PED1003/L23 Selective Toxicity & Antibiotics Flashcards
How do bacteriostatic drugs affect the number of total and viable cells?
Stops changes in both
Why has the number of new antibiotics reaching the market dropped dramatically in the last 10 years? (3)
Resistance reduces effective life of a product
Too little profit
Government restrictions
Lack of new biological targets
How do bacteriolytic drugs affect the number of total and viable cells?
Decrease both
How do bacteriocidal drugs affect the number of total and viable cells?
Drop in viable cells
Total cells remain the same
Give 3 common bacterial targets.
Cell membrane
Cell wall
Protein synthesis
RNA polymerase
DNA synthesis
Folate metabolism
Describe the structure of a B-lactam ring.
Cyclic amide with heteroatomic ring structure consisting of 3 carbon atoms and 1 nitrogen atom
Describe early penicillins. (3)
Acid labile
Not well-absorbed via oral route
Parenteral route - slow IV, high availability
Narrow spectrum of activity - Gram +ves and few Gram -ves
What did the amino group in penicillin facilitate?
Penetration of outer membrane of Gram -ve bacteria
How do B-lactam antibiotics work? (3)
Inhibit transpeptidases responsible for creating cross-linkage of peptidoglycan cell wall
Bacteria swell and rupture
Only effective against multiplying organisms
Which 2 amino acids are joined in a transpeptidation reaction?
Lys - Gly
Describe the absorption of penicillin. (2)
Varies orally
Delayed release preparations available
Describe the distribution of penicillin. (3)
Widely distributed throughout
Concentrations in tissues and body fluids vary
Do not normally enter CSF
What is the half-life of penicillin?
30-80 mins
Describe the excretion of penicillin. (3)
Mainly through kidney with 90% excreted by tubular secretion
Clearance reduced in neonates
Reduce excretion rate by use of probenecid which inhibits tubular secretion
Give 2 adverse reactions to penicillin.
Hypersensitivity
GIT disturbance
Haemostatic effect
Which 2 enzymes are involved in folate biosynthesis?
Dihydropteroate synthetase
Dihydrofolate reductase
Give the intermediates in folate biosynthesis. (5)
pABA
Folate
Tetrahydrofolate
Synthesis of thymidylate
DNA