Antifungal, Antiprotozoal, Antihelminthic Agents

Why is drug selectivity hard with fungal infections?

fungi re eukaryotes with membrane bund organelles and nucleus similar to humans

What are the general considerations of anti fungal treatment?

fungi are slow growing, must be on treatment for prolonged period

fungi are similar to humans, increased toxicity risk

antifungals are poorly soluble, hard to distribute

What is ergosterol?

part of plasma membrane of fungi

What is the MOA of azoles? (Fluconazole, Clotrimazole, Miconazole)

inhibit ergosterol synthesis by inhibiting fungal CYP450

What is the downside to using an -azole?

can affect human CYP450 and cause DDI

Are azoles fungistatic or fungicidal?

fungistatic

What does Fluconazole (Difucan) treat?

thrush

What are side effects of Clotrimazole and Miconazole (Monistat)?

topical irritation

hepatotoxicity (topical)

What is the MOA of polyenes?

Bind to ergosterol causing holes in the fungi membrane.

What drugs are polyenes?

Amphotericin B

Natamycin

What kind of drugs are Amphotericin B, Natamycin?

polyenes

Are polyenes fungicidal or fungistatic?

static, fungicidal at high concentrations

What is Amphotericin B used for?

life threatening infections

infections in immunocompromised patients

What are the side effects of Amphotericin B?

renal damage

anemia

What is Natamycin used for?

Treat fungal infections around the eye

What are the side effects of Natamycin?

Mild eye irritation, allergic reaction, change in vision, eye pain

What is the MOA of Terbinafine (Lamasil)?

inhibits squalene epoxidase --> decreses ergosterol synthesis

Is Terbinafine (Lamasil) fungistatic or tidal?

fungicidal

What is the MOA of Tavaborole (Kerydin)?

blocks fungal protein synthesis

What is Tavaborole (Kerydin) used for?

nail infection

What are side effects of Tavaborole (Kerydin)??

redness and inflammation of skin

What is the MOA of Griseofulvin (Gris-PEG)?

inhibits fungal cell division

What is Griseofulvin (Gris-PEG) used for?

systemically treats stubborn skin infection

What is a side effect of Griseofulvin (Gris-PEG)??

nephrotoxic

What is the MOA of Flucytosine (Cytoflu)?

blocks thymidine synthesis therefore inhibit DNA/RNA synthesis

What is the MOA of Caspofungin (Cancidas)?

targets/disrupts fungal cell wall

What stage of life do malarial parasites cause disease?

RBC stage (Merozoite)

What is the Merozoite stage?

parasites are released from liver and invade erythrocytes, causing illnesss

What drugs are used for prophylaxis of liver stage of malaria?

Primaquine

Malarone

What are the drugs used in prophylactic treatment of malaria?

Primaquine

Mefloquine

Chloroquine

Malarone

Doxycycline

What drugs are used for prophylaxis of the blood stage of malaria?

Mefloquine

Chloroquine

Doxycycline

What is the DOC for treatment and prophylaxis of malaria?

Chloroquine (Aralen)

What is a downside to using Chloroquine (Aralen)?

certain species have developed resistance

antacids interfere with absorption

What are the side effects of Chloroquine (Aralen)??

bulls eye retinopathy

GI problems

itching

What is the #2 treatment for malaria?

Mefloquine (Lariam)

What are the side effects of Mefloquine (Lariam)??

neurologic and psychiatric toxicities

What kind of drugs are Pryimethamine (Daraprim) and Proguanil?

Folate Synthesis Inhibitors in malaria

What is the MOA of Pryimethamine (Daraprim) and Proguanil??

inhibits dihydrofolate reductase in malarial parasites

What is the MOA of Malarone?

inhibits mitochondrial electron transport and dihydrofolate reductase in malarial paraistes

What's stage is Malarone effective against?

tissue + RBC stage

What malarial drug can be used during pregnancy?

Artemisinin

What is the MOA of Metronidazole (Flagyl)?

inhibits DNA synthesis/replication

What is unique about Metronidazole (Flagyl)?

it must enter protozoal/bacterial cell wall and be activated by the organisms enzyme to work

What are the side effects of Metronidazole (Flagyl)??

N/V/D

metallic taste

What are the treatments for toxoplasmosis?

Pryimethamine (Daraprim)

Sulfadiazine

Clindamycin

What are the categories of helminths?

1. Nematodes (round worm)

2. Platyhelminthes (flat worm)

-Trematodes (flukes)

-Cestodes (tapeworms)

Which drugs are used to treat nematode/roundworm infections?

Mebendazole (Vermox)

Thiabendazole (Mintezol)

Ivermectin

Pyrantel

What drug is used to treat a trematode/fluke infection?

Priaziquantel (Biltricide)

Which drugs are used to treat cestodes/tapeworm infections?

Priaziquantel (Biltricide)

Albendazole (Albenza)

What is MOA of mebendazole (Vermox), Thiabendazole (Mintezole), and Albendazole (Albenza)?

inhibits microtubules