OSPAMOKS
Active material: Amoksiцillin
When ATH: J01CA04
CCF: Antibiotics penicillin broad spectrum, collapsing penicillinase
When CSF: 06.01.02.01.01
Manufacturer: Sandoz GmbH (Austria)
PHARMACEUTICAL FORM, COMPOSITION AND PACKAGING
Capsules hard gelatin №2, opaque, yellow color; contents of capsules – powder from white to cream color.
| 1 caps. | |
| amoksicillina trigidrat | 287 mg, |
| that corresponds to the content of amoxicillin | 250 mg |
Excipients: magnesium stearate, microcrystalline cellulose.
The composition of the shell: Titanium dioxide, gelatin, iron oxide yellow.
10 PC. – blisters (100) – cardboard boxes.
Powder for oral suspension white or white with a yellowish tinge color with a characteristic fruity odor; cooked slurry of white or white with a yellowish tint, with a characteristic fruity odor and a bitter-sweet taste.
| 5 ml ready-r-ra | |
| amoksiцillin (in the form of trihydrate) | 125 mg |
[Ring] Citric acid anhydrous, Sodium benzoate, Aspartame, talc, trinatriya citrate bezvodnыy, guar gum (guar galaktomannan), precipitated silicon dioxide, Flavors (powdery – lemon, peach-apricot, orange).
5.1 g – vials of dark glass (1) – packs cardboard.
Powder for oral suspension white or white with a yellowish tinge color with a characteristic fruity odor; cooked slurry of white or white with a yellowish tint, with a characteristic fruity odor and a bitter-sweet taste.
| 5 ml ready-r-ra | |
| amoksiцillin (in the form of trihydrate) | 125 mg |
[Ring] Citric acid anhydrous, Sodium benzoate, Aspartame, talc, trinatriya citrate bezvodnыy, guar gum (guar galaktomannan), precipitated silicon dioxide, Flavors (powdery – lemon, peach-apricot, orange).
8.5 g – vials of dark glass (1) – packs cardboard.
Powder for oral suspension white or white with a yellowish tinge color with a characteristic fruity odor; cooked slurry of white or white with a yellowish tint, with a characteristic fruity odor and a bitter-sweet taste.
| 5 ml ready-r-ra | |
| amoksiцillin (in the form of trihydrate) | 250 mg |
[Ring] Citric acid anhydrous, Sodium benzoate, Aspartame, talc, trinatriya citrate bezvodnыy, guar gum (guar galaktomannan), precipitated silicon dioxide, Flavors (powdery – lemon, peach-apricot, orange).
11 g – vials of dark glass (1) – packs cardboard.
Powder for oral suspension white or white with a yellowish tinge color with a characteristic fruity odor; cooked slurry of white or white with a yellowish tint, with a characteristic fruity odor and a bitter-sweet taste.
| 5 ml ready-r-ra | |
| amoksiцillin (in the form of trihydrate) | 250 mg |
[Ring] Citric acid anhydrous, Sodium benzoate, Aspartame, talc, trinatriya citrate bezvodnыy, guar gum (guar galaktomannan), precipitated silicon dioxide, Flavors (powdery – lemon, peach-apricot, orange).
6.6 g – vials of dark glass (1) – packs cardboard.
Powder for oral suspension white or white with a yellowish tinge color with a characteristic fruity odor; cooked slurry of white or white with a yellowish tint, with a characteristic fruity odor and a bitter-sweet taste.
| 5 ml ready-r-ra | |
| amoksiцillin (in the form of trihydrate) | 500 mg |
[Ring] Citric acid anhydrous, Sodium benzoate, Aspartame, talc, trinatriya citrate bezvodnыy, guar gum (guar galaktomannan), precipitated silicon dioxide, Flavors (powdery – lemon, peach-apricot, orange).
12 g – vials of dark glass (1) – packs cardboard.
Powder for oral suspension white or white with a yellowish tinge color with a characteristic fruity odor; cooked slurry of white or white with a yellowish tint, with a characteristic fruity odor and a bitter-sweet taste.
| 5 ml ready-r-ra | |
| amoksiцillin (in the form of trihydrate) | 500 mg |
[Ring] Citric acid anhydrous, Sodium benzoate, Aspartame, talc, trinatriya citrate bezvodnыy, guar gum (guar galaktomannan), precipitated silicon dioxide, Flavors (powdery – lemon, peach-apricot, orange).
20 g – vials of dark glass (1) – packs cardboard.
Pills, coated white to slightly yellowish, Oval, lenticular, notched on both sides.
| 1 tab. | |
| amoksicillina trigidrat | 1.148 g, |
| that corresponds to the content of amoxicillin | 1 g |
Excipients: magnesium stearate, polyvidone, sodium starch glycolate, microcrystalline cellulose.
The composition of the shell: Titanium dioxide, talc, gipromelloza.
6 PC. – blisters (2) – packs cardboard.
Pills, coated white to slightly yellowish, oblong, lenticular, notched on both sides.
| 1 tab. | |
| amoksicillina trigidrat | 574 mg, |
| which corresponds to the content of amoxicillin | 500 mg |
Excipients: magnesium stearate, polyvidone, sodium starch glycolate, microcrystalline cellulose.
The composition of the shell: Titanium dioxide, talc, gipromelloza.
12 PC. – blisters (1) – packs cardboard.
DESCRIPTION OF ACTIVE SUBSTANCES
Pharmacological action
Combined formulations of amoxycillin and clavulanic acid – beta-lactamase inhibitor. Effective bactericidal, It inhibits the synthesis of bacterial cell wall.
It is active against aerobic gram-positive bacteria (including strains, producing beta-lactamase): Staphylococcus aureus; Aerobic Gram-negative bacteria: Enterobacter spp., Escherichia coli, Haemophilus influenzae, Klebsiella spp., Moraxella catarrhalis. The following pathogens are sensitive only in vitro: Staphylococcus epidermidis, Streptococcus pyogenes, Streptococcus anthracis, Streptococcus pneumoniae, Streptococcus viridans, Enterococcus faecalis, Corynebacterium spp., Listeria monocytogenes; anaerobic Clostridium spp., Peptococcus spp., Peptostreptococcus spp.; and Aerobic gram-negative bacteria (including strains, producing beta-lactamase): Proteus is wonderful, Proteus vulgaris, Salmonella spp., Shigella spp., Bordetella pertussis, Yersinia enterocolitica, Gardnerella vaginalis, Neisseria meningitidis, Neisseria gonorrhoeae, Haemophilus ducreyi, Yersinia multocida (Pasteurella ранее), Campylobacter jejuni; anaerobic gram-negative bacteria (including strains, producing beta-lactamase): Bacteroides spp., including Bacteroides fragilis.
Clavulanic acid inhibits II, III, IV and V types of beta-lactamases, not active against beta-lactamase I type, produced by Pseudomonas aeruginosa, Serratia spp., Acinetobacter spp. Clavulanic acid has a high affinity for penicillinases, thereby forming a stable complex with the enzyme, thus preventing the enzymatic degradation of amoxicillin under the influence of beta-lactamase.
Pharmacokinetics
After oral administration, the two components are quickly absorbed in the gastrointestinal tract. Simultaneous food intake does not affect absorption. TCmax – 45 m. After oral dose 250/125 mg every 8 h Cmax amoksiцillina – 2.18-4.5 ug / ml, clavulanic acid – 0.8-2.2 ug / ml, dose 500/125 mg every 12 h Cmax amoksiцillina – 5.09-7.91 ug / ml, clavulanic acid – 1.19-2.41 ug / ml, dose 500/125 mg every 8 h Cmax amoksiцillina – 4.94-9.46 ug / ml, clavulanic acid – 1.57-3.23 ug / ml, dose 875/125 mg Cmax amoksiцillina – 8.82-14.38 ug / ml, clavulanic acid – 1.21-3.19 ug / ml.
After the on / in the doses 1000/200 and 500/100 mg Cmax amoksiцillina – 105.4 and 32.2 ug / ml, respectively, and clavulanic acid – 28.5 and 10.5 ug / ml.
Time to reach the maximum inhibitory concentration 1 ug / mL for amoxycillin similar when applied through 12 and h 8 h in adults, and children.
Relationship to plasma proteins: amoksiцillin – 17-20%, Clavulanic acid – 22-30%.
Both components are metabolized in the liver: amoksiцillin – on 10% the dose of the administered dose, Clavulanic acid – on 50%.
T1/2 after receiving a dose of 375 and 625 mg – 1 and 1.3 h for amoxicillin, 1.2 and 0.8 no – for clavulanic acid, respectively. T1/2 after / in a dose of 1200 and 600 mg – 0.9 and 1.07 no – amoxicillin, 0.9 and 1.12 no – for clavulanic acid, respectively. Write mainly kidneys (glomerular filtration and tubular secretion): 50-78 and 25-40% of the administered dose of amoxycillin and clavulanic acid respectively output in unchanged form within the first 6 h after administration.
Testimony
- Bacterial infections, caused by susceptible pathogens: lower respiratory tract infections (bronchitis, pneumonia, empyema, lung abscess);
- Infections of upper respiratory tract (sinusitis, tonsillitis, otitis media);
- Infections of the urinary and pelvic organs (pyelonephritis, pyelitis, cystitis, uretrit, prostatitis, cervicitis, salpingitis, salpingo-oophoritis, tubo-ovarian abscess, endometritis, bacterial vaginosis, septic abortion, childbed fever, pelvioperitonit, chancroid, gonorrhea);
- Infections of the skin and soft tissues (mug, impetigo, secondarily infected dermatitis, abscess, flegmona, wound infection);
- Osteomyelitis;
- Postoperative infections;
- Prevention of infections in surgery.
Dosage regimen
Inside, I /.
Doses are based upon amoxicillin. The mode set individually depending on the severity and localization of infection, susceptibility.
Children up 12 years – in suspension, syrup or drops for the oral administration. A single dose is determined depending on the age: Children under 3 Months – 30 mg / kg / day 2 admission; 3 months and senior – at mild infections – 25 mg / kg / day 2 receiving or 20 mg / kg / day 3 admission, at severe infections – 45 mg / kg / day 2 receiving or 40 mg / kg / day 3 admission.
Adults and children over 12 years or with body weight 40 kg or more: 500 mg 2 times / day or 250 mg 3 times / day. When severe infection severity and respiratory tract infections – 875 mg 2 times / day or 500 mg 3 times / day.
The maximum daily dose of amoxicillin for adults and older children 12 years – 6 g, for children up to 12 years – 45 mg / kg body weight.
The maximum daily dose of clavulanic acid for adults and older children 12 years – 600 mg, for children up to 12 years – 10 mg / kg body weight.
With difficulty swallowing in adults is recommended to use suspension.
In preparing the slurry, syrup and drops as the solvent, use water.
At on / in adults and adolescents over 12 years imposed 1 g (for amoxicillin) 3 once a day, if necessary – 4 once a day. The maximum daily dose – 6 g. For children 3 months-12 years – 25 mg / kg 3 once a day; in severe cases – 4 once a day; for children up to 3 Months: prematurity and perinatal – 25 mg / kg 2 once a day, in postperinatalnom period – 25 mg / kg 3 once a day.
Duration of treatment – to 14 days, acute otitis media – to 10 days.
To prevention of post-surgical infections in operations, of less than 1 no, during the induction of anesthesia in the injected dose 1 g / in. At longer operations – by 1 g every 6 hours within a day. With the high risk of infection, administration may be continued for several days.
At chronic renal failure shall adjust the dose and frequency of administration depending on QC: at QC more 30 ml / min dose adjustment is required; at CC 10-30 ml / min: inside – 250-500 mg / day every 12 no; I / – 1 g, then 500 mg / in; at QC less 10 ml / min – 1 g, then 500 mg / in / or 250-500 mg / day orally in a single step. For children, the dose should be reduced in the same manner.
Patients, located at gemodialize – 250 mg or 500 mg orally in a single step or 500 mg / in, additionally 1 dose during dialysis and 1 dose at the end of dialysis.
Side effect
From the digestive system: nausea, vomiting, diarrhea, gastritis, stomatitis, glossitis, increase in liver transaminases, in a few cases – cholestatic jaundice, hepatitis, hepatic failure (most often in the elderly, Men, long-term therapy), psevdomembranoznыy and gemorragicheskiy colitis (also can develop after treatment), enterocolitis, black “hairy” language, browning of tooth enamel.
From the side of hematopoiesis: reversible increase in prothrombin time and bleeding time, thrombocytopenia, thrombocytosis, eozinofilija, leukopenia, agranulocytosis, gemoliticheskaya anemia.
From the nervous system: dizziness, headache, hyperactivity, alarm, behavior change, convulsions.
Local reactions: in some cases – phlebitis at the site / in the.
Allergic reactions: hives, erythematous rash, rarely – erythema multiforme exudative, anaphylactic shock, angioedema, rarely – exfoliative dermatitis, malignant exudative erythema (Stevens-Johnson syndrome), sensitization vasculitis, syndrome, similar to serum sickness, Acute generalized exanthematous pustullez.
Other: candidiasis, development of superinfection, interstitial nephritis, kristallurija, hematuria.
Contraindications
- Hypersensitivity (incl. cephalosporins etc.. beta-lactam antibiotics);
- Infectious mononucleosis (incl. the appearance of the rash morbilliform);
- Phenylketonuria;
- Jaundice episodes or abnormal liver function as a result of amoxycillin / clavulanic acid history;
- CC less than 30 ml / min (Pill 875 mg / 125 mg).
FROM caution: pregnancy, lactation, severe liver failure, gastrointestinal diseases (incl. a history of colitis, associated with the use of penicillins), chronic renal failure.
Pregnancy and lactation
Carefully: pregnancy, lactation.
There were cases of necrotizing enterocolitis in newborns, in pregnant women with premature rupture of membranes.
Cautions
In exchange treatment is necessary to monitor the state functions of blood, liver and kidneys.
To reduce the risk of side effects from the gastrointestinal tract should take the drug during meals.
Perhaps the development of superinfection due to growth insensitive to it microflora, which requires a corresponding change in antimicrobial therapy.
May give false positive results in the determination of glucose in urine. In this case, use glyukozoksidantny method of determining the concentration of glucose in the urine.
Once reconstituted suspension should be stored no more than 7 days in a refrigerator, but do not freeze.
Patients, with hypersensitivity to penicillins, possible cross-allergic reaction cephalosporin antibiotic.
There were cases of necrotizing enterocolitis in newborns, in pregnant women with premature rupture of membranes.
Since tablets contain the same amount of clavulanic acid (125 mg), should be considered, what 2 for tablets 250 mg (for amoxicillin) no equivalent 1 tablet of 500 mg (for amoxicillin).
Overdose
Symptoms: dysfunction of the gastrointestinal tract and water and electrolyte balance.
Treatment: symptomatic. Hemodialysis is effective.
Drug Interactions
Antacids, Glucosamine, laxative drugs, aminoglycosides slow down and reduce absorption; ascorbic acid increases absorption.
Bacteriostatic drugs (makrolidы, chloramphenicol, lincosamides, tetracikliny, sulfonamides) antagonize.
Improves the effectiveness of indirect anticoagulants (suppressing the intestinal microflora, It reduces the synthesis of vitamin K and prothrombin index). At the same time taking anticoagulants need to monitor the performance of blood clotting.
Reduces the effectiveness of oral contraceptives, drugs, during metabolism which is formed PABA, ethinyl estradiol – the risk of bleeding “Breakthrough”.
Diuretic, allopurinol, phenylbutazone, NSAIDs, etc.. drugs, block tubular secretion, increase the concentration of amoxicillin (Clavulanic acid is derived mainly by glomerular filtration).
Allopurinol increases the risk of skin rashes.
