Anti-parasitic + viral

Question 1

Primaquine

Answer 1

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

Question 2

Quinine

Answer 2

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

Question 3

Artemisinin

Answer 3

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

Question 4

Sulfadoxin

Answer 4

Anti-malarial
Inhibits DHPS and hence folic acid synthesis
Used in combination with pyrimethamine in Fansidar

Question 5

Pyrimethamine

Answer 5

Anti-Malarial
Inhibits DHFR therefore folic acid synthesis
Used in combination with Sulfadoxin in Fansidar

Question 6

Fansidar

Answer 6

Anti-Malarial
Combination of Sulfadoxin and pyrimethamine in the inhibition of folic acid synthesis
Particularly useful against Plasmodium Falciparum

Question 7

Proguanil

Answer 7

Prodrug converted into cycloguanil
Anti-Malarial
Inhibits DHFR therefore folic acid synthesis
Used prophylacticaly

Question 8

Melarsoprol

Answer 8

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

Question 9

Suramin

Answer 9

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

Question 10

Amphotericin B

Answer 10

Anti-Lesihmania

Targets ergosterol in cell membrane increasing membrane permeability

Question 11

Miconazole

Answer 11

Anti-Leishmania

Targets ergosterol synthesis - inhibiting it

Question 12

Oseltamivir

Answer 12

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

Question 13

Zanamivir

Answer 13

Analogue of N-Acetlyneuramic acid

Competitively inhibits neuraminisdase hence causes viral aggregation and prevents the release of new viral particles

Question 14

Amantidine

Answer 14

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.

Question 15

Rimantidine

Answer 15

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.

Question 16

Aciclovir

Answer 16

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

Question 17

Trifluridine

Answer 17

Anti-Herpes
Pyrimidine analogue
More toxic than aciclovir - only topical use
Monophosphorylated by cellular kinases therefore not specific
Inhibit DNA polymerase

Question 18

Idoxuridine

Answer 18

Anti-herpes
Pyrimidine analogue
Only for topical use and non selective for Viral or Mammalian DNA polymerase

Question 19

Enfuvirtide

Answer 19

Anti-HIV
Fusion inhibitor
Binds to alpha helices of Gp120 and prevents contraction required to bring to two membranes together

Question 20

Nevirapine

Answer 20

Anti-HIV
Non-nucleoside inhibitor of reverse transcriptase
Binds near the enzymes catalytic site and prevents action

Question 21

Zidovudine (AZT)

Answer 21

Anti-HIV
Nucleotide inhibitor of reverse transcriptase
Thymidine analogue - mimics nucleotides within cell
Also acts as chain terminator

Question 22

Protease inhibitors

Answer 22

These act to inhibit the HIV protease a required to cleave gag proteins for their functional use, the professes contain two aspartyl residues

Question 23

Interferon a2A

Answer 23

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

Question 24

Interferon a2B

Answer 24

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

Question 25

Chloroquine

Answer 25

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

Question 26

Maravioc

Answer 26

Anti-HIV fusion inhibitor, targets and binds co-receptor CCR5 and prevents GP120 interaction

Question 27

Enfuviritide

Answer 27

Anti-HIV fusion inhibitor, interacts with GP41 on HIV envelope and inhibits its function to penetrate the host membrane