Augmentin 625 mg Tablets

Brand name

The drug is known in the pharmaceutical market under the trade name Augmentin. This is the registered name under which it is manufactured and distributed in pharmacy chains all over the world.

International Nonproprietary Name (INN)

The international nonproprietary name of Augmentin is amoxicillin in combination with clavulanic acid. These two components form the basis of its therapeutic action, providing a wide range of antibacterial activity.

Form of release

Augmentin is presented in several dosage forms for ease of use depending on the age of the patient and the nature of the disease. Among them:

• Film-coated tablets with dosages of 250 mg + 125 mg, 500 mg + 125 mg, 875 mg + 125 mg (where the first digit is the content of amoxicillin, the second - clavulanic acid).
• Powder for preparation of suspension for oral administration with dosages of 125 mg + 31.25 mg/5 ml, 200 mg + 28.5 mg/5 ml, 400 mg + 57 mg/5 ml.
• Powder for preparation of solution for intravenous administration (500 mg + 100 mg, 1000 mg + 200 mg).

The variety of forms allows to adapt the therapy to the individual needs of the patient.

Composition

Augmentin contains two active substances:

• Amoxicillin - an antibiotic of the penicillin group, which has a bactericidal effect.
• Clavulanic acid - a beta-lactamase inhibitor that enhances the effect of amoxicillin against resistant microorganisms.

Auxiliary components depend on the form of release. For example, tablets contain the following:

• Microcrystalline cellulose - filler.
• Crospovidone - disintegrant, providing rapid dissolution.
• Magnesium stearate - lubricant.
• Silicon dioxide - stabilizer.
• Film shell (hypromellose, titanium dioxide, polyethylene glycol).

In suspensions are added flavorings (for example, orange or raspberry), xanthan gum as a thickener and sweeteners to improve the taste.

Pharmacologic Properties

Pharmacodynamics

Augmentin has a pronounced bactericidal effect, which means the ability to destroy bacteria, not just inhibit their growth. Amoxicillin disrupts the synthesis of the bacterial cell wall by binding to penicillin-binding proteins, which leads to the destruction of the microorganism. However, many bacteria produce beta-lactamases, enzymes that destroy amoxicillin. This is where clavulanic acid comes into action, which irreversibly blocks these enzymes, restoring the effectiveness of the antibiotic.

The drug is active against a wide range of Gram-positive and Gram-negative bacteria, including Staphylococcus aureus (except methicillin-resistant strains), Streptococcus pneumoniae, Escherichia coli, Klebsiella spp., Haemophilus influenzae and many other pathogens.

Pharmacokinetics

Augmentin shows favorable pharmacokinetic characteristics, which ensures its high bioavailability and efficacy.

Augmentin absorption

After oral administration, both components are rapidly absorbed in the gastrointestinal tract. The maximum concentration in plasma is reached in 1-2 hours. Food intake has little effect on absorption, which allows the drug to be taken independently of food, although coadministration with food may reduce the risk of gastric irritation.

Distribution

Amoxicillin and clavulanic acid penetrate well into tissues and body fluids, including the lungs, middle ear, sinuses, urine, and bile. However, penetration across the blood-brain barrier is limited except in cases of inflammation of the cerebral membranes.

Metabolism

Amoxicillin is partially metabolized in the liver (about 10-20%) to form inactive metabolites. Clavulanic acid is more extensively metabolized to inactive derivatives, which are excreted from the body.

Excretion

The main route of excretion is through the kidneys. About 50-70% of amoxicillin and 30-40% of clavulanic acid are excreted unchanged with urine during the first 6 hours after administration. The elimination half-life is approximately 1-1.5 hours for both substances in patients with normal renal function.

Indications for Use

Augmentin is prescribed for the treatment of infectious diseases caused by microorganisms sensitive to the drug. The main indications include:

• Infections of the upper respiratory tract: acute and chronic sinusitis, otitis media, tonsillitis, pharyngitis.
• Infections of the lower respiratory tract: bronchitis, pneumonia, exacerbation of chronic bronchitis.
• Infections of the urinary tract: cystitis, pyelonephritis, urethritis.
• Infections of the skin and soft tissues: furunculosis, abscesses, cellulitis, wound infections.
• Infections of bones and joints: osteomyelitis.
• Gynecologic infections: endometritis, salpingitis.
• Infections associated with surgical interventions (prevention and treatment).

The drug is often used in pediatrics and adult practice due to its versatility and broad spectrum of action.

Contraindications

The use of Augmentin is prohibited in the following cases:

• Individual hypersensitivity to amoxicillin, clavulanic acid, other penicillins or components of the drug.
• A history of severe allergic reactions (anaphylaxis, Stevens-Johnson syndrome) to beta-lactam antibiotics.
• Infectious mononucleosis or lympholeukemia, as taking amoxicillin may provoke a rash.
• Severe hepatic impairment or previous episodes of jaundice associated with the administration of amoxicillin/clavulanic acid combination.

With caution, the drug is administered to patients with impaired renal function or allergic diathesis.

Method of Administration and Dosage

How to take

Augmentin tablets should be swallowed whole, drinking enough water (at least 100 ml). It is recommended to take the drug at the beginning of a meal to minimize gastric irritation. The suspension is prepared by adding water up to the mark indicated on the bottle, shake before each administration. The solution for injection is administered by a healthcare professional by intravenous injection slowly (over 3-4 minutes) or by drip.

Dosages for adults and children

Dosage depends on the severity of infection, age and body weight of the patient:

• Adults and children over 12 years of age or with a body weight greater than 40 kg: the standard dose is 500 mg + 125 mg every 8 hours or 875 mg + 125 mg every 12 hours.
• Children from 3 months to 12 years: suspension at a dose of 20-40 mg/kg body weight per day (per amoxicillin) divided into 2-3 doses.
• Children younger than 3 months: 30 mg/kg/day (by amoxicillin), divided into 2 doses.

For intravenous administration: 1000 mg + 200 mg every 8 hours for severe infections.

Dose adjustment for certain conditions

In renal insufficiency the dosage is adjusted depending on creatinine clearance:

• Clearance 10-30 ml/min: 500 mg + 125 mg twice daily.
• Clearance less than 10 mL/min: 500 mg + 125 mg once daily.

In hepatic insufficiency, regular monitoring of liver function is required, but there are no strict recommendations for dose adjustment.

Side Effects

Augmentin is usually well tolerated, but the following adverse reactions are possible:

• Gastrointestinal disorders: nausea, diarrhea, vomiting, abdominal pain (more often when taking high doses).
• Allergic reactions: skin rash, itching, urticaria, rarely - angioedema.
• Hematologic disorders: reversible leukopenia, thrombocytopenia.
• Hepatic effects: increased transaminase levels, hepatitis (rare).
• Nervous system: dizziness, headache, seizures (in case of overdose).

If severe side effects occur, discontinue use immediately and consult a physician.

Overdose

Symptoms of overdose

Exceeding the recommended dose may cause nausea, vomiting, diarrhea, convulsions, disorders of water-electrolyte balance, crystalluria (precipitation of amoxicillin crystals in the urine).

First aid measures

In case of overdose it is necessary:

• Stop taking the drug.
• Rinse the stomach (if it has been less than 1 hour after intake).
• Take activated charcoal.
• Supply symptomatic treatment (hydration, correction of electrolytes).
• Seek medical attention.

Hemodialysis is effective in removing amoxicillin and clavulanic acid from the blood.

Drug Interactions

Augmentin may interact with other medicines:

• Anticoagulants (warfarin): increased effect, increased risk of bleeding.
• Methotrexate: increase in toxicity by reducing its excretion.
• Probenecid: slows the excretion of amoxicillin, increasing its concentration in the blood.

Compatibility with alcohol and food

Alcohol has no direct effect on the effect of Augmentin, but its use during infection may worsen the liver condition and delay recovery. Food does not affect bioavailability, but fatty foods may slow absorption.

Special Precautions

Use in pregnancy and breastfeeding

Augmentin is approved for use in pregnancy only for strict indications if the benefit outweighs the risk to the fetus. Both components penetrate through the placenta and are excreted with breast milk in small amounts, so in lactation requires an assessment of the need for therapy.

Effect on driving and mechanisms

The drug does not significantly affect the ability to drive a car or operate machinery. However, in case of occurrence of side effects (dizziness, convulsions) it is necessary to refrain from such actions.

Particularities of use in the elderly and children

In elderly patients with age-related changes in renal function, a dose reduction may be required. In children the drug is widely used, but the dosage is strictly calculated by body weight to avoid toxic effects.