Amoxiclav powder for suspension 156.25 mg/5 ml bottle 100 ml **

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Composition of Amoxiclav

  • Amoxiclav 250 mg/125 mg tablets contain the active ingredients amoxicillin (trihydrate form) and clavulanic acid (potassium salt form). The tablets also contain auxiliary components: MCC sodium croscarmellose.
  • Amoxiclav 2X 625 mg and 1000 mg tablets contain the active ingredients amoxicillin and clavulanic acid, as well as additional components: anhydrous colloidal silicon dioxide, flavorings, aspartame , yellow iron oxide, talc, hydrogenated castor oil, silicated MCC.
  • Amoxiclav Quiktab 500 mg and 875 mg tablets contain the active ingredients amoxicillin and clavulanic acid, as well as additional components: anhydrous colloidal silicon dioxide, flavorings, aspartame, yellow iron oxide, talc, hydrogenated castor oil, silicated MCC.
  • The powder from which the Amoxiclav suspension is prepared also contains amoxicillin and clavulanic acid, and also contains sodium citrate, MCC, sodium benzoate, mannitol, and sodium saccharin as inactive components.
  • The powder for preparing Amoxiclav IV infusion contains amoxicillin and clavulanic acid.

Pharmacokinetics and pharmacodynamics

As the Vidal drug reference book informs, after oral administration, both substances are actively absorbed from the gastrointestinal tract; the absorption of the components is not affected by food intake, so it does not matter how you take it - before or after meals. The highest concentration in the blood is observed one hour after the drug was taken. Both active ingredients of the drug are distributed in fluids and tissues. Amoxicillin also enters the liver, synovial fluid, prostate, tonsils, gall bladder, muscle tissue, saliva, and bronchial secretions.

If the membranes of the brain are not inflamed, both active substances do not penetrate through the BBB. At the same time, the active components penetrate the placental barrier and traces of them are detected in breast milk. They bind to blood proteins to a small extent.

In the body, amoxicillin undergoes partial metabolism , clavulanic acid is intensively metabolized. It is excreted from the body through the kidneys; small particles of active substances are excreted by the intestines and lungs. The half-life of amoxicillin and clavulanic acid is 1-1.5 hours.

Reviews about Amoxiclav

In the process of discussing the drug Amoxiclav, reviews from doctors and patients are predominantly positive. It is noted that the antibiotic is effective in the treatment of respiratory tract diseases, and it is suitable for both adults and children. Reviews mention the effectiveness of the product for sinusitis, otitis media, and genital tract infections. As a rule, adult patients take 875 mg + 125 mg tablets; if the dosage is correct, relief occurs quickly. Reviews note that after a course of antibiotic treatment, it is advisable to take drugs that restore normal microflora .

Reviews of the Amoxiclav suspension are also positive. Parents write that it is convenient to give the product to children, as it has a pleasant taste and is normally perceived by children.

Amoxiclav 250mg+62.5mg/5ml 25g 100ml powder for oral suspension

pharmachologic effect

Antibiotic - semi-synthetic penicillin + beta-lactamase inhibitor.

Composition and release form Amoxiclav 250 mg + 62.5 mg/5 ml 25 g 100 ml powder for the preparation of suspension for oral administration

Powder for the preparation of a suspension for oral administration - 5 ml of suspension:

  • active ingredients: amoxicillin (in the form of trihydrate) - 250 mg; clavulanic acid (in the form of potassium salt) - 62.5 mg;
  • excipients: citric acid (anhydrous) - 2.167 mg; sodium citrate (anhydrous) - 8.335 mg; sodium benzoate - 2.085 mg; MCC and carmellose sodium - 28.1 mg; xanthan gum - 10 mg; colloidal silicon dioxide - 16.667 mg; silicon dioxide - 0.217 g; sodium saccharinate - 5.5 mg; mannitol - 1250 mg; wild cherry flavor - 4 mg.

Powder for the preparation of suspension for oral administration 250 mg + 62.5 mg/5 ml. Primary packaging - 25 g of powder (100 ml of finished suspension) in a dark glass bottle with a ring mark (100 ml). The bottle is closed with a screw-on metal cap with a control ring, inside the cap there is a LDPE gasket.

Secondary packaging - 1 fl. with a dosing spoon with ring marks in the cavity for 2.5 and 5 ml (“2.5 SS” and “5 SS”), a maximum filling mark of 6 ml (“6 SS”) on the handle of the spoon in a cardboard box. Or 1 fl. together with a graduated dosage pipette in a cardboard box.

Description of the dosage form

Powder for oral suspension: white to yellowish-white powder. The finished suspension is an almost white to yellow homogeneous suspension.

Directions for use and doses

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 dosage pipette is inserted into each package of suspensions 125+31.25 mg/5 ml and 250+62.5 mg/5 ml, graduated at 5 ml, with a scale of division of 0.1 ml or a dosing spoon with a capacity of 5 ml, with ring marks in the cavity at 2.5 and 5 ml).

Newborns and children up to 3 months - 30 mg/kg/day (for amoxicillin), divided into 2 doses (every 12 hours).

Dosing of the drug Amoxiclav® with a dosing pipette - calculation of single doses for the treatment of infections in newborns and children up to 3 months (Table 3).

Table 3

Body weight, kg22,22,42,62,833,23,43,63,844,24,44,64.8
Suspension 156.25, ml (2 times a day)1,21,31,41,61,71,81,922,22,32,42,52,62,82,9
Suspension 312.5, ml (2 times a day)0,60,70,70,80,80,9111,11,11,21,31,31,41,4

Children over 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 h).

Dosing of the drug Amoxiclav® with a dosing pipette - calculation of single doses for the treatment of mild and moderate infections in children over 3 months (at the rate of 20 mg/kg/day (for amoxicillin) (Table 4).

Table 4

Body weight, kg5678910111213141516171819202122
Suspension 156.25, ml (3 times a day)1,31,61,92,12,42,72,93,23,53,744,34,54,85,15,35,65,9
Suspension 312.5, ml (3 times a day)0,70,80,91,11,21,31,51,61,71,922,12,32,42,52,72,82,9
Body weight, kg2324252627282930313233343536373839
Suspension 156.25, ml (3 times a day)6,16,46,76,97,27,57,788,38,58,89,19,39,69,910,110,4
Suspension 312.5, ml (3 times a day)3,13,23,33,53,63,73,944,14,34,44,54,74,84,95,15,2

Dosing of the drug Amoxiclav® with a dosing pipette - calculation of single doses for the treatment of severe infections in children over 3 months (at the rate of 40 mg/kg/day (for amoxicillin) (Table 5).

Table 5

Body weight, kg5678910111213141516171819202122
Suspension 156.25, ml (3 times a day)2,73,23,74,34,85,35,96,46,97,588,59,19,610,110,711,211,7
Suspension 312.5, ml (3 times a day)1,31,61,92,12,42,72,93,23,53,744,34,54,85,15,35,65,9
Body weight, kg2324252627282930313233343536373839
Suspension 156.25, ml (3 times a day)12,312,813,313,914,414,915,51616,517,117,618,118,719,219,720,320,8
Suspension 312.5, ml (3 times a day)6,16,46,76,97,27,57,788,38,58,89,19,39,69,910,110,4

Dosing of the drug Amoxiclav® with a dosing spoon (in the absence of a dosing pipette) - recommended doses of suspensions depending on the child’s body weight and the severity of the infection (Table 6).

Table 6

Body weight, kgAge (approx.)Mild/moderate courseSevere course
125+31.25 mg/5 ml250+62.5 mg/5 ml125+31.25 mg/5 ml250+62.5 mg/5 ml
5–103–12 months3 × 2.5 ml (½ spoon)3 × 1.25 ml3 × 3.75 ml3 × 2 ml
10–121–2 years3 × 3.75 ml3 × 2 ml3 × 6.25 ml3 × 3 ml
12–152–4 years3 × 5 ml (1 spoon)3 × 2.5 ml (½ spoon)3 × 7.5 ml (1½ spoons)3 × 3.75 ml
15–204–6 years3 × 6.25 ml3 × 3 ml3 × 9.5 ml3 × 5 ml (1 spoon)
20–306–10 years3 × 8.75 ml3 × 4.5 ml3 × 7 ml
30–4010–12 years3 × 6.5 ml3 × 9.5 ml
≥40≥12 yearsAmoxiclav® tablets

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 dosage pipette is inserted into each package of the 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 over 3 months.

Table 7

Recommended dose of suspension depending on the child’s body weight and severity of infection

Body weight, kgAge (approx.)Recommended dose, ml
Severe courseModerate course
5–103–12 months2×2,52×1,25
10–151–2 years2×3,752×2,5
15–202–4 years2×52×3,75
20–304 years - 6 years2×7,52×5
30–406–10 years2×102×6,5

Exact daily doses are calculated based on the child's body weight, not his 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 indicated dosage regimen is used for moderate and severe infections)

For patients with creatinine Cl 10-30 ml/min - 500/125 mg 2 times a day.

With Cl creatinine

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 creatinine Cl 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).

With Cl creatinine

For hemodialysis, the recommended dose is 15/3.75 mg/kg once a day. Before hemodialysis - 15/3.75 mg/kg. To restore 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 5–14 days. The duration of treatment is determined by the attending physician. Treatment should not continue for more than 14 days without repeated medical examination.

Pharmacodynamics

Mechanism of action

Amoxicillin is a semisynthetic broad-spectrum antibiotic that is active against many gram-positive and gram-negative microorganisms. At the same time, amoxicillin is susceptible to destruction by beta-lactamases, and therefore the spectrum of activity of amoxicillin does not extend to microorganisms that produce this enzyme.

Clavulanic acid is a beta-lactamase inhibitor, structurally related to penicillins, and has the ability to inactivate a wide range of beta-lactamases found in microorganisms resistant to penicillins and cephalosporins. Clavulanic acid is sufficiently effective against plasmid beta-lactamases, which most often cause bacterial resistance, and is not effective against type I chromosomal beta-lactamases, which are not inhibited by clavulanic acid.

The presence of clavulanic acid in the drug protects amoxicillin from destruction by enzymes - beta-lactamases, which expands the antibacterial spectrum of amoxicillin.

Below is the activity of the combination of amoxicillin and clavulanic acid in vitro.

Grampore-positive aerobes: Bacillus Anthracis, Enterococcus Faecalis, Listeria MonocyTogenes, NoCardia Asteroides, Streptococcus Pyogenes1,2, Streptococcus Agalactiae1,2, other beta-heemolytic statococci1, 2, Staphylococcus aureus (sensitive to methicillin) 1, Staphylococcus saprophyticus (sensitive to methicillin), coagulase-negative staphylococci (sensitive to methicillin).

Gram-negative aerobes: Bordetella pertussis, Haemophilus influenzae1, Helicobacter pylori, Moraxella catarrhalis1, Neisseria gonorrhoeae, Pasteurella multocida, Vibrio cholerae.

Other: Borrelia burgdorferi, Leptospira icterohaemorrhagiae, Treponema pallidum.

Gram-positive anaerobes: species of the genus Clostridium, Peptococcus niger, Peptostrepiococcus magnus, Peptostreptococcus micros, species of the genus Pepto streptococcus.

Gram-negative anaerobes: Bcicteroides fragilis, species of the genus Bacteroides, species of the genus Capnocytophaga, Eikenella corrodens, Fusobacterium nucleatum, species of the genus Fusobacterium, species of the genus Porphyromonas, species of the genus Prevotella.

Bacteria for which acquired resistance to the combination of amoxicillin and clavulanic acid is likely

Gram-negative aerobes: Escherichia coli1, Klebsiella oxytoca, Klebsiella pneumoniae, species of the genus Klebsiella, Proteus mirabilis, Proteus vulgaris, species of the genus Proteus, species of the genus Salmonella, species of the genus Shigella. Streptococcus pneumoniae1,2, streptococci of the Viridans group.

Gram-positive aerobes: species of the genus Corynebacterium, Enterococcus faecium.

Bacteria that are naturally resistant to the combination of amoxicillin and clavulanic acid

Gram-negative aerobes: species of the genus Acinetobacter, Citrobacter freundii, species of the genus Enterobacter, Hafhia alvei, Legionella pneumophila, Morganella morganii, species of the genus Providencia, species of the genus Pseudomonas, species of the genus Serratia, Stenotrophomonas maltophilia, Yersinia enterocolitica.

Other: Chlamydia pneumoniae, Chlamydia psittaci, species of the genus Chlamydia, Coxiella burnetii, species of the genus Mycoplasma.

1For these bacteria, the clinical effectiveness of the combination of amoxicillin with clavulanic acid has been demonstrated in clinical studies.

2 strains of these types of bacteria do not produce beta-lactamases. Sensitivity during amoxicillin monotherapy suggests similar sensitivity to the combination of amoxicillin and clavulanic acid.

Pharmacokinetics

Suction

The active ingredients of the drug are quickly and completely absorbed from the gastrointestinal tract (GIT) after oral administration. Absorption of active ingredients is optimal when the drug is used with food.

The following are the pharmacokinetic parameters of amoxicillin and clavulanic acid after administration at a dose of 45 mg/6.4 mg/kg, divided into two doses, by patients under 12 years of age.

Average value of pharmacokinetic parameters

Cmax (mg/ml)T max (h)AUC (mg in h/l)T1/2 (h)
Amoxicillin11,99±3,281,0 (1,0-2,0)35,2±5,01,22±0,28
Clavulanic acid5,49±2,711,0 (1,0-2,0)13,26±5,880,99±0,14
  • Cmax - maximum concentration in blood plasma;
  • Tmax is the time to reach the maximum concentration in the blood plasma;
  • AUC—area under the concentration-time curve;
  • T1/2 - half-life.

Metabolism

About 10-25% of the initial dose of amoxicillin is excreted by the kidneys in the form of an inactive metabolite (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-butan-2-one and is excreted by the kidneys, through the gastrointestinal tract, and also with exhaled air in the form of carbon dioxide.

Distribution

As with intravenous administration of a combination of amoxicillin and clavulanic acid, therapeutic concentrations of amoxicillin and clavulanic acid are found in various tissues and interstitial fluid (gallbladder, abdominal tissue, skin, adipose and muscle tissue, synovial and peritoneal fluids, bile, purulent discharge) .

Amoxicillin and clavulanic acid have a weak degree of binding to plasma proteins. Studies have shown that about 25% of the total amount of clavulanic acid and 18% of amoxicillin in the blood plasma is bound to plasma proteins.

The volume of distribution 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 when the meninges are not inflamed. Amoxicillin (like most penicillins) is excreted in breast milk.

Trace amounts of clavulanic acid may also be found in breast milk. With the exception of the possibility of sensitization, diarrhea and candidiasis of the oral mucosa, there are no other known negative effects of amoxicillin and clavulanic acid on the health of breastfed infants.

Animal reproductive studies have shown that amoxicillin and clavulanic acid cross the placental barrier. However, no negative effects on the fetus were detected.

Removal

Amoxicillin is eliminated primarily by the kidneys, while clavulanic acid is eliminated through both renal and extrarenal mechanisms. After a single oral dose of 875 mg/125 mg or 500 mg/125 mg, approximately 60-70% of amoxicillin and 40-65% of clavulanic acid are excreted unchanged by the kidneys during the first 6 hours. The average half-life (T1/2) of amoxicillin/clavulanic acid is approximately 1 hour, and the average total clearance is approximately 25 L/h in healthy patients. In various studies, it was found that amoxicillin excretion by the kidneys within 24 hours is approximately 50-85%, clavulanic acid - 27-60%. The largest amount of clavulanic acid is excreted during the first 2 hours after administration.

The pharmacokinetics of amoxicillin/clavulanic acid does not depend on the gender of the patient.

Patients with impaired renal function

The total clearance of amoxicillin/clavulanic acid decreases in proportion to the decrease in renal function. The decrease in clearance is more pronounced for amoxicillin than for clavulanic acid, because Most amoxicillin is excreted by the kidneys. Doses of the drug for renal failure should be selected taking into account the undesirability of amoxicillin accumulation while maintaining normal levels of clavulanic acid.

Patients with liver dysfunction

In patients with impaired liver function, the drug is used with caution. It is necessary to constantly monitor liver function.

Both components are removed by hemodialysis and minor amounts by peritoneal dialysis.

Indications for use Amoxiclav 250 mg + 62.5 mg/5 ml 25 g 100 ml powder for the preparation of suspension for oral administration

Infections caused by sensitive strains of microorganisms:

  • upper respiratory tract and ENT organs (including acute and chronic sinusitis, acute and chronic otitis media, retropharyngeal abscess, tonsillitis, pharyngitis);
  • lower respiratory tract (including acute bronchitis with bacterial superinfection, chronic bronchitis, pneumonia);
  • urinary tract (eg cystitis, urethritis, pyelonephritis);
  • in gynecology;
  • skin and soft tissues, including human and animal bites;
  • bone and connective tissue;
  • biliary tract (cholecystitis, cholangitis);
  • odontogenic.

Contraindications

  • hypersensitivity to the components of the drug;
  • history of hypersensitivity to penicillins, cephalosporins and other beta-lactam antibiotics;
  • history of cholestatic jaundice and/or other liver dysfunction caused by taking amoxicillin/clavulanic acid;
  • infectious mononucleosis and lymphocytic leukemia;

With caution: history of pseudomembranous colitis, gastrointestinal diseases, liver failure, severe renal impairment, pregnancy, lactation, simultaneous use with anticoagulants.

Application Amoxiclav 250mg+62.5mg/5ml 25g 100ml powder for the preparation of suspension for oral administration during pregnancy and breastfeeding

During pregnancy and lactation, Amoxiclav® is used only if the expected benefit to the mother outweighs the potential risk to the fetus and child.

Amoxicillin and clavulanic acid pass into breast milk in small quantities.

special instructions

During a course of treatment, it is necessary to monitor the state of the function of the hematopoietic organs, liver, and kidneys.

In patients with severe renal impairment, adequate dose adjustment or increased intervals between doses is required.

It is possible that superinfection may develop due to the growth of microflora that is insensitive to it, which requires a corresponding change in antibacterial therapy.

In patients who are hypersensitive to penicillins, cross-allergic reactions with cephalosporin antibiotics are possible.

In women with premature rupture of membranes, it was found that prophylactic therapy with amoxicillin + clavulanic acid may be associated with an increased risk of developing necrotizing colitis in the newborn.

Crystalluria very rarely occurs in patients with reduced diuresis. During the use of large doses of amoxicillin, it is recommended to take sufficient fluids and maintain adequate diuresis to reduce the likelihood of amoxicillin crystal formation.

Lab tests. High concentrations of amoxicillin give a false-positive reaction to urine glucose when using Benedict's reagent or Fehling's solution. It is recommended to use enzymatic reactions with glucosidase.

Impact on the ability to drive a car or perform work that requires increased speed of physical and mental reactions. Due to the possibility of developing side effects from the central nervous system, such as dizziness, headache, convulsions, during treatment, care should be taken when driving and other activities that require concentration and speed of psychomotor reactions.

Overdose

There are no reports of death or life-threatening side effects due to drug overdose.

Symptoms: in most cases - gastrointestinal disorders (abdominal pain, diarrhea, vomiting), anxiety, insomnia, dizziness are also possible, and in isolated cases - seizures.

Treatment: in case of overdose, the patient should be under medical supervision, treatment should be symptomatic.

In case of recent use (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.

Side effects Amoxiclav 250mg+62.5mg/5ml 25g 100ml powder for suspension for oral 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 (can also develop after therapy), enterocolitis, pseudomembranous colitis, disorder liver function, increased activity of ALT, AST, alkaline phosphatase and/or bilirubin levels in the blood plasma, liver failure (more often in the elderly, men, with long-term therapy), cholestatic jaundice, hepatitis.

Allergic reactions: itching, urticaria, erythematous rashes, erythema multiforme exudative, 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 lymphatic system: reversible leukopenia (including neutropenia), thrombocytopenia, hemolytic anemia, reversible increase in PT (when used together 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.

From the side of the central nervous system: hyperactivity. Feelings of anxiety, insomnia, behavior changes, agitation.

Drug interactions

Antacids, glucosamine, laxatives, aminoglycosides slow down absorption, ascorbic acid increases absorption.

Diuretics, allopurinol, phenylbutazone, NSAIDs and other drugs that block tubular secretion (probenecid) increase the concentration of amoxicillin (clavulanic acid is excreted mainly by glomerular filtration).

The simultaneous use of Amoxiclav® and methotrexate increases the toxicity of methotrexate.

Prescription together with allopurinol increases the incidence of exanthema. Concomitant use with disulfiram should be avoided.

Reduces the effectiveness of drugs, during the metabolism of which PABA is formed; ethinyl estradiol - risk of breakthrough bleeding.

The literature describes rare cases of increased INR in patients with the combined use of acenocoumarol or warfarin and amoxicillin. If simultaneous use with anticoagulants is necessary, PT 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® 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.

The drug Amoxiclav® and aminoglycoside antibiotics are chemically incompatible.

Amoxiclav® should not be mixed 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.

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