Components:
Method of action:
Treatment option:
Medically reviewed by Fedorchenko Olga Valeryevna, PharmD. Last updated on 25.03.2022
Attention! Information on this page is intended only for medical professionals! Information is collected in open sources and may contain significant errors! Be careful and double-check all the information on this page!
Betaklav
Amoxicillin, Clavulanic
Film-coated tablets, Powder for preparation of suspension for oral administration
For all dosage forms
Infections caused by sensitive strains of microorganisms:
upper respiratory tract and ENT organs (including acute and chronic sinusitis, acute and chronic otitis media, pharyngeal abscess, tonsillitis, pharyngitis),
lower respiratory tract (including acute bronchitis with bacterial superinfection, chronic bronchitis, pneumonia),
urinary tract infections (e.g. cystitis, urethritis, pyelonephritis),
in gynecology,
skin and soft tissue, including human and animal bites,
bone and connective tissue,
bile ducts (cholecystitis, cholangitis),
odontogenic.
Amoxiclav®
For powder for preparation of solution for intravenous administration in addition
infection of the abdominal cavity,
the sexually transmitted infections (gonorrhea, soft chancre),
prevention of infections after surgical interventions.
Amoxiclav®
Film-coated tablets
Inside. The dosage regimen is set individually, depending on the age, body weight, kidney function of the patient, as well as the severity of the infection.
The drug Amoxiclav® It is recommended to take it at the beginning of a meal for optimal absorption and to reduce possible side effects from the digestive system.
The course of treatment is 5 to 14 days. The duration of the course of treatment is determined by the attending physician. Treatment should not last more than 14 days without a second medical examination.
Children under 12 years old
The dose is prescribed depending on the age and body weight. The recommended dosage regimen is 40 mg / kg / day in 3 doses.
Children with a body weight of 40 kg or more should be given the same doses as adults. For children aged less than 6 years, it is more preferable to take a suspension of the drug Amoxiclav®.
Adults and children over 12 years of age (or >40 kg of body weight)
The usual dose in the case of mild and moderate infection is 1 tab. 250 125 mg every 8 hours or 1 tab. 500 125 mg every 12 hours, in the case of severe infection and respiratory tract infections-1 tab. 500 125 mg every 8 hours or 1 tab. 875 125 mg every 12 hours.
Since the tablets of the combination of amoxicillin and clavulanic acid of 250 125 mg and 500 125 mg contain the same amount of clavulanic acid-125 mg, then 2 tables of 250 125 mg are not equivalent to 1 table of 500 125 mg.
Dosage for odontogenic infections
1 tab. 250 125 mg every 8 hours or 1 tab. 500 125 mg every 12 hours for 5 days.
Patients with impaired renal function
Dose adjustment is based on the maximum recommended dose of amoxicillin and is carried out taking into account the values of Cl creatinine:
- adults and children over 12 years of age (or ≥40 kg of body weight) (Table 2),
- with anuria, the interval between dosing should be increased to 48 hours or more,
- tablets 875 125 mg should be used only in patients with creatinine Cl >30 ml/min.
Table 2
| Creatinine clearance | The dosage regimen of the drug Amoxiclav® |
| >30 ml / min | No dose adjustment is required |
| 10-30 ml / min | 1 tab. 50 125 mg 2 times a day or 1 tab. 250 125 mg (for mild and moderate infection) 2 times a day |
| <10 ml / min | 1 table. 500 125 mg 1 time per day or 1 table. 250 125 mg (for mild and moderate infection) 1 time per day |
| Hemodialysis | 1 table 500 125 mg or 2 table 250 125 mg every 24 hours 1 table 500 125 mg or 2 table 250 125 mg during dialysis and at the end of the dialysis session (due to a decrease in serum concentrations of amoxicillin and clavulanic acid) |
Patients with impaired liver function
Taking the drug Amoxiclav® it should be carried out with caution. It is necessary to conduct regular monitoring of liver function.
Powder for preparation of suspension for oral administration
Inside
The daily dose of suspensions is 125 31.25 mg/5 ml and 250 62.5 mg/5 ml (to facilitate correct dosing, a 5-ml graduated pipette with a 0.1-ml scale or a 5-ml dosing spoon with a 2.5-ml ring mark in the cavity is inserted into each package of suspensions 125 31.25 mg/5 ml and 250 62.5 mg/5 ml).
Newborns and children up to 3 months old — 30 mg / kg / day (according to amoxicillin), divided into 2 doses (every 12 hours).
The dosing of the drug Amoxiclav® dosage pipette-calculation of single doses for the treatment of infections in newborns and children up to 3 months (Table 3).
Table 3
| Body weight, kg | 2 | 2,2 | 2,4 | 2,6 | 2,8 | 3 | 3,2 | 3,4 | 3,6 | 3,8 | 4 | 4,2 | 4,4 | 4,6 | 4.8 |
| Suspension 156.25, ml (2 times a day) | 1,2 | 1,3 | 1,4 | 1,6 | 1,7 | 1,8 | 1,9 | 2 | 2,2 | 2,3 | 2,4 | 2,5 | 2,6 | 2,8 | 2,9 |
| Suspension 312,5, ml (2 times a day) | 0,6 | 0,7 | 0,7 | 0,8 | 0,8 | 0,9 | 1 | 1 | 1,1 | 1,1 | 1,2 | 1,3 | 1,3 | 1,4 | 1,4 |
Children older than 3 months — from 20 mg / kg for mild and moderate infections to 40 mg / kg for severe infections and lower respiratory tract infections, otitis media, sinusitis (amoxicillin) per day, divided into 3 doses (every 8 hours).
The dosing of the drug Amoxiclav® dosage pipette-calculation of single doses for the treatment of mild and moderate infections in children older than 3 months (at the rate of 20 mg/kg/day (according to amoxicillin) (Table 4).
Table 4
| Body weight, kg | 5 | 6 | 7 | 8 | 9 | 10 | 11 | 12 | 13 | 14 | 15 | 16 | 17 | 18 | 19 | 20 | 21 | 22 |
| Suspension 156.25, ml (3 times a day) | 1,3 | 1,6 | 1,9 | 2,1 | 2,4 | 2,7 | 2,9 | 3,2 | 3,5 | 3,7 | 4 | 4,3 | 4,5 | 4,8 | 5,1 | 5,3 | 5,6 | 5,9 |
| Suspension 312,5, ml (3 times a day) | 0,7 | 0,8 | 0,9 | 1,1 | 1,2 | 1,3 | 1,5 | 1,6 | 1,7 | 1,9 | 2 | 2,1 | 2,3 | 2,4 | 2,5 | 2,7 | 2,8 | 2,9 |
| Body weight, kg | 23 | 24 | 25 | 26 | 27 | 28 | 29 | 30 | 31 | 32 | 33 | 34 | 35 | 36 | 37 | 38 | 39 | |
| Suspension 156.25, ml (3 times a day) | 6,1 | 6,4 | 6,7 | 6,9 | 7,2 | 7,5 | 7,7 | 8 | 8,3 | 8,5 | 8,8 | 9,1 | 9,3 | 9,6 | 9,9 | 10,1 | 10,4 | |
| Suspension 312,5, ml (3 times a day) | 3,1 | 3,2 | 3,3 | 3,5 | 3,6 | 3,7 | 3,9 | 4 | 4,1 | 4,3 | 4,4 | 4,5 | 4,7 | 4,8 | 4,9 | 5,1 | 5,2 |
The dosing of the drug Amoxiclav® dosage pipette-calculation of single doses for the treatment of severe infections in children older than 3 months (at the rate of 40 mg / kg / day (according to amoxicillin) (Table 5).
Table 5
| Body weight, kg | 5 | 6 | 7 | 8 | 9 | 10 | 11 | 12 | 13 | 14 | 15 | 16 | 17 | 18 | 19 | 20 | 21 | 22 |
| Suspension 156.25, ml (3 times a day) | 2,7 | 3,2 | 3,7 | 4,3 | 4,8 | 5,3 | 5,9 | 6,4 | 6,9 | 7,5 | 8 | 8,5 | 9,1 | 9,6 | 10,1 | 10,7 | 11,2 | 11,7 |
| Suspension 312,5, ml (3 times a day) | 1,3 | 1,6 | 1,9 | 2,1 | 2,4 | 2,7 | 2,9 | 3,2 | 3,5 | 3,7 | 4 | 4,3 | 4,5 | 4,8 | 5,1 | 5,3 | 5,6 | 5,9 |
| Body weight, kg | 23 | 24 | 25 | 26 | 27 | 28 | 29 | 30 | 31 | 32 | 33 | 34 | 35 | 36 | 37 | 38 | 39 | |
| Suspension 156.25, ml (3 times a day) | 12,3 | 12,8 | 13,3 | 13,9 | 14,4 | 14,9 | 15,5 | 16 | 16,5 | 17,1 | 17,6 | 18,1 | 18,7 | 19,2 | 19,7 | 20,3 | 20,8 | |
| Suspension 312,5, ml (3 times a day) | 6,1 | 6,4 | 6,7 | 6,9 | 7,2 | 7,5 | 7,7 | 8 | 8,3 | 8,5 | 8,8 | 9,1 | 9,3 | 9,6 | 9,9 | 10,1 | 10,4 |
The dosing of the drug Amoxiclav® dosage spoon (in the absence of a dosage pipette) - recommended doses of suspensions depending on the child's body weight and the severity of the infection (Table 6).
Table 6
| Body weight, kg | Age (approximately) | Mild/moderate course | Heavy current | ||
| 125 31.25 mg/5 ml | 250 62.5 mg/5 ml | 125 31.25 mg/5 ml | 250 62.5 mg/5 ml | ||
| 5–10 | 3-12 months | 3 × 2.5 ml (½ spoon) | 3 × 1.25 ml | 3 × 3.75 ml | 3 × 2 ml |
| 10–12 | 1-2 years | 3 × 3.75 ml | 3 × 2 ml | 3 × 6.25 ml | 3 × 3 ml |
| 12–15 | 2-4 years old | 3 × 5 ml (1 teaspoon) | 3 × 2.5 ml (½ spoon) | 3 × 7.5 ml (1½ tablespoons) | 3 × 3.75 ml |
| 15–20 | 4-6 years old | 3 × 6.25 ml | 3 × 3 ml | 3 × 9.5 ml | 3 × 5 ml (1 teaspoon) |
| 20–30 | 6-10 years old | 3 × 8.75 ml | 3 × 4.5 ml | - | 3 × 7 ml |
| 30–40 | 10-12 years old | - | 3 × 6.5 ml | - | 3 × 9.5 ml |
| ≥40 | ≥12 years | The drug Amoxiclav® pills | |||
Daily dose of suspension 400 mg 57 mg/5 ml
The dose is calculated per kg of body weight, depending on the severity of the infection. From 25 mg / kg - for mild and moderate infections to 45 mg/kg-for severe infections and lower respiratory tract infections, otitis media, sinusitis (in terms of amoxicillin) per day, divided into 2 doses.
To facilitate correct dosing, a dosing pipette is inserted into each package of 400 mg 57 mg/5 ml suspension, graduated simultaneously into 1, 2, 3, 4, 5 ml and into 4 equal parts.
Suspension 400 mg 57 mg/5 ml is used in children older than 3 months.
Table 7
The recommended dose of the suspension depends on the child's body weight and the severity of the infection
| Body weight, kg | Age (approximately) | Recommended dose, ml | |
| Heavy current | The course of moderate severity | ||
| 5–10 | 3-12 months | 2×2,5 | 2×1,25 |
| 10–15 | 1-2 years | 2×3,75 | 2×2,5 |
| 15–20 | 2-4 years old | 2×5 | 2×3,75 |
| 20–30 | 4 years — 6 years | 2×7,5 | 2×5 |
| 30–40 | 6-10 years old | 2×10 | 2×6,5 |
The exact daily doses are calculated based on the child's body weight, not their age.
The maximum daily dose of amoxicillin is 6 g for adults and 45 mg/kg for children.
The maximum daily dose of clavulanic acid (in the form of potassium salt) is 600 mg for adults and 10 mg/kg for children.
In patients with impaired renal function, the dose should be adjusted based on the maximum recommended dose of amoxicillin.
Patients with creatinine Cl >30 ml / min do not require any dose adjustment.
Adults and children weighing more than 40 kg (the specified dosage regimen is used for moderate and severe infections)
Patients with creatinine Cl 10-30 ml / min — 500/125 mg 2 times a day.
When creatinine Cl <10 ml / min, the recommended dose is 500/125 mg once a day.
For patients on hemodialysis, the recommended dose is 500/125 mg every 24 hours, plus 500/125 mg during dialysis and another dose at the end of dialysis (since serum concentrations of amoxicillin and clavulanic acid are reduced).
Children weighing less than 40 kg
With a creatinine Cl of 10-30 ml / min, the recommended dose is 15/3. 75 mg / kg 2 times a day (maximum 500/125 mg 2 times a day).
When creatinine Cl <10 ml / min, the recommended dose is 15/3. 75 mg / kg once a day (maximum 500/125 mg).
For hemodialysis, the recommended dose is 15/3. 75 mg / kg once a day. Before hemodialysis — 15/3,75 mg/kg. To restore the appropriate concentrations of the drug in the blood,it is necessary to take another dose of 15/3. 75 mg/kg after hemodialysis.
The course of treatment is 5 to 14 days. The duration of the course of treatment is determined by the attending physician. Treatment should not last more than 14 days without a second medical examination.
Instructions for preparing the suspension
Powder for suspension preparation 125 31.25 mg/5ml - shake the bottle vigorously, add 86 ml of water in two doses (up to the mark), each time shaking well until the powder is completely dissolved.
Powder for preparation of oral suspension 250 62.5 mg/5ml - shake the bottle vigorously, add 85 ml of water in two doses (up to the mark), shaking well each time until the powder is completely dissolved.
Powder for preparation of oral suspension 400 mg 57 mg/5 ml - shake the bottle vigorously, add water in two steps (up to the label) in the amount indicated on the label and shown in the table, each time shaking well until the powder is completely dissolved.
Table 8
| Volume of the finished suspension, ml | Required amount of water, ml |
| 35 | 29,5 |
| 50 | 42 |
| 70 | 59 |
| 140 | 118 |
Shake vigorously before use!
To prepare the suspension, it is recommended to dilute the powder with boiled water at room temperature. It is recommended to place the finished suspension in the refrigerator.
It is not recommended to heat the suspension before use (it is necessary to bring the suspension to room temperature).
After taking the drug, it is recommended to rinse the dosage pipette with boiled water.
Powder for preparation of solution for intravenous administration
In/in.
Children: with a body weight of less than 40 kg-the dose is calculated depending on the body weight.
Under 3 months with a body weight of less than 4 kg - 30 mg / kg (in terms of the entire drug Amoxiclav®) every 12 hours.
Under 3 months with a body weight of more than 4 kg - 30 mg / kg (in terms of the entire drug Amoxiclav®) every 8 hours.
In children younger than 3 months, the drug Amoxiclav® it should be administered only slowly by infusion for 30-40 minutes.
Children from 3 months to 12 years old - 30 mg / kg (in terms of the entire drug Amoxiclav®) at intervals of 8 hours, in the case of severe infection - at intervals of 6 hours.
Children with impaired renal function
The dose adjustment is based on the maximum recommended dose of amoxicillin. In patients with creatinine Cl values above 30 ml/min, dose adjustment is not necessary.
Children weighing <40 kg:
| Cl creatinine at 10-30 ml/min | 25 mg/5 mg per 1 kg every 12 hours |
| Creatinine Cl <10 ml / min | 25 mg/5 mg per 1 kg every 24 hours |
| Hemodialysis | 25 mg / 5 mg per 1 kg every 24 hours plus a dose of 12.5 mg/2.5 mg per 1 kg at the end of the dialysis session (due to a decrease in the concentration of amoxicillin and clavulanic acid in the serum) |
Every 30 mg of Amoxiclav® They contain 25 mg of amoxicillin and 5 mg of clavulanic acid.
Adults and children over 12 years of age or weighing more than 40 kg - 1.2 g of the drug (1000-200 mg) at an interval of 8 hours, in case of severe infection - at an interval of 6 hours.
Prophylactic doses for surgical interventions: 1.2 g for introductory anesthesia (if the duration of the operation is less than 2 hours). For longer operations-1.2 g up to 4 times during the day.
For patients with renal insufficiency, the dose and / or interval between injections of the drug should be adjusted depending on the degree of insufficiency:
| Creatinine Cl | Dose and / or interval between injections |
| >0.5 ml / s (30 ml / min) | No dose adjustment is required |
| 0.166-0.5 ml / s (10-30 ml / min) | The first dose is 1.2 g (1000 200 mg), followed by 600 mg (500 100 mg) intravenously every 12 hours |
| <0.166 ml / s (less than 10 ml / min) | The first dose is 1.2 g (1000 200 mg), followed by 600 mg (500 100 mg) intravenously every 24 hours |
| Anuria | The dosing interval should be increased to 48 hours or more |
Since 85% of the drug is removed by hemodialysis, the usual dose of Amoxiclav should be administered at the end of each hemodialysis procedure®. In peritoneal dialysis, dose adjustment is not required.
The course of treatment is 5 to 14 days. The duration of the course of treatment is determined by the attending physician. With a decrease in the severity of symptoms, it is recommended to switch to oral forms of the drug Amoxiclav to continue therapy®.
Preparation of solutions for intravenous injection. Dissolve the contents of the vial in water for injection: 600 mg (500 100 mg) - in 10 ml of water for injection or 1.2 g (1000 200 mg) - in 20 ml of water for injection. The solution is administered slowly (over 3-4 min).
The drug Amoxiclav® it should be administered within 20 minutes after the preparation of solutions for intravenous administration.
Preparation of solutions for intravenous infusions. For infusion administration of the drug Amoxiclav® further dilution is necessary: prepared solutions containing 600 mg (500 100 mg) or 1.2 g (1000 200 mg) of the drug should be diluted in 50 or 100 ml of the infusion solution, respectively. The duration of the infusion is 30-40 minutes.
When using the liquids listed below in the recommended volumes, the necessary concentrations of the antibiotic are preserved in the infusion solutions:
| Liquids used | A period of stability, h | |
| at 25 °C | at 5 °C | |
| Water for injection | 4 | 8 |
| 0.9% sodium chloride solution for intravenous infusions | 4 | 8 |
| Normal saline and ringer's lactate for the on/in infusion | 3 | |
| Solution of calcium chloride and sodium chloride for intravenous infusions | 3 | |
Solution of the drug Amoxiclav® do not mix with dextrose, dextran, or sodium bicarbonate solutions.
Only clear solutions should be used. Prepared solutions should not be frozen.
Amoxiclav® Quicktab
Inside. The dosage regimen is set individually depending on the age, body weight, kidney function of the patient and the severity of the infection.
The tablets should be dissolved in half a glass of water (at least 30 ml) and thoroughly mixed, then drink or hold the tablets in your mouth until completely dissolved, then swallow.
In order to reduce the risk of side effects from the gastrointestinal tract, you should take the drug at the beginning of a meal.
Dispersible tablets of the drug Amoxiclav®Quicktab 500 mg/125 mg:
Adults and children over 12 years of age with a body weight of ≥40 kg
For the treatment of mild and moderate infections — 1 tablet (500 mg/125 mg) every 12 hours (2 times a day).
For the treatment of severe infections and respiratory infections — 1 tablet (500 mg/125 mg) every 8 hours (3 times a day).
The maximum daily dose of the drug Amoxiclav®Quicktab is 1500 mg of amoxicillin/375 mg of clavulanic acid.
Patients with impaired renal function. In patients with a creatinine Cl above 30 ml/min, there is no need for dose adjustment.
Adults and children over 12 years of age with a body weight of ≥40 kg (the indicated dosage regimen is used for moderate and severe infections):
| Cl creatinine clearance, ml/min | Dose | |
| 10–30 | 500 mg/125 mg 2 times a day (for moderate to severe infection) | |
| <10 | 500 mg/125 mg 1 time per day (for moderate to severe infection) | |
| Hemodialysis | 500 mg / 125 mg every 24 hours, plus 500 mg/125 mg during the dialysis session, with repeated use at the end of the dialysis session (since plasma concentrations of amoxicillin and clavulanic acid decrease) |
Dispersible tablets of the drug Amoxiclav®Quicktab 875 mg/125 mg:
Adults and children over 12 years of age with a body weight of ≥40 kg
For severe infections and respiratory infections — 1 table (875 mg / 125 mg) every 12 hours (2 times a day).
Daily dose of the drug Amoxiclav®Quicktab when used 2 times a day is 1750 mg of amoxicillin/250 mg of clavulanic acid.
Patients with impaired renal function. In patients with a creatinine Cl of more than 30 ml/min, there is no need for dose adjustment.
Patients with creatinine Cl less than 30 ml / min using dispersible tablets of Amoxiclav®Quicktab, 875 mg/125 mg is contraindicated.
Such patients should take the drug at a dosage of 500 mg/125 mg after a dose adjustment corresponding to the level of Cl creatinine.
Patients with impaired liver function. When taking the drug Amoxiclav®Quicktab should be careful. It is necessary to conduct regular monitoring of liver function. In the case of starting treatment with parenteral administration of the drug, therapy can be continued by taking tablets of the drug Amoxiclav®Quicktab.
The duration of the course of treatment is determined by the attending physician!
The minimum course of antibacterial therapy is 5 days. Treatment should not last more than 14 days without reviewing the clinical situation.
hypersensitivity to the components of the drug,
hypersensitivity to penicillins, cephalosporins and other beta-lactam antibiotics in the anamnesis,
a history of cholestatic jaundice and/or other liver disorders caused by amoxicillin/clavulanic acid,
infectious mononucleosis, lymphatic leukemia, and,
For Amoxiclav dispersible tablets® Quicktab optional
children under 12 years of age or with a body weight of less than 40 kg.
phenylketonuria,
renal insufficiency (Creatinine Cl <30 ml / min) (for dispersible tablets 875 mg 125 mg)
With caution: pseudomembranous colitis in the anamnesis, gastrointestinal diseases, liver failure, severe renal impairment, pregnancy, lactation, concomitant use with anticoagulants.
Amoxiclav® film-coated tablets and powder for the preparation of a solution for intravenous administration
From the digestive system: loss of appetite, nausea, vomiting, diarrhea, abdominal pain, gastritis, stomatitis, glossitis, black "hairy" tongue, darkening of tooth enamel, hemorrhagic colitis (also can develop after therapy), enterocolitis, pseudomembranous colitis, impaired liver function, increased ALT, AST, ALP and/or bilirubin levels in blood plasma, liver failure (more often in the elderly, men, with long-term therapy), cholestatic jaundice, hepatitis.
Allergic reactions: itching, urticaria, erythematous rashes, multiform exudative erythema, angioedema, anaphylactic shock, allergic vasculitis, exfoliative dermatitis, Stevens-Johnson syndrome, acute generalized exanthematous pustulosis, a syndrome similar to serum sickness, toxic epidermal necrolysis.
From the hematopoietic system and the lymphatic system: reversible leukopenia (including neutropenia), thrombocytopenia, hemolytic anemia, reversible increase in PV (when combined with anticoagulants), reversible increase in bleeding time, eosinophilia, pancytopenia, thrombocytosis, agranulocytosis.
From the central nervous system: dizziness, headache, convulsions (may occur in patients with impaired renal function when taking high doses of the drug).
From the urinary system: interstitial nephritis, crystalluria, hematuria.
Other: candidiasis and other types of superinfection.
Amoxiclav®
For film-coated tablets, powder for the preparation of a suspension for oral administration, powder for the preparation of a solution for intravenous administration in addition
From the central nervous system: hyperactivity. Anxiety, insomnia, behavior change, arousal.
Amoxiclav®
Amoxiclav® Quicktab
Amoxiclav® Quicktab and Amoxiclav® powder for preparation of suspension for oral administration
From the organs of hematopoiesis and the lymphatic system: rarely-reversible leukopenia (including neutropenia), thrombocytopenia, very rarely-eosinophilia, thrombocytosis, reversible agranulocytosis, increased bleeding time and reversible increase in PV, anemia, including reversible hemolytic anemia.
On the part of the immune system: the frequency is unknown — angioedema, anaphylactic reactions, allergic vasculitis, a syndrome similar to serum sickness.
From the nervous system: infrequently-dizziness, headache, very rarely-insomnia, agitation, anxiety, behavior changes, reversible hyperactivity, convulsions, convulsions can be observed in patients with impaired renal function, as well as in those who receive high doses of the drug.
From the gastrointestinal tract: often - loss of appetite, nausea, vomiting, diarrhea. Nausea is more common when ingested at high doses. If gastrointestinal disorders are confirmed, they can be eliminated if you take the drug at the beginning of a meal, infrequently-digestive disorders, very rarely-antibiotic-associated colitis induced by taking antibiotics (including pseudomembranous and hemorrhagic colitis), black "hairy" tongue, gastritis, stomatitis. In children, very rarely there was a change in the color of the surface layer of tooth enamel. Oral care helps prevent discoloration of the tooth enamel.
From the skin: infrequently-skin rash, itching, urticaria, rarely-multiform exudative erythema, frequency unknown-Stevens-Johnson syndrome, toxic epidermal necrolysis, bullous exfoliative dermatitis, acute generalized exanthematous pustulosis.
From the urinary system: very rarely — crystalluria, interstitial nephritis, hematuria.
From the liver and biliary tract: infrequently-increased activity of ALT and / or AST (this phenomenon is observed in patients receiving beta-lactam antibiotics, but its clinical significance is unknown), Adverse events from the liver were observed mainly in men and elderly patients and may be associated with long-term therapy. These adverse events are very rarely observed in children.
The listed signs and symptoms usually occur during or immediately after the end of therapy, but in some cases they may not appear for several weeks after the end of therapy. Adverse events are usually reversible. Adverse events from the liver can be severe, in extremely rare cases, there have been reports of fatal outcomes. In almost all cases, these were patients with serious comorbidities or patients receiving potentially hepatotoxic drugs at the same time. Very rarely-increased activity of alkaline phosphatase, increased bilirubin, hepatitis, cholestatic jaundice (observed with concomitant therapy with other penicillins and cephalosporins)
Other: often-candidiasis of the skin and mucous membranes, the frequency is unknown-the growth of insensitive microorganisms.
There are no reports of fatal or life-threatening side effects due to an overdose of the drug.
Symptoms: in most cases — disorders of the gastrointestinal tract (abdominal pain, diarrhea, vomiting), possibly also anxiety, insomnia, dizziness, in some cases — convulsive seizures.
Treatment: in case of overdose, the patient should be under the supervision of a doctor, treatment is symptomatic.
In the case of recent administration (less than 4 hours) of the drug, it is necessary to perform gastric lavage and prescribe activated charcoal to reduce absorption. Amoxicillin / potassium clavulanate is removed by hemodialysis.
The drug Amoxiclav® It is a combination of amoxicillin and clavulanic acid.
Amoxicillin is a semi-synthetic penicillin (beta-lactam antibiotic) that inhibits one or more enzymes (often referred to as penicillin-binding proteins, PSBs) on the pathway of the biosynthesis of peptidoglycan, which is an integral structural component of the bacterial cell wall. Inhibition of peptidoglycan synthesis leads to a loss of cell wall strength, which usually leads to the lysis and death of microbial cells.
Amoxicillin is destroyed by the action of beta-lactamases produced by resistant bacteria, so the spectrum of activity of amoxicillin does not include microorganisms that produce these enzymes.
Clavulanic acid is a beta-lactam structurally related to penicillins. It inhibits certain beta-lactamases, thereby preventing the inactivation of amoxicillin and expanding its range of activity, including bacteria that are usually resistant to amoxicillin, as well as other penicillins and cephalosporins. By itself, clavulanic acid does not have a clinically significant antibacterial effect.
The drug Amoxiclav® it has a bactericidal effect in vivo for the following microorganisms:
- gram-positive airbags — Staphylococcus aureus*, Streptococcus pneumoniae, Streptococcus pyogenes,
- gram-negative aerobes — Enterobacter spp.**, Escherichia coli*, Haemophilus influenzae*, species of the genus Klebsiella*, Moraxella catarrhalis* (Branhamella catarrhalis).
The drug Amoxiclav® it has a bactericidal effect in vitro for the following microorganisms (however, the clinical significance is still unknown):
- gram-positive airbags — Bacillis anthracis*, species of the genus Corynebacterium, Enterococcus faecalis*, Enterococcus faecium*, Listeria monocytogenes, Nocardia asteroides, coagulase-negative staphylococci* (including Staphylococcus epidermidis), Streptococcus agalactiae, other species of the genus Streptococcus, Streptococcus viridans,
- gram-positive anaerobes - species of the genus Clostridium, species of the genus Peptococcus, species of the genus Peptostreptococcus,
- gram-negative aerobes — Bordetella pertussis, species of the genus Brucella, Gardnerella vaginalis, Helicobacter pylori, species of the genus Legionella, Neisseria gonorrhoeae*, Neisseria meningitidis*, Pasteurella multocida, Proteus mirabilis*, Proteus vulgaris*, species of the genus Salmonella*, species of the genus Shigella*, Vibrio cholerae, Yersinia enterocolitica*,
- gram-negative anaerobes - species of the genus Bacteroides* (including Bacteroides fragilis), species of the genus Fusobacterium*,
- other — Borrelia burgdorferi, Chlamydia spp., Leptospira icterohaemorrhagiae, Treponema pallidum.
* Some strains of these bacterial species produce beta-lactamases, which contributes to their insensitivity to amoxicillin monotherapy.
** Most strains of these bacteria are resistant to the amoxicillin/clavulanic acid combination in vitro However, the clinical efficacy of this combination has been demonstrated in the treatment of urinary tract infections caused by these strains.
The main pharmacokinetic parameters of amoxicillin and clavulanic acid are similar. Amoxicillin and clavulanic acid are well soluble in aqueous solutions with a physiological pH value and after taking the drug Amoxiclav® inside, they are quickly and completely absorbed from the gastrointestinal tract. The absorption of the active substances-amoxicillin and clavulanic acid-is optimal in the case of taking the drug at the beginning of a meal.
The bioavailability of amoxicillin and clavulanic acid after oral administration is about 70%.
Peak plasma concentrations are reached approximately 1 h after administration. Values of Cmax make up for amoxicillin (depending on the dose) 3-12 mcg/ml, for clavulanic acid-about 2 mcg/ml.
Cmax in the blood plasma after bolus injection at a dose of 1.2 g (1000 200 mg) of the drug is 105.4 mg/l - for amoxicillin and 28.5 mg / l — for clavulanic acid.
When using the drug Amoxiclav® The plasma concentrations of amoxicillin/clavulanic acid are similar to those of oral administration of the corresponding doses of amoxicillin or clavulanic acid separately at equivalent doses.
Both components are characterized by a sufficient Vd in various organs, tissues and fluid environments of the body (including in the lungs, abdominal organs, adipose, bone and muscle tissues, pleural, synovial and peritoneal fluids, in the skin, bile, urine, purulent discharge, sputum, interstitial fluid).
Plasma protein binding is moderate — 25% for clavulanic acid and 18% for amoxicillin.
Vd it is approximately 0.3–0.4 l / kg for amoxicillin and approximately 0.2 l / kg for clavulanic acid.
Amoxicillin and clavulanic acid do not penetrate the blood-brain barrier in non-inflamed meninges.
Amoxicillin (like most penicillins) is excreted in breast milk. Trace amounts of clavulanic acid were also found in breast milk. Amoxicillin and clavulanic acid penetrate the placental barrier.
Amoxicillin is mainly excreted by the kidneys, whereas clavulanic acid is excreted by both the renal and extrarenal mechanisms. After a single oral administration of one tablet 250 125 mg or 500 125 mg, approximately 60-70% of amoxicillin and 40-65% of clavulanic acid are excreted unchanged in the urine for the first 6 hours. About 10-25% of the initial dose of amoxicillin is excreted in the urine as inactive penicillic acid. Clavulanic acid in the human body undergoes intensive metabolism with the formation of 2,5-dihydro-4 - (2-hydroxyethyl) - 5-oxo-1H-pyrrole-3-carboxylic acid and 1-amino-4-hydroxy-butane-2-one and is excreted in the urine and feces
Average T1/2 amoxicillin/clavulanic acid is approximately 1 h, the average total clearance is approximately 25 l / h in healthy patients. In the course of various studies, it was found that the excretion of amoxicillin in the urine for 24 hours is approximately 50-85%, clavulanic acid-27-60%. The greatest amount of clavulanic acid is excreted within the first 2 hours after ingestion.
The pharmacokinetic parameters of amoxicillin and clavulanic acid are summarized in Table 1.
Table 1
| Mean (±SD) pharmacokinetic parameters | |||||
| Active ingredients Amoxicillin/clavulanic acid | Dose, mg | Cmax, mcg / ml | Tmax, h | AUC(0–24), mcg * h/ml | T1/2, h |
| Amoxicillin | |||||
| 875 mg/125 mg | 875 | 11,64±2,78 | 1,5 (1–2,5) | 53,52±12,31 | 1,19±0,21 |
| 500 mg/125 mg | 500 | 7,19±2,26 | 1,5 (1–2,5) | 53,52±8,37 | 1,15±0,2 |
| Clavulanic acid | |||||
| 875 mg/125 mg | 125 | 2,18±0,99 | 1,25 (1–2) | 10,16±3,04 | 0,96±0,12 |
| 500 mg/125 mg | 125 | 2,4±0,83 | 1,5 (1–2) | 15,52±3,86 | 0,98±0,12 |
Patients with impaired liver function
In patients with severe renal insufficiency T1/2 increases to 7.5 hours for amoxicillin and 4.5 hours for clavulanic acid.
For patients with impaired liver function, the dose of the drug should be selected with caution: constant monitoring of the liver condition is necessary.
Both components are removed by hemodialysis and minor amounts are removed by peritoneal dialysis.
- Antibiotic-penicillin semi-synthetic beta-lactamase inhibitor [Penicillins in combinations]
For all dosage forms
Antacids, glucosamine, laxatives, aminoglycosides slow down the absorption, ascorbic acid increases the absorption.
Diuretics, allopurinol, phenylbutazone, NSAIDs and other drugs that block tubular secretion (probenecid) increase the concentration of amoxicillin (clavulanic acid is mainly excreted by glomerular filtration).
The simultaneous use of the drug Amoxiclav® and methotrexate increases the toxicity of methotrexate.
Administration together with allopurinol increases the frequency of exanthema. Concomitant use with disulfiram should be avoided.
Reduces the effectiveness of drugs, during the metabolism of which PABA is formed, ethinyl estradiol-the risk of breakthrough bleeding.
The literature describes rare cases of increased INR in patients with the combined use of acenocumarol or warfarin and amoxicillin. If concomitant use with anticoagulants is necessary, PV or INR should be carefully monitored when prescribing or discontinuing the drug.
The combination with rifampicin is antagonistic (mutual weakening of the antibacterial effect). The drug Amoxiclav® it should not be used simultaneously in combination with bacteriostatic antibiotics (macrolides, tetracyclines), sulfonamides due to a possible decrease in the effectiveness of the drug Amoxiclav®.
The drug Amoxiclav® reduces the effectiveness of oral contraceptives.
For dispersible tablets and powder for preparation of suspension for oral administration in addition
Increases the effectiveness of indirect anticoagulants (suppressing intestinal microflora, reduces the synthesis of vitamin K and prothrombin index). In some cases, taking the drug may prolong the PV, in this regard, caution should be exercised when using anticoagulants and Amoxiclav simultaneously®Quicktab.
Probenecid reduces the excretion of amoxicillin, increasing its serum concentration.
In patients receiving mycophenolate mofetil, after the start of the combination of amoxicillin with clavulanic acid, there was a decrease in the concentration of the active metabolite — mycophenolic acid, before taking the next dose of the drug by approximately 50%. Changes in this concentration may not accurately reflect the overall changes in mycophenolic acid exposure.
For powder for preparation of solution for intravenous administration in addition
The drug Amoxiclav® and aminoglycoside antibiotics are chemically incompatible.
The drug Amoxiclav® do not mix in a syringe or infusion bottle with other drugs.
Avoid mixing with solutions of dextrose, dextran, sodium bicarbonate, as well as with solutions containing blood, proteins, lipids.
