Anti-parasitic + viral Flashcards
Primaquine
Anti-malarial
Inhibits polymerisation in the food vacuous for hemozoin production, or acts to complex with heme - ROS generation and increase pH of vacuole reducing metabolism
Quinine
Anti-malarial
Inhibits polymerisation in the food vacuous for hemozoin production, or acts to complex with heme - ROS generation and increase pH of vacuole reducing metabolism
Artemisinin
Anti-malarial
Rapid but short action
Mechanism uncertain - creates ROS through peroxide bridge, inhibits electron transport chain, inhibits SERCA pumps (Ca2+) in cell signalling, inhibits development of oocyst and phosphatidiyinositol 3 kinase
Sulfadoxin
Anti-malarial
Inhibits DHPS and hence folic acid synthesis
Used in combination with pyrimethamine in Fansidar
Pyrimethamine
Anti-Malarial
Inhibits DHFR therefore folic acid synthesis
Used in combination with Sulfadoxin in Fansidar
Fansidar
Anti-Malarial
Combination of Sulfadoxin and pyrimethamine in the inhibition of folic acid synthesis
Particularly useful against Plasmodium Falciparum
Proguanil
Prodrug converted into cycloguanil
Anti-Malarial
Inhibits DHFR therefore folic acid synthesis
Used prophylacticaly
Melarsoprol
Prodrug from Merlarsen Oxide
Anti-trypanosome
Inhibits enzymes required in glycolysis and citrus acid cycle - Pyruvate dehydrogenase, Pyruvate kinase, and phosphofructokinase
Arsenic compound - reacts with thick groups forming covalent bonds between sulphur atoms
Accumulates within trypanosomes
Suramin
Anti-trypanosome
Non-arsenic compound therefore higher therapeutic index
Only effective in first stage of infection - cannot cross blood brain barrier
Inhibits glycolysis enzymes preventing metabolism
Amphotericin B
Anti-Lesihmania
Targets ergosterol in cell membrane increasing membrane permeability
Miconazole
Anti-Leishmania
Targets ergosterol synthesis - inhibiting it
Oseltamivir
Prodrug for Zanamivir - must be cleaved by esterases in the gut
Analogue of N-Acetlyneuramic acid
Competitively inhibits neuraminisdase hence causes viral aggregation and prevents the release of new viral particles
Zanamivir
Analogue of N-Acetlyneuramic acid
Competitively inhibits neuraminisdase hence causes viral aggregation and prevents the release of new viral particles
Amantidine
Anti-influenza
Inhibits M2 Proton - (stabilises the closed state) channels on viral envelope
Protons required to trigger viral replication and allow HA conformational change for release into cytoplasm
Also inhibits HA production at higher conc.
Rimantidine
Anti-influenza
Inhibits M2 Proton - (stabilises the closed state) channels on viral envelope
Protons required to trigger viral replication and allow HA conformational change for release into cytoplasm
Also inhibits HA production at higher conc.
Aciclovir
Anti-herpes drug
Mono phosphorylation by virally encoded thymidine kinase, then converted to triphosphate by cellular kinases
Competitively inhibits viral DNA polymerase and acts as a chain terminator
Trifluridine
Anti-Herpes
Pyrimidine analogue
More toxic than aciclovir - only topical use
Monophosphorylated by cellular kinases therefore not specific
Inhibit DNA polymerase
Idoxuridine
Anti-herpes
Pyrimidine analogue
Only for topical use and non selective for Viral or Mammalian DNA polymerase
Enfuvirtide
Anti-HIV
Fusion inhibitor
Binds to alpha helices of Gp120 and prevents contraction required to bring to two membranes together
Nevirapine
Anti-HIV
Non-nucleoside inhibitor of reverse transcriptase
Binds near the enzymes catalytic site and prevents action
Zidovudine (AZT)
Anti-HIV
Nucleotide inhibitor of reverse transcriptase
Thymidine analogue - mimics nucleotides within cell
Also acts as chain terminator
Protease inhibitors
These act to inhibit the HIV protease a required to cleave gag proteins for their functional use, the professes contain two aspartyl residues
Interferon a2A
Anti-Hepatitis B
Initiates anti-viral response: protein kinase activation to prevent ribosome initiation complex formation, endonuceleases to cleave DNA
Can cause flu-like symptoms, severe fatigue and infertility
Also used against herpes
Interferon a2B
Anti-Hepatitis C
Initiates anti-viral response: protein kinase activation to prevent ribosome initiation complex formation, endonuceleases to cleave DNA
Can cause flu-like symptoms, severe fatigue and infertility
Also used against herpes
