AMOKLAVIN 1.2 INJ

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 resistant to penicillins alone
• Sinusitis
• Pneumonia
• Urinary tract infections
• Skin and soft tissue infections

Dosage

Children: Refer to the BNF for Children for appropriate dosing in paediatric populations, as dosing may vary significantly based on age, weight, and clinical condition.

Adults: Refer to the specific product information for adult dosing recommendations, as it varies based on the formulation and the infection being treated.

Mechanism of action

Potassium clavulanate binds to and irreversibly inhibits various types of beta-lactamase enzymes produced by certain bacteria. By inhibiting these enzymes, it protects other beta-lactam antibiotics from being broken down, thus enhancing their antibacterial activity.

Pharmacodynamics

Potassium clavulanate exhibits bactericidal effects in combination with penicillins against susceptible strains of bacteria. It does not have significant antibacterial activity on its own but plays a crucial role in overcoming antibiotic resistance in bacteria that produce beta-lactamase.

Pharmacokinetics

Potassium clavulanate is absorbed well from the gastrointestinal tract, with peak plasma concentrations occurring within 1 to 2 hours after oral administration. It is widely distributed in body tissues and fluids. The elimination half-life is approximately 1 hour, primarily excreted unchanged in the urine. The drug's pharmacokinetics may be affected by renal function, necessitating dosage adjustments in patients with impaired renal clearance.

Contra-indications

• Hypersensitivity to potassium clavulanate or any component of the formulation
• Severe liver dysfunction or jaundice related to previous use of beta-lactam antibiotics

Adverse effects

• Diarrhea
• Nausea
• Vomiting
• Rash
• Hepatic dysfunction
• Allergic reactions including anaphylaxis
• Superinfection due to overgrowth of non-susceptible organisms

Interactions

• May interact with anticoagulants, increasing the risk of bleeding
• May reduce the efficacy of oral contraceptives
• Probenecid may increase the serum concentration of beta-lactam antibiotics

Precautions

• Use with caution in patients with a history of liver disease
• Monitor for signs of an allergic reaction
• Assess renal function in patients with renal impairment
• Caution in patients with a history of gastrointestinal disease, particularly colitis

Pregnancy

Potassium clavulanate is categorized as pregnancy category B. Animal studies have not demonstrated a risk to the fetus, but there are no adequate and well-controlled studies in pregnant women. Use only if clearly needed.

Breast-feeding

Potassium clavulanate is excreted in breast milk. Caution is advised when administering to nursing mothers, particularly if the infant is premature or has a medical condition.

Storage

Store at room temperature, away from moisture and heat. Keep out of reach of children.

Formulations

• Oral tablets
• Oral suspension
• Injectable formulations

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.