SKYCLAV 625MG TABLETS

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
• Intra-abdominal infections

Dosage

Children: Refer to the BNF for Children for appropriate dosing information, as it varies depending on the specific clinical scenario and age of the child.

Adults: Refer to the specific combination product's dosing guidelines, as doses often vary depending on the co-administered antibiotic.

Mechanism of action

Clavulanate works by irreversibly binding to the active site of beta-lactamase enzymes, which are produced by certain bacteria to confer resistance against beta-lactam antibiotics. By inhibiting these enzymes, clavulanate allows the co-administered antibiotic, such as amoxicillin, to retain its antibacterial properties, thereby increasing its effectiveness in treating infections caused by resistant organisms.

Pharmacodynamics

Clavulanate exhibits pharmacodynamic properties that are primarily based on its ability to inhibit beta-lactamase enzymes. The combination of clavulanate with a penicillin enhances the spectrum of activity of the penicillin against beta-lactamase-producing bacteria. The efficacy of this combination is particularly important in treating infections where resistant strains are prevalent.

Pharmacokinetics

Clavulanate is rapidly absorbed from the gastrointestinal tract and reaches peak plasma concentrations within one hour post-administration. It is primarily excreted by the kidneys, with about 60-70% of an oral dose being eliminated unchanged in the urine. The half-life of clavulanate is approximately 1 hour. It is also noted that clavulanate is not extensively metabolized in the liver, which is significant for its safety profile.

Contra-indications

• Hypersensitivity to clavulanate or any component of the formulation
• Severe hepatic impairment
• History of cholestatic jaundice or hepatic dysfunction associated with amoxicillin-clavulanate

Adverse effects

• Nausea
• Vomiting
• Diarrhea
• Rash
• Allergic reactions
• Hepatic enzyme elevation
• Clostridium difficile-associated diarrhea

Interactions

• Probenecid may increase the serum concentration of clavulanate
• Antibiotics may affect the efficacy of oral contraceptives
• May enhance the anticoagulant effect of warfarin

Precautions

• Use with caution in patients with renal impairment
• Monitor liver function in patients with a history of liver disease
• Caution in patients with a history of allergic reactions

Pregnancy

Clavulanate is classified as category B; animal studies have not demonstrated risk to the fetus, but caution is advised when prescribing during pregnancy.

Breast-feeding

Clavulanate is excreted in breast milk, and caution is advised when administered to nursing mothers as effects on the infant are unknown.

Storage

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

Formulations

• Tablets
• Oral suspension
• Injectable forms

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.