Composition, structure and packing
Gelatin capsules are white, the contents of capsules - white granules.
1 capsule. amoxicillin (in the form of trihydrate) 250 mg.
Excipients: potato starch.
Tablets are white or nearly white, ploskotsilindricheskie, with beveled and risks.
1 tab. amoxicillin (in the form of trihydrate) 250 mg - - 500 mg.
Excipients: potato starch, magnesium stearate, calcium stearate, magnesium hydrosilicate (talc), povidone (kollidon 90F).
Powder for suspension for oral white with a yellowish tint, with a specific smell, preparation of suspensions of white with a yellowish tint, with a specific smell.
A pack. amoxicillin (in the form of trihydrate) 125 mg.
Excipients: polyvinylpyrrolidone (povidone), dextrose, disodium salt of ethylenediaminetetraacetic acid (Trilon B) (edetate disodium), sodium phosphate, disodium (sodium hydrophosphate), sodium α-glutamate monohydrate, food flavoring, vanilla, sucrose.
Powder for suspension for oral white with a yellowish tint, with a specific smell, preparation of suspensions of white with a yellowish tint, with a specific smell.
A pack. amoxicillin (in the form of trihydrate) 250 mg.
Excipients: polyvinylpyrrolidone (povidone), dextrose, disodium salt of ethylenediaminetetraacetic acid (Trilon B) (edetate disodium), sodium phosphate, disodium (sodium hydrophosphate), sodium α-glutamate monohydrate, food flavoring, vanilla, sucrose.
Powder for suspension for oral white with a yellowish tint, with a specific smell, preparation of suspensions of white with a yellowish tint, with a specific smell.
A pack. amoxicillin (in the form of trihydrate) 500 mg.
Excipients: polyvinylpyrrolidone (povidone), dextrose, disodium salt of ethylenediaminetetraacetic acid (Trilon B) (edetate disodium), sodium phosphate, disodium (sodium hydrophosphate), sodium α-glutamate monohydrate, food flavoring, vanilla, sucrose.
Clinico-pharmacological group: Antibiotic penicillin group of broad-spectrum, collapsing penicillinase.
Pharmacological action
Broad-spectrum antibiotic of semisynthetic penicillins. Effective bactericidal. Inhibits transpeptidase, violates the synthesis of peptidoglycan (the reference polymer cell wall) in the period of division and growth, causes lysis of bacteria. Acid-resistant. Active against aerobic gram-positive bacteria: Staphylococcus spp. (With the exception of strains producing penicillinase), Streptococcus spp. and aerobic gram-negative bacteria: Neisseria gonorrhoeae, Neisseria meningitidis, Bacillus anthracis, Listeria monocytogenes, Helicobacter pylori, Klebsiella spp. Microorganisms, penicillinase-producing, resistant to the action of amoxicillin. The action develops within 15-30 min after injection and lasts 8 hours
Pharmacokinetics
Absorption
After oral amoxicillin quickly and almost completely (93%) absorbed from the gastrointestinal tract. Eating does not affect the absorption of the drug, is not destroyed in the acidic environment of the stomach. Cmax of the active substance in the plasma observed after 1-2 h. When administered at a dose of 125 mg and 250 mg Cmax plasma levels of 1.5-3 mg / ml and 3.5-5 mg / ml, respectively.
Distribution
It has a large volume of distribution: in high concentrations found in plasma, sputum, bronchial secretion (purulent bronchial secretion in the distribution of the poor), pleural and peritoneal fluid, urine, contents of skin blisters, tissue of the lung, intestinal mucosa, the female genital organs, prostate gland, middle ear fluid, bone, fat tissue, gall bladder (with normal liver function), fetal tissues.
With increasing doses of 2 times the concentration also increased by 2 times. The concentration in bile exceeds the concentration in plasma 2-4 times. In the amniotic fluid and umbilical cord vessels concentrations of amoxicillin - 25-30% of the level in plasma in pregnant women. Poorly crosses the BBB, the inflammation of the meninges (meningitis) concentration in cerebrospinal fluid - about 20%. Binding to plasma proteins - 17%. In small amounts excreted in breast milk.
Metabolism
Amoxicillin partly metabolized to form inactive metabolites.
Withdrawal
T1 / 2 of amoxicillin is 1-1.5 hours Amoxicillin output by 50-70% in the urine in unchanged form by tubular excretion (80%) and glomerular filtration rate (20%), with bile - 10-20%. Premature, Newborn and children under 6 months - 3-4 hours
Pharmacokinetics in special clinical situations
In preterm, newborns and children under 6 months of T1 / 2 of 3-4 h. In renal dysfunction (CC ≤ 15 mL / min) T1 / 2 of amoxicillin increased to 8.5 h. Amoxicillin is removed during hemodialysis.
Statement
Infectious-inflammatory diseases caused by microorganisms sensitive to the drug:
Respiratory infections (including bronchitis, pneumonia);
infection ENT organs (including sinusitis, pharyngitis, tonsillitis, acute otitis media);
infections of the genitourinary system (including pyelonephritis, pyelitis, cystitis, urethritis, gonorrhea);
gynecologic infections (including endometritis, cervicitis);
gastrointestinal tract infections (including peritonitis, enterocolitis, typhoid fever, cholangitis, cholecystitis);
infections of skin and soft tissue (including erysipelas, impetigo, secondarily infected dermatitis);
leptospirosis;
listeriosis;
Lyme disease (Lyme disease);
dysentery
salmonellosis, salmonellonositelstvo;
serologies
endocarditis (prophylaxis);
sepsis.
Dosage regimen
The drug, taken orally, either before or after meals.
Dosage regimen set individually, taking into account the severity of the disease, susceptible to the drug, the patient's age.
Adults and children over 10 years (with a body weight> 40 kg) each appoint 500 mg 3 times / day, in case of serious illness - at 0.75-1 g 3 times / day.
Children aged 5 to 10 years prescribed 250 mg 3 times / day, at the age of 2 to 5 years - 125 mg 3 times / day, up to 2 years - 20 mg / kg / day in 3 divided doses. The treatment course - 5-12 days.
Children aged under 5 years of drug administered in the form of suspension. For the treatment of acute uncomplicated gonorrhea drug administered in a dose of 3 g once, in the treatment of women should receive a second dose given.
In acute infectious diseases of the digestive tract (paratyphoid fever, typhoid fever), and biliary tract, gynecological infectious diseases of adults appoint 1.5-2 g 3 times / day or 1-1.5 g 4 times / day.
In leptospirosis adults appoint 500-750 mg 4 times / day for 6-12 days.
When salmonellonositelstve adults - 1.5-2 g 3 times / day for 2-4 weeks. For the prevention of endocarditis with small surgical interventions for adults prescribed a dose of 3-4 g for 1 h before the procedure.
If you want to be reappointed after a dose of 8-9 h. In children, the dose is reduced by half. Patients with impaired renal function (QC from 15 to 40 ml / min) interval between doses increased to 12 hours in the terminal stage of chronic renal failure (CC <10 ml / min) Amosina dose should be reduced by 15-50%, or increase the interval between doses up to 24 h, when anuria - the maximum dose of 2 g / day.
Terms preparation of the suspension
Single-dose pack
In a clean glass poured boiled and cooled water in the amount indicated in the table, then pour the contents of one packet and mix until a homogeneous suspension.
Side effect
Allergic reactions: Possible - urticaria, flushing of the skin, erythema, angioedema, rhinitis, conjunctivitis, rarely - fever, joint pain, eosinophilia, exfoliative dermatitis, erythema multiforme exudative, Stevens-Johnson syndrome, reactions similar to serum sickness and in individual cases - anaphylactic shock.
On the part of the digestive system: dysbacteriosis, change in taste, vomiting, nausea, diarrhea, stomatitis, glossitis, abnormal liver function, a moderate increase in liver transaminases; rarely - 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.
From the urinary system: rarely - interstitial nephritis.
On the part of the hemopoietic system: leukopenia, neutropenia, thrombocytopenic purpura, anemia.
Other: shortness of breath, tachycardia, candidiasis of the vagina, superinfection (especially in patients with chronic diseases or low resistance of the organism).
Contraindications
allergic diathesis;
bronchial asthma, pollinosis;
infectious mononucleosis;
lymphocytic leukemia;
hepatic impairment;
digestive diseases in the history of (especially colitis, associated with the use of antibiotics);
Lactation (breastfeeding);
Hypersensitivity to the drug's components;
sensitivity to other penicillins, cephalosporins, carbapenems);
Children under 3 years (for tablets and capsules).
Precautions should be prescribed the drug during pregnancy, renal insufficiency, as well as guidance on the history of bleeding.
Pregnancy and lactation
Use of the drug during pregnancy is possible only in cases where the intended use of therapy to the mother outweighs the potential risk to the fetus.
Use during lactation is contraindicated. If necessary, use during lactation should stop breastfeeding.
Application for violations of liver function
Contraindicated in hepatic failure.
Application for violations of renal function
Patients with impaired renal function (QA - 15-40 ml / min) interval between doses increased to 12 hours in the terminal stage of chronic renal failure (CC <10 ml / min) Amosina dose should be reduced by 15-50%, or increase the interval between doses up to 24 h, when anuria - the maximum dose of 2 g / day.
Cautions
In the course of treatment Amosinom need to monitor the state functions of blood, liver and kidneys. Perhaps the development of superinfection due to growth insensitive to amoxicillin microflora, which requires a corresponding change in antimicrobial therapy.
When treating patients with bacteremia rarely develops bacteriolysis reaction (reaction Jarisch-Herxheimer). Patients who have an increased sensitivity to penicillin, may be cross-allergic reactions to cephalosporin antibiotics.
In the treatment of mild diarrhea during treatment Amosina avoid appointment antidiarrhoeal drugs that reduce intestinal motility; can use kaolin or attapulgitsoderzhaschie antidiarrhoeal funds.
Patients with severe diarrhea should make a differential diagnosis and assign the appropriate therapy.
Treatment should be continued even 48-72 hours after the disappearance of clinical signs of disease.
With simultaneous use of oral contraceptives estrogensoderzhaschih and amoxicillin should, if possible, to use additional methods of contraception.
Overdose
Symptoms: nausea, vomiting, diarrhea, disruption of water and electrolyte balance (as a consequence of vomiting and diarrhea). Treatment: gastric lavage, activated charcoal, saline laxatives, measures aimed at maintaining water and electrolyte balance; hemodialysis.
Drug Interactions
Antacids, glucosamine, laxatives, diet, aminoglycoside antibiotics, while applying slow and reduce the absorption of amoxicillin, ascorbic acid - increases its absorption. Bactericidal antibiotics (including aminoglycosides, cephalosporins, cycloserine, vancomycin, rifampicin) often synergy with amoxicillin; bacteriostatic drugs (macrolides, chloramphenicol, Lincosamides, tetracyclines, sulfonamides) - antagonism.
Amoxicillin, while the application increases the effectiveness of indirect anticoagulants (suppressing the intestinal microflora, reduces the synthesis of vitamin K and prothrombin index); estrogensoderzhaschih reduces the effectiveness of oral contraceptives, ethinyl estradiol (the risk of intermenstrual bleeding), as well as medicines, which are formed during metabolism of para-aminobenzoic acid . Diuretics, allopurinol, oxyphenbutazone, fenilbutazon, NSAIDs and drugs that block tubular secretion, while reducing the use of Amosinom tubular secretion, increase the concentration of amoxicillin.
With simultaneous application Amosina with allopurinol increases the risk of developing skin rashes.
Amoxicillin with simultaneous application reduces clearance and increases the toxicity of methotrexate. Amoxicillin, while the application increases the absorption of digoxin.
Terms and Conditions of storage
List B. The drug should be stored out of reach of children, dry, dark place.
Powder for suspension should be stored at a temperature of 15 ° to 25 ° C. Tablets and capsules should be stored at temperatures not above 25 ° C. Shelf life - 2 years.
Gelatin capsules are white, the contents of capsules - white granules.
1 capsule. amoxicillin (in the form of trihydrate) 250 mg.
Excipients: potato starch.
Tablets are white or nearly white, ploskotsilindricheskie, with beveled and risks.
1 tab. amoxicillin (in the form of trihydrate) 250 mg - - 500 mg.
Excipients: potato starch, magnesium stearate, calcium stearate, magnesium hydrosilicate (talc), povidone (kollidon 90F).
Powder for suspension for oral white with a yellowish tint, with a specific smell, preparation of suspensions of white with a yellowish tint, with a specific smell.
A pack. amoxicillin (in the form of trihydrate) 125 mg.
Excipients: polyvinylpyrrolidone (povidone), dextrose, disodium salt of ethylenediaminetetraacetic acid (Trilon B) (edetate disodium), sodium phosphate, disodium (sodium hydrophosphate), sodium α-glutamate monohydrate, food flavoring, vanilla, sucrose.
Powder for suspension for oral white with a yellowish tint, with a specific smell, preparation of suspensions of white with a yellowish tint, with a specific smell.
A pack. amoxicillin (in the form of trihydrate) 250 mg.
Excipients: polyvinylpyrrolidone (povidone), dextrose, disodium salt of ethylenediaminetetraacetic acid (Trilon B) (edetate disodium), sodium phosphate, disodium (sodium hydrophosphate), sodium α-glutamate monohydrate, food flavoring, vanilla, sucrose.
Powder for suspension for oral white with a yellowish tint, with a specific smell, preparation of suspensions of white with a yellowish tint, with a specific smell.
A pack. amoxicillin (in the form of trihydrate) 500 mg.
Excipients: polyvinylpyrrolidone (povidone), dextrose, disodium salt of ethylenediaminetetraacetic acid (Trilon B) (edetate disodium), sodium phosphate, disodium (sodium hydrophosphate), sodium α-glutamate monohydrate, food flavoring, vanilla, sucrose.
Clinico-pharmacological group: Antibiotic penicillin group of broad-spectrum, collapsing penicillinase.
Pharmacological action
Broad-spectrum antibiotic of semisynthetic penicillins. Effective bactericidal. Inhibits transpeptidase, violates the synthesis of peptidoglycan (the reference polymer cell wall) in the period of division and growth, causes lysis of bacteria. Acid-resistant. Active against aerobic gram-positive bacteria: Staphylococcus spp. (With the exception of strains producing penicillinase), Streptococcus spp. and aerobic gram-negative bacteria: Neisseria gonorrhoeae, Neisseria meningitidis, Bacillus anthracis, Listeria monocytogenes, Helicobacter pylori, Klebsiella spp. Microorganisms, penicillinase-producing, resistant to the action of amoxicillin. The action develops within 15-30 min after injection and lasts 8 hours
Pharmacokinetics
Absorption
After oral amoxicillin quickly and almost completely (93%) absorbed from the gastrointestinal tract. Eating does not affect the absorption of the drug, is not destroyed in the acidic environment of the stomach. Cmax of the active substance in the plasma observed after 1-2 h. When administered at a dose of 125 mg and 250 mg Cmax plasma levels of 1.5-3 mg / ml and 3.5-5 mg / ml, respectively.
Distribution
It has a large volume of distribution: in high concentrations found in plasma, sputum, bronchial secretion (purulent bronchial secretion in the distribution of the poor), pleural and peritoneal fluid, urine, contents of skin blisters, tissue of the lung, intestinal mucosa, the female genital organs, prostate gland, middle ear fluid, bone, fat tissue, gall bladder (with normal liver function), fetal tissues.
With increasing doses of 2 times the concentration also increased by 2 times. The concentration in bile exceeds the concentration in plasma 2-4 times. In the amniotic fluid and umbilical cord vessels concentrations of amoxicillin - 25-30% of the level in plasma in pregnant women. Poorly crosses the BBB, the inflammation of the meninges (meningitis) concentration in cerebrospinal fluid - about 20%. Binding to plasma proteins - 17%. In small amounts excreted in breast milk.
Metabolism
Amoxicillin partly metabolized to form inactive metabolites.
Withdrawal
T1 / 2 of amoxicillin is 1-1.5 hours Amoxicillin output by 50-70% in the urine in unchanged form by tubular excretion (80%) and glomerular filtration rate (20%), with bile - 10-20%. Premature, Newborn and children under 6 months - 3-4 hours
Pharmacokinetics in special clinical situations
In preterm, newborns and children under 6 months of T1 / 2 of 3-4 h. In renal dysfunction (CC ≤ 15 mL / min) T1 / 2 of amoxicillin increased to 8.5 h. Amoxicillin is removed during hemodialysis.
Statement
Infectious-inflammatory diseases caused by microorganisms sensitive to the drug:
Respiratory infections (including bronchitis, pneumonia);
infection ENT organs (including sinusitis, pharyngitis, tonsillitis, acute otitis media);
infections of the genitourinary system (including pyelonephritis, pyelitis, cystitis, urethritis, gonorrhea);
gynecologic infections (including endometritis, cervicitis);
gastrointestinal tract infections (including peritonitis, enterocolitis, typhoid fever, cholangitis, cholecystitis);
infections of skin and soft tissue (including erysipelas, impetigo, secondarily infected dermatitis);
leptospirosis;
listeriosis;
Lyme disease (Lyme disease);
dysentery
salmonellosis, salmonellonositelstvo;
serologies
endocarditis (prophylaxis);
sepsis.
Dosage regimen
The drug, taken orally, either before or after meals.
Dosage regimen set individually, taking into account the severity of the disease, susceptible to the drug, the patient's age.
Adults and children over 10 years (with a body weight> 40 kg) each appoint 500 mg 3 times / day, in case of serious illness - at 0.75-1 g 3 times / day.
Children aged 5 to 10 years prescribed 250 mg 3 times / day, at the age of 2 to 5 years - 125 mg 3 times / day, up to 2 years - 20 mg / kg / day in 3 divided doses. The treatment course - 5-12 days.
Children aged under 5 years of drug administered in the form of suspension. For the treatment of acute uncomplicated gonorrhea drug administered in a dose of 3 g once, in the treatment of women should receive a second dose given.
In acute infectious diseases of the digestive tract (paratyphoid fever, typhoid fever), and biliary tract, gynecological infectious diseases of adults appoint 1.5-2 g 3 times / day or 1-1.5 g 4 times / day.
In leptospirosis adults appoint 500-750 mg 4 times / day for 6-12 days.
When salmonellonositelstve adults - 1.5-2 g 3 times / day for 2-4 weeks. For the prevention of endocarditis with small surgical interventions for adults prescribed a dose of 3-4 g for 1 h before the procedure.
If you want to be reappointed after a dose of 8-9 h. In children, the dose is reduced by half. Patients with impaired renal function (QC from 15 to 40 ml / min) interval between doses increased to 12 hours in the terminal stage of chronic renal failure (CC <10 ml / min) Amosina dose should be reduced by 15-50%, or increase the interval between doses up to 24 h, when anuria - the maximum dose of 2 g / day.
Terms preparation of the suspension
Single-dose pack
In a clean glass poured boiled and cooled water in the amount indicated in the table, then pour the contents of one packet and mix until a homogeneous suspension.
Side effect
Allergic reactions: Possible - urticaria, flushing of the skin, erythema, angioedema, rhinitis, conjunctivitis, rarely - fever, joint pain, eosinophilia, exfoliative dermatitis, erythema multiforme exudative, Stevens-Johnson syndrome, reactions similar to serum sickness and in individual cases - anaphylactic shock.
On the part of the digestive system: dysbacteriosis, change in taste, vomiting, nausea, diarrhea, stomatitis, glossitis, abnormal liver function, a moderate increase in liver transaminases; rarely - 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.
From the urinary system: rarely - interstitial nephritis.
On the part of the hemopoietic system: leukopenia, neutropenia, thrombocytopenic purpura, anemia.
Other: shortness of breath, tachycardia, candidiasis of the vagina, superinfection (especially in patients with chronic diseases or low resistance of the organism).
Contraindications
allergic diathesis;
bronchial asthma, pollinosis;
infectious mononucleosis;
lymphocytic leukemia;
hepatic impairment;
digestive diseases in the history of (especially colitis, associated with the use of antibiotics);
Lactation (breastfeeding);
Hypersensitivity to the drug's components;
sensitivity to other penicillins, cephalosporins, carbapenems);
Children under 3 years (for tablets and capsules).
Precautions should be prescribed the drug during pregnancy, renal insufficiency, as well as guidance on the history of bleeding.
Pregnancy and lactation
Use of the drug during pregnancy is possible only in cases where the intended use of therapy to the mother outweighs the potential risk to the fetus.
Use during lactation is contraindicated. If necessary, use during lactation should stop breastfeeding.
Application for violations of liver function
Contraindicated in hepatic failure.
Application for violations of renal function
Patients with impaired renal function (QA - 15-40 ml / min) interval between doses increased to 12 hours in the terminal stage of chronic renal failure (CC <10 ml / min) Amosina dose should be reduced by 15-50%, or increase the interval between doses up to 24 h, when anuria - the maximum dose of 2 g / day.
Cautions
In the course of treatment Amosinom need to monitor the state functions of blood, liver and kidneys. Perhaps the development of superinfection due to growth insensitive to amoxicillin microflora, which requires a corresponding change in antimicrobial therapy.
When treating patients with bacteremia rarely develops bacteriolysis reaction (reaction Jarisch-Herxheimer). Patients who have an increased sensitivity to penicillin, may be cross-allergic reactions to cephalosporin antibiotics.
In the treatment of mild diarrhea during treatment Amosina avoid appointment antidiarrhoeal drugs that reduce intestinal motility; can use kaolin or attapulgitsoderzhaschie antidiarrhoeal funds.
Patients with severe diarrhea should make a differential diagnosis and assign the appropriate therapy.
Treatment should be continued even 48-72 hours after the disappearance of clinical signs of disease.
With simultaneous use of oral contraceptives estrogensoderzhaschih and amoxicillin should, if possible, to use additional methods of contraception.
Overdose
Symptoms: nausea, vomiting, diarrhea, disruption of water and electrolyte balance (as a consequence of vomiting and diarrhea). Treatment: gastric lavage, activated charcoal, saline laxatives, measures aimed at maintaining water and electrolyte balance; hemodialysis.
Drug Interactions
Antacids, glucosamine, laxatives, diet, aminoglycoside antibiotics, while applying slow and reduce the absorption of amoxicillin, ascorbic acid - increases its absorption. Bactericidal antibiotics (including aminoglycosides, cephalosporins, cycloserine, vancomycin, rifampicin) often synergy with amoxicillin; bacteriostatic drugs (macrolides, chloramphenicol, Lincosamides, tetracyclines, sulfonamides) - antagonism.
Amoxicillin, while the application increases the effectiveness of indirect anticoagulants (suppressing the intestinal microflora, reduces the synthesis of vitamin K and prothrombin index); estrogensoderzhaschih reduces the effectiveness of oral contraceptives, ethinyl estradiol (the risk of intermenstrual bleeding), as well as medicines, which are formed during metabolism of para-aminobenzoic acid . Diuretics, allopurinol, oxyphenbutazone, fenilbutazon, NSAIDs and drugs that block tubular secretion, while reducing the use of Amosinom tubular secretion, increase the concentration of amoxicillin.
With simultaneous application Amosina with allopurinol increases the risk of developing skin rashes.
Amoxicillin with simultaneous application reduces clearance and increases the toxicity of methotrexate. Amoxicillin, while the application increases the absorption of digoxin.
Terms and Conditions of storage
List B. The drug should be stored out of reach of children, dry, dark place.
Powder for suspension should be stored at a temperature of 15 ° to 25 ° C. Tablets and capsules should be stored at temperatures not above 25 ° C. Shelf life - 2 years.
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