Tinea and onchomycosis Flashcards

Tx of infections; MOA; Elim and dose mod in dysfxn; drugs producing hepatic or CV dysfxn; CYP interactions; teratogenic actions; immune suppression

1
Q

For widespread tinea infections, what can be used?

A

terbinafine; itraconazole; fluconazole;

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2
Q

localized tinea infection Tx

A

Azoles; terbinafine; naftifine; ciclopirox

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3
Q

Tx for onychomycosis

A

terbinafine; itraconazole; fluconazole

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4
Q

Tx for onchomysis topical

A

ciclopirox; amorolfine

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5
Q

What is the MOA for ciclopirox?

A

blocks fungal transmembrane transport and depletes essential substrates thus interfering with DNA/RNA synthesis (high [ ] cause intracellular leakage)

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6
Q

does Ciclopriox have effects on the fungal cell wall?

A

NO=> does not inhibit synthesis or cause lysis

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7
Q

What are significant toxicities with systemic Azole admin?

A

organ dysfxn; contraindication in concurrent disease or drug (CYP) interactions

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8
Q

What are the advantages and disadvantages of topical tx of azoles?

A

Tx occurs w/o significant systemic toxicity but not suitable for all infections

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9
Q

Ketoconazole use is limited for what reasons?

A

Hepatoxicity; adrenal insuffiency; DDI with CYP

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10
Q

What is a DDI of fluconazole, posaconazole and voriconazole?

A

CYP 3A4 interactions

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11
Q

Which drugs affect 2C9 and 2C19?

A

fluconazole; voriconazole

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12
Q

Posaconazole affects what type of activity?

A

P-gp activity

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13
Q

What are ADEs associated with fluco, posacon and voricon -azoles?

A

QT prolongation and dysrhythmias; hepatotoxicity; elevated LFTs

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14
Q

What are specific ADEs of voriconazole?

A

visual disturbances (optic neuritis: color change, photophobia); photosensitizes the skin in SCC and melanoma

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15
Q

Can flucon, posacon and voricon reach the CSF?

A

yes (dep on molec weight and P-gp affinity):

Flucon > voricon > itracon

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16
Q

What is significant for administration with posaconazole?

A

MUST be with full meal or acidic carbonated drink for adequate bioavailability

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17
Q

What is the effect of flucon, posacon and voricon in pregnancy?

A

contraindicated in pregnancy (Cat C)

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18
Q

What is the elimination of fluconazole?

19
Q

Dose adjustment with fluconazole?

A

yes with organ dysfxn

20
Q

Metabolism of flucon, posacon and voricon

A

extensie hepatic metab

21
Q

Terbinafine metabolism

A

hepatic (long half life)

22
Q

terbinafine elimination

23
Q

What ADEs are associated w/ oral terbinafine usage

A

lymphopenia and neutropenia

24
Q

What patients should avoid taking terbinafine?

A

immunosuppressed => cause opportunistic infections

25
admin of amorolfine
topical only with limited absorption
26
Terbinafine use in pregnancy
category B so risk is very little
27
MOA for naftifine?
anti-inflam via inhibition of inflam mediators such as PG, LTs and histamines => causes vasoconstriction
28
Naftifine static or cidal
locally cidal against G+ and G-
29
Metabolism of naftifine (topical)
hepatic
30
elimination of naftifine (topical)
renal
31
Contraindications for naftifine use
Hx of hypersensitivity to drug or co-formulated materials
32
What should naftifine not be used with?
topical azoles
33
Why cant topical azoles and naftifine be used together?
pharmacodynamic interference=> inhibits sterol production at earlier points so will diminish effectiveness
34
DDI with naftifine
no systemic DDI
35
Ciclopirox admin
topical only but limited absorption
36
Possible ADE with ciclopirox or amorolfine
hypersensitivity/allergy to drug or co-formulation materials; irritate if on skin abrasions
37
MOA of amorolfine
inhibits ergosterol synthesis
38
What are BBW with itraconazole?
heart failure; ventricular dysfunction; co-admin w/ drugs
39
MOA of itraconazole?
negative inotropic action (decrease force of heart contraction)
40
Metabolism of itraconazole
extensive hepatic
41
elimination of itraconazole
renal
42
Contraindications of itraconazole
concurrent drugs with CYP interaction; liver dysfxn/hepatic toxicity => monitor LFTs; post-partum
43
Pregnancy and itraconazole
Cat C but congenital deformities present
44
Post-partum and itraconazole
distributed in breast milk