Antibiotics Flashcards
Penicillin - Example
- benzylpenicillin
- phenoxymethylpenicillin
Penicillin - Indication
- Streptococcal Infections: tonsilitis, pneumonia, endocarditiis , skin/soft tissue infections
- Meningococcal infection: meningitis and septicaemia
- Clostridial infection such as tetanus
Is penicillin narrow or broad spectrum?
Narrow
Penicillin - MOA
Penicillin act by inhibiting the peptidoglycans in the bacterial cell wall which weakens the cell walls. They cannot maintain an osmotic gradient and this leads to uncontrolled entry of water. The cells begin to swell and eventually lysing and dying.
What gives Penicillin it’s antibiotic properties?
Penicillin contains a B-lactam ring which is responsible for their bacteriacidal activity.
What do side chains on B-lactam ring do?
The side chains can be linked to the B-lactam ring and influence the nature of the antibiotic determining the antibacterial spectrum and other properties of the drug.
How do bacteria resist Penicillin?
bacteria resist the action of penicillin by synthesising B-lactamases which break down the B-lactam ring and thus
What are side effects of Penicillin?
- Penicillin allergy = presents as a skin rash 7-10 days after first exposure and 1-2days after repeat exposure
- Less common : anaphylactic reaction- Characterised by hypotension, bronchial and laryngeal spasm/oedema and angioedema.
- Central nervous system toxicity which usually happens in high doses of penicillin or where severe renal impairment delays excretion = pt usually has convulusions or coma
What are the contraindications of Penicillin?
- a history of penicillin allergy
2. renal impairment - reduced dose required because other can lead to a delay in excretion leading to toxicity.
What are the interactions of Penicillin?
reduces renal excretion of methotrexate increasing the risk of toxicity.
Broad spectrum penicillin - Examples
Amoxicillin and co-amoxiclav.
Broad spectrum penicillin - Indication
- Susceptible infections such as
- community acquired pneumonia
- otitis media
- UTIs
- sinusitis - H.Pylori associated peptic ulcers
- Severe-resistant hospital acquired infections - usually co-amoxiclav
Broad spectrum penicillin- MOA
How does it differ to other kinds of penicillin?
Some MOA of weakening bacterial cell wall leading to cell swelling and lysis of the bacteria. Bactericidal properties brought about by the B-lactam ring.
They way it differs is that it’s synthesised with additional amino group to the B-lactam ring side chain ehich broadens the activity against aerobic Gram negative bacteria
Broad spectrum penicillins - Side Effects
- GI upset including nausea and diarrhoea
- penicillin allergy which usually presents as a skin rash or can lead to delayed or immediate IgE-mediated anaphylactic reaction
- Acute liver injury/jaundice or hepatitis may develop during or shortly after co-amoxiclav and is usually self-limiting once the Tx is stopped.
- less commonly antibiotic-associated colitis
Broad spectrum penicillins - Contraindication
- History of allergy
- pt in risk of C.difficile infection - hospitalised pts and elderly
- penicillin associated liver injury
- severe renal impairment - dose should be reduced (risk of crystalluria)
Broad spectrum penicillins - Interaction
They can enhance to anticoagulant effect of warfarin by killing normal gut flora that synthesise vitamin K
Macrolides - Examples
- clarithromycin
- erythromycin
- azithromycin
Macrolides - Indications
- Respiratory, skin and soft tissue infections = usually as an alternative to penicillin
- Severe pneumonia - added to penicillin to cover atypical pathogens such as legionella pneumophila and mycoplasma pneumoniae.
- H.Pylori eradication Tx in combination with PPI and either amoxicillin and metronidazole
Macrolides - Spectrum of activity
erythromycin is relatively broad spectrum active against gram-positive and some gram-negative pathogens
synthetic macrolides such as clarithromycin and azithromycin have increased activity against gram-negative pathogens particularly haemophilus influenzae
Macrolides - MOA
Type of Abx
Macrolides inhibit bacterial protein synthesis. They do this by binding to the 50S subunit of the bacterial ribosome blocking translocation (needed to elongate polypeptide/protein).
it is a bacteriostatic antibiotic = prevents the growth/multiplication of bacteria thus providing the immune system with more time to kill and remove bacteria.
Macrolide - Side Effects
most common and severe in eythromycin
side effects:
1. irritant causing nausea, vomiting, abdo pain and diarrhoea and also thrombophlebitis when given via IV.
- allergy
- antibiotic associated coiltis
- liver abnormalities such as cholestatic jaundice
- prolongation of QT interval thus predisposing arrythmias
- ototoxicity at high doses
Macrolide - Contraindication /Caution
- History of hypersensitivity/allergy
- severe hepatic impairment
- severe renal impairment
Macrolide - Interaction
- Macrolide inhibit CYP enzymes : increases conc of drugs metabolised by them