Drugs: Anti-malaria, Anti-protozoal, Anti-Helminths Flashcards
Chloroqiune
(Hydroxychloroqione)
MOA
Anti-Malaria: Prevents heme polymerization to hemozoin leading to malaria and RBC lysis via oxidative damage
Chloroqiune
(Hydroxychloroqione)
Used For
Anti-Malaria Prophlyaxis, Autoimmune disorders
Amebiasis
Chloroqiune
(Hydroxychloroqione)
Resistance
Common in P. falciparum
Increasing in P. vivax -> adminster with Verapamil or Despiramine to prevent drug efflux!
Chloroqiune
(Hydroxychloroqione)
Interactions
CYP450 2D6 inhibitor
Chloroqiune
(Hydroxychloroqione)
Adverse Rxns
GI, Rash, Pruritis, Exfoliatve dermatitis
Ototoxicty
Retinopathy
Neuropathy
Hemolysis (G6PD)
Quinine
Quinidine
MOA
Anti-Malaria: Rapdily acting blood schiontocide, blooks DNA replication and RNA tx
Quinine
Quinidine
Used For
1 Anti-Malaria for Severe falciparum malaria, can use with doxy of clinadmycin to shorten therpay
Quinine
Quinidine
Adverse Rxns
** “Cinchonsim” - tinnitus, headache, dizziness, flushing, visual disturbances
**Hypersensitivity rxn
Hematologic abnormalities
**Hemolysis->Anemia (G6PD)
Thrombophlebitis, EKG changes, hypotension with IV administration
Mefloquin MOA
Anti-Malaria: Induces distruption of Ca2+ homeostasis
Mefloquin Used For
Anti-Malaria Prophylaxis in Chloroquine resistant area
Mefloquin Adverse Rxns
GI Sleep disturbance, Neurospychiatric seizure Rash ** QT PROLONGATION
Primaquine MOA
Anti-Malaria: oxidzes GSH->GSSG make cell more susceptible to oxidative damage
Primaquine Activity
Tissue schizonticide
Gametocide
Dormant hynozoite (vixax, ovale)
Primaquine Used For
vivax and ovale endemic areas
** ERADICATION OF DORMANT LIVER FORMS
Relapse prevention and limits transmission
Primaquine Adverse Rxns
Contraindicated in Pregnancy!!!!!!
- Leukopenia
- Hemolytic anemia (G6PD)
Sulfadoxine and Pyrimethamine MOA
Anti-Malaria (anti-metabolite): Inhibits dihydropteroate reductase and tetrahydrofolate reductase.
SLOW acting, Blood schizonticide
Sulfadoxine and Pyrimethamine Used For
prophylaxis
rx falciparum
AND Toxoplasmosis
Sulfadoxine and Pyrimethamine Adverse Rxns
- Bone marrow suppression
Stevens Johnsons
CNS, GI, Renal toxicity - REVERSIBLE MEGALOBLASTIC ANEMIA (Pyrimethamine)
Doxycycline MOA
Abx and Anti-Malaria: Protein synthesis inhibitor (30s ribo subunit)
Doxycycline Used For
Malaria Porphylaxis in highly resistant areas
Doxycycline Adverse Rxns
GI
*Photosensitivity
Atovaquone MOA
Anti-Malaria: Disrupts mitochondrial electron transport
Artemisinin Uses
MOA: Free radical killing
Use: * Severe MDR (multi drug resistant) falci
AE: QT prolongation
Metronadizole MOA
Anti-Protozoal: forms reactive cytotoxic products to interfere with pathogen’s energy metabolic pathways
Metronadizole Activity
Tissue amebicide against trophozoites (not cysts)
Matronadizole Uses
Amebiasi, Giardia, Trichomonas
Metronadizole Adverse Rxns
*ALCOHOL (disulfiram-like rxn)
Nausea, Headache, CNS toxicity
Emetine
Dehydroemitine
MOA
Anti-Amebicide: Irreversible protein synthesis inhibitors (trophozoites)
Emetine
Dehydroemitine
Uses
Back up for very severe Amebiasis
Emetine
Dehydroemitine
Adverse Rxns
NVD, Weakness
- CARDIAC ARRHYTHMIA
- Heart failure, hypotension
- ONLY available at CDC bc of HIGH TOXICITY
Chlorquine MOA
Amebicide: Irreversible protein synthesis inhibitor. works in tissue (concentrates in liver)
Chlorquine Uses
Extraluminal Amebiasis (after metronadizole) Given with luminal agent (Diloxanide furoate or Iodouinol)
Diloxanide furoate MOA
Luminal Amebicide: Inhibits protein synthesis
Iodoquinol MOA
Luminal Amebicide: Mutagenic activity to inihbit amebic growth. 90% NOT absorbed in GI
Iodoquinol Adverse Rxns
Diarrhea
- *Iodine toxicity
- > limit by taking with food
Pentamidine MOA
Anti-Protozoal: Protein synthesis inhibitor (does NOT cross BBB)
Pentamidine Uses
** T. cruzi, Leichmaniasis Pneumocystis
Pentamidine Adverse Rxns
Hypotension Arrhythmias Pancreatitis Hypoglycemia Nephtotoxicity Electrolyte abormalities
Melarsoprol MOA
Anti-Protozoal: Prevents ATP synthesis (& crosses BBB)
Melarsoprol Uses
- trypanosomiasis cruzi, especially CNS disease
Melarsoprol Adverse Rxns
Fever, GI, Arthralgia, cardiac effects
Enchepalopathy
Nephrotoxicity
Hypersensitivity
Nifurtimox MOA
Anti-Protozoal: inhibits trypanothione reductase (essential for thiol metabolism)
Nifurtimox Uses
** Drug of choice for: African and American Trypanosomiasis
Albendazole/Mebenazole MOA
(luminal) Binds to beta tubulin to prevent polymerization of microtubules, and inhibits glucose uptake by wormsn
Albendazole/Mebenazole Uses
- *Nematode treatment (hydatid disease, neurocysticercosis).
- *Thiabendazole (systemic) or Ivermectin used for Strongyloides.
Albendazole/Mebenazole Adverse Rxns
well tolerated. Albendazole may cause long term GI problems, alopecia, elevated LFTS. (Thiabenazole is not well tolerated)
Pyrantel Pamoate MOA
(luminal) depolarizes NMJ -> AchR always on = Spastic paralysis
Pyrantel Pamoate Uses
Nematode treatment. NOT effective for cestodes or trematodes.
Diethylcarbamazine MOA
(systemic) Immobilizes microfilariae and alters surface structure displacing them from tissues and making them more susceptible to host defenses
Diethylcarbamazine Uses
(Wuchereria bancrofti) Lymphatic Filariasis
Diethylcarbamazine Adverse Rxns
Headache, weakness, dizziness RXN TO DYING WORMS (min with steroids, antihistamines) Fever, rash, GI, pain, proteinuria, retinal hemorrhage, encepalopathy
Ivermectin MOA
(systemic) Tonic paralysis of nematodes and arthropods by intensifying GABA-mediated transmission of signals in peripheral nerves
Ivermectin Uses
Strongyloides (threadworm) (dog heart worm medication)
Ivermectin Adverse Rxns
MAZZOTTI RXN= Reactions due to dying worms. Fever, headache, dizziness.
Praziquantel MOA
(systemic) Spastic paralysis by increasing the permeability of trematode and cestode cell membranes to calcium.
Praziquantel Uses
Flukes (schistomiasis) and cestodes
Praziquantel Adverse Rxns
Due to dying worms-> Rash, fever, eosinophilia Don’t use for Ocular cysticerosis bc of potential for irreversible damage
Niclosamine MOA
(luminal) Depletes ATP in worms, possibly by interfering with oxidative phosphoylation
Niclosamine Uses
Second line for tapeworms
Niclosamine Adverse Rxns
Avoid alcohol (minimal absoprotion, not available in the US)
Oxamniquine MOA/Use
paralysis (moa unknwn), Effective only for Schistosoma mansoni, all stages of disease
Sodium Stibogluconate
** Drug of choice for: Leishmaniasis (ROS and NOS dependent killing of parasite)