Drugs: Anti-malaria, Anti-protozoal, Anti-Helminths

Question 1

Chloroqiune
(Hydroxychloroqione)
MOA

Answer 1

Anti-Malaria: Prevents heme polymerization to hemozoin leading to malaria and RBC lysis via oxidative damage

Question 2

Chloroqiune
(Hydroxychloroqione)
Used For

Answer 2

Anti-Malaria Prophlyaxis, Autoimmune disorders

Amebiasis

Question 3

Chloroqiune
(Hydroxychloroqione)
Resistance

Answer 3

Common in P. falciparum

Increasing in P. vivax -> adminster with Verapamil or Despiramine to prevent drug efflux!

Question 4

Chloroqiune
(Hydroxychloroqione)
Interactions

Answer 4

CYP450 2D6 inhibitor

Question 5

Chloroqiune
(Hydroxychloroqione)
Adverse Rxns

Answer 5

GI, Rash, Pruritis, Exfoliatve dermatitis

Ototoxicty
Retinopathy
Neuropathy

Hemolysis (G6PD)

Question 6

Quinine
Quinidine
MOA

Answer 6

Anti-Malaria: Rapdily acting blood schiontocide, blooks DNA replication and RNA tx

Question 7

Quinine
Quinidine
Used For

Answer 7

1 Anti-Malaria for Severe falciparum malaria, can use with doxy of clinadmycin to shorten therpay

Question 8

Quinine
Quinidine
Adverse Rxns

Answer 8

** “Cinchonsim” - tinnitus, headache, dizziness, flushing, visual disturbances
**Hypersensitivity rxn
Hematologic abnormalities
**Hemolysis->Anemia (G6PD)
Thrombophlebitis, EKG changes, hypotension with IV administration

Question 9

Mefloquin MOA

Answer 9

Anti-Malaria: Induces distruption of Ca2+ homeostasis

Question 10

Mefloquin Used For

Answer 10

Anti-Malaria Prophylaxis in Chloroquine resistant area

Question 11

Mefloquin Adverse Rxns

Answer 11

GI
 Sleep disturbance,
 Neurospychiatric seizure
 Rash
** QT PROLONGATION

Question 12

Primaquine MOA

Answer 12

Anti-Malaria: oxidzes GSH->GSSG make cell more susceptible to oxidative damage

Question 13

Primaquine Activity

Answer 13

Tissue schizonticide
Gametocide
Dormant hynozoite (vixax, ovale)

Question 14

Primaquine Used For

Answer 14

vivax and ovale endemic areas
** ERADICATION OF DORMANT LIVER FORMS
Relapse prevention and limits transmission

Question 15

Primaquine Adverse Rxns

Answer 15

Contraindicated in Pregnancy!!!!!!

• Leukopenia
• Hemolytic anemia (G6PD)

Question 16

Sulfadoxine and Pyrimethamine MOA

Answer 16

Anti-Malaria (anti-metabolite): Inhibits dihydropteroate reductase and tetrahydrofolate reductase.
SLOW acting, Blood schizonticide

Question 17

Sulfadoxine and Pyrimethamine Used For

Answer 17

prophylaxis
rx falciparum
AND Toxoplasmosis

Question 18

Sulfadoxine and Pyrimethamine Adverse Rxns

Answer 18

• Bone marrow suppression
  Stevens Johnsons
  CNS, GI, Renal toxicity
• REVERSIBLE MEGALOBLASTIC ANEMIA (Pyrimethamine)

Question 19

Doxycycline MOA

Answer 19

Abx and Anti-Malaria: Protein synthesis inhibitor (30s ribo subunit)

Question 20

Doxycycline Used For

Answer 20

Malaria Porphylaxis in highly resistant areas

Question 21

Doxycycline Adverse Rxns

Answer 21

GI

*Photosensitivity

Question 22

Atovaquone MOA

Answer 22

Anti-Malaria: Disrupts mitochondrial electron transport

Question 23

Artemisinin Uses

Answer 23

MOA: Free radical killing
Use: * Severe MDR (multi drug resistant) falci
AE: QT prolongation

Question 24

Metronadizole MOA

Answer 24

Anti-Protozoal: forms reactive cytotoxic products to interfere with pathogen’s energy metabolic pathways

Question 25

Metronadizole Activity

Answer 25

Tissue amebicide against trophozoites (not cysts)

Question 26

Matronadizole Uses

Answer 26

Amebiasi, Giardia, Trichomonas

Question 27

Metronadizole Adverse Rxns

Answer 27

*ALCOHOL (disulfiram-like rxn) | Nausea, Headache, CNS toxicity

Question 28

Emetine Dehydroemitine MOA

Answer 28

Anti-Amebicide: Irreversible protein synthesis inhibitors (trophozoites)

Question 29

Emetine Dehydroemitine Uses

Answer 29

Back up for very severe Amebiasis

Question 30

Emetine Dehydroemitine Adverse Rxns

Answer 30

NVD, Weakness * CARDIAC ARRHYTHMIA * Heart failure, hypotension * ONLY available at CDC bc of HIGH TOXICITY

Question 31

Chlorquine MOA

Answer 31

Amebicide: Irreversible protein synthesis inhibitor. works in tissue (concentrates in liver)

Question 32

Chlorquine Uses

Answer 32

``` Extraluminal Amebiasis (after metronadizole) Given with luminal agent (Diloxanide furoate or Iodouinol) ```

Question 33

Diloxanide furoate MOA

Answer 33

Luminal Amebicide: Inhibits protein synthesis

Question 34

Iodoquinol MOA

Answer 34

Luminal Amebicide: Mutagenic activity to inihbit amebic growth. 90% NOT absorbed in GI

Question 35

Iodoquinol Adverse Rxns

Answer 35

Diarrhea * *Iodine toxicity - >limit by taking with food

Question 36

Pentamidine MOA

Answer 36

Anti-Protozoal: Protein synthesis inhibitor (does NOT cross BBB)

Question 37

Pentamidine Uses

Answer 37

** T. cruzi, Leichmaniasis Pneumocystis

Question 38

Pentamidine Adverse Rxns

Answer 38

``` Hypotension Arrhythmias Pancreatitis Hypoglycemia Nephtotoxicity Electrolyte abormalities ```

Question 39

Melarsoprol MOA

Answer 39

Anti-Protozoal: Prevents ATP synthesis (& crosses BBB)

Question 40

Melarsoprol Uses

Answer 40

* trypanosomiasis cruzi, especially CNS disease

Question 41

Melarsoprol Adverse Rxns

Answer 41

Fever, GI, Arthralgia, cardiac effects Enchepalopathy Nephrotoxicity Hypersensitivity

Question 42

Nifurtimox MOA

Answer 42

Anti-Protozoal: inhibits trypanothione reductase (essential for thiol metabolism)

Question 43

Nifurtimox Uses

Answer 43

** Drug of choice for: African and American Trypanosomiasis

Question 44

Albendazole/Mebenazole MOA

Answer 44

(luminal) Binds to beta tubulin to prevent polymerization of microtubules, and inhibits glucose uptake by wormsn

Question 45

Albendazole/Mebenazole Uses

Answer 45

* *Nematode treatment (hydatid disease, neurocysticercosis). * *Thiabendazole (systemic) or Ivermectin used for Strongyloides.

Question 46

Albendazole/Mebenazole Adverse Rxns

Answer 46

well tolerated. Albendazole may cause long term GI problems, alopecia, elevated LFTS. (Thiabenazole is not well tolerated)

Question 47

Pyrantel Pamoate MOA

Answer 47

(luminal) depolarizes NMJ -> AchR always on = Spastic paralysis

Question 48

Pyrantel Pamoate Uses

Answer 48

Nematode treatment. NOT effective for cestodes or trematodes.

Question 49

Diethylcarbamazine MOA

Answer 49

(systemic) Immobilizes microfilariae and alters surface structure displacing them from tissues and making them more susceptible to host defenses

Question 50

Diethylcarbamazine Uses

Answer 50

(Wuchereria bancrofti) Lymphatic Filariasis

Question 51

Diethylcarbamazine Adverse Rxns

Answer 51

Headache, weakness, dizziness RXN TO DYING WORMS (min with steroids, antihistamines) Fever, rash, GI, pain, proteinuria, retinal hemorrhage, encepalopathy

Question 52

Ivermectin MOA

Answer 52

(systemic) Tonic paralysis of nematodes and arthropods by intensifying GABA-mediated transmission of signals in peripheral nerves

Question 53

Ivermectin Uses

Answer 53

Strongyloides (threadworm) (dog heart worm medication)

Question 54

Ivermectin Adverse Rxns

Answer 54

MAZZOTTI RXN= Reactions due to dying worms. Fever, headache, dizziness.

Question 55

Praziquantel MOA

Answer 55

(systemic) Spastic paralysis by increasing the permeability of trematode and cestode cell membranes to calcium.

Question 56

Praziquantel Uses

Answer 56

Flukes (schistomiasis) and cestodes

Question 57

Praziquantel Adverse Rxns

Answer 57

Due to dying worms-> Rash, fever, eosinophilia Don’t use for Ocular cysticerosis bc of potential for irreversible damage

Question 58

Niclosamine MOA

Answer 58

(luminal) Depletes ATP in worms, possibly by interfering with oxidative phosphoylation

Question 59

Niclosamine Uses

Answer 59

Second line for tapeworms

Question 60

Niclosamine Adverse Rxns

Answer 60

Avoid alcohol (minimal absoprotion, not available in the US)

Question 61

Oxamniquine MOA/Use

Answer 61

paralysis (moa unknwn), Effective only for Schistosoma mansoni, all stages of disease

Question 62

Sodium Stibogluconate

Answer 62

** Drug of choice for: Leishmaniasis (ROS and NOS dependent killing of parasite)