Antibiotics Flashcards
(135 cards)
Name two penicillin antibiotics? - actual penicillin e.g. not amoxicillin
- Benzylpenicillin (Penicillin G)
2. Phenoxymethylpenicillin (Penicillin V)
What is the mechanism of action of penicillins?
Penicillins inhibit the enzymes responsible for cross-linking peptidoglycans in bacterial cell walls. This weakens cell walls, preventing them from maintaining an osmotic gradient. Uncontrolled entry of water into bacteria causes cell swelling, lysis and death.
What is the significance of the beta-lactam ring in penicillins?
Beta-lactam rings are responsible for antimicrobial activity. Side chains attached to the beta-lactam ring can be modified to make semi-synthetic penicillins. The nature of the side chain determines the antimicrobial spectrum and other properties of the drug.
How does bacterial resistance to beta-lactams occur?
Bacteria resist the actions of penicillins by making beta-lactamase, an enzyme which breaks the beta-lactam ring and prevents antimicrobial activity. Other mechanisms of resistance include limiting the intracellular concentration of penicillin (reduced bacterial permeability or increased extrusion) or changes in the target enzyme to prevent penicillin binding.
What percentage of people have a penicillin allergy?
1-10%
On first exposure, how does a penicillin allergy present?
Skin rash, 7-10 days after first exposure
What are the indications for use of penicillin V / penicillin G?
Streptococcal infections;
1. Tonsillitis
2. Pneumonia (in combination with a macrolide if severe)
3. Endocarditis
4. In combination with flucloxacillin for severe skin and soft tissue infections
Clostridium perfringens infections e.g. gas gangrene
Meningococcal infections:
1. Meningitis
2. Septicaemia
Which immunoglobulin is involved in the more common, less severe penicillin reaction, which can appear 1-2 days on repeat exposure?
IgG
In more severe penicillin allergies, which immunoglobulin is involved, and what kind of reaction is it? (this applies to all penicillins)
IgE-mediated anaphylactic reaction- this can be life threatening, occurring within minutes to hours, with hypotension, bronchial and laryngeal spasm/oedema and angioedema.
What can occur with high doses of penicillin or when severe renal impairment may delay excretion of penicillin?
Central nervous system toxicity (including convulsions and coma)
What is the obvious contraindication for use of penicillin?
Penicillin allergy
When should a reduced dose of penicillin be used? (this applies to all penicillins)
In someone with renal impairment
Penicillins reduce the excretion of which drug (often used to treat RA), increasing the risk of toxicity?
Methotrexate
Benzylpenicillin can only be administered via which routes?
IV or IM (as gastric acid prevents GI absorption)
Name the antipseudomonal penicillin?
Piperacillin with tazobactam = Tazocin
What are antipseudomonal penicillins reserved for (1) and in what conditions are they used? (3)
Antipseudomonal penicillins are reserved for severe infections, particularly where there is:
- a broad spectrum of potential pathogens (including Pseudomonas aeruginosa) OR
- antibiotic resistance is likely OR
- patients are immunocompromised
Which clinical infections are treated by piperacillin with tazobactam (Tazocin)? (4 - broad areas of infection)
- Lower respiratory tract infection
- Urinary tract infection
- Intra-abdominal sepsis
- Skin and soft tissue infection
How has the beta-lactam side chain been modified to form piperacillin?
The side chain of broad-spectrum penicillins has been converted to a form of urea. This longer side chain may improve affinity to penicillin binding proteins, increasing the spectrum of antimicrobial activity to include Pseudomonas aeruginosa.
Why is tazobactam combined with piperacillin?
Tazobactam is a beta-lactamase inhibitor, so confers antimicrobial activity against beta-lactamase-producing bacteria e.g. staph aureus, and gram-negative anaerobes.
What is the common possible side effect caused by Tazocin?
GI upset; nausea and diarrhoea are common
Less frequently, what side effects an occur from using Tazocin?
Antibiotic-associated colitis can occur (when broad-spectrum antibiotics kill normal GI flora, allowing overgrowth of toxin-producing C.diff).
What are the warnings (2)/contraindications (1) associated with using Tazocin?
- Use in caution with people at risk of C.diff infection
- Use in caution/reduced dose in patients with moderate/severe renal impairment
- Contraindicated in penicillin allergy
As with other penicillins, which drug do they reduce the renal excretion of?
Methotrexate
Antipseudomonal penicillins enhance the anticoagulant effect of which drug, and how?
Warfarin, by killing normal GI flora that synthesises vitamin K.