Amoxiclav

Amoxiclav is a combination antibiotic that contains two active ingredients: amoxicillin and clavulanic acid.

1. Amoxicillin: This is an antibiotic from the penicillin group that is effective against a wide range of bacteria. It works by destroying bacterial cells or by preventing them from growing and multiplying. Amoxicillin is used to treat upper respiratory tract infections, urinary tract infections, skin infections, gastrointestinal infections, and other bacterial infections.

2. Clavulanic acid: This is a beta-lactamase inhibitor that is usually added to amoxicillin to protect it from being destroyed by beta-lactamases produced by certain bacteria. This allows amoxicillin to fight infections caused by beta-lactamase-producing bacteria more effectively, making amoxiclav particularly useful in treating penicillin-resistant infections.

Amoxiclav is widely used to treat a variety of bacterial infections, including respiratory tract infections, sinusitis, acute and chronic ear infections, urinary tract infections, skin and soft tissue infections, and other infections.

It is important to use amoxiclav only as prescribed by a doctor and follow the recommended dosage and duration of treatment to prevent the development of resistance to the antibiotic and minimize the risk of side effects.

Indications Amoxiclav

1. Upper respiratory tract infections:

   • Acute sinusitis
   • Acute otitis media
   • Pharyngitis and tonsillitis

2. Lower respiratory tract infections:

   • Acute bronchitis and exacerbation of chronic bronchitis
   • Pneumonia (especially when suspected "atypical" bacteria are not treated with standard antibiotics)

3. Urinary tract infections:

   • Cystitis
   • Pyelonephritis
   • Infections associated with medical devices (e.g., catheters)

4. Skin and soft tissue infections:

   • Abscesses
   • Ulcers
   • Wound infections
   • Animal and human bites

5. Bone and joint infections:

   • Osteomyelitis
   • Septic arthritis

6. Odontogenic infections:

   • Periodontitis
   • Infectious complications from dental procedures

7. Other infections:

   • Infections that develop after surgical procedures
   • Intra-abdominal infections
   • Sepsis associated with infections

Release form

1. Pills

Amoxiclav tablets are the most commonly used form of the drug. They come in different dosages:

• Coated tablets:
  • 250 mg amoxicillin + 125 mg clavulanic acid
  • 500 mg amoxicillin + 125 mg clavulanic acid
  • 875 mg amoxicillin + 125 mg clavulanic acid

2. Powder for oral suspension

This form of release is most often used for children and allows you to accurately dose the medicine depending on the weight and age of the child. The powder is diluted in water according to the instructions on the package.

• Powder dosages may include:
  • 125 mg amoxicillin + 31.25 mg clavulanic acid per 5 ml
  • 250 mg amoxicillin + 62.5 mg clavulanic acid per 5 ml

3. Powder for injection

Amoxiclav is also available as a powder to prepare a solution for injection, which is used for intravenous administration, usually in hospital settings.

• Dosages include:
  • 500 mg amoxicillin + 100 mg clavulanic acid
  • 1000 mg amoxicillin + 200 mg clavulanic acid

Pharmacodynamics

Amoxicillin:

• Mechanism of action: Amoxicillin belongs to the penicillin class and exerts its bactericidal action by inhibiting the synthesis of the bacterial cell wall. It binds to proteins called transpeptidases, which are involved in the formation of peptidoglycan, the main component of the bacterial cell wall, and prevents them from splicing, resulting in weakening and destruction of the wall.
• Spectrum of action: Amoxicillin is active against a wide range of bacteria, including Gram-positive and Gram-negative microorganisms. Amoxiclav is generally active against a wide range of bacteria, including many Gram-positive and Gram-negative microorganisms, as well as some anaerobic bacteria. Here are some of them:

Gram-positive bacteria:

• Streptococcus pneumoniae
• Streptococcus pyogenes
• Streptococcus viridans
• Staphylococcus aureus (in sensitive cases)
• Enterococcus faecalis
• Corynebacterium diphtheriae
• Listeria monocytogenes

Gram-negative bacteria:

• Haemophilus influenzae
• Moraxella catarrhalis
• Escherichia coli
• Klebsiella pneumoniae
• Proteus mirabilis
• Salmonella spp.
• Shigella spp.
• Helicobacter pylori (in combination with other eradication drugs)

Anaerobic bacteria:

• Bacteroides fragilis
• Clostridium perfringens
• Peptostreptococcus spp.
• Prevotella spp.

Clavulanic acid:

• Mechanism of Action: Clavulanic acid is an inhibitor of beta-lactamases, an enzyme that degrades the beta-lactam ring general mechanism of amoxicillin. It binds to these enzymes, preventing their action and protecting amoxicillin from degradation.
• Spectrum of action: Clavulanic acid itself has little activity against bacteria, but its main role in amoxiclav is to protect amoxicillin from being destroyed by beta-lactamases. This makes amoxicillin effective against a wide range of bacteria, including those that normally produce beta-lactamases and become resistant to antibiotics.

Pharmacokinetics

1. Absorption: Amoxicillin and clavulanic acid are usually rapidly and completely absorbed from the gastrointestinal tract after oral administration. Food may slow absorption but usually does not affect the amount of drug absorbed into the blood.
2. Distribution: Both components of Amoxiclav are distributed to various tissues and body fluids, including the lungs, middle ear, synovial fluid, urine, and bile.
3. Metabolism: Amoxicillin and clavulanic acid are almost completely metabolized in the liver. They do not form active metabolites.
4. Excretion: Both components are excreted mainly by the kidneys in unchanged form. A small amount is excreted through the intestine.
5. Half-life: The half-life of amoxicillin is about 1-1.5 hours and that of clavulanic acid is about 1 hour. This means that the drug can be used considering these periods during the day.

Dosing and administration

Method of Application:

• Orally (tablets or suspension):

  • Tablets should be taken at the beginning of a meal to improve absorption and reduce the risk of gastrointestinal side effects.
  • The suspension should be shaken well before use.

• Parenterally (injections):

  • Amoxiclav injection is given intravenously (not intramuscularly or subcutaneously), usually in a hospital setting.

Dosage for adults and children weighing more than 40 kg:

1. Infections of the upper and lower respiratory tract, urinary tract, skin and soft tissue:

   • The usual dose is 500 mg amoxicillin/125 mg clavulanic acid every 8 hours or 875 mg amoxicillin/125 mg clavulanic acid every 12 hours.

2. More severe infections or infections caused by less sensitive organisms:

   • 875 mg amoxicillin/125 mg clavulanic acid every 8 hours or 500 mg amoxicillin/125 mg clavulanic acid every 8 hours.

Dosage for children weighing less than 40 kg:

• The dosage is calculated according to the formula 20-40 mg of amoxicillin per kg of the child's weight per day, divided into 2-3 doses, depending on the severity of the infection.
• The maximum daily dose of clavulanic acid for children should not exceed 10 mg per kg of weight.

Intravenous administration:

• For adults and children ages 12 and up:
  • 1.2 g every 8 hours depending on the severity of the infection.
• For children under 12 years of age:
  • 30 mg amoxicillin/kg body weight every 8 hours, not to exceed the adult dose.

Special Instructions:

• Treatment should usually not exceed 14 days without review by a health care provider.
• An adequate drinking regimen should be provided to reduce the risk of crystal formation in the urine.
• Carefully monitor the function of the liver, kidneys and hematopoietic system during prolonged therapy.
• Amoxiclav may interact with other medicines, so it is important to tell your doctor about all medicines you are taking.

Use Amoxiclav during pregnancy

The drug Amoxiclav containing amoxicillin and clavulanic acid is usually not recommended for use during pregnancy without consulting a doctor. However, in some cases, the doctor may decide that the potential benefit of the drug exceeds the potential risks to the fetus.

Amoxicillin, the main component of Amoxiclav, is generally considered relatively safe for pregnant women. However, clavulanic acid may increase the risk of diarrhea and other side effects. In addition, standard recommendations for antibiotics during pregnancy may change depending on medical necessity, individual circumstances, and other factors.

Contraindications

1. Hypersensitivity: People with known hypersensitivity to amoxicillin, clavulanic acid or other penicillins should avoid Amoxiclav.
2. Mononucleosis-type infections: The use of Amoxiclav is not recommended in infections accompanied by mononucleosis syndrome due to the risk of urticaria.
3. Severe hepatic impairment: Patients with severe hepatic impairment should take Amoxiclav with caution or avoid its use.
4. History of allergic reactions: Patients with a history of allergic reactions to other beta-lactam antibiotics (e.g., cephalosporins or carbapenems) may have an increased risk of allergic reactions to amoxicillin or clavulanic acid.
5. Children and adolescents: The use of Amoxiclav in children and adolescents requires special attention and supervision by a physician, especially with regard to dosage.
6. Pregnancy and breastfeeding: Amoxiclav use during pregnancy and breastfeeding may be authorized only in case of extreme necessity and under medical supervision.
7. Diarrhea and superinfections: Use of antibiotics, including Amoxiclav, may cause diarrhea and increase the risk of superinfections.
8. Prolonged use: Prolonged use of Amoxiclav may lead to the development of resistance of microorganisms, therefore the drug should be used with caution and only when prescribed by a doctor.

Side effects Amoxiclav

1. Digestive disorders: Diarrhea, nausea, vomiting, stomach pain, dyspepsia and dysbiosis may occur.
2. Allergic reactions: Including urticaria, pruritus, skin rash, angioedema, anapylactic shock and other allergic manifestations.
3. Increased activity of liver enzymes: Changes in indices of liver function may occur.
4. Increase in heart rate: Tachycardia may occur in some patients.
5. Increased sensitivity to sunlight: Some people may experience increased sensitivity to sunlight, which can lead to sunburn or solar dermatitis.
6. Headaches and dizziness: These symptoms may occur in some patients while taking amoxiclav.
7. Changes in blood composition: Anemia, leukopenia and thrombocytopenia may develop.
8. Dysbacteriosis: The use of antibiotics can lead to changes in the intestinal microflora and the development of dysbacteriosis.

Overdose

1. Gastrointestinal disorders: Overdose may lead to a sharp increase in side effects characteristic of this drug, such as nausea, vomiting, diarrhea and dyspepsia.
2. Allergic reactions: Some patients may develop allergic reactions such as hives, itching, facial swelling, difficulty breathing, and anaphylactic shock.
3. Liver and kidney disorders: Overdose may lead to toxic effects on the liver and kidneys, which may manifest as an increase in the level of hepatic enzymes in the blood and signs of renal failure.
4. Neurotoxic effects: Some patients may experience neurotoxic symptoms such as headache, dizziness, impaired consciousness and seizures.

Interactions with other drugs

1. Probenecid: Probenecid may slow the excretion of amoxicillin, which may lead to an increase in its level in the blood and increase its duration of action.
2. Allopurinol: Allopurinol may increase the risk of skin rash when used concomitantly with amoxicillin.
3. Anticoagulants: Amoxicillin may increase the effect of anticoagulants such as warfarin, which may lead to increased clotting time and increased risk of bleeding.
4. Drugs affecting the digestive tract: Antacids, drugs containing iron, or drugs that slow intestinal peristalsis may reduce the absorption of amoxicillin, which may lead to a decrease in its effectiveness.
5. Methotrexate: Amoxicillin may increase the toxicity of methotrexate, especially at high doses, by increasing its blood levels and exacerbating its side effects.