Anti Protozoal /malaria

Question 1

What does distributional selectivity mean

Answer 1

Where the drug is directed/administered to into a limited compartment concentrated with parasite

Question 2

Why are protozoan plasmodium hard to target

Answer 2

Eukaryotic

Question 3

What causes malarial symptoms like fever pain

Answer 3

Rbc lysis

Question 4

What are the 4 types of plasmodium

Answer 4

Falciparum

Virax

Ovale

Malarie

Question 5

Which plasmodium takes shortest time (6 days) to infect

Answer 5

Falciparum

Question 6

Which 2 plasmodium exist as hypnozoites in liver

Answer 6

Virax and ovale

Question 7

Who is the definitive host for plasmodium (sexual reproduction)

Answer 7

Female mosquito

Question 8

What are injected into our blood from mosquito saliva and where do they go

Answer 8

Sporozoites

Enter blood to the liver

Question 9

After replication in liver what is released to go to the rbc

Answer 9

Merozoites

Question 10

What is the stage in the liver called

Answer 10

Exo erythrocytic cycle

Question 11

Once merozoites penetrate rbc, what are they called

Answer 11

TrophoZoites

Question 12

What are trophozoites whixh then lay dormant in liver called

Answer 12

Hypnozoites (ovale and virax)

Question 13

Name some things which trophozoites do in asexual reproduction in the rbc

Answer 13

Digest AA, Hb for energy

Convert heme to hemeozoin (less toxic for them)

Question 14

Trophozoites which are released from burst rbc are called merozoites again. What do they develop into

Answer 14

Gametocytes

Which then infect next mosquito in blood

Question 15

What are the 4 targets in life cycle

Answer 15

Exo erythrocytic cycle

Erythrocytic cycle

Link between liver and rbc

Gametocytes infecting a new mosquito

Question 16

What are drugs called which act on exo erythrocytic cycle and which parasites do they work best on

Answer 16

radical cure

Work best on hypnozoites eg virax or ovale

Question 17

What is a clinical cure

Answer 17

Works on erythrocytic cycle for ones which don’t reproduce in the liver

Question 18

What do prophylaxis treatment do

Answer 18

Stop the transfer between liver and rbc

Question 19

What are 4 amino quinolones and give example

Answer 19

Drugs which target clinical and prophylaxis (erythrocytic forms)

Chloroquine example

Question 20

What 2 effects do 4 amino quinolones have eg chloroquine

Answer 20

Stop Hb digestion in RBCs to stop energy transfer

Stop production of hemeozoin from toxic heme

Question 21

Which enzyme does chloroquine (4amino quinolones) inhibit to stop production of hemeozoin

Answer 21

Heme polymerase

Question 22

What are the good things about chloroquine (4 amino quinolone)

Answer 22

Well absorbed

Long t1/2

Question 23

How do chloroquines stay in the parasite to block heme polymerase and digestion of Hb

Answer 23

Get ionised by acid in the parasitic lysosomes

Question 24

What is an issue with chloroquine 4 amino quinolone for clinical cure

Answer 24

Parasites become resistant due to efflux of drug

Question 25

Which types of drugs are quinine methanols

Answer 25

Also clinical / prophylaxis

Question 26

Give 2 examples of quinine methanols which target erythrocytic forms (clinical)

Answer 26

Quinine Mefloquine

Question 27

Which 2 effects does quinine methanols like quinine have on erythrocytic forms

Answer 27

Bind to their dna to prevent rep Block heme polymerase forming hemeozoin

Question 28

What is a disadvantage to quinine compared to chloroquine

Answer 28

Quinine has shorter half life

Question 29

Which Quinine methanol has longest half life

Answer 29

Mefloquine

Question 30

What are the side effects of Quinine methanols eg quinine

Answer 30

Cns effects like delerious or headache

Question 31

What do 8 amino quinolones target

Answer 31

Exo erythrocytic stages / radical cure/ hypnozoites eg ovale or virax

Question 32

Which 2 types of cells do 8 amino quinolone skill

Answer 32

Hypnozoites and gametocytes

Question 33

What is produced by pro drugs 8 amino quinolones when metabolised in liver which is cytotoxic to host

Answer 33

Quinolone

Question 34

What does metabolism of 8 amino quinolones cause in people with a G6PDH deficiency

Answer 34

Haemolysis of rbc

Question 35

Which ADME negative do 8 amino quinolone have

Answer 35

Short t1/2

Question 36

How do 8 amino quinolone a work for radical / exo erythrocytic cure

Answer 36

Produce ROS which stops dna synthesis and also mt disruption of energy

Question 37

What type of drugs are anti folates and give example

Answer 37

Prophylaxis Proguanil

Question 38

Which metabolic enzyme activated proguanil prodrug

Answer 38

Cyp 2c19

Question 39

Which enzyme does anti folate proguanil inhibit (type II anti folate)

Answer 39

Dihydrofolate reductase

Question 40

How have parasites become resistant to anti folates like proguanil

Answer 40

Mutation to their dihydrofolate reductase enzyme

Question 41

What can anti folates type II like proguanil be given with to stop full dna synthesis

Answer 41

Type I eg sulphonamides

Question 42

What is the other prophylaxis drug apart from anti folates

Answer 42

Hydroxynapthoquinone

Question 43

How does hydroxynapthoquinone work

Answer 43

Disrupts ETC to stop getting mt energy Looks like ubiquinol

Question 44

What is hydroxynapthoquinone given with for synergistic reasons and to stop resistance

Answer 44

Proguanil anti folate

Question 45

Which mutation acquired by parasites causes its resistance to hydroxynapthoquinone

Answer 45

Cyt BC1 complex in mitochondria

Question 46

What are given with anti malarial drugs to stop resistance and enhance their ADME

Answer 46

Artemisin (ACTs)

Question 47

Which 4 mutations have given malarial parasites resistance

Answer 47

Falciparum transporter gene Falciparum Na/H exchanger gene Dihydrofolate reductase (stop anti folates) Cyt BC1 complex (stops hydroxynapthoquinone)

Question 48

Which antigen on falciparum is used to detect type

Answer 48

HRP 2

Question 49

Which other 2 other than falciparum HRP2 antigen is used for diagnostic

Answer 49

Aldolase Lactate dehydrogenase