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Antifungals Flashcards

(54 cards)

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1
Q

3 most common systemic antifungals

A

Candidiasis
Cryptococcus
Aspergillosis

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2
Q

Drugs that alter cell membraine permeability

A

Polyenes
Azoles
Allylamines

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3
Q

Drugs that block nucleic acid synthesis

A

Flucytosine

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4
Q

Drugs that disrupt microtubule function

A

Griseofulvin

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5
Q

Drugs that disrupt the fungal cell wall

A

Echinocandins

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6
Q

Systemic drugs for subcutaneous and systemic mycoses

A

Ampotericin B
Flucytosine
Azoles
Echinocandins

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7
Q

Amphotericin B
MOA
RANGE of USE

A

Polyene antibiotic

  • binds ergosterol and forms pores IN CELL MEMBRANE
  • leakage of intracellular ions and macromolecules–>cell death
  • Broadest spectrum - yeast, endemic mycoses, pathogenic molds
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8
Q

Amphotericin B
PK
What procedure can cause seizures as a side effect?

A
  • highly insoluble:
  • IV only (SLOW IV INFUSION)
    poorly absorbed from the gut
    LOW CSF penetration
  • INTRATHECAL therapy WARNING can cause seizures!
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9
Q

Amphotericin B USES

A
  • Broad spectrum fungicidal
  • Often used as initial induction regimen to rapidly reduce fungal burden.
  • patients then continue therapy with an azole.
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10
Q

Amphotericin B prefere treatment for

A

deep fungal infections during pregnancy!!

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11
Q

Amphotericin B AE:

A

Infusion related toxicity

  • Nearly universal: Fever and chills, muscle spasms, vomiting, headache and hypotension.
  • Pre medication with Antiistamines, glucocorticoids, antipyetics or meperidine can be helpful!
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12
Q

Amphotericin B AE SLOWER TOXICITY?

A

Also binds cholesterol and forms mammalian cell membrane pores, leading to renal toxicity!!
- Renal impairment in all pts
• Azotemia occurs in most patients.
• GFR may be decreased.
• Renal toxicity commonly presents with renal tubular
acidosis with severe magnesium and potassium
wasting.
• Renal damage can be attenuated with sodium
loading: it is common practice to administer SALINE INFUSION with amphotericin B.

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13
Q

Amphotericin B AE SLOWER toxcicty 2?

A

• Hypochromic normocytic anemia, due to reduced
erythropoietin production.
• Renal function should be monitored frequently
during amphotericin B therapy.
• It is also advisable to monitor liver function, serum
electrolytes (particularly magnesium and
potassium), blood counts, and hemoglobin.

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14
Q

Amphotericin Lipid formulations use?

A

Package in lipid carriers to reduce interaction with nephron

  • Liposomal amphotericin B (L-AMB)
  • Amphotericin B Lipid complex (ABLC)
  • Amphotericin B colloidal dispersion ( ABCD)
  • Nephrotoxicity is less common and less severe with the lipid formulations
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15
Q

Flucytosine analogue of?

A

Cytosine

- pyramidine antimetabolite

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16
Q

Flucytosine MOA?

A

Taken up by fungal cells via cytosine permease
- disrupts RNA and DNA synthesis

Flucytosine –> 5-Fluorouracil (intracellular conversion) –> 5-fluorodeoxyuridine monophosphate –> inhibits THYMIDYLATE SYNTHASE thus blocking dTMP.

Flurorouridine triphosphate is also formed, which inhibits protein synthesis (5-FUTP)

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17
Q

Can mammalian cell convert Flucytosine to its active metabolites?

A combo with what drug shows synergism with Flucytosine?

A
  1. NO

2. Amphotericin B

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18
Q

Flucytosine spectrum

A

Fungistatic
Narrow spectrum
Not used as a single agent because of synergy with other agents, and to avoid resistance

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19
Q

Fucytosine USES

A

• Indicated only for serious infections caused by
susceptible strains of Candida and/or
Cryptococcus.
• Should be used in combination with
amphotericin B for the treatment of systemic
candidiasis and cryptococcosis in order to avoid
resistance.

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20
Q

Flucytosine AE:

A

Results from metabolism (intestinal flora) to 5-fluorouracil

- Bone marrow toxicity is the mot common.

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21
Q

AZOLES

A

Non toxic oral drugs
systemic therapy
IMIDAZOLES and TRIAZOLES

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22
Q

Imidazoles

Study These Flashcards
A

“KMC”
Ketoconazole–> (inhibits 17, 20 desmolase 1st step of steroid synthesis)
Miconazole (my cone)–> tinea infections
Clotrimazole (close trim)–> tinea infections

23
Q

Triazoles

Study These Flashcards
A 
"VIP Flu"
Itraconazole
Fluconazole
Voriconazole
Posaconazole (posaco)
24
Q

Azoles: MOA

Study These Flashcards
A

Inhibit CYP 450 enzyme 14 alpha demethylase from converting Lanosterol to ergosterol.
- increases permeability by disrupting membrane function.

25
CYP 450 enzyme specifity for azoles? | which ones have higher specificity?
High affinity for fungal CYP450 than human | Triazoles
26
Azoles AE
Relatively non toxic | minor GI upset
27
Ketoconazole MOA
- Inhibits mammalian CYP450 (CYP3A4) enzymes - decreases plasma testorsterone levels and causes gynecomastia - decreaed libido in men and loss of potency - menstrual irregularities in womne - high doses may inhibit adrenal steroid synthesis and decrease plasma cortisol concentrations
28
Ketoconazole is a CYP3A4 inhibitor what drugs can it potentiate toxcicities? when is it best absorbed?
Warfarin and cyclosporine At low gastric levels - antacids, H2 blockers or proton pump inhibitots interfere w/ absorption -poor CSF penetration
29
Ketoconazole is rarely used for? Why? still used for?
due to narrow spectrum and AE | used for cutaneous mycoses
30
Flucanazole PK?
GOOD CSF PENETRATION**** High oral bioavailability IV and Oral Moderate inhibitor of CYP3A4 Strong inhibitor of CYP2C9 --> increases plasma phenytoin, zidovudine and warfarin!
31
Fluconazole DOC
DOC in esophageal, oropharyngeal, vulvovaginal or urinary candidiasis DOC for Candidemia DOC for coccidoidomycosis DOC for consolidation and maintenance of crytpococcal meninigitis after induction w/ amphotericin B - alternative to amphotericin B for non-severe criptococcal meningitis DOC for initiial and secondary prophylaxis against cryptococcal meningitis!
32
Fluconazole USES: | is ineffective against?
Aspergillus or other filamentous fungi!
33
``` Itraconazole: Metabolizes and inhibits? causes what fatal problem when administered w/ what 2 drugsl? PK? Can penetrate? what reduces absorption? ```
``` CYP3A4 arryhthmias when adminisitered w/ cisapride and quinidine Poor bioavaibility Penetrates poorly in CSF Antacids, H2 blockers and PPIs ```
34
Itraconazole uses? | butterfly is dimorphic
• Preferred azole for mycoses due to the dimorphic fungi Blastomyces, Sporothrix and Histoplasma. • Effective against Aspergillus, but has been replaced by voriconazole for this indication. • Used for dermatophytoses and onychomycosis
35
Voriconazole DOC
DOC invasive ASPERGILLLOSIS | -spectrum similar to itraoncazole
36
Voriconazole AE
• Transient visual disturbances occur in up to 30% of patients. • metabolized by and inhibits CYP2C19, CYP2C9 and CYP3A4. • The significant number of drug interactions due to its metabolism through the various hepatic enzymes may limit its use.
37
Posaconazole USES | inhibits?
used against zygomycetes (MUCOR) | - inhibits CYP3A4
38
ECHINOCANDINS: CASPOFUNGIN | spectrum of activity
• Active against candida and aspergillus but not Cryptococcus neoformans. • Only available IV.
39
ECHINOCANDINS: CASPOFUNGIN MOA?
• Inhibit synthesis of β(1-3)-D-glucans in the fungal cell wall. • This results in disruption of the fungal cell wall and cell death
40
Systemic drugs for superficial mycoses
``` "FIT Keys onto Surface": • Griseofulvin • Terbinafine • Ketoconazole • Fluconazole • Itraconazole ```
41
Griseofulvin whats its only use? Absorbs best with? MOA
* Only use: treatment of severe dermatophytosis of skin, hair and nails * Absorption improved when given with fatty foods. MECHANISM OF ACTION • Disrupts mitotic spindle and inhibits mitosis.
42
Griseofulvin has been replaced w/? | Is an inducer of?
- newer antifungal drugs like itraconazole and terbinafine. • Induces P450 enzymes: increases metabolism of a number of drugs, including warfarin.
43
Terbinafine what type of antifungal is it? PK?
* Allylamine. | * Available in oral formulation
44
Terbiafine MOA
inhibits squalene epoxidase!! prevents synthesis of ergosterol. • It also causes accumulation of toxic levels of squalene in the fungal cell.
45
Terbinafine like griseofulvin accumulates in? | Its more effective in?
Keratin! | Much more effective in onychomycosis!!
46
what Azoles are commonly used in the treatment of dermatophytoses?
"KIt Fits the skin (derm)" Ketoconazole Itraconazole Fluconazole
47
Topical drugs for superficial mycoses?
* Nystatin * Amphotericin B * Clotrimazole * Miconazole * Ketoconazole * Terbinafine
48
NYSTATIN
• Polyene macrolide. • Structurally similar to amphotericin B. • Same mechanism of action. 68 NYSTATIN • Too toxic for IV administration. • Used only for candidiasis. • Supplied in preparations for cutaneous, vaginal, or oral administration. • Not absorbed from the GI tract, skin, or vagina. • As a result it has little significant toxicity
49
What is topical amphotericin B used for?
Cutaneous candidiasis
50
The two azoles most commonly used | topically?
CLOTRIMAZOLE MICONAZOLE -available over the counter
51
Terbanafine effective against?
* Available as topical creams. | * Effective for tinea cruris and tinea corporis.
52
WHAT FUNGUS DOES NOT RESPOND TO ANTIFUNGALS?
Pneumpcystis Jirovecii Penumonia (PCP)
53
DOC for PCP, also DOC for prevention of PCP n immunocompromised individuals?
Co-trimoxazole
54
PNEUMOCYSTIS JIROVECII PNEUMONIA | Therapies:
``` • Alternative therapies are: • Clindamycin + primaquine • Dapsone + trimethoprim • Atovaquone • Pentamidine • Patients with moderate-to-severe disease should also be given prednisone. ```

Pharmacology (27 decks)

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