Antimicrobials Flashcards
Penicillin
Binds to transpeptidases involved in the synthesis of cell-wall peptidoglycans in gram-positive bacteria.
Can be degraded by β-lactamases secreted by bacteria
Penicillin-like drugs include amoxicillin and ampicillin.
Cephalosporins are another class of β-lactams.
Tetracycline
Used against gram-negative bacteria.
Binds 70S bacterial ribosomes - able to bind RNA and protein sites on the 30S subunit.
Other compounds targeting bacterial ribosomes include aminoglycosides (streptomycin), chloramphenicol, and macrolides (erythromycin).
Quinolones: levofloxacin, ciprofloxacin
Used against gram-negative bacteria.
DNA gyrase (topoisomerase II) and topoisomerase IV inhibitors - prevent DNA transcription, replication and repair.
Quorum-sensing pathways
Quorum sensing is involved in bacterial communication for biofilm and colony formation.
Potential target to combat antibiotic resistance.
Pore forming peptides
Form a membrane attack complex and cause cell lysis.
As bacterial membranes differ from human ones, these can be specifically targeted.
Bacteriophages
Potential treatment of bacterial infections.
HIV treatment: enfuvirtide, fostemsavir
CD4 attachment inhibitors - prevent entry into host cells
HIV treatment: Maraviroc
CCR5 inhibitor - prevents entry into host cells
Reverse transcriptase inhibitors
Used against retroviruses, prevent conversion of viral RNA into DNA.
Can be nucleosides, nucleotides or non-nucleotides.
HIV protease inhibitors
Ritonavir and Saquinavir
Ritonavir can also be used for SARS-CoV-2
HIV integrase inhibitors
Raltegravir, Dolutegravir, Elvitegravir
SARS-CoV-2 treatment: Sotrovimab
ACE2 receptor inhibitor
Blocks viral entry into host cells
SARS-CoV-2 treatment: molnupiravir, remdesevir
RNA replication inhibitors
SARS-CoV-2 protease inhibitors
Paxlovid and the HIV inhibitor Ritonavir
Quinine
Malaria treatment
Interferes with Plasmodium’s ability to use haemoglobin
Inhibits purine nucleoside phosphorylase, resulting in deficient RNA, DNA and protein biosynthesis
