Download Overview of Anti-microbials

Overview of Anti-microbials and Target Site of Activity
22/8/10
Yung, A. et al (2004) “Infectious Disease: A Clinical Approach” Second Edition, IP
Communications Ltd
Anti-microbial = kill or suppress the growth of micro-organisms.
ANTI-BACTERIALS
(i) Inhibition of cell wall synthesis
- Beta-lactams (penicillins, cephalosporins, carbapenems, monobactams)
- Glycopeptides (vancomycin, teicoplanin)
- Others (cycloserine, bacitracin)
(ii) Inhibition of protein synthesis
-
Macrolides (ethyromycin, roxithromycin, azithromycin)
Aminoglycosides (gentamycin, tobramycin)
Tetracyclines (doxycycline)
Chloramphenicol
Clindamycin
Fusidic acid
(iii) Inhibition of nucleic acid synthesis
-
Trimethoprim
Sulphonamides (sulphamethoxazole)
Fluoroquinolones (ciprofloxacin, norfloxacin)
Rifamycins (rifamipicin)
(iv) Inhibitors of cell membrane function
- Colistin
ANTI-VIRALS
- are all virustatic rather than virucidal
- they all suppress virus and allow the host immune system to irradicate disease
- majority = nucleoside analogues -> gain access to the infected cell and then are
phosphorylated by viral and/or cellular enzymes.
(1) Drugs for HSV and VZV – inhibition of DNA polymerase
- Acyclovir
- Famciclovir
- Valaciclovir
(2) Drugs for CMV
- Ganciclovir – inhibition of CMV DNA polymerase
Jeremy Fernando (2011)
- Foscarnet – inihibitor of virion DNA polymerase
- Cidofovir
- Formivirsen – antisense oligonucleotide that inhibits CMV replication
(3) Drugs for HIV
HAART = highly active anti-retroviral therapy
- Nucleoside reverse transcriptase inhibitors (NRTI’s - zidovudine, didanosine, stavudine,
lamivudine)
- Nucleotide reverse transcriptase inhibitors (RTI’s - tenofovir)
- Non-nucleoside reverse transcriptase inhibitors (NNRTI’s – nevirapine, efavirenz)
- Protease inhibitors (PI’s - saquinavir, ritonavir, indanvir, nelfinavir, amprenavir, lopinavir)
- Others (enfuvirtide)
(4) Drugs for Influenza
- M2 Channel Inhibitors (amantadine and rimantadine) – disrupts the process of dissociation
of matrix and ribonucleoprotein
- Neuraminidase inhibitors (oseltamivir and zanamivir) – impairs release of virus from infected
cells
(5) Drugs for other viruses
- Ribavirin – mechanism uncertain
- Alpha-interferon – very complex
- Pleconaril – prevent virus binding and viral uncoating
ANTI-FUNGALS
(i) Interference with ergosterol (sterol in fungal cell membrane)
- Azoles (ketoconazole, fluconazole, itraconazole, voriconazole)
- Allylamines (terbinafine)
(ii) Disruption of fungal cell wall
- Polyenes (amphotericin B, nystatin)
- Echinocandins (caspofungin, micafungin)
ANTI-PARASITICS
Protozoan Parasites
Nitroimidazoles – inhibiting DNA synthesis
- metronidazole
- tinidazole
Other agents:
- Paromomycin
- Nitazoxanide
Jeremy Fernando (2011)
Metazoan Parasites (nematodes and cestodes = worms)
Benzimidzoles – prevents formation of microtubules and cell division
- albendazole
- mebendazole
Diethylcarbamazine – mechanism unknown
Praziquantel – mechanism unknown
Ivermectin – causes influx of Cl- into cells -> muscular paralysis
Jeremy Fernando (2011)