Antimalarial and Anti Parasitic

Question 1

4-aminoquinolone derivative that prevents polymerizarion of the hemoglobin breakdown product heme into hemozoin

Drug of choice for P falciparum (chloroquine sensitive)

Heme accumulation is toxic to parasite

Blood schizonticide

Answer 1

Chloroquine

GI upset
Rash
Headache

Question 2

Chloroquine resistance is brought about by

Answer 2

Decreased intracellular accumulation via increased activity of membrane transporters

Decreased accumulation of chloroquine via a transporter encoded by the pfcrt gene (chloroquine-resistance transporter gene)

Question 3

Complexes with double stranded DNA to prevent strand separation resulting in blockade of DNA replication and transcription to RNA

Drug of choice for chloroquine resistant malaria

Solely a schizonticide

Answer 3

Quinine

Question 4

Rare and fatal complication in quinine-sensitized persons

Blood lysis -> hemoglobinuria -> fatal

Contraindicated in pregnancy

Answer 4

Blackwater fever

Question 5

Forms quinoline-quinone metabolites which are electron-transferring redox compounds that act as cellular oxidants

Tissue schizonticide and limits transmission by acting as a gametocide

Active against liver forms of P vivax and ovale

Answer 5

Primaquine

Also PCP

Question 6

Metabolism to toxic free radicals in protozoa

Blood schizonticide

Answer 6

Artemisinins

GI upset

Question 7

Disrupts mitochondrial metabolism

For falciparum

Answer 7

Atovaquone

Alternative for PCP

Fever
Rash
GI upset

Question 8

Can cause blood cytopenias

Hemolysis in G6PD deficiency

Answer 8

Primaquine

Question 9

Inhibits folate synthesis

Mostly blood schizonticides

Answer 9

Antifolates
Pyrimethamine
Proguanil
Fansidar (Pyrimethamine + Sulfadoxine)

GI upset
Rashes (sometime severe severe)
Cytopenias

Question 10

Undergoes a reductive bioactivation of its nitro group by ferredoxin (present in anaerobic parasites) to form reactive cytotoxic products

E hystolitica
Giardiasis
Trichomonas vaginalis 
Gardnerella vaginalis
Bacteroides fragilis
C difficile

Answer 10

Metronidazole

Question 11

Drug of choice for trichomonas

Giardiasis, Gardnerella vaginalis, Anaerobic bacteria (B fragilis, C difficle)
H. pylori

Answer 11

Metronidazole

Question 12

Amebiasis

trophozoites
cyst

Answer 12

Metronidazole

Diloxanide - luminal

Question 13

Giardiasis

Answer 13

Metronidazole

Question 14

Trichomoniasis

Answer 14

Metronidazole

treat both partners

Question 15

Pneumocystis

Answer 15

TMP-SMX

Question 16

Toxoplasmosis

Answer 16

Pyrimethamine-Sulfadiazine

If with HIV TMP-SMX

Question 17

Leishmania

Answer 17

Stibogluconate

Question 18

Trypanosome

Answer 18

Nifurtimox - Chagas

Suramin - African

Question 19

Crosses CNS and placenta
For acute attacks of malaria
Because of antiinflammatory effect, it is sometimes used in autoimmune disease

Answer 19

Chloroquine

Question 20

Chloroquine SE

Answer 20

Low dose: GI, headache, rash

High dose: Retinal damage, neuropathies, myocardial depression, psychosis, hearing loss

Long term: discoloration of mucous membrane, hemolytic anemia in G6PD

Question 21

Quinine SE

Answer 21

Cinchonism
Hemolytic anemia G6PD
Blackwater fever

Question 22

MOA unknown

Excreted in feces

Used in prophylaxis and treatment of chloroquine-resistant P falciparum

May cause seizures, hallucinations, depression at high doses

Answer 22

Mefloquine

Question 23

(Pyrimethamine) Dihydrofolate reductase inhibitor
For chloroquine-resistant species

Drug of choice for toxoplasmosis

Answer 23

Pyrimethamine-Sulfadoxine (Fansidar)

Question 24

Forms redox compounds acting as cellular oxidants

Used for relapsing malaria -> eradicates liver stages of P vivax and ovale

Answer 24

Primaquine

Question 25

Primaquine SE

Answer 25

Hemolytic anemia G6PD Granulocytopenia Headache Methemoglobinemia

Question 26

Drug of choice for toxoplasmosis

Answer 26

Pyrimethamine with sulfadiazine with folinic acid

Question 27

From infected sandflies Leishmaniasis Kala azar

Answer 27

Sodium stibogluconate

Question 28

Inhibits PFK reaction of glycolysis Monitor renal and hepatic function Adverse effect: Arrythmia

Answer 28

Sodium stibogluconate

Question 29

Prophlaxis and treatment of African sleeping sickness without CNS involvement Kerandel’s sign

Answer 29

Suramin

Question 30

Drug of choice for African sleeping sickness with CNS involvement

Answer 30

Melarsoprol

Question 31

Drug of choice for hemolymphatic stages of African Sleeping Sickness Kerandel’s sign

Answer 31

Pentamidine

Question 32

Drug of choice for American sleeping sickness Chagas Chagoma Romana’s sign

Answer 32

Nifurtimox

Question 33

Metronidazole SE

Answer 33

``` Disulfiram-like reactions with alcohol Metallic taste Potentiation of Warfarin’s effect Nausea and vomiting Urine discoloration Oral candidias CNS disturbance - dizziness, vertigo, numbness, paresthesia Contraindicated in pregnancy ```

Question 34

H pylori triple treatment

Answer 34

Clarithromycin + Metronidazole/Amoxicillin + PPI

Question 35

Drug of choice for asymptomatic cyst shedders ameba | Contrandicated in pregnant women and those <2

Answer 35

Diloxanide furoate Iodoquinol tetracycline emetine dehydroemetine chloroquine

Question 36

Drug of choice for pinworm (enterobius) and whipworm (trichiuris), hookworm (necator) Effective against round worm (ascaris) Teratogenic Mild SE: nausea and vomiting

Answer 36

Mebendazole

Question 37

Drug of choice for ascaris and hookworm (necator) Depolarizing neuromuscular blockade -> paralyzes the worm

Answer 37

Pyrantel pamoate

Question 38

For threadworm (Strongyloides stercoralis) May cause tingling, numbness, diarrhea, nausea and SJS

Answer 38

Thiabendazole

Question 39

For cysticercosis, hydatid cyst, cutaneous larva migrans Inhibits uptake of glucose

Answer 39

Albendazole

Question 40

Inhibits microtubule synthesis and glucose uptake in nematodes

Answer 40

Mebendazole

Question 41

Drug of choice for filariasis caused by Wuchereria bancrofti Unknown MOA

Answer 41

Diethylcarbamazine

Question 42

``` Dying microfilariae Pruritus Lymphadenopathy Hypotension Tachycardia ``` In treatment of Wuchereria and onchocerca

Answer 42

Mazzotti reaction

Question 43

Drug of choice for onchocerca volvulus, threadworm (strongyloides) Intensifies GABA transmission -> paralysis of worm

Answer 43

Ivermectin

Question 44

For schistosomiasis Increases permeability to calcium -> tetanic contraction of nematode

Answer 44

Praziquantel

Question 45

Drug of choice for tapeworm (cestode) infection Inhibits mitochondrial anaerobic phosphorylation of adenosine diphosphate within cestodes

Answer 45

Niclosamide

Question 46

Treats river blindness | Oncocerca volvulus

Answer 46

Ivermectin