DIOCLAV 625 MG

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
• Respiratory tract infections
• Skin and soft tissue infections
• Urinary tract infections

Dosage

Children: Refer to the BNF for Children for appropriate dosing guidelines in paediatric patients.

Adults: Refer to the specific prescribing information for the appropriate combination dosage with amoxicillin, as it varies based on the severity and type of infection.

Mechanism of action

Clavulanate works by irreversibly binding to and inhibiting beta-lactamase enzymes produced by certain bacteria. These enzymes typically hydrolyze beta-lactam antibiotics, rendering them ineffective. By inhibiting these enzymes, clavulanate protects the penicillin antibiotics from degradation, allowing them to exert their antibacterial effect.

Pharmacodynamics

Clavulanate exhibits bactericidal activity predominantly through its action as a beta-lactamase inhibitor. The combination of clavulanate and a beta-lactam antibiotic increases the spectrum of activity against resistant strains, making it effective against many gram-positive and some gram-negative bacteria. The synergistic effect improves the overall therapeutic outcome in treating infections.

Pharmacokinetics

Clavulanate is well absorbed from the gastrointestinal tract when administered orally. It reaches peak plasma concentrations within one hour after administration. The drug is primarily eliminated via the kidneys, with a half-life of approximately one hour. Metabolism occurs in the liver, with renal excretion being the primary route of elimination. The pharmacokinetic profile may vary based on the specific formulation used in combination with antibiotics.

Contra-indications

• History of hypersensitivity to clavulanic acid, penicillins or any of the components
• Severe hepatic impairment

Adverse effects

• Nausea
• Diarrhea
• Rash
• Hepatotoxicity
• Allergic reactions
• Superinfection due to resistant organisms

Interactions

• May increase the anticoagulant effect of warfarin
• Probenecid may increase plasma concentrations
• May reduce the efficacy of oral contraceptives

Precautions

• Use with caution in patients with a history of liver disease
• Monitor for signs of anaphylaxis in patients with a history of allergies
• Caution in patients with renal impairment

Pregnancy

Clavulanate is generally considered safe for use during pregnancy, but should be used only if clearly needed.

Breast-feeding

Clavulanate is excreted in breast milk, caution should be exercised when administered to nursing mothers.

Storage

Store in a cool, dry place below 25°C, protect from light.

Formulations

• Oral 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.