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Antifungals and Antiparasitics - Coggle Diagram
Antifungals and Antiparasitics
Antifungal Drugs
Systemic Drugs
Amphotericin B
Mechanism
Disrupts fungal cell membrane
Binds selectively to ergosterol
Therapeutic uses
Used for most systemic fungal infections
Broad spectrum
Must be given by IV
Basically no resistance, ergostol is essential and they can't come up with something new
Adverse effects
Permanent nephrotoxicity due to it's lipid soluability
Caspofungin
(Is an Echinocandin)
Mechanism
Inhibits cell wall polysacharides
Therapeutics
Alternate therapy for serious systemic fungal infections
Must be given by IV
Flucytosine
Mechanism
Prodrug that is activated to 5-fluorouracil by a fungal specific enzyme
blocks DNA synthesis
Therapeutics
Synergistic with Amphotericin B
Adverse effects
Enterocolitis
High prolonged serum levels may cause bone marrow suppression cuz it's legit 5-fluorouracil
Fluconazole
Mechanism
Inhibits CYP450 mediated synthesis of ergosterol
Therapeutics
Extended to broad spectrum
Drug interactions
CYP450 inhibitor can increase plasma levels of other drugs by way of decreased metabolism of those drugs
Superficial Drugs
Nystatin
Same mechanism as Amphotericin B
Only useful for candidiasis
Not orally bioavailable
Miconazole
Inhibits synthesis of ergosterol
Terbinafime
Mechanism
inhibits ergosterol synthesis by a different mechanism than miconazole
Therapeutic uses
Tken orally for treatment of severe or extensive superficial infections (because it's lipophilic, so it really likes fatty things like skin - also really takes a long time to be completely excreted, so only small doeses are needed)
Can be used topically
Antiparasitic Drugs
Protozoal Drugs
Metronidazole
Selectively activated in anaerobic parasites and bacteria (C. diff)
Disulfiram affect - Inhibits metabolism of alcohol and other drugs
Chloroquine
(Quinoline drug)
Selectively concentrated in infected erythrocytes
Useful for prophylaxis and treatment of erythrocytic forms of parasite
Inhibits polymerization of heme into unreactive form (hemozoin) in the parasite
Atovaquone-Proguanil
Mechanism
Atovaquone inhibits mitochondrial electron transport in parasite
Proguanil inhibits purine and pyrimidine synthesis
Active against erythrocytic form of parasite, but not latent hepatic form
Used for treatment and prophylaxis
Doxycycline
Mechanism
Tetracycline drug
Inhibits bacterial-like mitochondrial protein synthesis in parasite
Only active against erythrocytic form of parasite
Useful for prophylaxis of malaria
Primaquine
Mechanism unclear
Only effective against hepatic form of parasite
Drug of choice for Plasmodia vivax or ovale - used in combination with chloroquine to effect a "radical cure"
Can cause hemolytic anemia in patients with G6D deficiency (like sulfonamides)
Worm infections
Nematodes (round worms)
Pyrantel
Cholinomimetic drug that causes paralysis
Toxic to humans, but not absorbed
Mebendazole
Inhibits microtubule function - selective for nematode tubulin
Prevents endocytosis of food
Platyhelminths (flat worms)
Praziquantel
Is absorbed
Causes massive calcium relsease in worms which paralyzes them and changes the surface of their bodies to allow antibodies to bind
Toxic to humans - near 100% first- pass metabolism :D (so it doesn't actually get into us)