antifungal drugs Flashcards

1
Q

name the triazoles

A

fluconazole
itra
posa
vori

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2
Q

which triazole has good penetration into CSF to treat fungal meningitis

A

fluconazole

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3
Q

why is fluconazole used to treat candiduria

A

largely excreted unchanged in the urine

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4
Q

itraconazole is active against a wide range of…

A

dermatophytes

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5
Q

which capsules need acid environment in stomach for optimal absorption

A

itraconazole

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6
Q

which drug has been associated with liver damage and should be avoided or used with caution in patients with liver disease? and which one would. you use instead

A

Itraconazole has been associated with liver damage and should be avoided or used with caution in patients with liver disease; fluconazole is less frequently associated with hepatotoxicity.

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7
Q

name the imidazoles

A

clotrimazole, econazole nitrate, ketoconazole, and tioconazole, miconazole

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8
Q

3 indications for imidazoles

A

local treatment of vaginal candidiasis and for dermatophyte infections. Miconazole can be used locally for oral infections; it is also effective in intestinal infections

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9
Q

name the polyene antifungals

A

amphotericin B and nystatin

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10
Q

are the polyenes (amph, nystatin) absorbed when given by mouth

A

no

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11
Q

which drug is highly protein bound and penetrates poorly into body fluids and tissues

A

amph B (polyene antifungal)

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12
Q

when conventional forms of amph B are CI because of toxicity (esp nephrotixicty) or when response is inadeqaute, what can you give instead

A

liposomal amph B

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13
Q

name the echinocandins

A

anidulafungin, caspofungin and micafungin.

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14
Q

activity of the echinocandins

A

They are only active against Aspergillus spp. and Candida spp.; however, anidulafungin and micafungin are not used for the treatment of aspergillosis

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15
Q

are echinocandins effective against CNS fungal infections

A

no

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16
Q

Flucytosine is used with amphotericin B in a synergistic combination. what side effect can occur, esp in HIV +ve pt

A

bone marrow depression
this limits its use
weekly blood counts needed with prolonged therapy

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17
Q

resistance to this drug can develop during therapy so you must do sensitivity testing before and during treatment

A

flucytosine

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18
Q

for this drug, when given parenterally, toxicity is common so close supervision necessary and close observation required for at least 30 minutes after test dose

A

amphotericin B

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19
Q

to avoid potential toxicity with amph B what must you do when given parenterally

A

close supervision necessary and close observation required for at least 30 minutes after test dose

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20
Q

why is test dose advisable for amph B

A

Anaphylaxis can occur with any intravenous amphotericin B product and a test dose is advisable before the first infusion in a new course; the patient should be carefully observed for at least 30 minutes after the test dose.

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21
Q

somebody has previously experienced infusion-related reactions but continued treatment with amph B is essential. what should you do

A

Manufacturer advises prophylactic antipyretics or hydrocortisone can be used in patients who have previously experienced infusion-related reactions (in whom continued treatment with amphotericin B is essential).

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22
Q

what to do if hepatic function abnormal with amph B

A

discontinue

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23
Q

monitoring for amph B

A

Hepatic and renal function tests, blood counts, and plasma electrolyte (including plasma-potassium and magnesium concentration) monitoring required.

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24
Q

amph B is …toxic

A

nephro
(reduced with liposomal)

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25
Q

what electrolyte disturbance can amph B cause

A

hypokalaemia

potentially increases risk of TDP when given with other drugs e.g. amiodarone, antipsychotics, theophylline, apomorphine, clomipramine, citalopram, fluconazole, flucytosine, hydroxychloroquine, hydroxyzine, quinine etc

26
Q

clotrimazole conception and contraception

A

Cream and pessaries may damage latex condoms and diaphragms.

27
Q

use of clotrimazole in pregnancy with vaginal use

A

With vaginal use:
Pregnant women need a longer duration of treatment, usually about 7 days, to clear the infection. Oral antifungal treatment should be avoided during pregnancy.

28
Q

fluconazole dose for vaginal candidiasis

A

150mg for one dose

29
Q

triazole (fluconazole, itraconazole etc) main interactions

A

hypokalaemia (increased TDP risk): theophylline, antifungals, diuretics, CCs,

QT interval prolongation: antipsychotics, amiodarone, apomorphine, citalopram, clomipramine, domperidone, quinine, hyroxyzine, methadone

hepatotoxicity

30
Q

interaction of fluconazole with this antiplatelet

A

Fluconazole is predicted to decrease the efficacy of Clopidogrel. Manufacturer advises avoid.

31
Q

fluconazole monitoring

A

Monitor liver function with high doses or extended courses—discontinue if signs or symptoms of hepatic disease (risk of hepatic necrosis).

32
Q

The CHMP has recommended that the marketing authorisation for oral ……. to treat fungal infections should be suspended. The CHMP concluded that the risk of hepatotoxicity associated with oral ….. is greater than the benefit in treating fungal infections

A

ketoconazole

33
Q

ketoconazole is only used orally for

A

Cushing’s syndrome

34
Q

the use of carbonated drinks, such as cola, improves ….. bioavailability.

A

ketoconazole

35
Q

miconazole fungal skin infections dose

A

Apply twice daily continuing for 10 days after lesions have healed.

36
Q

miconazole oral candidiasis dose

A

2.5 mL 4 times a day treatment should be continued for at least 7 days after lesions have healed or symptoms have cleared, to be administered after meals, retain near oral lesions before swallowing (dental prostheses and orthodontic appliances should be removed at night and brushed with gel).

37
Q

miconazole interactions

A

vit K antagonists - increases AC effect, avoid unless closely monitoring INR, monitor for signs of bleeding

carbamazepine, phenytoin, fosphenytoin - increased risk toxicity, monitor and adjust dose

avoid simvastatin, increased exposure

ciclosprin, tacrolimus, sildenafil, disopyramide - increases conc. monitor and adjust dose

38
Q

avoid this statin + miconazole

A

avoid simvastatin, increased exposure of simvastatin

39
Q

discontinue terbinafine if the following 2 occur

A

With oral use; discontinue treatment if liver toxicity develops (including jaundice, cholestasis and hepatitis).

With oral use; discontinue treatment in progressive skin rash (including Stevens-Johnson syndrome and toxic epidermal necrolysis).

40
Q

terbinafine age otc

A

over 16 years

41
Q

terbinafine increases exposure to…

A

TCAs (clomi, imi, lofep, nort etc) - moniotr for toxicity and adjust dose

SSRIs

atomoxetine - markedly increasex exposure, adjust dose

42
Q

terbinafine interaction with this antipsychotic

A

Terbinafine is predicted to increase the exposure to Clozapine. Manufacturer advises use with caution and adjust dose.

43
Q

terbinafine and tamoxifen

A

Terbinafine is predicted to decrease the efficacy of Tamoxifen. Manufacturer advises avoid.

44
Q

terbinafine and tramadol, codeine

A

Terbinafine is predicted to decrease the efficacy

45
Q

nystatin dose oral candidiasis

A

100 000 units 4 times a day usually for 7 days, and continued for 48 hours after lesions have resolved.

46
Q

ketoconazole interactions (imidazole)

A

DOACS - it increases their exposure, avoid apixaban
Statins - increases exposure - avoid or adjust dose and monitor for rhabdomyolosis
CCs - increases exposure, avoid or monitor adverse effects
Alfentanil, buprenorphine, buspirone - increases exposure, monitor and adjust dose

47
Q

ketoconazole and colcichine

A

Ketoconazole is predicted to increase the exposure to Colchicine. Manufacturer advises avoid potent CYP3A4 inhibitors or adjust Colchicine dose. (Reduce dose by 75% to one quarter of usual dose)

48
Q

ketoconazole and digoxin

A

Ketoconazole is predicted to markedly increase the concentration of Digoxin. Manufacturer advises monitor Digoxin concentration.

49
Q

ketoconazole and dronedarnoe

A

Ketoconazole very markedly increases the exposure to Dronedarone. Manufacturer advises avoid.

50
Q

ketoconazole and eplerenone

A

Ketoconazole is predicted to markedly increase the exposure to Eplerenone. Manufacturer advises avoid.

51
Q

ketoconazole and simvastatin

A

Ketoconazole is predicted to increase the exposure to Simvastatin. Manufacturer advises avoid.

52
Q

monitoring pt parameters for systemic terbinafine

A

Monitor hepatic function before treatment and then periodically after 4–6 weeks of treatment—discontinue if abnormalities in liver function tests.

53
Q

griseofulvin oral use - contraception and conception

A

Effective contraception required during and for at least 1 month after administration to women (important: effectiveness of oral contraceptives may be reduced, additional contraceptive precautions e.g. barrier method, required).

Men should avoid fathering a child during and for at least 6 months after administration

54
Q

If a pt is on a triazole e.g. fluconazole and they get a rash what should they do

A

If rash occurs, discontinue treatment (or monitor closely if infection invasive or systemic); severe cutaneous reactions are more likely in patients with AIDS.

55
Q

Which antifungal has been associated with heart failure

A

Itraconazole

At risk pt:
- higher doses
- longer courses
- cardiac disease
- chronic lung disease
- CCB treatment

Manufacturer advises avoid in patients with ventricular dysfunction, such as history of congestive heart failure, unless the infection is serious.

56
Q

itraconazole conception and contraception

A

Ensure effective contraception during treatment and until the next menstrual period following end of treatment.

57
Q

itraconazole monitoring

A

Monitor liver function if treatment continues for longer than one month, if receiving other hepatotoxic drugs, or if history of hepatotoxicity with other drugs.

58
Q

Which antifungal has the uncommon but important SE of phototoxicity

A

Phototoxicity occurs uncommonly with VORICONAZOLE

If phototoxicity occurs, consider treatment discontinuation; if treatment is continued, monitor for pre-malignant skin lesions and squamous cell carcinoma, and discontinue treatment if they occur.

59
Q

Which antifungal has this label
Protect your skin from sunlight—even on a bright but cloudy day. Do not use sunbeds

A

voriconazole

60
Q

Which antifungals may have risk of SJS and TEN

A

The azole antifungals (fluconazole, itraconazole, voriconazole, and posaconazole) and terbinafine are particularly associated with SJS and TEN.