Composition, structure and packing
Powder for solution for injection microcrystalline, white or nearly white, with faint characteristic odor; hygroscopic.
1 vial. amoxicillin (in the form of sodium salt) 1 PM
Clinico-pharmacological group: Antibiotic penicillin group of broad-spectrum, collapsing penicillinase.
Pharmacological action
Broad-spectrum antibiotic of semisynthetic penicillins. Effective bactericidal. On the mechanism of action is to inhibit the synthesis of bacterial cell wall.
It is active against Gram-positive microorganisms: Staphylococcus spp. (Not forming penicillinase), Streptococcus spp. (Including Str.pyogenes, Str. Pneumoniae, Str.viridans), most strains of Enterococcus faecalis, Bacillus anthracis, Clostridium spp., Corynebacterium spp.; Majority of Gram-negative microorganisms: Neisseria gonorrhoeae, Neisseria meningitidis, Haemophilus influenzae, Moraxella catarrhalis , Escherichia coli, Salmonella spp., Shigella spp., Proteus mirabilis, Helicobacter pylori, Campylobacter spp., Prevotella melaninogenica. To the drug resistant Proteus spp. (Indole-positive), Moraxella morganii, Pseudomonas spp., Serratia spp., Enterobacter spp., As well as rickettsia, mycoplasma, viruses. Amoksisar destroyed by penicillinase, and therefore not active against penitsillinazoobrazuyuschih strains of pathogens.
Pharmacokinetics
Absorption and distribution
After parenteral administration is rapidly absorbed and distributed in tissues and body fluids. Cmax observed after 1 h after i / m administration and after 30 minutes - after a / c; stored on a therapeutic level of 6-8 hours with serum proteins bound slightly (about 17%). Amoxicillin is found in high concentrations in sputum, bronchial secretion, lung tissue, soft tissue, ENT organs, prostate, gall.
Penetrates into peritoneal, pleural and synovial exudates. Normally poorly crosses the BBB. When inflammation of the meninges, its concentration in the cerebrospinal fluid (with a / in the introduction of maximum doses of antibiotic) achieves an effective level in respect of highly sensitive pathogens.
Penetrates through the placental barrier. The concentration of drug in amniotic fluid and umbilical vein blood of the fetus is 25-30% from its level in blood plasma. In a minimum amount excreted in breast milk.
Withdrawal
Amoxicillin is derived mainly from urine, and partly from the bile. Concentrations of amoxicillin, created in the urine and bile, significantly higher than the IPC for the infectious agents of this localization.
In the absence of renal dysfunction T1 / 2 of amoxicillin is 1.3 hours cumulation of amoxicillin in normal renal function under conditions of repeated administration at intervals of 8 h was observed.
Pharmacokinetics in special clinical situations
When expressed renal dysfunction (CC <10 ml / min) T1 / 2 of amoxicillin increased to 24 h, while anuria - up to 48 hours or more with increasing concentration of amoxicillin in plasma.
Statement
Infectious-inflammatory diseases caused by microorganisms sensitive to the drug:
sepsis
serologies
endocarditis;
peritonitis;
respiratory infection (bronchitis and acute exacerbation of chronic pneumonia, empyema, lung abscess);
otitis;
infection of urogenital system (pyelitis, pyelonephritis, cystitis, urethritis, prostatitis);
gynecologic infections (endometritis, parameters, cervicitis);
gonorrhea;
aggravation of gastric ulcer and duodenal ulcer associated with Helicobacter pylori (in the complex therapy);
infections of skin and soft tissues;
infections of the musculoskeletal system (ostemielit, arthritis);
burn and wound infections. Prevention of postoperative complications.
Dosage regimen
The drug is introduced into the / m or / in the jet or drip. Adult drug injected by 1-2 g every 8-12 h (3-6 g / day). A single dose of i / m administration should not exceed 1, the maximum daily dose for adults - 6 PM
Newborns, and preterm infants (under 1 year), the medication prescribed in a daily dose of 100 mg / kg, for children aged over 1 year - 50 mg / kg body weight.
A single dose of i / m administration - not above 500 mg. In severe infections these doses for adults and children can be increased by 1.5-2 times. In this case, the dose is introduced into / in. The daily dose distributes to the introduction of 2-3 with intervals of 8-12 h. To prevent postoperative complications of introducing drug / in 30 min or in / m for 1 h before surgery at a dose of 0.5-1 town again during the first postoperative days drug is used in the same dose every 8-12 hours
In operations on the infected areas of the duration of the prophylactic use may be extended to 3-5 days.
In case of violation of renal function should reduce the dose of the drug or increase the interval between infusions (24-48 h). When spacecraft 10 to 30 ml / min the drug is introduced at a daily dose of 1 g, then 500 mg every 12 h and CC less than 10 ml / min - 1 g, then 500 mg every 24 hours
Patients in a state of anuria daily dose should not exceed 2 Patients who are on hemodialysis, an additional 1 g of product: 500 mg during hemodialysis, and 500 mg thereafter.
Terms of preparing and implementing a solution for i / m and / in the introduction
For i / m administration solution is prepared before the introduction, adding to the contents of the vial (1 g), 3 ml of water for injection.
For iv administration a single dose of jet preparation (no more than 2 g) dissolved in 10-20 ml 0.9% sodium chloride solution and injected slowly over 3-5 minutes. When a single dose greater than 2 g, a drug is introduced into / in the drip. For iv drip a single dose (2.4 g) dissolved in 125-250 ml 0.9% sodium chloride or 5-10% dextrose and injected at a speed of 60-80 drops / min. When a drip children as a solvent using 5% dextrose (50-100 ml depending on age) and injected at 10 Cap. / min daily dose distributes 2-3 introduction.
Side effect
Allergic reactions: urticaria, flushing of the skin, erythema, angioedema, rhinitis, conjunctivitis, rarely - fever, arthralgia, eosinophilia, exfoliative dermatitis, erythema multiforme, Stevens-Johnson syndrome, reactions similar to serum sickness, and in some cases - anaphylactic shock.
On the part of the digestive system: dysbacteriosis, alteration of taste, nausea, vomiting, diarrhea, stomatitis, glossitis, abnormal liver function, a moderate increase in liver transaminases, pseudomembranous enterocolitis.
From the central nervous system and peripheral nervous system: agitation, anxiety, insomnia, ataxia, confusion, behavioral change, depression, peripheral neuropathy, headache, dizziness, convulsive reaction.
On the part of the hemopoietic system: leukopenia, neutropenia, thrombocytopenic purpura, anemia.
On the part of the urinary tract: interstitial nephritis.
Other: shortness of breath, tachycardia, interstitial nephritis, vaginal candidiasis, superinfection (especially in patients with chronic diseases and low resistance of the organism).
Contraindications
infectious mononucleosis;
marked disturbances of liver function;
Hypersensitivity to the drug or other antibiotics of penicillin and cephalosporins.
Precautions should be prescribed the drug to patients with polyvalent allergies, digestive diseases (especially pseudomembranous colitis associated with antibiotics), and renal insufficiency.
Pregnancy and lactation
Precautions should use the drug during pregnancy and lactation.
Application for violations of liver function
Contraindications disturbancies liver function.
Application for violations of renal function
In case of violation of renal function should reduce the dose of the drug or increase the interval between infusions (24-48 h). When spacecraft 10 to 30 ml / min the drug is introduced at a daily dose of 1 g, then 500 mg every 12 h and CC less than 10 ml / min - 1 g, then 500 mg every 24 hours
Patients in a state of anuria daily dose should not exceed 2 Patients who are on hemodialysis, an additional 1 g of product: 500 mg during hemodialysis, and 500 mg thereafter.
Cautions
In applying Amoksisara should regularly monitor the function of blood, liver and kidneys.
In applying the drug may develop superinfection due to growth insensitive microflora, which requires a change in antibiotic therapy.
When treating patients with bacteremia may develop bacteriolysis reaction (reaction Jarisch-Herxheimer). There is cross-resistance and cross-hypersensitivity to penicillins, cephalosporins.
In the treatment of mild diarrhea, which appeared on the background of Amoksisara should avoid appointment antidiarrhoeal drugs that reduce peristalsis, you can use kaolin or attapulgite. The emergence of severe diarrhea is the reason for the termination of the drug.
Treatment should be continued even 48-72 hours after the disappearance of clinical signs of disease.
With simultaneous use of oral contraceptives and estrogensoderzhaschih Amoksisara should use additional methods of contraception. Overdose Symptoms: neurotoxic reactions, thrombocytopenia (with prolonged use at high doses). These phenomena are reversible and disappear after drug discontinuation.
Drug Interactions
With simultaneous application of Amoksisara with antibiotics, has a bactericidal action (including aminoglycosides, cephalosporins, cycloserine, vancomycin, rifampicin) is observed synergies, and with antibiotics that provide a bacteriostatic effect (tetracyclines, macrolides, chloramphenicol, Lincosamides, sulfonamides), - antagonism. Amoksisar while the application increases the effectiveness of indirect anticoagulants (due to the suppression of intestinal microflora, reduces the synthesis of vitamin K and prothrombin index).
Amoksisar estrogensoderzhaschih reduces the effectiveness of oral contraceptives, which is accompanied by risk of breakthrough bleeding. Amoksisar while the application reduces the effectiveness of drugs, in the process of metabolism that produce Pabco.
Diuretics, allopurinol, fenilbutazon, oxyphenbutazone, NSAIDs, drugs that block tubular secretion, while the use of Amoksisarom reduce its tubular secretion and increase the concentration of amoxicillin in plasma. Allopurinol while applying with Amoksisarom increases the risk of skin rashes. Amoksisar reduces clearance and increases the toxicity of methotrexate. Amoksisar while the application increases the absorption of digoxin.
Terms and Conditions of storage
List B. The drug should be stored in dry, protected from light, away from children at or above 25 ° C. Shelf life - 2 years.
Powder for solution for injection microcrystalline, white or nearly white, with faint characteristic odor; hygroscopic.
1 vial. amoxicillin (in the form of sodium salt) 1 PM
Clinico-pharmacological group: Antibiotic penicillin group of broad-spectrum, collapsing penicillinase.
Pharmacological action
Broad-spectrum antibiotic of semisynthetic penicillins. Effective bactericidal. On the mechanism of action is to inhibit the synthesis of bacterial cell wall.
It is active against Gram-positive microorganisms: Staphylococcus spp. (Not forming penicillinase), Streptococcus spp. (Including Str.pyogenes, Str. Pneumoniae, Str.viridans), most strains of Enterococcus faecalis, Bacillus anthracis, Clostridium spp., Corynebacterium spp.; Majority of Gram-negative microorganisms: Neisseria gonorrhoeae, Neisseria meningitidis, Haemophilus influenzae, Moraxella catarrhalis , Escherichia coli, Salmonella spp., Shigella spp., Proteus mirabilis, Helicobacter pylori, Campylobacter spp., Prevotella melaninogenica. To the drug resistant Proteus spp. (Indole-positive), Moraxella morganii, Pseudomonas spp., Serratia spp., Enterobacter spp., As well as rickettsia, mycoplasma, viruses. Amoksisar destroyed by penicillinase, and therefore not active against penitsillinazoobrazuyuschih strains of pathogens.
Pharmacokinetics
Absorption and distribution
After parenteral administration is rapidly absorbed and distributed in tissues and body fluids. Cmax observed after 1 h after i / m administration and after 30 minutes - after a / c; stored on a therapeutic level of 6-8 hours with serum proteins bound slightly (about 17%). Amoxicillin is found in high concentrations in sputum, bronchial secretion, lung tissue, soft tissue, ENT organs, prostate, gall.
Penetrates into peritoneal, pleural and synovial exudates. Normally poorly crosses the BBB. When inflammation of the meninges, its concentration in the cerebrospinal fluid (with a / in the introduction of maximum doses of antibiotic) achieves an effective level in respect of highly sensitive pathogens.
Penetrates through the placental barrier. The concentration of drug in amniotic fluid and umbilical vein blood of the fetus is 25-30% from its level in blood plasma. In a minimum amount excreted in breast milk.
Withdrawal
Amoxicillin is derived mainly from urine, and partly from the bile. Concentrations of amoxicillin, created in the urine and bile, significantly higher than the IPC for the infectious agents of this localization.
In the absence of renal dysfunction T1 / 2 of amoxicillin is 1.3 hours cumulation of amoxicillin in normal renal function under conditions of repeated administration at intervals of 8 h was observed.
Pharmacokinetics in special clinical situations
When expressed renal dysfunction (CC <10 ml / min) T1 / 2 of amoxicillin increased to 24 h, while anuria - up to 48 hours or more with increasing concentration of amoxicillin in plasma.
Statement
Infectious-inflammatory diseases caused by microorganisms sensitive to the drug:
sepsis
serologies
endocarditis;
peritonitis;
respiratory infection (bronchitis and acute exacerbation of chronic pneumonia, empyema, lung abscess);
otitis;
infection of urogenital system (pyelitis, pyelonephritis, cystitis, urethritis, prostatitis);
gynecologic infections (endometritis, parameters, cervicitis);
gonorrhea;
aggravation of gastric ulcer and duodenal ulcer associated with Helicobacter pylori (in the complex therapy);
infections of skin and soft tissues;
infections of the musculoskeletal system (ostemielit, arthritis);
burn and wound infections. Prevention of postoperative complications.
Dosage regimen
The drug is introduced into the / m or / in the jet or drip. Adult drug injected by 1-2 g every 8-12 h (3-6 g / day). A single dose of i / m administration should not exceed 1, the maximum daily dose for adults - 6 PM
Newborns, and preterm infants (under 1 year), the medication prescribed in a daily dose of 100 mg / kg, for children aged over 1 year - 50 mg / kg body weight.
A single dose of i / m administration - not above 500 mg. In severe infections these doses for adults and children can be increased by 1.5-2 times. In this case, the dose is introduced into / in. The daily dose distributes to the introduction of 2-3 with intervals of 8-12 h. To prevent postoperative complications of introducing drug / in 30 min or in / m for 1 h before surgery at a dose of 0.5-1 town again during the first postoperative days drug is used in the same dose every 8-12 hours
In operations on the infected areas of the duration of the prophylactic use may be extended to 3-5 days.
In case of violation of renal function should reduce the dose of the drug or increase the interval between infusions (24-48 h). When spacecraft 10 to 30 ml / min the drug is introduced at a daily dose of 1 g, then 500 mg every 12 h and CC less than 10 ml / min - 1 g, then 500 mg every 24 hours
Patients in a state of anuria daily dose should not exceed 2 Patients who are on hemodialysis, an additional 1 g of product: 500 mg during hemodialysis, and 500 mg thereafter.
Terms of preparing and implementing a solution for i / m and / in the introduction
For i / m administration solution is prepared before the introduction, adding to the contents of the vial (1 g), 3 ml of water for injection.
For iv administration a single dose of jet preparation (no more than 2 g) dissolved in 10-20 ml 0.9% sodium chloride solution and injected slowly over 3-5 minutes. When a single dose greater than 2 g, a drug is introduced into / in the drip. For iv drip a single dose (2.4 g) dissolved in 125-250 ml 0.9% sodium chloride or 5-10% dextrose and injected at a speed of 60-80 drops / min. When a drip children as a solvent using 5% dextrose (50-100 ml depending on age) and injected at 10 Cap. / min daily dose distributes 2-3 introduction.
Side effect
Allergic reactions: urticaria, flushing of the skin, erythema, angioedema, rhinitis, conjunctivitis, rarely - fever, arthralgia, eosinophilia, exfoliative dermatitis, erythema multiforme, Stevens-Johnson syndrome, reactions similar to serum sickness, and in some cases - anaphylactic shock.
On the part of the digestive system: dysbacteriosis, alteration of taste, nausea, vomiting, diarrhea, stomatitis, glossitis, abnormal liver function, a moderate increase in liver transaminases, pseudomembranous enterocolitis.
From the central nervous system and peripheral nervous system: agitation, anxiety, insomnia, ataxia, confusion, behavioral change, depression, peripheral neuropathy, headache, dizziness, convulsive reaction.
On the part of the hemopoietic system: leukopenia, neutropenia, thrombocytopenic purpura, anemia.
On the part of the urinary tract: interstitial nephritis.
Other: shortness of breath, tachycardia, interstitial nephritis, vaginal candidiasis, superinfection (especially in patients with chronic diseases and low resistance of the organism).
Contraindications
infectious mononucleosis;
marked disturbances of liver function;
Hypersensitivity to the drug or other antibiotics of penicillin and cephalosporins.
Precautions should be prescribed the drug to patients with polyvalent allergies, digestive diseases (especially pseudomembranous colitis associated with antibiotics), and renal insufficiency.
Pregnancy and lactation
Precautions should use the drug during pregnancy and lactation.
Application for violations of liver function
Contraindications disturbancies liver function.
Application for violations of renal function
In case of violation of renal function should reduce the dose of the drug or increase the interval between infusions (24-48 h). When spacecraft 10 to 30 ml / min the drug is introduced at a daily dose of 1 g, then 500 mg every 12 h and CC less than 10 ml / min - 1 g, then 500 mg every 24 hours
Patients in a state of anuria daily dose should not exceed 2 Patients who are on hemodialysis, an additional 1 g of product: 500 mg during hemodialysis, and 500 mg thereafter.
Cautions
In applying Amoksisara should regularly monitor the function of blood, liver and kidneys.
In applying the drug may develop superinfection due to growth insensitive microflora, which requires a change in antibiotic therapy.
When treating patients with bacteremia may develop bacteriolysis reaction (reaction Jarisch-Herxheimer). There is cross-resistance and cross-hypersensitivity to penicillins, cephalosporins.
In the treatment of mild diarrhea, which appeared on the background of Amoksisara should avoid appointment antidiarrhoeal drugs that reduce peristalsis, you can use kaolin or attapulgite. The emergence of severe diarrhea is the reason for the termination of the drug.
Treatment should be continued even 48-72 hours after the disappearance of clinical signs of disease.
With simultaneous use of oral contraceptives and estrogensoderzhaschih Amoksisara should use additional methods of contraception. Overdose Symptoms: neurotoxic reactions, thrombocytopenia (with prolonged use at high doses). These phenomena are reversible and disappear after drug discontinuation.
Drug Interactions
With simultaneous application of Amoksisara with antibiotics, has a bactericidal action (including aminoglycosides, cephalosporins, cycloserine, vancomycin, rifampicin) is observed synergies, and with antibiotics that provide a bacteriostatic effect (tetracyclines, macrolides, chloramphenicol, Lincosamides, sulfonamides), - antagonism. Amoksisar while the application increases the effectiveness of indirect anticoagulants (due to the suppression of intestinal microflora, reduces the synthesis of vitamin K and prothrombin index).
Amoksisar estrogensoderzhaschih reduces the effectiveness of oral contraceptives, which is accompanied by risk of breakthrough bleeding. Amoksisar while the application reduces the effectiveness of drugs, in the process of metabolism that produce Pabco.
Diuretics, allopurinol, fenilbutazon, oxyphenbutazone, NSAIDs, drugs that block tubular secretion, while the use of Amoksisarom reduce its tubular secretion and increase the concentration of amoxicillin in plasma. Allopurinol while applying with Amoksisarom increases the risk of skin rashes. Amoksisar reduces clearance and increases the toxicity of methotrexate. Amoksisar while the application increases the absorption of digoxin.
Terms and Conditions of storage
List B. The drug should be stored in dry, protected from light, away from children at or above 25 ° C. Shelf life - 2 years.
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