CLAVUNOVA 457MG SUSPENSION

Indications

• Bacterial infections
• Urinary tract infections
• Sinusitis
• Uncomplicated community-acquired pneumonia
• Salmonellosis
• Oral infections
• Lyme disease (under expert supervision)
• Acute exacerbation of bronchiectasis
• Anthrax (treatment and post-exposure prophylaxis)

Dosage

Children: 1 month–11 years: 30 mg/kg 3 times a day for 21 days; children 1–4 years: 250 mg 3 times a day; children 5–11 years: 500 mg 3 times a day.

Adults: 500 mg 3 times a day; increased if necessary up to 1 g 3 times a day in severe infections.

Mechanism of action

Amoxicillin works by inhibiting bacterial cell wall synthesis, leading to cell lysis and death. It binds to penicillin-binding proteins (PBPs) located inside the bacterial cell wall, interfering with the transpeptidation process necessary for cell wall integrity.

Pharmacodynamics

Amoxicillin exhibits bactericidal activity against susceptible bacteria. Its action is time-dependent, meaning that its effectiveness is related to the duration of time that the drug concentration remains above the minimum inhibitory concentration (MIC) for the target pathogen.

Pharmacokinetics

Amoxicillin is well absorbed from the gastrointestinal tract, with peak plasma concentrations achieved within 1-2 hours after oral administration. It is widely distributed in body tissues and fluids, and it is excreted primarily via the kidneys. The elimination half-life is approximately 1 hour, and renal impairment may necessitate dosage adjustments.

Adverse effects

• Skin rash
• Gastrointestinal disturbances (nausea, vomiting, diarrhea)
• Allergic reactions (including anaphylaxis)
• Superinfection (due to resistant organisms)

Interactions

• Allopurinol (increases risk of skin rash)

Precautions

• History of penicillin allergy
• Renal impairment (reduce dose)
• Use with caution in patients with mononucleosis

Pregnancy

Use only if clearly needed; no adequate studies in pregnant women.

Breast-feeding

Amoxicillin is excreted in breast milk; use with caution.

Storage

Store in a cool, dry place away from direct sunlight.

Formulations

• Phenoxymethylpenicillin 250mg/5ml oral solution
• Phenoxymethylpenicillin 250 mg tablets

Indications

• Bacterial infections caused by beta-lactamase producing organisms
• Respiratory tract infections
• Urinary tract infections
• Skin and soft tissue infections

Dosage

Children: Refer to specific product guidelines as dosing may vary depending on the formulation and indication.

Adults: Refer to specific product guidelines as dosing may vary depending on the formulation and indication.

Mechanism of action

Clavulanate works by irreversibly binding to and inhibiting beta-lactamase enzymes. These enzymes are produced by certain bacteria to destroy the beta-lactam ring structure of penicillins and cephalosporins, rendering these antibiotics ineffective. By inhibiting beta-lactamases, clavulanate protects the accompanying antibiotic from degradation, allowing it to exert its antibacterial effect.

Pharmacodynamics

Clavulanate exhibits a synergistic effect when used in combination with beta-lactam antibiotics, enhancing their potency against resistant strains of bacteria. While clavulanate has weak antibacterial properties on its own, its primary role is to prevent the breakdown of the co-administered antibiotic, thus maintaining its efficacy in treating infections. The combination of clavulanate with antibiotics like amoxicillin results in a broader spectrum of activity against various gram-positive and gram-negative organisms.

Pharmacokinetics

Clavulanate is rapidly absorbed following oral administration, with peak plasma concentrations typically achieved within one hour. It is widely distributed throughout body tissues and fluids. The drug is primarily excreted by the kidneys, with a significant portion eliminated as unchanged drug in the urine. The half-life of clavulanate is approximately 1 hour, which necessitates frequent dosing when used in combination therapies.

Contra-indications

• Hypersensitivity to clavulanate or any component of the formulation
• History of jaundice or hepatic dysfunction associated with beta-lactam antibiotics

Adverse effects

• Diarrhea
• Nausea
• Vomiting
• Rash
• Elevated liver enzymes
• Hepatitis
• Anaphylaxis
• Clostridium difficile-associated diarrhea

Interactions

• May enhance the anticoagulant effect of warfarin
• Probenecid may increase levels of clavulanate

Precautions

• Use with caution in patients with a history of liver disease
• Monitor for signs of allergic reactions
• Consider potential for superinfection with prolonged use

Pregnancy

Clavulanate should be used in pregnancy only if clearly needed; data on its safety are limited.

Breast-feeding

Clavulanate is excreted in breast milk; caution is advised when administering to nursing mothers.

Storage

Store at room temperature, away from moisture and heat; protect from light.

Formulations

• Tablets
• Oral suspension
• Injectable solution

Mechanism of action

Amoxicillin competitively inhibits penicillin-binding protein 1 and other high molecular weight penicillin binding proteins. Penicillin bind proteins are responsible for glycosyltransferase and transpeptidase reactions that lead to cross-linking of D-alanine and D-aspartic acid in bacterial cell walls. Without the action of penicillin binding proteins, bacteria upregulate autolytic enzymes and are unable to build and repair the cell wall, leading to bacteriocidal action. The penicillins and their metabolites are potent immunogens because of their ability to combine with proteins and act as haptens for acute antibody-mediated reactions. The most frequent (about 95 percent) or "major" determinant of penicillin allergy is the penicilloyl determinant produced by opening the beta-lactam ring of the penicillin. This allows linkage of the penicillin to protein at the amide group. "Minor" determinants (less frequent) are the other metabolites formed, including native penicillin and penicilloic acids. /Penicillins/ Amoxicillin is similar to penicillin in its bactericidal action against susceptible bacteria during the stage of active multiplication. It acts through the inhibition of cell wall biosynthesis that leads to the death of the bacteria.

Pharmacodynamics

Amoxicillin competitively inhibit penicillin binding proteins, leading to upregulation of autolytic enzymes and inhibition of cell wall synthesis. Amoxicillin has a long duration of action as it is usually given twice daily. Amoxicillin has a wide therapeutic range as mild overdoses are not associated with significant toxicity. Patients should be counselled regarding the risk of anaphylaxis, _Clostridium difficile_ infections, and bacterial resistance.