Cell Wall Synthesis Inhibitors Flashcards
Penicillin types?
Benzylpenicillin, Cloxacillin,
Amoxicillin, Ampicillin
Penicillin SOA?
Covers most gram positives
– Spectrum: Amoxicillin > Cloxacillin > Penicillin
Penicillin ROA?
Benzylpenicillin (IV), Penicillin V (oral)
Amox vs Amp?
Amoxicillin > Ampicillin in terms of oral
bioavailability due to acid stability
Penicillin Pharmacokinetics?
Pharmacokinetics: Wide distribution except to CSF
Minimal Hepatic metabolism
Penicillin mechanism?
- Bacteriostatic: Inhibit transpeptidase thereby inhibiting the crosslinking of the peptidoglycan in cell wall synthesis
- Bactericidal: Activation of murein hydrolase leading to autolysis of the cell with degradation of the peptidoglycans in the cell wall
Penicillin Side Effects & Contraindications?
- Allergy (Rash & Fever)
- Neurotoxicity (rare): Convulsion, Hallucination, Confusion
- aaPMC due to broad spectrum activity
Cephalosporins drugs?
Cefalexin, Cefuroxime,
Ceftriaxone, Cefepime
Cephalosporins ROA?
IV or IM preparations for 3rd gen beyond
Cephalosporins Pharmacokinetics?
Wide distribution and beyond 3rd Gen can penetrate CSF well
Minimal hepatic metabolism
Cephalosporins Mechanisms?
- Same as Penicillin
* Resistance evolving due to extended spectrum β lactamases
Cephalosporins Side Effects & Contraindications?
- Allergy (Rash & Fever) with crossreactivity with Penicillin
- GIT disturbances with dhiarrhoea
- Thrombophlebitis
- (Ceftriaxone) Forms precipitates in lung and kidney when given with calcium containing agents
Carbapenems drugs?
Imipenem, Meropenem
Carbapenems SOA?
Broad spectrum as it is even able to penetrate the membrane of even gram negatives
Carbapenems Pharmacokinetics?
Pharmacokinetics: Poor oral bioavailability (mainly IV & IM),
Imipenem is broken down in the renal tubules (increase half life by giving with cilastin)
Carbapenems Side Effects & Contraindications?
- Allergy (Rash & Fever)
- GIT Toxicity
- Neurotoxicity when overdosed
Monobactams drugs?
Aztreonam
Why are monobactams safe?
High therapeutic index with low potential toxicity
Monobactams Pharmacokinetics?
Pharmokinetics: Only given IV, minimal hepatic
metabolism, 60-70% renal excretion
Monobactams MOA?
- Same as penicillin
* Minimal crossreactivity with penicillin
Monobactams Side Effects & Contraindications?
- Allergy (Rash & Fever)
- Transaminaemia
- GIT disturbances
Vancomycin Spectrum?
Active only against Gram Positives
-Used for clostridium difficile infection in gut
Vancomycin Pharmacokinetics?
Given IV with wide distribution (but not CSF), mostly excreted at the kidneys
Vancomycin MOA?
• Bind to D-Ala-D-Ala terminal residue on
transpeptidase and prevents both the further synthesis of peptidoglycan and crosslinking
• Rare resistance due to mutations to
transpeptidase (VRSA, VRE)
Vancomycin Side Effects & Contraindications?
• Allergy: Red Man Syndrome with a characteristic rash above the nipple line due to histamine release
especially with rapid infusions
- Nephrotoxicity & Ototoxicity especially upon interaction with other agents such as loop diuretics, aminoglycosides, amphotericin B
- Thrombophlebitis
Polymyxin ROA?
Parenteral or Topical preparations
Polymyxin MOA?
Binds to LPS in the cell wall and causes detergent like damage
Polymyxin Side Effects & Contraindications?
Nephrotoxicity