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Anti-fungals Cheat Sheet (DRAFT) by

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This is a draft cheat sheet. It is a work in progress and is not finished yet.

Agansit cell wall Poly­ene­s/m­acr­ocyclic lactone

Nyasta­tin­/My­cos­tatin
Amphot­ericin B
No oral absorp­tio­b/t­oxi­city.
broadest spectrum of all antifu­ngals.
Uses: GIT candid­iasis. DOC for vaginal or cutaneous candid­iais.
Uses: DOC for deep fungal infection
 
SE/tox­icity: Phlebitis, nephro­tox­icity.
MOA: integrate within cell wall ergost­erols, causing leakage of small molecules.
Have higher affinity to fungal ergost­erols than mammalian sterols.

Against fungal nucleus

Griseo­fulvin
5-fluo­roc­ytosine (Flucy­tosine)
Natural. Oral intake since topically inactive.
Synthetic pyrimidine analogue.
MOA: stops mitosi­s/M­-phase
MOA: get incorp­orated into RNA, thus ruining protein synthesis.
SAR: Has 2 stereo­cen­ters( Cl and C-O-CH3)
Prodrug activated by fungal cytosine deaminase
-Cl can be replaced by fluorine only.
-Increased activity: if Methoxy becomes propoxy or butoxy invitro due to increased lipoph­ili­city. - Decreased activity: if methoxy becomes NH2.
Uses: agansit mycelial fungi only; fungis­tatic for growing dermat­ophytes (ringw­orm­,tinea)
Uses: systemic fungal and candida infect­ions.
 

Affecting ergosterol biosyn­thesis

Thiocarbamates
Allylamine deriv.
Azole deriv.
MOA: inhibit squalene epoxidase.
MOA: inhibit squalene epoxidase.
Imidazole "1st gen."
Imidazoles "2nd gen."
Triazoles
Tolnaftate
Terbin­afine, Lamisil
Clotri­mazole, Miconazole
Ketoconazole
1) Fluconazole
Uses: topical for dermat­oph­ytes, Tinea cure, for skin mycoses such as athletes foot.
Oral & topically active.
Broad-­spe­ctrum with no problems topically but system­ically may cause hepato­tox­icity.
Improved systemic bioavail. by improving water solubi­lity.
Use: for vaginal candid­iasis.
Not very effective for nail & scalp mycoses.
Uses: for ring worm and nail infections "­ony­cho­myc­ose­s"
Miconazole is used for oral candid­iasis.
The structure includes a dioxolane ring (ketal structure) respon­sible for the improved water solubi­lity.
only 2,4-di­fluro variants were active and non-toxic.
   
Ticoconazole
  
2) Itraconazole
   
x4 more potent than micona­zole.
  
Synthetic dioxolane triazole
   
AB also to some G+ve bacteria (like metron­ida­zole).
  
Uses: oropha­ryngeal or vaginal candid­iasis. Asperg­illosis candid­iasis.