๐ About
Always check the BNF or equivalent for prescribing advice.
- ๐ Penicillin was the first antibiotic, discovered by Alexander Fleming in 1928.
He observed that the mould Penicillium notatum inhibited growth of Staphylococcus aureus in culture.
- โ๏ธ Its clinical development was advanced in the 1940s, revolutionising treatment of bacterial infections.
- ๐ Remains a cornerstone of antimicrobial therapy despite increasing resistance.
โก Mechanism of Action
- ๐ช Bactericidal: inhibits bacterial cell wall synthesis.
- Blocks formation of peptidoglycan cross-links in the bacterial cell wall.
- Contain a beta-lactam ring, which is vulnerable to hydrolysis by bacterial beta-lactamases.
๐ Notes
- ๐ Clavulanic acid is a beta-lactamase inhibitor โ protects penicillins against resistant organisms (e.g. co-amoxiclav).
- ๐ Different classes: narrow-spectrum (benzylpenicillin), broad-spectrum (ampicillin, amoxicillin), anti-staphylococcal (flucloxacillin), and anti-pseudomonal (piperacillin-tazobactam).
๐ฉบ Indications
- Refer to the BNF for up-to-date prescribing indications (e.g. pneumonia, cellulitis, endocarditis, syphilis).
๐ Interactions
- ๐ Ampicillin/amoxicillin may reduce efficacy of the oral contraceptive pill (OCP) (advise extra precautions).
- โฌ๏ธ Probenecid inhibits renal excretion โ doubles serum penicillin levels (sometimes used therapeutically).
- โฌ๏ธ Increased methotrexate toxicity (reduced clearance).
โ ๏ธ Cautions
- Consult the BNF for detailed cautionary advice.
- ๐ Dose adjustment required in renal impairment.
- ๐งช Beware in patients with a history of severe allergy or asthma (higher risk of hypersensitivity).
๐ฝ Excretion
- Undergo enterohepatic recirculation and renal clearance.
- Primarily excreted by active tubular secretion in the kidneys.
- ๐ Probenecid blocks this process โ prolongs serum half-life.
๐ซ Contraindications
- โ ๏ธ Known hypersensitivity to penicillins (risk of anaphylaxis).
- Refer to the BNF for full list.
๐ฅ Side Effects
- ๐ซ Acute anaphylaxis: rare (~5 per 10,000 patients) but potentially fatal.
- ๐ก๏ธ Rashes โ including maculopapular rash with ampicillin/amoxicillin in EBV or CLL.
- ๐ฉธ Haematological: haemolytic anaemia, thrombocytopenia, neutropenia.
- ๐ฉบ Renal: interstitial nephritis.
- ๐ง Neurotoxicity: convulsions at high IV/intrathecal doses.
- ๐ Cross-sensitivity with cephalosporins (~10%).