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Antifungals
Antifungals
83
Pharmacology
Graduate
09/03/2012

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Cards

Term
Polyenes
Definition
Ampthotercin B
Nystatin
Term
Ampho B- MOA
Definition
Binds egosterol to disrupt fungal membrane
Term
Ampho-B role of deoxycholate
Definition
Must be compexed to deoxycholate for solubitliy
Term
Ampo- B- admin
Definition
IV
Intrathecally
bladder wash
Term
Ampo B - uses
Definition
Systemic fungal infections
Term
Ampo-B-AE
Definition
Attacks renal cells and RBC's
K, Mg, HCO3 wasting- hydrate and monitor
Infusion related- fever, chills, riggor, hypotenstion, myalgia, arthralgia, HA- premedicate with APAP, NSAIDS and others
Thrombophlebitis- prevent with heparin
Amenia- suppresses EPO
Term
Ampho-B- newer preps
Definition
Better formulations dec nephrotoxicity and allow larger doses BUT
don't do anything for rigor and infusion rxn
much more expensive
Term
Nystatin- MOA
Definition
binds to ergosterol and disrupts membrane
Term
Nystatin- Uses
Definition
oral, vaginal, skin candidiasis
Term
Nystatin- Admin
Definition
topical
swish and swallow
not orally absorbed
Term
Nystatin- AE
Definition
not many
Term
Pyrimidines?
Definition
Flucytosine
Term
Flucytosine- MOA
Definition
Flucytosine --> 5- Flurouridylic acid via cytosine deaminase--> inhibits translation
5- Flurodeoxyuridylic acid --> inhibits thymylate synthase --> inhibits DNA synthesis
Term
Flucytosine- Uses
Definition
used with Amphoteracin B for cryptococcal meningitis
Never use alone, resistance develops to quickly
Term
Flucytosinse- administration
Definition
Oral
Term
Flucytosine- distribution
Definition
well absorbed orally
Term
Flucytosine- 1/2 life
Definition
3-6 hrs
Term
Flucytosine- Excretion
Definition
Renal
Term
Flucytosine- AE
Definition
Bone marrow suppression
GI- N/V/D
Livertoxicity- reversible
Term
Echinocandins
Definition
Caspofugin
Micafugin
Andidafugin
Term
Echinocandins- MOA
Definition
inhibit beta 1,3 glucan synthesis- inhibit cell wall production
Term
Echinocandins- Admin
Definition
IV
Term
Echninocandins- uses
Definition
systemic Candida or Apergillus infections
Term
Echinocandins - drug interactions
Definition
Cyclosporine inc blood levels of Caspofugin
Term
Echinocandins- Protein binding
Definition
Highly protein bound
Term
Echinocandins- 1/2 life
Definition
1-2 days
Term
Echinocandins- CNS penetration
Definition
Minimal
Term
Echinocandins- AE
Definition
Histamine related rxns- warmth, swelling, rash
Headache
Hepatotoxicity
Term
Griseofluvin- MOA
Definition
Inhibits mitotic spindle formation
binds to human keratin which prevents invasion of fungus.
Infected cells slough off eventually non-infected keratinocytes at the basal layer eventually replace
Term
Griseofluvin- Admin
Definition
Oral- best with fatty foods
Term
Griseofluvin- uses
Definition
Fungal infections of: Hair, skin, and nails
Term
Griseofluvin- 1/2 life
Definition
1 day
Term
Griseofluvin- Excretion
Definition
Renal
Term
Griseofluvin- AE
Definition
Headache, Hepatotoxicity, Neuro/leuckopenia, basophilia, photosensitivity, GI, Rash
Term
Griseofluvin- Effect on enzymes
Definition
Inducer
Term
Griseofluvin- Drug interactions
Definition
Inc metabolism of Warfarin and Oral contraceptives
Term
Terbinafine- MOA
Definition
binds squalene epoxidase --> inhibits ergosterol synthesis
Term
Terbinafine- Admin
Definition
Oral
Term
Terbinafine- Uses
Definition
Mycoses of nails, drug accumulates in the nail beds
Term
Terbinafine- T 1/2
Definition
400 hrs b/c accumulates in hair, skin, and fat and slowly releases
Term
Terbinafine- Protein binding
Definition
High
Term
Terbinafine- AE
Definition
Well tolerated
Uncommon AE- GI, hepatatoxicity, stevents Johnson syndrome
Term
Terbinafine- drug interactions
Definition
Cimetidine- increases levels of Terbinafine
Term
Azoles- Types
Definition
Imidazoles, Triazoles
Term
Imidazoles
Definition
Ketoconazole, Clotrimazole, Miconazole, Econazole, Butoconazole, Oxiconazole
Term
Imidazoles- Admin
Definition
All topical except Ketoconazole which is for systemic
Term
Triazoles
Definition
Terconazole, Itraconazole, Fluconazole, Voriconazole, Poscanzole
Term
Triazoles- Admin
Definition
All systemic except for Terconazole which is topical
Term
Azoles- MOA
Definition
bind 14 alpha demethylase --> inhibit ergosterol synthesis
Term
Azoles- CYP450
Definition
inhibitors
Term
Azoles- Uses
Definition
Mostly, topical, but some systemic
Superficial infections- ringworm, candidiasis, tinea versicolor/ nigra, fungal keratitis
NOT FOR NAIL/HAIR- THOSE REQ SYSTEMIC
Term
Ketoconazole- Admin
Definition
Oral.
Require acidic environment for absorption. Drugs that inhibit acidity in the stomach dec absorption (Histamine2 and PPI)
Term
Ketoconazole- CYP450
Definition
Inhibitor
Inc levels of other drugs
Term
Ketoconazole- AE- hormonal effects
Definition
Hormonal due to CYP450 inhib- dec libido, gynecomastia, menstral irregularities. Blocks androgen, cortisol, aldosterone syntehsis and adronergic receptor antagonist
Term
Ketoconazole- AE- non hormonal
Definition
GI- dose dependent
rash
hepatotoxicity
Term
Itracanazole- Admin
Definition
Oral, IV
Term
Itraconazole- Uses
Definition
Candida, Aspergillus
Term
Itraconazole- absorption
Definition
GI absorption- empty stomach and acid
Term
Itraconazole- t1/2
Definition
30 hr
Term
Itraconazole- protein binding
Definition
protein binding parent and metabolites
Term
Iraconazole- AE
Definition
GI, Rash, LFTs. hypoTG, Hypokalemia
Term
Itraconazole- drug interactions
Definition
Fatal arrhythmia if given with cisapride or quinidine
Term
Intriconazole- Liver enzyme
Definition
Potent CYP3A4 inhibitor
Term
Fluconazole- Admin
Definition
Oral, IV
Term
Fluconazole- Use
Definition
Candida
Term
Fluconazole- absorption
Definition
not affected by food
Term
Fluconazole- excretion
Definition
Kidney
Term
Fluconazole- t1/2
Definition
30 hr
Term
Fluconazole- protein binding
Definition
not extensive
Term
Fluconazole- AE
Definition
Reversible alopecia
GI, Rash, LFTs
Term
Fluconazole- Contraindications
Definition
Pregnancy- results in fatal skeletal and cardiac muscle deformities
Term
Voricaonazole- Admin
Definition
Oral, IV
Term
Voriconazole- Uses
Definition
Candida, Aspergillus
Term
Voriconazole- t1/2
Definition
variable- dependson drug concentration, non linear kinetics
Term
Voriconazole- liver enzymes
Definition
Potent CYP3A4 inhibitor--> drug interactions
Term
Voriconazole- AE
Definition
Visual changes, Cardiovascular, CNS
Rash, LFTs
Term
Posconazole- admin
Definition
Oral- w/full meals
Term
Posconazole- Uses
Definition
Candida, Apergillus, Zygomycetes
Term
Posconazole- protein binding
Definition
high
Term
Posconazole- excretion
Definition
hepatic metabolism --> feces
Term
Posconazole- t1/2
Definition
30 h
Term
Posconazole- liver enzymes
Definition
CYP3A4- moderate inhibitor
Term
Posconazole- AE
Definition
Cardiovacular- HTN, hpokalemia
CNS- headache, dizziness
GI, LFTs
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