases the risk of developing a skin rash. Reduces clearance and increases toxicity of methotrexate. Enhances the absorption of digoxin. In high doses, it reduces the level of atenolol in the blood, so it is recommended to take these drugs separately, and take atenolol before using ampicillin.

Hypersensitivity to penicillin antibiotics and other β-lactam antibiotics (cephalosporins, carbapenems), lymphocytic leukemia, severe liver failure, breastfeeding period (interrupt during treatment), childhood up to 3 years.

Symptoms: signs of toxic effects on the central nervous system (especially in patients with renal failure); nausea, vomiting, diarrhea, water and electrolyte imbalance (as a result of vomiting and diarrhea). Treatment:, prescribing activated carbon, saline laxatives, medications to maintain water-electrolyte balance and symptomatic. In patients with impaired renal function, it is not effective, it is excreted through.

For one tablet:

active substance: ampicillin trihydrate (in terms of ampicillin) - 250.0 mg, excipients: potato starch, talc, magnesium stearate, povidone (low molecular weight medical polyvinylpyrrolidone 12600 + 2700).

Semi-synthetic penicillin, broad-spectrum, bactericidal. Acid resistant. Suppresses bacterial cell wall synthesis.

Active against gram-positive (alpha- and beta-hemolytic streptococci,Streptococcus pneumoniae, Staphylococcus spp., Bacillus anthracis, Clostridium spp.), Listeria spp., and gram-negative(Haemophilus influenzae, Neisseria meningitidis, Proteus mirabilis, Yersinia multocida(previously Pasteurella), many types Salmonella spp., Shigella spp., Escherichia coli) microorganisms, aerobic non-spore-forming bacteria.

Moderately active against most enterococci, incl.Enterococcus faecalis. Ineffective against penicillinase-producing strainsStaphylococcus spp., all strains Pseudomonas aeruginosa, most strainsKlebsiella spp. And Enterobacter spp.

Absorption when taken orally is high, bioavailability is 40%; the time to reach the maximum concentration when taking 500 mg orally is 2 hours, the maximum concentration is 3-4 mcg/ml. Communication with plasma proteins - 20%. Evenly distributed in organs and tissues of the body, found in therapeutic concentrations in pleural, peritoneal, amniotic and synovial fluids, cerebrospinal fluid, the contents of blisters, urine (high concentrations), intestinal mucosa, bones, gall bladder, lungs, tissues of the female genital organs, bile , in bronchial secretions (in purulent bronchial secretions the accumulation is weak), paranasal sinuses, middle ear fluid (with inflammation), saliva, fetal tissues. It penetrates the blood-brain barrier poorly, its permeability increases with inflammation. The half-life is 1-2 hours. It is predominantly excretedkidneys (70-80%), and very high concentrations of unchanged antibiotic are created in the urine; partially - with bile, in nursing mothers - with milk. Does not cumulate. Removed by hemodialysis.

Infectious inflammatory diseases caused by sensitive microorganisms: respiratory tract and ENT organs (sinusitis, tonsillitis, pharyngitis, otitis media, bronchitis, pneumonia, lung abscess), kidney and urinary tract infections (pyelonephritis, pyelitis, cystitis, urethritis), gonorrhea, biliary system infections ( cholangitis, cholecystitis), chlamydial infections in pregnant women (with intolerance to erythromycin), cervicitis, skin and soft tissue infections (erysipelas, impetigo, secondary infected dermatoses); musculoskeletal infections; pasteurellosis, listeriosis, gastrointestinal tract infections (typhoid and paratyphoid, dysentery, salmonellosis, salmonellosis carriage).

Hypersensitivity to drugs of the penicillin group and other beta-lactam antibiotics, infectious mononucleosis, lymphocytic leukemia, liver failure, history of gastrointestinal diseases (especially colitis associated with the use of antibiotics), lactation period, children under 3 years of age and/or overweight less than 20 kg.

Bronchial asthma, hay fever and other allergic diseases, renal failure, history of bleeding.

During pregnancy, ampicillin can be used if the benefit to the mother outweighs the potential risk to the fetus. excreted in breast milk in low concentrations. If it is necessary to use ampicillin during lactation, the issue of stopping breastfeeding should be decided.

Orally 0.5-1 hour before meals with a small amount of water. The dosage regimen is set individually depending on the severity and localization of the infection, the sensitivity of the pathogen to the drug.

Adults and children over 3 years old with body weight over 20 kg - 250-500 mg every 6 hours. The maximum daily dose is 4 g/day.

For gonococcal urethritis - 3.5 g once.

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).

From the digestive system: glossitis, stomatitis, gastritis, dry mouth, change in taste, nausea, vomiting, diarrhea, abdominal pain, pseudomembranous enterocolitis, increased activity of liver transaminases.

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

From the central nervous system: headache, tremor, convulsions (with high dose therapy).

Allergic reactions: erythematous and maculopapular rash,exfoliative dermatitis, erythema multiforme, skin peeling, itching, urticaria, rhinitis, conjunctivitis, Quincke's edema, fever, arthralgia, eosinophilia; anaphylactic shock.

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

Symptoms: manifestations of toxic effects on the central nervous system (especially in patients with renal failure); nausea, vomiting, diarrhea, water and electrolyte imbalance (as a result of vomiting and diarrhea).

Treatment: gastric lavage, salinelaxatives, medications to maintain water-electrolyte balance and symptomatic. Eliminated by hemodialysis.

Antacids, laxatives, food and aminoglycosides (when taken enterally) slow down and reduce absorption; increases absorption. Bactericidal antibiotics (including aminoglycosides, cephalosporins) have a synergistic effect; bacteriostatic drugs (macrolides, lincosamides, tetracyclines, sulfonamides) - antagonistic. Increases the effectiveness of indirect anticoagulants (suppressing intestinal microflora, reduces the synthesis of vitamin K and prothrombin index); reduces the effectiveness of estrogen-containing oralcontraceptives (it is necessary to use additional methods of contraception), medications, during the metabolism of which para-aminobenzoic acid is formed, ethinyl estradiol (in the latter case, the risk of breakthrough bleeding increases). Diuretics, oxyphenbutazone, non-steroidal anti-inflammatory drugs and other drugs that block tubular secretion increase the concentration of ampicillin in plasma (by reducing tubular secretion). When taken together with allopurinol, the likelihood of skin rash increases.

Reduces clearance and increases toxicity of methotrexate. Enhances the absorption of digoxin.

During a course of treatment, it is necessary to monitor the state of the function of the hematopoietic organs, liver and kidneys.

When using high doses in patients with renal failure, it is possible toxic effect on the central nervous system.

When treating patients with bacteremia (sepsis), the development of a bacteriolysis reaction (Jarisch-Herxheimer reaction) is possible.

In patients who are hypersensitive to penicillins, cross-allergic reactions with cephalosporin antibiotics are possible.

When treating mild diarrhea during a course of treatment, antidiarrheal drugs that reduce intestinal motility should be avoided; You can use kaolin- or attapulgite-containing antidiarrheal drugs; discontinuation of the drug is indicated. If diarrhea is severe, consult a doctor.

Tablets 250 mg.

List B. In a dry place, protected from light, at a temperature not exceeding 25° C.

Keep out of the reach of children.