Antibiotics and Antivirals Flashcards
What is meant by
a) Bacteriostatic
b) Bacteriocidal
a) Inhibits bacterial growth/replication
b) Kills the bacteria
In the gram-stain what colour are organisms that are
a) gram +ve
b) gram -ve
c) Have thick peptidoglycan wall
a) Purple
b) Pink
c) Purple (gram +ve)
What is the mechanism of action of the Beta-lactams e.g. penicillin, cephalosporins, carbapenems
Inhibition of peptidoglycan synthesis by irreversibly binding to the enzyme (penicillin binding proteins) that catalyses the crosslinking of peptidoglycan subunits
Ie prevents cell wall synthesis
What is the mechanism of action of vancomycin?
Disruption of peptidoglycan cross-linkage by binding to peptidoglycan monomers (n-acetylmuramic acid)
What is the mechanism of action of bacitracin?
Disrupts lipid carrier require for glycan transport across the bacterial cell membrane
Which drugs work by altering the cell/plasma membrane, causing depolarisation of the cell and leakage of its contents?
- Polymyxins (B+E)
- Daptomycin
Which drugs act on the 30s ribosome site to prevent protein synthesis and what actions do they inhibit?
Tetracyclines - entry of incoming acetyl tRNA
Aminoglycosides e.g. gentamycin - correct reading of mRNA
Which drugs act on the 50s ribosome site to prevent protein synthesis and what actions do they inhibit?
Macrolides e.g. erythromycin - Translocation
Chloramphenicol - Transpeptidation
Clindamycin - Translocation
What do Quinalones (e.g. Ciprofloxacin) effect?
DNA
They inhibit DNA gyrases or topoisomerases required for supercoiling of DNA
What does Metronidazole effect?
DNA
Cause inhibition of DNA replication, loss of DNA helical structure and fragmentation of existing DNA and mutates bacterial genome
What does Rifampicin effect?
RNA (transcription)
Binds to RNA polymerase
What pathway is a target for the drugs sulphonamides, trimethoprim and dapsone?
Folate synthesis leading to the synthesis of DNA
What is the MOA of sulphonamides in the folic acid pathway?
Prevent PABA being converted to dihydrofolic acid by dihydropterote synthetase - enzyme not active in humans
What is the MOA of trimethoprim?
Inhibits dihydrofolate
What is MRSA treated with?
- Vancomycin
- Teicoplanin
- Linezolid (inhibit protein synthesis)
What are the mechanisms bacteria have adopted to prevent the action of antibiotics (ie resistance)?
- Efflux of antibiotic - reverse transport systems in the membrane e.g. tetracycline transported out
- Enzyme modification
- Enzyme degredation - e.g. penicillinases cleave beta-lactam ring on penicillin
What is the acquired resistance mechanism ‘Vertical gene transfer’?
Spontanous mutation causing resistance genes which are transferred directly to all bacteria progeny during DNA replication
What are the 3 forms of horizontal gene transfer?
1) Conjugation - direct cell to cell contact transferring plasmids
2) Transformation - DNA taken up from external environment
3) Transduction - Bacteriophages transfer DNA
What antibiotics are contraindicated in pts with liver disease?
- Tetracyclines (can cause jaundice, fever and fatty liver)
- Macrolides e.g. erythromycin (bile retention and jaundice)
- Metronidazole (metabolised in liver by p450 so half life and clearance prolonged and adverse reaction)
What is the safest antibiotic to use in pts with liver disease?
Penicillin
What antibiotics are contraindicated in pts with kidney disease?
- Tetracycline
- Reduce dose of amoxicillin and erythromycin
What antibiotics are contraindicated in pts with glandular fever/infectious mononucleosis?
Ampicillin and amoxicillin as they cause rashes
What antibiotics are contraindicated in pts with lymphocytic leukaemia?
Ampicillin and amoxicillin as they cause rashes
What antibiotics are contraindicated in pts with pre-existing diarrhoea?
Clindamycin and co-amoxiclav
Which antibiotic is the safest option for pregnancy and breastfeeding?
Amoxicillin
erythromycin also safe
What is the advice on metronidazole and pregnancy / breast feeding?
- High doses are contraindicated
- Avoid in women at risk of pre-term labour
What is the advice on clindamycin and pregnancy / breastfeeding?
Caution in breast feeding as risk of diarrhoea, candidiasis and colitis in newborns
What is the advice on co-amoxiclav and pregnancy / breastfeeding?
Avoid in women at risk of preterm labour as risk of necrotising enterocolitis
What is the advice on tetracycline and pregnancy / breastfeeding?
- Avoid in pregnancy
- Risk of neural tube defects, clefts, cardiovascular defects, discolouration of dental tissues
What antibiotics should be avoided if a patient has anaphylactoid reactions to penicillin?
Cephalosporins (have beta-lactam ring)
What is the major adverse effect pseudomembranous colitis? What antibiotic especially causes this?
- Inflammation of the colon associated with C.diff. Severe = toxic megacolon
- Clindamycin
What drug is the most common cause of the major adverse effect idiosyncratic liver damage?
Co-amox, and has been reported for amoxicillin
What drug can cause the major adverse effect hypokalaemia and what do its symptoms include?
- Penicillin
- Weakness, constipation, cardiac arrhythmias, leg cramps etc
What drug is used to improve compliance in alcohol dependent patients?
Disulfiram
What antibiotic is it advised against consuming alcohol whilst taking and after 48 hours of stopping treatment due to nausea, vomiting and tachycardia effects?
Metronidazole
Which antibiotics have drug interactions with anti-metabolite drugs?
Penicillin and tetracyclines
Which antibiotic reacts with allopurinol used for gout causing skin rashes?
Amoxicillin
Which antibiotics will increase the effect of warfarin and cause greater risk of bleeding?
Erythromycin, penicillin, metronidazole
In what situation is Amoxicillin the first choice for treatment?
- For dento-alveolar infections and to limit the spread of infection
- Prior to implants or extraction of those at risk of osteoradionecrosis
In what situation is Metronidazole the first choice for treatment?
- Necrotising periodontal disease and pericoronitis
- In penicillin allergies
- Adjunct to amoxicillin for dento-alveolar infection (extends spectrum of activity to anaerobes)
Why is clindamycin more appropriate than erythromycin as a second line drug?
Some bacteria have developed resistance to erythromycin and has increased adverse effects
A patient you are treating has the following symptoms: - Elevated temperature - Evidence of systemic spread - Local lymph gland involvement They have an acute dento-alveolar infection / peridontal abscess. What antibiotics do you prescribed a) First line? b) Second line?
a) Amoxicillin 500mg TDS 5 days
If penicillin allergy: Metronidazole 400mg TDS 3 days or Clindamycin 150-300mg QDS 5 days
b) Co-amoxiclav 500/125mg TDS 5 days or Clindamycin 150-300mg QDS 5 days
A patient you are treating has pericoronitis which you have irrigated but they have an elevated temperature and evidence of systemic spread. What do you prescribe:
a) First line?
b) Second line?
a) Metronidazole 400mg TDS 3 days
b) Amoxicillin 500mg TDS 3 days or clindamycin 150-300mg QDS 7 days
A patient you are treating has necrotising ulcerative gingivitis which you have provided scaling and OHI. What would you prescribe:
a) First line?
b) Second line?
a) Metronidazole 400mg TDS 3 days
b) Amoxicillin 500mg TDS 3 days or Clindamycin QDS 7 days
A patient you are treating has sinusitis which is prolonged and severe. What would you prescribe:
a) First line?
b) Second line?
c) Third line?
a) Amoxicillin 500mg TDS 5 days and Ephedrine Hydrochloride 0.5% nasal drops QDS 7 days. Review healing after 2 weeks
b) Doxycycline first day 200mg OD then 100mg OD 6 days
c) Co-amoxiclav 500/125mg TDS 5 days
A patient you are treating has oral antral communication/ fistula. What would you prescribe:
a) First line?
b) Second line?
c) Third line?
a) Amoxicillin 500mg TDS 5 days and Ephedrine Hydrochloride 0.5% nasal drops QDS 7 days. Review healing after 2 weeks
b) Doxycycline first day 200mg OD then 100mg OD 6 days
c) Co-amoxiclav 500/125mg TDS 5 days
A patient you are treating needs antibiotic cover due to head and neck radiotherapy/ immunosupression. What would you prescribe:
a) First line pre op and post op?
b) Second line pre op and post op?
a) Pre op = Amoxicillin 3g 1 hr before and chlorhexidine 0.2% 10ml rinse pre XLA
Post op = Amoxicillin 500mg TDS 7 days and chlorhexidine 0.2% rinse twice daily for 2 weeks
b) Pre op = Clindamycin 600mg 1 hr before and chlorhexidine 0.2% pre XLA
Post op = Clindamycin 150mg QDS 7 days and chlorhexidine rinse twice daily for 2 weeks
What dental conditions are antibiotics not appropriate for?
- Early pericoronitis
- Post op oedema
- Fibrinolytic conditions e.g. alveolar osteitis
- Non-bacterial infections e.g. fungal and viral
Why are antibiotics given 1 hr before surgery?
Blood clots impenetrable by antibiotics 3hrs after formation
What type of antiviral agents are anti-herpetic agents predominantly?
Nucleoside analogues
What is Aciclovir? How does it work?
- Analogue of guanosine
- Transformed into active state by viral enzymes
- Incorporates into viral DNA to inhibit DNA synthesis
For Aciclovir:
a) What is its half life?
b) Why can it be used for viral encephalitis?
c) Where is it excreted?
d) How is it administered?
a) 2.5 hrs
b) Crosses the blood brain barrier
c) Kidneys
d) Topical or IV
What is Idoxuridine?
How does it work?
How is it administered?
- Antiviral that is a thymidine analogue
- Phosphorylated in cells and incorporated intp cellular and viral DNA
- Mainly used against DNA viruses
- Too toxic for systemic use so only used topically
What is Zidovudine (AZT) and what is it used against?
- Thymidine analogue
- HIV-1
For Zidovudine (antiviral):
a) What is the MOA?
b) What drugs have a synergistic effect?
c) How is it administered?
a) Inhibits viral RNA-dependent DNA polymerase so stops growing strand of DNA
b) Aciclovir and interferon
c) Orally or IV
What are the unwanted effects of the antiviral Zidovudine?
- Anaemia
- Granulocytopenia (fewer cells)
- Must do regular blood count every 2 weeks
What are non-nucleoside analogues used to treat? Name the drugs.
- AIDS
- Nevirapine and Delavirdine
What are the antiviral interferons and what do they do?
- Group of cytokines (alpha, beta, gamma) and are glycoproteins produced by the body in response to a virus
- Enhance the cytotoxic capacity of T-lymphocytes
What are the 3 antibiotics that inhibit cell wall synthesis?
Beta lactams (penicillin, cephalosporin, carbapenems)
Vancomycin
Bacitracin
Name 2 diseases caused by prions
Bovine spongiform encephalitis (cattle) /BSE
Creutzfeldt-Jakob disease (CJD)