Ampicillin 250 mg No. 10 tab.

Pharmacodynamics and pharmacokinetics

Pharmacodynamics

Semi-synthetic antibiotic of the penicillin series , has a bactericidal . The mechanism of action is associated with inhibition of the synthesis of the cell membrane of dividing microorganisms: it disrupts the peptide bonds in it, which leads to a decrease in the resistance of the bacterial cell and to lysis. Acid resistant. Shows activity against gram-positive ( staphylococcus , streptococcus ) and gram-negative microorganisms ( Klebsiella pneumoniae , Protea , Salmonella , Shigella , Escherichia coli , influenza bacteria).

It is of interest as a drug for the treatment of purulent surgical infections , urinary tract infections , cholangitis and cholecystitis . Effective for the treatment of bacterial respiratory tract infections (community-acquired pneumonia , bronchitis , otitis media , sinusitis ), meningitis , endocarditis (in combination with Gentamicin ), intestinal infections ( shigellosis )

It is destroyed by penicillinase and is therefore ineffective against penicillinase-forming staphylococci . Attempts have been made to “protect” the antibiotic from destruction by bacterial enzymes. “Protected” penicillins are combinations with enzyme inhibitors: Ampicillin + Sulbactam (drug Unazin , Sultasin and others). Sulbactam does not have an antibacterial effect, but inhibits beta-lactamases, so in this combination the antibiotic also acts on resistant strains of microorganisms.

Pharmacokinetics

Absorption is rapid, bioavailability is 40%. The maximum concentration in the blood is determined after 2 hours. It is 20% bound to proteins. In therapeutic concentrations it is found in pleural and synovial fluids, the contents of blisters, high concentrations in urine, gall bladder, lungs, genitals, bile, bronchial secretions, bones, paranasal sinuses, middle ear, saliva.

Excreted by the kidneys (70-80%), partly with bile, and with breast milk. High concentrations of the antibiotic are found in the urine. Does not accumulate with repeated use.

Ampicillin 250 mg No. 10 tab.

APPROVED by the Order of the Chairman of the Pharmaceutical Control Committee of the Ministry of Health of the Republic of Kazakhstan dated "____" __________ 200__ No. ____________________ Instructions for the medical use of the drug AMPICILLIN Trade name Ampicillin International nonproprietary name Ampicillin Dosage form Tablets 250 mg Composition One tablet contains the active substance - ampicillin trihydrate (in terms of for ampicillin) 250 mg, excipients: potato starch, magnesium stearate, povidone, polysorbate, talc. Description White, flat-cylindrical tablets with an imprint of the company's trademark on one side, a score and a chamfer on the other side. Pharmacotherapeutic group Broad-spectrum penicillins. ATC code J01CA01 Pharmacological properties Pharmacokinetics After oral administration, ampicillin is rapidly absorbed, bioavailability is 40%; time to reach maximum concentration after oral administration of 500 mg is 2 hours, maximum concentration in blood plasma is 3-4 ng/ml. Connection with blood 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, saliva, fetal tissues. It penetrates the blood-brain barrier poorly (permeability increases with inflammation). It is excreted primarily by the kidneys (70-80%), and very high concentrations of unchanged antibiotic are created in the urine; partly with bile, in nursing mothers - with milk. Does not accumulate. Removed by hemodialysis. Pharmacodynamics Ampicillin is a broad-spectrum antibacterial bactericidal agent from the group of semisynthetic penicillins, obtained by acytylation of 6-aminopenicillanic acid with an aminophenylacetic acid residue, acid-stable. Inhibits peptidoglycan polymerase and transpeptidase, prevents the formation of peptide bonds and disrupts the late stages of cell wall synthesis of a dividing microorganism, which leads to a decrease in the osmotic stability of the bacterial cell and causes its lysis. Shows the greatest activity against gram-positive aerobic bacteria: Staphylococcus spp. (except beta-lactamase-producing strains), Staphylococcus aureus (except beta-lactamase-producing 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, moderately active against 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. Beta-lactamase-producing strains of Staphylococcus spp. are resistant to ampicillin. and other gram-negative bacteria, Pseudomonas aeruginosa, indole-positive strains of Proteus spp., Bacteroides spp., Enterobacter aerogenes, Klebsiella pneumoniae, Rickettsia spp., Mycoplasma spp., Chlamydia spp., H. pylori, Mycobacterium tuberculosis. Currently, most hospital strains of Escherichia coli and Proteus mirabilis are resistant to the drug (resistance level 20-30%). Indications for use - bronchitis, pneumonia, lung abscess - sinusitis, tonsillitis, pharyngitis, otitis media - pyelonephritis, pyelitis, cystitis, urethritis - cholangitis, cholecystitis - gonorrhea - cervicitis - erysipelas, impetigo, secondarily infected dermatoses - infections of the musculoskeletal system - pasteurellosis - listeriosis - typhoid and paratyphoid fever, dysentery, salmonellosis, salmonella carriage, peritonitis. Method of administration and dosage: Orally, adults – 0.25 g 4 times a day 0.5-1 hour before meals with a small amount of water; if necessary, the dose is increased to 3 g/day. Infections of the gastrointestinal tract and genitourinary system: 0.5 g 4 times a day. For gonococcal urethritis - 3.5 g orally once. Children over 6 years old are prescribed 1-2 g per day. The daily dose is divided into 4-6 doses. The duration of treatment depends on the severity of the disease (5-10 days). Side effects Allergic reactions: Sometimes: - skin peeling, itching, urticaria, rhinitis, conjunctivitis, Quincke's edema - dysbacteriosis, abdominal pain, nausea, vomiting Rarely: - fever, arthralgia, eosinophilia, erythematous and maculopapular rash, exfoliative dermatitis, exudative multiforme erythema, incl. Stevens-Johnson, reactions similar to serum sickness - stomatitis, gastritis, dry mouth, change in taste, diarrhea, stomatitis, glossitis, impaired liver function, moderate increase in the level of "liver" transaminases, pseudomembranous enterocolitis - agitation or aggressiveness, anxiety, confusion consciousness, changes in behavior - leukopenia, neutropenia, thrombocytopenia Very rare: - anaphylactic shock. - depression, convulsions (with high-dose therapy) - agranulocytosis, anemia Other adverse reactions: Sometimes: - vaginal candidiasis Rarely: - interstitial nephritis, nephropathy, superinfection (especially in patients with chronic diseases or reduced body resistance) Contraindications - hypersensitivity to the drug - infectious mononucleosis - lymphocytic leukemia - liver failure - history of gastrointestinal tract diseases (especially colitis associated with the use of antibiotics) - lactation period - children's age (up to 6 years) Drug interactions Antacids, glucosamine, laxatives, food slow down and reduce absorption, ascorbic acid increases the absorption of Ampicillin. Bactericidal antibiotics (including aminoglycosides, cephalosporins, cycloserine, vancomycin, rifampicin) – synergistic effect; bacteriostatic drugs (macrolides, chloramphenicol, lincosamides, tetracyclines, sulfonamides) – antagonistic. Ampicillin increases the effectiveness of indirect anticoagulants (by suppressing intestinal microflora, reducing the synthesis of vitamin K and the prothrombin index); reduces the effectiveness of estrogen-containing oral contraceptives (it is necessary to use additional methods of contraception), drugs during the metabolism of which para-amino-benzoic acid, ethinyl estradiol are formed (in the latter case, the risk of “breakthrough” bleeding increases). Diuretics, allopurinol, oxyphenbutazone, phenylbutazone, non-steroidal anti-inflammatory drugs; drugs that block tubular secretion increase the concentration (by reducing tubular secretion) of Ampicillin. When used together with Allopurinol, the risk of developing a skin rash increases. Ampicillin reduces the clearance and increases the toxicity of methotrexate and enhances the absorption of digoxin. Special instructions Use with caution: bronchial asthma, hay fever and other allergic diseases, renal failure, history of bleeding. During a course of treatment, it is necessary to monitor the function of the hematopoietic organs, liver and kidneys. It is possible that superinfection may develop due to the growth of microflora that is insensitive to it, which requires a corresponding change in antibacterial therapy. 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 agents. Treatment must be continued for another 48-72 hours after the disappearance of clinical signs of the disease. When using estrogen-containing oral contraceptives and ampicillin simultaneously, other or additional methods of contraception should be used if possible. Effect on laboratory parameters When treated with ampicillin, false-positive results may occur when determining glucose in urine using Benedict's solution, Fechtling. With the enzymatic method of determining glucose levels, the introduction of ampicillin does not affect the result of the analysis. Pregnancy Use during pregnancy is possible only for health reasons in cases where the expected benefit to the mother outweighs the potential risk to the fetus. When taking ampicillin, it is possible to develop decreased tone and weakness of uterine contractions during childbirth. Influence on the ability to drive vehicles and operate machinery. During the treatment period, it is necessary to refrain from driving vehicles and engaging in potentially hazardous activities that require increased concentration and speed of psychomotor reactions. Overdose 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, activated carbon, saline laxatives, drugs to maintain water-electrolyte balance and symptomatic. Eliminated by hemodialysis. Release form and packaging 250 mg tablets. 10 tablets in blister packs. 1 blister pack together with instructions for medical use in the state and Russian languages ​​are placed in a cardboard pack. Storage conditions Store in a dry place, at a temperature of + 15 to + 25 ° C. Keep out of the reach of children! Shelf life: 2 years Do not use after expiration date. Conditions for dispensing from pharmacies By prescription. Russian Federation, 640008, Kurgan, Constitution Avenue, 7. tel./fax

Indications for use

• sinusitis , tonsillitis , otitis , pharyngitis , bronchitis , abscess , pneumonia ;
• urinary tract infection;
• pyelonephritis;
• cholangitis;
• gonorrhea , cervicitis ;
• chlamydia in pregnant women;
• erysipelas , impetigo , infected dermatoses ;
• scarlet fever;
• pasteurellosis , listeriosis ;
• salmonellosis and its carriage, typhoid fever , dysentery ;
• peritonitis;
• endocarditis;
• meningitis;
• septicemia.

Side effects

• itching, peeling of the skin;
• rhinitis , urticaria , Quincke's edema ;
• rarely - maculopapular rash, fever, dermatitis , erythema and anaphylactic shock ;
• dysbiosis , gastritis , change in taste, dry mouth, abdominal pain, nausea, diarrhea, vomiting;
• stomatitis , glossitis , pseudomembranous enterocolitis ;
• agitation, aggressiveness, anxiety, depression, convulsions;
• leukopenia , thrombocytopenia , agranulocytosis ;
• nephritis , nephropathy ;
• vaginal candidiasis.

Side effects of the drug Ampicillin

Allergic reactions, nausea, vomiting, diarrhea, candidiasis of the oral mucosa, pseudomembranous colitis (both during treatment and several weeks after its cessation) are possible; reversible disorders of hematopoiesis and, in some cases, interstitial nephritis are rarely observed. During treatment with ampicillin, transient increases in serum aminotransferases, LDH, ALP and creatinine, a false-positive glucosuric test and a false-positive Coombs test may occur.

Instructions for use of Ampicillin (Method and dosage)

Ampicillin tablets, instructions for use

The drug in tablets or capsules is taken orally. Dosage for adults: 250-500 mg (depending on the severity of the disease) 1 hour before meals 4 times a day.

For urinary tract infections, 500 mg 4 times a day. For gonococcal urethritis, a single dose of 3.5 g is prescribed. Adults can take ampicillin tablets in a maximum daily dose of 4 g. For children, it is preferable to prescribe it in the form of a suspension, as will be discussed below.

Ampicillin/sulbactam tablets contain two parts standard dosage ampicillin and one part sulbactam. The method of their use and dosage is the same.

Ampicillin injections, instructions for use

After preparing the solution, it is administered intramuscularly or intravenously. When performing intramuscular injections, add 2 ml of Novocaine , water for injection or Lidocaine . For intravenous administration, a single dose is dissolved in 10 ml of isotonic solution or glucose solution. For a single dose of more than 2 g, it is administered dropwise; for this, 250 ml of an isotonic solution is added to the resulting antibiotic solution and 60 drops per minute are administered.

For moderate infections, adults and children weighing more than 20 kg - intramuscularly 250 - 500 mg 4 times a day, in more severe cases - 1 - 2 g 4 times a day. For meningitis - 14 g/day, divided into 6 - 8 injections. For children weighing up to 20 kg, the dose is 12.5 - 25 mg/kg per day, over 20 kg - 50-100 mg/kg per day. For meningitis, newborns weighing up to 2 kg are prescribed intravenously 25 mg per kg body weight every 12 hours throughout the first week, then 50 mg per kg body weight every 8 hours.

Special instructions for the use of Ampicillin

Before using ampicillin, a sensitivity test to the antibiotic should be performed. Use extreme caution in patients with hypersensitivity to cephalosporins, griseofulvin or penicillamine. During long-term treatment with ampicillin, it is recommended to periodically monitor the function of the kidneys, liver and hematopoietic organs. The possibility of superinfection caused by pathogenic fungi or resistant bacteria should be considered. If superinfection develops, adequate therapy is prescribed.

Interaction

Bacteriostatic agents ( macrolides , chloramphenicol , sulfonamides , lincosamides , tetracyclines ) have an antagonistic effect, bactericidal antibiotics ( aminoglycosides , Vancomycin , cephalosporins , Rifampicin ) have a synergistic effect.

Antacids and laxatives , food intake reduce absorption, and ascorbic acid .

Strengthens the effect of anticoagulants , reduces the effectiveness of estrogen- containing contraceptives .

Diuretics , Allopurinol , Phenylbutazone , Oxyphenbutazone , NSAIDs , increase the concentration of the active substance due to a decrease in tubular secretion.

Concomitant use of Allopurinol causes a risk of skin rash.

Enhances the absorption of Digoxin . Increases the toxicity of Methotrexate .

Drug interactions Ampicillin

If combined parenteral treatment with ampicillin and aminoglycoside antibiotics is necessary, they should be administered at different sites with an interval of 1 hour due to the risk of inactivation. Ampicillin may cause a decrease in the effectiveness of oral hormonal contraceptives. Ampicillin in high doses reduces the level of atenolol in the blood plasma, so it is recommended to use these drugs separately, and take atenolol before using ampicillin. Concomitant use with allopurinol significantly increases the likelihood of skin rash. Probenecid may reduce the renal excretion of ampicillin and lead to increased plasma concentrations. During treatment with ampicillin, false-positive results of non-enzymatic glucosuric tests can be determined.

Ampicillin for children

The suspension for children is intended for use from one month of age. To prepare it, add boiled water to the bottle with granules to the mark, shake, and store at room temperature for 2 weeks. Shake thoroughly before use. Pay attention to the dosage - there are suspensions containing 125 mg and 250 mg of active substance. If we take the last option, then in 1 full measuring spoon (5 ml of suspension) there will be 250 mg of the active substance, the bottom mark of the spoon corresponds to 125 mg.

Dosage for children with mild infection: up to 1 year - at the rate of 100 mg/kg body weight per day, from 1 year to 4 years - 100-150 mg/kg body weight per day, over 4 years - 1-2 g per day. The required dose should be given in 4 or 6 doses.

Ampicillin and alcohol

The instructions do not mention anything about whether alcohol and ampicillin are combined. However, upon reflection, we can conclude that drinking alcohol can cause or intensify adverse reactions, reduce the content of the active substance in tissues and reduce the effectiveness of antibiotic therapy. And this is due to the fact that when drinking alcohol, the cytochrome P450 (it is induced), and the enzymes of other cytochromes necessary for drug metabolism are suppressed. of glucuronic acid , which is necessary for binding toxic substances and drug metabolites, is also reduced

Ampicillin analogues

Level 4 ATC code matches:
Hiconcil

Ampioks

Ampicillin Trihydrate

Ospamox

Amoxicar

Penicillin

Flemoxin Solutab

Amoxicillin

Amosin

Amoxil

Ecoball

Analogs with one active ingredient: Pentrexil , Penodil , Zetsil , Standacillin .

Reviews about Ampicillin

What is Ampicillin tablets for? This is an antibiotic of the penicillin , so it is used for various infections, including, has not lost its relevance in the treatment of shigellosis . Ampicillin is still widely used today, primarily due to the fact that it is available to the vast majority of patients and practically does not cause liver dysfunction (frequency less than 0.1%, compared to Cefotaxime 8% and aminoglycodides - 15%). In medical practice, Ampicillin capsules and tablets are used in the form trihydrate , as well as granules for preparing a suspension. It must be said that oral forms of this drug have low bioavailability - only 40%. As a drug for intramuscular administration, it is effective in the treatment of many infections, but as a drug for oral administration in most cases it is inferior to Amoxicillin , the advantage of which is better and stable absorption, the absence of influence on it by food intake, and also a smaller frequency of use. In addition, oral administration of this drug can cause dysbiosis , while Amoxicillin slightly suppresses the flora. Frequent use of the drug in children (every 4 months) can lead to fluorosis - a defect in tooth enamel.

Reviews of Ampicillin are mostly related to its use for sore and sinusitis , for severe cases of which injections of “pure” ampicillin or its combination with sulbactam - Ampisulbin , Sultasin or Ouanazine .

Indications for use include its use for infections of the ear, throat, paranasal sinuses, cystitis and pyelonephritis . The choice of this drug for pyelonephritis is explained by the lack of nephrotoxicity, the effect on E. coli (the main cause of urinary tract infections) and the ability to be excreted in urine in therapeutic concentrations.

For uncomplicated pyelonephritis, treatment began with ampicillin. fluoroquinolones or cephalosporins were added after 2–3 days . Only some patients experienced nausea, vomiting, stool upset, rash and itching during treatment.

Pharmacological properties of the drug Ampicillin

Semi-synthetic antibiotic of the penicillin group. It has a bactericidal effect by competitively blocking transpeptidases involved in the synthesis of mucopeptide, which is part of the cell membrane. Active against proliferating bacteria. Effective against gram-positive and some gram-negative microorganisms, including E. coli, Proteus mirabilis, Salmonella spp., Shigella spp., Haemophilus influenzae, Bordetella pertussis, Neisseria gonorrhoeae, Neisseria meningitidis. Ampicillin is also active against gram-positive anaerobic cocci and bacteria (Peptococcus spp., Pertosteptococcus spp., Clostridium spp., Corynebacterium spp.). Penicillinase-forming staphylococci are resistant to ampicillin. When taken orally, ampicillin is not destroyed in the acidic environment of the stomach and is well absorbed in the digestive tract. Concomitant food intake reduces the absorption of the antibiotic. The maximum concentration in the blood is reached 1–2 hours after administration and decreases slowly over 6 hours. The maximum concentration in the blood plasma after intramuscular administration is reached after 1 hour. About 28% of ampicillin is bound to plasma proteins. The half-life from blood plasma is 1–2 hours; in newborns, elderly patients and patients with impaired renal function, it may be prolonged. Ampicillin is well distributed in tissues and body fluids. It weakly penetrates the blood-brain barrier; during meningitis, its concentration in the cerebrospinal fluid increases. Penetrates through the placental barrier. Found in small quantities in breast milk. It is excreted unchanged by the kidneys through glomerular filtration and tubular secretion; about 20% of the antibiotic is excreted in the bile. Partially removed during hemodialysis.

Ampicillin price, where to buy

You can buy this drug in many pharmacies in Moscow.

The price of Ampicillin tablets 250 mg No. 20 ranges from 16 rubles. up to 21 rub. One bottle of Ampicillin sodium salt powder 500 mg costs 7-9 rubles.

To purchase the drug, you will need a prescription in Latin, issued by a doctor.

• Online pharmacies in RussiaRussia
• Online pharmacies in UkraineUkraine
• Online pharmacies in KazakhstanKazakhstan

LuxPharma* special offer

• Ampicillin amp.
  1 g No. 10 1900 rub. order

show more

Pharmacy24

• Ampicillin-KMP 250 mg No. 10 tablets PAT "Kievmedpreparat", Ukraine
  20 UAH. order
• Ampicillin-KMP 250 mg No. 20 tablets PAT "Kievmedpreparat", Ukraine

  36 UAH order

• Ampicillin-KMP 0.5 g PAT "Kievmedpreparat", Ukraine

  7 UAH order

• Ampicillin-KMP 1 g PAT "Kievmedpreparat", Ukraine

  9 UAH order

PaniPharmacy

• Ampicillin tablets Ampicillin t/g tablet. 0.25g No. 20 Ukraine, Kievmedpreparat OJSC

  42 UAH order

• Ampicillin bottle Ampicillin sodium salt powder for injection 1g Ukraine, Kievmedpreparat OJSC

  11 UAH order

• Ampicillin tablets Ampicillin t/g tablet. 0.25g No. 10 Ukraine, Kievmedpreparat OJSC

  21 UAH order

show more